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Captopril sustained-release microcapsule and preparation method thereof

A technology of sustained-release microcapsules and inner core layers, applied in microcapsules, capsule delivery, pharmaceutical formulations, etc., can solve problems such as unfavorable human health, dizziness, headaches, gastrointestinal disorders, etc., to improve sustained-release performance and prolong storage. Duration, the effect of improving the therapeutic effect

Pending Publication Date: 2022-01-14
HUAZHONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The most common one on the market is to make captopril into tablets, but captopril tablets will slowly degrade into toxic captopril disulfide, basically every 3 months at about 0.2% Incrementally, taking captopril tablets that have been stored for a long time is not conducive to human health. In addition, since the biological half-life of captopril is only 1.9h, it needs to be taken 3-4 times a day. When the total intake reaches 37.5-75.0 The effect can only be maintained for 6-8 hours at mg
Clinically, in order to improve the curative effect, it is usually achieved by increasing the agent to prolong the action time in the body, resulting in the phenomenon of "peaks and troughs"
This large "peak and trough" concentration difference may cause dizziness, headache, gastrointestinal disorders and other adverse reactions

Method used

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  • Captopril sustained-release microcapsule and preparation method thereof
  • Captopril sustained-release microcapsule and preparation method thereof
  • Captopril sustained-release microcapsule and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0038] A captopril slow-release microcapsules, comprising an outer shell and an inner core layer, the inner core layer is a modified pseudophysalis seed material, the inner core layer wraps captopril, and the outer shell layer is chitosan quaternary An amine salt material, the outer shell layer covers the inner core layer. The mass ratio of the modified pseudophysalis seeds, the captopril and the chitosan quaternary ammonium salt is 1:0.5:1.5.

[0039] The modified pseudophysalis seeds are prepared through chemical modification and graft modification.

[0040] The specific operation method of the chemical modification is as follows: dry, pulverize and sieve the pseudophysalis seeds, add an aqueous solution 20 to 30 times the weight of the pseudophysalis seed powder and swell for 36 to 60 hours, and then add an acidic pH regulator Adjust the pH to 3-6, hydrolyze at 90-100° C. for 10-24 hours, and finally concentrate under vacuum to 15-30% of the original volume to obtain a con...

Embodiment 2

[0047] A captopril slow-release microcapsules, comprising an outer shell and an inner core layer, the inner core layer is a modified pseudophysalis seed material, the inner core layer wraps captopril, and the outer shell layer is chitosan quaternary An amine salt material, the outer shell layer covers the inner core layer. The mass ratio of the modified pseudophysalis seeds, the captopril and the chitosan quaternary ammonium salt is 1.5:0.7:2.5.

[0048] The modified pseudophysalis seeds are prepared through chemical modification and graft modification.

[0049] The specific operation method of the chemical modification is as follows: dry, pulverize and sieve the pseudophysalis seeds, add an aqueous solution 20 to 30 times the weight of the pseudophysalis seed powder and swell for 36 to 60 hours, and then add alkaline pH adjustment The pH is adjusted to 8-10 with an agent, hydrolyzed at a temperature of 90-100°C for 10-24 hours, and finally concentrated under vacuum to 15-30%...

Embodiment 3

[0056] A captopril slow-release microcapsules, comprising an outer shell and an inner core layer, the inner core layer is a modified pseudophysalis seed material, the inner core layer wraps captopril, and the outer shell layer is chitosan quaternary An amine salt material, the outer shell layer covers the inner core layer. The mass ratio of the modified pseudophysalis seeds, the captopril and the chitosan quaternary ammonium salt is 2:0.8:3.

[0057] The modified pseudophysalis seeds are prepared through chemical modification and graft modification.

[0058] The specific operation method of the chemical modification is as follows: dry, pulverize and sieve the pseudophysalis seeds, add an aqueous solution 20 to 30 times the weight of the pseudophysalis seed powder and swell for 36 to 60 hours, and then add an acidic pH regulator Adjust the pH to 3-6, hydrolyze at 90-100° C. for 10-24 hours, and finally concentrate under vacuum to 15-30% of the original volume to obtain a conce...

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Abstract

The invention discloses a captopril sustained-release microcapsule. The captopril sustained-release microcapsule comprises a shell layer and an inner core layer, the inner core layer is made of a modified nicandra physaloides seed material, captopril is wrapped by the inner core layer, the shell layer is made of a chitosan quaternary ammonium salt material, and the inner core layer is wrapped by the shell layer. Nicandra physaloides seeds are primarily modified by a chemical method, then the Nicandra physaloides seeds are further modified by a grafting modification method, the modified Nicandra physaloides seeds with significantly improved slow-release performance are prepared, and the slow-release performance of the slow-release microcapsule is further improved through a synergistic effect of the modified Nicandra physaloides seeds and chitosan quaternary ammonium salt; the captopril is wrapped in the inner core, so that the captopril is further prevented from being degraded into captopril disulfide, and the generation of impurities is reduced; and the captopril sustained-release tablet can be slowly and stably released, so that the purposes of sustained administration and sustained treatment are achieved, and the curative effect of captopril medicine can be improved to the greatest extent.

Description

technical field [0001] The invention belongs to the technical field of preparation of pharmaceutical preparations, and in particular relates to a captopril sustained-release microcapsule and a preparation method thereof. Background technique [0002] Captopril (captopril, also known as captopril, Kaibotong) is the first orally effective representative drug of angiotensin converting enzyme inhibitor (Angiotensin converting enzyme inhibitor, ACEI) developed by Squibb company in the United States . Captopril is a white or off-white crystal or crystalline powder, with a special odor similar to garlic, tasteless, melting point 104-110°C, specific rotation -126--132°; easily soluble in methanol, ethanol, Chloroform and acetone are slightly soluble in water, and their chemical structural formula is shown in formula I: [0003] [0004] Captopril is mainly used clinically to treat diseases such as hypertension, heart failure and glomerulus, and its main pharmacological effects ...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/401A61K47/36A61K47/46A61P9/12A61P9/04A61P13/12
CPCA61K9/5036A61K9/5063A61K9/5073A61K9/5089A61K31/401A61P9/12A61P9/04A61P13/12
Inventor 邓伟吴淑梅詹顺昌王洪伟
Owner HUAZHONG PHARMA
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