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					                               ‫آزمایشگاه اشکال دارویی‬
                                                                                          ‫نام دانشجو:نرگس مالباشی‬

                                                                                   ‫شماره دانشجویی:861111149‬

                                                            ‫مو ضو ع ت ح ق ی ق : ت ه ی ه ی م ح لو ل ک ل ی ن د ا م ا ی س ین 1 %‬



                                                                         ‫ل و س ی و ن د ا ال س ی ن‬            ‫ن ا م ف ر آو ر د :‬



                                                                                                                ‫نام تجاری‬

                                                                                                                 ‫‪Cleocin‬‬



              ‫‪tUe eQeeU‬‬             ‫‪desU e i nheQ nhe eU se P eht ei esU‬‬
    ‫‪eAeUQsriteU isshis e‬‬                      ‫1‪e‬‬         ‫‪lU e ret siesA‬‬
                     ‫‪PP‬‬                     ‫‪rA 11 ,P ehe vs eve ,tsAveU‬‬
                                                              ‫‪seret sU‬‬
                  ‫‪˚01 .lAt‬‬          ‫‪rA 111sQ .h.q‬‬                ‫‪eesetAe‬‬

                                                              ‫موارد مصرف لوسیون داالسین :‬

              ‫آکنه ، جوش سر و صورت ، عفونت های پوستی و زخم های سطحی عفونی‬

                                                                                        ‫ویژگی فیزیکی اجزا:‬

‫کلیندامایسین فسفات پودری سفیدرنگ وکریستالی میباشدو پروپیلن گلیکول مایعی تاحدی‬
 ‫ویسکوزتراز آب وبه همین دلیل قوام و ماندگاری محلول برروی پوست را می افزاید.الکل نیز‬
 ‫مایع وفرارمی باشداحساس سردی بعدازاستعمال محلول به دلیل تبخیر الکل فرموالسیون‬
                                                                               ‫است.‬

                                                                                     ‫روش ومراحل تهیه:‬

  ‫یک گرم از پودر کلیندامایسین را وزن کرده و داخل ظرف مناسب می ریزیم ، ابتدا آن رادرآب‬
   ‫حل کرده(کلیندامایسین درآب محلول ولی درالکل نامحلول است) و بعد از حل شدن پودر‬
‫مقداری از الکل فرموالسیون را اضافه می نماییم. در مرحله بعد پروپیلن گلیکول را اضافه کرده‬
                                           ‫و در نهایت با الکل به حجم 110 ‪ lm‬می رسانیم.‬

  ‫پروپیلن گلیکول باعث افزایش قوام و گسترش آن بر روی پوست شده و مانع از خشک‬
                                   ‫شدن پوست در اثر تماس مکرر با الکل می شود.‬

                                ‫محاسبه حچم الکل مطلق مورد نیاز برای ساخت الکل ˚10 :‬

                                                   ‫00˚ => =56.05 ‪l‬‬                             ‫‪= 01lm‬‬                ‫10 ˚‬

                                                                                               ‫فرم بسته بندی:‬

          ‫محلول موضعی کلیندامایسین ـ 1% بطری پلی اتیلنی 10 میلی لیتری (داخل جعبه همراه با قطره چکان)‬
                       ‫آزمایشگاه اشکال دارویی‬



                                                    ‫:‪References‬‬


               ‫‪www.daroology.blogfa.com‬‬


                                                    ‫‪www.irannajo.com‬‬

                                                                  ‫به نام خدا‬


                                                  ‫تحقیق آزمایشگاه اشکال‬


                                                 ‫موضوع:پماد موپیروسین‬
                               ‫استاد ارجمند:جناب آقای دکتر شاه طالبی‬
                             ‫861111149‬             ‫گرد آورنده:فرهاد پوپل‬


                              ‫1.مواد تشکیل دهنده و ویژگیهای فارماکوپه ای آن:‬


                                                                  ‫موپیروسین:‬


‫پودر سفید یا تقریبا سفید،کم محلول در آب،بسیار محلول در استون،اتانول انیدر و در‬
                                              ‫متیلن کلراید.دارای پلی مورفیسم.‬
                          ‫آزمایشگاه اشکال دارویی‬
                                                                 ‫روغن کرچک:‬


           ‫عصاره دانه های ‪ ricinus communis‬تقریبا بیرنگ ،محلول در الکلهای‬
                                      ‫دهیدراته،کلروفرم،اتر و استیک اسید گالسیال‬


                                                                    ‫اولئیل الکل:‬


  ‫مایع روغنی،بیرنگ تا حدودی زرد،نامحلول در آب،محلول در اتر،ایزوپروپیل الکل و‬
                                                                 ‫پارافین مایع.‬


                                        ‫چربی سخت(‪:)softisan 378()Hard fat‬‬


‫توده سفید،تقریبا بدون بو و چرب در هنگام لمش.نقطه ذوب بین 27 تا 66.ماده ذوب شده‬
            ‫بیرنگ تا حدی زرد،که با حل کردن در آب داغ تشکیل یک امولسیون زرد‬
                     ‫میدهد.نامحلول در آب،کم محلول در الکل.آزادانه محلول در اتر.‬


                                                  ‫پروپیلن گالیکول مونواستئارات:‬


‫جامدی سفیدرنگ،‪،Wax-like‬نامحلول در آب است ولی با کمک سورفاکتانتها میتواند در‬
                                       ‫آب داغ پراکنده شود.محلول در حاللهای آلی.‬


                                           ‫7.ویژگیهای فارماکوپه ای ماده تولیدی:‬


                          ‫پماد نامحلول در آب،سفید رنگ تا حد کمی متمابل به زرد.‬
                        ‫آزمایشگاه اشکال دارویی‬


                                                             ‫1.موارد استفاده:‬


  ‫این ماده آنتی بیوتیک است و از آن به عنوان آنتی بیوتیک موضعی استفاده میشود.‬


                                                                ‫6.طرز تهیه:‬


               ‫این پماد 7% است.موپریسین در پایه ای حاوی مواد باال حل میشود.‬


                                                    ‫8.بسته بندی و نگه داری:‬


                           ‫در تیوبهای 81 گرمی و 61 گرمی بسته بندی میشوند.‬

                                    ‫در دمای 67 تا 87 درجه نگه داری می شود‬


                                                                     ‫4.منابع:‬

                                             ‫1.‪Martindale edition 35,CD‬‬

                                 ‫7.6041 ‪BP,edition 2009,page 1404 to‬‬

                                           ‫1.‪www.meddaily.nlm.nih.go‬‬
‫اقای پوپل بهتر نبست در همان فرمت که قرار است بصورت یک کتاب در اختیار همه‬
                                                     ‫قرار گیرد مرتب کنید‬
                                                                     ‫متشکرم‬
                                     ‫آزمایشگاه اشکال دارویی‬

