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Question

Posted on: November 29 2016

How to prepare stable medroxyprogesterone acetate suspension

Formula: Medroxyprogesterone acet 2g; Salicylz 6g; Lactic acid 6g; Zn Sulf 2g; Propylene glycol 20g; Antisept. OPL 200 ml Aqua ad 300ml Should excipients be added (Tween 80?) or simply rub progesterone with propylene glycol and then complement with the remainder.

Answer

This is a complex formula with a mixture of water-soluble raw materials and alcohol-soluble. The first question, which I suggest is the behavior of znsulfate in this solvent mixture. The second question is the solubility of medroxyprogesterone acetate. The first is soluble in water but by addition of alcohol risks the solubility to reduce so that crystallization is very probable.  

Medroxyprogesterone acetate:   Freely soluble in chloroform; soluble in acetone and in dioxane; sparingly soluble in alcohol and in methanol; slightly soluble in ether; Insoluble in water. This data is very little useful in the context of this composition.  

Medroxyprogesterone acetate will need to be suspended. As a viscosite booster, Hydroxypropylcellulose (HPC) is considered due to the large amount of alcohol.  

Perhaps it is easiest to resolve the znsulfate to a very fine powder and mix it in a mortar with medroxyprogesterone acetate and HPC. The remaining ingredients can be dissolved in the alcohol and the content of the mortar is slowly and stirring well this alcoholic solution is added. This whole is transferred quantitatively into a measuring cylinder, with water on volume brought. The suspension is well-stirred to homogenous and poured into a bottle.   "Shake before use"  

An interesting modification may be the replacement Ofznsulfate by Znacetate, which is also used in the erythromycin lotio. The solubility of the acetate in alcohol-water mixtures is better as for the sulfate. Of course, a small conversion is required.  

 

 

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