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EP0129435A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Ester of flurbiprofen and emulsion containing the same

Assignee: Kaken Pharmaceutical Co Ltd
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Filing: 1984-06-18
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Granted: —
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Expires: 2004-06-18
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Abstract

Abstract A pharmaceutical emulsion comprises a physiologically acceptable emulsifier and particles of a vegetable oil containing an ester of flurbiprofen having the formula wherein R is a group of the formula wherein R, is a hydrogen atom or a C 1 -C 3 alkyl group, R 2 is a C 1 -C 15 alkyl group ora C 2 -C 6 alkenyl group, and m is zero or an integer of 1; or a lactone group of the formula wherein R 3 and R. are same as or different from each other and are a hydrogen atom or a C,-C 3 alkyl group, and n is an integer of 1 or 2. The emulsion can be orally or parenterally administered to humans or animals for analgesia, antiphlogosis and antipyresis in various diseases and exhibits a high activity with small amounts in terms of flurbiprofen as compared with flurbiprofen itself.

Inventors

  • 👤 Yutaka Mizushima
  • 👤 Katsuhiro Uchida
  • 👤 Shozoh Masumoto
  • 👤 Masao Tohno
  • 👤 Yoshinobu Hashimoto
  • 👤 Kazumasa Yokoyama
  • 👤 Hiroyuki Okamoto
  • 👤 Kiichiro Nabeta
  • 👤 Tadakazu Suyama

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-26 19:43
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/335; A61K31/365; A61K31/21; A61K31/215; A61K9/00; A61K9/10; A61K9/107; A61K9/1075; A61P; A61P25/00; A61P25/04; A61P29/00

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 115 words
A pharmaceutical emulsion comprising a physiologically acceptable emulsifier and particles of a vegetable oil containing at least one ester of flurbiprofen of the formula wherein R is a group of the formula wherein R 1 is a hydrogen atom or a C 1 -C 3 alkyl group, R 2 is a C 1 -C 15 alkyl group or a C 2 -C 8 alkenyl group, and m is zero or 1; or a lactone group of the formula wherein R 3 and R 4 are same as or different from each other and are a hydrogen atom or a C l -C 3 alkyl group, and n is 1 or 2; and an aqueous medium.
Claim 2
Dependent Claim 115 words
A pharmaceutical emulsion comprising a physiologically acceptable emulsifier and particles of a vegetable oil containing at least one ester of flurbiprofen of the formula wherein R is a group of the formula wherein R 1 is a hydrogen atom or a C 1 -C 3 alkyl group, R 2 is a C 1 -C 15 alkyl group or a C 2 -C 8 alkenyl group, and m is zero or 1; or a lactone group of the formula wherein R 3 and R 4 are same as or different from each other and are a hydrogen atom or a C l -C 3 alkyl group, and n is 1 or 2; and an aqueous medium.
Claim 3
Dependent Claim 14 words
A pharmaceutical emulsion of Claim I wherein the physiologically acceptable emulsifier is a phospholipid.
Claim 4
Dependent Claim 14 words
A pharmaceutical emulsion of Claim 1 or 2, wherein the vegetable oil is-soybean oil.
Claim 5
Dependent Claim 29 words
A pharmaceutical emulsion of any preceding claim, which additionally contains, as an emulsifying adjuvant, a fatty acid having 6 to 22 carbon atoms or a physiologically acceptable salt thereof.
Claim 6
Dependent Claim 19 words
A pharmaceutical emulsion of any preceding claim, which additionally contains cholesterol, phosphatidic acid or mixture thereof as a stabilizer.
Claim 7
Dependent Claim 52 words
A pharmaceutical emulsion of any preceding claim, which additionally contains, as a stabilizer, an albumin, a dextran, a polyvinyl pyrrolidone, a polyalkylene glycol having a molecular weight of 1,000 to 10,000 a polyoxyethylene-polyoxypropylene copolymer having a molecular weight of 1,000 to 20,000, a hardened or unhardened caster oil-polyoxyalkylene ether, gelatin or hydroxyethylstarch.
Claim 8
Dependent Claim 17 words
A pharmaceutical emulsion of any preceding claim, which additionally contains glycerol and/or glucose as an isotonifying agent.
Claim 9
Dependent Claim 65 words
A pharmaceutical emulsion of claim 1, which comprises from 5 to 50% inclusive (w/v), based on the volume of the emulsion, of soybean oil, from 0.01 to 30% inclusive (w/v), based on the volume of the emulsion, of the ester of flurbiprofen, from 1 to 50 parts inclusive, by weight per 100 parts by weight of the soybean oil, of phospholipid, and an aqueous medium.
Claim 10
Dependent Claim 43 words
A pharmaceutical emulsion of Claim 8, further comprising 0.3% (w/v).or less of a fatty acid having 6 to 22 carbon atoms or a physiologically acceptable salt thereof and 0.1% (w/v) or less of a cholesterol or 0.5% (w/v) or less of phosphatidic acid.
Claim 11
Dependent Claim 25 words
A pharmaceutical emulsion of Claim 8 or 9, wherein the aqueous medium is of phosphate and/or citrate buffer solution having a pH of 6-8 inclusive.

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