Abstract

AN APPROACH TO FORMULATE AND EVALUATE LABETALOL AS FAST DISSOLVING TABLETS

Manoj Varma Gottumukkala *, Senthil Kumar K , Dr. Mohammed Gulzar Ahmed and
Krishna K

Abstract

Delivery of drugs is always been a challenge and is the most important aspect in formulation. Drugs are usually delivered via different delivery systems and selection of the system depends on drug solubility, bio availability, half life, site of action, etc. Oral delivery is usually the most preferred route of drug administration, and there have been many advances in controlling the release rate of a drug and its bioavailability. Increased patient compliance is important for any Drug delivery system. Many patients do not adhere to a regime of prescribed drugs because of difficulty in administration or the taste of a drug. So it is vital to ensure the convenient administration of a drug. In the present work, fast dissolving tablets of Labetalol were prepared using novel co-processed superdisintegrants and physical mixtures consisting of crospovidone and sodium starch glycolate in the different ratios 1:1, 1:2, 1:3 and in vice versa. Labetalol is a drug of choice which is used in treatment of Hypertension and Angina. Drug compatibility with excipients was checked by FTIR studies. After examining the flow properties of the powder blends the results are found to be with in prescribed limits and indicated good flow properties. It was then subjected to tablet compression. All the formulations were subjected to post compression parameters like hardness and friability and they showed good mechanical strength and resistance. The wetting time is an important criteria for understanding the capacity of disintegrants to swell in the presence of little amount of water and were found to be in the range of 21 to 55 sec. Among all the designed formulations, formulation F5 was found to be promising and it showed an in-vitro disintegration time of 21 sec, which facilitates its faster disintegration in the mouth. The formulation F5containing co-processedsuperdisintegrant(3:1 mixture of crospovidone and sodium starch glycolate) emerged as the overall best formulation based on drug release characteristics with 6.8 pH Phosphate buffer as dissolution medium. Short-term stability studies on promising formulation F5 indicating no significant changes in hardness, drug content and in-vitro drug release. From this study, it can be concluded that dissolution rate of Labetalol FDTs can be enhanced by the use of co-processed superdisintegrants.

Keywords: Co-processed superdisintegrants, Labetalol, Crospovidone, sodium starch glycolate and direct compression.