A kind of oridonin sustained-release tablet and preparation method thereof

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...

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

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