Fast release formulation of tianeptine sodium: Formulation, design, characterization and toxicity study

Background: Tianeptine sodium is an antidepressant drug possessing analgesic and anti-asthmatic property. Orodispersible tablets rapidly disintegrates with in oral cavity and drug undergoes rapid absorption through oral mucosa resulting in rapid therapeutic effect. The objective of present study was development and characterization of the fast release tablets of tianeptine sodium in order to target the population with inflammatory bowel disease as it is more prevailing disorder. Method: Fast release tablets prepared by direct compression method and evaluated for pre and post compression parameters. Cross povidone is most superior to cross carmellose sodium and sodium starch glycolate as a disintegrating agent. Combination of cross povidone and cross carmellose resulted in gel like mass; prolonging the disintegration time of formulation and retarding the release of drug from formulation. Results: Drug release showed that cross povidone provided the good release profile as compared to the other superdisintegrants. Superdisintegrant concentration is also a rate limiting step for disintegration time. FTIR, DSC, TGA and XRD studies showed compatibility, thermal stability and amorphous nature of the samples used in study. Acute toxicity study conducted on swiss albino mice showed that that developed dosage form is nontoxic as no changes in physical activity and function of organs was observed. Histopathological study revealed that developed dosage form did not develop any kind of necrotic changes indicating the safety of dosage form. Conclusion: Fast release tablets of tianeptine sodium could be developed by direct compression method using the different concertation of superdisintegrants. Directly compressed tablet were safe for use in animal as administered tablets did not show any toxicity at organ level.