CHAPTER 7 GELATIN CAPSULES Capsules *solid dosage forms in which the medicinal agents and/or inert substances are

e enclosed in a small edible container (usually made of gelatin) Types of Capsules 1. Hard Gelatin Capsules (Dry-Filled Capsules) 2. Soft Gelatin Capsules (Pearls) Advantages: *Mask the unpleasant tastes, aroma, or appearance of a drug. *Allow powders to be dispensed in an uncompressed form, thus allowing for quicker dissolution and absorption of the drug following oral dosing (as compared with tablets.) *Easier than tablets for some people to swallow, due to slippery texture of the gelatin capsule shell. 5. Can be made to alter the release rate of the drug. Disadvantages: *Subject to the effects of relative humidity and to microbial contamination. *Difficult to administer for some people who have problems in swallowing. *More expensive to produce commercially because of costly materials used. Hard Gelatin Capsules *Used by community pharmacist in extemporaneous compounding of prescriptions. *Commonly employed in clinical drug trials to compare investigational drug to another drug or a placebo. *May be made opaque by adding agents such as titanium oxide. Capsule Shells *Made of gelatin, sugar, and water *Clear, colorless and essentially tasteless *May be colored with various FD&C and D&C dyes *May be made opaque by adding TiO Approximate Capacity Sizes of Capsules Capacity Fill weight Cap Sizes (mL) at 0.8 g/mL 5 0.12 0.10 4 0.20 0.19 3 0.27 0.24 2 0.37 0.30 1 0.48 0.40 0 0.67 0.54 00 000 0.95 1.36 0.76 1.10

*Lubricant/ Glidant improve flow properties and reduce interparticulate friction of powder mixture (fumed silicon dioxide, magnesium stearate, steric acid or talc) *Surface-Active Agent facilitates wetting of powder by the GI fluids (sodium lauryl sulfate) Soft Gelatin Capsule *Made of gelatin in which glycerin or sorbitol has been added to render it elastic or plastic like. *Contains more moisture than hard gelatin capsules thus contains preservatives like Parabens. *Hermetically seal and encapsulate liquids, suspensions, pasty materials or dry powders. Methods in Preparing Gelatin Capsule *Plate Process oldest commercial process that uses set of molds to form capsules. *Rotary Die Process a continuous process; two plasticized gelatin ribbons are continuously and simultaneously fed with liquid or paste fill between the rollers of the rotary die mechanism. Compendial Requirements for Capsules 1. Added Substances *are harmless in the quantities used *do not exceed the minimum amounts required to provide their intended effects *it includes formulation excipients to produce a safe, efficacious and stable dosage form *do not impair the products bioavailability, therapeutic efficacy or safety *do not interfere with requisite compendial assays and tests 2. Containers for Dispensing *tightly closed and light resistant container (depending on the item) 3. Disintegration Test *measures the time it takes for a tablet to break-up into smaller fragments, with no visible palpable core left on the mesh/ basket screen *uses the Disintegration Apparatus 4. Dissolution Test *measures the amount of the active ingredient dissolved in a given fluid (such as water or simulated gastric/ intestinal fluid) 5. Weight Variation *determines the uniformity of the weights of each individual unit (capsule) 6. Content Uniformity *determines the homogeneity of the distribution of the active ingredient in each individual unit (capsule) *USP Specs: NLT 85% and NMT 115% of the labeled potency for 9 out of 10 dosage units tested 7. Content labeling Requirement *visual inspection, checking, and proofreading of the reformulation contents per container of package of finished capsules 8. Stability Testing (accelerated and real time stability tests) *determination of the shelf life, expiry date, appropriate storage conditions, degradation products of the active drug 9. Moisture Permeation Test *the degree and rate of moisture penetration are determined by (a) packaging the unit dose together with a color-revealing dessicant pellet; (b) exposing the packaged unit to a known RH over a specified time; (c) observing the dessicant pellet for a color change; (d) color change indicates the absorption of moisture of the packaged dosage form

Capsule Formation Contains: *Active Ingredient *Diluent/Filler produce the proper capsule fill volume (lactose, microcrystalline cellulose, starch) *Disintegrant assist break-up and distribution of the capsule contents in the stomach (pregelatinized starch, cross carmellose sodium starch glycolate)