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Method for preparing oridonin solid dispersion

A technology of oridonin A and solid dispersion, which is applied in the directions of medical preparations containing active ingredients, pharmaceutical formulations, organic active ingredients, etc. Side effects, etc.

Inactive Publication Date: 2011-05-25
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The heating and cooling rate of the melting method is difficult to control, the reproducibility between batches is poor, and the preparation conditions are severe, requiring a higher temperature, often exceeding 100 ° C, which will degrade the thermally unstable drug and easily destroy the activity of the drug; the solvent method A large amount of organic solvents need to be used, the environment is seriously polluted, and there will be residual organic solvents, which will cause toxic and side effects in the human body; the solid dispersion obtained by the grinding method is difficult to crush and sieve, which limits its further preparation into pharmaceutical preparations

Method used

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  • Method for preparing oridonin solid dispersion
  • Method for preparing oridonin solid dispersion
  • Method for preparing oridonin solid dispersion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1 (selection of auxiliary material)

[0028] 1.1 Mix PVP K17 and Rubescensin A at a mass ratio of 1:4, place in an autoclave, and react for 12 hours at 55°C and 8MPa to obtain a reaction product, and measure its dissolution rate.

[0029] 1.2 Mix PVP K-29 / 30 and Rubescensin A at a mass ratio of 1:4, place in an autoclave, and react for 12 hours at 55°C and 8MPa to obtain a reaction product, and measure its dissolution rate.

[0030] 1.3 Mix HPMC 5cp and Rubescensin A at a mass ratio of 1:4, place in an autoclave, and react for 12 hours at 55°C and 8MPa to obtain a reaction product, and measure its dissolution rate.

[0031] 1.4 Mix HPMC 15cp and Rubescensin A at a mass ratio of 1:4, place in an autoclave, and react for 12 hours at 55°C and 8MPa to obtain a reaction product, and measure its dissolution rate.

[0032] 1.5 Mix mannitol and Rubescensin at a mass ratio of 1:4, place in an autoclave, and react for 12 hours at 55°C and 8MPa to obtain a reaction pro...

Embodiment 2

[0038] Embodiment 2 (preparation of Rubescensine A / PVP K17 solid dispersion)

[0039] 2.1 Mix PVP K17 and Rubescensin A at a mass ratio of 1:10, place in an autoclave, and react for 24 hours at 55°C and 14MPa to obtain a reaction product, and measure its dissolution rate.

[0040] 2.2 Mix PVP K17 and Rubescensin A at a mass ratio of 1:10, place in an autoclave, and react for 24 hours at 55°C and 14MPa to obtain a reaction product, and measure its dissolution rate.

[0041] 2.3 Mix PVP K17 and Rubescensin A at a mass ratio of 1:7, place in an autoclave, and react for 18 hours at 55°C and 11 MPa to obtain a reaction product, and measure its dissolution rate.

[0042] 2.4 Mix PVP K17 and Rubescensin A at a mass ratio of 1:7, place in an autoclave, and react for 18 hours at 55°C and 11 MPa to obtain a reaction product, and measure its dissolution rate.

[0043] According to the dissolution test results of Examples 1.1 and 2.1-2.4, the optimal conditions for the reaction are: Rube...

Embodiment 3

[0045] Embodiment 3 (pharmacokinetic research of Rubescensine A in dogs)

[0046] Taking Beagle dogs as animal models, the in vivo pharmacokinetic characteristics of dogs after oral administration of a physical mixture of oridonin A and PVP K17 and a solid dispersion of oridonin A were investigated, in order to clarify the relative effects of oridonin A solid dispersion on The superiority of oridonin.

[0047] Two beagle dogs were given oral administration of the physical mixture of oridonin and PVPK17 or the solid dispersion of oridonin, and a cross-administration test was performed one week later. Fasting for 12 hours (without water) before the medication, and eating uniformly after the experiment. Insert the capsule directly into the epiglottis in a complete form, so that the beagle can swallow it automatically and inject an appropriate amount of water to send it down.

[0048] About 2 mL of blank blood sample was taken before administration, and about 2 mL of blood was c...

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Abstract

The invention discloses a method for preparing oridonin solid dispersion, comprising the following steps: evenly mixing oridonin with auxiliary according to the mass ratio of 1:4 to 1:10, putting the mixture into an autoclave and then sealing the autoclave, wherein the auxiliary is polyvinylpyrrolidone PVP K17; placing the autoclave in ice-water bath for cooling and feeding CO2 into the autoclave; placing the autoclave in water bath at 55 to 60 DEG C, implementing static reaction for 12 to 24 hours after the autoclave reaches 55 DEG C and 8-14MPa for 10 to 15 minutes, rapidly decompressing and collecting reaction products in the autoclave. The oridonin solid dispersion prepared according to the method, compared with physical mixture thereof, is increased in AUC value, which shows that theoridonin solid dispersion has obvious absorption promoting effect for oridonin.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy, and in particular relates to a method for preparing a solid dispersion of an insoluble natural anticancer drug oridonin. Background technique [0002] Oridonin (oridonin) is from Lamiaceae Camellia plant Rabdosin rubescens or broken rice (Rabdosin rubescens), fragrant tea (Rabdosia amethystoides), veined leaf fragrant tea (Rabdosianervosa), hairy leaves Rabdosia jabdsia, Rahdosia downsis and Isodon japonicus are natural organic compounds of kaurene-type tetracyclic diterpenoids. Its chemical structural formula is as follows: [0003] [0004] Oridonin is a colorless prismatic crystal with an extremely bitter taste, very slightly soluble in water, and soluble in organic solvents such as ether, methanol, and ethanol. It has strong anti-tumor activity and is effective against a variety of transplanted tumors. It is mainly used in the treatment of primary liver cancer, esophageal cancer, pancrea...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P35/00
Inventor 冯年平李淞明赵玲刘涛
Owner SHANGHAI UNIV OF T C M