Transcript Industrial Pharmaceutical Technology / Part 2

INDUSTRIAL
PHARMACEUTICAL
TECNOLOGY
(ESSENTIALS)
Part 2
Dr. Yauheni Hryniuk,
Associate professor
Raw Materials For Gelatin Capsules
 Gelatin
1-Non- toxic
2-readily soluble in biological fluids at body temp.
3-It is good film forming material.
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Raw Materials For Gelatin Capsules
Plasticizers: Glycerol, sorbitol , PEG …
Colorants: titanium dioxide (white& is used as
opacifying agent, Oxides of iron ( black, red &
yellow).
Preservatives: are sometimes added to capsules as inprocess aid in order to prevent microbiological
contamination during manufacture.
HARD GELATIN CAPSULES
Manufacturing
 Metal moulds
dipped
hot gelatin solution: gels to form
into
Dried, cut, removed from the moulds
& two parts are joined together.
film
Filling
Hard gelatin capsules are most frequently filled
with powders
The only limitation is that they should not react
with the gelatin, e.g. aldehydes, or interfere
with the integrity of the shell, e.g. water which
will soften the wall.
Examples of Soft Gelatin Capsules
Suppositories
Advantages:
•
Useful when it is desirable to seal the medication within the capsule. The
drug may hydrolyze or oxidize on long term storage.
drug poorly soluble in water or gastric juice and the bioavailability from
some solid dosage forms might be poor.
can be protected from the environment by solution or dispersion in oil
and encapsulation by gelatin. (resist gaseous diffusion and contain little
labile water.)
• The soft capsules are especially important to contain liquid drugs or drug
solutions → rapid release of the contents with enhanced bioavailability.
• Volatile drug substances or drug materials especially susceptible to
deterioration in the presence of air may be better suited to a soft gelatin
capsule.
• Soft gelatin capsules are handsome and are easily swallowed by the
patient.
Disadvantages:
• Soft gelatin capsules are not easily prepared except on a large
scale and with specialized equipment.
• They are an expensive dosage form, when compared with
direct compression tablets or hard shell capsules.
• There is a more intimate contact between the shell and its
liquid contents than exists with dry-filled hard gelatin
capsules, which increases the possibility of interactions.
• Not adaptable to incorporation of more than one kind of fill
into the same capsule (compare with hard shell capsules).
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PREPARATION OF SOFT GELATIN
CAPSULES
Rotary Die Process
Drip-feed Process
Quality standards and compendial
requirements
Weight and weight variation
 Content uniformity
 Disintegration
 Dissolution
in-process controls
verification after the production
Liquid
dosage forms
Liquid dosage forms are prepared:
(1) by dissolving the active drug
substance(s) in an aqueous or
nonaqueous (e.g. alcohol, ether,
glycerin) solvent, (2) by suspensing
the drug in appropriate medium, or
(3) by incorporating the drug
substance into an oil or water
phases.
Liquid dosage forms can be
administered:
• Topically - lotions or
suspension applied to the skin, eye drops,
nasal drops, ear drops
• Orally (p.o.) - oral
suspension and solution
• Parenterally subcutaneous injection (s.c.),
intramuscular injection (i.m.)
and intravenous administration (i.v.)
Sterile dosage forms for
injection
 These forms contain solutions, powder
or lyophilized powder ready to be
dissolve, suspensions, and emulsions.
They are packaged in ampoules, vials,
plastic bags, one-point cut ampoules,
and prefilled disposable syringes.
Sterile dosage forms for
injection
Semisolid dosage forms
Ointments
Suppositories
Semisolid dosage forms
Ointments
 Definition: semisolid preparations intended for
external application are termed ointments.
