C 6 POWDERS by qfK0DH

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									POWDERS    and
GRANULES
 POWDERS
        -pulvis-
Powders are mixtures of
finely divided drugs
and/or chemicals used
externally or internally in
dry form.
  Advantages                        Disadvantages
-More stable than liquid
                                    - Undesirability of taking bitter or
- More convenient to swallow than          unpleasant tasting of drugs
        tablet or capsules
                                    - Difficulty of protecting from
- Used in blending with medicated            decomposition those
        application as ointments,            powders containing
        suppositories and pastes             hygroscopic, deliquescent
                                             or aromatic materials
- Can be prepared into granules
       for use in preparing         -Time and expenses require in the
       tablets and or                      preparation of uniform
       reconstituted to liquid             powders are great
       form
                                    - Inaccuracy of bulk powders
- Rapid therapeutic effect due to
         large surface area
            Characteristics
• Chemical & physical
  features
 morphology               stability
 purity                   particle size
 solubility               uniformity
 flowability              compatibility
PRECAUTIONS IN
PREPARING POWDERS TO
BE OF HIGH EFFICACY
1. The powders must be
     homogenous blend
     of all the components
2. Must be of the most
    advantageous particle
    size
 STEPS in
PREPARING       Particle size
POWDERS          reduction




 Packaging of
  Powders
                                Mixing of
                                Powders
Particle Size
Reduction
     Comminution or
grinding may be defined as
the process of particle size
reduction
METHODS OF COMMINUTION IN SMALL SCALE
        Trituration - Is the process of grinding a powder in a mortar and pestle
        to reduce its particle size.

        Pulverization by Intervention - Is the reduction of particle size with
        the aid of a second agent which can be readily removed from the
        pulverized product
        Example: applies to camphor where it is readily triturated when a few drops
        of alcohol or other volatile solvent is added. The pulverized camphor is
        readily recovered as the solvent evaporates.

Levigation - Is the process of
reducing particle size by first
forming a paste of the solid with a
minimum amount of a levigating
agent and then triturating the
paste in a mortar or on slab with a
spatula.
The Basis of Choice of
 Levigating Agent is:
1.Its ability to form a smooth
  paste with the substance
2.Its compatibility in the
  product so water cannot
  be used for levigating a
  substance for oleaginous
  ointment base
OPENING OF STANDARD SIEVES



     SIEVE   SIEVE       SIEVE    SIEVE
     NUMBER OPENING      NUMBER   OPENING


     2.0     9.50 mm     70.0     212.00 um
     3.5     5.60 mm     80.0     180.00 um
     4.0     4.75 mm     100.0    150.00 um
     8.0     2.36 mm     120.0    125.00 um
     10.0    2.00 mm     200.0    75.00 um
     20.0    850.00 um   230.0    63.00 um
     30.0    600.00 um   270.0    53.00 um
     40.0    425.00 um   325.0    45.00 um
     50.0    300.00 um   400.0    38.00 um
     60.0    250.00 um
Medicated Powders
     @ Some medicated powders are intended to be used internally;
            others externally
     @ Most powders for internal use are taken orally after mixing
            with water
     @ Some powders are intended to be inhaled for local or
            systemic effects

@ Medicated powders for external use are
       dusted on the affected area from
       sifter-type container or applied from
       powder aerosol
@ External use should bear a label marked
       EXTERNAL USE ONLY
@ Medicated for oral use may be intended for
       local effects (laxatives) or systemic
       effect (analgesic)
     AEROSOL POWDERS
@ administered by inhalation with the
   aid of dry-powder inhalers, which
   deliver micronized particles of
   medication in metered quantities
   (range of 1 to 6 um)
@ example: Alupent; each dose is
   delivered through the
   mouthpiece upon activation of the
   aerosol unit’s valve
@ it use in the treatment of asthma
    and other bronchial disorders
         Particle Size Analysis
      Powders of vegetable and animal drugs

