Abstract:
:Development of age-appropriate formulation suitable for pediatric and geriatric patients involves various challenges. The objective of this research was to develop extended-release oral flexible tablet (ER-OFT) formulation using carbamazepine (CBZ) as model drug for pediatric and geriatric compliance. ER-microparticles of carbamazepine, a BCS class 2, and narrow therapeutic index (NTI) drug, were prepared using ethyl cellulose as matrixing polymer and hypromellose as hydrophilic pore former. Microparticles were prepared using high-shear granulator fitted with an atomizing spray system. Granulation of carbamazepine and ethyl cellulose (EC-FP) with ethanolic binder solution resulted in ER-microparticles with extended-release >16 h. Release kinetics of ER microparticles showed Higuchi model by drug diffusion and erosion. Korsemeyer-peppas release exponent "n" value 0.42 suggested Fickian diffusion. ER-OFT was prepared by blending of ER-microparticles with water-insoluble compressible aid and disintegrating agent. ER-OFT was characterized for performance characteristics and elemental impurities. As the polymer content in formulation was <10%, the size of ER-OFT was smaller compared to marketed ER-formulations. ER-OFT showed in vitro disintegration time of <30 s as per USP and dispersion time of ∼60 to 180 s in 5 to 10 mL of water. Drug release profiles of ER-microparticles and ER-OFT were comparable as f2 values were >50. In vitro dissolution of ER-OFT was comparable to the marketed ER formulation in the pH range of GIT. ER-OFT can be orally swallowed, orally disintegrating, and used as dispersible tablets. Compared to non-disintegrating type ER-formulations, ER-OFT would provide uniform drug release in GIT with low within-subject variability an essential criterion for NTI drug.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Chandrasekaran P,Kandasamy Rdoi
10.1208/s12249-017-0715-3subject
Has Abstractpub_date
2017-10-01 00:00:00pages
2394-2409issue
7issn
1530-9932pii
10.1208/s12249-017-0715-3journal_volume
18pub_type
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