Design of Salbutamol EOP Tablets from Pharmacokinetics Parameters

• Published in: Pharmaceutical development and technology Vol. 8; no. 2; pp. 135 - 142
• Main Authors: Sinchaipanid, Nuttanan, Pongwai, Sansanee, Limsuwan, Pichet, Mitrevej, Ampol
• Format: Journal Article
• Language: English
• Published: New York, NY Informa UK Ltd 01.01.2003; Taylor & Francis; Informa Healthcare
• Subjects: Albuterol - administration & dosage; Albuterol - chemistry; Albuterol - pharmacokinetics; Algorithms; Biological and medical sciences; Biological Availability; Bronchodilator Agents - administration & dosage; Bronchodilator Agents - chemistry; Bronchodilator Agents - pharmacokinetics; Excipients; General pharmacology; Hardness; laser; Lasers; Medical sciences; Microscopy, Electron, Scanning; Osmogent; Osmotic Pressure; Osmotic pump tablet; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Porosity; Pressure; Respiratory system; Salbutamol; Solubility; Tablets; Compression; Pharmaceutical technology; Bronchodilator; Carbon dioxide; CO2 laser; In vitro; Osmotic pump tablet; Dosage form; Active ingredient; Salbutamol; Coated tablet; Osmogent; Osmotic pump; Release
• ISSN: 1083-7450; 1097-9867
• DOI: 10.1081/PDT-120018479

Salbutamol elementary osmotic pump (EOP) tablets were developed, and fundamental variables affecting their release characteristics were evaluated. The effects of film thickness and compression force on drug release from the tablets containing fixed amount of sodium chloride used as osmogent were evaluated. The core tablets were directly compressed at four compression forces and coated with 3% wt vol cellulose acetate in acetone to levels of 2%, 3%, and 4% wt wt. Coated tablets were drilled with CO2 laser beam to form drug delivery orifice of ∼400 μm in diameter. The drug release was found to follow zero order fashion. The release rate decreased with the increased film thickness and was not affected by the compression force or porosity. The tablets coated to 3% and 4% levels exhibited the release rates within the range calculated from pharmacokinetic data. To illustrate the effect of osmogent content, the tablets were prepared at four osmogent levels and compressed at a constant compression force. The core tablets were coated to a level of 3% wt wt. The release rate was initially increased with osmogent content and then decreased. At higher osmogent contents, the drug fraction in soluble component was decreased and resulted in the reduction of drug release. In conclusion, film thickness and osmogents played important roles in drug release from EOP tablets.