Capsaicin beta-cyclodectrin inclusion-compound and liposome and gel of inclusion-compound

Abstract

The invention discloses a capsaicin beta-cyclodextrin inclusion compound, as well as liposome and gel thereof. The capsaicin beta-cyclodextrin inclusion compound is prepared by the following method: (1) beta-cyclodextrin is dissolved in an aqueous phase and prepared into a solution, and the solution is added with capsaicin or a capsaicin solution so as to obtain a mixed solution of capsaicin and beta-cyclodextrin; and (2) the solution-type capsaicin beta-cyclodextrin inclusion compound is obtained from the mixed solution prepared in a step (1) through at least one treatment mode of standing, heating, stirring, ultrasound or grinding. The apparent solubility of the capsaicin of the inclusion compound increases by 2 to 20 times. In vitro transdermal study shows that the capsaicin inclusion compound can obviously raise the transdermal rate of medicine by 5 to 20 times as compared with cream and hydrogel, and obviously reduce the irritation of capsaicin at skin. Besides transdermal drug administration, the prepared inclusion compound and the inclusion compound liposome can also be orally taken, injected or administrated in bladders. In addition, the invention is simple in production process, and the quality is stable and easy to control.

Description

Capsaicin β-cyclodextrin inclusion complex and liposome and gel of inclusion complex technical field The invention belongs to the field of pharmaceutical preparations, and relates to a capsaicin beta-cyclodextrin inclusion compound and liposome and gel of the inclusion compound. Background technique Capsaicin, also known as capsaicin, is an alkaloid widely present in ripe fruits of peppers. Capsaicin mainly acts on substance P on C-type sensory neurons, and some unmyelinated slow conduction fibers in C-type nerve fibers can conduct skin pain and pathological itching. In response to noxious stimuli, C-type nerve fibers release substance P to cause hypersensitivity. When the local substance P is reduced by the application of drugs, it can prevent the conduction of certain types of pain, itching and other sensations. The non-central analgesic effect of topical capsaicin is due to the action of capsaicin on peripheral nerve axons, resulting in the elimination of small sensory...

AI Technical Summary

Problems solved by technology

However, the oil-water partition coefficient of capsaicin is too high, resulting in very small solubility in water, which is very unfavorable for human body absorption, so the bioavailability is also very low

And because capsaicin has very strong skin irritation, common capsaicin cream is more irritating, and skin burning sensation, tingling sensation and flushing may occur at the medication site, and continuous medication for more than 3 to 4 days is required to make the patient tolerance

Although liposomes of capsaicin can reduce the irritation of capsaicin, the solubility of capsaicin has little improvement

Therefore, the above-mentioned side effects limit the clinical application of capsaicin to a large extent.

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