Title:
LONG-ACTING INJECTABLE FORMULATIONS AND CRYSTALLINE FORMS OF BUPRENORPHINE DERIVATIVES
Document Type and Number:
WIPO Patent Application WO/2019/214726
Kind Code:
A1
Abstract:
This disclosure relates to crystalline forms of 3-acyl-buprenorphine derivatives and sustained release injectable pharmaceutical compositions for treatment of opioid dependence, pain or depression, including an aqueous suspension of crystalline 3-acyl-buprenoprhine, or a pharmaceutically acceptable salt thereof, wherein the composition does not include an organic solvent, a polylactide polymer, a polyglycolide polymer, or a copolymer of polylactide and polyglycolide. This disclosure also includes 3-acyl-buprenoprhine or a pharmaceutically acceptable salt thereof prepared in a controlled release matrix, including poly (lactide-co-glycolide), sucrose acetoisobutyrate, lecithin, diolein and a combination of two or more thereof.
Inventors:
LIN TONG-HO (CN)
WEN YUNG-SHUN (CN)
LIANG JUI-WEI (CN)
WEN YUNG-SHUN (CN)
LIANG JUI-WEI (CN)
Application Number:
PCT/CN2019/086449
Publication Date:
November 14, 2019
Filing Date:
May 10, 2019
Export Citation:
Assignee:
ALAR PHARMACEUTICALS INC (CN)
International Classes:
C07D489/12; A61K31/485; A61P1/10; A61P25/30; A61P29/00
Domestic Patent References:
| WO2016142877A1 | 2016-09-15 |
Other References:
AUDRA L. ET AL.: "A solubility and related physicochemical property composition of burenorphine and its 3-alkyl esters", PHARMACEUTICAL RESEARCH, vol. 12, no. 10, 31 December 1995 (1995-12-31), pages 1526 - 1529, XP008016370, DOI: 10.1023/A:1016299824162
HIROFUMI IMOTO ET AL.: "Transdermal Prodrug concepts:permeation of burenorphine and its alkyl esters through hairless mouse skin and influence of vehicles", BIOL. PHARM. BULL., vol. 19, no. 2, 31 December 1996 (1996-12-31), pages 263 - 267, XP008060357
AUDRA L. STINCHCOMB ET AL.: "Permeation of burenorphine and its 3-alkyl-esters prodrugs through human skin", PHARMACEUTICAL RESEARCH, vol. 13, no. 10, 31 December 1996 (1996-12-31), pages 1519 - 1523, XP008016388, DOI: 10.1023/A:1016079513007
See also references of EP 3790881A4
HIROFUMI IMOTO ET AL.: "Transdermal Prodrug concepts:permeation of burenorphine and its alkyl esters through hairless mouse skin and influence of vehicles", BIOL. PHARM. BULL., vol. 19, no. 2, 31 December 1996 (1996-12-31), pages 263 - 267, XP008060357
AUDRA L. STINCHCOMB ET AL.: "Permeation of burenorphine and its 3-alkyl-esters prodrugs through human skin", PHARMACEUTICAL RESEARCH, vol. 13, no. 10, 31 December 1996 (1996-12-31), pages 1519 - 1523, XP008016388, DOI: 10.1023/A:1016079513007
See also references of EP 3790881A4
Attorney, Agent or Firm:
GE CHENG & CO., LTD. (CN)
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