Solid dispersion of protopanaxadiol and preparation method thereof

A technology of protopanaxadiol and solid dispersion, which is applied in the field of medicine to achieve the effect of accelerating the dissolution rate and increasing the solubility

Inactive Publication Date: 2006-12-20
浙江金石亚药医药科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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And the research of protopanaxadiol solid dis

Method used

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  • Solid dispersion of protopanaxadiol and preparation method thereof

Examples

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Example Embodiment

[0047] Example 1

[0048] Take 800mg of polyvinylpyrrolidone K30 and 200mg of 20(S)-protopanaxadiol, mix them evenly, put them in a mortar and grind them at a speed of 200rpm for 30min. Take it out and pass through a 100-mesh sieve. The solid dispersion of the invention has an in vitro cumulative dissolution rate of 40.5±2.3% (n=6) within 45 minutes.

Example Embodiment

[0049] Example 2

[0050]Take 4000 mg of microcrystalline cellulose and 200 mg of 20(R)-protopanaxadiol, mix them evenly, and grind them in a mortar with a rotation speed of 100 rpm and a grinding time of 60 minutes. Take it out and pass through an 80-mesh sieve. The cumulative dissolution rate of the solid dispersion of the invention is 48.7±1.4% (n=6) in 45 minutes in vitro.

Example Embodiment

[0051] Example 3

[0052] Take 1600mg of poloxamer-188 and 200mg of 20(S)-protopanaxadiol in an evaporating dish, heat and stir on a water bath at 60°C until completely melted, and then place the melt in an ice-salt bath under vigorous stirring. Cool to solid, place it in a desiccator at room temperature and dry for 2 days, take it out, grind it, and pass it through a 60-mesh sieve. The solid dispersion of the invention has an in vitro cumulative dissolution rate of 98.1±3.4% (n=6) within 45 minutes.

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Abstract

The invention provides a protopanaxadiol solid dispersion and its preparing method, wherein the weight ratio of the protopanaxadiol and carrier material is 1:1-50, and protopanaxadiol solid dispersion can be prepared through melting method, solvent method, solvent-melting method, grinding method, spray-drying method or freeze drying method. The preparation can be made into the dosage forms of capsules, tablets, suppositories and drop pills.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a protopanaxadiol solid dispersion and a preparation method thereof. Background technique [0002] Screening antitumor active ingredients from traditional Chinese medicine has become one of the hot spots in international research. Tonic ginseng has been used in Asian countries for thousands of years, and its main active ingredient is ginsenoside, which has various pharmacological activities. In recent years, researchers at home and abroad have found that ginsenosides Rg3, Rh2, C-K (Compound K) and aglycones protopanaxadiol and protopanaxatriol have strong antitumor activity, and the activity is greatly affected by sugar groups. The law of tumor activity is: aglycon>monoglycoside>diglycoside>triglycoside>tetraglycoside (Dou Deqiang et al. Journal of Shenyang Pharmaceutical University 1999; 16(2): 151-156.David G, et al.Archives of Biochemistry and Biophysics 2002; 4...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K36/258A61K9/14A61K9/19A61K47/32A61P35/00
Inventor 金圣煊孙静芸张龙清雷荣剑林燕飞晏桂敏徐淑媛
Owner 浙江金石亚药医药科技有限公司
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