Claims for Patent: 8,865,220

Summary for Patent: 8,865,220

Title:	Method for controlled release of parathyroid hormone from encapsulated poly(lactic-glycolic)acid microspheres
Abstract:	The present invention provides a method for producing a controlled release microsphere with mean average size greater than 50 .mu.m, comprising preparing a water-in-oil (w/o) emulsion comprising an inner aqueous layer containing a pharmaceutically effective amount of a biologically active polypeptide with activity similar to parathyroid hormone, and an oil layer containing a polymer substance of poly(lactic-co-glycolic acid) (PLGA), then adding the w/o emulsion into aqueous polyvinyl alcohol (PVA) solution to form a water-in-oil-in-water (w/o/w) double emulsion and then desorbing the solvent in the oil layer. The present invention also provides a controlled release microsphere prepared by the method and use thereof.
Inventor(s):	Ho; Mei-Ling (Kaohsiung, TW), Wang; Gwo-Jaw (Taipei, TW), Chang; Je-Ken (Kaohsiung, TW), Fu; Yin-Chih (Kaohsiung, TW), Tzeng; Cherng-Chyi (Kaohsiung, TW), Rajalakshmanan; Eswaramoorthy (Kaohsiung, TW)
Assignee:	Kaohsiung Medical University (Kaohsiung, TW)
Application Number:	12/814,955
Patent Claims:	1. A method for controlled release delivery of biologically active polypeptide with activity similar to parathyroid hormone to a subject suffering from osteoarthritis in effective therapeutic concentration comprising: administrating to the subject a controlled release microsphere with mean average size greater than 50 .mu.m, which is produced by preparing a water-in-oil (w/o) emulsion comprising an inner aqueous layer containing the biologically active polypeptide, and an oil layer containing a polymer substance of poly(lactic-co-glycolic acid) (PLGA), then gradually adding the w/o emulsion into aqueous polyvinyl alcohol (PVA) solution to form a water-in-oil-in-water (w/o/w) double emulsion and then desorbing the solvent in the oil layer, whereby the polypeptide is released in the effective therapeutic concentration ranging from about 1.times.10.sup.-7 M to about 5.times.10.sup.-9 M for at least 18 days. 2. The method of claim 1, wherein the biologically active polypeptide with activity similar to parathyroid hormone is SEQ ID NO: 2. 3. The method of claim 1, wherein the poly(lactic-co-glycolic acid) (PLGA) is PLGA(50:50) or PLGA (65:35). 4. The method of claim 1, wherein the polypeptide is stabilized in a stock solution comprising hydrochloric acid and bovine serum albumin. 5. The method of claim 4, wherein concentration of the hydrochloric acid is from about 1 mM to about 8 mM, concentration of the bovine serum albumin is from about 0.01% to about 5%. 6. The method of claim 1, wherein weight percentage of the aqueous PVA solution is from about 0.1% to about 5%. 7. The method of claim 1, wherein encapsulation rate of the biologically active polypeptide is not lower than about 60%. 8. The method of claim 1, wherein the subject is human.

Details for Patent 8,865,220

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Nps Pharmaceuticals, Inc.	NATPARA	parathyroid hormone	For Injection	125511	01/23/2015		2039-03-29