Oral mucosal bioadhesive tablets of pectin and HPMC: In vitro and in vivo evaluation

S. Miyazaki; N. Kawasaki; T. Nakamura; M. Iwatsu; T. Hayashi; W. M. Hou; D. Attwood

doi:10.1016/S0378-5173(00)00491-9

Oral mucosal bioadhesive tablets of pectin and HPMC: In vitro and in vivo evaluation

S. Miyazaki, N. Kawasaki, T. Nakamura, M. Iwatsu, T. Hayashi, W. M. Hou, D. Attwood

Research output: Contribution to journal › Article › peer-review

Abstract

The potential of tablets containing 1:4, 1:1 and 4:1 weight ratios of pectin and hydroxypropyl methylcellulose (HPMC) for the sustained release of diltiazem by sublingual administration has been investigated. Measurements of maximum adhesive force to rat peritoneal membrane indicated a satisfactory bioadhesive strength. An in vitro sustained release of diltiazem over 5 h was achieved with bilayer tablets composed of a drug-free ethylcellulose layer in addition to the pectin/HPMC layer containing drug. Plasma concentration-time curves obtained following sublingual administration to rabbits of single and bilayer tablets with 1:1 weight ratios of pectin and HPMC showed evidence of sustained release of diltiazem. Bioavailability of diltiazem was 2.5 times that achieved by oral administration for single layer tablets and 1.8 times for the bilayered tablets. (C) 2000 Elsevier Science B.V.

Original language	English
Pages (from-to)	127-132
Number of pages	5
Journal	International Journal of Pharmaceutics
Volume	204
Issue number	1-2
DOIs	https://doi.org/10.1016/S0378-5173(00)00491-9
Publication status	Published - 20 Jun 2000

Keywords

Diltiazem
Pectin/HPMC tablets
Sublingual drug delivery
Sustained release

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10.1016/S0378-5173(00)00491-9

Cite this

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title = "Oral mucosal bioadhesive tablets of pectin and HPMC: In vitro and in vivo evaluation",

abstract = "The potential of tablets containing 1:4, 1:1 and 4:1 weight ratios of pectin and hydroxypropyl methylcellulose (HPMC) for the sustained release of diltiazem by sublingual administration has been investigated. Measurements of maximum adhesive force to rat peritoneal membrane indicated a satisfactory bioadhesive strength. An in vitro sustained release of diltiazem over 5 h was achieved with bilayer tablets composed of a drug-free ethylcellulose layer in addition to the pectin/HPMC layer containing drug. Plasma concentration-time curves obtained following sublingual administration to rabbits of single and bilayer tablets with 1:1 weight ratios of pectin and HPMC showed evidence of sustained release of diltiazem. Bioavailability of diltiazem was 2.5 times that achieved by oral administration for single layer tablets and 1.8 times for the bilayered tablets. (C) 2000 Elsevier Science B.V.",

keywords = "Diltiazem, Pectin/HPMC tablets, Sublingual drug delivery, Sustained release",

author = "S. Miyazaki and N. Kawasaki and T. Nakamura and M. Iwatsu and T. Hayashi and Hou, {W. M.} and D. Attwood",

year = "2000",

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doi = "10.1016/S0378-5173(00)00491-9",

language = "English",

volume = "204",

pages = "127--132",

journal = "International Journal of Pharmaceutics",

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publisher = "Elsevier BV",

number = "1-2",

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TY - JOUR

T1 - Oral mucosal bioadhesive tablets of pectin and HPMC: In vitro and in vivo evaluation

AU - Miyazaki, S.

AU - Kawasaki, N.

AU - Nakamura, T.

AU - Iwatsu, M.

AU - Hayashi, T.

AU - Hou, W. M.

AU - Attwood, D.

PY - 2000/6/20

Y1 - 2000/6/20

N2 - The potential of tablets containing 1:4, 1:1 and 4:1 weight ratios of pectin and hydroxypropyl methylcellulose (HPMC) for the sustained release of diltiazem by sublingual administration has been investigated. Measurements of maximum adhesive force to rat peritoneal membrane indicated a satisfactory bioadhesive strength. An in vitro sustained release of diltiazem over 5 h was achieved with bilayer tablets composed of a drug-free ethylcellulose layer in addition to the pectin/HPMC layer containing drug. Plasma concentration-time curves obtained following sublingual administration to rabbits of single and bilayer tablets with 1:1 weight ratios of pectin and HPMC showed evidence of sustained release of diltiazem. Bioavailability of diltiazem was 2.5 times that achieved by oral administration for single layer tablets and 1.8 times for the bilayered tablets. (C) 2000 Elsevier Science B.V.

AB - The potential of tablets containing 1:4, 1:1 and 4:1 weight ratios of pectin and hydroxypropyl methylcellulose (HPMC) for the sustained release of diltiazem by sublingual administration has been investigated. Measurements of maximum adhesive force to rat peritoneal membrane indicated a satisfactory bioadhesive strength. An in vitro sustained release of diltiazem over 5 h was achieved with bilayer tablets composed of a drug-free ethylcellulose layer in addition to the pectin/HPMC layer containing drug. Plasma concentration-time curves obtained following sublingual administration to rabbits of single and bilayer tablets with 1:1 weight ratios of pectin and HPMC showed evidence of sustained release of diltiazem. Bioavailability of diltiazem was 2.5 times that achieved by oral administration for single layer tablets and 1.8 times for the bilayered tablets. (C) 2000 Elsevier Science B.V.

KW - Diltiazem

KW - Pectin/HPMC tablets

KW - Sublingual drug delivery

KW - Sustained release

U2 - 10.1016/S0378-5173(00)00491-9

DO - 10.1016/S0378-5173(00)00491-9

M3 - Article

VL - 204

SP - 127

EP - 132

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -

Oral mucosal bioadhesive tablets of pectin and HPMC: In vitro and in vivo evaluation

Abstract

Keywords

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