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Oridonin sustained release tablet and preparation method thereof

A technology of oridonin A and sustained-release tablets is applied in the directions of pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. Difficult to achieve therapeutic concentration, low bioavailability and other problems, to achieve the effect of prolonging drug action time, optimizing particle fluidity and anti-caking properties, and improving sustained release effect

Inactive Publication Date: 2019-05-17
SHANDONG PROVINCIAL HOSPITAL AFFILIATED TO SHANDONG FIRST MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Oridonin is a 7,20-epoxy-type ent-kaurane diterpene compound, soluble in methanol, ethanol, propylene glycol, ethyl acetate, acetone and other organic alcohols, insoluble in water, and classified as biopharmaceutical Class IV drugs in the system have dissolution barriers and permeation barriers during oral administration; after oral administration, the blood drug concentration in the body is low, and the concentration of oridonin around tumor cells is even lower, making it difficult to achieve clinical Effective therapeutic concentration, which seriously affects the anticancer effect of oridonin
Currently on the market, organic ethanol plus surface active substances are mainly used to increase the solubility of oridonin. Intravenous infusion can easily cause vasculitis, pain and other adverse reactions, while oral preparations only have oridonin crude extract tablets. Low content and low bioavailability; therefore, it is necessary to develop new dosage forms to improve the bioavailability of oridonin

Method used

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  • Oridonin sustained release tablet and preparation method thereof
  • Oridonin sustained release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] A sustained release tablet of oridonin, consisting of the following components in weight percentage: 0.3% oridonin, 30% diacylglycerol, 40% soybean lecithin, 7% chitosan, 15% ethanol, viscose Mixture 2%, low-substituted hydroxypropyl cellulose 2%, magnesium stearate 3%, sorbitol 0.7%.

[0037] The binder is formed by mixing methylcellulose and ethylcellulose in a weight ratio of 1:1-3.

[0038] This embodiment provides a preparation method of Oridonin Sustained-release Tablets, comprising the following steps:

[0039] S1. Mix the Rubescensin A in the weight percentage with phospholipids and diacylglycerol evenly, then add ethanol and mix to obtain a Rubescensin A solution;

[0040] S2, adding chitosan and adhesive to the oridonin A solution, mixing under stirring conditions, the stirring rate is 600rpm, and the stirring time is 40min, so that the above raw materials are mixed evenly;

[0041] S3. Perform high-pressure homogenization of the oridonin A cubic liquid crys...

Embodiment 2

[0046] A sustained release tablet of oridonin, consisting of the following components in weight percentage: 0.1% oridonin, 20% diacylglycerol, 50% soybean lecithin, 5% chitosan, 10% ethanol, viscose Mixture 5%, low-substituted hydroxypropyl cellulose 5%, magnesium stearate 4%, sorbitol 0.9%.

[0047] The binder is formed by mixing methylcellulose and ethylcellulose in a weight ratio of 1:1.

[0048] This embodiment provides a preparation method of Oridonin Sustained-release Tablets, comprising the following steps:

[0049] S1. Mix the Rubescensin A in the weight percentage with phospholipids and diacylglycerol evenly, then add ethanol and mix to obtain a Rubescensin A solution;

[0050] S2. Add chitosan and adhesive to the oridonin A solution, mix under stirring conditions, the stirring rate is 500rpm, and the stirring time is 1h, so that the above raw materials are mixed evenly;

[0051] S3. Perform high-pressure homogenization of the oridonin A cubic liquid crystal coarse ...

Embodiment 3

[0056] A sustained-release tablet of oridonin, consisting of the following components by weight percentage: 0.5% oridonin, 40% diacylglycerol, 30% soybean lecithin, 10% chitosan, 5% ethanol, viscose Mixture 4%, low-substituted hydroxypropyl cellulose 5%, magnesium stearate 5%, sorbitol 0.5%.

[0057] This embodiment provides a preparation method of Oridonin Sustained-release Tablets, comprising the following steps:

[0058] S1. Mix the Rubescensin A in the weight percentage with phospholipids and diacylglycerol evenly, then add ethanol and mix to obtain a Rubescensin A solution;

[0059] S2. Add the oridonin A solution to chitosan and binder, and mix under stirring conditions, the stirring rate is 800rpm, and the stirring time is 0.5h, so that the above raw materials are mixed evenly;

[0060] S3. Perform high-pressure homogenization of the oridonin A cubic liquid crystal coarse dispersion solution, the homogenization pressure is 2000 bar, and the homogenization times are 3 t...

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Abstract

The invention discloses an oridonin sustained release tablet and a preparation method thereof. The oridonin sustained release tablet consists of the following components in percentage by weight: 0.1-0.5 % of oridonin, 20-40 % of diacylglycerol, 30-50 % of phospholipid, 5-10 % of chitosan, 5-15 % of ethanol, 2-5 % of an adhesive and 2-5 % of low-substituted hydroxypropyl cellulose, 2-5 % of a lubricant and 0.5-0.9 % of a sweetener; the preparation method comprises the following steps of: mixing phospholipid, diacylglycerol and oridonin; adding ethanol, and uniformly mixing; adding chitosan andthe adhesive to mix evenly; homogenizing and granulating under high pressure; adding low-substituted hydroxypropyl cellulose, the lubricant and the sweetener, and uniformly mixing; tabletting; the oridonin sustained release tablet prepared by the method has obvious sustained-release effect and uniform release speed, and can reduce medication times; the tablet has the advantages of good uniform strength, good taste and convenient oral administration, the relative bioavailability of oral administration of oridonin is obviously improved, and a novel oral preparation of oridonin which can be slowly released with good absorption and high bioavailability is provided.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an oridonin sustained-release tablet and a preparation method thereof. Background technique [0002] Rubescensin A is a natural organic compound of kaurene diterpenoids isolated from Lamiaceae plant Rubescens, which has a strong anti-tumor effect on a variety of tumor cells; clinically, it is mainly used as A new anti-cancer drug or anti-cancer adjuvant drug, used for the treatment of digestive system cancers such as liver cancer, esophageal cancer, and pancreatic cancer. [0003] Oridonin is a 7,20-epoxy-type ent-kaurane diterpene compound, soluble in methanol, ethanol, propylene glycol, ethyl acetate, acetone and other organic alcohols, insoluble in water, and classified as biopharmaceutical Class IV drugs in the system have dissolution barriers and permeation barriers during oral administration; after oral administration, the blood drug concentration in th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/352A61K47/38A61K47/36A61K47/10A61K47/24A61P35/00
Inventor 朱洪梅
Owner SHANDONG PROVINCIAL HOSPITAL AFFILIATED TO SHANDONG FIRST MEDICAL UNIVERSITY
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