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Baicalin nano crystal suspension, nano crystal dry powder and methods for preparing baicalin nano crystal suspension and nano crystal dry powder

A technology of baicalin nanocrystal and suspension, which is applied in the field of medicine, can solve the problems of difficult mass production, low drug loading and the like, and achieves the effects of increasing absorption opportunities, simple process engineering, and low equipment requirements.

Inactive Publication Date: 2012-12-19
JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
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  • Application Information

AI Technical Summary

Problems solved by technology

The preparation process of the precipitation method requires the addition of a large amount of organic solvents, and the drug loading is low, making it difficult to produce in batches

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0052] Weigh 600mg of poloxamer 188, add it to 100ml of aqueous solution, heat it slightly at 30-40°C to dissolve it completely, add 2g of micronized baicalin under magnetic stirring, and pre-disperse with a 10,000rpm internal cutting homogenizer 5min, the primary suspension was prepared; the primary suspension was subjected to high-pressure homogenization under the conditions of 10 cycles at 500 bar; 10 cycles at 1000 bar; 20 cycles at 1500 bar to obtain baicalin nanocrystal suspension agent, with an average particle size of 320nm.

example 2

[0054] Weigh 100mg of poloxamer 188, add it to 100ml of aqueous solution, heat it slightly at 30-40°C to dissolve it completely, add 1g of micronized baicalin under magnetic stirring, and pre-disperse with a 10,000rpm internal cutting homogenizer 5min, the initial suspension was obtained; the initial suspension was subjected to high-pressure homogenization, and the condition was to circulate 10 times under 500bar; then circulate 20 times under 1000bar; then circulate 20 times under 1500bar to obtain the baicalin nanocrystal suspension agent, with an average particle size of 308nm.

example 3

[0056] Weigh 600mg of Poloxamer 188 and 300mg of Tween-80, add them into 20ml of aqueous solution, heat at a slight temperature at 30-40°C to dissolve completely, add 2g of micronized baicalin under magnetic stirring, and internally cut at 10,000rpm Type homogenizer pre-emulsification for 5min to obtain the primary suspension; the primary suspension was subjected to high-pressure homogenization under the condition of 10 cycles at 500 bar; 10 cycles at 1000 bar; 30 cycles at 1500 bar to obtain Baicalin nanocrystal suspension, 1g of mannitol was dissolved in the nanocrystal suspension, Co-60 sterilized, subpackaged in vials, pre-frozen at -80°C for 10 hours, then freeze-dried for 12 hours, and the nanocrystal jelly was prepared. dry powder. The lyophilized powder was reconstituted with water for injection, and the average particle size was 265nm.

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Abstract

The invention relates to a baicalin nano crystal suspension, a nano crystal dry powder and methods for preparing the baicalin nano crystal suspension and the nano crystal dry powder, which are used for effectively solving the problems that baicalin has bad water solubility, low oral bioavailability and common injections hardly achieve high drug-loading rate and a targeting function. A baicalin nano crystal intermediate is characterized by consisting of 1 part by weight of baicalin, 0.01-10 parts by weight of stabilizer and 0-30 parts by weight of filling protective. The baicalin nano crystal intermediate can be a nano crystal suspension and the dry power of the nano crystal suspension, which are prepared by the following steps: 1, preparing a nano primary suspension by using a dispersion method; 2, preparing the nano crystal suspension by a grain size reducing method which can be a high-pressure homogenization method or an ultrasound grinding method; and 3, preparing nano crystal dry powder by using a freeze-drying method and a spray drying method.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a baicalin nanocrystal suspension, nanocrystal dry powder and a preparation method thereof. Background technique [0002] Scutellaria baicalensis, first recorded in "Shen Nong's Materia Medica", a Chinese Pharmacopoeia 2000 edition, records that it is the dry root of Scutellaria baicalensis, a plant in the labiatae family. It is cold in nature and bitter in taste. . Baicalin is the main active ingredient of Scutellaria baicalensis. Pharmacological studies have shown that baicalin has anti-inflammatory, antibacterial, antipyretic, sedative, antihypertensive, diuretic, choleretic, hepatoprotective, anti-allergic, immune-regulating, and asthma-relieving effects. A traditional Chinese medicine with good development prospect. Among them, baicalin has a significant protective effect on animal models of liver injury caused by carbon tetrachloride, and has a liver-protecting effect on acute sev...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K9/10A61K9/14A61P1/16A61P31/14A61P31/20
Inventor 岳鹏飞杨明郑琴伍振峰胡鹏翼万晶
Owner JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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