title: Rapidly disintegrating tablets containing taste masked metoclopramide hydrochloride prepared by extrusion-precipitation method.
abstract: The purpose of this study was to mask the intensely bitter taste of metoclopramide HCl and to formulate a rapid disintegrating tablet (RDT) of the taste-masked drug. Taste masking was done by complexing metoclopramide HCl with aminoalkyl methacrylate copolymer (Eudragit EPO) in different ratio by the extrusion-precipitation method. Drug-polymer complexes (DPCs) were tested for drug content, in vitro taste in simulated salivary fluid (SSF) of pH 6.8, taste evaluation in oral cavity and molecular property. The complex having drug-polymer ratio of 1 : 2 shows significant taste masking, confirmed by drug release in SSF and in-vivo taste evaluation; therefore, it was selected for further study. Taste evaluation of DPCs in human volunteers revealed considerable taste masking with the degree of bitterness below threshold value (0.5) within 10 s, whereas, metoclopramide HCl was rated intensely bitter with a score of +3 for 10 s. Tablets were evaluated for various parameters like tensile strength, wetting time, water absorption ratio, in-vitro disintegration time, and disintegration in oral cavity. The effect of diluents, lubricants and sweetening agent (Xylisorb) on the disintegration time was also evaluated. Tablets of batch F3 containing mannitol and microcrystalline cellulose in the ratio 1 : 1 and 8% w/w crosspovidone showed faster disintegration (within 20 s) than the marketed formulation (180 s). Good correlation between in vitro disintegration behavior and in the oral cavity was recognized. Tablets of batch F3 also revealed rapid drug release (t(90), 90 s) in SGF compared with marketed formulation (t(90), 600 s).
authors.affiliation: Department of Pharmaceutics, R C Patel Institute of Pharmaceutical Education and Research, Shirpur, India.
authors.forename: Shivsagar Ashok
authors.initials: SA
authors.lastname: Randale
authors.forename: Chandu Somatbhai
authors.initials: CS
authors.lastname: Dabhi
authors.forename: Avinash Ramrao
authors.initials: AR
authors.lastname: Tekade
authors.forename: Veena Shailendra
authors.initials: VS
authors.lastname: Belgamwar
authors.forename: Surendra Ganeshlal
authors.initials: SG
authors.lastname: Gattani
authors.forename: Sanjay Javarilal
authors.initials: SJ
authors.lastname: Surana
mesh_terms: D000932:Antiemetics / Q000737:chemistry* / Q000378:metabolism; D004339:Drug Compounding / Q000379:methods; D005079:Excipients / Q000737:chemistry; D006801:Humans; D008787:Metoclopramide / Q000737:chemistry* / Q000378:metabolism; D011109:Polymethacrylic Acids / Q000737:chemistry* / Q000378:metabolism; D012995:Solubility; D013607:Tablets; D013649:Taste
chemical_list: D000932:Antiemetics; D005079:Excipients; D011109:Polymethacrylic Acids; D013607:Tablets; C038300:methylmethacrylate-methacrylic acid copolymer; D008787:Metoclopramide