FORMULATION DEVELOPMENT OF ANTIHYPERTENSIVE DRUG LABETALOL HCl INJECTION
H. Padmalatha*, G. Shirisha, P.S. Vasahi Laxmi, K. Manasa, M. Sravan Kumar, Y. Madhu and N. Jyothi Reddy
The aim of the present study to develop a pharmaceutically acceptable, stable and reproducible generic formulation of labetalol hydrochloride injection. Labetalol is a unique parenteral that competitively blocks alpha- and beta-adrenergic receptors. The main objective of the study was to formulate a safe and stable Labetalol Hydrochloride Injection USP (labetalol hydrochloride) with the dose of 5 mg/ mL. Drug, methyl paraben, propyl paraben, EDTA, dextrose, order of mixing was determined in pre-formulation development. Based on D-value, moist-heat sterilization method (121°C for 20 mins) is chosen for the developed injection formulation. The Process compatibility study reveals that injection potency and purity did not affected when exposed to stainless steel and process tubing. The filter compatibility study demonstrates that the Labetalol Hydrochloride Injection passes through filter without having drug loss due to binding of the drug to the membrane. Stability study of developed formulation conducted at Nitrogen purged environment, different pH, and various temperatures are tested over time for the amount of drug, methylparaben, propylparaben, EDTA, impurities, and particulate matter clearly indicated the drug product was stable. Labetalol Hydrochloride injection passes the entire quality control release test and there were no mechanical issues during the process. Thus, the product can be manufactured at a large scale.
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