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A kind of medicinal gelatin microsphere and preparation method thereof

A gelatin and microsphere technology, which is applied in the direction of making medicines into special physical or oral form devices, non-active components of polymer compounds, and bulk delivery, etc. inconvenience etc.

Active Publication Date: 2016-03-16
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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  • A kind of medicinal gelatin microsphere and preparation method thereof
  • A kind of medicinal gelatin microsphere and preparation method thereof
  • A kind of medicinal gelatin microsphere 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

Disclosed are a gelatin microsphere for pharmaceutical use and a preparation method thereof, with the active ingredient being trimetazidine or pharmaceutically acceptable salts thereof. The microsphere is prepared by a chemical cross-linking method comprising the steps of emulsifying, removing oil and water, chemical cross-linking, and washing and drying. Using particle size and appearance, encapsulation rate and drug loading rate of the microsphere as indexes, reagents such as carrier, oil phase, water removing and oil removing agent and cross-linking curing agent suitable for the microsphere of the present invention are optimally selected. The microsphere prepared according to the present invention has a particle size in the range of 50 to 200 µm and a drug loading rate of 30 to 35%.

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 Patents(China)
IPC IPC(8): A61K9/16A61K31/495A61K47/42A61J3/00
CPCA61K9/1658A61K31/495
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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