Development and mathematical simulation of theophylline pulsatile release tablets.
Theophylline pulsatile release tablets consisting of a fast-swelling core with a water-insoluble ethylcellulose were developed. Effects of coating material, the amount of the plasticizer, subcoating, the type of the disintegrant, and coating level on the release profiles were investigated. Results showed that ethylcellulose was the best candidate polymer for pulsatile release tablets. Rupture time increased with increasing the amount of the plasticizer, but 15% plasticizer provided the best release profiles. Tablets with Methocel E50 as subcoating was most optimal in order to achieve a long lag time and followed by a rapid release. The lag time of tablets containing different disintegrants increased in the following order: croscarmellose (Ac-Di-Sol) < sodium starch glycolate (Explotab) < low-substituted hydroxypropyl cellulose (L-HPC) < crospovidone (Kollidon CL). And the rupture time increased with higher coating level. A mathematical model was presented to predict the lag time prior to rupture. Results of the water uptake experiment were used to estimate the apparent diffusion coefficient of the coating tablets. The prediction of the lag time based on the presented model is in good agreement with the experimental results.
Zhu
Ying
Y
Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, Liaoning, P.R. China.
Zheng
Liangyuan
L
D000042:Absorption; D000465:Algorithms; D001993:Bronchodilator Agents / Q000008:administration & dosage* / Q000737:chemistry; D002482:Cellulose / Q000031:analogs & derivatives; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004058:Diffusion; D005079:Excipients; D006244:Hardness; D007700:Kinetics; D008855:Microscopy, Electron, Scanning; D015233:Models, Statistical; D010968:Plasticizers; D012995:Solubility; D013806:Theophylline / Q000008:administration & dosage* / Q000737:chemistry
D001993:Bronchodilator Agents; D003692:Delayed-Action Preparations; D005079:Excipients; D010968:Plasticizers; C013517:ethyl cellulose; D002482:Cellulose; D013806:Theophylline