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Butylphthalide preparation and preparation method thereof

A technology of butylphthalide and preparations, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the difference in effectiveness, large coefficient of variation of butylphthalide soft capsules, and Problems such as low utilization, to achieve the effects of easy industrial production, good drug stability, and simple preparation process

Pending Publication Date: 2022-02-22
BEIJING COLLAB PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The butylphthalide oral preparation currently on the market is "Enbipu" of CSPC, which is butylphthalide soft capsules. Chinese patent CN1623542A is the patent of CSPC's butylphthalide soft capsules, which involves The capsule and its preparation process are composed of butylphthalide, diluent vegetable oil and capsule material. The butylphthalide soft capsule has the problem of low oral bioavailability
[0007] Chinese patent CN1726909A relates to butylphthalide self-emulsifying drug release system and its preparation method and application, wherein emulsifiers are added, such as polyoxyethylene castor oil, caprylic capric acid polyethylene glycol glyceride, polyoxyethylene sorbitan oleate, etc. Surfactants, none of these emulsifiers can achieve the purpose of improving bioavailability
[0008] The doctoral dissertation "Studies on the Pharmacokinetics of Butylphthalide in Humans, Peking Union Medical College, Ye Zhongkai" involved Butylphthalide Soft Capsules. The blood concentration cannot be measured, and inter-individual differences can easily cause inter-individual differences in effectiveness

Method used

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  • Butylphthalide preparation and preparation method thereof
  • Butylphthalide preparation and preparation method thereof
  • Butylphthalide preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Soft capsules with butylphthalide content of 100mg / capsule

[0036]

[0037] Preparation:

[0038] a. Capsule shell preparation: weigh 2kg of gelatin, 0.8kg of glycerin, and 2kg of water;

[0039] b. Glue: Stir and mix water and glycerin first, heat at 65°C, add gelatin, and keep stirring until it is completely dissolved, then keep vacuum to defoam until the bubbles completely disappear, and finally, place it in an insulated bucket at 55°C to keep warm.

[0040] c. Heat butylphthalide and oleic acid at 50°C to dissolve and stir evenly, and heat to 50°C before use.

[0041] d. Put the uniformly stirred capsule contents into the automatic soft capsule press machine, and press out soft capsules. The specific conditions are: the temperature of the content insulation barrel is 50°C, the air pressure is 0.5MPa, the heating temperature of the glue is 65°C, and the direct injection method is adopted. , spray washing temperature 44 ℃, rubber thickness 0.8mm.

Embodiment 2

[0043] Butylphthalide content 100mg / tablet

[0044]

[0045] Preparation:

[0046] a. Dibasic calcium phosphate and β-cyclodextrin are mixed uniformly to be a solid mixture;

[0047] b. Mix butylphthalide and oleic acid evenly to be a liquid mixture;

[0048] c. Add the liquid mixture of step b to the solid mixture of step a, stir, absorb the oil, and granulate;

[0049] d. Add Magnesium Stearate and total blend.

[0050] e. Tabletting to prepare a tablet with a butylphthalide content of 100 mg / tablet.

Embodiment 3

[0052] Soft capsules with butylphthalide content of 100mg / capsule

[0053]

[0054] The preparation method refers to Example 1.

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Abstract

The invention provides a butylphthalide preparation and a preparation method thereof. Specifically, the invention provides the butylphthalide preparation, and oleic acid is used as a solubilizing auxiliary material, so that the oral bioavailability of the butylphthalide preparation is improved, the individual difference is reduced, and the adverse reaction is reduced. The preparation has the advantages of being good in medicine stability, convenient to package, transport and store and the like, the preparation process is simple, and industrial production is easy.

Description

technical field [0001] The invention relates to a butylphthalide preparation and a preparation method thereof, in particular to a butylphthalide oral preparation. Background technique [0002] Butylphthalide is one of the main components of celery seed volatile oil. It is a domestic new drug of category 1.1. It is an anti-ischemic drug and is suitable for the treatment of mild and moderate acute ischemic stroke. Butylphthalide can increase cerebral perfusion, the number of capillaries, and cerebral blood flow in ischemic areas, improve energy metabolism in global cerebral ischemia, enhance protein synthesis, and protect neurons from various causes; it can also reduce cerebral edema, Protect mitochondrial function, increase antioxidant effect, thereby exert anti-apoptotic effect, and protect damaged brain cells. [0003] The chemical name of butylphthalide is (±)-3-butyl-1(3H)-isobenzofuranone, and its structural formula is as shown in formula (I), which is light yellow or c...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61K47/12A61P9/10
CPCA61K31/365A61K47/12A61P9/10
Inventor 邹德超陈先红
Owner BEIJING COLLAB PHARMA
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