PHYSICAL CHARACTERISTICS AND AVAILABILITY OF KETOROLAC

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PHYSICAL CHARACTERISTICS AND AVAILABILITY OF KETOROLAC Powered By Docstoc
					Aim of work
The main objective of this
 investigation was to optimize the
 formulation of chitosan beads with
 Ketorolac tromethamine to
 minimize the gastrointestinal side
 effects of the drug and to prolong
 its release . Design the effect of the
 formulation variables on drug
 release.
CONCLUSION •
 1-The formulation variables, namely,
 chitosan concentration and
 stabilization time markedly influenced
 the drug content. Increasing chitosan
 concentration from 0.75 to 1.25 % and
 (SPP) concentration from 1 to 3 %
 significantly decreased the drug
 content of the beads. While, increasing
 the stabilization time from 30 to 90 min
 significantly increased the drug
 content.
2-Statistical analysis of the release data
revealed that the increase in chitosan
concentration from0.75 to 1.25 %, and
stabilization time from 30 to 90 min increased
significantly the t50% of the drug. Kinetic
analysis of the release data revealed that
zero order and diffusion controlled
mechanisms prevailed.
3-Based on the previous findings , it is
evident that the preparation of the beads
using chitosan,( SPP) and gluteraldehyde
resulted in retardation of release of the
highly water soluble KT.
4-The experimental design used was
the factorial design
Table(1): The Experimental Plan of the 33 Factorial Design.


                                      Levels
        Variables
        Chitosan           0.75         1.00       1.25
    concentration(%)
           SPP             1.00         2.00       3.00
    concentration(%)
    Stabilization time     30.0         60.0       90.0
                          1.04

                          1.02

                            1
Mean Particle Size (mm)




                          0.98

                          0.96

                          0.94

                          0.92

                           0.9

                          0.88

                          0.86

                          0.84
                                 1   2    3   4   5   6   7   8   9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27

                                                                         Formula Number

                                         Fig (1): Mean Particle Size of Ketorolac Tromethamine Beads Prepared Using Chitosan
                          110                                                                                       110




                                                                                 %Ketorolac Tromethamine Released
                          100                                                                                       100
%Ketorolac Tromethamine




                           90                                                                                       90
                           80                                                                                       80
                           70                              Powd.D                                                   70
        Released




                           60                                                                                                                                 Powd.D
                                                                                                                    60
                                                           Com. F
                           50                                                                                       50                                        Com. F
                           40                              F1                                                                                                 F4
                                                                                                                    40
                           30                              F2                                                                                                 F5
                                                                                                                    30
                           20
                                                           F3                                                       20                                        F6
                           10
                                                                                                                    10
                            0
                                                                                                                     0
                                0 60 120 180 240 300 360 420 480 540
                                                                                                                          0   60   120 180 240 300 360 420 480 540
                                             Time(min)                                                                                     Time(min)
                           Fig(4):Release Pattern of Ketorolac                                                        Fig(5):Release Pattern of Ketorolac Tromethamine from
                           Tromethamine from Beads Prepared with 1%                                                   Beads Prepared with 1% Drug , 0.75% Chitosan,2% SPP,1%
                                                                                                                      Gluteraldehyde at Different Stabilization Time Using a
                           Drug , 0.75% Chitosan,1% SPP,1% Gluteraldehyde
                                                                                                                      Gradient pH System.
                           at Different Stabilization Time Using a Gradient pH
                          110
                          100
%Ketorolac Tromethamine


                           90
                           80




                                                                             %Ketorolac Tromethamine
                           70                                                                    110
        Released




                                                             Powd. D.                            100
                           60                                                                     90
                                                             Com. F
                           50                                                                     80




