Microemulsion preparation of methylprednisolone aceponate and preparation method thereof

Abstract

Belonging to the technical field of pharmaceutical preparations, the invention relates to a microemulsion preparation of methylprednisolone aceponate and a preparation method thereof. The microemulsion preparation of methylprednisolone aceponate is composed of the following components by mass: 0.01-1% of methylprednisolone aceponate, 10%-30% of a surfactant, 15-40% of a cosurfactant, 10-20% of an oil phase, and the balance water. The preparation method includes: mixing the oil phase, the surfactant and the co-surfactant evenly, adding methylprednisolone aceponate, conducting stirring for dissolving, then adding water, and performing stirring to obtain the microemulsion. According to the invention, methylprednisolone aceponate is made into a microemulsion state, and the dissolvability of methylprednisolone aceponate in the matrix is increased so as to make methylprednisolone aceponate highly diffusive, thus improving bioavailability. Also, the microemulsion has smaller particle size, is isotropic and more uniform, belongs to the homodisperse system, and has more excellent thermodynamic stability.

Description

technical field [0001] The invention relates to a methylprednisolone acetate microemulsion preparation and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Glucocorticoid, also known as "adrenocorticoid", is a class of steroid hormones secreted by the adrenal cortex, which regulates the biosynthesis and metabolism of sugar, fat, and protein, and has anti-inflammatory effects. [0003] Glucocorticoids are widely used clinically. Among them, topical glucocorticoids have been the first-line drug for the treatment of many eczematous dermatitis and psoriasis such as atopic dermatitis and contact dermatitis. [0004] The earliest glucocorticoid used to treat skin diseases was synthetic hydrocortisone in 1950, with the following structure: [0005] [0006] Since then, all glucocorticoid drugs have been obtained by modifying the basic structure of cortisone, and dozens of drugs with clinical value have...

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Problems solved by technology

[0013] Chinese patent application CN101347436B discloses the application of methylprednisolone and its derivatives in the preparation of medicines for the treatment of allergic rhinitis, but the particle size of methylprednisolone and its derivatives needs to be strictly controlled in the technology of this application, and the process is relatively complex

[0014] Chinese patent application CN101347437B discloses a pharmaceutical composition for the treatment of respiratory diseases; but the technical solution of this application is an aerosol, which also requires strict control of the particle size of methylprednisolone acetate, and the process is more complicated

[0015] A hormone cream is disclosed in Chinese patent application CN101468024B; but in the technical scheme of the application, the active ingredient methylprednisolone is dispersed into the cream in the form of an aqueous suspension, which requires strict control of methylprednisolone The particle size of nylon requires adding a suspending agent to the suspension, which is complicated and unnecessary

[0016] Disclosed in Chinese patent application CN101601651A is a kind of liposome emulsifiable cream of methylprednisolone acetate; But do not reflect the advantage of liposome in the technical scheme in this application, and process is complicated

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