Title: Drug excipient of silicone rubber

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Claims: What is claimed is:

1. A non-toxic sustained release pharmaceutical composition in the form of a shaped object having a Shore A hardness of 45-70, consisting essentially of a safe and pharmaceutically active amount of a nonionic lipophilic drug having a dissociation constant of less than 10.sup..sup.-7 and which is olefinically or acetylenically unsaturated and soluble in ether, chloroform or benzene, said drug being dissolved or uniformly suspended in a non-toxic vulcanized LTV linear dimethylpolysiloxane elastomer and said composition being prepared by reacting, at an elevated temperature and in contact with a catalytic amount of a platinum-based vulcanization catalyst capable of catalyzing the reaction between silicon-linked hydrogen residues and silicon-linked vinyl residues a mixture of said drug and a vulcanizable composition consisting essentially of:

a. a polydimethylsiloxane having vinyl groups on both ends;

b. a copolymer consisting essentially of SiO.sub.2 units, (CH.sub.3).sub.3 SiO.sub.0.5 units, Vinyl (CH.sub.3).sub. 2 SiO.sub.0.5 units; and

c. a cross-linking Si-H component, consisting essentially of (CH.sub.3).sub.3 SiO.sub.0.5 units, (CH.sub.3).sub.2 SiO units and CH.sub.3 HSiO units.

2. A pharmaceutical composition according to claim 1, further comprising a catalytic amount of a platinum metal-based catalyst dissolved therein.

3. A pharmaceutical composition according to claim 1, wherein component a) comprises 20-100 parts by weight of vinyl terminated linear organopolysiloxane having a viscosity of 500-200,000 centistokes (at 25.degree. C.) of the general formula: ##EQU2## wherein R.sub.2 is lower alkyl and n is an integer of about 200-1600; b. comprises 0-50 parts by weight of an organopolysiloxane copolymer consisting essentially of:

i. R'.sub.3 SiO.sub.0.5 units

ii. R'.sub.2 ViSiO.sub.0.5 units, and

iii. SiO.sub.2 units

wherein Vi is a vinyl group, R'.sub.2 and R'.sub.3 are each a saturated, lower alkyl, at least 50% of R' being methyl; and

c. comprises 5-15 parts by weight of an organohydrogen polysiloxane of the general formula ##STR3## wherein R" is lower alkyl, a and b are each positive numbers, the ratio of a:b is 0.5-10; the sum of a+b is 1-2.5; at least three hydrogen atoms linked to different Si atoms are present per molecule; and said component contains 50-500 molar percent, based on unsaturated end groups contained in components (a) and (b), of vinyl groups attached to Si-H.

4. A pharmaceutical composition according to claim 3 adapted for implantation into a human or animal body.

5. A pharmaceutical composition according to claim 3 in the form of a prosthetic device.

6. A pharmaceutical composition according to claim 3 wherein said medicament is a steroid.

7. A pharmaceutical composition according to claim 3 in a form suitable for intrauterine or intravaginal administration.

8. A pharmaceutical composition according to claim 7 in the form of a vaginal ring.

9. A pharmaceutical composition according to claim 8, wherein said medicament is a steroid.

Other info:

Inventors: Schopflin, Gisela (Berlin, DT)

Application Number: 616001
Filing Date: 1975-09-23
Publication_date: 1977-03-15
Assignee: Schering Aktiengesellschaft (Berlin & Bergkamen, DT)
Primary Class(es): 424/432 128/833
Other Classes:
US Patent Ref:

3279996	Oct, 1966	Long et al.	424/32.
3545439	Dec, 1970	Duncan	128/130.
3920805	Nov, 1975	Roseman	424/15.

Other Refs: 2,158,226

May, 1973	DT.

Primary Examiner: Rose, Shep K.
Assistant Examiner:
Attorney: Millen & White