Tiopronin sterile powder and preparation and preparation method thereof

A technology for tiopronin and sterile powder injection, which is applied in the field of sterile tiopronin powder and its preparation and preparation, can solve the problems of decomposition of tiopronin, easy generation of impurities, poor stability, etc., and achieves high yield and purity high effect

Active Publication Date: 2012-06-27
HAINAN JINXING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, in the production of the reported tiopronin sterile powder preparations, the tiopronin sterile powder is mainly purified by recrystallization from ethyl acetate, but the boiling point of ethyl acetate is higher, being 77 ° C, while tiopronin Tiopron

Method used

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  • Tiopronin sterile powder and preparation and preparation method thereof
  • Tiopronin sterile powder and preparation and preparation method thereof
  • Tiopronin sterile powder and preparation and preparation method thereof

Examples

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Example Embodiment

[0031] A preparation method of tiopronin sterile powder, comprising:

[0032] Step 1: Take tiopronin raw material, add 4 to 10 times of ethyl formate to dissolve in g / mL, heat to reflux, add 0.1% to 0.5% injection based on weight / volume percentage in g / mL Adsorb and filter with activated carbon;

[0033] Step 2: Take the filtrate obtained in Step 1, add ethyl formate 5v / v%-30v / v% ether or methyl tert-butyl ether, heat and stir to dissolve, and filter with 0.22μm microporous membrane below 0.1Mpa;

[0034] Step 3: Take the filtrate obtained in step 2 and freeze it to -5~5°C for crystallization, collect the obtained crystals, filter, dry under reduced pressure at 15~30°C, and pulverize.

Example Embodiment

[0035] In order to further understand the present invention, the present invention will be described in detail below in conjunction with embodiments. Example 1: Preparation of Tiopronin Sterile Powder Injection

[0036] (1) Weigh 500g of Tiopronin raw material with a purity of 95.3%, add it to the reactor, add 6 times the amount, that is, 3L of ethyl formate, and heat to reflux;

[0037] (2) After Tiopronin is dissolved, add 9g of activated carbon for injection, heat and reflux for 30 minutes and then filter;

[0038] (3) After filtering, add 300 mL of methyl tert-butyl ether to the filtrate, heat and stir to dissolve;

[0039] (4) After dissolving, filter under positive pressure with 0.22μm microporous membrane below 0.1Mpa;

[0040] (5) After filtering, freeze the filtrate to 0°C and crystallize at low temperature for 2 hours;

[0041] (6) After the crystallization is completed, filter and vacuum-dry the obtained crystals at 15°C for 4 hours;

[0042] (7) After drying, pulverize the cr...

Example Embodiment

[0044] Example 2: Preparation of Tiopronin Sterile Powder Injection

[0045] (1) Weigh 500g of Tiopronin raw material with a purity of 95.3%, add it to the reactor, add 10 times the amount, that is, 5L of ethyl formate, and heat to reflux;

[0046] (2) After Tiopronin is dissolved, add 25g of activated carbon for injection, heat to reflux for 30 minutes and then filter;

[0047] (3) After filtering, add 1000 mL of methyl tert-butyl ether to the filtrate, heat and stir to dissolve;

[0048] (4) After dissolving, filter under positive pressure with 0.22μm microporous membrane below 0.1Mpa;

[0049] (5) After filtering, freeze the filtrate to 5°C and crystallize at low temperature for 2 hours;

[0050] (6) After the crystallization is completed, filter and vacuum-dry the obtained crystals at 30°C for 3 hours;

[0051] (7) After drying, the crystals are crushed to obtain 456.5 g of white tiopronin sterile powder with a yield of 91.3%. The purity is 99.5%;

[0052] (8) Sterile tiopronin powder...

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Abstract

The invention relates to the field of pharmaceutical engineering, in particular to a tiopronin sterile powder and a preparation and a preparation method thereof. The preparation method disclosed by the invention comprises the following steps of: adding an ethyl formate-dissolvable tiopronin raw material into an active carbon heat removing source for injection; adding ether or methyl tert-butyl ether for recrystallizing; and drying at a low temperature to obtain tiopronin sterile powder which is free from pyrogen and has high purity. The preparation method disclosed by the invention is easy and convenient to operate, and has high yield; and the obtained tiopronin sterile powder has high purity and safe and reliability quality, is suitable for preparing a tiopronin sterile powder injection, and can be widely applied to mass production of tiopronin sterile powder injections.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a tiopronin aseptic powder and its formulation and preparation method. Background technique [0002] Tiopronin, English name Tiopronin, chemical name N-(2-mercaptopropionyl)-glycine, is a new type of glycine derivative containing free sulfhydryl, molecular formula is C 5 h 9 NO 3 S, the molecular weight is 163.20, the structural formula is as follows: [0003] [0004] Tiopronin is a thiol-containing drug similar in nature to penicillamine, and has the effect of protecting liver tissue and cells. Animal experiments have shown that tiopronin can prevent liver damage caused by carbon tetrachloride, ethionine, acetaminophen, etc. by providing sulfhydryl groups, and can inhibit the accumulation of triglycerides in chronic liver damage. The activity of ATPase in the mitochondria of liver cells is reduced, thereby protecting the structure of liver mitochondria and impr...

Claims

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Application Information

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IPC IPC(8): C07C323/60C07C319/28A61K31/198A61K9/14A61P1/16A61P39/02A61P39/06A61P35/00
Inventor 刘敏张丽杰刘全胜
Owner HAINAN JINXING PHARMA
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