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A kind of racemic 2-(alpha-hydroxypentyl) benzoate freeze-dried powder for injection and preparation method thereof

A technology of hydroxypentyl and benzoate, which is applied in the field of medicine, can solve problems such as easy degradation and poor stability, and achieve the effect of solving stability problems

Active Publication Date: 2016-01-20
南通协生元医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to solve the problem that the active ingredient racemic 2-(α-hydroxypentyl)benzoate is prone to degradation and poor stability in the preparation process of conventional freeze-dried agents, a racemic 2-(α- Hydroxypentyl) benzoate freeze-dried powder injection and preparation method thereof

Method used

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  • A kind of racemic 2-(alpha-hydroxypentyl) benzoate freeze-dried powder for injection and preparation method thereof
  • A kind of racemic 2-(alpha-hydroxypentyl) benzoate freeze-dried powder for injection and preparation method thereof
  • A kind of racemic 2-(alpha-hydroxypentyl) benzoate freeze-dried powder for injection and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0035] Prescription composition (1000 sticks, 25mg / stick)

[0036] Racemic 2-(α-hydroxypentyl)sodium benzoate 25g

[0037] Sodium chloride 15g

[0038] Anhydrous disodium hydrogen phosphate 3g

[0039] Preparation method: dissolve the excipients in water for injection, adjust the pH value to 12.0 with aqueous sodium hydroxide solution after dissolving; add the main drug to the above excipient solution with a pH value of 12.0 to dissolve, add water for injection, and adjust the pH value of the solution with sodium hydroxide solution to 12.0, with a final volume of 1000mL; sterilized by passing through a 0.22μm microporous membrane; filling, 1ml / bottle; semi-pressed butyl rubber stoppers, and freeze-drying in a freeze dryer: put the filled medicinal solution in - Pre-freeze at 35°C, and when the temperature of the liquid medicine reaches -35°C, maintain it for 4 hours; raise the temperature to -30°C in 4 hours, maintain it for 20 hours, and keep the vacuum degree <20Pa; raise ...

Embodiment 2

[0041] Prescription composition (1000 sticks, 25mg / stick)

[0042] Racemic 2-(α-hydroxypentyl)sodium benzoate 25g

[0043] Sodium chloride 90g

[0044] Anhydrous disodium hydrogen phosphate 5g

[0045] Preparation method: with embodiment 1.

Embodiment 3

[0047] Prescription composition (1000 sticks, 25mg / stick)

[0048] Racemic potassium 2-(α-hydroxypentyl)benzoate 25g

[0049] Sodium chloride 90g

[0050] Anhydrous disodium hydrogen phosphate 6g

[0051] Preparation method: with example 1.

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Abstract

The invention relates to a racemized 2-(alpha-hydroxypentyl) benzoate freeze-dried powder needle for injection, and a preparation method thereof. The racemized 2-(alpha-hydroxypentyl) benzoate freeze-dried powder for injection comprises the following ingredients in percentage by weight: 5-95% of racemized 2-(alpha-hydroxypentyl) benzoate and 5-95% of needle auxiliaries. According to the preparation method, the problems that the active ingredient racemized 2-(alpha-hydroxypentyl) benzoate is easily degraded and poor in stability in the preparation technique of the freeze-dried agent can be solved by adopting the alkalinization preparation technique capable of regulating the pH value to be 11.0-13.0 with officinal alkaline, the stability of main drugs in the injective racemized 2-(alpha-hydroxypentyl) benzoate freeze-dried powder needle can be obviously increased, thereby being applicable to preparation of the racemized 2-(alpha-hydroxypentyl) benzoate freeze-dried powder needle.

Description

technical field [0001] The invention relates to a racemic 2-(α-hydroxypentyl) benzoate freeze-dried powder injection and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Racemic 2-(α-hydroxypentyl)benzoate is the drug precursor of racemic butylphthalide, which can be rapidly converted into racemic butylphthalide in the body to exert its drug effect. After intravenous injection of racemic 2-(α-hydroxypentyl)benzoate in dogs and rats, it can be rapidly and completely converted into racemic butylphthalide in vivo, and the exposure value of racemic butylphthalide in plasma Compared with the exposure value of direct intravenous injection of racemic butylphthalide, they were 97.4 (rats) and 112.5% ​​(dogs). Explain that after racemic 2-(α-hydroxypentyl) benzoate enters the body, it can be quickly and completely converted into racemic butylphthalide, and its pharmacokinetic parameters are the same as those of direct intraven...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/192
Inventor 刘宇航高哲伟韩亚雄
Owner 南通协生元医药科技有限公司