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A kind of microencapsulated butylphthalide pharmaceutical composition and its preparation method and application

A technology of microencapsulation and butylphthalide, applied in the field of medicine, can solve problems such as research reports on the preparation method of butylphthalide pharmaceutical composition that have not yet been found, and achieve the effects of improving drug release behavior, improving drug efficacy, and improving solubility

Active Publication Date: 2017-06-16
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

Recently, drug microencapsulation technology has been widely used in the pharmaceutical field. Various drugs are often used to make microcapsules, and then processed into various common dosage forms by adding other excipients, such as powders, tablets, capsules, granules, injections, Liquid suspensions, lotions, powder injections, paints, thin films, inhalants, etc., so far no research reports on microencapsulated butylphthalide pharmaceutical composition products and their preparation methods have been found

Method used

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  • A kind of microencapsulated butylphthalide pharmaceutical composition and its preparation method and application
  • A kind of microencapsulated butylphthalide pharmaceutical composition and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1 Preparation of Microencapsulated Butylphthalide Pharmaceutical Composition by Single Coagulation Method

[0048] Weigh 2.5 g of sodium alginate and 0.5 g of starch and dissolve them in distilled water so that the concentrations of sodium alginate and starch are 2.5% and 0.5% (w / w), respectively. Weigh 3.5g of racemic butylphthalide, dissolve it with a small amount of isooctane, add it to the sodium alginate-starch solution, use a stirrer to uniformly disperse at 200r / min to make an emulsion, add 25% CaCl 2 The sodium alginate is generated into calcium alginate to agglomerate into a capsule and solidified, filtered, washed with distilled water for 3-5 times, and vacuum dried for 12 hours to obtain a microencapsulated butylphthalide pharmaceutical composition.

Embodiment 2

[0049] Example 2 Preparation of microencapsulated butylphthalide pharmaceutical composition by complex aggregation method

[0050] Weigh 3 g of gelatin, add 20 ml of water to fully swell, and dissolve in heat preservation. Disperse 1.5 g of L-butylphthalide in the gelatin solution, and stir with a stirrer at 200 r / min for 30 minutes to an emulsified state. Weigh 1.4g gum arabic, prepare a 3.5% gum arabic solution, add the L-butylphthalide-gelatin solution to the gum arabic in a linear fashion at a certain speed, adjust the pH to 4.0-4.5 with hydrochloric acid, and use an ice water bath The solution was cooled to 5℃, the new microcapsules were cross-linked and solidified with 25% glutaric acid amide, the solution system was raised to room temperature, filtered, and the excess colloids and glutaric acid amide were washed with distilled water, and dried in vacuum for 12 hours to obtain Microencapsulated butylphthalide pharmaceutical composition.

Embodiment 3

[0051] Example 3 Preparation of microencapsulated butylphthalide pharmaceutical composition by spray drying method

[0052] Dissolve 10g methylcellulose and 15g sodium carboxymethylcellulose in distilled water to prepare spray liquids with concentrations of 10% and 15% respectively. Disperse 3g of L-butylphthalide in methylcellulose-carboxymethyl In the sodium cellulose solution, use a stirrer to stir at 200r / min for 30 minutes for spray drying. The inlet air temperature is 135-145°C, the outlet temperature is 65-80°C, the feeding speed is 10ml / min, and the compressed air flow rate is 600 NL / h to obtain the microencapsulated butylphthalide pharmaceutical composition.

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Abstract

The invention relates to a microencapsulated butylphthalide pharmaceutical composition, a preparation method and application thereof. In order to improve the solubility of butylphthalide, prevent volatilization, develop clinically required solid preparations and liquid preparations, so as to better exert the therapeutic effect of butylphthalide, the present invention microencapsulates butylphthalide. The microencapsulated butylphthalide pharmaceutical composition of the present invention contains 1-55% butylphthalide active ingredient by mass percentage, and utilizes natural or synthetic polymer materials as capsule material or carrier material to wrap butylphthalide into Microcapsules can be used to prepare powders, capsules, chewable tablets, embedded tablets, buccal tablets, other oral compressed tablets, injections, liquid suspensions, lotions, powder injections, paints, films and other dosage forms.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and relates to a pharmaceutical composition, specifically, to a microencapsulated butylphthalide pharmaceutical composition, and a preparation method and application thereof. Background technique [0002] Butylphthalidle (Butylphthalidle, NBP), also known as apigenin, is a natural compound extracted from celery seeds. It can also be artificially synthesized. Its structure contains a chiral carbon atom, so it There are two optical isomers, namely L-butylphthalide and D-butylphthalide, the chemical structure of which is as follows, [0003] . [0004] Butylphthalide is a light yellow clear oily liquid with a celery aroma and strong volatility. It is easily soluble in methanol, soluble in ethanol, ether and chloroform, but insoluble in water. Butylphthalide can shrink the infarcts after focal cerebral ischemia, increase 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 Patents(China)
IPC IPC(8): A61K9/50A61K31/365A61P9/10A61P25/28
Inventor 王金戌曹金娜耿佳
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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