3-n-butylphthalide injection and preparation method thereof

A technology of butylphthalide and injection, which is applied in the field of medicine and can solve the problems of unstable quality, complicated formulation of butylphthalide, and inability to meet clinical drug requirements well.

Active Publication Date: 2014-01-15
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This dosage form needs to be compatible with glucose injection or sodium chloride injection when used, it is difficult to operate when diluted in clinical application, and it is still intravenous injection or infusion
[0006] To sum up, the butylphthalide dosage forms disclosed in the prior art have complex processes, unstable quality, and still cannot well meet the needs of clinical medication.

Method used

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  • 3-n-butylphthalide injection and preparation method thereof
  • 3-n-butylphthalide injection and preparation method thereof
  • 3-n-butylphthalide injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0109] Example 1 Butylphthalide injection (water injection): contains butylphthalide, soybean lecithin, and water for injection. The prescription dosage of the three is shown in the following table:

[0110] In 100mL:

[0111] Material name Prescription amount % by weight Butylphthalide 0.25g 0.25 Soy Lecithin 4g 4 water for injection Replenish water to 100ml

[0112] Preparation process: Dissolve soybean lecithin in about 90ml of water for injection at 40~60°C, slowly add butylphthalide dropwise, stir well, break up with a high-pressure homogenizer, control the particle size to be less than 50 nanometers, obtain a clear liquid, replenish water To 100ml, add 0.1% activated carbon and stir for 30 minutes, filter to remove carbon, sterilize, pack in 10ml each, and sterilize.

Embodiment 2

[0113] Example 2 Butylphthalide injection (water injection): contains butylphthalide, polyethylene glycol-12-hydroxystearate and water for injection. The prescription dosage of the three is shown in the following table:

[0114] Material name Prescription amount % by weight Butylphthalide 0.25g 0.25 Polyethylene glycol-12-hydroxystearate 1g 1 water for injection Replenish water to 100ml

[0115] Preparation process: Dissolve polyethylene glycol-12-hydroxystearate in about 90ml of water for injection at 20~30°C, slowly add butylphthalide dropwise, stir well, no oil droplets appear on the liquid surface, and a clear liquid is obtained. Replenish water to 100ml, add 0.2% activated carbon and stir for 30 minutes, filter to remove carbon, sterilize, pack in aliquots, 10ml each, and sterilize.

Embodiment 3

[0116] Example 3 Butylphthalide injection (freeze-dried powder injection): contains butylphthalide, polyethylene glycol-12-hydroxystearate and water for injection. The prescription dosage of the three is shown in the following table:

[0117] Material name Prescription amount % by weight Butylphthalide 0.5g 0.5 Polyethylene glycol-12-hydroxystearate 2g 2 Mannitol 6g 6 glucose 1.5g 1.5 water for injection Replenish water to 100ml

[0118] Preparation process: Dissolve polyethylene glycol-12-hydroxystearate in about 90ml of water for injection at 20~30°C, slowly add butylphthalide dropwise, stir well, until no oil drops appear on the liquid surface, add mannitol and glucose Dissolve to obtain a clear liquid, add water to 100ml, add 0.1% activated carbon and stir for 30 minutes, filter to remove carbon, sterilize, subpackage, 5ml each, and freeze-dry.

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Abstract

The invention relates to a 3-n-butylphthalide injection and a preparation method thereof. The 3-n-butylphthalide injection disclosed by the invention comprises 3-n-butylphthalide or a derivant thereof, a surfactant and water for injection, wherein the surfactant is selected from one or more of phospholipid, polyethylene glycol-12-hydroxy stearate, polyethylene glycol-VE (Vinyl Ether) carbonic ester, polyethylene glycol-VE succinate, polyethylene glycol-DSPE (distearoyl phosphoethanolamine), polyethylene glycol-cholesteryl hemisuccinate, polyethylene glycol-cholesterol methyl ester, polyethylene glycol-cholesterol sulfate, polyoxyethylene dehydration sorbitol fatty acid ester and poloxamer. By adopting the 3-n-butylphthalide injection disclosed by the invention, a special fragrance of the 3-n-butylphthalide can be effectively concealed; the 3-n-butylphthalide injection is stable in quality, high in 3-n-butylphthalide content, simple in preparation technology, strong in operability and beneficial to industrialization, can be separately subpackaged into small volume of preparation, can be applied to intravenous injection, and also can be applied to intramuscular injection; the clinical drug delivery requirements are met.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a drug injection and a preparation method thereof, in particular to a butylphthalide injection and a preparation method thereof. Background technique [0002] Butylphthalide (3-n-butylphthalide, NBP for short), full name 3-butyl-1(H)-isobenzofuranone, also known as apigenin A, is a racemate extracted from celery seed , can also be artificially synthesized. Butylphthalide is an oily liquid that is insoluble in water and has a strong celery smell. The molecule contains a chiral carbon atom, so it exists in 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 cerebral ischemic area, protect the mitochondrial function, reduce the degree of neurological damage, and improve the cerebral ischemia. Energy meta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/19A61K31/365A61K47/34A61K47/24A61P9/10A61P25/28A61P7/02
Inventor 王莉芳马玉秀郝卫华白敏陈亚平陈玉洁杨敏冯小龙杨汉煜刘英发
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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