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Ciclosporin A proliposome, pharmaceutical composition and preparation method thereof

A proliposome, cyclosporine technology, applied in the directions of drug combination, liposome delivery, pharmaceutical formulation, etc., can solve the problems of poor oral absorption and low bioavailability of breviscapine, and achieve the promotion of oral absorption, Simplified process steps and good stability

Active Publication Date: 2011-04-13
SHENZHEN NEPTUNUS PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the Chinese patent (authorized announcement number CN1444948B) "breviscapine liposome and its preparation method", Deng Yingjie et al. described a breviscapine proliposome, which improved the poor oral absorption and bioavailability of breviscapine. Insufficiency of low density, and improve the stability of liposome formulations

Method used

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  • Ciclosporin A proliposome, pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1, cyclosporin A proliposome and its suspension preparation

[0030] Weigh 500 mg of cyclosporin A, 4000 mg of hydrogenated soybean lecithin, 1500 mg of cholesterol and 100 mg of vitamin E, add 50 mL of ethanol and ultrasonically dissolve to obtain solution (1). Weigh 18.0 g of sorbitol, pulverize it in a universal grinder, sieve, put the sorbitol powder in a round-bottomed flask, add solution (1), and rotate under reduced pressure at 54 °C until ethanol volatilizes completely to obtain dry The white powder was taken out, sieved, and oven-dried at 40°C for 1 hour to obtain cyclosporine A proliposome.

[0031] Disperse an appropriate amount of this product in water and shake to obtain a translucent cyclosporine A liposome suspension. The encapsulation efficiency was determined by micro-column centrifugation, and the result was greater than 85%.

Embodiment 2

[0032] Embodiment 2, the preparation of cyclosporin A proliposomal capsule

[0033] Weigh 18.9 g of cyclosporin A proliposome powder prepared in Example 1, 2.5 g of microcrystalline cellulose, 1.2 g of crospovidone and 0.25 g of colloidal silicon dioxide, mix uniformly, and fill to a size of 0 hard In capsule shell, ready to serve.

Embodiment 3

[0034] Embodiment 3, cyclosporin A proliposome preparation process

[0035] Get 1.8kg of sorbitol, grind and sieve for subsequent use. Take 50.0g of cyclosporin A, 400.0g of hydrogenated soybean lecithin, 150.0g of cholesterol and 10.0g of vitamin E, dissolve them in propylene glycol, and spray the resulting solution on the above-mentioned sorbitol powder by spraying at the bottom of the fluidized bed, dry, and sieve , that is.

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Abstract

The invention discloses a ciclosporin A proliposome for oral administration, a pharmaceutical composition and a preparation method thereof. The ciclosporin A proliposome comprises the following pharmaceutical active ingredients and non-active ingredients by weight percent: 1-25% of ciclosporin A, 2-40% of lecithin, 0.5-12.5% of cholesterol, 21-96.45% of polyol and 0.05-1.50% of vitamin E. The proliposome is prepared from the ciclosporin A, a lipid membrane material, a hydrophilic matrix and the like through the ultrasonic dispersion method and the reverse phase evaporation method, and a liposome is formed spontaneously after the dispersion in water. The proliposome can improve the dispersity and the oral bioavailability of ciclosporin A which is an insoluble drug, lead the stability to be good and be more applicable to industrial production in comparison with the ordinary liposome.

Description

technical field [0001] The invention relates to a cyclosporin A proliposome preparation and a preparation method thereof. Background technique [0002] Cyclosporin A (C 62 h 111 N 11 o 12 ) is a cyclic polypeptide composed of 11 amino acids. It is a potent immunosuppressant that can specifically and reversibly act on lymphocytes without affecting the functions of hematopoietic and phagocytic cells. It has been widely used in the anti-rejection reaction of organ transplant patients and various autoimmune diseases, and is an important clinical drug. Because cyclosporin A has poor water solubility and low oral bioavailability, it is of great significance to design a reasonable dosage form for it. Oral administration of cyclosporine A is the first choice. At present, the marketed products at home and abroad include oral solutions, capsules and self-emulsifying soft capsules. Wherein, the oral solution is a non-aqueous solution, which needs to be mixed with drinks such as m...

Claims

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Application Information

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IPC IPC(8): A61K38/13A61K9/127A61K9/10A61K9/14A61K9/20A61K9/48A61K47/28A61P37/06
Inventor 李宁王志国崔婧王丽丽
Owner SHENZHEN NEPTUNUS PHARM CO LTD
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