Preformulation Study of Dolasetron: An Insight for Formulation and Development of Nasal Formulation

Abstract

The objective of preformulation study is to develop the elegant, stable, effective and safe dosage form by establishing kinetic profile, compatibility with other formulation excipients and to establish physico-chemical parameter of new drug substance. This could provide important information for formulation design or support the need for molecular modification. So, in the present study preformulation studies were performed on Dolasetron (DS) to assess its suitability for nasal formulation. DS is a specific and selective serotonin subtypes 3 (5-HT) receptor antagonists, used to treat chemotherapy induced nausea and vomiting. The authenticity of DS was established by DSC and FITR spectra. An UV spectrophotometric method and HPLC method were employed for determination of DS in bulk and blood plasma respectively. Saturation solubility, micromeritical properties, melting point, pH, hygroscopicity and stability profile were studied. The UV method was linear in the range of 5-50 μg/ml. The low % CV values of intra-day and inter-day variations revealed that the proposed method is robust. The retention time of DS in HPLC method was found to be 2.8 min. The method was proven robust by obtaining very high regression coefficient value (0.999). The results of the physicochemical study of drug revealed suitability of DS for nasal route. Moreover, the drug was found stable in both solid as well as liquid state at different conditions.