A formulation of octreotide or pharmaceutically acceptable salts thereof, which provides controlled release of a therapeutically effective amount of octreotide for a period of at least about two months. Methods of treating acromegaly, decreasing growth hormone, decreasing IGF-1, and treating conditions associated with carcinoid tumors and VIPomas by administering a controlled release formulation of octreotide are provided herein.
|US4131604||Nov 23, 1977||Dec 26, 1978||Thermo Electron Corporation||Polyurethane elastomer for heart assist devices|
|US4285987||Nov 1, 1979||Aug 25, 1981||Alza Corporation||Process for manufacturing device with dispersion zone|
|US4386039||Feb 27, 1981||May 31, 1983||Thermo Electron Corporation||Process for forming an optically clear polyurethane lens or cornea|
|US4523005||Apr 17, 1984||Jun 11, 1985||Thermedics, Inc.||Extrudable polyurethane for prosthetic devices prepared from a diisocyanate, a polytetramethylene ether polyol, and 1,4-butane diol|
|US4743673||Dec 19, 1986||May 10, 1988||Tyndale Plains-Hunter, Ltd.||Hydrophilic carboxy polyurethanes|
|US4751133||May 11, 1987||Jun 14, 1988||Thermedics, Inc.||Medical patches and processes for producing same|
|US4954587||May 23, 1989||Sep 4, 1990||Ciba-Geigy Corporation||Dimethylacrylamide-copolymer hydrogels with high oxygen permeability|
|US4959217||May 22, 1986||Sep 25, 1990||Syntex (U.S.A.) Inc.||Delayed/sustained release of macromolecules|
|US5254662||May 18, 1992||Oct 19, 1993||PolyMedia Industries, Inc.||Biostable polyurethane products|
|US5266325||Dec 3, 1990||Nov 30, 1993||Hydro Med Science Division of National Patent Development Corp.||Preparation of homogeneous hydrogel copolymers|
|US5273752||Sep 19, 1991||Dec 28, 1993||Alza Corporation||Controlled release dispenser comprising beneficial agent|
|US5292515||Mar 31, 1993||Mar 8, 1994||Hydro Med Sciences, a Division of National Patent Development Corporation||Manufacture of water-swellable hydrophilic articles and drug delivery devices|
|US5342622||Oct 31, 1990||Aug 30, 1994||The State of Victoria|
Victorian College of Pharmacy Ltd.
Monash Medical Centre
|Subdermal biocompatible implants|
|US5354835||Jul 23, 1993||Oct 11, 1994||Saudi Basic Industries Corporation||Desalination process|
|US5431921||Mar 12, 1993||Jul 11, 1995||Pfizer Inc||Dispensing device containing a hydrophobic medium|
|US5464933||Jun 7, 1993||Nov 7, 1995||Duke University||Synthetic peptide inhibitors of HIV transmission|
|US5468811||Aug 24, 1994||Nov 21, 1995||National Patent Development Corporation||Hydrophilic composite polymer articles formed from a settable paste comprising a mixture of hydrophilic polymer and unsaturated monomer|
|US5614223||Jul 17, 1995||Mar 25, 1997||Digestive Care Inc.||Intraoral medicament-releasing device|
|US5637309||Sep 20, 1994||Jun 10, 1997||Shiseido Company, Ltd.||Physiologically active substance-prolonged releasing-type pharmaceutical preparation|
|US5686411||May 23, 1995||Nov 11, 1997||Amylin Pharmaceuticals, Inc.||Amylin agonist peptides and uses therefor|
|US5756127||Oct 29, 1996||May 26, 1998||Wright Medical Technology, Inc.||Implantable bioresorbable string of calcium sulfate beads|
|US5817343||May 14, 1996||Oct 6, 1998||Alkermes, Inc.||Method for fabricating polymer-based controlled-release devices|
|US5854127||Mar 13, 1997||Dec 29, 1998||Micron Technology, Inc.||Method of forming a contact landing pad|
|US5876761||Jun 6, 1995||Mar 2, 1999||Novartis AG||Sustained release formulations of water soluble peptides|
|US5894458||Sep 12, 1996||Apr 13, 1999||Nippon Chemi-Con Corporation||Apparatus for supporting and connecting a magnetic field modulation head to be used for a photomagnetic recording including a spring plate member having a conductive part electrically connecting the head to a supporting frame|
|US6087334||Aug 21, 1998||Jul 11, 2000||Amylin Pharmaceuticals, Inc.||Anti-diabetic peptides|
