Physicochemical, pharmacokinetic, and pharmacodynamic characterization of isradipine tablets for controlled release

• Type: Article in International Scientific Journal
• Date: 2020

Authors

Venkatesh, DN (Author) Other; Meyyanathan, SN (Author) Other; Shanmugam, R (Author) Other; Kamatham, SS (Author) Other; Campos, JR (Author) Other; Dias Ferreira, J (Author) Other; Sanchez Lopez, E (Author) Other; Cardoso, JC (Author) Other; Severino, P (Author) Other; Souto, EB (Author) Other

Journal

Title: Pharmaceutical Development and Technology

Pages: 1-9

ISSN: 1083-7450

Publisher: Taylor & Francis

Indexing

ISI Web of Knowledge - 3 Citations

Scopus - 3 Citations

Other information

Authenticus ID: P-00S-W09

DOI: 10.1080/10837450.2020.1839495

Abstract (EN): Isradipine is a dihydropyridine calcium channel blocker (CCB) commonly used as vasodilator with antihypertensive properties. A remote-controlled release formulation for isradipine would substantially improve the clinical outcomes of the patients requiring chronic long-term treatment. In this work, sustained release (SR) tablets of isradipine, composed of hydroxypropylmethyl cellulose (HPMC), have been produced by wet granulation and their in vitro and in vivo characterization was compared to a conventional tablet dosage form of immediate release (IR) as preliminary assessment. Tablets composed of 15.0% (wt/wt) HPMC exhibited a SR profile over a period of 24 hours. The release of isradipine followed a Fickian diffusion pattern obeying to the first order kinetics and the extent of absorption was even higher in comparison to the developed conventional tablets, which showed immediate drug release. In vivo studies were carried out in rabbits, showing that the extent of isradipine absorption from the developed tablets was higher in comparison to IR tablets due to the modified release profile obtained for the former (p < 0.05). Our results suggest that SR tablets of isradipine are an efficient solid dosage form to overcome the limitations encountered in conventional IR tablets.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 9