Soft gelatin capsules and processes for their manufacture

Details Soft gelatin capsules and processes for their manufacture Soft gelatin capsules and processes for their manufacture

1988-10-14

1990-01-02

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Capsules

A61K 964

Patent

active

048912298

DESCRIPTION:

BRIEF SUMMARY
DESCRIPTION OF THE INVENTION

The present invention concerns soft gelatin capsules with a gelatin shell, at least one plasticizer and a capsule filling which contains at least one pharmacologically-active substance and a solvent, as well as processes for their manufacture.
Gelatin capsules, especially soft gelatin capsules, have become increasingly important as a form of medication since it became feasible, in the 1930's, to manufacture them by making and filling the capsules in one operation. Compared to other dosage forms they show a number of advantages. Thus they are odorless and tasteless, they can be taken easily and, owing to their swelling capability and water solubility, the drugs are readily liberated in the stomach. Numerous drugs which, on account of their sensitivity to oxidation and to light, their thermal stability or their hygroscopicity, may not be processed into other medicinal forms, can be encapsulated without impairment of their function.
Soft gelatin capsules serve chiefly for the containment of liquids, i.e. oily solutions, suspensions or emulsions. Vegetable, animal and mineral oils, liquid hydrocarbons, ethereal oils and also polyethylene glycols are in use as fillings. Fats and waxes are also applied or admixed to increase the consistency.
Polyethylene glycols are superior to other possible filling materials for soft gelatin capsules in a number of ways. In contrast to oily liquids, polyethylene glycols are mixable with water in all proportions.
At the same time, because polyethylene glycols are able to dissolve many drugs which are sparingly soluble or insoluble in water, the use of polyethylene glycols with such drugs makes possible a particularly favourable liberation of the active material. In many cases, sparingly water soluble drugs which have been dissolved in polyethylene glycols and then put into soft gelatin capsules are outstanding, by virtue of an exceptionally good bio-availability of the drug.
From DE-OS No. 33 07 353 of the applicant, soft gelatin capsules are known in which the dried capsule shell contains 4 to 40% by weight of sorbitol and/or sorbitan, the polyethylene glycol used in the capsule filling for solution and suspension of the active material is at least 50% by weight a polyethylene glycol having a mean molecular weight of 600, and the capsule filling contains up to 20% by weight of glycerol and/or propylene glycol. These soft gelatin capsules have been remarkably successful, yet they still have the disadvantage that a number of active materials are not sufficiently soluble in polyethylene glycol. Consequently, large capsules are necessary for the encapsulation of such sparingly soluble active materials. There exists, therefore, a continuing need for solvents which are able to dissolve larger amounts of active materials and yet can be processed into stable soft gelatin capsules. Solvents suitable for human consumption, such as ethanol, propylene glycol, dimethyl acetamide, lactic acid, glycerol, butanediol and the polyethylene glycol ether of tetrahydrofurfuryl alcohol, have been shown by the investigations of the applicant to be unsuitable for introduction into soft gelatin capsules in larger quantities, because the capsule fillings made with these solvents cause, after a short time, softening and deformation of the capsules produced, which therefore are not marketable. The reasons for these stability problems are evidently to be sought in the good water miscibility and the lower molecular weight of these solvents.
Surprisingly, it has now been found that mixtures of polyethylene glycol ethers of tetrahydrofurfurol are suitable solvents for active materials in soft gelatin capsules, if the capsule filling is encapsulated in a wet gelatin shell and the capsules obtained are intensively dried for at least 5 days, and preferably for 6 to 10 days. After 5 to 10 days, the quantities of water which pass from the wet gelatin shell into the capsule filling during encapsulation have obviously been removed to such an extent that they, together with the polyethyl

REFERENCES:
patent: 2638686 (1953-05-01), Stirn et al.
patent: 4088750 (1978-05-01), Creswell et al.
patent: 4609403 (1986-09-01), Withwer et al.
The Merck Index, Ninth Edition, 1976, p. 583.
"Die Kapsel", Stuttgart 1982, pp. 58-82.
"Arzneimittel-Forschung", Feb. 1956, pp. 75-77.

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