•   Very coarse (No.8)
•   Coarse (no. 20)
•   Moderately coarse (No. 40)
•   Fine (No. 60)
•   Very Fine (No. 80)
         Particle Size Analysis
        The powders fineness for chemicals

•   Coarse (No. 20)
•   Moderately coarse (No. 40)
•   Fine (No. 80)
•   Very Fine (No. 120)
Purpose of particle size analysis
• To obtain quantitative data on the size,
  distribution, and shapes of drug and non
  drug components to be used in
  pharmaceutical formulation
Methods Of Determining Particle Size
 SEDIMENTATION RATE, in which particles
is determined by measuring the terminal settling velocity
  of particles through a liquid medium in gravitational or
  centrifugal environment (range: 0.8-300 micrometers)
    Light Energy diffraction, in which particle size is
determine by the reduction in light reaching the sensor
   as the particle, dispersed in a liquid or gas, passes
through the sensing zone (range: 0.2 - 500 micrometers)
Laser halography, in which a pulsed laser is fired through
an aerolized particle spray and photographed in three
dimension with a halographic camera, allowing the
particles to be individually imaged and sized (range: 1.4 -
100 micrometers)
Cascade Impaction is based on the principle that a
particle, driven by an airstream, will impact on a
surface in its path, provided that its inertia is
sufficient to overcome the drag force that tends to
keep it in the airstream
SIEVING – particles are passed by mechanical
shaking through a series of sieves (from 40 to 9500
micrometers, depending upon sieve sizes)
MICROSCOPY – particles are sized through the
use of calibrated grid background or other measuring
devise ( range 0.2 to 100 micrometers)
Powders may be mixed or
prepared depending upon the
   Mixing ingredients, the
nature of Of Powders
amount of powders to be
prepared, equipment available
SPATULATION Is a method by
which small amount of powders may be
blended by a spatula on a sheet of paper
or pill till.
This is also applied to solid substances
which liquefy or form eutectic mixtures

Examples: phenol, camphor, menthol,
thymol,   ASA, phenylsalicylate, and
phenacetin
TRITURATION may be employed
both to comminute and to mix powder
using mortar preferably with a rough
inner surface.
       In case a small amount of potent
substance is to be mixed with a large
amount of diluent, a general method
known as “geometric          dilution” is
employed to obtain a uniform mix
SIFTING is the process of mixing
     by passing the powder
     through sifters. Not
     generally acceptable for
     potent drugs. Sifting
     results in light puffy
     product.
TUMBLING BY MECHANICAL
MIXING is the process of mixing
powders by placing in large
containers or powder blenders
the rotates by tumbling motion.
Mixing by this process is
thorough but time consuming
THUMBLERS
2. Dry Granulation - Dry
granulating, also called slugging
or roller compaction, involves
the pressing of mixed powders
into an object to be reground
into a precise powder.
This action increases particle
density, and improves powder
flow.
          Milling
Milling equipment is used
to improve flow, reduce
segregation, enhance
drying, and limit wide
particle size distribution.
Blending of Powders


              The "V" BLENDER is an efficient
               and versatile blending machine
                 for mixing and lubrication
                   process of dry powders
                       homogeneously
 The RIBBON BLENDER is an
efficient and versatile blending
  machine for mixing of dry
       granules & powders
         homogeneously
PACKAGING
   of POWDERS
BULK POWDERS
1. Antacid or laxative powders, which the
  patient generally takes by mixing the directed
  amount of powder
2. Douche powder usually dissolved in warm
  water by the patient for vaginal use
3. Dusting powders
4. Medicated or non medicated powders
5. Dentifrices or dental cleansing powders
6. Insufflations
7. Triturations
  DIVIDED
 POWDERS
Latin - Chartulae,
Abbr. “charts” or
     chartula
After the powders have
been properly mixed by
the geometric dilution, it
may be divided into
individual units based
upon the dose. Method
used is called “block and
divide”
Powder papers:
2 3/4 x 3 3/4 inches,
3 x 4 1/2 inches,
3 3/4 x 5 inches and
4 1/2 x 6 inches
SELECTION OF PAPER
1. Hygroscopic or deliquescent - use
   water proof or waxed paper

