1
Q
Capsules
A
- Solid dosage forms containing drug/excipients in a “shell”
- Shells can be made of gelatin, cellulose, or other suitable substances
- Shells can be hard or soft
2
Q
Capsule Uses (3)
A
- Oral - swallowed whole (most common)
- Sprinkle on food - good for those with trouble swallowing (Ex: Theo-dur, Feverall sprinkles)
- Inhalation - Ventolin Rotocaps, Intal capsules
3
Q
Gelatin Physiochemical Properties
A
- Obtain from partial hydrolysis of collagen (retrieved from skin, connective tissue, or bones of cows and pigs)
- Stable in dry air, microbial decomposition when moist or in solution
- Insoluble (swellable) in cold water
- Soluble in hot water and gastric fluid
4
Q
Hard Gelatin Capsules
A
- Basic formulation - gelatin, sugar, water (13-16%)
- Optional additions - colorants and opacifiers (opacity)
- 2 piece design - capsule body and shorter cap, “locking mechanism”
- Purchased as empty capsules
5
Q
Manufacturing of Hard Gelatin Capsules
A
- Dipping metal pins into gelatin solution
- Defects - sizing/joining, external grease, bubbles, uneven cuts
- Must control levels of humidity (too dry or too sticky) and water sources (clean or purified) in manufacturing process
6
Q
Advantages of Hard Gelatin Capsules (5)
A
- Rapid dissolution in stomach and lack of powder compaction (good bioavailability)
- Flexibility of contents (powder, liquid, pellets)
- Protection against light (if opaque) and oxygen (if sealed)
- No taste. Non direct contact with tongue
- Good patient compliance
7
Q
Disadvantages of Hard Gelatin Capsules (6)
A
- Potential adhesion to esophagus
- Not suitable for hydrolytic, deliquescent, or hydroscopic drug (absorbs water out of shell)
- Cost (drug + shell)
- Filling equipment - slower than tablets (adds to cost)
- Not suitable for vegetarian patients and patients with religious restrictions
* *6. Problems with powder blending (homogeneity) and flow)
8
Q
HGC Appearance Variations
A
- Color
- Opacity
- Size (4-00) - 4 is smallest and 00 is largest
- Printing
- Flavors
9
Q
HGC Shape Variations (4)
A
- Conventional - rounded at the ends
- Pulvule - tapered at one end
- Spansule - tapered at both ends
- DB Capsule - used in overencapsulation, larger diameters and capsule cap
10
Q
Types of Fills for HGC
A
- Solids - powders, granules, pellets, tablets, capsules
- Semisolids - thixotropic mixtures, thermosoftening mixtures, pastes
- Liquids - oily, suspensions, solutions
11
Q
Amount of Fill Dilemma
A
More you put into the capsule, the great risk of non homogeneous mixture and the longer it takes to make up.
12
Q
Band-Seals
A
- Gelatin used to seal around the cap/body joint
- Necessary for liquid-filled products (prevents leaking)
- Optional for solid filled. Ex: Benadryl “Kapseal”
13
Q
Use of Inactive Ingredients in HGC
A
- Only use when necessary
- Use filler/diluent, disintegrant, glidant, lubricant to fill capsules in addition to API
14
Q
HGC Blending & Filling Process
A
- Add ingredients and mix well
- Add lubricant and don’t mix as vigorously
- Add powder blend to empty capsules
- Goes through deduster
- Inspected and weighed
- Rejects separated out and approved, finished capsules are packaged
15
Q
Mechanisms of Filling HGC (4)
A
- “Punch” filling powders in HGC for a small number of capsules
- Hand operated capsule filling machines - larger quantities than punch filling
- Semi-automatic Machines
- Automatic Machines
16
Q
Do you need tap density or bulk density for calculating minimum capsule sizes?
A
Tap Density
17
Q
Vegetable-Based Capsules
A
- Cellulose derivative (HPMC)
- Strength mechanism isn’t dependent on residual water
- Less residual water in shell and absorbs less water out of atmosphere
18
Q
NCE
A
New Chemical Entity
19
Q
Methods to Minimize Contact with Incompatible Materials (3)
A
- *When necessary**
1. Add more diluent
2. Put small capsule or tablet in a larger capsule with other API/excipients
3. Produce granules from one API & mix with other API and excipients
20
Q
Soft Gelatin Capsules
A
- Characteristically flexible - platicizer (not water) in shell
- Wide ranges of shapes - oblong, spherical, tube-shaped, elliptical, etc.
- Fill material, usually liquid
- Capsules are generally prepared, filled, and sealed in continuous operation via a Rotary Die Process
- Filling and Sealing occurs simultaneously
21
Q
SGC Applications (5)
A
- Oral - swallow whole, chewable, lozenges, Delayed-Release (EC)
- Rectal/vaginal suppositories - use moisture to dissolve
- Opthalmic and topical
- Cosmetics
- Other
22
Q
SGC Advantages (9)
A
- Good for low melting solids
- Good/enhanced bioavailability
- Tamper evident
- Easy to swallow
- Content uniformity (overcomes homogeneity issues, especially in low dosing)
- Taste and odor masking
- Fast onset of action
- Protects against oxygen and light (opacifier)
- Overcomes certain tableting problems
23
Q
SGC Disadvantages (2)
A
- *Same disadvantages pertaining to water in shells**
1. Specialized equipment - increases cost since you need contract manufacturers to produce this dosage form, still must control humidity and water source
2. More intimate contact between shell and fill (liquid)
24
Q
Dynamic Nature of SGC Shell
A
- Water can get into shell AND fill
- Plasticizer can go in and out of shell
- Drug can precipitate out and not be in solution
25
How to deal with dynamic nature of SGC Shell
- Choose plasticizer that won't evaporate out (water)
| - Pick fillant liquids that don't evaporate out (not aqueous based)
26
Composition of SGC Shell
- Gelatin
- Plasticizer - glycerin, propylene glycol, sorbitol
- Preservatives
- Colorants - opacifiers, dyes, lakes
- Residual moisture - 6-10%
27
Liquids Used in SGC
- Water immmiscible volatile or non-volatile (can't leave fill to enter shell) Ex: vegetable oil, hydrocarbons (mineral oil), medium triglycerides
- Water miscible nonvolatile - PEG 400/600. Can enter shell but not atmosphere
- Fill liquids can affect drug absorption rate
28
Requirements of SGC Fills
- pH - 2.5-7.5
- Low water concentrations (<5%)
- Drug - not soluble in water but is chemically stable
- Use of ethanol in as a cosolvent in special packaging (aluminum blister pack)
- DON'T use aldehydes and aqueous emulsions
29
Filling Liquids in HGC
- Alternative to SGC
- Advantages - all SGC advantages and well as having possible in-house development (cost/time)
- Disadvantages - same as SGC plus having physical/chemical stability
30
Dispensing Capsules
- Stored in cool, dry place
- Bulk package - manually count desired quantity before dispensing (counting tray)
- Unit dose packaging/strip packaging - hospitals, nursing homes, OTC allergy/cold/cough medicines
31
Counting Devices (3)
1. Counting Trays
2. Electronic Sensors
3. Baker Cell
**Cleaning = important consideration**
802
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