Tiopronin soft capsule

A technology of tiopronin and soft capsules, which is applied in capsule delivery, digestive system, antiviral agents, etc., can solve the problems of inability to eliminate gastrointestinal irritation, low bioavailability, and large individual differences, and achieve high biological Utilization, fast onset, and low gastrointestinal irritation

Inactive Publication Date: 2008-01-16
上海华源医药科技发展有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although the existing tiopronin oral preparations are convenient to use, slow absorption, low bioavailability and large individual differences are the main obstacles affecting its curative effect
At the same time, tiopronin has the peculiar smell of sulfhydryl compounds and irritation to the gastrointestinal tract, and it is prepared into enteric-coated tablets, which cannot eliminate its irritation to the gastrointestinal tract. Long-term use can lead to loss of appetite, nausea, vomiting, abdominal pain , abdominal distension, diarrhea, etc.

Method used

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  • Tiopronin soft capsule
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  • Tiopronin soft capsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Preparation of Tiopronin Quick Release Soft Capsules:

[0029] 1. Prescription for soft capsule contents:

[0030] Tiopronin 100g

[0031] Edetate Disodium 0.1g

[0032] Sodium bisulfite 0.25g

[0033] Add polyethylene glycol 400 to 250ml

[0034] ------------------------

[0035] Makes 1000 capsules

[0036] 2. Preparation of soft capsule contents: Dissolve 0.1 g of edetate disodium and 0.5 g of sodium sulfite in 2 ml of distilled water, drop into 200 ml of PEG400, and mix well. Take tiopronin 100g, dissolve in the above solution, add appropriate amount of PEG400 to adjust the total volume to 250ml.

[0037]3. Preparation of soft capsules: Press the prepared contents and 60°C gelatin solution with a rotary molding machine (adjust the thickness of the rubber to 90-110 silk, and use liquid paraffin as a lubricant) to make capsules and solidify them in a tumbler cage with cold air After molding, wash off the surface oil layer with ethanol, and dry under hot air con...

Embodiment 2

[0043] Preparation of tiopronin-acrylic resin enteric-coated soft capsule II:

[0044] 1. Prescription for soft capsule contents:

[0045] Tiopronin 100g

[0046] Edetate Disodium 0.1g

[0047] Sodium bisulfite 0.25g

[0048] Acrylic resin enteric coating II 100g

[0049] Span 60 5g

[0050] Add salad oil to 500ml

[0051] --------------------------------

[0052] Makes 1000 capsules

[0053] 2. Preparation of the contents of the soft capsule: 100 g of tiopronin, 100 g of acrylic resin enteric coating II, 0.1 g of disodium edetate and 0.25 g of sodium bisulfite were dissolved in 400 ml of ethanol. Add the prepared ethanol solution into 500ml of salad oil in which Span is dissolved, stir vigorously to obtain an emulsion, reduce the stirring speed, and evaporate the ethanol.

[0054] 3. Preparation of soft capsules: Press the prepared contents and 60°C gelatin solution with a rotary molding machine (adjust the thickness of the rubber to 90-110 silk, and use liquid paraff...

Embodiment 3

[0058] The preparation of tiopronin-ethylcellulose soft capsule:

[0059] 1. Prescription for soft capsule contents:

[0060] Tiopronin 100g

[0061] Edetate Disodium 0.1g

[0062] Sodium bisulfite 0.25g

[0063] Ethylcellulose 25g

[0064] Span 60 5g

[0065] Add salad oil to 500ml

[0066] ---------------------------

[0067] Makes 1000 capsules

[0068] 2. Preparation of the contents of the soft capsule: 100 g of tiopronin, 25 g of ethyl cellulose, 0.1 g of disodium edetate and 0.25 g of sodium bisulfite were dissolved in 400 ml of ethanol. Add the prepared ethanol solution into 500ml of salad oil in which Span is dissolved, stir vigorously to obtain an emulsion, reduce the stirring speed, and evaporate the ethanol.

[0069] 3. Preparation of soft capsules: Press the prepared contents and 60°C gelatin solution with a rotary molding machine (adjust the thickness of the rubber to 90-110 silk, and use liquid paraffin as a lubricant) to make capsules and solidify them i...

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Abstract

The present invention relates to a kind of new preparation of hepatitis B treating medicine, and is especially hepatitis B treating soft Tiopronin capsule preparation suitable for being taken orally. The soft capsule contains physiologically effective Tiopronin and medicine carrier suitable for soft capsule, and the pharmaceutically acceptable carrier includes dispersing medium, antioxidant, metal chelate and / or medicine release regulating material.

Description

Technical field: [0001] The invention relates to a new preparation of anti-hepatitis B medicine, in particular to a soft capsule preparation of anti-hepatitis B medicine tiopronin which is suitable for oral administration. Background technique: [0002] Tiopronin is a glycine derivative of free thiol, which can reduce the activity of mitochondrial ATPase, increase the content of ATP in cells, improve cell structure and function, participate in cell metabolism, maintain the concentration of glutathione in liver cells, and inhibit peroxidation Liposome formation prevents accumulation of triglycerides and protects liver cell membranes. Therefore, the clinical indications of tiopronin include (Matsuura K., et al, Pharmacokinetics of Tiopronin after Oral Administration in Healthy Volunteers, Pharmacy and Pharmacology Communications, 1999; 5 (5): 345-347): 1. It is used to improve the liver function of various acute and chronic hepatitis and early cirrhosis; 2. It is used for the...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/197A61K9/48A61P1/16A61P31/12
Inventor 涂家生毛宇锋岳翔刘道金肖隽
Owner 上海华源医药科技发展有限公司
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