<abstract xmlns="http://www.w3.org/1999/xhtml"><p>The present research work deals with the development of a time delayed chronotherapeutic formulation of felodipine (FD) aimed at rapid drug release after a desired lag time in the management of hypertension. The developed system comprises a drug core embedded within a swellable layer and coated with an insoluble, water permeable polymeric system. FD cyclodextrin complex was used as an active core while ethyl cellulose was used as an effective coating layer. Dissolution studies of the complex revealed that there was a 3-fold increase in dissolution of the complex compared to plain FD. This dissolution enhancement and rapid drug release resulted from FD amorphisation, as confirmed by XRD, DSC and SEM studies. FTIR and 1H NMR studies confirmed the complex formation between FD and cyclodextrin based on the observed hydrogen bond interactions. FD release was adequately adjusted by using a pH independent polymer, <italic>i.e.</italic>, ethyl cellulose, along with dibutyl phthalate as plasticizer. Influence of formulation variables like polymer viscosity, plasticizer concentration, super disintegrant concentration in the swellable layer and percent coating weight gain was investigated to characterize the lag time. Upon permeation of water, the core tablet swelled, resulting in the rupture of the coating layer, followed by rapid drug release. The developed formulation of FD showed a lag time of 5-7 h, which is desirable for chronotherapeutic application.</p></abstract>

The present research work deals with the development of a time delayed chronotherapeutic formulation of felodipine (FD) aimed at rapid drug release after a desired lag time in the management of hypertension. The developed system comprises a drug core embedded within a swellable layer and coated with an insoluble, water permeable polymeric system. FD cyclodextrin complex was used as an active core while ethyl cellulose was used as an effective coating layer. Dissolution studies of the complex revealed that there was a 3-fold increase in dissolution of the complex compared to plain FD. This dissolution enhancement and rapid drug release resulted from FD amorphisation, as confirmed by XRD, DSC and SEM studies. FTIR and 1H NMR studies confirmed the complex formation between FD and cyclodextrin based on the observed hydrogen bond interactions. FD release was adequately adjusted by using a pH independent polymer, i.e., ethyl cellulose, along with dibutyl phthalate as plasticizer. Influence of formulation variables like polymer viscosity, plasticizer concentration, super disintegrant concentration in the swellable layer and percent coating weight gain was investigated to characterize the lag time. Upon permeation of water, the core tablet swelled, resulting in the rupture of the coating layer, followed by rapid drug release. The developed formulation of FD showed a lag time of 5-7 h, which is desirable for chronotherapeutic application.

Felodipine β-cyclodextrin complex as an active core for time delayed chronotherapeutic treatment of hypertension

Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Mumbai, India

Acta Pharmaceutica

The present research work deals with the development of a time delayed chronotherapeutic formulation of felodipine (FD) aimed at rapid drug release after a...

Felodipine β-cyclodextrin complex as an active core for time delayed chronotherapeutic treatment of hypertension

Pubblicato online: 06 nov 2012

Pagine: 395 - 410

DOI: https://doi.org/10.2478/v10007-012-0023-0

Parole chiave
felodipine, b-cyclodextrin, chronotherapeutic, ethyl cellulose

This content is open access.

Felodipine β-cyclodextrin complex as an active core for time delayed chronotherapeutic treatment of hypertension

Pubblicato online: 06 nov 2012

Pagine: 395 - 410

DOI: https://doi.org/10.2478/v10007-012-0023-0

Parole chiavefelodipine, b-cyclodextrin, chronotherapeutic, ethyl cellulose

This content is open access.

Parole chiave
felodipine, b-cyclodextrin, chronotherapeutic, ethyl cellulose