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Sirolimus micro-emulsion particles and preparation method and application thereof

A technology of micro- and micro-emulsion granules of sirolimus, applied in the field of pharmaceutical preparations, can solve problems to be improved, etc., and achieve the effects of good stability and simplified operation steps

Active Publication Date: 2014-03-26
HUBEI BIO PHARMA IND TECHCAL INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Therefore, the current sirolimus pharmaceutical preparations still need to be improved.

Method used

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  • Sirolimus micro-emulsion particles and preparation method and application thereof
  • Sirolimus micro-emulsion particles and preparation method and application thereof
  • Sirolimus micro-emulsion particles and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] Embodiment 1, preparation of sirolimus microemulsion particles

[0081] Add 2 g of polyethylene glycol 4000 (Tianjin Tiancheng Pharmaceutical Co., Ltd., Zhunzi H12020043), poloxamer 188 (registration number F20130004, BASF, Germany) 8 g, and 10 g of glycerin into 160 mL of purified water; then add sirolimus Mix 25g evenly, heat and stir in a water bath at 80°C until it reaches a molten state, use a high-speed tissue masher to shear and stir at a speed of 8000 rpm, and shear and stir for 30 minutes to obtain a primary microemulsion, which is then circulated and emulsified by a high-pressure homogenizer 4 times to obtain a microemulsion, and then spray drying to obtain 41.4 g of sirolimus microemulsion particles with a yield of 92.0%.

Embodiment 2

[0084] Embodiment 2, preparation of sirolimus microemulsion particles

[0085] Add 60g of polyethylene glycol 4000, 240g of poloxamer 188, and 100g of glycerin into 3000mL of purified water; then add 50g of sirolimus and mix well, heat and stir in a water bath at 80°C until it melts, and use a high-speed tissue grinder to shear and stir , the rotating speed is 10000 rpm, shearing and stirring for 20 minutes to obtain the primary microemulsion, and then circulate and emulsify for 4 times through the high-pressure homogenizer to obtain the microemulsion, and then freeze-dry in a large plate to obtain 430 g of sirolimus microemulsion particles. The rate is 95.6%.

Embodiment 3

[0088] Embodiment 3, preparation of sirolimus microemulsion particles

[0089] Add 100 g of polyethylene glycol 4000, 400 g of poloxamer 188, and 150 g of glycerin into 3900 mL of water for injection; then add 100 g of sirolimus and mix evenly, heat and stir in a water bath at 80°C until it melts, and use a high-speed tissue grinder to shear Cutting and stirring, the rotating speed is 10000 rpm, shearing and stirring for 20 minutes to obtain the primary microemulsion, and then circulate emulsification 4 times through the high-pressure homogenizer to obtain the microemulsion, then spray dry to obtain 709g of sirolimus microemulsion particles, Yield 94.5%.

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Abstract

The invention provides sirolimus micro-emulsion particles and a preparation method and an application thereof. The sirolimus micro-emulsion preparation and sirolimus micro-emulsion particles are prepared from the following steps: mixing an emulsifier, a co-emulsifier and water; adding sirolimus into the mixture obtained, and heating up to a melting state at a temperature ranging from 70 DEG C to 90 DEG C; shearing and stirring the mixture in the melting state by adopting a high speed tissue stamping machine, wherein the shearing and stirring rotating speed is 8000-12000r / m, and the shearing and stirring time is 10-30 minutes to obtain an initial micro-emulsion; circularly emulsifying the initial micro-emulsion to obtain a micro-emulsion; and drying the micro-emulsion to obtain the sirolimus micro-emulsion particles. The stability of the sirolimus preparation provided by the invention is improved, the dissolution rate of the preparation is improved, and the bioavailability is increased.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a sirolimus microemulsion preparation. Specifically, the invention relates to a sirolimus microemulsion preparation subjected to microemulsification treatment and a preparation method and application thereof. Background technique [0002] Sirolimus, also known as rapamycin, has the following structural formula: [0003] [0004] Sirolimus is a new type of macrolide immunosuppressant, which was first developed by Wyeth Pharmaceuticals. It was first launched in the United States in October 1999. As a relatively safe drug, it is used clinically to prevent and treat renal transplant rejection. , It can also be used for the maintenance use of the prevention of renal transplant rejection after withdrawal of cyclosporine in patients using HAART. In recent years, sirolimus has been found to play an important role in the prevention of rejection after allogeneic kidne...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/436A61K47/34A61K47/38A61K47/32A61P37/06A61P13/12A61P9/12
Inventor 张绪文黄璐许勇
Owner HUBEI BIO PHARMA IND TECHCAL INST
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