Claims for Patent: 5,039,660

Summary for Patent: 5,039,660

Title:	Partially fused peptide pellet
Abstract:	A bioerodible pellet capable of administering an even and continuous dose of a peptide over a period of up to a year, when subcutaneously implanted, is provided. The bioerodible implant is a partially-fused pellet, which pellet has a peptide drug homogeneously-bound in a matrix of a melted and recrystallized, nonpolymer carrier. Preferably, the nonpolymer carrier is a steroid and in particular is cholesterol or a cholesterol derivative. In one embodiment, the peptide drug is growth hormone-releasing hormone. A method for making the bioerodible pellet also is provided.
Inventor(s):	Leonard; Robert J. (Lynnfield, MA), Harman; S. Mitchell (Ellicott City, MD)
Assignee:	Endocon, Inc. (South Walpole, MA)
Application Number:	07/163,328
Patent Claims:	1. A pellet capable of sustained release of a peptide when implanted in the body comprising a peptide drug homogeneously bound in a matrix of a melted and recrystallized, nonpolymer carrier, said peptide drug having a higher melting temperature than said nonpolymer carrier and said nonpolymer carrier being bioerodible, highly crystalline and lipophilic. 2. A pellet as claimed in claim 1 wherein the carrier is a steroid or a steroid derivative. 3. A pellet as claimed in claim 2 wherein the carrier is cholesterol of a cholesterol derivative. 4. A pellet as claimed in claim 1 wherein the carrier is selected from the group consisting of cholesterol, cholesterol acetate and cholesterol chloride. 5. A pellet as claimed in claim 1 wherein the carrier includes a steroid selected from the group consisting of aldosterone, androstane, androstene, androstenedione, androsterone, cholecalciferol, cholestane, cholic acid, corticosterone, cortisol, cortisol acetate, cortisone, cortisone acetate, deoxycorticosterone, digitoxigenin, ergocalciferol, ergosterol, estradiol, 17-.alpha., estradiol 17.beta., estriol, estrane, estrone, hydrocortisone, lanosterol, lithocholic acid, mestranol, .beta.-methasone, norethindrone, piednisolone, pregnane, pregnenolone, progesterone, spironolactone, testosterone, triamcinolone and their derivatives. 6. A pellet as claimed in claim 2 wherein the peptide is selected from the group consisting of growth hormone and growth hormone-releasing hormone, gonadotropin releasing hormone, and its agonist and antagonist analogues, somatostatin and its analogues, gonadotropins such as luteinizing hormone and follicle stimulating hormone, peptide-T, thyrocalcitonin, parathyroid hormone, glucagon, vasopressin, oxytocin, alpha and beta melanocyte stimulating hormones, peptide molecules which stimulate erythrocyte, leucocyte and immunocyte growth and function such as colony stimulating factors (CFS 1 and 2), erythropoietin and lymphokines (including interleukin I and II), angiotensin I and II, bradykinin, kallidin, adrenocorticotropic hormone, thyroid stimulating hormone, insulin, glucagon and the numerous analogues and congeners of the foregoing peptides. 7. A pellet as claimed in claim 3 wherein the peptide is selected from the group consisting of growth hormone factors, growth hormone and growth hormone-releasing hormone gonadotropin-releasing hormone, and its agonist and antagonist analogues, somatostatin and its analogues, gonadotropins such as luteinizing hormone and follicle-stimulating hormone, peptide-T, thyrocalcitonin, parathyroid hormone, glucagon, vasopressin, oxytocin, alpha and beta melanocyte-stimulating hormones, peptide molecules which stimulate erythrocyte, leucocyte and immunocyte growth and function such as colony stimulating factors (CFS 1 and 2), erythropoietin and lymphokines (including interleukin I and II), angiotensin I and II, bradykinin, kallidin, adrenocorticotropic hormone, thyroid stimulating hormone, insulin, glucagon and the numerous analogues and congeners of the foregoing peptides. 8. A pellet as claimed in claim 4 wherein the peptide is selected from the group consisting of growth hormone factors, growth hormone and growth hormone-releasing hormone, gonadotropin-releasing hormone, and its agonist and antagonist analogues, somatostatin and its analogues, gonadotropins such as luteinizing hormone and follicle-stimulating hormone, peptide-T, thyrocalcitonin, parathyroid hormone, glucagon, vasopressin, oxytocin, alpha and beta melanocyte stimulating hormones, peptide molecules which stimulate erythrocyte, leucocyte and immunocyte growth and function such as colony stimulating factors (CFS 1 and 2), erythropoietin and lymphokines (including interleukin I and II), angiotensin I and II, bradykinin, kallidin, adrenocorticotropic hormone, thyroid stimulating hormone, insulin, glucagon and the numerous analogues and congeners of the foregoing peptides. 9. A pellet as claimed in claim 5 wherein the peptide is selected from the group consisting of growth hormone factors, growth hormone and growth hormone-releasing hormone, gonadotropin-releasing hormone, and its agonist and antagonist analogues, somatostatin and its analogues, gonadotropins such as luteinizing hormone and follicle-stimulating hormone, peptide T, thyrocalcitonin, parathyroid hormone, glucagon, vasopressin, oxytocin, alpha and beta melanocyte-stimulating hormones, peptide molecules which stimulate erythrocyte, leucocyte and immunocyte growth and function such as colony stimulating factors (CFS 1 and 2), erythropoietin and lymphokines (including interleukin I and II), angiotensin I and II, bradykinin, kallidin, adrenocorticotropic hormone, thyroid stimulating hormone, insulin, glucagon and the numerous analogues and congeners of the foregoing peptides. 10. A pellet as claimed in claim 1 wherein said carrier is cholesterol acetate and said peptide drug is growth hormone-releasing hormone. 11. A method for delivering a peptide to the body comprising, implanting in the body a partially-fused pellet containing a peptide drug bound in a matrix of a melted and recrystallized, non-polymer carrier. 12. A method for delivering a peptide to a body comprising, implanting into the body a pellet of a peptide drug homogeneously bound in a matrix of melted and recrystallized, non-polymer carrier, said peptide drug having a higher melting temperature than said non-polymer carrier and said non-polymer carrier being bioerodible, highly crystalline and lipophilic. 13. A partially-fused pellet capable of sustained release of a peptide when implanted in the body, comprising a substantially non-melted peptide drug homogeneously bound in a matrix of a substantially melted and recrystallized non-polymer carrier, said peptide drug having a higher melting temperature than said non-polymer carrier and said non-polymer carrier being bioerodible, highly crystalline and lipophilic.

Details for Patent 5,039,660

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Nps Pharmaceuticals, Inc.	NATPARA	parathyroid hormone	For Injection	125511	01/23/2015		2039-02-26