 ‫محمد‬    ‫اقای احسان استادحسینی- 851111104 و‬
   ‫طاهری 511111134 (در خصوص ‪DMSO‬قرار نیست یک‬
   ‫فایل به صورت کپی ارسال گردد. لطفا سعی کنید در قالب‬
                ‫پیشنهاد شده اماده و ارسال گردد. متشکرم.‬
                                                    ‫ژل اسیکلوویر از ارام قادری‬
‫‪Components g/_100 g‬‬
‫00.5 ‪Acyclovir‬‬
‫00.1 ‪Lidocaine‬‬
‫00.2 001 ‪Eudragit E‬‬
‫00.4 )‪Hydroxypropylcellulose (Klucel MF‬‬
‫00.1 ‪Citric acid‬‬
‫00.42 ‪Purified water‬‬
‫00.36 °69 ‪Ethanol‬‬


                                                                                             ‫00.001 ‪Total‬‬


                                                                 ‫حمید محمدخاني861111107‬
                                                                                           ‫اجزاي فراورده:‬

                                                                                  ‫‪Foscarnet Sodium‬‬
                                                                           ‫‪Triamcinolone Acetonide‬‬
                                                                                    ‫‪Ethoxydiglycol‬‬
                                                                          ‫‪Pluronic™ F-127 20% Gel‬‬
                                                                                ‫‪Water, Purified USP‬‬

                                                                   ‫ویژگیهاي فارماكوپه اي مواد تشكیل دهنده:‬

            ‫فوسكارنت:پودر كریستالین با ظاهري سفید یا تقریبا سفید/حاللیت:محلول در آب و در عمل غیر محلول در‬
                                                           ‫72.7 ‪PKa‬اتانول06%/نقطه ذوب باالتر از 150‬

  ‫تریامسینولون:پودر كریستالین سفید خیلي ریز/فرمهاي پلي مرف دارد و نقطه ذوب بین 760 تا 150 درجه/حاللیت:1‬
   ‫گرم در حدود 1115 میلي لیتر آب. 18 سي سي پروپیلن گالیكول و در كمتر از 10 سي سي دي متیل سولفوكساید و‬
                                                                                ‫محلول در الكل و كلروفرم‬

            ‫‪ HIV‬پلی مراز، مهار ترانس کریپتاز معکوس ‪ DNA‬پلی مراز، مهار ‪RNA‬مکانیسم اثر: مهار‬
                                  ‫آزمایشگاه اشکال دارویی‬
                                                                           ‫رفرانسها:‬



‫‪remington‬‬

‫‪USP‬‬

‫داروها/5/‪www.iran-forum.ir/tags‬‬

‫..‪www.wipo.int/pctdb/en/wo.jsp?IA...wo...DISPLAY‬‬

‫‪compoundingtoday.com‬‬




                                       ‫به نام خدا‬
                                                    ‫تحقیق آزمایشگاه فارماسیوتیکس‬
                                                    ‫استاد:جناب آقای دکتر شاه طالبی‬


                                                       ‫861111149‬       ‫فرهاد پوپل‬


                             ‫کرم %1.0 ‪mometasone furoate cream‬‬


                                                                 ‫مواد تشکیل دهنده:‬


      ‫مومتاسن،هگزیلن گالیکول،فسفریک اسید،پروپیلن گالیکول،استئاریل الکل،تیتانیم دی‬
                                                       ‫اکساید،‪،white wax‬وازلین،آب‬


                                           ‫خصوصیات فارماکوپه ای مواد تشکیل دهنده:‬
                         ‫آزمایشگاه اشکال دارویی‬
                                                                   ‫مومتاسن:‬
      ‫پودر سفید،نامحلول در آب،کم محلول در الکل،محلول در استون و دی کلرو متان‬


                                                            ‫هگزیلن گالیکول:‬
‫مایع شفاف بی رنگ.در مواجهه با هوای مرطوب جاذب الرطوبه است.قابل حل شدن در‬
                                               ‫آب و بسیاری از حاللهای آلی.‬


                                                              ‫فسفریک اسید:‬
                 ‫دارای 89 تا 99 درصد ‪ w/w‬فسفریک اسید.محلول در آب و الکل.‬


                                                            ‫پروپیلن گالیکول:‬
‫ماده سفید،چرب با بوی چربی مانند.دمای ذوب کمتر از 86 درجه نیست.غیر محلول در‬
  ‫آب ولی نا حدی میتواند در آب داغ و کمک بعضی سورفاکتانتها پخش شود.محلول در‬
                                                               ‫حاللهای الی.‬


                                                              ‫استئاریل الکل:‬
                       ‫غلظت باید 68% باشد.نامحلول درآب،محلول در الکل و اتر‬


                                                          ‫تیتانیوم دی اکساید:‬
       ‫پودر سفید بدون بو.نامحلول در آب،هیدروکلوریک اسید،نیتریک اسید و در ‪2N‬‬
         ‫سولفوریک اسید.در هیدروفلوریک اسید و اسید سولفوریک داغ حل میشود.‬


                                                              ‫‪:White wax‬‬
                          ‫آزمایشگاه اشکال دارویی‬
‫جامد سفید متمایل به زرد.نامحلول در آب.کم محلول در الکل سرد.محلول در کلروفرم و‬
                                                                          ‫اتر.‬


                                                                         ‫وازلین:‬
  ‫ماده تقریبا بدون رنگ با توده مایل به زرد.نامحلول در آب.کم محلول در الکل.آزادانه‬
                          ‫محلول در کلروفرم،بنزن و کربن دی سولفید.محلول در اتر‬


                                                                             ‫آب:‬
                                                     ‫از آب مقطر باید درست شود.‬


                                                                       ‫طرز تهیه:‬


                   ‫1.6% مادهع موثره را در پایه ای متشکل از مواد باال حل میکنیم.‬


                                                                  ‫موارد مصرف:‬


                                  ‫به عنوان ضد التهاب و ضد خارش به کار میرود.‬


                                                                    ‫طرز مصرف:‬


 ‫یک بار در روز کرم را به قسمت مورد نظر می مالیم.در کودکان زیر 7 سال پیشنهاد‬
                         ‫نمی شود.وقتی بیماری بهبود یافت درمان باید متوقف شود.‬


