Clonidine hydrochloride sustained-release micro-tablets as well as preparation method and application thereof

Abstract

The invention relates to the technical field of sustained-release drugs, in particular to clonidine hydrochloride sustained-release micro-tablets as well as a preparation method and application thereof. The clonidine hydrochloride sustained-release micro-tablets comprise the following components in percentage by weight of 3-6% of clonidine hydrochloride, 68-86% of a gel skeleton, 0.5-2% of a lubricant and 10-25% of a filler. The preparation method comprises the following steps of irradiating and sterilizing all the raw materials by gamma-rays before use, and performing the following operationsin a sterile environment: uniformly mixing and grinding all the raw materials by using a mortar, and performing pressing into small pieces with the diameter of 3mm through an anisotropic tabletting machine under the maximum pressure by a direct tabletting method. Compared with clonidine hydrochloride eye drops, the ophthalmic clonidine hydrochloride sustained-release micro-tablets disclosed by the invention have a good controlled-release effect, can prolong the residence time of drugs in eyes, reduce the administration times, improve the compliance of patients, improve the bioavailability ofthe drugs and reduce the toxic and side effects of a central nervous system, are simple in preparation process and have good practical application value.

Description

technical field [0001] The invention relates to the technical field of sustained-release medicines, in particular to a clonidine hydrochloride sustained-release microtablet and a preparation method and application thereof. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Clonidine hydrochloride, whose chemical name is 2-[(2,6-dichloroaniline)-2imino]-imidazolidine hydrochloride, is an α-adrenoceptor agonist and is currently used as a second-line drug for hypertension In 2009, the FDA approved the clonidine hydrochloride sustained-release tablets developed by Addrenex Pharmaceuticals for the treatment of high blood pressure. In 2010, it was approved by the US FDA to add ind...

AI Technical Summary

Problems solved by technology

However, its long-term application is limited due to its influence on the central nervous system and the significant decrease in systemic arterial pressure.

[0004] In the treatment of glaucoma, eye drops are most commonly used in topical administration of the eye, but due to rapid clearance caused by blinking and tear drainage, the bioavailability is very low, so the amount entering the conjunctival blood vessels is very limited. With liquid administration, approximately 75% of the dose is drained almost immediately through the nasolacrimal duct, requiring more frequent dosing or higher doses to maintain therapeutic drug levels

Some macromolecule thickeners such as methyl cellulose, hydroxypropyl cellulose, polyvinylpyrrolidone and polyvinyl alcohol are added into eye drops, in order to prolong the residence time of the drug in the eye and improve the bioavailability of the drug , but the release rate of the drug is not easy to control, resulting in the rapid outflow of the drug from the polymer

[0005] In the prior art, clonidine hydrochloride dosage forms include oral immediate-release tablets, sustained-release tablets, dropping pills, injections and transdermal patches, etc., but the inventors have found that existing clonidine hydrochloride dosage forms are used for the treatment of eye diseases. The treatment effect is not very good

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