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Stability-improved butylphthalide oral freeze-dried powder as well as preparation method and application thereof

A technology of freeze-dried powder and butylphthalide, which is applied in the field of butylphthalide oral freeze-dried powder and its preparation, can solve the problems of ring-opening polymerization and achieve good purity and stability

Active Publication Date: 2021-08-03
奥信阳光(北京)药业科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Under the reaction conditions of this patent, lactone cannot be ring-opened and polymerized, and only cyclodextrin derivatives grafted with butyric acid on the surface can be obtained

Method used

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  • Stability-improved butylphthalide oral freeze-dried powder as well as preparation method and application thereof
  • Stability-improved butylphthalide oral freeze-dried powder as well as preparation method and application thereof
  • Stability-improved butylphthalide oral freeze-dried powder as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0061] Under nitrogen atmosphere, drop into sulfobutyl beta cyclodextrin sodium, 4-methylbutyrolactone, stannous octanoate to the reactor containing the MDF solvent of anhydrous treatment; Wherein sulfobutyl beta cyclodextrin sodium, The molar ratio of 4-methylbutyrolactone and stannous octoate is 1:20:0.005, heat up to 110°C, react under reflux and stirring conditions for 24 hours, cool to room temperature, and pour the reaction solution directly into glacial ether to precipitate and precipitate Dissolve in water, recrystallize from absolute ethanol, and recrystallize twice to obtain white crystals, which are the product 4-methylbutyrolactone-modified sulfobutylbeta cyclodextrin sodium. After GPC molecular weight test, the weight molecular weight is about 3620, PDI=1.31.

preparation example 2

[0063] Other conditions were the same as in Preparation Example 1, except that the molar ratio of sulfobutylbeta cyclodextrin sodium to 4-methylbutyrolactone was 1:15. After the GPC molecular weight test, the weight average molecular weight of the obtained product is about 2850, and the PDI=1.28.

preparation example 3

[0065] Other conditions were the same as in Preparation Example 1, except that the molar ratio of sulfobutylbeta cyclodextrin sodium to 4-methylbutyrolactone was 1:30. After GPC molecular weight test, the weight average molecular weight of the obtained product is about 4360, and PDI=1.33.

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Abstract

The invention relates to stability-improved butylphthalide oral freeze-dried powder which is characterized by being prepared from the following raw and auxiliary materials by a freeze-drying method: butylphthalide and 4-methylbutyrolactone modified sulfobutyl beta-cyclodextrin sodium, the 4-methylbutyrolactone modified sulfobutyl-beta-cyclodextrin sodium has the following simple structural formula: the butylphthalide oral freeze-dried powder provided by the invention overcomes the defects of capsule preparations and injections, and the freeze-dried powder is liquid after being redissolved, so that the freeze-dried powder is easier for patients to take. Besides, the plasma peak reaching time of butylphthalide capsules is 60-80 min, after the butylphthalide oral freeze-dried powder is redissolved, the peak reaching time of oral liquid is less than 30 min, and the butylphthalide oral freeze-dried powder can take effect quickly after being taken and has important significance for rescuing cerebral apoplexy patients. Meanwhile, the butylphthalide oral freeze-dried powder has good stability, and can keep good purity, solubility and bioavailability of butylphthalide after being stored for 10 days under the conditions of 25 DEG C and 40RH%.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an oral freeze-dried powder of butylphthalide with improved stability, a preparation method and application thereof. Background technique [0002] Butylphthalide, also known as apigenin (CAS NO.6066-49-5) is a physiologically active substance extracted from celery seeds. It is my country's first national first-class new drug with independent intellectual property rights in cerebrovascular treatment (trade name: Enbipu). Since its launch in 2004, the drug has obvious anti-ischemic effects and can improve energy metabolism exhaustion in cerebral ischemia. , reduce the size of cerebral infarction caused by local cerebral ischemia, improve cerebral blood circulation, reduce cerebral edema and other symptoms caused by local cerebral ischemia, and is an effective drug for the treatment of acute ischemic stroke. The raw material of butylphthalide is a yel...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K47/69A61K31/365A61J3/02A61P9/10
CPCA61K31/365A61K9/0053A61K47/6951A61K9/19A61J3/02A61P9/10
Inventor 孔小轶李金花王蕾
Owner 奥信阳光(北京)药业科技有限公司
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