Progesterone self-emulsifying composition and application

Abstract

The invention discloses a progesterone self-emulsifying composition and an application. The progesterone self-emulsifying composition is prepared from the raw materials in parts by mass of 1 part of progesterone, 2-15 parts of solvent, 6-75 parts of vitamin E polyethylene glycol succinate and 0.5-2 parts of stabilizer. The solvent is oleic acid or ethyl oleate; and the stabilizer is one or a mixture of several of benzyl alcohol, sodium sulfite and ethylenediamine tetraacetic acid disodium salt in any proportion. The progesterone preparation composition disclosed by the invention is high in chemical stability, an acceleration experiment is carried out according to the requirements of acceleration experiments in four stability experiments in Chinese Pharmacopoeia 2015 edition, single impurities do not exceed 0.5% at the end point of 6 months, the total impurity mass does not exceed 2.0%, the content is 93%-107%, the progesterone injection meets the requirements of progesterone injectionin Chinese Pharmacopoeia 2015 edition on content and impurity acceptance standards, and is high in product stability and suitable for commercial production.

Description

[0001] (1) Technical field [0002] The invention relates to a progesterone self-emulsifying composition and its application. [0003] (2) Background technology [0004] Progesterone, also known as progesterone, is the main biologically active progesterone secreted by the ovary. Progesterone is widely used in the treatment of menstrual disorders, such as amenorrhea, dysfunctional uterine bleeding, corpus luteum insufficiency, threatened miscarriage and habitual miscarriage, premenstrual tension syndrome, menopausal syndrome, etc. However, progesterone is a steroid hormone with low solubility, so it is poorly absorbed in the body after oral administration, and is easily metabolized and inactivated by the liver. These factors lead to low bioavailability of progesterone in the human body. degree is only about 10%. The unabsorbed progesterone is mainly metabolized by the liver, which causes great damage to the liver. However, the progesterone injection is highly irritating durin...

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Problems solved by technology

[0007] The purpose of the present invention is to provide a self-emulsifying composition of progesterone, which is suitable for commercial progesterone non-injection formulations, in view of the defects of low dissolution rate and low bioavailability in the non-injection formulations of progesterone currently available in the market. While improving the bioavailability of progesterone, it also has a progesterone self-emulsifying preparation composition with good physical and chemical stability. The self-emulsifying composition is composed of a progesterone raw material drug completely dissolved in an oily solvent, a solubilizer and a cosolvent While achieving the purpose of improving the dissolution rate and bioavailability of progesterone in emulsion droplets, the self-emulsifying composition has good long-term physical and chemical stability and is suitable for commercial production

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