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Thipronin enteric-coated delayed-release agent

A tiopronin enteric and slow-release preparation technology, which is applied in antidote, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of large fluctuations in drug concentration and reduce direct stimulation Sexuality, good for long-term treatment, avoid nausea effect

Inactive Publication Date: 2007-10-03
魏秀华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tiopronin is a commonly used drug in clinical practice. The existing dosage forms in China include ordinary capsules, injections, etc., and the oral preparations are taken 3 times a day, which brings a lot of inconvenience to patients, especially chronic patients and patients who take medicine for a long time, and the number of times of taking medicine often causes the drug Defects with large fluctuations in concentration in the body

Method used

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  • Thipronin enteric-coated delayed-release agent
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  • Thipronin enteric-coated delayed-release agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Preparation of Tiopronin Tablets:

[0023] prescription:

[0024] Names of raw and auxiliary materials (1000 tablets)

[0025] Tiopronin 300.0g

[0026] Microcrystalline Cellulose 50.0g

[0027] Pregelatinized starch 50.0g

[0028] 15% povidone K30 ethanol solution 150ml

[0029] Magnesium Stearate 6.0g

[0030] Preparation Process:

[0031] Weigh the prescribed amount of tiopronin, microcrystalline cellulose, and pregelatinized starch fully and evenly, add an appropriate amount of binder to make a soft material, granulate, and dry at 50°C; for whole granules, add the prescribed amount of stearic acid Magnesium is thoroughly mixed and pressed into tablets.

[0032] Dissolution Determination:

[0033] According to the release assay method (Chinese Pharmacopoeia version two appendix XD second method (two) method in 2005), the first method device of the dissolution assay method is adopted, and phosphate buffer (pH6.8) 500ml is used as solvent, and the rotating spee...

Embodiment 2

[0035] Preparation of Tiopronin Enteric-coated Sustained-release Tablets (1000 Tablets Quantity)

[0036] Sustained release layer prescription:

[0037] Tiopronin 300.0g

[0038] Hypromellose K4MCR 100.0g

[0039] Hypromellose K100MCR 75.0g

[0040] Microcrystalline Cellulose 50.0g

[0041] Pregelatinized starch 50.0g

[0042] 15% povidone K30 ethanol solution 150ml

[0043] Magnesium Stearate 6.0g

[0044] Enteric coating layer prescription:

[0045] Ethyl cellulose 60.0g

[0046] Macrogol 4000 28.0g

[0047] 95% ethanol 2000ml

[0048] Preparation Process:

[0049] Weigh the prescribed amount of tiopronin, microcrystalline cellulose, pregelatinized starch, hypromellose K4MCR, hypromellose K100MCR fully uniform, add an appropriate amount of binder to make a soft material, granulate, 50 ℃ Blow drying; whole grain, add prescription amount of magnesium stearate, mix thoroughly, and compress into tablets. Spray coating solution and enteric coating.

Embodiment 2~11

[0051] According to the release assay method (Chinese Pharmacopoeia version two appendix XD second method (two) method in 2005), the dissolution assay method first method device is adopted, with 0.1mol / L hydrochloric acid solution 500ml as solvent, and the rotating speed is 100 revolutions per minute , operate according to law. After 2 hours, no cracks or disintegration should be found on the test pieces. Precisely measure 10ml, filter, take the filtrate to measure, the released amount must not exceed 10% of the marked amount; take the above test piece and add 500ml of phosphate buffer (pH6.8) immediately, keep the speed constant, continue to operate according to the law, Accurately measure 10ml of the solution for a certain period of time, and add 10ml of phosphate buffer (pH6.8) at the same temperature to the operating container in time, and take the subsequent filtrate for determination.

[0052] The results showed that the tiopronin sustained-release tablets prepared with...

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Abstract

A slow-releasing enteric tiopronin without stimulation and by-effect is prepared from tiopronin (3-65 Wt%), slow-releasing material (5-90) and enteric coating material (3-30).

Description

technical field [0001] The invention relates to an enteric-coated slow-release preparation of tiopronin, which belongs to the field of chemical drug preparations. Background technique [0002] Tiopronin (English name: Tiopronin) is a metabolic improvement antidote, its molecular formula: C 5 h 9 NO 3 S, molecular weight: 163.20, structural formula as follows: [0003] [0004] Tiopronin can be used to restore liver function and adjuvant therapy in patients with chronic hepatitis. Animal experiments have shown that tiopronin has a preventive effect on acute liver injury in mice caused by carbon tetrachloride, ethanol and D-galactosamine. It can protect the structure of liver mitochondria and improve its function. This product is to TAA (thioacetamide), CCl 4 (Carbon tetrachloride) can reduce the increase of serum AST and ALT in the acute liver injury model of animals, and can inhibit the accumulation of triglycerides caused by the chronic liver injury model; it can p...

Claims

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Application Information

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IPC IPC(8): A61K31/198A61K47/00A61P3/00A61P39/02
Inventor 魏秀华
Owner 魏秀华
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