Ginkgolide nano sustained and controlled release oral preparation and preparation method thereof

Abstract

The invention discloses a bilobalide nanometer controlled-release oral preparation and a preparation method. The preparation is prepared from, by weight, 0.5-60% of nanometer carrier, 0.1-30% of bibobalide, 0.1-15% of coating and the balance auxiliary materials, the sum of weight percentages is 100%, and a nanometer mesoporous material is used as the nanometer carrier. According to the preparing method, at first, the nanometer carrier with good biocompatibility is prepared; then by means of a physical or chemical mode, bilobalide is loaded onto the nanometer carrier and coated with the coating, and a nanometer controlled-release drug-loading system is constructed; finally, the adjuvants such as starch, sugar and microcrystalline cellulose are added and mixed uniformly to prepare the oral preparation. The bilobalide nanometer controlled-release oral preparation has the advantages of being small in drug particle size, high in utilization rate, long in action time, small in blood concentration fluctuation and low in price, dosing is convenient, preparation is easy, and the preparation has high application and development value.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine sustained and controlled release preparations, in particular to a ginkgolide nano sustained and controlled release oral preparation and a preparation method thereof. Background technique [0002] Ginkgolide is a fat-soluble physiologically active component in Ginkgo biloba, a highly specific platelet activating factor receptor antagonist, and has the functions of dilating coronary blood vessels, improving cerebral circulation, inhibiting platelet aggregation, and preventing atherosclerosis. The natural medicine of choice for the treatment of cardiovascular and cerebrovascular diseases has long occupied the top position in the natural medicine list in the international pharmaceutical market, and has been growing at a rate of more than 10% year by year. However, the currently used preparations generally have short drug effects, large fluctuations in blood drug concentration, need for mult...

AI Technical Summary

Problems solved by technology

[0004] Although the various sustained and controlled release preparations reported in the above-mentioned patents and papers prolong the action time of ginkgolide and improve the drug effect to a certain extent, they still have the following disadvantages compared with the nano sustained and controlled release oral preparation of the present invention: injection It is inconvenient for patients to go to the hospital for injections on a regular basis. At the same time, a large amount of organic solvents are used as adjuvants, which increases the cost and is prone to allergic reactions and other side effects. In addition, early morning is the peak time for cardiovascular and cerebrovascular diseases. Providing effective treatment to patients at dangerous times has brought serious hidden dangers to patients' life safety; the patent "Ginkgolide B nanoliposome drug and its preparation method authorization number: ZL 200710098391.5)" uses liposomes, which are expensive; The preparation methods of the patents "A Ginkgolide B Sustained Release Preparation and Its Preparation Method (Application No.: 200610126051.4)" and "Ginkgolide Controlled Release Tablets and Its Preparation Method (Application No.: 201310575789.9)" are to directly mix Ginkgolide B It is prepared by mixing with matrix sustained-release materials and then adding auxiliary agents. It is an ordinary sustained-controlled release preparation with large drug particle size (in the micron order), uneven particle size distribution, and limited slow-controlled release function. The preparation method is the same as that of the present invention. There are essential differences; the sustained and controlled release agents reported in other published papers also belong to the micron level, and the preparation method is also completely different from the present invention

However, the research on ginkgolide nano-sustained and controlled-release oral preparations has not been reported at home and abroad.

Images