Orlistat compositions

Inactive Publication Date: 2005-06-23
BARBIER PIERRE +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0012] A method of treating obesity in an obese patient is also provided. This method comprises administering to a patient in need of such treatment (a) a therapeutically effective amount of a lipase inhibitor and (b) a pharmaceutically acceptable bile acid sequestrant in an amount effective to reduce gastrointestinal side effects associated with the lipase inhibitor. The lipase inhibitor and bile acid sequestrant can

Problems solved by technology

However, in a subgroup of the patients, unpleasant gastrointestinal side effects such as oily spo

Method used

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  • Orlistat compositions
  • Orlistat compositions
  • Orlistat compositions

Examples

Experimental program
Comparison scheme
Effect test

Example

Example 1

Study A

[0067] Xenical was ingested t.i.d. by two middle aged healthy male volunteers on a normal average mixed diet. Both individuals frequently experienced one or more of the above mentioned unpleasant gastrointestinal side effects. After 4 weeks on Xenical they started to ingest in addition to Xenical b.i.d. cholestyramine containing sachets (4 g / meal) which were emptied into about 100 ml water, swirled and drunk during the meals. The side effects were immediately reduced in frequency and completely disappeared. After 2-4 weeks of combined intake together with Xenical, cholestyramine was discontinued. When treatment with Xenical alone was carried on the gastrointestinal adverse events reappeared.

Example

Example 2

Study B

[0068] The anti-GI side effect potential of bile salt sequestrants was extended further in short-term studies in human volunteers. To precipitate the tendency for side effects in this model three meals (lunch, dinner, breakfast) are ingested together with Xenical and 120 mg orlistat in 10 g butter, each. The model is based on the idea that GI side effects following orlistat ingestion are precipitated by the formation of free oil. Free oil is oil, which will coalesce in the dietary fat emulsion passing down the GI tract and separate from the stool matrix. In this model the amount of oil which is separated from the stool matrix is determined after the production of stools.

[0069] It was demonstrated in human volunteers that after co-administration of cholestyramine and colestipol, respectively, the formation of free oil was dramatically reduced (cholestyramine: 44% of the respective control experiment without addition of cholestyramine) or nearly completely suppresse...

Example

Example 3

Orlistat Pharmaceutical Compositions

[0070]A)IngredientQuantity mg / Capsuleorlistat120.00microcrystalline cellulose (AVICEL PH-101)93.60sodium starch glycolate (PRIMOJEL)7.20sodium lauryl sulfate7.20polyvinylpyrrolidone (Povidone (K-30))12.00purified Water*—talc0.24Total240.24mg

*Removed during processing

Procedure:

[0071] Blend orlistat, microcrystalline cellulose, and sodium starch glycolate in a suitable mixer. Granulate with a solution of polyvinylpyrrolidone and sodium lauryl sulfate in purified water.

[0072] Pass the granulation through an extruder and pass the extrudate through a spheronizer to form pellets.

[0073] Dry the pellets at 30° C.

[0074] Add talc and mix.

[0075] Fill into hard gelatin capsules. B)IngredientQuantity mg / Capsuleorlistat60microcrystalline cellulose46.8sodium starch glycolate3.6sodium lauryl sulfate3.6polyvinylpyrrolidone6.0purified water*—talc0.12Total120.12mg

*Removed during processing.

Procedure:

[0076] Blend orlistat, microcrystalline cellu...

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Abstract

A pharmaceutical combination or composition containing a lipase inhibitor, preferably orlistat, and a bile acid sequestrant is useful for treating obesity.

Description

[0001] This application is a continuation of U.S. patent application Ser. No. 10 / 718,049, filed Nov. 20, 2003, currently pending, which is a divisional of U.S. patent application Ser. No. 09 / 912,957, filed Jul. 25, 2001, now U.S. Pat. No. 6,756,364, issued Jun. 29, 2004.BACKGROUND OF THE INVENTION [0002] 1. Field [0003] The present invention relates to pharmaceutical combinations, compositions and methods for treating obesity. [0004] 2. Description [0005] Bile acids are synthesized in the liver and enter the bile as glycine and taurine conjugates. They are released in salt form in bile during digestion and act as detergents to solubilize and consequently aid in digestion of dietary fats. Following digestion, bile acid salts are mostly reabsorbed in the ileum, complexed with proteins, and returned to the liver through the hepatic portal vein. The small amount of bile acid salts which are not reabsorbed by active transport are excreted via the distal ileum and large intestine as a por...

Claims

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Application Information

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IPC IPC(8): A61K31/16A61K31/21A61K45/00A61K31/337A61K31/365A61K31/56A61K31/70A61K31/715A61K31/717A61K31/718A61K31/721A61K31/724A61K31/785A61K45/06A61P1/16A61P3/04A61P3/06
CPCA61K31/365A61K31/70A61K31/715A61K31/716A61K31/717A61K31/721A61K31/785A61K45/06A61K2300/00A61P1/00A61P1/16A61P31/18A61P3/04A61P3/06A61P43/00A61K31/337
Inventor BARBIER, PIERREHADVARY, PAULLENGSFELD, HANS
Owner BARBIER PIERRE
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