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Sirolimus lipidosome freeze-dried acanthopanax powder and technique of preparing the same

A technology for sirolimus liposome and freeze-dried powder injection, which is applied in the field of sirolimus liposome freeze-dried powder injection and its preparation technology, can solve the problems of low bioavailability of sirolimus and the like, and achieves prolonged blood circulation. Circulation time, improved efficacy, improved bioavailability

Inactive Publication Date: 2008-02-27
山东华诺生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to overcome the deficiencies of the prior art, to solve the problem of low bioavailability of sirolimus, to provide a sirolimus with good stability, high encapsulation efficiency, low cost and little side effects Liposome lyophilized powder for injection, and a preparation process for the liposome lyophilized powder for injection

Method used

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  • Sirolimus lipidosome freeze-dried acanthopanax powder and technique of preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Prepare raw materials with the following weights or volumes:

[0057] Sirolimus 500mg

[0058] Soy Lecithin 2.3g

[0059] Cholesterol 1g

[0060] Vitamin E 21mg

[0061] Phosphate buffer (p H7.4, 0.01mol / L) 300ml

[0062] Mannitol 100g

[0063] Chloroform 400ml

[0064] Sodium chloride 9g

[0065] Water for injection 1000ml

[0066] Dissolve sirolimus, phospholipids, cholesterol, and vitamin E in chloroform according to the weight ratio of raw materials in the formula and mix uniformly; remove the organic solvent in the solution under reduced pressure with a rotary evaporator (temperature is not higher than 40° C.), and A lipid film is formed on the glass bottle wall; add 300ml of isotonic phosphate buffer (pH6-7.4, 0.01mol / L, containing 0.9% Nacl), stir for 30min, and place it at room temperature for 2h to make the film imbibition; Stir at room temperature for 2 hours to obtain an aqueous liposome suspension; the obtained aqueous liposome suspension is processe...

Embodiment 2

[0068] Prepare raw materials with the following weights or volumes:

[0069] Sirolimus 1000mg

[0070] Egg yolk lecithin 7g

[0071] Distearoylphosphatidylcholine 5g

[0072] Cholesterol 7g

[0073] Vitamin E 100mg

[0074] Phosphate buffer (p H7.4, 0.01mol / L) 300ml

[0075] Mannitol 150g

[0076] Chloroform 500ml

[0077] Sodium chloride 9g

[0078] Water for injection 1000ml

[0079] Sirolimus, phospholipid, cholesterol, vitamin E are dissolved in 2: 1 chloroform-ethanol mixed solvent according to the weight ratio of raw material in the formula and mix homogeneously; With rotary evaporator, the organic solvent in the solution is removed under reduced pressure (temperature not higher than 40°C), a lipid film is formed on the glass bottle wall; add 300ml of isotonic phosphate buffer (p H6-7.4, 0.01mol / L, containing 0.9% Nacl), stir for 30min, and place at room temperature 2h, make film imbibition; Stir at room temperature 2h again, obtain liposome water suspension; 0...

Embodiment 3

[0081] Prepare raw materials with the following weights or volumes:

[0082] Sirolimus 1000mg

[0083] Soy Lecithin 3g

[0084] Distearoylphosphatidylcholine 5g

[0085] Cholesterol 7g

[0086] Vitamin E 100mg

[0087] Phosphate buffer (pH7.4, 0.01mol / L) 300ml

[0088] Mannitol 150g

[0089] Chloroform 500ml

[0090] Sodium chloride 9g

[0091] Water for injection 1000ml

[0092] Sirolimus, phospholipid, cholesterol, vitamin E are dissolved in 2: 1 chloroform-ethanol mixed solvent according to the weight ratio of raw material in the formula and mix homogeneously; With rotary evaporator, the organic solvent in the solution is removed under reduced pressure (temperature Not higher than 40°C), a lipid film is formed on the glass bottle wall; add 300ml of isotonic phosphate buffer (pH6-7.4, 0.01mol / L, containing 0.9% Nacl), stir for 30min, and place at room temperature for 2h , to make the film imbibition; then stirred at room temperature for 2 hours to obtain an aqueous li...

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Abstract

The invention discloses a xiluomosi liposome freeze dried and making technique, which comprises the following steps: selecting liposome component, buffer, organic solvent, antioxidant and freeze-drying protective as raw material; adopting film diffusion method to make the liposome turbid liquor with xiluomosi through high-pressure or hypersonic dispersing method evenly; drying the liposome to improve the storage stability obviously; dispersing the freeze dried at random proportion in the water evenly without any sediment and impurity; making the packing rate of liposome at 96% with the grain size at 50-250nm; improving the drug effect greatly in comparison with oral agent; lengthening the circulating time in the blood; elevating the biological utility of drug.

Description

Technical field: [0001] The present invention relates to a preparation of sirolimus, that is to say a liposome freeze-dried powder for injection containing sirolimus and a preparation method thereof, specifically sirolimus liposome freeze-dried powder and Its preparation process. Background technique: [0002] Sirolimus (Sirolimus, Rapamune, also known as rapamycin) is a metabolite of the hygroscopic Streptomyces AYB P44 isolated from the soil of Easter Mountain Island in the Pacific Ocean by scientists from the Ayerst Research Institute in Canada in the early 1970s. The product, with a relative molecular mass of 914.2, was initially used as a low toxicity antifungal antibiotic. In 1978, it reported its immunosuppressive activity in rat adjuvant arthritis and experimental allergic meningitis models, and began related basic and clinical experiments. Experiments show that it not only has a significant curative effect on various autoimmune abnormalities, but also shows signif...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/436A61K9/127A61K9/19A61K47/28A61P37/06
Inventor 许振华
Owner 山东华诺生物科技有限公司
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