2. Powders        containing   volatile
   components - should be wrapped in
   waxed or in glassine papers

3. Powders containing neither volatile
   components       nor      ingredients
   adversely affected by air or moisture
   are usually be wrapped in white
   papers
Papers may be:
1. Simple bond papers
2. Vegetable parchment
3. Glassine, a glazed,
   transparent paper
4. Waxed paper, a transparent
   waterproof paper
Examples Of Finely Divided Powders
1. Oral powders are supplied as finely divided
   powders or as effervescent granules
2. Douche powders, generally dissolved in warm
   water for vaginal use
3. Medicated or non medicated powders for
   external application usually dispensed in sifter
   cans for convenient application to the skin
4. Dentifrices or dental cleansing powder
5. Denture powders, for dentifrices or for adhesive
   to hold dentures
Advantages Of Divided Powders
1.Flexibility
2. Rapid therapeutic effect
3.Stability
4.Ease of administration
Disadvantages Of Divided Powders
1. Time consuming to prepare

2. Not well suited for dispensing of many
   unpleasant tasting hygroscopic drug

3. Inaccuracy
Official Powdered Vegetable
 Drugs
1.   Powdered Belladona Extract, NF
2.   Powdered Digitalis Extract
3.   Powdered Ipecac, USP
4.   Powdered Opium, USP
5.   Powdered Rauwolfia Serpentina, NF
Official Powders
1. Ampicillin Soluble Powder - dry mixture of the ampicillin
   and diluents and stabilising agents - anti-infectives
2. Polymixin B Sulfate and Bacitracin Zinc Topical
   Powder, USP - used as a topical anti-infective
3. Compound Clioquinol Powder, USP - mixture of
   Clioquinol, lactic acid, zinc stearate, and lactose -
   vaginal insufflation as an antitrichomonal
4. Nystatin Topical Powder, USP - employed as a topical
   dusting powder in          the treatment of mycotic
   infections
5. Tolnaftate Powder, USP - used topically in the
   treatment of fungal infection
3 Official Powders For Topical Use:
1. Absorbable Dusting powder- gloves lubricant

2. Compound Iodochlorhydroxyquin Powder NF -
   vaginal Insufflations as antimicrobial

3. Methylbenzenethonium Choride Powders NF -
   local anti-infectives for diaper rash in infants
               GRANULES

     are prepared agglomerates of
smaller particles. They are generally
irregularly shaped and behave as single
larger particles. They are usually in the
4 to 12 sieve size range.
Examples:
1. Pricipen (Ampicillin) for oral suspension
     (for reconstitution)
2. Senokot Granules - for laxative
3. Effervescent products as Bromo Seltzer
4. K-lyte - Granulations of
     effervescent products
     - compressed into
           tablet
EFFERVESCENT GRANULATED SALTS
Effervescent salts are granules or coarse to very
      coarse powders containing a soluble
      medicinal agent in a dry mixture
Composition: Sodium bicarbonate, citric acid, and
    tartaric acid
Note: When added to water, the acids and base
      react to liberate CO2 resulting in
      effervescence
Example: Sodium Phosphate - cathartic
Reasons why effervescent salts are usually prepared from a combination
         of citric acid and tartaric acid rather than a single acid because
         of difficulties presented as follows:
1. When tartaric acid is the sole acid, resulting granules lose their
        firmness readily and crumble
2. Citric acid alone results in a sticky mixture difficult to granulate
So combination will give a balance and obtain a satisfactory product.
Method Of Preparation
1. Dry or Fusion method
2. Wet method


