Preparation method of capsicine micro spheres

Abstract

The invention discloses a preparation method of capsicine micro spheres, which comprises the following steps: (1) dissolving capsicine and carrier materials into an organic solvent to obtain an oil phase according to the mixing ratio of 100 to 250 mg / 27 to 100 mg / 2 to 5 mL; (2) dissolving emulsifying agents into water as a water phase, wherein the concentration of the emulsifying agents in the water phase is between 5 and 30 mg / mL; and (3) adding the oil phase into the water phase for forming oil-in-water latex emulsion according to the volume ratio of 1 / 20 to 1 / 40 under the conditions of the temperature between 20 and 30 DEG C and the stirring speed between 500 and 1200 rpm, continuously stirring the oil-in-water latex emulsion for volatilizing the organic solvent, carrying out centrifugation for collecting micro spheres, washing the micro spheres by distilled water, and preparing the capsicine micro spheres through freeze drying. The capsicine micro spheres prepared by the method of the invention can be made into various slow-release preparations, the stimulation of the capsicine can be reduced, and the medicine concentration can be maintained for a long time, so the medication times can be reduced, the toxic and side effect can be reduced, and the adaptability of patients can be improved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a preparation method of capsaicin microspheres. Background technique [0002] Capsaicin (Capsaicin) is a vanilla amide alkaloid extracted from natural peppers. Its chemical structure name is: N-[(4-hydroxy-3-methoxy-phenyl)-methyl]-8 -Methyl-(trans)-6-nonenamide can be obtained through methods such as plant extraction, biosynthesis, chemical synthesis and cell culture. Capsaicin has a variety of complex physiological and pharmacological activities, including anti-inflammatory, analgesic, antibacterial, antipruritic, prevention and treatment of cardiovascular diseases, promotion of fat metabolism, mediation of tumor cell apoptosis, etc., among which the more unique is its long-acting Analgesic effect and new analgesic mechanism: mainly by affecting the release, synthesis and storage of neuropeptide P substance, it has analgesic and antipruritic effects. Experimental stu...

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Problems solved by technology

[0003] However, because capsaicin has a high degree of hepatic first-pass effect, the half-life is too short, and the oral bioavailability is also low. At present, capsaicin is mostly used in topical dosage forms, such as creams, patches, ointments, films and cataplasms. etc., but all have different degrees of skin irritation, such as skin burning sensation, local area hyperemia and neurogenic inflammatory response, which limit its clinical application. How to use new drug delivery technology to develop various dosage forms of capsaicin to avoid its Hepatic first-pass effect, prolonging biological half-life and reducing irritation for clinical use have become an important direction for new drug development

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