Fluorohydrocortisone acetate tablet and preparation method thereof

Abstract

The fluhydrocortisone acetate tablet is mainly prepared from fluhydrocortisone acetate, lactose, a disintegrating agent, a flow aid and a lubricant, the disintegrating agent is directly pressed starch, and the fluhydrocortisone acetate tablet does not contain ionic auxiliary materials. The preparation method comprises the following steps: (1) sieving the fluorohydrocortisone acetate and the lactose, adding the sieved fluorohydrocortisone acetate and lactose into a mixer, and then adding the directly pressed starch for mixing; (2) adding a flow aid into the mixed material obtained in the step (1), and continuously mixing; (3) adding a lubricant into the mixed material obtained in the step (2), and carrying out final mixing; and (4) tabletting and molding the mixed material obtained in the step (3) to obtain the hydrocortisone acetate tablet. The direct-pressed starch is innovatively adopted to replace a traditional ionic auxiliary material to serve as a disintegrating agent, so that negative effects caused by the use of the ionic auxiliary material can be avoided, and the storage stability of the hydrocortisone acetate tablet can be improved under the condition of ensuring that the dissolution rate of the product is consistent with that of an original developed agent; and the use safety of the product is further ensured.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparation, in particular to a fludrocortisone acetate tablet with high storage stability and a preparation method thereof. Background technique [0002] Fludrocortisone acetate tablets are used for the treatment of salt-depriving congenital adrenal hypersensitivity and salt-depriving chronic adrenal insufficiency (Addison's disease). [0003] The original preparation of fludrocortisone acetate tablets is Florinef Funeng Tablet produced by Aspen Japan K.K. According to the instructions, the excipients used in the original preparation are: calcium hydrogen phosphate dihydrate, corn starch, talc, magnesium stearate, sodium benzoate, anhydrous lactose and lactose monohydrate. The stability of the original preparation agent is poor, and fludrocortisone acetate is easily degraded. In the original preparation agent, it is necessary to strictly control the storage temperature to control the degradation im...

AI Technical Summary

Problems solved by technology

Although it can be stored at room temperature, the rate of increase of related substances is still relatively fast. It is stored at 40°C and RH75%. The changes of related substances are shown in Table 2 in Comparative Example 2 below.

Generic pharmaceutical companies such as Mylan have improved the prescription of fludrocortisone acetate tablets, and the storage stability has been improved to a certain extent under the condition that the product dissolution rate is consistent. However, fludrocortisone acetate will degrade when stored under accelerated conditions. There is still a large increase in impurities, which affects the safety of the product

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