Screening, preparation, characterization, solubility, stability and bioavailability of polymorphic forms of contraception drugs

抄録

Solid drugs possess generally crystal structures. Different crystal forms of the

same drug can directly affect its clinical effect by influencing the physical and

chemical properties. Therefore, it is important to screen the polycrystalline type of drugs and determine the crystal type of drugs, furthermore, the druggability analysis and safety evaluation of all kinds of crystal type were performed to determine the optimal crystal form for the drug, which is significant for the drugs to control the quality, increase the stability, and ensure clinical curative effect.

We screened the polymorphic forms about 20 contraception drugs by means of physical or chemical methods. All polymorphs have been synthesized by means of physical or chemical methods, characterized by X-ray powder diffraction, thermogravimetric, differential scanning calorimetry, IR spectra. Meanwhile, the crystal structure of the new solvates were determined by single crystal X-ray structure analysis.

We got more than 50 polymorphs. The polymorphs' solubility was tested by high performance liquid chromatography and dissolution curves were drawn. The pharmacokinetics in wistar rats of some polymorphs was also investigated, the results indicating that the bioavailability of these contraception drugs can be improved.

Our study on polymorphs of contraception drugs could provide a variety of

crystal material composition, preparation methods and solubility.