                                                     ‫طرز بسته بندی و نگه داری:‬
                        ‫آزمایشگاه اشکال دارویی‬


            ‫بسته 86 گرمی این فرآورده حاوی این کرم و امونیم الکتات 71% است.‬

                            ‫در دمای بین 81 تا 61 درجه سانتیگراد نگه داری شود.‬


‫منابع:‬
‫‪.1Martindale 35th edition‬‬

‫‪2.USP 29th edition‬‬

‫‪.1www.dailymed.nlm.nih.gov‬‬

‫‪.6JSJ Pharmaceutical company‬‬




                                           ‫نام فرآورده: ‪Dexpanthenol‬‬
                                      ‫شکل دارویی مورد نظر:ژل 8 %‬
   ‫نام شیمیایی:-3,3-)‪(R)-2,4-Dihydroxy-N-(3-hydroxypropyl‬‬
                                  ‫‪dimethylbutyramide‬‬
   ‫مجموعه ویژگی های فارماکوپه ای:الکل آنالوگ از پانتوتنیک اسید /‬
 ‫ماده ای بی رنگ و یا زرد کمرنگ/جاذب الرطوبه/مایع ویسکوز و یا‬
  ‫پودر کریستالی/محلولیت در آب فوق العاده باالست/آزادانه محلول در‬
                                                             ‫الکل‬
                              ‫آزمایشگاه اشکال دارویی‬

      ‫موارد مصرف:دکسپانتنول و فرم راسمات پانتوتنول به صورت‬
   ‫موضعی در درمان اختالالت پوستی خفیف مختلف استفاده میشود.و‬
                    ‫دراغلب فراورده های ویتامینی نیز وجود دارد.‬
 ‫طرز تهیه:یک فرموالسیون از این ماده- ترکیبی از موارد زیر برای‬
‫درمان ترک پا است:اوسرین- النولین-روغن بادام شیرین-دکسپانتنول-‬
                                                    ‫اکسید روی‬
       ‫طرز بسته بندی:در ظروف سربسته و به دور از هوا نگه داری‬
           ‫میشود.هر تیوب حاوی 66 گرم دارو میباشد.(‪)pantogel‬‬
                        ‫تهیه کننده:مژگان سعیدی 171111149‬




‫‪Benzamycin‬‬
‫‪Erythromycin & benzoyl peroxide topical gel, USP‬‬
‫‪Acne therapy‬‬
                                                                                ‫مقدمه :‬

     ‫1- اریترومایسین : یک انتی بیوتیک ماکرولید باکتریواستاتیک است اما در دوز باال میتواند‬
                                                                     ‫باکتریوسیدال باشد.اگرچه‬
‫مکانیسم اریترومایسین در کاهش التهاب زخم ایجاد شده توسط ‪ vulgaris‬به طور کامل روشن نشده‬
                                ‫آزمایشگاه اشکال دارویی‬
    ‫اما احتماال به علت عمل آنتی بیوتیکی آن است که رشد ‪ propionibacterium acnes‬را در‬
                   ‫سطح پوست مهار میکند و غلظت اسید چرب آزاد را در سبوم کاهش میدهد.‬

    ‫اریترومایسین باعث مهار کردن سنتز پروتیین در ارگانیسم های حساس به وسیله متصل شدن به‬
 ‫‪ subunit 50s‬ریبوزومال میشود بنابراین باعث مهار جایگیری ‪ aminoacyl-tRNA‬و مهار سنتز‬
                                                                      ‫پلی پپتید می شود.‬



               ‫2 - بنزیل پروکساید : یک ماده ای است که نشان داده شده میتواند بر روی‬
   ‫‪ ( propionibacterium acnes‬باکتری بی هوازی که در غدد چربی و ‪comedon‬‬
                                                       ‫موجود است ) مؤثر باشد .‬

‫*‪ : Comedon‬یک توده بسته یا سرباز متشکل از کراتین و سبوم در فولیکول مو که حاوی‬
                  ‫پروپیونوباکتریوم آکنه و استافیلوکوک طالیی و پیتیرسپوروم اوال است.‬
        ‫اثر آنتی باکتلایر بنزیل پروکساید به علت ریلیز اکسیژن فعال است. .بنزیل پروکساید اثرات‬
           ‫کراتولیتیک و ‪( desquamative‬ریزش اجزا، اپی تلیال به صورت فلس یا ورقه ) و‬
                                    ‫‪( antiseborrheic‬ضد ترشح بیش از حد از سبوم ) دارد.‬

    ‫میشود.‬   ‫نشان داده شده بنزیل پروکساید در جایی که به بنزوییک اسید تبدیل به وسیله پوست جذب‬

                                                                   ‫:‬   ‫موارد مصرف‬
  ‫بنزومایسین در درمان آکنه وولگاریس که با ‪ comedon‬مشخص شده و پاپول های ملتهب چه با‬
                                            ‫کیست وندول چه بدون کیست به کار میرود.‬

                                            ‫بنزومایسین در درمان ‪ cyctic acne‬استفاده نمیشود.‬

                                           ‫اطالعات فارماسیوتیکال دارو :‬
                     ‫فرمول مولکولی :31‪C37H67NO‬‬                              ‫1-اریترومایسین :‬

                              ‫وزن مولکولی : 68.112‬

‫اریترومایسین یک پودر کریستالین سفید و تا حدی زرد رنگ است.فاقد بوست.به مقدار کم در آب حل‬
                                       ‫میشود ولی در اتر و الکل و کلروفرم محلول می باشد.‬



                          ‫فرمول مولکولی : 4‪C14H10O‬‬                        ‫7-بنزیل پروکساید :‬
                                ‫آزمایشگاه اشکال دارویی‬
                                ‫وزن مولکولی : 17.767‬

‫بنزیل پروکساید یک پودر گرانوله سفید رنگ است.دارای بو می باشد.در آب و الکل کم محلول ولی‬
                                                 ‫در استون و کلروفرم و اتر محلول است .‬

                                     ‫%3 ( ‪ ) 30 mg/g‬اریترومایسین‬             ‫ترکیبات :‬
                                      ‫8% (‪ ) 50 mg/g‬بنزیل پروکساید‬

                ‫اسانس لیمو‬                                            ‫الکل‬
             ‫متیل سالیسیالت‬                                       ‫کاربومر‬
                  ‫آب مقطر‬                                ‫‪Docusate sodium‬‬

                                                         ‫سدیم هیدروکساید‬

                                                                       ‫روش تهیه :‬
  ‫بنزومایسین در بسته های حاوی 66 ‪ g‬از ژل بنزیل پروکساید و 4.1‪ g‬از پودر اریترومایسین در‬
                                                          ‫ویال پالستیکی در دسترس است .‬

‫قبل از توزیع کردن باید به ویال اریترومایسن ضربه زد تا همه پودرها به صورت آزاد جریان یابند‬
                                                                                        ‫.‬

