Claims
- 1. A microparticle having a diameter of between 1 and 250 microns comprising octreotide in a free base, acid addition salt or complex form, in a biodegradeable, biocompatible polymeric matrix of a 40/60 to 60/40 polylactide-co-glycolide ester of a polyol, said polyol being selected from the group consisting of 1) a (C.sub.3-6) carbon chain containing alcohol having 3 to 6 hydroxyl groups, 2) a mono-saccharide and 3) a di-saccharide, and said esterified polyol having at least 3 polylactide-co-glycolide chains, wherein said octreotide is present in an amount from 0.2 to 20 percent by weight relative to said polymeric matrix and said octreotide is distributed throughout said polymeric matrix.
- 2. A microparticle according to claim 1 wherein the octreotide is in a polymeric matrix of poly(D,L-lactide co-glycolide)glucose.
- 3. A sustained relase formulation comprising a microparticle of claim 1.
- 4. A sustained release formulation comprising a microparticle of claim 2.
- 5. A microparticle according to claim 2 wherein the surface is free of octreotide.
- 6. A sustained release formulation according to claim 4 which when administered subcutaneously to a rat at a dosage of 10 mg of octreotide per kg of body weight exhibits an octreotide concentration in the blood plasma of at least 0.3 ng/ml and less than 20 ng/ml during a 30 day term.
- 7. A sustained release formulation according to claim 4 which when administered to a rabbit intramuscularly at a dosage of 5 mg of octreotide per kg of body weight exhibits an octreotide concentration of at least 0.3 ng/ml and at most 20 ng/ml during a 50 day term.
- 8. A sustained release formulation according to claim 4 which when administered to a rabbit intramuscularly at a dosage of 5 mg of octreotide per kg of body weight exhibits a retardation of at least 70% over a period of from 0 to 42 or 43 days.
- 9. A sustained release formulation according to claim 4 which when administered to a rat subcutaneously at a dosage of 10 mg of octreotide per kg of body weight exhibits an average blood plasma level of from 2.5 to 6.5 ng/ml over a period of from 0 to 42 days.
- 10. A sustained release formulation according to claim 4 which when administered to a rabbit intramuscularly at a dosage of 5 mg of octreotide per kg of body weight exhibits an average blood plasma level of from 3.5 to 6.5 ng/ml.
- 11. A microparticle of claim 1 wherein said octreotide is an acetate salt.
- 12. A microparticle of claim 1 wherein said octreotide is a pamoate salt.
Priority Claims (2)
Number |
Date |
Country |
Kind |
3974/90 |
Jun 1990 |
HUX |
|
9016840 |
Aug 1990 |
GBX |
|
Parent Case Info
This is a continuation-in-part of U.S. patent application Ser. No. 07/411,347, filed Sep. 22, 1989, which in turn is a continuation-in-part of U.S. patent application Ser. No. 07/377,023, filed Jul. 7, 1989, both now abandoned.
US Referenced Citations (7)
Foreign Referenced Citations (8)
Number |
Date |
Country |
0058481 |
Aug 1982 |
EPX |
0092918 |
Nov 1983 |
EPX |
0052510 |
Aug 1986 |
EPX |
2842089 |
Apr 1979 |
DEX |
2145422 |
Mar 1985 |
GBX |
2208200 |
Mar 1989 |
GBX |
2209937 |
Jun 1989 |
GBX |
2234169 |
Jan 1991 |
GBX |
Non-Patent Literature Citations (1)
Entry |
Mason-Garcia et al, PNAC 85, 5688-5692.(1988). |
Continuation in Parts (2)
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Number |
Date |
Country |
Parent |
411347 |
Sep 1989 |
|
Parent |
377023 |
Jul 1989 |
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