Progesterone ethosome, and preparation method and application thereof

Abstract

The invention provides a progesterone ethosome. Progesterone is encapsulated in an ethosome. The progesterone ethosome comprises the following components in percentage by weight: 0.1 to 1 percent of progesterone, 1 to 8 percent of lipid materials, 0 to 0.6 percent of cholesterol, 20 to 50 percent of short-chain alcohols, 0 to 3 percent of nonionic surfactant and the balance of water. The preparation method comprises the following steps of: mixing and dissolving the progesterone, the lipid materials, the cholesterol and the short-chain alcohols to prepare an alcohol phase; with stirring, adding the alcohol phase into a nonionic surfactant-containing aqueous phase to prepare primary emulsion under the condition of stirring; homogenizing the primary emulsion under a high pressure to obtain asuspension; stirring the ethosome suspension for 15 to 30 minutes to perform emulsification for the second time; and curing the suspension by cooling the suspension at 0 to 4 DEG C to obtain the progesterone ethosome. Because the high-pressure homogenization method is adopted to prepare the progesterone ethosome, the progesterone ethosome is low in stimulation to skin and high in transdermal delivery ability, and metal ion pollution which is easy to cause by the probe ultrasound method of the traditional homogenization method is avoided. Therefore, the progesterone ethosome is suitable for industrial production. The progesterone ethosome can be prepared into a transdermal drug delivery system, a mucosal drug delivery system, and topical dosage forms, such as a paster, a gel and the like. The progesterone ethosome is mainly applied to hormone replacement therapy, secondary amenorrhea, functional aplastic bleeding, premenstrual syndrome and the like clinically.

Description

technical field [0001] The invention relates to a progesterone ethosome and a preparation method and application thereof, belonging to the technical field of pharmacy. technical background [0002] Progesterone was synthesized and sold for the first time in 1934, which is exactly the same in structure and composition as endogenous progesterone. It often produces effects on the basis of estrogen, which can transform the endometrium from the proliferative phase to the secretory phase, thereby promoting the endometrial maturation, exfoliation and maintenance of the menstrual cycle; it can also prepare the uterus for embryo implantation, It can stabilize the endometrium and protect the fetus in the first trimester, which is a necessary condition for successful pregnancy. [0003] Progesterone is a physiological hormone, which has the advantages of not counteracting the increase of high-density lipoprotein (HDL) and the reduction of cardiovascular disease (CVD). Clinically, it ...

AI Technical Summary

Problems solved by technology

In the prior art, the colostrum is often subjected to probe ultrasound under ice-water bath conditions to obtain ethosomes, but the probe will generate metal ions during the ultrasound process, which is easy to contaminate the sample. At the same time, the amount of sample prepared by this method is small, and it is difficult to realize industrialization. mass production

In addition, when the progesterone solution is directly used for transdermal research, its cumulative penetration and penetration rate are low, which limits the wide application of progesterone as a transdermal drug delivery system

And there is no report of progesterone ethosome in the prior art

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