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Pharmaceutical composition and use thereof

A composition and drug technology, applied in the direction of antibacterial drugs, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve problems such as long use time and liver function damage

Inactive Publication Date: 2009-03-11
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As an anti-tuberculosis drug, isoniazid is usually used for a long time, and liver function damage is one of its main side effects

Method used

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  • Pharmaceutical composition and use thereof
  • Pharmaceutical composition and use thereof
  • Pharmaceutical composition and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: the pharmaceutical composition of the present invention consists of 100 grams of isoniazid, 20 grams of tiopronin, 30 grams of carboxymethylcellulose, 20 grams of sucrose, 50 grams of medicinal starch (or select other pharmaceutically acceptable carriers and / or excipients such as maltose, etc.), made into 1000 capsules. The preparation method is as follows: the mixture of isoniazid, tiopronin and pharmaceutically acceptable carrier and / or excipient is placed in the feeding pot of a centrifugal coating granulator to form granules, and then filled with enteric-coated capsules, each capsule Contains isoniazid 100mg, tiopronin 20mg.

Embodiment 2

[0027] Example 2: The pharmaceutical composition of the present invention is made of 300 grams of isoniazid, 30 grams of tiopronin, 25 grams of ethyl cellulose, 0.15 grams of sodium bisulfite, and 50 grams of medicinal starch, and made into 1000 capsules. Its preparation method is as in Example 1, and each capsule contains 300 mg of isoniazid and 20 mg of tiopronin.

Embodiment 3

[0028] Embodiment 3: The pharmaceutical composition of the present invention consists of 100 grams of isoniazid, 50 grams of tiopronin, 50 grams of maltose (or select other pharmaceutical carriers and / or excipients such as sucrose, fructose, etc.), plus injection Make up to 1000ml with water, and pack into 1000 sticks. The preparation method is as follows: dissolve 100 grams of tiopronin and 50 grams of maltose in 1 liter of water for injection, fully stir and dissolve, add 0.01 to 0.1% activated carbon for injection to absorb pyrogens, filter to remove activated carbon, and positive pressure microporous filtration to sterilize , subpackaged, each containing isoniazid 100mg, tiopronin 50mg.

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Abstract

The invention relates to a pharmaceutical composite which contains isoniazide, tiopronin or sodium salt thereof that are taken as the active constituents, and a pharmaceutical carrier and / or an excipient, wherein, the mass ratio of the isoniazide and the tiopronin is 1-10:1. The tiopronin has specific action on inhibiting hepatic CYP2E1, and can specifically treat liver damage caused by the isoniazide which is an antituberculotic, and purposefully reduces the toxic and side effect of the isoniazide on the liver. The pharmaceutical composite not only further expands the pharmaceutical value of the tiopronin which is an inhibitor of the hepatic CYP2E1, but also contributes to the safe clinical application of the related pharmaceutical (isoniazide). Therefore, the pharmaceutical composite has important medical value and social and economic benefits.

Description

1. Technical field [0001] The invention relates to a pharmaceutical composition and application thereof. The pharmaceutical composition contains isoniazid, tiopronin or sodium salt thereof as active ingredients and a pharmaceutically acceptable carrier and / or excipient; it can be used for treating tuberculosis. 2. Background technology [0002] Tiopronin (English name Tiopronin, chemical name: mercaptopropionylglycine), its molecular formula: C 5 h 9 NO 3 SH, molecular weight: 163.2, structural formula as follows: [0003] [0004] The liver is the main organ for the transformation and metabolism of various substances in the body. It expresses a variety of enzyme systems involved in the metabolism of substances, the most important of which is cytochrome P450 (CYPs for short). CYPs is a superfamily enzyme system with multiple subtypes, which metabolizes a variety of endogenous substances (substances synthesized by the body's own metabolism) and exogenous substances (inc...

Claims

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Application Information

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IPC IPC(8): A61K31/4409A61K31/195A61P31/06
Inventor 彭仁琇乐江
Owner WUHAN UNIV
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