title: Development of Polyethylene Glycol and Hard Fat-Based Mucoadhesive Tablets Containing Various Types of Polyvinyl Alcohols as Mucoadhesive Polymers for Buccal Application.
abstract: Topical drug application has the advantage of avoiding systemic side effects. We attempted to develop a long-acting matrix-type tablet containing indomethacin (IM) with low physical stimulus and potent mucoadhesive force to treat pain caused by oral aphtha. A mixture of polyethylene glycol (PEG) and hard fat was used as the tablet base. Ethylcellulose was added to the base in an attempt to control drug release. Tablets with PEG as a base were also prepared for comparison. Polyvinyl alcohols (PVAs) with various degrees of saponification were added to increase the mucoadhesive force. From the optical microscopic observations, formulations using PEG and hard fat exhibit PEG/hard fat dispersions caused by the stabilizing effects of PVA. Although the tablets using PEG and hard fat showed sufficient adhesiveness and sustained drug release, those using PEG as the base did not. Drug release was controlled by the amount of hard fat and the saponification degree of PVA. The drug release rate was most increased in a tablet containing PVA with an intermediate degree of saponification, PEG and hard fat. From differential scanning calorimetry and powder X-ray diffraction, IM was considered to exist in the molecular phase. From the results of buccal administration of tablets to rats, highest tissue concentrations were observed in the tablet containing PVA with the intermediate degree of saponification using PEG and hard fat, and the plasma concentrations were sufficiently low in comparison.
authors.affiliation: Department of Drug Delivery Research, Hoshi University.
authors.forename: Yuri
authors.initials: Y
authors.lastname: Ikeuchi-Takahashi
authors.affiliation: The Nippon Synthetic Chemical Industry Co., Ltd.
authors.forename: Ayaka
authors.initials: A
authors.lastname: Kobayashi
authors.affiliation: Department of Drug Delivery Research, Hoshi University.
authors.forename: Hiraku
authors.initials: H
authors.lastname: Onishi
mesh_terms: D000268:Adhesiveness; D000278:Administration, Buccal; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D065546:Drug Liberation; D005223:Fats / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D007213:Indomethacin / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D009061:Mouth Mucosa / Q000737:chemistry / Q000378:metabolism*; D011092:Polyethylene Glycols / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D011142:Polyvinyl Alcohol / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D017207:Rats, Sprague-Dawley; D013607:Tablets
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D005223:Fats; D013607:Tablets; D011092:Polyethylene Glycols; D011142:Polyvinyl Alcohol; D007213:Indomethacin
keywords: buccal; controlled release; formulation; indomethacin; mucosal delivery; solid dosage form