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Published on:Oct 2016
Indian Journal of Pharmaceutical Education and Research, 2016; 50(4):549-562
Original Article | doi:10.5530/ijper.50.4.7

Dissolution Rate Enhancement of Entacapone and Formulation of its Oro- Dispersible Tablets: Applying Statistical Design


Authors and affiliation (s):

Mahapatra Anjan Kumar1*, Padala Narasimha Murthy1, Nagampalli Haritha Sameeraja2 and Palei Narahari Narayan3

1Royal College of Pharmacy and Health Sciences, Berhampur-2, INDIA.

2Central Drugs Standard Control Organization (Head Quarter), New Delhi, INDIA. 3Sree Vidyanikethan College of Pharmacy, Tirupati, INDIA.

Abstract:

The major aim of the study was to enhance the solubility and dissolution rate of entacapone by complexation with cyclodextrins (β-CD/HP β-CD). Further the selected cyclodextrin complexes are deigned to formulate oro-dispersible tablets (ODTs) using selected concentration of PEG 4000 as hydrophilic polymer and crospovidone as superdisintegrant. The phase solubility behavior of entacapone in presence of various concentrations of β-CD, HP β-CD, PEG 4000, PVP and Poloxamer 188 (0.25-5% w/v) was studied at 37 ± 2oC. Gibbs free energy (ΔG° tr) values in negative, indicates the spontaneous nature of entacapone solubilization. From dissolution rate studies it was observed β-CD complexes were better over HP β-CD and are formulated to ODTs by direct compression method. Response surface modeling approach (23 full factorial design) was used for design, development and data interpretation. The responses of the design were analyzed using Design Expert 8.0.7.1 (Stat-Ease Inc., USA). The optimized formulation was selected on the basis of software analysis with an overall desirability factor. The optimized formulation showed disintegration time of 40-42s, friability of 0.55% and a release of more than 85% within 45 m. The physicochemical characterizations of inclusion complexes and the optimized tablet formulation were done by Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD).

Key words: Cyclodextrins, Entacapone, Inclusion complexation, Dissolution rate, Disintegration, 23 Factorial design.

 

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The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.

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