Research On Preparation And Quality Of TY-202Tablets

Currently, pulmonary hypertension is an uncommon clinical disease, with high mortality and morbidity. The clinical diagnosis has been an important problem of the medical profession. Clinical studies showed that, pulmonary hypertension have a great relations to the vasoconstriction and situ thrombosis. Reduce cardiac load and improve blood supply situation is an important way to treat pulmonary hypertension. With the deepening of clinical studies, endothelin receptor antagonists get more attentions with its significant clinical effects in the treatment of pulmonary arterial hypertension. TY-202as an endothelin antagonist, has a significant clinical effect on inhibiting pulmonary vasoconstriction and vascular remodeling by suppressing the receptor of ETA and ETB. The effect of TY-202has been popular affirmed, and various preparations have been approved by FDA in the United States and neighboring countries. Therefore, the research and development of TY-202has considerable market prospects, which plays an important role in alleviating the lack of clinical drugs and reducing the economic cost of medical for pulmonary hypertension patients.By examining the TY-202solubility, oil-water partition coefficient, melting point and other physicochemical properties, founding that it belongs to BCS Class Ⅱ drugs. The establishment of vitro dissolution evaluation methods, according to the dissolution assay (Chinese Pharmacopoeia Ⅱ, Appendix XC, method Ⅱ), giving priority to pH5.0acetate buffer900ml as solvent, speed of50r/min, detected at220nm wavelength, through the HPLC to calculate the dissolution of each piece and comparison with foreign commercial product, evaluate the consistency of the original research. The prescription process includes tablet preparation and coating treatment, through orthogonal test, take the tablet weight difference, dissolution and hardness as the composite indicator, screening the best prescription and optimization, at last determine the final prescription. Executed tablet coating operation, and taked the coating efficiency as index, orthogonal experiment determine the optimum of the coating conditions.in accordance with the tablet formulations and coating conditions, we produced three batches of pilot production.Establish HPLC method for the studies of content, high performance liquid chromatography for the related substances, and evaluate the quality of the tablet. The accelerated test showed that appearance, content and dissolution of three batches of sample had no significant change, related substances had varying degrees of change, but they are all in compliance; long-term test showed that the parameters of commercially packaging sample were not changed significantly, and all in the quality control range.