Drug – bio-affecting and body treating compositions – Designated organic nonactive ingredient containing other... – Aftertreated solid synthetic organic polymer
Patent
1997-04-14
1998-05-26
Kunz, Gary L.
Drug, bio-affecting and body treating compositions
Designated organic nonactive ingredient containing other...
Aftertreated solid synthetic organic polymer
514781, 514784, A61K 908, A61K 4736
Patent
active
057565520
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a lyophilized pharmaceutical preparation which can provide an aqueous drug composition having property of reversible thermosetting gelation when reconstituted with a solvent for reconstitution. The aqueous drug composition having property of reversible thermosetting gelation reconstituted from the lyophilized pharmaceutical preparation is characterized in that the aqueous drug composition is a fluid liquid at room temperature or lower and, when administered to eyes or body cavities or spreaded on skin, gelation happens at body temperature of mammal, so as to achieve a greater degree of bioavailability of the pharmacologically effective component and maintain the effect of the drugs for long period.
BACKGROUND ART
The pharmaceutical preparation having property of reversible thermosetting gelation which causes a sol-gel transition at the drug-administered site exhibits various advantages such as improvement in the drug delivery and patient's compliance as compared with the conventional pharmaceutical preparations.
Hitherto, there have been proposed several aqueous drug compositions which are liquid at room temperature or lower and form a semi-solid or gel at body temperature of mammal, as aqueous drug compositions which effectively release a pharmacologically effective component to mammal to be treated. U.S. Pat. No. 4,188,373 discloses an aqueous composition having property of thermosetting gelation, which comprises PLURONIC (trademark) and form gel by application of heat, and a desired sol-gel transition temperature thereof is obtained by controlling the concentration of PLURONIC. Moreover, U.S. Pat. Nos. 4,474,751, 4,474,752, 4,474,753 and 4,478,822 disclose drug delivery systems utilizing aqueous drug compositions having property of thermosetting gelation.
The inventors of this invention already provided a drug composition having property of reversible thermosetting gelation for treating eyes, body cavities and skin which comprises an effective amount of a drug used for pharmacological therapy or diagnosis, methylcellulose, citric acid and polyethylene glycol and whose pH ranges from 3 to 10, wherein the composition is a highly fluid liquid prior to administration or application and undergoes gelation immediately after administration or application thereof due to the temperature of the site to which the composition is administered or spreaded (PCT/JP93/01636).
However, it is difficult to store the foregoing aqueous composition over a long time period, since in case where an drug unstable to water is applied to the composition, the drug undergo decomposition, although the composition exhibits satisfactory effects such as enhancement of the bioavailability of the drug and the long acting drug efficacy.
Accordingly, an object of the present invention is to provide an aqueous drug composition having property of reversible thermosetting gelation which can be applied to drugs unstable to water, as well.
DISCLOSURE OF INVENTION
The present inventors have diligently conducted many researches in order to develop an aqueous drug composition which can be applied to drugs unstable to water as well and, as a result, have found out that a drug can be formed into a pharmaceutical preparation by incorporating, into the drug, appropriate amounts of methylcellulose, citric acid and polyethylene glycol and then lyophilizing the resulting mixture, even if the drug is unstable to water and thus have completed the present invention.
That is, the present invention provides a lyophilized pharmaceutical preparation which is prepared by lyophilizing an aqueous composition having property of reversible thermosetting gelation comprising an effective amount of a drug used for pharmacological therapy or surgical operations, 0.2 to 2.1 (W/V)% of methylcellulose (the content of methoxyl group is within the range of 26 to 33%), 1.2 to 2.3 (W/V)% of citric acid and 0.5 to 13 (W/V)% of polyethylene glycol (PEG) (wherein (W/v)% means weight/volume %).
One of the excellent advantageous
REFERENCES:
patent: 5624962 (1997-04-01), Takeuchi et al.
Maeda Makoto
Maruyama Hiroki
Naito Keiko
Oguma Touru
Sasaki Miyako
Kunz Gary L.
Wakamoto Pharmaceutical Co., Ltd.
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