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Preparations for preventing bile acid diarrhea

A technology for bile acid and diarrhea, which is applied in the field of preparations for preventing bile acid diarrhea

Inactive Publication Date: 2003-06-04
SHIONOGI & CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, no preparations of cholestyramine have been reported so far, which are designed to be selectively released at specific locations in the gastrointestinal tract, especially around the region between the lower part of the small intestine and the cecum in order to more effectively suppress bile acid diarrhea

Method used

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  • Preparations for preventing bile acid diarrhea
  • Preparations for preventing bile acid diarrhea
  • Preparations for preventing bile acid diarrhea

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] The first fluid (pH about 1.2) of the Japanese Pharmacopoeia was added to a 10 mL test cylinder containing 2 mL of coated particles to the full scale, and then the swelling rate and volume of the CAS resin were measured over time. The state of the coating was observed by SEM (scanning electron microscope), and the relationship between the swelling rate and the cracking rate of the coating was detected. (Example 1) Preparation of enteric-coated cholestyramine (CSA) preparation (pH-dependent)

[0061] As the enteric layer, HPMCAS-HF (Shin-Etsu Chemical Co., Ltd.) having a dissolution pH of 6.5 or more was used. By using HPMCAS-HF / triethyl citrate / (EtOH / CH 2 Cl 2 , 7:3v / v)=7 / 1 / 92% (weight) of the coating solution can prepare enteric coating particles. Given HPMCAS'-COC 2 h 4 The cause of the interaction between COOH" and trimethylamine of CSA, a barrier layer was inserted between the enteric layer and CSA. The solution was coated with calcium hydrogen phosphate / HPC-...

Embodiment 2

[0069] It is proved that the isolation layer and the enteric coating layer are uniform coating layers respectively, and their contents are respectively 13.6% (coating thickness=about 10 μm) and 30.5% (coating thickness = about 10 μm) and 30.5% (coating thickness = about 30 μm). The results of the immersion test were figure 1 shown. The swelling rate was 170% at 30 minutes, 250% at 1 hour and 300% at 2 hours. The progress of the burst release of the coating layer was confirmed by SEM examination to be about 20% at 30 minutes, about 80% at 1 hour, and 100% at 2 hours. (Example 2) Preparation of Ethylcellulose Coated Cholestyramine (CSA) Formulations (Type Controlled by Coating Thickness)

[0070] Five kinds of ethylcellulose (EC) granules were prepared using a coating solution of EC / EtOH=5 / 95% by weight, wherein the coating amount thereof was changed according to the coating time. Its composition is shown below. (Table 2)

[0071] Composition A B C D E

[0072] DOWEX...

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PUM

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Abstract

Preparations for preventing bile acid diarrhea characterized by containing a bile acid adsorbent coated with a polymer so as to allow the release thereof around the lower part of the small intestine and the cecum; and medicines (for example, antilipemics) comprising a combination of bile acid re-absorption inhibitors with the above-described preparations for preventing bile acid diarrhea.

Description

technical field [0001] The present invention relates to a preparation for preventing bile acid diarrhea, a pharmaceutical composition comprising a combined form of a bile acid reabsorption inhibitor and the preparation for preventing diarrhea, and the like. Background technique [0002] According to LRC-CPPT (lipid Research Clinics Coronary Primary Prevention Trial), U.S.A. reported in 1984 that hypercholesterolemia can be treated with bile acid secretion promoters to reduce the crisis rate of coronary artery disease. Therefore, various therapeutic agents for hypercholesterolemia are based on already developed pharmacological mechanisms. Among them, bile acid reabsorption inhibitors, such as lignan analogs (Japanese Patent Publication (A) 1993 / 310634, USP5,420,333) or their glucuronic acid conjugates (Japanese Patent Publication (A) 1997 / 241206) etc.) are known to reduce the concentration of LDL-cholesterol by inhibiting the reabsorption of bile acid from the small intestin...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K9/52A61K31/235A61K31/785A61P1/12A61P3/06
CPCA61K31/235A61K31/785A61K9/5042A61K9/5047A61K9/5073A61P1/12A61P3/06A61K47/30
Inventor 益田和义杉田勝二早川洋初代秀一铃木裕介
Owner SHIONOGI & CO LTD
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