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Pharmaceutical Compositions Containing Lipase Inhibitors

a technology of lipase inhibitors and pharmaceutical compositions, which is applied in the direction of drug compositions, biocides, metabolic disorders, etc., can solve the problems of increased local side effects, adverse effects, and increased lipase inhibitor concentrations in pharmaceutical compositions,

Inactive Publication Date: 2011-11-10
DE SMIDT PASSCHIER CHRISTIAAN +5
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The invention is a pharmaceutical composition that contains a lipase inhibitor, a surfactant, and a dispersant. The lipase inhibitor can be present in 1% to 50% of the composition, the dispersant can be present in 5% to 70%, and the surfactant can be present in 0.1% to 90%. The composition can also contain other excipients such as carbohydrates, antioxidants, co-solvents, thickening agents, preservatives, and lubricants. The technical effect of this invention is to provide a pharmaceutical composition that can help in the treatment of gastrointestinal and pancreatic lipase-related diseases."

Problems solved by technology

Lipase inhibitor compositions currently administered inhibit around 30% of fat absorption after consumption of a mixed meal; an increase of the lipase inhibitors concentration in the pharmaceutical composition does not increase its clinical efficacy while the intensity of local side effects increases.
Anal leakage of oil (oily spotting) is an adverse effect that is occasionally observed in patients treated with lipase inhibitors.

Method used

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  • Pharmaceutical Compositions Containing Lipase Inhibitors
  • Pharmaceutical Compositions Containing Lipase Inhibitors

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0061]150 mg of MCT (Medium Chain Triglycerides, fractionated coconut oil, Miglyol 812, Hüls AG; Neobee M-5, Stepan; Captex 355, Abitec) and 120 mg vitamin E polyethylene glycol 1000 succinate (TPGS, Eastman Chemicals) were weighed into a glass container and mixed by heating / stirring at 45° C. 30 mg orlistat were then dissolved in the so obtained clear liquid and stirred till homogeneity. 200 mg of finely milled effervescent vitamin C tablets were added under stirring and upon cooling to room temperature (25° C.), wherein the mixture solidified. The so obtained composition was filled into hydroxypropylmethylcellulose capsules.

[0062]Capsules containing 60 mg orlistat in the above composition were applied to human volunteers during a single meal test. Human subjects consumed a meal consisting of 130 g hamburger meat, 10 g butter and 100 g French fries (fried in peanut oil) and containing overall about 35 g fat. Stools were collected from day −1 (a day before eating the single meal) un...

example 2

[0063]A composition consisting of 180 mg Cremophor EL (polyethoxylated castor oil, BASF), 60 mg MCT, 60 mg orlistat and 200 mg of finely milled effervescent vitamin C tablets was obtained according to the preparation described in example 1. Hydroxypropylmethylcellulose capsules containing each 60 mg orlistat in the above composition were applied to human volunteers according to the method described in example 1.

example 3

[0064]A composition consisting of 450 mg Gelucire 44 / 14 (lauroyl macrogol-32 glycerides, Gattefossé, France), 90 mg MCT, 60 mg orlistat and 200 mg of finely milled effervescent vitamin C tablets was obtained according to the preparation described in example 1. Hydroxypropylmethylcellulose capsules containing each 60 mg of orlistat in the above composition were applied to human volunteers according to the method described in example 1.

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Abstract

A pharmaceutical composition comprises at least one inhibitor of lipases, preferably an inhibitor of gastrointestinal and pancreatic lipases, such as orlistat, at least one surfactant, and at least one dispersant.

Description

[0001]This application is a divisional of U.S. patent application Ser. No. 10 / 794,123, filed Mar. 5, 2004, now pending, which is a continuation of U.S. patent application Ser. No. 10 / 419,346, filed Apr. 21, 2003, now abandoned, which is a continuation of U.S. patent application Ser. No. 09 / 660,297, filed Sep. 13, 2000, now abandoned, which claims the benefit of European Patent Application 99118180.1, filed Sep. 13, 1999. The entire contents of the above-identified applications are hereby incorporated by reference.BACKGROUND OF THE INVENTION[0002]1. Field[0003]The present invention relates to pharmaceutical compositions comprising lipase inhibitors.[0004]2. Description[0005]Examples of lipase inhibitors include lipstatin and orlistat. The latter is also known as tetrahydrolipstatin or THL and is derived from a natural product excreted by Streptomyces toxytricini. This class of compounds was found to exhibit in vitro as well as in vivo activity against various lipases, such as lingual...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/337A61P3/04A61K9/10A61K9/00A61K9/107A61K9/48A61K31/365A61K45/08A61K47/10A61K47/12A61K47/14A61K47/20A61K47/22A61K47/24A61K47/26A61K47/32A61K47/34A61K47/36A61P3/06A61P43/00
CPCA61K9/0007A61K9/1075A61K31/365A61K9/4858A61K9/485A61P1/00A61P3/04A61P3/06A61P43/00A61K9/10
Inventor DE SMIDT, PASSCHIER CHRISTIAANHADVARY, PAULLENGSFELD, HANSRADES, THOMASSTEFFEN, HANSTARDIO, JOSEPH
Owner DE SMIDT PASSCHIER CHRISTIAAN