‫را به ویال اریترومایسین اضافه‬     ‫برای بنزومایسین 4.46 ‪ g‬باید 4 میلی لیتر از اتیل الکل 62%‬
                                     ‫کرد و فورا به هم زد تا پودر به صورت کامل حل شود.‬

                  ‫سپس این محلول را به ژل اضافه می کنیم و تا هموژنه شدن آن به هم می زنیم.‬




                                                                             ‫رفرانس :‬
                                ‫‪www.sanofi-aventis.ca/products/en/benzamycin pdf‬‬

                                                                  ‫‪www.wikipedia.com‬‬
                           ‫آزمایشگاه اشکال دارویی‬


                                    ‫به نام خدا‬
‫81/2/8911‬

                                            ‫فرموالسیون قطره گلیسرین فنیکه(41%)‬

‫‪1(phenol‬‬           ‫‪16 g‬‬

‫‪7(glycerin‬‬          ‫‪84 g‬‬
                                            ‫مورد مصرف:درمان التهاب و درد گوش‬
                                                                ‫خصوصیات مواد:‬
       ‫فنل به شکل کریستالهای سوزنی شکل به هم پیچیده یا جدا از هم یا توده کریستالی‬
                               ‫بیرنگ یا کمی صورتی و با بوی مخصوص وجود دارد.‬
‫گلیسرین مایعی است شفاف ، بدون بو ، غلیظ و چسبنده كه دارای طعم شیرینی می باشد.‬
                                                                     ‫مراحل تهیه:‬
  ‫ابتدا مقدار مورد نیاز از مواد را توزین نموده و به کمک بن ماری (گرما)،فنل را در‬
‫گلیسرین حل میکنیم. با توجه به آن که گلیسرین به صورت مایع است و توزین آن مشکل‬
  ‫می باشد برای سهولت کار بوسیله فرمول چگالی حجم مورد نیاز گلیسرین را محاسبه‬
                                                              ‫میکنیم )1/3=‪(p‬‬
 ‫برای تهیه قطره گوشی گلیسرین فنیکه فرمول مذکور را با هم حجم آب مخلوط میکنیم.‬
                                 ‫بسته بندی در ظروف 30 گرمی قرار داده می شود.‬
                                                                         ‫رفرانس:‬
                      ‫1) کتاب دارو شناسی نسخه های رایج، تالیف دکتر سیمین دشتی‬
‫?‪What is Alum‬‬


   ‫?‪What is alum‬‬
                                     ‫آزمایشگاه اشکال دارویی‬
    Been reading labels again, have you?


Alum is a salt that in chemistry is a combination of an alkali metal, such as sodium, potassium, or
ammonium and a trivalent metal, such as aluminum, iron, or chromium. The most common form,
potassium aluminum sulfate, or potash alum, is one form that has been used in food processing.
Another, sodium aluminum sulfate, is an ingredient in commercially produced baking powder. (Have
you never noticed the faint metallic taste in baking powder? It comes from the alum.)


The potassium-based alum has been used to produce crisp cucumber and watermelon-rind pickles
as well as maraschino cherries, where the aluminum ions strengthen the fruits' cell-wall pectins.


Alum is approved by the U.S. Food and Drug Administration as a food additive, but in large quantities
— well, an ounce or more — it is toxic to humans. As a result, efforts have been made and are being
made to wean us of our alum dependency. The U.S. Department of Agriculture says that if good
quality produce and modern canning methods are employed, there is no need to use alum to bolster
the crispness of our pickles and cherries. In any event, the department says, even if alum is used to
soak the pickles, it should not be used in the final pickling liquid.
                   ‫آزمایشگاه اشکال دارویی‬




ALUMINUM SULFATE

AND ALUMS

1. Introduction
                                    ‫آزمایشگاه اشکال دارویی‬
Aluminum sulfate octadecahydrate [7784-31-8], Al2(SO4)3Á18H2O, and its aque- ous solutions are
used primarily in the paper (qv) industry for sizing and as a flocculating agent in water (qv) and
wastewater treatment. This material is often called papermakers’ alum or alum. Because this salt is
precipitated from aqueous solution, aluminum sulfate hydrate [17927-65-0], Al2(SO4)3ÁnH2O, can
have variable composition and is sometimes referred to as cake alum or patent alum. The solid
commercial hydrate, generally written as the 18-hydrate, is typi- cally dehydrated to correspond to
from 17.0 – 17.5% Al2O3wheren ¼ 13À14 (1,2). This dehydrated form is called dry alum, ground or
lump. Aluminum sulfate solutions are typically 7.5–8.5% Al2O3and are known as liquid alum.

      Confusion arises in the nomenclature of alum because double salt com- pounds, M(I)Al(SO4)2,
where M is in theþ1 oxidation state, have also tradition- ally been called alums. In particular,
potassium aluminum sulfate [15007-61-1] KAl(SO4)2ÁnH2O, is referred to as ordinary alum or
potash alum.

Anhydrous aluminum sulfate [10043-01-3], Al2(SO4)3, is a specialty item

used in food applications.

2. Properties

Over 50 acidic, basic, and neutral aluminum sulfate hydrates have been reported. Only a few of
these are well characterized because the exact composi- tions depend on conditions of precipitation
from solution. Variables such as supersaturation, nucleation and crystal growth rates, occlusion,
nonequilibrium conditions, and hydrolysis can each play a role in the final composition. Commer- cial
dry alum is likely not a single crystalline hydrate, but rather it contains significant amounts of
amorphous material.

2.1. Hydrates.Aluminum sulfate hydrates, Al2(SO4)3ÁnH2O, wheren

ranges from 0 to 27 have been reported (3 – 6). Relative decreasing vapor pressure studies indicate
the presence of an octadecahydrate, hexadecahydrate, dodecahy- drate, dihydrate, and the
anhydrous salt, assuming that basic aluminum sulfates are not formed during the dehydration (3).

      Thermal analysis of the dehydration of Al2(SO4)3Á18H2O shows loss of 15 moles of water
between 408C and 2508C and 3 moles between 2508C and 4208C (7). Heating rate can affect the
product. Although rapid heating can fuse hydrated aluminum sulfate containing>35% water and puff
material contain- ing 25–35% water, these problems do not occur during slow heating in an agitated
bed. An aluminum sulfate hydrate can dissolve in its water of crystal- lization during heating.

2.2. Solubility.The aqueous solubility of a typical commercial alumi-

num sulfate, Al2(SO4)3ÁnH2O, wheren ¼ 14À18, is shown compared to the solu-

bility of the octadecahydrate in Table 1 (2,8). Differences in solubilities probably
                                   ‫آزمایشگاه اشکال دارویی‬




result from small amounts of impurities such as iron, and the slight excess of

Al2O3base present in technical grade commercial aluminum sulfate hydrate.

