Stable butylphthalide small squirt, and preparation method and application thereof

A technology of butylphthalide and small water injection, which is applied in the field of preparation of small water injection of butylphthalide to treat cerebral apoplexy, can solve the problems of inconvenient clinical use and poor stability of butylphthalide injection, etc. Achieve the effects of easy use and portability, good safety, and scientific design

Pending Publication Date: 2021-11-19
CHENGDU SHIBEIKANG BIOLOGICAL MEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] One of the objectives of the present invention is to provide a small water injection of butylphthalide, which has good stability and safety, and solves the problems of poor stability and inconvenient clinical use of butylphthalide injection in the prior art

Method used

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  • Stable butylphthalide small squirt, and preparation method and application thereof
  • Stable butylphthalide small squirt, and preparation method and application thereof
  • Stable butylphthalide small squirt, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] This example discloses the preparation method of the small water injection of butylphthalide (5mL: 25mg, 5mg / ml) of the present invention. Its preparation prescription (prescription quantity 100) is:

[0037]

[0038] Preparation method: Take the prescribed amount of purified water, boil and cool to 80°C. Weigh 75 g of sodium sulfobutylbeta cyclodextrin (degree of substitution 6.2-6.9, average degree of substitution 6.4, molecular weight 2145.2 g / mol), add it to 400 mL of purified water at 80°C, and stir to dissolve completely. Weigh 2.5 g of butylphthalide, add it to the sodium sulfobutylbeta cyclodextrin solution, stir in an oil bath at 80°C for 120 min to dissolve completely. Allow to cool to room temperature, add 0.2M hydrochloric acid solution to adjust the pH value to 4.5, and add purified water to 500mL. Filter through a 0.45 μm filter membrane with a circulating water-type multi-purpose vacuum pump. Fill the prepared solution at 5mL / bottle. After filling,...

Embodiment 2

[0046] This embodiment discloses the investigation of the solubilizing ability of butylphthalide with the dosage of sulfobutylbeta cyclodextrin sodium, specifically:

[0047] According to the method of Example 1, small water injections of butylphthalide (5mL: 25mg, 5mg / ml) were prepared, the only difference being the amount of sodium sulfobutylbeta cyclodextrin. Then the properties of the prepared small water needles of butylphthalide and the content of butylphthalide in the small water needles were investigated.

[0048] The patent application number is CN2020113980997 "a stable butylphthalide sodium chloride injection, its preparation method and application", the molar ratio of butylphthalide to sulfobutylbeta cyclodextrin sodium is 1:1.60~2.20 , converted into a mass ratio of 1:18 to 25. The dosages of butylphthalide and sulfobutylbeta cyclodextrin sodium in Table 3 refer to the dosage settings.

[0049] Table 3 The comparison results of the solubilization ability of diff...

Embodiment 3

[0059] In this example, the effect of pH value on the stability of butylphthalide small water injection (5 mL: 25 mg, 5 mg / ml) at high temperature (60° C.) for 10 days was investigated.

[0060] According to the method of Example 1, the small water needles of butylphthalide are prepared, the difference is only that the adjusted pH values ​​of the small water needles of butylphthalide are different, and the specific pH values ​​of the prepared small water needles of butylphthalide are shown in Table 5. Table 5 shows the results of the impurity content in the small water needle.

[0061] The different pHs of table 5 affect the result table of embodiment prescription stability

[0062] Numbering 1 2 3 4 5 6 7 8 pH value 4.0 4.5 5.0 5.5 6.0 6.5 7.0 7.5 Maximum Simplex % 0.05 0.02 0.021 0.023 0.22 0.63 0.90 1.03 Total Miscellaneous % 0.10 0.02 0.023 0.025 0.29 0.69 0.95 1.05

[0063] It can be seen from Table 5 that ther...

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Abstract

The invention discloses a stable butylphthalide small squirt, and a preparation method and application thereof, and solves the problems of poor stability and inconvenience in clinical use of a butylphthalide injection in the prior art. The butylphthalide small squirt is prepared from the following raw materials: butylphthalide, sodium sulfobutyl-beta-cyclodextrin and water, wherein the weight ratio of the butylphthalide to the sodium sulfobutyl-beta-cyclodextrin to the water is 1:(30-35):(40-400). The preparation method comprises the following steps: weighing a prescription amount of sodium sulfobutyl-beta-cyclodextrin, and adding water for injection to dissolve the sodium sulfobutyl-beta-cyclodextrin so as to prepare an auxiliary material solution; adding butylphthalide into the auxiliary material solution, conducting stirring to enable the sulfobutyl beta-cyclodextrin sodium to be clathrated with the butylphthalide, and after the clathration of the butylphthalide is completed, adjusting the pH value of the solution to 4.5-5.5; and conducting filtering, filling and sterilizing to obtain the product. The butylphthalide small squirt has good stability and safety, and is suitable for industrial production. Compared with a butylphthalide sodium chloride injection, the injection provided by the invention has better stability.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a pharmaceutical preparation for treating cerebral apoplexy, and more specifically to a stable small water injection of butylphthalide, its preparation method and application. Background technique [0002] Butylphthalide: (3-n-butylphthalide, NBP for short), the chemical name is 3-butyl-1(H)-isobenzofuranone, and its structural formula is as follows: [0003] [0004] Butylphthalide, also known as apigenin A, is extracted from celery seeds, has a strong celery flavor, and can also be synthesized artificially. Butylphthalide is an oily liquid, insoluble in water, and contains a chiral carbon atom in the molecule, so it has two optical isomers, namely, L-butylphthalide and D-butylphthalide. Butylphthalide can reduce the infarction after focal cerebral ischemia, increase the cerebral blood flow in the ischemic area and improve the microcirculation in the cere...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/69A61K31/365A61P9/10
CPCA61K9/0021A61K47/6951A61K31/365A61P9/10
Inventor 聂昱曾燕群张海牟霞苏永文易泽琴
Owner CHENGDU SHIBEIKANG BIOLOGICAL MEDICINE TECH CO LTD
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