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Dosage - Chapter 7

Dosage - Chapter 7

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Published by Kim Manlangit

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Published by: Kim Manlangit on Aug 08, 2010
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1
 Name:Pharmaceutical DosageChapter 7: CapsulesCapsules and Tablets
y
 
Preferred when administered orally by adults: convenientlycarried, readily identified, easily taken
y
 
V
ariety of dosage strengths, providing:
 
F
lexibility to the prescriber 
 
A
ccurate individualized dosage for the patientPharmaceutical Standpoints
y
 
Solid dosage forms:
 
M
anufactured efficiently and productively
 
Packaged and shipped at lower cost and with less breakage
 
M
ore stable
 
H
ave longer shelf life than liquidsDisadvantages of Tablets and Capsules
y
 
Swallowing
y
 
F
ormulation difficulties
y
 
Some have poor bioavailability or poor water solubility
y
 
Some have irritant effect on the GIT when taken orallyKey
F
eatures of a Good Tablet or Capsule
y
 
Stability of the active drug
y
 
A
ccurate dose
y
 
U
niformity (weight, amount of active ingredient, coatingthickness, etc)
y
 
Consistent performance (manufacturing parameters, pharmacokinetics)
y
 
A
 ppropriate disintegration and dissolution
y
 
Can withstand packaging, shipping, handling without breakage
y
 
M
asking of taste and odor 
y
 
Pharmaceutically elegant
y
 
Production economically soundOverview of Capsules
y
 
Capsules
 
M
edicinal agents and/or inert substancesenclosed in a small shell of gelatin
 
Swallowed wholly
y
 
Open capsule or crushed tablets
 
M
ixed with food or drink (children or patientswho are unable to swallow solid dosage forms)Solid Dosage
F
orms that must be Left Intact
y
 
E
nteric coated tablets
 
To pass through the stomach for drug release andabsorption in the intestine
y
 
E
xtended-release dosage forms
 
Provide prolonged release of the medication
y
 
Sublingual or buccal tablets
 
To dissolve under the tongue or in the mouth
A
lternative Products if Patients cannot Swallow an Intact SolidDosage
F
orm
y
 
Chewable tablet
y
 
Instant dissolving tablet
y
 
Oral liquid
y
 
Oral or nasal inhalation solution
y
 
Suppository
y
 
InjectionCharacteristics
y
 
M
ay be swallowed whole by patient
y
 
M
ay be inserted into the rectum for drug release andabsorption from site
y
 
The content may be removed from the gelatin shell andemployed as pre measured medicinal powder, the capsuleshell being use to contain a dose of the medicinalsubstance.
 
E
x: Theo-dur Sprinkle
y
 
E
legance
y
 
E
ase of use
y
 
Portability
y
 
Tasteless shell to mask the unpleasant taste/ odor 
y
 
Permits physician to prescribe the exact medication needed buy the patient
y
 
Conveniently carried
y
 
eadily identified
y
 
E
asily taken
y
 
Tasteless when swallowed
y
 
Commonly embossed or imprinted on their surface themanufacturer¶s name and product code readily identified
y
 
A
vailable in variety of dosage strength
y
 
Provide flexibility to the prescriber and accurateindividualized dosage for the patient
y
 
Packaged and shipped by manufacturers at lower cost, less breakage than liquid forms
y
 
M
ore stable and longer shelf life
H
ard Gelatin Capsules
y
 
A
lso referred to as ³D
F
C´ Dry
F
illed Capsule,manufactured into two sections, the capsule body and ashorter cap
y
 
M
anufacture most of the commercially available medicatedcapsules
 
E
mployed in clinical drug trials
 
F
or extemporaneous compounding of  prescriptions
y
 
Contains 13% to 16% moisture
y
 
M
anufactured form:
 
Gelatin
 
Titanium dioxide (opacifying agent)
 
0
.15% SO
2
(prevents decomposition of gelatin)
 
