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).
journal_name
Chem Pharm Bull (Tokyo)journal_title
Chemical & pharmaceutical bulletinauthors
Randale SA,Dabhi CS,Tekade AR,Belgamwar VS,Gattani SG,Surana SJdoi
10.1248/cpb.58.443subject
Has Abstractpub_date
2010-04-01 00:00:00pages
443-8issue
4eissn
0009-2363issn
1347-5223pii
JST.JSTAGE/cpb/58.443journal_volume
58pub_type
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journal_title:Chemical & pharmaceutical bulletin
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更新日期:1998-07-01 00:00:00
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更新日期:2002-01-01 00:00:00
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更新日期:1990-09-01 00:00:00
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更新日期:2013-01-01 00:00:00
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更新日期:2001-09-01 00:00:00
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更新日期:2006-07-01 00:00:00
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journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.40.2954
更新日期:1992-11-01 00:00:00
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journal_title:Chemical & pharmaceutical bulletin
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更新日期:2000-03-01 00:00:00
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更新日期:2000-03-01 00:00:00
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journal_title:Chemical & pharmaceutical bulletin
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更新日期:2008-10-01 00:00:00
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更新日期:1994-12-01 00:00:00
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更新日期:2000-07-01 00:00:00
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pub_type: 临床试验,杂志文章
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更新日期:2007-05-01 00:00:00