Ciclopirox olamine pessary and preparation method thereof

Abstract

The invention relates to a ciclopirox olamine pessary capable of reducing toxic and side effects of a medicament caused by systemic delivery, increasing local concentration of the medicament, fully playing the therapeutic effectiveness of the medicament and improving the adaptability of patients. The pessary can realize zero order release and is prepared by the following materials by weight portion: 1 portion of ciclopirox olamine, 65 to 90 portions of substrate, 0.2 to 3 portions of stearic acid, 0.1 to 5 portions of hydrogenated castor oil and 0.05 to 2 portions of sodium benzoate.

Description

Technical field [0001] The invention relates to a suppository for vaginal administration, in particular to a ciclopirox vaginal suppository and a preparation method thereof, and the application of the suppository in the preparation of a medicine for curing fungal vaginitis. Background technique [0002] Fungal vaginitis is mainly caused by infection with Candida albicans, Cryptococcus neoformans and other Candida bacteria. This kind of fungus can often be isolated in patients with vaginitis who are ineffective or frequently relapsed. Clinically, vaginal discharge increases. It looks like tofu residue, with itching and burning pain as the main manifestations. The predisposing factors are related to the body's low cellular immunity. The application of immunosuppressants, long-term use of broad-spectrum antibiotics, adrenal cortex hormones, anti-tumor drugs, etc. can cause imbalance of the flora in the body and change the mutual inhibition relationship between microorganisms in the ...

AI Technical Summary

Problems solved by technology

However, the systemic therapeutic effects produced by general common suppositories have the same "peak and valley" phenomenon as other common preparations. When the drug concentration is high, it may exceed the appropriate therapeutic concentration, so as to cause adverse reactions. When the drug concentration is low, it cannot produce the desired effect. curative effect

Disclosed in the Chinese patent document CN101147725A is the ketoconazole suppository for vaginal administration, which is composed of active ingredients and a hydrophilic matrix, and the systemic absorption produced by vaginal mucosal administration is reduced from 30% to 5%, which improves the safety of the drug. But there is still a "peak and valley" phenomenon, and zero-order release has not been achieved

[0007] As we all know, as a suppository for external use in the vagina, it is required that the drug can be completely spread on the surface of the vaginal mucosa in order to exert its efficacy. In addition, the speed of drug release and absorption varies with the matrix, and the prescription of the preparation directly affects the drug on the surface of the vaginal mucosa. The dose and exposure time of the drug can affect the efficacy

However, many researchers simply believe that because the vaginal epithelium has multiple layers of cells to form an absorption barrier, it is difficult for general drugs to exert systemic effects through vaginal absorption, and the mucosa basically does not absorb them, and no longer consider the systemic absorption of drugs when they are applied locally , thus causing safety hazards in the use of some drugs

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