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Lyophiliced powder containing tiprenolol and its preparing method

A technology of freeze-dried powder and drying, which is applied in the field of medicine and can solve problems such as reduced stability

Inactive Publication Date: 2005-12-21
乔杰
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Although tepronine API is acidic, it is more stable under acidic conditions and less stable under neutral or alkaline conditions

Method used

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  • Lyophiliced powder containing tiprenolol and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Example 1 - Tepronine freeze-dried powder

[0075] Tepronine

arginine

meglumine

trometamol

Triethanolamine

Diethanolamine

Monoethanolamine

Ethylenediamine

NaOH

Mannitol

lactose

Dextran-40

Glycine

Sodium chloride

cysteine ​​hydrochloride

sodium bisulfite

EDTA-2Na

Sodium citrate

potassium tartrate

Potassium sorbate

Water for Injection

5g

13g

1.5g

1g

10mg

10mg

10mg

10mg

5mg

200g

5g

5g

5g

2g

100mg

100mg

100mg

50mg

50mg

0.8g

Add to 1000ml

[0076] Preparation:

[0077] a. Weigh the prescribed amount of tepronine that meets the requirements for injection, and add about 500ml of water for injection to dissolve;

[0078] b. Add EDTA-2Na, sodium citrate, potassium tartrate, potassium sorbate, cysteine ​​hydrochloride, sodium bisulfite and support agent manni...

Embodiment 2

[0089] Example 2 - Tepronine freeze-dried powder

[0090] Tepronine

arginine

Mannitol

EDTA-2Na

1M NaOH or

1M hydrochloric acid solution

Water for Injection

50g

49g

45g

0.4g

Appropriate amount, adjust the pH value to 4.5±0.2

Add to 1000ml

[0091] Preparation:

[0092] Weigh the prescribed amount of tepronine, arginine, mannitol and EDTA-2Na that meet the requirements for injection, add about 950ml of water for injection to dissolve; add 0.5g of activated carbon for injection, heat the solution to 60-70°C, and stir for 20 minutes , decarbonize by initial filtration, measure the pH value, adjust the pH value to 4.5±0.2 with 1M sodium hydroxide or 1M hydrochloric acid solution if necessary, add water for injection to 1000ml, mix well; Filter until the solution is clear; the sterilized filtrate is divided into cillin bottles, each bottle can be filled with 1ml, 2ml, 5ml, 10ml, and the ventilation rub...

Embodiment 3

[0095] Example 3 - Tepronine freeze-dried powder

[0096] Tepronine

meglumine

Glycine

EDTA2Na

Water for Injection

50g

75g

45g

0.1g

Add to 1000ml

[0097] Preparation:

[0098] Weigh the prescribed amount of tepronine, meglumine, glycine and EDTA2Na that meet the requirements for injection, add about 950ml of water for injection to dissolve; add 0.5g of activated carbon for injection, heat the solution to 60-70°C, stir for 20 minutes, and initially Filter and remove carbon, add water for injection to 1000ml, mix well; use 0.22μm microporous membrane filter to sterilize, and filter until the solution is clear; divide the sterilized filtrate into vials, each bottle can hold 1ml, 2ml, 5ml , 10ml, 20ml, ventilated rubber stopper half stopper; Carry out freeze-drying by the method for embodiment 1, obtain freeze-dried powder of the present invention.

[0099] In this embodiment, the molar ratio of tepronine to acid-bas...

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Abstract

The present invention provides a freeze-dried powder preparation containing pharmacological active component tiprelonin and its preparation method. Said freeze-dried powder preparation contains 1 mol fraction of tiprelonin and 0.2-3 mol fractions of acid-alkali neutralizing agent. When said freeze-dried powder preparation is dissolved by using injection water to obtain solution containing tiprelonin whose concentration is 50 mg / ml, the pH value of said solution is 3.0-9.0. Said invention has good pharmaceutic property and stability in quality.

Description

【Technical field】 [0001] The invention belongs to the technical field of medicine, and relates to a freeze-dried powder containing a pharmacological active ingredient tepronine and a preparation method of the freeze-dried powder. 【Background technique】 [0002] Tepronine (also known as tiopronin, English name tiopronin), chemical name: N-(2-mercaptopropionyl)-glycine, molecular formula: C 5 h 9 NO 3 S, the molecular weight is: 163.2, and its chemical structural formula is: [0003] [0004] Tepronine is mainly used for the improvement of liver function in chronic liver diseases. Animal experiments have shown that tepronine can reduce the increase of serum AST and ALT in animal models of acute liver injury caused by thioacetamide and carbon tetrachloride. It has an inhibitory effect on the accumulation of triglycerides caused by chronic liver injury models; it can promote the synthesis of glycogen in the liver, inhibit the increase of cholesterol, and is beneficial to t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/197
Inventor 乔杰
Owner 乔杰