       Aqueous solutions of aluminum sulfate can hydrolyze at temperatures of about 1508C (9)
resulting in products having a formula such as 3Al2O3Á 4SO3Á9H2O, which is structurally related to
alunite [12588-67-9], K2Al6(SO4)4 (OH)12 (10).

2.3. Crystallization.Acidified aluminum sulfate solutions can be super-

cooled 108C or more below the saturation point. However, once nucleation begins, the
crystallization rate is rapid and the supersaturated solution sets up. The onset of nucleation in a
gently stirred supersaturated solution is marked by the appearance of silky, curling streamers of
microscopic nuclei resulting from orientation effects of hydraulic currents on the thin, platelike
crystals. Without agitation, nucleation in an acidified solution, in glass tubes, can yield extended
crystalline membranes of such thinness to exhibit colors resulting from optical interference.

2.4. Other Properties.The formula weight for the octadecahydrate is

666.45 and its specific gravity is 1.69 at 178C (11). Other physical properties such as percentage of
Al2O3in alum liquor vs specific gravity at 15.68C, pH as a function of alum concentration, heat
evolved on mixing Al2(SO4)3Á18H2O and water, viscosity of aqueous alum solutions as a function of
temperature, crystallization temperature of Al2(SO4)3Á18H2O as a function of the alum
concentration, and the boiling point of alum solutions as a function of the alum concentration have
been reported (2,11). Representative data are given in Tables 2 and 3.

3. Manufacture

In the United States, aluminum sulfate is usually produced by the reaction of bauxite or clay (qv)
with sulfuric acid (see SULFURIC ACID AND SULFUR TRIOXIDE). Bauxite is imported and more
expensive than local clay, generally kaolin, which is more often used. Clay is first roasted to remove
organics and break down the crystalline structure in order to make it more reactive. This is an energy
intensive process. The purity of the starting clay or bauxite ore, especially the iron and potassium
contents, are reflected in the assay of the final product. Thus the selection of the raw material is
governed by the overall economics of producing a satisfying product.

       The optimum conditions for roasting the clay and the optimum strength (30 –60%) of the
sulfuric acid used depend on the particular rawmaterial. Finely ground bauxite or roasted clay is
digested with sulfuric acid near the boiling

point of the solution (100 – 1208C). The clay or bauxite-to-acid ratio is adjusted to produce either
acidic or basic alum as desired and solids are removed by sedi- mentation. If necessary, the solution
                                   ‫آزمایشگاه اشکال دارویی‬
can be treated to remove iron. However, few, if any, of the many methods claimed to be useful for
iron removal have been used industrially (12). Instead, most alum producers prefer to use raw
materials that are naturally low in iron and potassium.

      The clear supernatant solution is decanted and sold in liquid form or con- centrated to
approximately 61.58 Be´ and then allowed to solidify to form blocks that are crushed, ground, and
graded. A typical analysis for the dry product is: total Al2O3, 17.0–17.5%; Fe2O3<0:5%; water of
composition 42–43%; insoluble

<1:0%. Liquid alum contains 7.5–8.5% Al2O3. At concentrations>8:5% Al2O3,

crystallization of the solution may occur.

       The iron-free grade of aluminum sulfate hydrate contains less than 0.005% iron as Fe2O3. It is
manufactured from pure alumina trihydrate [12252-70-9] Al2O3Á3H2O, rather than from bauxite or
clay. Although a technical or commer- cial grade alumcan be treated to remove iron, such processes
are not sufficiently economical to meet the requirements for the iron-free grade (12). The presence
of iron can cause discoloration or staining of the product employing the aluminum sulfate.

A process to produce aluminum sulfate fromcoal ash has been reported (13).

4. Economic Aspects

In the United States 79 companies produced aluminum sulfate in 1997 (14). The

total U.S. production was 1161Â 103/t on a 17% Al2O3 basis.

The United States exported 7690 t of aluminum sulfate and imported

23,500 t in 2000 (15).

       Aluminum sulfate hydrate is marketed as material commercial or technical grade containing a
maximum of 0.5% Fe2O3. The commercial grade is available as a dry ground product containing from
17.0 to 17.5% Al2O3, 57–59% Al2(SO4)3, and as an aqueous solution containing from 7.5 to 8.5%
Al2O3. The price of alu- minum sulfate from $152 to 292 /t in October 2002 (16).

5. Health and Safety Factors

Aluminum sulfate is orderless. When it is heated or burned, irrirant sulfur oxide

fumes are produced.

The ACGIH threshold limit (TWA) is 2.0 mg/m3OSHA PEL is 2.0 mg/m3(17).

6. Uses

The pulp and paper industry and potable and wastewater treatment industry are the principal
markets for aluminum sulfate. Over half of the U.S. aluminum sul- fate produced is employed by the
pulp and paper industry. About 37% is used to
                                   ‫آزمایشگاه اشکال دارویی‬
precipitate and fix rosin size on paper fibers, set dyes, and control slurry pH. Another 16% is utilized
to clarify process waters. The alum sold for these pur- poses is usually liquid alum. It is frequently
acidic as a result of a slight excess of H2SO4. Aluminum sulfate consumption by the pulp and paper
industry is projected to remain constant or decline slightly in the near term because of more
efficient use of the alum and an increased use of alkaline sizing processes (18).

      Aluminum sulfate is used as a flocculating agent or coagulant in water and wastewater
treatment (see FLOCCULATING AGENTS). This use, excluding the 16% employed in process water
treatment by the pulp and paper industry, accounts for 44% of U.S. consumption. Alum sold to
municipalities in the United States is required by the American Water Works Association (AWWA) to
be basic as a result of a slight excess of Al2O3. When alum is added to water, positively charged
hydrated or hydroxylated aluminum ions neutralize and adsorb nega- tively charged colloidal and
suspended matter in the water causing the material to floc and settle out (19). Increased use of
organic polymeric coagulants and com- binations of organic and inorganic coagulants has decreased
somewhat the alu- minum sulfate market. Polyaluminumchloride, basic aluminum sulfate (20 –22),
and a more recent basic aluminum chlorosulfate (23,24) are all effective coa- gulants. The near term
market for aluminum sulfate in water treatment is projected to remain flat.

