Ciclopirox olamine vaginal suppository composition and preparation method thereof

Abstract

The invention discloses a ciclopirox olamine vaginal suppository composition. The composition contains a spectrum antifungal drug ciclopirox olamine, a water-soluble matrix, a dissolution-assisting agent and a suitable acid, can be dissolved in vagina to be released, and also has a significant increase in stability. The composition contains the pharmaceutically effective amount of ciclopirox olamine dispersed in a suppository matrix, and the suppository matrix contains the water soluble matrix and the dissolution-assisting agent. The suppository matrix also contains purified water and the acid, and the dissolution-assisting agent is a combination of poloxamer 188 and polysorbate 80.

Description

technical field [0001] The invention relates to a vaginal suppository, in particular to a ciclopirox olamine vaginal suppository composition and a preparation method thereof. It belongs to the field of medical technology. Background technique [0002] Suppositories are widely used for rectal and vaginal administration. The base of suppositories has an important impact on the formation of suppositories and the release of active ingredients. There are two types of bases, oil-soluble bases and water-soluble bases. Vaginal suppositories require the matrix to have appropriate hardness at room temperature and not deform or break when inserted into the cavity. It is easy to soften and melt at body temperature, and can be mixed or dissolved in body fluids; it has wetting ability, high water value, and is suitable for the pH environment of the vagina; it does not affect the formation of suppositories due to the transformation of crystal forms; it is suitable for cold The suppositor...

AI Technical Summary

Problems solved by technology

[0004] 1. The ciclopirox olamine vaginal suppository with oil-soluble matrix softens at a body temperature of 37°C to exert its curative effect, so it is greatly affected by the environmental temperature in terms of transportation and storage. At present, the packaging of suppositories is mostly aluminum foil or plastic. It is easily deformed by extrusion, and what is more serious is that the softened active ingredient is incompatible with the matrix, which leads to easy stratification. Even if it is cooled and formed again, the stratified suppository cannot return to the mixed state, resulting in drug loss. Efficiency problem

[0005] 2. The active ingredient is a hydrophilic drug, which is incompatible with the mixed fatty acid glycerides of the oily matrix, which limits the choice of acidity regulators. Ciclopirox olamine can exert the greatest ability to inhibit fungi in an environment of pH 5.0-7.0. Water-soluble acids cannot be used, only low-melting solid acids can be used to melt and mix in the oily matrix when heated, such as benzoic acid, etc.

After the matrix is ​​softened, the active ingredient wrapped in an oil-soluble matrix cannot be released into the vaginal fluid at the same time due to the different solubility of the active ingredient and the acid in the vaginal fluid, so it cannot be guaranteed that the active ingredient will exert its curative effect within the optimal pH range

[0006] 3. For suppositories prepared with oil-soluble bases, in terms of pH monitoring and detection methods, affected by the base, the suppositories can only be placed in a certain amount of water, heated to melt them, shake vigorously, and placed in a cold place to solidify the base. The encapsulated active ingredient and acid are dissolved in water to measure the pH. The disadvantage of this method is that despite vigorous shaking, the active ingredient and acid are encapsulated by the matrix and cannot be completely dissolved in water, resulting in a large deviation in pH measurement.

The suppository prepared from the above composition, because the proportion of the water-soluble base poloxamer 188 is 65 to 90 times that of the active substance, the weight of each suppository reaches 7.6g or even more; the weight of the vaginal suppository is 2g to 5g The most suitable weight is 2.5g-3.5g, and the most suitable weight is 2g-3g. Excessive weight will reduce the patient's compliance with drug administration; in the preparation process, the mixing of water-soluble and oil-soluble materials It is impossible to completely avoid the miscibility of the two when used. The active ingredient is suspended in the molten matrix in an unstable state. It must be stirred before dispensing, otherwise it is easy to separate.

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