Alchlorine dipropionate containing cream preparation and preparation method thereof

Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to an alchlorine dipropionate composition. The composition comprises absolute ethyl alcohol, dimethyl sulfoxide, an oil phase component, a pH regulator, a bacteriostatic agent, a humectant and a metal ion chelating agent. A mixed solvent of absolute ethyl alcohol-dimethyl sulfoxide is adopted as a solvent and a stabilizer of a main drug, the problems that alchlorine dipropionate is difficult to dissolve and unstable in a dissolved state are successfully solved, and the dissolving time of the bulk drug is shortened. In the preparation process of the composition, no special requirement for the particle size of the bulk drug exists, the bulk drug does not need to be subjected to micronization pretreatment, and the preparation process steps are reduced; the prepared alchlorine dipropionate cream is uniform and fine in cream body; and auxiliary materials in the prescription are economical and easy toobtain, the process operation is simple, and industrial mass production is facilitated. The adopted solvent system provides an idea for development of other external dosage forms of alchlorine dipropionate including ointment, lotion and gel.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a cream preparation of aclomethasone dipropionate and a preparation process thereof. Background technique [0002] Glucocorticoids often have obvious anti-inflammatory effects when used externally, and have good curative effects on a variety of skin diseases, and they occupy an important position in externally applied drugs in dermatology. Aclomethasone dipropionate is a low-medium-efficiency corticosteroid drug, which has anti-inflammatory, antipruritic and vasoconstrictive effects clinically. Aclomethasone dipropionate has definite clinical curative effect, can significantly relieve skin inflammation and pruritus symptoms, and improve the quality of life of patients; it is applicable to a wide range of people, and can be applied to adults, the elderly and children aged ≥1 year; the incidence of adverse reactions is low, and patients Well tolerated, aclomethasone dipr...

AI Technical Summary

Problems solved by technology

The cream preparation of aclomethasone dipropionate was first developed by Schering-Plough Company, and there is no such formulation in the market in China

When the particle size of the raw material D90> 10μm, use 10% propylene glycol to dissolve 0.05% aclomethasone dipropionate, even if it is stirred at 60-70℃ for more than 2 hours, there will still be a large amount of raw materials The drug cannot be completely dissolved; even when the particle size of the raw material D90≤10μm, some raw materials still cannot be completely dissolved under the same temperature and for the same time

On the one hand, the increase in the amount of solvent will undoubtedly lead to an increase in the cost of the preparation. On the other hand, the long-term stirring process at high temperature increases the risk of alclomethasone dipropionate degradation. The preparation process of clomethasone is more cumbersome and further increases the cost. In addition, aclomethasone dipropionate is unstable and prone to degradation in the solvent of propylene glycol, so propylene glycol is not the best solvent

[0006] Patent CN201810239914.1 discloses a suspension type cream component and preparation method of aclomethasone dipropionate, the alclomethasone dipropionate cream It is prepared into a suspension type cream to increase its stability, but this patent has not yet solved the problem of preparation of a solution type cream, and the particle size of the main ingredient still needs to be controlled before it is dispersed

[0007] Alclomethasone dipropionate is poorly soluble, and there is no report on polymorphic forms. Tests show that alclomethasone dipropionate precipitates in various solvents The crystal form of aclomethasone dipropionate is consistent, and there is no suitable means to change the solubility of aclomethasone dipropionate

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