 Ingredients: drug substance + ointment base +
Excipients (Antioxidants, Antimicrobial
preservatives)
Ointment bases
Ointment bases are classified into four general
groups:
 (1) Hydrocarbon bases (petrolatum, paraffin,
Lanolin)
 (2) Absorption bases (Hydrophilic Petrolatum and
Anhydrous lanolin)
 (3) Water-Removable Bases (+ Emulsifying
agents)
 (4) Water-Soluble Bases (Polyethylene glycols,
Carbopols)
Antioxidants
preparations
aqueous
oleaginous
Antioxidants
Sodium sulfite(Na2SO3)
sodium bisulfite(NaHSO3),
hypophosphorous acid(H3PO2)
ascobic acid( vitamin C)
Alpha tocopherol(vitamin E)
Butylhydroxyanisole(BHA)
ascorbyl palmitate
Suppositories
Suppositories are semisolid dosage forms
intended for insertion into body orifices where
they melt, soften, or dissolve and exert localized or
systemic effects.
Suppositories
Suppositories are commonly employed rectally,
vaginally and occasionally urethrally.
They have various shapes and weights
depending upon the density of the base and the
medicaments present in it, and the individual
manufacturer's product.
advantages over oral therapy (I)
(a) drugs destroyed or inactivated by the pH or enzymatic
activity of the stomach or intestines need not be exposed
to these destructive environments;
(b) drugs irritating to the stomach may be given without
causing such irritation;
(c) drugs destroyed by portal circulation may bypass the liver
after rectal absorption (drugs enter the portal circulation
after oral administration and absorption);
advantages over oral therapy (II)
(d) the route is convenient for administration of
drugs to adult or pediatric patients who may be
unable or unwilling to swallow medication;
(e) it is an effective route in the treatment of
patients with vomiting episodes.
Classification of Suppository Bases
 According to bases physical characteristics the
bases can be classified into
(1) fatty or oleaginous bases (cocoa butter,
compounds of glycerin)
(2)water-soluble or water-miscible bases
(Glycerinated gelatin, Polyethylene glycols)
Preparation of Suppositories
Suppositories are prepared by two
methods:
(1) Preparation by compression
(2) Fusion or preparation by mold
Molding
(a) the melting of the base
(b) incorporating of any required medicaments
(c) pouring the melt into molds
(d) allowing the melt to cool and congeal into suppositories
(e) removing the formed suppositories from the mold.
 Notice: Suppositories of cocoa butter, glycerinated gelatin,
polyethylene glycol, and most other suppository bases are
suitable for preparation by molding.
Aerosols, Sprays and Inhalations
o PHARMACEUTICAL AEROSOLS are pressurized
dosage forms containing one or more active ingredients
which upon actuation emit a fine dispersion of liquid
and/or solid materials in a gaseous medium.
o They depend upon the function of the container, its
valve assembly, and an added component--the
propellant--for the physical delivery of the medication
in proper form.
Advantages over other types of
dosage forms
1. A portion of medication maybe easily withdrawn from the package
without contamination or exposure to the remaining material
2. By virtue of its hermetic character, the aerosol container protects
medicinal agents adversely affected by atmospheric oxygen and
moisture. If the product is packaged under sterile conditions,
sterility may also be maintained during the shelf-life of the product.
3. Topical medication may be applied in a uniform, thin layer to the
skin, without touching the affected area.
4. Aerosol application is a "clean" process, requiring little or no
"wash-up" by the user.
Disadvantages of the pharmaceutical aerosol:
 High cost.
 Because of the volatility, the propellants has the
refrigeration effect which can irritate the skin.
 To certain individuals, who may be sensitive to the
propellant agent and who utilize an inhalation
aerosol, the fluorinated hydrocarbons may exhibit
cardiotoxic effects following rapid and repeated use
of the aerosol product.
An aerosol formulation consists of two component parts,
the product concentrate and the propellant.
1 The product concentrate is the active ingredient of
the aerosol combined with the required adjuncts,
such as antioxidants, surface-active agents, and
solvents, to prepare a stable and efficacious product.
2 the propellant
 When the propellant is a liquefied gas or a mixture
of liquefied gases, it frequently serves the dual role
of propellant and solvent or vehicle for the product
concentrate.
 In certain aerosol systems, no liquefied compressed
gases, as carbon dioxide, nitrogen, and nitrous
oxide, are employed as the propellant.
Testing the Filled Containers
 The aerosol container is tested under various
environmental conditions for leaks or weakness in
the valve assembly or container.
 The valve discharge rate is determined by
discharging a portion of the contents of a
previously weighed aerosol during a given period
of time, and calculating.
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