|US6143718||Jun 7, 1995||Nov 7, 2000||Amylin Pharmaceuticals, Inc.||Treatment of Type II diabetes mellutis with amylin agonists|
|US6159490||Apr 5, 2000||Dec 12, 2000||Implants containing bioactive peptides|
|US6313254||May 17, 1999||Nov 6, 2001||Cardiac CRC Nominees PTY LTD||Polysiloxane-containing polyurethane elastomeric compositions|
|US6337318||Feb 19, 1999||Jan 8, 2002||Peptech, Ltd.||Sustained GnRH peptide-release formulation|
|US6361797||Dec 7, 2000||Mar 26, 2002||Hydro Med Sciences, Inc.||Hydrogel compositions useful for the sustained release of macromolecules and methods of making same|
|US6417164||Nov 6, 2000||Jul 9, 2002||Amylin Pharmaceuticals, Inc.||Treatment of type II diabetes mellitus with amylin agonists|
|US6579851||Mar 14, 2001||Jun 17, 2003||Amylin Pharmaceuticals, Inc.||Effects of glucagon-like peptide-1 (7-36) on antro-pyloro-duodenal motility|
|US6602694||Jun 27, 2001||Aug 5, 2003||Amylin Pharmaceuticals, Inc||Uncoupling protein 4 (UCP-4)|
|US6770623||May 31, 2000||Aug 3, 2004||Eli Lilly and Company||Stabilized teriparatide solutions|
|US6872700||Jan 14, 2000||Mar 29, 2005||Amylin Pharmaceuticals, Inc.||Methods for glucagon suppression|
|US6942264||Feb 10, 2003||Sep 13, 2005||Disposable pet waste receptacle|
|US6969480||Feb 13, 2003||Nov 29, 2005||matRegen Corp.||Method of producing structures using centrifugal forces|
|US7008927||May 29, 2001||Mar 7, 2006||Kaken Pharmaceutical Co., Ltd.||Pralmorelin-containing nasal drop preparations|
|US7056887||Dec 18, 2002||Jun 6, 2006||Amylin Pharmaceuticals, Inc.||Treatment of acute coronary syndrome with GLP-1|
|US7101853||May 6, 1997||Sep 5, 2006||Amylin Pharmaceuticals, Inc.||Method for treating or preventing gastritis using amylin or amylin agonists|
|US7105489||Dec 11, 2002||Sep 12, 2006||Amylin Pharmaceuticals, Inc.||Methods and compositions for treating polycystic ovary syndrome|
|US7115569||Oct 15, 2004||Oct 3, 2006||Amylin Pharmaceuticals, Inc.||Exendins, exendin agonists, and methods for their use|
|US7118737||Jul 12, 2001||Oct 10, 2006||Amylin Pharmaceuticals, Inc.||Polymer-modified synthetic proteins|
|US7153825||Mar 18, 2005||Dec 26, 2006||Amylin Pharmaceuticals, Inc.||Methods for glucagon suppression using modified exendins|
|US7220721||Nov 13, 1998||May 22, 2007||Amylin Pharmaceuticals, Inc.||Exendin agonist peptides|
|US7259136||Mar 5, 2002||Aug 21, 2007||Amylin Pharmaceuticals, Inc.||Compositions and methods for treating peripheral vascular disease|
|US7271238||Aug 26, 2003||Sep 18, 2007||Amylin Pharmaceuticals, Inc.||Amylin agonist peptides and uses therefor|
|US7452868||Mar 10, 2006||Nov 18, 2008||Indevus Pharmaceuticals, Inc.||Controlled release formulations of octreotide|
|US20020141985||Dec 14, 2001||Amylin Parmaceuticals, Inc.||Peptide YY and peptide YY agonists for treatment of metabolic disorders|
|US20030036504||Jan 9, 2001||Amylin Pharmaceuticals, Inc.||Use of exendins and agonists thereof for modulation of triglyceride levels and treatment of dyslipidemia|
|US20040002454||Dec 18, 2002||Amylin Pharmaceuticals, Inc.||Treatment of acute coronary syndrome with GLP-1|
|US20050037078||Aug 10, 2004||Valera Pharmaceuticals||Long term drug delivery devices with polyurethane based polymers and their manufacture|
|US20050287320||Aug 18, 2005||matRegen Corp.||Method of producing structures using centrifugal forces|
|US20060019903||Jun 17, 2005||Compositions and methods for treating precocious puberty|
|US20060030528||Aug 5, 2005||Amylin Pharmaceuticals, Inc.||Compositions and methods for treating peripheral vascular disease|
|US20060035836||Oct 20, 2005||Amylin Pharmaceuticals, Inc.||Treatment of acute coronary syndrome with an exendin|
|US20060067911||Apr 22, 2005||MEDERIO AG||Metered medication dose|
|US20060122106||Jun 13, 2003||Prevention and/or treatment of inflammatory bowel disease using pyy or agonists thereof|
|US20060148713||Mar 3, 2006||Amylin Pharmaceuticals, Inc.||Use of exendins and agonists thereof for the reduction of food intake|
