Abstract

FORMULATION AND DEVELOPEMENT OF TOLVAPTAN SELF MICRO EMULSIFYING DRUG DELIVERY SYSTEMS

Pullemla Madhuri*

ABSTRACT

Tolvaptan is an oral, once-daily, nonpeptide vasopressin V2 receptor antagonist without intrinsic agonist activity. In patients with mild heart failure, the administration of tolvaptan added to standard therapy that included non–potassium-sparing diuretics caused a significant decrease in body weight without causing hypokalemia or worsening renal function. The clinical effects of tolvaptan in patients hospitalized for heart failure were assessed in the ACTIV in CHF trial. Tolvaptan is a vasopressin receptor antagonist mainly prescribed in cases of diseases such as hyponatremia and autosomal dominant polycystic kidney disease (ADPKD). Nevertheless, clinical performance of this drug is usually hindered by its poor solubility and bioavailability. Thus, in relation to such a problem, the purpose of the study is to prepare aSMEDDS for Tolvaptan, thus improving the drug's solubility and absorption. Different surfactants and co-surfactants were used to formulate a stable SMEDDS by following a systematic approach towards oil screening. Characterization of the optimized formulation was conducted regarding droplet size, zeta potential MALVERN Zeta sizer, and stability under various conditions. In vitro studies indicated a drastic increase in solubility along with a dissolution rate compared with conventional formulations. Furthermore, permeability across intestinal cell membranes was significantly improved with microemulsion, indicating greater bioavailability potential.

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