Other uses for aluminum sulfate include tanning (see LEATHER), and as a pH

stabilizer, cement (qv) hardening accelerator, mordant in dyeing (see DYES AND

DYE INTERMEDIATES), anticaking agent, fire extinguisher, and as a flame retardant

additive, a use which dates to the early Egyptians (see FLAME RETARDANTS). Wood (qv) and
cellulose (qv) treatment, catalysis (qv), and pharmaceutical and cos- metic applications are known
(see COSMETICSAND PHARMACEUTICALS). Japanese literature suggests uses as an absorbent for
odor and gases (25). Alum is effective in reducing the phosphate content of sewage and wastewater
and in combating the eutrophication of lakes (26,27). Russian literature cites uses in drilling muds
(28).

      Aluminum sulfate is a starting material in the manufacture of many other aluminum
compounds. Aluminum sulfate from clay could potentially provide local sourcing of raw materials for
aluminum production. Processes have been studied (29) and the relative economics of using clay
versus bauxite have been reviewed (30). It is, however, difficult to remove impurities economically
by pre- cipitation, and purification of aluminum sulfate by crystallization is not practiced
commercially because the resulting crystals are soft, microscopic, and difficult to wash effectively on
a production scale (31–33).

Patents have been issued for the production of animal litter from ammo-

nium sulfate (34,35).

7. Other Alums

The word alum is derived from the Latinalumen, which was applied to several astringent substances,
most of which contained aluminum sulfate (25). Unfortu- nately, the term alum is now used for
several different materials. Papermakers lum or simply alum refers to commercial aluminum sulfate.
                                   ‫آزمایشگاه اشکال دارویی‬
Common alum or ordinary alum usually refers to potash alum which can be written in the form
K2SO4ÁAl2(SO4)3Á24H2O, or it can refer to ammonium alum, ammonium alumi- num sulfate. The
term is also applied to a whole series of crystallized double sul- fates [M(I)M0(III)(SO4)2Á12H2O]
having the same crystal structure as the common alums, in which sodium and other univalent metals
may replace the potassium or ammonium, and other metals may replace the aluminum. Even the
sulfate radical may be replaced, by selenate, for example. Some examples of alums are cesium alum
[7784-17-0], CsAl(SO4)2Á12H2O; iron alum [13463-29-1], KFe(SO4)2Á12H2O; chrome alum
[7788-99-0], KCr(SO4)2Á12H2O; and chromoselenic alum [17855-06-0], KCr(SeO4)2Á12H2O.

       Pseudoalums are a series of double sulfates, such as iron(II) aluminum sul- fate [22429-82-9],
FeSO4ÁAl2(SO4)3Á24H2O, containing a bivalent metal ion in place of the univalent element of
ordinary alums. These pseudoalums have dif- ferent crystal structures from those of the ordinary
alums.

      In industrial practice it is generally the aluminumcontent of alums that is important. Because
aluminum sulfate is widely available, other alums are more specialty items and are no longer
produced in quantities comparable to those of aluminum sulfate (19).

7.1. Ammonium Aluminum Sulfate.Ammonium aluminum sulfate

[7784-26-1], NH4Al(SO4)2Á12H2O, is also known as ammonium alum or ammonia alum. It is a
colorless crystal having a strong, astringent taste; formula weight 453.33; mp, 94.58C; sp gr 1.64;
and solubility of 12.0 g per 100 mL H2O at 208C (8). It is soluble in dilute acid and insoluble in
alcohol. The material dehydrates at about 2508C (36) to porous, dry ammonium alum [7784-25-0],
NH4Al(SO4)2, formula weight 237.14, which is also called dried or burnt alum. Decomposition of the
anhydrous material begins at 2808C andg-Al2O3is formed between 1000 and 12508C.

      Ammonium alum is manufactured by crystallization from a mixture of ammonium sulfate and
aluminum sulfate or by the treatment of aluminum sul- fate and sulfuric acid with ammonia gas.
Ammonium alum is used in medicine, as a mordant in dyeing, dressing furs in tanning, paper sizing,
and water puri- fication. It can be used in baking powders (see BAKERY PROCESSES AND LEAVENING

AGENTS). It has also been used as the starting material to produce finely powdered

aluminum oxide for the manufacture of synthetic corundum gems (see GEMS,

SYNTHETIC) (19).

7.2. Potassium Aluminum Sulfate.Potassium aluminum sulfate

[7784-24-9]. KAl(SO4)2Á12H2O, is a white, astringent crystal known as potassium alum, ordinary
alum, or potash alum. Its formula weight is 474.39; mp 92.58C; sp gr 1.75; and solubility 11.4 g per
100 mL H2O at 208C (8). It is soluble in dilute acid and insoluble in alcohol. It dehydrates at about
2008C to porous desiccated potassium alum[10043-67-1], KAl(SO4)2, a dried or burnt alum, which
has a for- mula weight of 258.20.

       Potassium alum is manufactured by treating bauxite with sulfuric acid and then potassium
sulfate. Alternatively, aluminum sulfate is reacted with potas- sium sulfate, or the mineral alum
                                      ‫آزمایشگاه اشکال دارویی‬
stone, alunite, can be calcined and leached with sulfuric acid. Alunite is a basic potassium aluminum
sulfate [1302-91-6], K2Al6(SO4)4(OH)12, sp gr 2.58–2.75.




       Potassium alum, which also occurs naturally as the mineral kalinite [7784- 24-9],
KAl(SO4)2Á12H2O, sp gr 1.75, is used in tanning skins, as a mordant in dye- ing, and in the
pharmaceutical and cosmetic industries (see PHARMACEUTICALS; COSMETICS). It is used as a styptic
pencil and as a hardening agent and set accel- erator for cement and plaster. The ACGIH threshold
limit value TWA is 2 mgAl/ m3(12).

7.3. Sodium Aluminum Sulfate.Sodium aluminum sulfate [7784-28-3],

NaAl(SO4)2Á12H2O, known as sodium alum, is a colorless crystal having an astringent taste; mp
618C; and sp gr 1.675. It is the most water soluble alum: 75 g per 100 mL H2O at 208C (8). It is
soluble in dilute acid and insoluble in alcohol.

       Sodium alum occurs naturally as the mineral mendozite. Commercially, it is produced by the
addition of a sodium sulfate solution to aluminum sulfate. Small amounts of potassium sulfate,
sodium silicate, and soda ash can be added to improve product handling and performance. After
adjustment of the ratio of aluminum sulfate to sodium sulfate, water is evaporated to give a hard
cake in the cooling pans. This cake is further heated in roasters and ground to a fineness of 99%
through a 100-mesh ($150 m) sieve.

In the United States, sodium aluminum sulfate is used as a leavening agent

in baking applications.