|US20060204540||Mar 10, 2006||Controlled release formulations of octreotide|
|US20060233747||Jun 5, 2006||Amylin Pharmaceuticals, Inc.||Polymer-modified synthetic proteins|
|US20060293232||Aug 17, 2005||Amylin Pharmaceuticals, Inc.||Hybrid polypeptides with selectable properties|
|US20070010656||Aug 28, 2006||Amylin Pharmaceuticals, Inc.||Novel exendin agonist compounds|
|US20080311170||Apr 25, 2008||IMPLANT DEVICE RELEASE AGENTS AND METHODS OF USING SAME|
|US20090035343||Jul 11, 2008||DELIVERY OF DRY FORMULATIONS OF OCTREOTIDE|
1. A method of treating a patient suffering from one or more symptoms associated with carcinoid tumors, said method comprising:
- implanting subcutaneously into a patient in need thereof at least one implant comprising a hydrogel and a pharmaceutical formulation comprising octreotide;
- wherein said pharmaceutical formulation is contained within said hydrogel, which hydrogel comprises a copolymer obtained from the copolymerization of a mixture comprising at least two hydrophilic, ethylenically unsaturated monomers;
- wherein said pharmaceutical formulation contains between about 20 to about 150 milligrams of octreotide, in free form or salt form;
- wherein said pharmaceutical formulation further comprises hydroxypropylcellulose; and
- wherein said at least one implant releases a therapeutically effective amount of said octreotide to said patient over a period of at least about two months.
2. The method of claim 1, wherein said effective amount of said octreotide provides an in vivo average Css in said patient of about 0.1 ng/ml to about 9 ng/ml of octreotide.
3. The method of claim 1, wherein said pharmaceutical formulation contains from about 40 to about 90 milligrams of octreotide.
4. The method of claim 1, wherein said octreotide is octreotide acetate.
5. The method of claim 4, wherein said pharmaceutical formulation contains about 50 milligrams of said octreotide acetate.
6. The method of claim 4, wherein said pharmaceutical formulation contains about 80 milligrams of said octreotide acetate.
7. The method of claim 2, wherein said effective amount of said octreotide provides an in vivo average Css in said patient of about 1 ng/ml to about 2 ng/ml of octreotide.
8. The method of claim 1, wherein said at least one implant releases a therapeutically effective amount of octreotide over a period of about two months to about two years.
9. The method of claim 1, wherein said at least one implant releases a therapeutically effective amount of said octreotide over about six months.
10. The method of claim 1, wherein said at least two hydrophilic, ethylenically unsaturated monomers are 2-hydroxyethyl methacrylate and hydroxypropyl methacrylate.
11. The method of claim 1, wherein said copolymer comprises about 20% of 2-hydroxyethyl methacrylate and about 80% hydroxypropylmethacrylate.
12. The method of claim 1, wherein the pharmaceutical formulation contains about 0.5 to 20% w/w of the hydroxypropylcellulose.
13. The method of claim 1, wherein said pharmaceutical formulation further comprises magnesium stearate.
14. The method of claim 13, wherein the pharmaceutical formulation contains about 0.5 to 5% w/w of the magnesium stearate.
15. The method of claim 1, wherein said at least one implant releases said octreotide at a rate of about 10 ug to about 1000 ug per day over a period of about six months.
16. The method of claim 1, wherein said at least one implant is two or more implants.
17. The method of claim 1, wherein said at least one implant releases said octreotide at a rate of about 30 μg to about 250 μg per day in vitro.
18. The method of claim 1, wherein the at least one implant is implanted in a dry state.
19. The method of claim 1, wherein the at least one implant is implanted in a hydrated state.
20. The method of claim 1, wherein said copolymer comprises about 40% of 2-hydroxyethyl methacrylate and about 60% hydroxypropylmethacrylate.