Objectives Of Using The Methods
1. To determine the proper formula for the preparation that will result in
        effective effervescence and effect of the product
2. Efficient use of the acids and base present
3. Stable granulation
4. Pleasant taste
Preparation of Granules
1. Dry Granulation
        = the dry powder is passed through a roll compactor and then
        through a granulating machine
        = a roll compactor, also called a roll press or roller compactor,
        processes a fine powder into dense sheets
        = the surface of the compacting rolls may be smooth or may have
        pocket indentations or corrugations that allow compaction of
        different forms and textures
        = the compacted powder is granulated to uniform particle size in
        mechanical granulator
        = or dry method also termed slugging
2. Wet Granulation
Examples: Zantac EFFERdose tablets
        Lactinex Granules = mixed culture of Lactobacillus acidophilus and
        Lactobacillus bulgaricus in 1 g packets used in the treatment of
        uncomplicated diarrhea; mixed with water, beverages, sprinkled on
        food, or eaten plain
Official Effervescent Salt: Sodium Phosphate NF


Dried Sodium Phosphate (Dried and Powdered)         200 g
Sodium Bicarbonate (Dry Powder)                     477 g
Tartaric acid (Dry Powder)                          252 g
Citric acid, (Uneffluorescence crystals)            162 g
         to make                                    1000 g
A good working formula
         Citric acid              15%
         Tartaric acid            28%
         Sodium bicarbonate      53%


NOTE: Dose is assumed to be a heaping teaspoon (5g). Granules should be
        packaged in tight, dry wide mouth glass jars in cool place
Reactions:
1. H3C6H507.H20     + 3NaHCO3               Na3C6H5O7 + 4H2O + 3CO2
         citric acid                          sodium citrate
2. H2C4H4O6      + 2NaHCO3           Na2C4H4O6 + 2H2O      + 2CO2
         tartaric acid
         It should be noted that it requires 3 molecules of NaHCO3 to
neutralize 1 molecule of citric acid (1) and 2 molecules of NaHCO 3 to
neutralize 1 molecule of tartaric acid (2)
1. For the amount of NaHCO3 required to neutralize 162 g citric acid:
         162 g           X                  (84 X 3 molecules)
         210.13          252.03 MW NaHCO3
                    X = 194.3 g of NaHCO3
2. For the amount of NaHCO3 for neutralizing 252 g tartaric acid
         252 g tartaric              X                 (84 x2)
         150.09 MW                   168.02 g NaHCO3
                    X= 282.1 g NaHCO3
         Total    194.3 + 282.1 = 476.4 g
THE PROCEDURE: FUSION OR DRY METHOD


1. Powder citric acid crystals
2. Mix with other powders previously sieved through #60 to ensure
        uniformity
3. Place in a suitable dish in an oven previously heated between 93-104oC
4. During the heating, turn the powder with an acid resistant spatula.
5. It is removed from the oven and rubbed through an acid resistant sieve
           to produce granules of desired size
         no. 4 sieve produce large granules
         no. 8 sieve produced medium size granules
         no. 10 sieve produced small granules
6. After sieving the granules are immediately dried at a temperature not
         exceeding 54oC the transfer immediately to a container and
         promptly and tightly sealed.
WET METHOD
          This differs from the fusion method in that the source of binding agent
is not necessarily the water crystallization of citric acid but may be water added
to the nonsolvent (such as alcohol) which is employed as the moistening agent
to form the pliable mass of material for granulation.
        This granules may be compressed into tablets form ( Bromo Seltzer
by Warner Lambert)



