FORMULATION DEVELOPMENT AND EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF TRAZODONE HYDROCHLORIDE

Vivek Jain1, Halki Kushwah*1, Anwar Iqbal Khan1, Geeta Parkhe2

NRI Institute of Pharmacy, Bhopal, Madhya Pradesh, India.

ABSTRACT

Formulation development is an important part of drug design and development. Bioavailability and bioequivalence are totally dependent on formulation development. Now-a-days formulation development is done by following QbD (Quality by Design).Floating drug delivery systems are the gastro retentive forms that precisely control the release rate of target drug to a specific site which facilitate an enormous impact on health care. This can be achieved by use of various polymeric substances. Trazodone Hydrochloride (TRZ), is a well-known chemical compound that is used as an antidepressant that belongs to a selective serotonin reuptake inhibitors (SARI). TRZ is used as anti-anxiety and sleep-inducing agent. The tablets of TRZ were prepared by direct compression method using gas generating agent and different polymer combinations. The prepared tablets of TRZ were evaluated for hardness, thickness, friability, weight variation, drug content uniformity, buoyancy lag time, total floating time, swelling index, in-vitro dissolution study, etc. All the compositions were resulted in adequate Pharmacopoeial limits. The varying concentration of gas generating agent and polymers was found to effect on in-vitro drug release and floating lag time. In vitro drug release of floating gastro retentive tablet of TRZ shown that the formulation F9 was found to be the best formulation as it releases 97.98% TRZ in a controlled manner for an extended period of time (up to 12 hours). The release data was fitted to various mathematical models such as higuchi, Korsmeyer-Peppas, first order and zero order to evaluate the kinetics and mechanism of the drug release. Prepared floating tablets of TRZ may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system.

Keywords:

Trazodone Hydrochloride, Gastro retentive, floating tablet, Total floating time.