Development of pulsatile drug delivery system using novel solubilizers for antihypertensive drug
Article
Domala, R, Eedara, BB, Dhurke, RK. (2014). Development of pulsatile drug delivery system using novel solubilizers for antihypertensive drug
. 6(5), 659-664.
Domala, R, Eedara, BB, Dhurke, RK. (2014). Development of pulsatile drug delivery system using novel solubilizers for antihypertensive drug
. 6(5), 659-664.
Objective: The objective of present work was to formulate and evaluate an oral pulsatile drug delivery system to achieve time release of felodipine, based on chronopharmaceutical approach for management of hypertension. Methods: The strategy adopted was to improve solubility of felodipine by using novel solubilizers like Sepitrap 4000 and Sepitrap 80 in different ratios. Core tablets (CR) of felodipine were prepared by direct compression method using optimum ratio of felodipine and solubilizers. CR tablet was then press coated using different grades of HPMC like E5, E15 and E50 in varying ratios. Pulsatile tablets were evaluated for pre-compressional and post-compressional parameters. Swelling studies and water uptake studies were also carried out to select optimum concentration of polymer that could provide desired lag time. Results: CR tablet formulated with Sepitrap 4000 and Sepitrap 80 (1:1 ratio) showed 100.16±2.06% release in 15 and 30 min respectively. On the basis of in vitro release profile it was found that the optimized formulation F6showed the lag time of about 7.5h which showed compliance with chronotherapeutic objective of hypertension. A direct correlation between swelling and lag time was observed from swelling index and water uptake studies. Solid state characterization (FTIR, XRD studies) indicated that there was decrease in crystallinity of the drug with no interaction between drug and excipients. Conclusion: Pulsatile drug delivery system is capable of delivering the drug when and where it is required. Drug is released as a burst after a lag time (during peak morning hours) giving relief from morning surge hypertension effect.