Colorants
E
mpty Capsule Shells
y
 
M
ade of gelatin, sugar and water 
y
 
H
ard or soft
y
 
Softened (made elastic or plasticized) by adding glycerin or  polyhydric alcohol like sorbitol)
y
 
Can be: clear, colorless, tasteless
y
 
Colored with various
F
D&C and D&C dyes
y
 
M
ade opaque by adding agents like titanium oxide
 
2
 
Gelatin
y
 
Obtained by partial hydrolysis of collagen from the skin,white connective tissue and bones of animals
y
 
Properties:
 
Stable in air (dry)
 
Subject to microbial decompositions whenmoistened
 
Insoluble in cold water, softens throughabsorption of up to 1
0
times its weight of water 
 
Soluble in hot water and in warm gastric fluid
 
A
protein, digested by proteolytic enzymes andabsorbed
 
H
igh humidity: additional moisture is absorbed
 
B
ecomes distorted and lose their rigidshape
 
emedy: use desiccant material (silicagel, slay, or activated charcoal)
 
E
xtreme dryness: moisture is lost
 
B
ecomes brittle and crumble whenhandledGelatin Capsule
y
 
Dissolves and exposes its contents
y
 
U
nsuitable for aqueous liquids (softens gelatin anddistorted, resulting in leakage of contents)
A
dditives
y
 
Desiccant
 
To protect against the absorption of atmosphericmoisture
 
Dried silica gel
 
Clay
 
A
ctivated charcoal
y
 
Diluents or filter 
 
To produce the proper capsules fill volume
 
Provide cohesion to the powders
 
F
or the transfer of the powder blend into thecapsule shells
 
Lactose
 
M
icrocrystalline cellulose
 
Starch
E
xcipients
A
dded for Capsule
F
ill
y
 
W
etting agents (Li
2
CO
3
)
 
A
dded to capsule formulation to enhance drugdissolution
y
 
A
 bsorbent
 
Separates interacting agents
 
A
 bsorbs any liquefied material that may form
 
M
agnesium carbonate
 
Kaolin or light
M
gO
y
 
Disintegrants
 
To assist the break up and disintegration of thecapsule¶s contents in the stomach
 
Pregelatinized starch
 
Croscarmellose
 
Sodium starch glycolate
y
 
Lubricant or glidant
 
E
nhances flow properties
 
Silicon dioxide
 
M
agnesium stearate
 
Stearic acid or talc (about
0
.25-1%)
y
 
Surface active agent (surfactant)
 
To facilitate wetting by GI fluids
 
Sodium lauryl sulfate
F
ixed or 
V
olatile Oils
y
 
Do not interfere with stability of the gelatin shells
E
utectic
M
ixture of Drugs
y
 
M
ixtures of agents that have a propensity to liquefy whenadmixed
M
ethods to Track the Passage of Capsules and Tablets through theGIT to
M
ap their Transit Time and Drug
elease Patterns
y
 
Gamma scintigraphy
 
Gamma ray emitting radiotracer incorporated intothe formulation with gamma camera coupled to adata recording system
y
 
Pharmacoscintographic evaluation
 
I
V
I
V
C for bioavailability of immediate release products
 
Combination of scintigraphy and pharmacokineticstudies
 
A
ssesses integrity and transit of time of entericcoated tablets through the stomach to theintestines
 
Drug and dosage form evaluation in new productdevelopment
y
 
H
eidelberg capsule (No.
0
gelatin capsule)
 
 p
H
sensitive (non indigestible radio telemetricdevice)
 
A
non-radioactive means to measure solid dosageforms (fasting and non fasting human subjects)
 
Gastric p
H
, gastric emptying time,gastric residence time
M
anufacture of 
H
ard Gelatin Capsule Shells
y
 
M
anufactured in 2 sections:
 
Capsule body
 
Shorter capDrug
A
 bsorption Depends on a Number of 
F
actors
y
 
Solubility of the drug
y
 
Type of product formulation (immediate release, modifiedenteric)
y
 
Gastrointestinal contents
y
 
Physiologic character and responseInnovations to Provide Distinctions (Distinctive Looking Capsules)
y
 