DENTIFRICES
         Form of bulk powder, generally containing flavors, soap or detergent,
mild abrasive, and an polishing agent.
Forms: paste, powder, liquid, and block or solid
Use: used with a tooth brush for the purpose of cleansing the accessible
         surfaces of the teeth.
         These contain abrasives such as Calcium carbonate, calcium
         phosphate, calcium sulfate, insoluble sodium metaphosphate,
         hydrated Al2 O3 , MgCO3 and phosphates, NaHCO3 and NaCl
         Dentifrices contain non-carbohydrates sweetening agents but a
         few contain sugar.
          Toothpaste contain liquids such as glycerin, propylene glycol, sorbitol
solution, water and thickeners such as starch, tragacanth, alginate and cellulose
derivatives.
         Block form consist the following:
1. Polishing agents - calcium carbonate, dibasic calcium phosphate
         dihydrate or anhydrous, tricalcium phosphate, calcium
         pyrophosphate, insoluble sodium metaphosphate and hydrated
         alumina
2. Massed with 20% to 30% of hard soap and sufficient glycerol and
        flavoring oils to retain an attractive appearance and flavor
3. Tooth powders contain an abrasive, a surface active detergent e.g.
        sodium lauryl sulfate
4. Flavoring oils - spearmint, peppermint, wintergreen, and cinnamon mint
5. Sweetening agents - saccharin
6. Water 7. Humectant - glycerol, sorbitol, propylene glycol
8. Binder - gums, karaya and tragacanth, seaweed colloids: sodium
        alginate and Irish moss extract, and synthetic derivatives of
        cellulose: methylcellulose and carboxymethylcellulose
9. Preservatives - dichlorophene, benzoates, and esters
10. Fluoride compounds - stannous and sodium fluoride
Example Formula Of Dentifrices

CMC        120 H                          0.9 g
Glycerin                                  1.0 g
Propylene Glycol                          18.0 g
Purified water                            13.5 g
Methyl paraben                             0.1 g
Saccharin sodium solution 50%              0.1 g
Peppermint oil                             0.3 g
Mineral oil                               1.0 g
Sodium Lauryl Sulfate                     2.5 g
Dicalcium Phosphate in very fine powder   54.0 g
      DOUCHE POWDERS

       Are products which are
completely soluble and are
intended to be dissolved in
water prior to use as antiseptic
or cleansing agent for a body
cavity
     How to use: simply
add the prescribed amount
or powder to the
appropriate volume of warm
water and stirs until
dissolved
Components:

1. Boric acid or Borax
2. Astringents as K alum, ammonium alum,
         ZnSO4
3. Antimicrobial as oxyquinoline sulfate or
         povidone iodine
4. Quaternary ammonium compounds as
         benzethonium chloride
5. Detergents as sodium lauryl sulfate
6. Oxidizing agents as sodium perborate
7. Salts, as sodium citrate, sodium chloride
8. Aromatic as menthol, thymol, eucalyptol, methyl
         salicylate, and phenol
Packaging: may be in
a wide mouth glass
jars to protect from
volatile constituents
and by bulk powder
boxes
              DUSTING POWDERS
      Are non-toxic preparations for local
application and therefore no systemic effect.
Dispensing: should be dispensed in a very fine
     state    of    subdivision  to      enhance
     effectiveness and minimized irritation
Packaging: available in sifter-type containers or
     pressure aerosols, the latter more
     expensive but protects content from air,
     moisture and contamination
Uses:      lubricants,   absorbents,    antiseptics,
        antipruritics,      astringents,        and
        antiperspirant
TRITURATIONS

         Are dilution of potent powdered drugs prepared by
intimately mixing them with a suitable diluents in a definite proportion
by weight. They were at one time official as 1-10 dilutions.

Preparation: in making trituration, geometric dilution is used to assure
         thorough mixing. The active ingredient is placed in a clean
smooth, dry mortar. An equal bulk (by estimation) of the      weight
diluents is added. It is mixed quickly and twice as much diluents, not
equal to the amount in the mortar is added and mixed.

Examples: Strychnine sulfate, arsenic, mercury bichloride, atropine in
convenient concentration using lactose as the diluents for use at the
Rx counter.
            INSUFFLATIONS
        Are finely divided powders introduced
into the body cavities such as the ears, nose,
throat, tooth sockets and vagina.
Administration: Insufflator (powder blower) is
usually used, pressure aerosols are being
employed especially for potent drugs.
Examples:
       1.    Norisodrine    Sulfate    Aerohaler
       Cartridge (Abbott) - specialized
       equipment or inhalation
       2. Cromolyn Sodium Powder - relieve
       bronchial asthma
          TEA

       Also    known      as
“species” are made from
coarsely powdered dried
herbs and are intended for
use in making medicinal teas
and poultices.
END

								
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