                                                                                     Released
                                                                                                  70                             Powd. D.
                           40                                F7
                                                                                                  60                             Com. F
                           30                                F8                                   50
                           20                                                                     40                             F10
                                                             F9                                   30
                           10                                                                                                    F11
                                                                                                  20
                            0
                                                                                                  10                             F12
                                0 60 120 180 240 300 360 420 480 540                               0
                                                                                                       0   60 120 180 240 300 360 420 480 540
                                                 Time(min)
                          Fig(6):Release Pattern of Ketorolac                                                       Time (min)
                          Tromethamine Beads Prepared with 1% Drug,
                                                                                           Fig(7):Release Pattern of
                          0.75% Chitosan ,3% SPP, 1% Gluteraldehyde at                    KetorolacTromethaminefromBeads Prepared with
                          Different Stabilization Time Using a Gradient pH                1%Drug,1%Chitosan,1%SPP,1%Gluteraldehyde at
                          System.                                                         Different Stabilization Time Using a Gradient pH
                                                                                          System.
                          110
%Ketorolac Tromethamine   100                                                                             110
                           90                                                                             100




                                                                               %Ketorolac Tromethamine
                           80                                                                              90
                           70                                  Powd. D                                     80
        Released




                           60                                  Com. F                                      70




                                                                                       Released
                           50                                                                              60                                 Powd. D
                                                               F13
                           40                                                                              50                                 Com. F
                           30                                  F14
                                                                                                           40
                           20                                                                                                                 F16
                                                               F15                                         30
                           10                                                                                                                 F17
                                                                                                           20
                            0
                                                                                                           10                                 F18
                                0   60 120 180 240 300 360 420 480 540                                      0
                                                  Time(min)                                                     0 60 120 180 240 300 360 420 480 540
                            Fig(8):Release Pattern of Ketorolac Tromethamine                                                   Time(min)
                            from Beads Prepared with 1% Drug ,                                           Fig(9):Release Pattern of Ketorolac
                            1%Chitosan,2%SPP,1%Gluteraldehyde at Different                               Tromethamine from Beads Prepared with 1%
                            Stabilization Time Using a Gradient pH System.                               Drug, 1% Chitosan,3%SPP,1% Gluteraldehyde
                                                                                                         atDIfferent Stabilization Time Using a Gradient pH
                                                                                                         System.
                                                                                                                          110
                                                                                                                          100




                                                                                                %Ketorolac Tromethamine
                                                                                                                           90
                                                                                                                           80
%Ketorolac Tromethamine Released




                                   110                                                                                                                                      Powd. D
                                                                                                                           70




                                                                                                        Released
                                   100
                                    90                                                                                     60                                               Com. F
                                    80                                                                                     50
                                    70
                                                                                                                                                                            F22
                                                                              Powd. D.                                     40
                                    60                                                                                                                                      F23
                                    50
                                                                              Com F                                        30
                                    40                                        F19                                          20                                               F24
                                    30                                        F20                                          10
                                    20                                        F21                                           0
                                    10
                                                                                                                                0      60 120 180 240 300 360 420 480 540
                                     0
                                         0    60 120 180 240 300 360 420 480 540                                                                       Time(min)
                                                            Time(min)
                                         Fig(10):Release Pattern of Ketorolac Tromethamine                                          Fig(11):Release Pattern of Ketorolac Tromethamine from
                                         from Beads Prepared with 1% Drug,1.25% Chitosan ,                                          Beads Prepared with 1% Drug, 1.25%Chitosan,2% SPP, 1%
                                         1% SPP , 1%Gluteraldehyde at Different Stabilization
                                                                                                                                    Gluteraldehyde at Different Stabilization Time Using a
                                         Time Using a Gradient pH system.
                                                                                                                                    Gradient pH System.
                          110
                          100

%Ketorolac Tromethamine
                           90
                           80
                                                                        Pow d. D
        Released           70
                           60                                           Com . F
                           50                                           F25
                           40                                           F26
                           30
                                                                        F27
                           20
                           10
                            0
                                0   60   120 180   240 300    360 420    480 540
                                                   Tim e(m in)
                          Fig(12):Release Pattern of Ketorolac Trom etham ine from
                          Beads Prepared w ith 1% Drug,1.25%Chitosan,3% SPP, 1%
                          Gluteraldehyde at Different Stabilization Tim e Using a
                          Gradient pH System .

				
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