BIBLIOGRAPHY

‘‘Aluminum Sulfate and Alums,’’ under ‘‘Aluminum Compounds,’’ inECT 1st ed., Vol. 1, pp. 653–656,
by W. F. Phillips, American Cyanamid Company; inECT 2nd ed., Vol. 2, pp. 58–65, by W. C. Saeman,
Olin Matheson Chemical Corporation; inECT 3rd ed., Vol. 2, pp. 244–251, by K. V. Darragh, Stauffer
Chemical Company; inECT 4th ed., Vol. 2, pp. 330–338, by K. V. Darragh and C. A. Ertell, Rhoˆne-
Poulenc, Inc.; ‘‘Aluminum Sulfate and Alums’’ inECT (online), posting date: December 4, 2000, by K.
V. Darragh and C. A. Ertell, Rhoˆne-Poulenc, Inc.




                       158188558 - ‫علی رستگاری‬                        ‫آمفوتریسین ب‬


‫خصوصیات فارماکوپه ای‬

‫آمفوتریسرین :یک پودر زرد رنگ تا نارنجی ، بدون بو و یا نسبتا بدون بو است. در هر میلی گرم نباید مقدار‬
C47H73NO17 ‫از 158 میکرو گرم کم تر باشد. در داخل آب،الکل دهیدراته ،اتر،بنزن و تولوئن نامحلول است و در دی متیل‬
‫فرمامید،دی متیل سولفوکسید و پروپیلن گالیکول محلول است و خیلی کم در متیل الکل حل می شود. باید در دمایی که از 7 درجه‬
                                      ‫آزمایشگاه اشکال دارویی‬
‫سانتی گراد بیش تر است نگاه داری نشود و در بسته های درب در و محافظ در برابر نور نگهداری شود. آمفوتریسین ب در پی اچ‬
.)1(‫اسیدی غیر فعال است‬

‫کربوکسی متیل سلولز: یک پودر سفید رنگ روان با دانسیته 65.1 و بدون بو ؛محلول د رآب است و به راحتی در آب سرد حل‬
.)1( ‫می شود‬



:‫مواد تشکیل دهنده فرآورده موضعی‬

:‫شیاف آمفوتریسین ب به صورت زیر تهیه می شود‬

______________________________________
        Ingredient Amount (% w/w)
______________________________________
Amphotericin B                                                 1%

Hydrocolloid (sodium carboxy- methyl cellulose) 3%

Low melting suppository base                                  96 %

(Witepsol W35 (31.2%))

(Witepsol H15 (68.8%))

*Witepsol suppository base is a mixture of mono, di, and triglycerides which are glyceryl
esters of mixtures of vegetable fatty acids derived from palm seed oils such as coconut oil
and palm kernel oil, and includes C 12 to C 18 ac ids in which lauric acid predominates.
Witepsol W35 has a melting point range of 33.5 to 35.5° C., a solidification point range of 27
to 32° C. and a hydroxy value of 40 to 50. Witepsol H15 has a melting point range of 33.5 to
35.5° C., a solidification point range of 32.5 to 34.5° C. and a hydroxy value of 15. % of each
Witepsol component is based on the total amount of suppository base.

A mixture of about 30 g Witepsol W35 and about 66 g of Witepsol H15 were heated to
melting (about 35°) and retained at about 45° until ready to add the other components. The
temperature of the mass was reduced to 40° by cooling in air with stirring and the resulting
liquid was stirred while 2 g of hydrocolloid (sodium carboxymethylcellulose) was added.
Stirring was continued for 10 minutes until a relatively uniform suspension was formed. 2 g
of nystatin was added while stirring was continued for 10 minutes until a relatively uniform
suspension was obtained. Throughout the above procedure, the temperature of the various
mixes was maintained above about 36°-37° by the thermal energy produced during stirring.

Stirring was then discontinued and the resulting liquid suspension was poured into suitable
molds to form 0.03 g supporitories of the invention for animal studies described below and 1
g suppositories for human use (2).

‫ویژگی فارماکوپه ای ماده تولیدی‬

‫این فرآورده یک ترکیب ضد قارچ و باکتری است و این شیاف در دمای بدن ذوب شده و ترکیب ضدقارچ و هیدروکلوئید را آزاد‬
.‫می کند که به مخاط واژن چسبیده و یک آزادسازی یکنواخت فرآورده ضد قارچ در محل عفونت انجام می گیرد‬
                                        ‫آزمایشگاه اشکال دارویی‬
.‫آمفوتریسین ب با اتصال به ترکیبات استرول در غشا سلولی در نفوذپدیری غشا تغییر ایجاد کرده و منجر به مرگ سلول می شود‬
‫با وجود آنکه آمفوتریسین ب تمایل بسیار زیادی به ارگسترول غشا سلولی قارچ داردولی به کلسترول سلول های پستانداران نیز‬
.)5‫متصل شده و به همین دلیل سمیت سلولی خواهد داشت(0و‬



:‫موارد مصرف‬

.)6(‫در درمان عفونت کاندیدیایی واژن مقاوم به درمان استفاده می شود‬



:‫طرز بسته بندی‬

.)0(‫در ظروف در بسته و مقاوم به نفوذ نور باید بسته بندی شودو در جای خنک نگهداری شود‬



:‫منابع‬

         (1) MARTINDALE: THE COMP LETE DRUG REFERENCE, 36 ED. 523-525
(2) Long-lasting adhesive antifungal suppositories. United States Patent 4542020; The web site:
http://www.freepatentsonline.com

(3) The web site: http://www.chemicalland21.com

(4) Phillips AJ..Treatment of non-albicans Candida vaginitis with amphotericin B vaginal
suppositories.Am J Obstet Gynecol .2005 Jun;192(6):2009-12; discussion 2012-3

(5) The web site: http://dailymed.nlm.nih.gov

(6) USP Pharmacopeia (USP 30-NF25)




How Supplied/Storage and Handling
Voltaren® Gel is available in tubes containing 100 g of the topical gel in each tube. Physician
samples are packaged in 20 g tubes. Each tube contains diclofenac sodium in a gel base (10
mg of diclofenac sodium per gram of gel or 1%).
20 gram tube (physician’s sample) NDC 63481-684-83
100 gram tube NDC 63481-684-47
                               ‫آزمایشگاه اشکال دارویی‬
3 Carton (3 Tubes containing 100 gram each) NDC 63481-684-03
5 Carton (5 Tubes containing 100 gram each) NDC 63481-684-05
Storage
Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F) [See USP Controlled Room
Temperature]
Keep from freezing.


