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Medicinal gelatin microspheres and preparation method thereof

A technology of microspheres and gelatin, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, and devices that make drugs into special physical or ingestion forms, and can solve the problems of single varieties, poor dosage safety, and use Inconvenience and other issues

Active Publication Date: 2012-05-30
CHANGZHOU SIMM DRUG RES & DEV CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Trimetazidine or its pharmaceutically acceptable salt preparations are currently sold in the market mainly as ordinary tablets, which are single in variety and difficult to meet the needs of patients. Trimetazidine is absorbed rapidly and has a short elimination half-life. The daily dosage for adults is one day. 3 times, 20 mg each time, the concentration of trimetazidine in patients taking ordinary tablets is unstable and prone to large fluctuations, which is not conducive to treatment and prevention; It is also extremely inconvenient to use, so it is urgent to develop a preparation that can delay release in vivo

Method used

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  • Medicinal gelatin microspheres and preparation method thereof
  • Medicinal gelatin microspheres and preparation method thereof
  • Medicinal gelatin microspheres and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Trimetazidine Hydrochloride Gelatin Microspheres

[0024] 1 prescription

[0025]

[0026] 2 preparation steps

[0027] a. Emulsification: Weigh 0.596kg of trimetazidine hydrochloride and dissolve it in 440mL of 15% (w / v) gelatin solution, bathe in water at 60°C for 10 minutes, then slowly add the gelatin solution to preheat 60°C, and dissolve 3 % (w / v) in the liquid paraffin of mixed emulsifier, the oil-water volume ratio is 3: 1, and mixed emulsifier is made up of Span 80, 1% glyceryl monostearate by mass ratio (3: 1), while adding While stirring, the stirring speed is 200r / min, stirring for 20min;

[0028] b. Deoiling and dehydration: quickly cool the emulsion obtained in "a" to below 5°C in an ice-water bath, add 2000mL of a mixture of isopropanol and n-butanol, stir for 10min, and filter with suction;

[0029] c. Cross-linking and solidification: Take out the filter cake obtained in "b" and place it in a closed container, add 1000 mL of isopropanol solution c...

Embodiment 2

[0043] Trimetazidine Gelatin Microspheres

[0044] 1 prescription

[0045]

[0046] 2 preparation steps

[0047] a. Emulsification: Weigh 0.61kg of trimetazidine and dissolve it in 400mL of 20% (w / v) gelatin solution, bathe in water at 60°C for 15 minutes, then slowly add the gelatin solution to preheat 60°C, and dissolve 2% (w / v) In the liquid paraffin of the mixed emulsifier, the oil-water volume ratio is 4:1, and the mixed emulsifier is composed of Span 85 and Tween-20 according to the mass ratio (4:1), stirring while adding, the stirring speed 300r / min, stirring for 30min;

[0048] b. Deoiling and dehydration: quickly cool the emulsion obtained in "a" to below 5°C in an ice-water bath, add 1600mL of isopropanol, stir for 5min, and filter with suction;

[0049] c. Cross-linking and curing: take out the filter cake obtained in "b" and put it in a closed container, add 800mL of isopropanol solution containing 10% (v / v) formaldehyde, put it in an environment below 5°C for ...

Embodiment 3

[0063] Determination of Plasma Concentration of Trimetazidine Hydrochloride Sustained Release Gelatin Microspheres

[0064] Healthy subjects were divided into two groups, one group was given trimetazidine hydrochloride tablets sold on the market, one tablet every 8 hours, each containing 20 mg of medicine, and one group was given trimetazidine hydrochloride sustained-release gelatin microspheres, once every 12 hours, 0.1g each time, monitor the blood drug concentration for 24 hours, take 4ml of venous blood at 0.5, 1, 2, 2.5, 3, 6, 8, 12, 14, 16, 20, 24 points in total after taking the medicine, and measure Blood concentration, (see appendix Figure 7 )

[0065] Depend on Figure 7 , the plasma concentration of trimetazidine hydrochloride gelatin microspheres was more stable than that of trimetazidine hydrochloride tablets, and the difference between peak and trough was smaller, indicating that trimetazidine hydrochloride gelatin microspheres had sustained-release characteri...

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Abstract

The invention relates to medicinal gelatin microspheres and a preparation method thereof, and belongs to the field of medicine preparation. The active ingredient of the medicinal gelatin microspheres is trimetazidine or a medicinal salt of the trimetazidine. The preparation of the microspheres adopts a chemical cross-linking method, and comprises steps of emulsification, deoiling and dewatering, chemical cross-linking, washing and drying, and the like. According to the preparation method, the particle size, the appearance, the encapsulation efficiency, the drug loading rate are adopted as indexes to comprehensively optimize the carrier, the oil phase, the dewatering and deoiling agent, the cross-linking curing agent, and other reagents added in the process, wherein the carrier, the oil phase, the dewatering and deoiling agent, the cross-linking curing agent, and other reagents are suitable for preparation of the microspheres of the present invention. The prepared microspheres have characteristics of smooth surface, particle size of 50-200 mum, drug loading rate of 30-35%, and has a slow release effect under the common dissolution conditions. In addition, the blood drug level of the microspheres is stable in vivo, and is better than the blood drug level of ordinary tablets.

Description

technical field [0001] The invention relates to a pharmaceutical gelatin microsphere containing an active ingredient trimetazidine or a pharmaceutically acceptable salt thereof and a preparation method thereof. technical background [0002] Trimetazidine or its pharmaceutically acceptable salt preparations are currently sold in the market mainly as ordinary tablets, which are single in variety and difficult to meet the needs of patients. Trimetazidine is absorbed rapidly and has a short elimination half-life. The daily dosage for adults is one day. 3 times, 20 mg each time, the concentration of trimetazidine in patients taking ordinary tablets is unstable and prone to large fluctuations, which is not conducive to treatment and prevention; It is also extremely inconvenient to use, so there is an urgent need to develop a preparation that can delay release in vivo. Contents of the invention [0003] One of the objectives of the invention: to provide a slow-release gelatin mi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/495A61K47/42A61J3/00
CPCA61K31/495A61K9/1658
Inventor 顾书华张继稳翁秋萍张超李庆宜谢和兵
Owner CHANGZHOU SIMM DRUG RES & DEV CENT
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