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 biodegradable, 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 a therapeutically effective amount from at least 0.2 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 release formulation comprising a microparticle of claim 2.
- 4. A sustained release formulation according to claim 3 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.
- 5. A sustained release formulation according to claim 3 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.
- 6. A sustained release formulation according to claim 3 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.
- 7. A sustained release formulation according to claim 3 which when administered to a rat subcutaneously at a dosage of 10 mg of octreotide per kg of body weight exhibits an average plasma level of from 2.5 to 6.5 ng/ml over a period of from 0 to 42 days.
- 8. A sustained release formulation according to claim 3 which when administered to a rabbit intramuscularly at a dosage of 5 mg of octreotide per kg of body weight exhibits an average plasma level of from 3.5 to 6.5 ng/ml.
- 9. A microparticle according to claim 2 wherein the octreotide is in pamoate salt form.
- 10. A sustained release formulation comprising a microparticle of claim 9.
- 11. A microparticle according to claim 2 wherein the surface is substantially free of octreotide.
- 12. A sustained release formulation comprising a microparticle of claim 1.
- 13. A microparticle of claim 1 wherein said octreotide is an acetate salt.
Priority Claims (1)
Number |
Date |
Country |
Kind |
3974/90 |
Jun 1990 |
HUX |
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Parent Case Info
This is a continuation of application Ser. No. 07/643,880, filed Jan. 18, 1991, now U.S. Pat. No. 5,538,739, which in turn is a continuation-in-part of application Ser. No. 07/411,347, filed Sep. 22, 1989, which in turn is a continuation-in-part of application Ser. No. 07/377,023, filed Jul. 7, 1989, the latter two of which are now abandoned.
US Referenced Citations (7)
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EPX |
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Entry |
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Continuations (1)
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Number |
Date |
Country |
Parent |
643880 |
Jan 1991 |
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Continuation in Parts (2)
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Number |
Date |
Country |
Parent |
411347 |
Sep 1989 |
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Parent |
377023 |
Jul 1989 |
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