Title:
LOCAL-ANESTHETIC LONG-LASTING SUSTAINED-RELEASE LIPOSOME PREPARATION
Document Type and Number:
WIPO Patent Application WO/2014/046191
Kind Code:
A1
Abstract:
Provided is a local-anesthetic long-lasting sustained-release liposome preparation which is capable of maintaining effective drug concentration over a long period of time in a local affected area and has excellent long-lasting pain-relieving effect. The local-anesthetic long-lasting sustained-release liposome preparation is manufactured by encapsulating a local anesthetic in an aqueous phase in an internal region using remote loading in a liposome composition, which is obtained by mixing a first aqueous-phase solution in a volume ratio of 3/1 to 12/1 with respect to a volume 1 of a water-miscible organic solution in which phospholipid and cholesterol are contained in a total concentration of 100 to 200 w/v%, obtaining an emulsion in which the total concentration of the phospholipid and cholesterol in a mixed phase is 15 to 50 w/v%, and subjecting the emulsion to external solution exchange with a second aqueous phase solution, wherein an ion gradient is formed in the liposome composition, between the aqueous phase in an internal region of a liposome membrane composed of the first aqueous phase solution and an aqueous phase in an external region of the liposome membrane composed of the second aqueous phase solution.
Inventors:
YAMASHITA KEIKO (JP)
KUROSAKI YASUO (JP)
HARUMOTO MAKOTO (JP)
SHIMAMURA KYOKO (JP)
KAIBORI MASAKI (JP)
ARAKI YOSHIRO (JP)
KON MASANORI (JP)
ITO SEIJI (JP)
KUROSAKI YASUO (JP)
HARUMOTO MAKOTO (JP)
SHIMAMURA KYOKO (JP)
KAIBORI MASAKI (JP)
ARAKI YOSHIRO (JP)
KON MASANORI (JP)
ITO SEIJI (JP)
Application Number:
PCT/JP2013/075323
Publication Date:
March 27, 2014
Filing Date:
September 19, 2013
Export Citation:
Assignee:
TERUMO CORP (JP)
KANSAI MEDICAL UNIVERSITY EDUCATIONAL CORP (JP)
KANSAI MEDICAL UNIVERSITY EDUCATIONAL CORP (JP)
International Classes:
A61K47/44; A61K9/127; A61K31/167; A61K31/445; A61K47/28; A61P23/02
Domestic Patent References:
| WO2012091054A1 | 2012-07-05 | |||
| WO2012133121A1 | 2012-10-04 | |||
| WO2001000173A1 | 2001-01-04 |
Foreign References:
| JP2009513621A | 2009-04-02 | |||
| JP2002522470A | 2002-07-23 |
Other References:
GRANT, G.J. ET AL.: "A novel liposomal bupivacaine formulation to produce ultralong- acting analgesia", ANESTHESIOLOGY, vol. 101, no. 1, 2004, pages 133 - 137
Attorney, Agent or Firm:
WATANABE Mochitoshi et al. (JP)
Mochitoshi Watanabe (JP)
Mochitoshi Watanabe (JP)
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