Enhancement of Drug Dissolution of Erlotinib Tablets by Micronization Technique Using Pharmaceutical Experimental Design

Abstract

Lung cancer is the second most frequent cancer and among the top cause of death worldwide. Chemotherapy is the main therapeutic option for non-small-cell lung cancer (NSCLC), which accounts for the majority of all lung malignancies. The aim of the current work was to develop a tablet formulation having increased drug release profile to improve the bioavailability in order to reduce the dose of the drug. In this present study, Erlotinib tablet was prepared using micronization technique which showed increase drug release profile. Film-coated tablets containing Erlotinib hydrochloride (150 mg) were prepared by dry granulation technique and coated using Opadry ready-mix. Tablets were characterized for Hardness, Friability, Potency and Drug release profile. Drug release was checked in 0.1 N HCL containing 0.5 % SLS and biorelevant dissolution media up to 60 minutes. Tablets of the selected batch were subjected to dissolution in biorelevant media and compare with reference product. The improvement in the drug release was observed in the biorelevant media in comparison with reference product. The in-vitrodissolution data demonstrated the potential of micronization technology to prepare tablets with improved bioavailability of the drug.

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“…The drug dissolution of a tablet formulation made by co-sifting functional excipients and micronized erlotinib hydrochloride in biorelevant media was compared to that of a reference medication. [14] In the current scenario, various research are being done to resolve and understand and predict the BA and factor affecting the BA. Various regulatory agencies are accepting the in vitro based approaches using solubility and dissolution tests and in silico approaches with PBPK modeling.…”

“…Uncoated tablets were coated with aqueous-based Opadry white ready mix in GansCoater to a weight build-up of roughly 5.0%. [14] Table 1: Formulation of erlotinb tablets [14] The 393.4 = Mol. wt of erlotinib and 429.9 = Mol.…”