Gryshchenko M. Development of composition and technology of tablets Succiphenate

The dissertation provides theoretical and experimental grounding of the formulation and manufacturing technology for a new medical agent in the form of coated tablets with haemostatic properties. We conducted the study of physical-chemical and technological properties of the testing substance sodium salt of acetylsuccinanilic acid (named Succiphenate). This includes crystallography, particle size, apparent density, true density, angle of repose, dissolution ability and other characteristics of the substance. The pharmacokinetic parameters of Succiphenate tablets were evaluated in the dose of 50mg/kg on rabbits with average weight of 3kg. The results showed statistically significant differences between Succiphenate given orally in the form of powder, enteric-coated tablets and tablets without coating in the area under the curve, as well as the absolute and relative bioavailability, maximum concentration, mean time for absorption, and other pharmacokinetic aspects. The analysis showed a five fold increase in mean retention time and over two fold increase in absolute bioavailability with enteric-coated tablets compare to the drug given in the form of a powder or uncoated tablets. We performed stability study of Succiphenate tablets, which consisted of three steps: forced degradation, packaging selection and formal stability testing. A shelf life of 48 months was determined. Succiphenate tablets in blister packaging are demonstrated to be chemically, physically and microbiologically stable.