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Thymalfasin sustained-release microsphere preparation and preparation method thereof

A new technology of sustained-release microsphere preparation and thymus method, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., and can solve problems such as difficulties in clinical application.

Inactive Publication Date: 2011-06-29
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The drug loading of thymofaxin sustained-release microspheres prepared in his articles and patents is not more than 0.9%, which brings great difficulties to practical clinical application

Method used

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  • Thymalfasin sustained-release microsphere preparation and preparation method thereof
  • Thymalfasin sustained-release microsphere preparation and preparation method thereof
  • Thymalfasin sustained-release microsphere preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Weigh 300mg of thymofasin and 200mg of gelatin and dissolve in 1ml of water for injection as the internal water phase; weigh 4g of glycolide-lactide copolymer and dissolve in 10ml of dichloromethane as the oil phase; add the oil phase to the internal In the water phase, use high-speed stirring (20000rpm) for 15 seconds to obtain colostrum and store it in an environment below 20 °C; add this colostrum to 5000 ml of 0.5% (W / V) polyvinyl alcohol under stirring The solution was double-emulsified, and the double-emulsion was continuously stirred for 3 hours to evaporate dichloromethane, centrifuged and washed to collect microspheres, the particle size of which was less than 100 microns, and the drug loading was 6.1%.

Embodiment 2

[0028] Weigh 500mg thymofasin and 300mg gelatin and dissolve in 2ml water for injection as the inner water phase; weigh 8g glycolide-lactide copolymer and dissolve it in 80ml dichloromethane as the oil phase; add the oil phase to the inner In the water phase, use an ultrasonic cell breaker (Branson S-250D) to perform ultrasonication for 10 seconds to obtain colostrum, which is stored in an environment below 20°C; add this colostrum to 8000 ml of 1.0% (W / V) polyvinyl alcohol solution to obtain double emulsion, the double emulsion was continuously stirred for 3 hours to evaporate dichloromethane, centrifuged and washed to collect microspheres, the particle size of the microspheres was less than 50 microns, and the drug loading was 4.5%.

Embodiment 3

[0030] Determination of release in vitro of thymofaxin sustained-release microspheres

[0031] The Thymusfaxin slow-release microsphere preparation prepared by the above-mentioned examples was tested for release in vitro, and the assay method was as follows: accurately weigh 100 mg of the drug-containing microsphere and place it in a 10 ml stoppered test tube, and use pH 7.4 phosphate buffer ( Containing 0.02% sodium azide as a bacteriostatic agent, 0.05% Tween 80 as a wetting agent) 10ml as a release medium, placed in a constant temperature water bath shaker, at a shaking speed of 100rpm, and a temperature of 37°C±0.5°C. In vitro release assay of microspheres. On 1d, 2d, 4d, 7d, 14d, 21d, and 28d, 0.5ml of release medium was used to determine the content of thymus method by high performance liquid chromatography, and fresh release medium was added. figure 1 , 2 The in vitro cumulative release curves of the Thymofaxin sustained-release microsphere preparations prepared in E...

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Abstract

The invention provides a thymalfasin sustained-release microsphere preparation and a preparation method thereof. The thymalfasin sustained-release microsphere preparation comprises the following components in percentage by weight: 0.1 to 10 percent of thymalfasin, and 85 to 99 percent of poly(glycolide-co-lactide), wherein the poly(glycolide-co-lactide) is copolymer of glycolide and lactide, the ratio of the glycolide to the lactide is (25:75)-(75:25), the molecular weight of the poly(glycolide-co-lactide) is between 5,000 and 35,000 dalton, and the intrinsic viscosity is between 0.1 and 0.5dL / g. The pH value of the external water phase of the thymalfasin sustained-release microsphere preparation is between 3.0 and 5.0, and can be regulated by adopting acetic acid, hydrochloric acid, sulfuric acid and the like. The inventor discovers that by controlling the pH value of the external water phase, the stability of the thymalfasin can be improved and the entrapment rate in a preparation process also can be improved, so that the drug-loading rate of sustained-release microspheres can be improved.

Description

technical field [0001] The invention relates to pharmaceutical preparations of polypeptide drugs and a preparation method thereof, in particular to a Thymofaxin slow-release microsphere preparation and a preparation method thereof. Background technique [0002] Thymosin is an important regulator of T lymphocytes discovered in 1984 and secreted by the thymus, which is related to the regulation of cellular immunity. Thymalfasin as an immune modulator, its good curative effect has been confirmed, the clinical application prospect is extremely bright. In the case of hepatitis B, hepatitis B virus (HBV) infection is one of the most common viral infections in humans. There are about 300 million people with chronic HBV infection in the world, most of them in Asia. Chronic HBV carriers account for about 10%-15% of the population in my country, and cirrhosis and hepatocellular carcinoma occur in 2% and 1% of chronic hepatitis B (CHB) patients every year, respectively. Obviously, i...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K38/22A61K47/34A61P37/02A61K47/10A61K47/26
Inventor 陶安进袁建成马亚平郑春莲
Owner HYBIO PHARMA
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