Enantiomophous kauri pine alkane style diterpine compound microcaspules and their preparation

A technology of kaurane-type and compound, applied in the field of en-kaurene-type diterpene compound microcapsules and its preparation, which can solve the research reports and patent applications of microcapsules that have not yet been discovered of kaurene-type diterpene compounds To achieve the effect of improving patient compliance, reducing clinical dose, and improving bioavailability

Inactive Publication Date: 2005-12-28
云南一尧科技开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, no microcapsule research reports and patent ap

Method used

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  • Enantiomophous kauri pine alkane style diterpine compound microcaspules and their preparation

Examples

Experimental program
Comparison scheme
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Example Embodiment

[0026] Example 1

[0027] formula:

[0028] Oridonin (ultrafine powder) 2g

[0029] Gelatin 24g

[0030] Preparation process: firstly, the enantio-kaurane type diterpene compound is ultrafinely treated by the airflow freezing pulverization method in the superfine pulverization method, so that the particle size is less than 25 μm, and then Oridonin is prepared by the single aggregation method Microcapsules, specifically: under the condition of 100,000 grades, add Rubescensine A into 600ml of 60°C non-salt water, carefully adjust the pH to 7.2-7.8 with 0.01% NaOH, add gelatin at 37°C, and keep warm Stir to dissolve at 37°C, add 10% acetic acid solution dropwise to pH 3.5-3.8, place the reactor in a water bath at 50°C and keep stirring for 45 minutes. Add sodium sulfate solution (diluent) dropwise, observe under a microscope until it forms capsules, immediately pour it into the diluent that is being stirred, after gelling and settling, pour off the supernatant, and wash with d...

Example Embodiment

[0031] Example 2

[0032] formula:

[0033] Oridonin (particle size<10μm) 8g

[0034] Gelatin 60g

[0035] Pectin 40g

[0036] Preparation process: Firstly, the enantio-kaurane type diterpene compound is ultrafinely treated by the airflow freezing pulverization method in the ultrafine pulverization method, so that the particle size is less than 25 μm, and then the oridonin is prepared by the complex coacervation method Microcapsules, specifically: under the condition of 100,000 grades, first add oridonin into 96ml of ethyl acetate, and fully stir, and set aside; take appropriate amount of pectin and oridonin above The liquid is made into colostrum, and the colostrum is diluted with 4800ml of 3% pectin solution to become an O / W emulsion. In addition, the gelatin was dissolved into 4800ml of gelatin solution, the pH was adjusted to 8 with 10% sodium hydroxide, and the two-liquid reactor was placed in a water bath at 50° C. for 45 minutes with stirring. Use 10% acetic acid s...

Example Embodiment

[0037] Example 3

[0038] Solvent-non-solvent method to prepare samiculin microcapsules, formula:

[0039] Melipin (particle size<10μm) 3g

[0040] Butyl cellulose acetate 90g

[0041] Butanone 2000g

[0042] Preparation process: The superfine treatment is the same as above. Under the condition of 100,000 grades, first dissolve cellulose acetate butyl in 2000ml of methyl ethyl ketone, and pay attention to make it completely dissolved before use. Then add sliverin into it, place the reactor containing the reaction solution in a water bath at 55° C., heat and stir for 45 minutes. Slowly add the non-solvent isopropyl ether under the condition of stirring, and wrap the suspended core material into microcapsules when the condensed phase separation occurs. Slowly cool down to room temperature, separate the microcapsules by centrifugation, wash with isopropyl ether, and dry in vacuum to obtain the required microcapsules of samiculin.

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Abstract

A p-kaurane diterpenoid microsoftgel is proportionally prepared from the p-kaurane diterpenoid as its active component and the wall material or carrier or medical auxiliary. Its preparing process and the medicines containing it are also disclosed.

Description

technical field [0001] The present invention relates to a bioactive drug with antibacterial and antitumor effects, more precisely, it is an enantio-kaurane type diterpene compound with better bioavailability, higher activity and better stability Microcapsules and methods for their preparation. Background technique [0002] Plants of the genus Isodon belong to the family Lamiaceae (Labiatae=Lamiaceae) and the subfamily Ocimoideae are perennial herbs, shrubs, and subshrubs. There are more than 150 species of plants in this genus, 90 species and 21 varieties in China, which are distributed all over the country, and more are distributed in Yunnan. For example, the calyx and fragrant tea are all plants that are unique to Yunnan or have abundant storage. Camellia plants are rich in secondary metabolites of ent-kaurenoids. More than 80 of them have been studied and more than 500 diterpenoids have been found. Most of them The ingredients have antibacterial activity, some have stro...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K9/50A61P31/04A61P35/00
Inventor 任杨帆
Owner 云南一尧科技开发有限公司
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