Preparation method of whitmania pigra whitman extract sustained-release pellet

Abstract

The invention relates to a preparation method of a whitmania pigra whitman extract sustained-release pellet. The method comprises steps of preparing a drug-loaded pellet from a whitmania pigra whitman extract, and sequentially covering a swelling coating, a controlled-release coating and an enteric coating outside the drug-loaded pellet. The sustained-release pellet disclosed by the invention is a sustained-release preparation that pH control and time control are combined; and by virtue of the sustained-release preparation, the controlled release of the contained whitmania pigra whitman extract is delayed to the end of small intestine and to the part of colon, so that the effective components of the whitmania pigra whitman are protected from being damaged by various proteases in digestive tract and the bioavailability of medicines is enhanced.

Description

technical field [0001] The invention relates to a pharmaceutical preparation containing peptide, in particular to a method for preparing a pharmaceutical preparation from an extract derived from leeches. Background technique [0002] Wide-body golden leech is a kind of leech. Leech is one of the traditional Chinese medicines used in my country for a long time. It was first recorded in "Shen Nong's Materia Medica", and its function is to break blood and remove blood stasis. There are many varieties of leeches, about 400-500 species in the world, and 89 species have been found in my country [1]. "Chinese Pharmacopoeia" records leech as the dried body of leech (WhitmaniapigraWhitman), leech (HirudonipponicaWhitman) or willow leaf leech (WhitmaniaacranulataWhitman). Among them, the wide-bodied golden line leech, also known as leech, is the most clinically used leech species, accounting for 95% of the total. [0003] The clinical application of leech has always been oral admini...

AI Technical Summary

Problems solved by technology

[0005] Existing research results have shown that both Hirudo phenatinae and Hirudo japonica contain thrombin, which acts through thrombin. However, thrombin is very unstable and easy to degrade. No matter what kind of preparation method is used, it is difficult to make oral and the active ingredient of the broad-bodied leeches is not thrombin, although its ingredients are proteins or polypeptides (experimentally proven), they are relatively stable and can be kept basically undamaged during the extraction and preparation process, but if using At present, the most conventional oral administration method has the disadvantages of being easily destroyed and difficult to absorb. The concentration of proteolytic enzymes in the colon is much lower than that of other intestinal segments, and the drug stays here for a long time, and the colon wall can penetrate macromolecules. The resistance is small, which is conducive to the absorption of drugs. Now many studies have made oral preparations of polypeptides into colonic drug preparations. The use of additives such as absorption enhancers can properly improve the stability and bioavailability of such drugs, but Absorption remains slow due to lack of villi in the colon and poor intestinal penetration of peptides

[0006] For the oral preparation of leeches, some research reports and patents have been disclosed or authorized; people such as Tang Peixu have done the research on oral chylomicrons of recombined leeches; patent CN101584859A discloses a kind of leeches microsphere preparation and its preparation method, For oral administration; patent CN1393266A discloses a preparation method of hirudin sustained (controlled) release preparation, the goal is to maintain the effective blood concentration of hirudin after administration, and overcome the shortcoming of its short half-life; patent CN1428173A authorizes a hirudin The method of recombinant hirudin enteric-coated slow-release preparation is a kind of enteric-coated slow-release oral preparation that adds a stabilizing protective agent and gastrointestinal enzyme inhibitor; patent CN01810561A discloses a polyion micelle composition of hirudin Preparation method; patent CN102362874B authorized a leech colon-targeted oral preparation and its preparation method

The above documents and patents are mainly designed with natural or recombinant hirudin to solve the problem of low oral absorption and low utilization of hirudin. However, hirudin is very unstable, and it is difficult to solve its preparation process, storage and stability after oral administration. Even if the colonic administration is designed, the colonic absorption is slow and the dissolved drug will still be degraded by enzymes and microorganisms in the colon for a long time, which cannot solve the problem of hirudin oral absorption well, and the above patents The pH-sensitive colonic drug delivery system selected in the study, because the pH of the colon is less different from that of the small intestine, also has the problem of releasing the drug in advance or entering the colon for a long time without dissolving; in the above patent applications, some mentioned that leech extract can be used. But the active ingredients of hirudin-containing leeches are completely different from those of broad-bodied golden leeches without hirudin

Images