Perfusion cells for studying regional variation in oral-mucosal permeability in humans. I: Kinetic aspects in oral-mucosal absorption of alkylparabens

Yuji Kurosaki, Koji Yano, Toshikiro Kimura

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

Purpose. To evaluate regional differences in permeability of human oral mucosa. Methods. Newly designed perfusion cells were used for the investigation. The cells were applied to 5 different sites, i.e., dorsum of tongue, ventral surface of tongue, labial mucosa, floor of mouth and buccal mucosa of human volunteers. Model drugs used were methyl-, ethyl-, propyl- and butylparaben, which are passively absorbed from oral mucosa and have different lipophilicities. Biexponential disappearance profiles of the alkylparabens were analyzed kinetically using a two-compartment linear open model. Results. Both the partitioning parameters to the oral mucosa and the absorption rate constants to the blood circulation correlated to the lipophilicities of the compounds in all mucosa. As to the former parameter, no significant difference was recognized in all mucosa. While, the latter parameter exhibited the regional difference; the absorption rate constants in buccal mucosa were approximately one-half of those estimated in other oral mucosa. A positive relation was recognized between the retention in oral-mucosal compartment and the drug lipophilicity. Conclusions. The newly designed perfusion cells used in this study were useful to examine the regional variations of drug absorption from oral mucosa in humans. The absorption rate constant, the partition to oral mucosa and the residence time in oral mucosa increased with lipophilicity of the compound. The regional difference in the drug absorption process was demonstrated; the slow absorption and the prolonged retention were demonstrated in buccal mucosa.

Original languageEnglish
Pages (from-to)1241-1245
Number of pages5
JournalPharmaceutical Research
Volume14
Issue number9
DOIs
Publication statusPublished - 1997

Fingerprint

Mouth Mucosa
Permeability
Perfusion
Kinetics
Mucous Membrane
Rate constants
Tongue
Pharmaceutical Preparations
Oral Mucosal Absorption
Mouth Floor
Blood Circulation
Lip
Hemodynamics
Volunteers
Linear Models

Keywords

  • Alkylparaben
  • Human
  • Oral mucosa
  • Perfusion cell
  • Permeability
  • Regional difference

ASJC Scopus subject areas

  • Chemistry(all)
  • Pharmaceutical Science
  • Pharmacology

Cite this

Perfusion cells for studying regional variation in oral-mucosal permeability in humans. I : Kinetic aspects in oral-mucosal absorption of alkylparabens. / Kurosaki, Yuji; Yano, Koji; Kimura, Toshikiro.

In: Pharmaceutical Research, Vol. 14, No. 9, 1997, p. 1241-1245.

Research output: Contribution to journalArticle

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N2 - Purpose. To evaluate regional differences in permeability of human oral mucosa. Methods. Newly designed perfusion cells were used for the investigation. The cells were applied to 5 different sites, i.e., dorsum of tongue, ventral surface of tongue, labial mucosa, floor of mouth and buccal mucosa of human volunteers. Model drugs used were methyl-, ethyl-, propyl- and butylparaben, which are passively absorbed from oral mucosa and have different lipophilicities. Biexponential disappearance profiles of the alkylparabens were analyzed kinetically using a two-compartment linear open model. Results. Both the partitioning parameters to the oral mucosa and the absorption rate constants to the blood circulation correlated to the lipophilicities of the compounds in all mucosa. As to the former parameter, no significant difference was recognized in all mucosa. While, the latter parameter exhibited the regional difference; the absorption rate constants in buccal mucosa were approximately one-half of those estimated in other oral mucosa. A positive relation was recognized between the retention in oral-mucosal compartment and the drug lipophilicity. Conclusions. The newly designed perfusion cells used in this study were useful to examine the regional variations of drug absorption from oral mucosa in humans. The absorption rate constant, the partition to oral mucosa and the residence time in oral mucosa increased with lipophilicity of the compound. The regional difference in the drug absorption process was demonstrated; the slow absorption and the prolonged retention were demonstrated in buccal mucosa.

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