Studies On Bupropion Hydrochloride Osmotic Pump Controlled Release Tablets

Bupropion hydrochloride is a structurally novel antidepressant drug with neurochemical properties different from those of the commonly used tricyclic antidepressants. In this paper, based on investigation of the properties of the drug and excipients, bupropion hydrochloride was selected as the model drug to prepare elementary osmotic pump tablets . In this controlled release tablets, MCC,NaCl and PVP-K30 were chosen to prepare the core tablets, acetate cellulose and PEG1500 were used in coating .Under the condition of constant coating parameters, single factor tests were carried out on the formulation of core tablets and coating materials, procedure as well as the in vitro release condition, which affect the release behavior of bupropion hydrochloride controlled release tablets. Different factors on drug release behavior were analyzed by similarity factor method. Results showed that the amount of NaCl, the amount and the kind of PEG, the weight of coating all influenced the drug release behavior, while the diameter of orifice, the release medium and the method of dissolution had no significant effects. Hardness of core tablets also had no obvious effect on the release behavior of bupropion hydrochloride controlled release tablets.In the paper, based on the investigation of factors analysis, orthogonal experiment designs were used to optimize the formulation. The results indicated that the drug release profiles of the optimal formulation had excellent zero-order release character in vitro (r =0.9943) from 0 to 10 hours. In addition, the results of stability experiments showed that this product was sensitive to humidity but was stable under other conditions.The method of detecting drug concentration in plasma was based on the reference and our own exploration. The two periods cross-over design was used and the time-concentration curve of the test and reference tablets was plotted. AUC_0-∞, T_max, C_max, and t_1/2 were...