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Mini-tablets versus pellets as promising multiparticulate modified release delivery systems for highly soluble drugs.
Int J Pharm. 2015 Jul 05; 488(1-2):86-94.IJ

Abstract

Whether mini-tablets (tablets, diameters ≤6mm) belong to single- or multiple-unit dosage forms is still questionable. Accordingly, Pharmacopoeial evaluation procedures for mini-tablets are lacking. In this study, the aforementioned points were discussed. Moreover, their potential for oral controlled delivery was assessed. The antidepressant venlafaxine hydrochloride (Vx), a highly soluble drug undergoing first pass effect, low bioavailability and short half-life was selected as a challenging payload. In an attempt to weigh up mini-tablets versus pellets as multiparticulate carriers, Vx-loaded mini-tablets were compared to formulated pellets of the same composition and the innovator Effexor(®)XR pellets. Formulations were prepared using various polymer hydrogels in the core and ethyl cellulose film coating with increasing thickness. Mini-tablets (diameter 2mm) showed extended Vx release (<60%, 8h). Indeed, release profiles comparable to Effexor(®)XR pellets were obtained. Remarkably higher coating thickness was required for pellets to provide equivalent retardation. Ethyl cellulose in the core ensured faster release due to polymer migration to the surface and pore formation in the coat. mini-tablets showed higher stability to pellets upon storage. Industrially speaking, mini-tablets proved to be superior to pellets in terms of manufacturing, product quality and economical aspects. Results point out the urgent need for standardized evaluation procedures for mini-tablets.

Authors+Show Affiliations

Department of Pharmaceutics, Pharos University, Alexandria, Egypt. Electronic address: dinagaber84@gmail.com.Department of Pharmaceutics, Alexandria University, Alexandria, Egypt. Electronic address: n.nafe3@gmail.com.Department of Pharmaceutics, Alexandria University, Alexandria, Egypt. Electronic address: Ossama.Y.Abdallah@gmail.com.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

25869450

Citation

Gaber, Dina M., et al. "Mini-tablets Versus Pellets as Promising Multiparticulate Modified Release Delivery Systems for Highly Soluble Drugs." International Journal of Pharmaceutics, vol. 488, no. 1-2, 2015, pp. 86-94.
Gaber DM, Nafee N, Abdallah OY. Mini-tablets versus pellets as promising multiparticulate modified release delivery systems for highly soluble drugs. Int J Pharm. 2015;488(1-2):86-94.
Gaber, D. M., Nafee, N., & Abdallah, O. Y. (2015). Mini-tablets versus pellets as promising multiparticulate modified release delivery systems for highly soluble drugs. International Journal of Pharmaceutics, 488(1-2), 86-94. https://doi.org/10.1016/j.ijpharm.2015.04.021
Gaber DM, Nafee N, Abdallah OY. Mini-tablets Versus Pellets as Promising Multiparticulate Modified Release Delivery Systems for Highly Soluble Drugs. Int J Pharm. 2015 Jul 5;488(1-2):86-94. PubMed PMID: 25869450.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Mini-tablets versus pellets as promising multiparticulate modified release delivery systems for highly soluble drugs. AU - Gaber,Dina M, AU - Nafee,Noha, AU - Abdallah,Osama Y, Y1 - 2015/04/11/ PY - 2014/12/12/received PY - 2015/04/08/revised PY - 2015/04/09/accepted PY - 2015/4/15/entrez PY - 2015/4/15/pubmed PY - 2016/2/4/medline KW - Mini-tablets KW - Modified release KW - Multiparticulate system KW - Pellets KW - Venlafaxine hydrochloride SP - 86 EP - 94 JF - International journal of pharmaceutics JO - Int J Pharm VL - 488 IS - 1-2 N2 - Whether mini-tablets (tablets, diameters ≤6mm) belong to single- or multiple-unit dosage forms is still questionable. Accordingly, Pharmacopoeial evaluation procedures for mini-tablets are lacking. In this study, the aforementioned points were discussed. Moreover, their potential for oral controlled delivery was assessed. The antidepressant venlafaxine hydrochloride (Vx), a highly soluble drug undergoing first pass effect, low bioavailability and short half-life was selected as a challenging payload. In an attempt to weigh up mini-tablets versus pellets as multiparticulate carriers, Vx-loaded mini-tablets were compared to formulated pellets of the same composition and the innovator Effexor(®)XR pellets. Formulations were prepared using various polymer hydrogels in the core and ethyl cellulose film coating with increasing thickness. Mini-tablets (diameter 2mm) showed extended Vx release (<60%, 8h). Indeed, release profiles comparable to Effexor(®)XR pellets were obtained. Remarkably higher coating thickness was required for pellets to provide equivalent retardation. Ethyl cellulose in the core ensured faster release due to polymer migration to the surface and pore formation in the coat. mini-tablets showed higher stability to pellets upon storage. Industrially speaking, mini-tablets proved to be superior to pellets in terms of manufacturing, product quality and economical aspects. Results point out the urgent need for standardized evaluation procedures for mini-tablets. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/25869450/Mini_tablets_versus_pellets_as_promising_multiparticulate_modified_release_delivery_systems_for_highly_soluble_drugs_ DB - PRIME DP - Unbound Medicine ER -