Asiatic acid injectable sustained-release microballoons and preparation method thereof

A technology of asiatic acid and slow-release microspheres, which is applied in the direction of pharmaceutical formulas, medical preparations containing no active ingredients, medical preparations containing active ingredients, etc., can solve the problems of low blood drug concentration and poor oral absorption, and achieve Good biocompatibility, low manufacturing cost, and stable preparation technology

Inactive Publication Date: 2009-07-08
ZHEJIANG ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Asiaticoside has clear efficacy, but its oral absorption is poor, and its blood concentration is extremely low

Method used

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  • Asiatic acid injectable sustained-release microballoons and preparation method thereof
  • Asiatic acid injectable sustained-release microballoons and preparation method thereof
  • Asiatic acid injectable sustained-release microballoons and preparation method thereof

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preparation example Construction

[0017] The preparation steps of asiatic acid injectable slow-release microspheres of the present invention are as follows:

[0018] 1. Take 2% glacial acetic acid solution as solvent, add chitosan, fully swell, stir to dissolve, filter, discard insoluble matter, and make into 5% concentration (W / V).

[0019] 2. Asiatic acid (particle diameter<10 μ m, chromatographic purity greater than 90%) is added in the above-mentioned 5% chitosan solution and mixes uniformly as the water phase (the addition of Asiatic acid is 0.5-2 times of chitosan (W / W)); under the condition of mechanical stirring (800-1200r / min), slowly add the water phase to the oil phase containing emulsifier, and keep stirring for 5-10min to form a water-in-oil type (W / O) Emulsion.

[0020] 3. Under stirring at 200r / min, control the temperature at 25-30°C, add the crosslinking agent dropwise to the emulsion in an amount of 1-2ml, and cure for 1-6h. The solid microspheres are collected, washed and dried to obtain ...

Embodiment 1

[0024] Weigh 1 g of chitosan (molecular weight 200 kDa), add 20 ml of 2% glacial acetic acid solution to fully swell, stir to dissolve, filter, discard insoluble matter, and make into 5% concentration (W / V). Add 448 mg of asiatic acid (particle size<10 μm) into 4 ml of the above 5% chitosan solution, mix well as the water phase. Under the condition of mechanical stirring (900r / min), slowly add dropwise in the liquid paraffin (80ml) that contains 1.6g Span-80, keep stirring for 5min, make to form water-in-oil type (W / O) emulsion; Under stirring, control the temperature at 25-30°C, add 1.5ml of 25% glutaraldehyde solution, solidify for 1 hour, filter, wash with petroleum ether, distilled water, petroleum ether / isopropanol (1:1) and petroleum ether, and dry in vacuum , to obtain asiatic acid sustained-release microspheres. The drug-loading capacity of the microspheres is 15.6%, and the cumulative release in 24 hours (release on the first day): 9.6%.

Embodiment 2

[0026] Weigh 1 g of chitosan (molecular weight 126 kDa), add 20 ml of 2% glacial acetic acid solution to fully swell, stir to dissolve, filter, discard insoluble matter, and make into 5% concentration (W / V). Add 224mg of Asiatic acid (particle size<10 μm) into the above 4ml 5% chitosan solution, and mix well as the water phase. Under the condition of mechanical stirring (1000r / min), slowly add it dropwise into the liquid paraffin (80ml) containing 1.6g Span-80, keep stirring for 10min to form water-in-oil (W / O) emulsion; at 200r / min Under stirring, control the temperature at 25-30°C, add 2ml of 25% glutaraldehyde solution, solidify for 3 hours, filter, wash with petroleum ether, distilled water, petroleum ether / isopropanol (1:1) and petroleum ether, and dry in vacuum. The asiatic acid sustained-release microspheres were obtained. The drug loading amount of the microspheres is 7.8%, and the cumulative release in 24 hours (release amount on the first day): 10.5%.

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Abstract

The invention relates to the technical field of pharmaceutical preparation, in particular to an asiatic acid sustained-release microsphere used for injection and a preparation method thereof. A biodegradable chitosan is taken as a carrier, an asiatic acid is taken as principal agent, and the asiatic acid sustained-release microsphere used for injection is obtained by the technology of cross-linked emulsion. Due to the obtained medicament carried microspheres, the surfaces are relatively smooth; the particle diameters range from 20mum to 110mum; and the medicament loading rate of the microspheres ranges from 4.8% to 15.6%. The asiatic acid microsphere has the characteristics that the burst effect is modest (the burst size on the first day is smaller than 15%); the release rate is stable; the sustained release time is long (4-10 weeks); and the asiatic acid microsphere is biodegradable. The implantation and the removal by operation before and after the medicament is used are avoided.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a biodegradable asiatic acid injectable sustained-release microsphere preparation capable of prolonging the drug action time. Background technique [0002] Centella asiatica (L) Urban is the dry or rooted whole plant of Centella asiatica (L) Urban, which has the effects of clearing heat and dampness, detoxifying and reducing swelling (Zhang Leilei, et al. Research on the chemical constituents of Centella asiatica[ J]. Chinese herbal medicine, 2005, 36 (12): 1761-1763.), its active ingredients asiaticoside, hydroxyasiaticoside, and asiaticoside extract, etc. can significantly soften the connective tissue and make the tissue Uniform growth, commonly used in the treatment of scars associated with beautification of the skin (WS 3 -B-2596-97-2002 drug standard), has been widely used clinically in my country, Europe and Southeast Asia. [0003] Ordinary oral prepa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/56A61K47/36A61P17/02
Inventor 王胜浩尹丽娜
Owner ZHEJIANG ACAD OF MEDICAL SCI
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