Read more: http://www.drugs.com/pro/voltaren-gel.html#ixzz11WDxotZ8



Preparation:
EXAMPLE 1

Diclofenac sodium (1 g) was dissolved in 95% ethanol (30 g) with stirring. Propylene glycol
(10 g), a 4% aqueous solution (25 g) of a carboxyvinyl polymer (Carbopol 940), and purified
water (20 g), were separately and uniformly mixed, and triethanolamine (1.5 g) was thereafter
added to the mixture with continued stirring. The previously prepared alcoholic solution of
diclofenac sodium was then added to the gel base, and the volume of the mixture was
adjusted to 100 g by the further addition of purified water. After stirring well, a gel
preparation having a viscosity of 20,000 centipoises and a pH of 7.15 was obtained.

EXAMPLE 2

A further gel preparation was prepared in the same manner as described in Example 1,
containing the following ingredients:

______________________________________
        COMPONENT AMOUNT
______________________________________


Diclofenac sodium 2.0 g

95% ethanol 30.0 g

Propylene glycol 10.0 g

Carbopol 940 (4% aqueous

30.0 g

solution)

Triethanolamine 2.0 g
                                    ‫آزمایشگاه اشکال دارویی‬

Water 26.0 g

Total 100.0 g

______________________________________

CONTROL A

Diclofenac sodium (1.0 g) and peppermint oil (3.0 g) were dissolved in 95% ethanol (40 g)
by stirring. Separately, a 3% solution (20 g) of Carbopol 940 in propylene glycol, and a 4%
aqueous solution (25 g) of Carbopol 940, citric acid (0.3 g) and purified water (8.0 g) were
uniformly mixed by stirring; triethanolamine (0.05 g) was added thereto with continued
stirring to produce the desired gel base. The alcoholic solution of diclofenac sodium and
peppermint oil was added to the gel base, and the mixture was adjusted to 100 g by the
further addition of purified water. After stirring, a gel preparation having a viscosity of
22,000 centipoises and a pH of 5.2 was obtained.


                                                   ‫استاد محترم:آقای دکتر شاه طالبی‬
                241011168                             ‫نام:سید مصطفی کاظمی علوی‬
     Carac® (fluorouracil cream) Cream, 0.5%
   FLUOROURACIL FOR TOPICAL DERMATOLOGIC USE. CHEMICALLY, FLUOROURACIL IS 5-FLUORO-
   2,4(1H, 3H)-PYRIMIDINEDIONE. THE MOLECULAR FORMULA IS C4H3FN2O2. FLUOROURACIL HAS A
                                MOLECULAR WEIGHT OF 130.08.

                                         PHARMACOLOGY:

Fluracil is an antineoplastic anti-metabolite. Anti-metabolites masquerade as purine or pyrimidine -
which become the building blocks of DNA. They prevent these substances becoming incorporated in
to DNA during the "S" phase (of the cell cycle), stopping normal development and division. Fluracil
blocks an enzyme which converts the cytosine nucleotide into the deoxy derivative. In addition, DNA
synthesis is further inhibited because Fluracil blocks the incorporation of the thymidine nucleotide
into the DNA strand

 (5-FU or f5U) (sold under the brand names Adrucil, Carac, Efudex and Fluoroplex) is a drug that is a
pyrimidine analog which is used in the treatment of cancer. It works through noncompetitive
inhibition of thymidylate synthase. Due to its noncompetitive nature and effects on thymidine
synthesis, 5-FU is frequently referred to as the "suicide inactivator". It belongs to the family of drugs
called antimetabolites. It is typically administered with leucovorin.



uses
                                    ‫آزمایشگاه اشکال دارویی‬
The chemotherapy agent 5-FU (fluorouracil), which has been in use against cancer for about 40
years, acts in several ways, but principally as a thymidylate synthase inhibitor. Interrupting the
action of this enzyme blocks synthesis of the pyrimidine thymidine, which is a nucleotide required
for DNA replication. Thymidylate synthase methylates deoxyuridine monophosphate (dUMP) into
thymidine monophosphate (dTMP).

Like many anti-cancer drugs, 5-FU's effects are felt system wide but fall most heavily upon rapidly
dividing cells that make heavy use of their nucleotide synthesis machinery, such as cancer cells
(other parts of the body with rapidly dividing cells include the cells lining the digestive tract).

Some of its principal uses are in colorectal cancer, and pancreatic cancer, in which it has been the
established form of chemotherapy for decades (platinum-containing drugs approved for human use
in the US since 1978 are also very well established). It is also sometimes used in the treatment of
inflammatory breast cancer, an especially aggressive form of breast cancer.

5-FU is also used in ophthalmic surgery, specifically to augment trabeculectomy (an operation
performed to lower the intraocular pressure in patients with glaucoma) in patients deemed to be at
high risk for failure. 5-FU acts as an anti-scarring agent in this regard, since excessive scarring at the
trabeculectomy site is the main cause for failure of the surgery.

Fluorouracil can be used topically (as a cream) for treating actinic (solar) keratoses and some types
of basal cell carcinomas of the skin. It is often referred to by its trade names Efudex, Carac or
Fluoroplex.

Due to Fluorouracil's toxicity and the fact that it can be manufactured using the same reaction as
uracil, its precursor, 5-Fluoroorotic Acid, is commonly used in laboratories to screen against
organisms capable of synthesizing uracil.

It is a key component in Tegafur-uracil.


                              Synthesis




5-FU was designed, synthesized and patented by Charles Heidelberger in 1957. [1] [2][3]

Since uracil is a normal component of RNA, the rationale behind the development of the drug was
that cancer cells, with their increased genetic instability, might be more sensitive to 'decoy'
molecules that mimic the natural compound than normal cells. The scientific goal in this case was to
                                   ‫آزمایشگاه اشکال دارویی‬
synthesize a drug which demonstrated specific uracil antagonism. The drug proved to have anti-
tumor capabilities.

When elemental fluorine is reacted with uracil, 5-fluorouracil is produced. 5-Fluorouracil
masquerades as uracil during the nucleic acid replication process. Because 5-Fluorouracil is similar in
shape to, but does not perform the same chemistry as uracil the drug inhibits RNA replication
enzymes, thereby eliminating RNA synthesis and stopping the growth of cancerous cells.


Mode of action
As a pyrimidine analogue, it is transformed inside the cell into different cytotoxic metabolites which
are then incorporated into DNA and RNA, finally inducing cell cycle arrest and apoptosis by inhibiting
the cell's ability to synthesize DNA. It is an S-phase specific drug and only active during certain cell
cycles. In addition to being incorporated in DNA and RNA, the drug has been shown to inhibit the
activity of the exosome complex, an exoribonuclease complex of which the activity is essential for
cell survival.

Capecitabine is a prodrug that is converted into 5-FU in the tissues. It can be administered orally

				
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