1. INDUSTRIAL PHARMACEUTICAL TECNOLOGY (ESSENTIALS) Part 2
Dr. Yauheni Hryniuk,
Associate professor

2. Raw Materials For Gelatin Capsules
1-Non- toxic
2-readily soluble in biological fluids at body temp.
3-It is good film forming material.
2/21/2018

3. 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 in-process aid in order to prevent microbiological contamination during manufacture.

4. HARD GELATIN CAPSULES

5. Manufacturing dipped Metal moulds hot gelatin solution: gels to form
into
Dried, cut, removed from the moulds film
& two parts are joined together.

6. 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.

7. Examples of Soft Gelatin Capsules
Suppositories

8. 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.

9. 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).
2/21/2018

10. PREPARATION OF SOFT GELATIN CAPSULES
Drip-feed Process
Rotary Die Process

11. Quality standards and compendial requirements
Weight and weight variation
Content uniformity
Disintegration
Dissolution
in-process controls
verification after the production

12. Liquid dosage forms

13. 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.

14. 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.)

15. 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.

16. Sterile dosage forms for injection

17. Semisolid dosage forms
Ointments
Suppositories

18. Semisolid dosage forms
Ointments
Definition: semisolid preparations intended for external application are termed ointments.
Ingredients: drug substance + ointment base + Excipients (Antioxidants, Antimicrobial preservatives)

19. 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)

20. Antioxidants preparations Antioxidants aqueous Sodium sulfite(Na2SO3)
sodium bisulfite(NaHSO3), hypophosphorous acid(H3PO2)
ascobic acid( vitamin C)
oleaginous
Alpha tocopherol(vitamin E)
Butylhydroxyanisole(BHA)
ascorbyl palmitate

21. Suppositories
Suppositories are semisolid dosage forms intended for insertion into body orifices where they melt, soften, or dissolve and exert localized or systemic effects.

22. 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.

23. 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);

24. 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.

25. 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)

26. Preparation of Suppositories
Suppositories are prepared by two methods:
(1) Preparation by compression
(2) Fusion or preparation by mold

28. 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.

29. Aerosols, Sprays and Inhalations
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.
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.

30. Advantages over other types of dosage forms
A portion of medication maybe easily withdrawn from the package without contamination or exposure to the remaining material
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.
Topical medication may be applied in a uniform, thin layer to the skin, without touching the affected area.
Aerosol application is a "clean" process, requiring little or no "wash-up" by the user.

31. 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.

32. 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.

33. 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.

34. 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.

35. THANK YOU