Pulvules
 
E
nd of the body-producing peg is tapered whileleaving the cap-making peg rounded
y
 
Spansule capsules
 
Capsules with the ends of both the bodies andcaps highly taperedInnovations in Capsule Shell Designs
y
 
Snap-fit
 
Two halves of capsule shells positively joinedthrough locking grooves in the shell walls
 
3
 
 
E
nsure reliable closing of the filled capsule
y
 
Coni-snap
 
im of the capsule body is tapered slightly, notstraight
 
educes the risk of the capsule rims touching or  joining
 
E
liminates splitting (telescoping) and/or dentingof capsule shell
y
 
Coni-snap supro
 
im is tapered, upper capsule part extends(rounded edge of lower surface is visible)
 
Opening is difficult, lower surface less grippingto pull 2 halves apart
 
Increases security of contents and integrity of thecapsule
 
E
liminates splitting (telescoping) and/or dentingof capsule shell***Check the book: coni-snap capsule parts, coni-snap and coni-snapsupro capsule sizes (as in actual size of capsule in relation to a quart)Capsule Sizes
000
15 grains 972mg (largest)
00
1
0
grains 648mg
0
7.5 grains 486mg1 5 grains 324mg2 4 grains 259mg3 3 grains 194mg4 2 grains 13
0
mg5 1 grain 64.8mg (smallest)Preparation of 
F
illed
H
ard Gelatin Capsules
y
 
F
ormulation development and preparation and selection of capsule size
y
 
F
illing the capsule shells
y
 
Capsule sealing (optional)
y
 
Cleaning and polishing of filled capsules
E
xamples of 
F
ill in
H
ard Gelatin Capsules
y
 
Powder or granulate
y
 
Pellet mixture
y
 
Paste
y
 
Capsule
y
 
TabletDeveloping the
F
ormulation and Selection of Capsule Size
y
 
Goals in preparing a capsule:
 
A
ccurate dosage
 
Good availability
 
E
ase of filling and production
 
Stability
 
E
leganceDry
F
ormulations
y
 
B
lended thoroughly (active and inactive components) toensure uniformity of powder mix for the fillCare in
B
lending
y
 
Lack of homogeneity for low dose drugs
 
esults in significant therapeutic consequencesPreformulation Studies
y
 
Determine whether all of the formulation¶s bulk powders
 
E
ffectively blended together 
 
equire reduction of particle size
 
Other processes to achieve homogeneity
M
ethods in
educing Particle Size
y
 
M
illing
 
Particles ranging from 5
0
-1
000
micrometer 
y
 
M
icronization
 
Drugs of lower dose or when smaller particles arerequired
 
Particles ranging from 1-2
0
micrometer 
F
illing
H
ard Capsule Shells
y
 
U
se punch method
 
Steps:
 
Count the capsules
 
Powder encapsulated placed on a sheet of clean paper or a glass or porcelain plate
 
Powder mixed formed into a cake depth of approximately ¼ to 1/3 the length of thecapsule body
 
E
mpty capsule punched vertically into the powder cake until filledProcess of Capsule
F
illing
y
 
M
illing or sieving of all ingredients
y
 
B
lending
 
Powder blender or empty capsules
y
 
Capsule filler 
y
 
Capsule deduster or cleaner 
y
 
Capsule injection screen
y
 
Capsule check-weighing system or reject
y
 
F
inished capsules
y
 
Packaging***Check book: profill systemCapsule Sealing
y
 
F
or the manufacturers:
 
Sealing the joint between the 2 capsule partsusing:
 
Colored band of gelatin (K 
A
PS
EA
LS,Parker Davis)
 
H
eat welding process
o
 
F
uses the capsule cap to the body through the double wallthickness at their juncture(distinctive ³ring´ around thecapsule)
 
Liquid wetting agent (liquid sealing-water and ethanol sprayed around theseam area), followed by thermal bonding
 
E
xtemporaneously
o
 
W
arm gelatin solution,lightly coating the inner surface of the cap prior to

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