US5039660A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Partially fused peptide pellet
Assignee: ENDOCON Inc A MD CORP
•
Filing: 1988-03-02
•
Granted: 1991-08-13
•
Expires: 2008-03-02
Abstract
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.
Inventors
- 👤 Robert J. Leonard
- 👤 S. Mitchell Harman
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 21:06
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K9/0024; A61K9/14; A61K9/16; A61K9/1605; A61K9/1617
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
52 words
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.
Claim 2
Dependent Claim
52 words
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.
Claim 3
Dependent Claim
17 words
A pellet as claimed in claim 1 wherein the carrier is a steroid or a steroid derivative.
Claim 4
Dependent Claim
16 words
A pellet as claimed in claim 2 wherein the carrier is cholesterol of a cholesterol derivative.
Claim 5
Dependent Claim
23 words
A pellet as claimed in claim 1 wherein the carrier is selected from the group consisting of cholesterol, cholesterol acetate and cholesterol chloride.
Claim 6
Dependent Claim
63 words
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-α, estradiol 17β, estriol, estrane, estrone, hydrocortisone, lanosterol, lithocholic acid, mestranol, β-methasone, norethindrone, piednisolone, pregnane, pregnenolone, progesterone, spironolactone, testosterone, triamcinolone and their derivatives.
Claim 7
Dependent Claim
109 words
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.
Claim 8
Dependent Claim
109 words
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.
Claim 9
Dependent Claim
110 words
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.
Claim 10
Dependent Claim
110 words
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.
Claim 11
Dependent Claim
21 words
A pellet as claimed in claim 1 wherein said carrier is cholesterol acetate and said peptide drug is growth hormone-releasing hormone.
Claim 12
Independent Claim
32 words
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.
Claim 13
Independent Claim
32 words
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.
Claim 14
Independent Claim
53 words
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.
Claim 15
Independent Claim
53 words
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.
Claim 16
Dependent Claim
56 words
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.
Claim 17
Dependent Claim
56 words
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.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1994-08-12 | 1995-02-11 | 1995-08-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-08-12 | 1999-02-11 | 1999-08-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-08-12 | 2003-02-11 | 2003-08-13 | $7700.00 | Window Closed / Lapsed |