Suppositories manufacture

Solid oral dosage forms, particularly tablets, are the preferred type of formulation in the United States. Not only are these products widely accepted by consumers, but they are also relatively cheaper to develop and manufacture than oral liquids or suspensions, par-enterals, or suppositories. Figure 4 shows, quite clearly, that even the elderly primarily make use of solid oral dosage forms [162]. 

Gelatin is produced by partial acid or partial alkaline hydrolysis of animal collagen. It has a wide variety of therapeutic and pharmaceutical uses. It is often used in the manufacture of hard and soft capsule shells, suppositories and tablets, and is sometimes used as a sponge during surgical procedures, as it can absorb many times its own weight of blood. 

Cocoa butter NF is defined as the fat obtained from the seed of Theobroma Cacao Linne (Family Sterculiaceae) (44). Cocoa butter softens at 30°C and melts at 34°C. It contains four different forms alpha, beta, beta prime, and gamma with melting points of 22°C, 34°C to 35°C, 28°C and 18°C, respectively. The beta form is the most stable and is desired for suppositories. The biggest challenge with the polymorphism of cocoa butter is the impact of the manufacturing process on the characteristics of the suppository itself. When cocoa butter is hastily melted at a temperature greatly exceeding the minimum required temperature and then quickly chilled, the result is metastable crystalline form (a crystals), which may not even... 

Theobroma Theobroma cacao (Sterculiaceae) kernel 35-50 oleic (35), stearic (35), palmitic (26), linoleic (3) suppository base, chocolate manufacture Theobroma oil (cocoa butter) is a solid... 

Other barbiturates are manufactured as a powder that is injected into the patient s vein. In addition, pentobarbital is manufactured as a suppository that is inserted in the rectum. Pentobarbital is also available in capsule, tablet, elixir, and injection dosages. Phenobarbital is produced in capsule, tablet, injection, and elixir dosages. 

Dronabinol. Dronabinol is a synthetic form of THC that was approved for medical use by the FDA in 1985. Sold under the trade name Marinol, it is prescribed as an antiemitic for cancer patients undergoing chemotherapy and as an appetite stimulant for AIDS patients who become anorexic. Marinol is manufactured in 2.5-, 5-, and 10-mg capsules, which are taken orally. Critics argue that suppositories would be more useful than capsules since cancer and AIDS patients are often unable to keep food down. 

Attempts to make nonirritant orally reliable preparations of theophylline have resulted in choline theophyllinate and numerous variants. Sustained-release formulations are convenient for asthmatics, but they cannot be assumed to be bioequivalent and repeat prescriptions should adhere to the formulation of a particular manufacturer. Suppositories are available. Aminophylline is used in ... 

Biopharmaceutic considerations in the design and manufacture of a drug product to deliver the active drug with the desired bioavailability characteristics include 1) the type of drug product (e.g., solution, suspension suppository) 2) the nature of the excipients in the drug product 3) the physicochemical properties of the drug molecule and 4) the route of drug administration. 

Suppositories and other rectal dosage forms are more expensive to prepare and dispense than simple tablets. Therefore, unless there is a significant need and advantage by utilizing a rectal dosage form, suppositories are not likely to be used. Recently, techniques have been developed to prepare suppositories more efficiently which could lead to lower manufacturing costs. 

The large-scale manufacture of suppositories and pessaries uses either the fusion method where the drug is dispersed in a molten base and the mixture poured into molds to solidify, or the cold compression methodJ In the latter process, the medicament and cold-grated base, usually theobroma oil or witepsol base, are intimately mixed and placed in a cylinder. The mass is extruded by means of a piston through small holes that connect with the mold. The cavities are filled by pressure with the mass which is prevented from escaping by movable end plates. The plates are removed and the suppositories ejected by further extrusion. The extrusion equipment is chilled to prevent melting of the components due to the heat generated by the friction of compression. 

In soft gelatin capsules, powdered cellulose may be used to teduce the sedimentation rate of oily suspension fills. It is also used as the powder base material of powder dosage forms, and as a suspending agent in aqueous suspensions for peroral delivery. It may also be used to reduce sedimentation during the manufacture of suppositories. 

Glyceryl monostearate is a lubricant for tablet manufacturing and may be used to form sustained-release matrices for solid dosage forms.Sustained-release applications include the formulation of pellets for tablets or suppositories and the preparation of a veterinary bolus. Glyceryl monostearate has also been used as a matrix ingredient for a biodegradable, implantable, controlled-release dosage form. ... 

El Assasy AH, Foda NH, Badawi SS, Abd-El-Rehim RT. Release characteristics and bioavallability of pirprofen from suppository bases. Egyptian ] Pharm Sci 1995 36(1-6) 15-29. Harmia-Pulkkinen T, Ojantakanen S. In vitro release kinetics of timolol and tlmol oleate from polyethylcyanoacrylate nanoparticles. Part 2. Nanoparticles manufacture with timolol maleate using different surfactants and organic solvents. Acta Pharm Penn 1992 101(2) 57-63. 

Additives Some grades of commercial bases already contain additives, and these are usually identified by the manufacturers by means of suitable letters and numbers. Additives may also be incorporated by formulators. Properties of suppositories that have been modified and additives or types of additives that have been used are shown in Table I. Water is undesirable as an additive because it enhances hydrolysis and... 

Senior N. Review of rectal suppositories 1 formulation and manufacture. Pharm ] 1969 203 703-706. 

In spite of the many papers published on them and the often major improvements in bioavailability and the stability they provide, solid solutions and dispersions in povidone have up to now only found use in a few commercial products. Tables 81 and 82 show how phenytoin and nifedipine, for example, can be processed relatively straightforwardly in the form of a physical mixture or coprecipitate with povidone. Cyclosporine, oxodipine and spironolactone tablets or nor-ethindrone suppositories are further examples [508,533,566,575]. It is interesting to compare the dissolution data for phenytoin after manufacture and after two years storage at room temperature in Figs. 52 and 53 no major difference can be seen. 

As one example for the development of innovative uses of tabletting presses, the manufacture of suppositories shall be mentioned. It was found that up to 100000 good quality suppositories can be produced per hour if punches, dies and air in the machine housing are cooled, an appropriate quality of hard fat (i.e. a... 

Building B of ABC Pharmaceutical is designed to manufacture liquids and semisolid products. The conventional pharmaceutical dosage forms include drops, syrups, suspensions, creams/ointments, and suppositories. 

---