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Formulation, release characteristics, and bioavailability study of gastroretentive floating matrix tablet and floating raft system of Mebeverine HCl.
Drug Des Devel Ther. 2017; 11:1081-1093.DD

Abstract

To prolong the residence time of dosage forms within the gastrointestinal tract until all drug is released at the desired rate is one of the real challenges for oral controlled-release drug delivery systems. This study was designed to develop a controlled-release floating matrix tablet and floating raft system of Mebeverine HCl (MbH) and evaluate different excipients for their floating behavior and in vitro controlled-release profiles. Oral pharmacokinetics of the optimum matrix tablet, raft system formula, and marketed Duspatalin® 200 mg retard as reference were studied in beagle dogs. The optimized tablet formula (FT-10) and raft system formula (FRS-11) were found to float within 34±5 sec and 15±7 sec, respectively, and both remain buoyant over a period of 12 h in simulated gastric fluid. FT-10 (Compritol/HPMC K100M 1:1) showed the slowest drug release among all prepared tablet formulations, releasing about 80.2% of MbH over 8 h. In contrast, FRS-11 (Sodium alginate 3%/HPMC K100M 1%/Precirol 2%) had the greatest retardation, providing sustained release of 82.1% within 8 h. Compared with the marketed MbH product, the Cmax of FT-10 was almost the same, while FRS-11 maximum concentration was higher. The tmax was 3.33, 2.167, and 3.0 h for marketed MbH product, FT-10, and FRS-11, respectively. In addition, the oral bioavailability experiment showed that the relative bioavailability of the MbH was 104.76 and 116.01% after oral administration of FT-10 and FRS-11, respectively, compared to marketed product. These results demonstrated that both controlled-released floating matrix tablet and raft system would be promising gastroretentive delivery systems for prolonging drug action.

Authors+Show Affiliations

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Misr University for Science and Technology, 6th of October, Egypt.National Egyptian Center of Environment and Toxicological Research (NECTER), Faculty of Medicine, Cairo University, Cairo, Egypt.Department of Quality Control, Holding Company for Biological Products and Vaccines, Cairo, Egypt.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28435220

Citation

El Nabarawi, Mohamed A., et al. "Formulation, Release Characteristics, and Bioavailability Study of Gastroretentive Floating Matrix Tablet and Floating Raft System of Mebeverine HCl." Drug Design, Development and Therapy, vol. 11, 2017, pp. 1081-1093.
El Nabarawi MA, Teaima MH, Abd El-Monem RA, et al. Formulation, release characteristics, and bioavailability study of gastroretentive floating matrix tablet and floating raft system of Mebeverine HCl. Drug Des Devel Ther. 2017;11:1081-1093.
El Nabarawi, M. A., Teaima, M. H., Abd El-Monem, R. A., El Nabarawy, N. A., & Gaber, D. A. (2017). Formulation, release characteristics, and bioavailability study of gastroretentive floating matrix tablet and floating raft system of Mebeverine HCl. Drug Design, Development and Therapy, 11, 1081-1093. https://doi.org/10.2147/DDDT.S131936
El Nabarawi MA, et al. Formulation, Release Characteristics, and Bioavailability Study of Gastroretentive Floating Matrix Tablet and Floating Raft System of Mebeverine HCl. Drug Des Devel Ther. 2017;11:1081-1093. PubMed PMID: 28435220.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Formulation, release characteristics, and bioavailability study of gastroretentive floating matrix tablet and floating raft system of Mebeverine HCl. AU - El Nabarawi,Mohamed A, AU - Teaima,Mahmoud H, AU - Abd El-Monem,Rehab A, AU - El Nabarawy,Nagla A, AU - Gaber,Dalia A, Y1 - 2017/04/03/ PY - 2017/4/25/entrez PY - 2017/4/25/pubmed PY - 2017/12/26/medline KW - Compritol® KW - GRDDS KW - HPMC KW - Na alginate KW - Precirol® SP - 1081 EP - 1093 JF - Drug design, development and therapy JO - Drug Des Devel Ther VL - 11 N2 - To prolong the residence time of dosage forms within the gastrointestinal tract until all drug is released at the desired rate is one of the real challenges for oral controlled-release drug delivery systems. This study was designed to develop a controlled-release floating matrix tablet and floating raft system of Mebeverine HCl (MbH) and evaluate different excipients for their floating behavior and in vitro controlled-release profiles. Oral pharmacokinetics of the optimum matrix tablet, raft system formula, and marketed Duspatalin® 200 mg retard as reference were studied in beagle dogs. The optimized tablet formula (FT-10) and raft system formula (FRS-11) were found to float within 34±5 sec and 15±7 sec, respectively, and both remain buoyant over a period of 12 h in simulated gastric fluid. FT-10 (Compritol/HPMC K100M 1:1) showed the slowest drug release among all prepared tablet formulations, releasing about 80.2% of MbH over 8 h. In contrast, FRS-11 (Sodium alginate 3%/HPMC K100M 1%/Precirol 2%) had the greatest retardation, providing sustained release of 82.1% within 8 h. Compared with the marketed MbH product, the Cmax of FT-10 was almost the same, while FRS-11 maximum concentration was higher. The tmax was 3.33, 2.167, and 3.0 h for marketed MbH product, FT-10, and FRS-11, respectively. In addition, the oral bioavailability experiment showed that the relative bioavailability of the MbH was 104.76 and 116.01% after oral administration of FT-10 and FRS-11, respectively, compared to marketed product. These results demonstrated that both controlled-released floating matrix tablet and raft system would be promising gastroretentive delivery systems for prolonging drug action. SN - 1177-8881 UR - https://www.unboundmedicine.com/medline/citation/28435220/Formulation_release_characteristics_and_bioavailability_study_of_gastroretentive_floating_matrix_tablet_and_floating_raft_system_of_Mebeverine_HCl_ L2 - https://dx.doi.org/10.2147/DDDT.S131936 DB - PRIME DP - Unbound Medicine ER -