Search

In the present study esomeprazole sustained release tablet matrix was prepared by utilizing different grades of hydroxypropyl methylcellulose (HPMC) polymers such as Methocel K15M & Methocel K100 LVCR by direct compression method. Different amount of Methocel K15M was used to develop matrix builder in the seven proposed formulations (F1-F7) for the study of release rate retardant effect at 20%, 25%, 30%, 35%, 40%, 45% and 50% of total weight of tablet matrix respectively. The dissolution study of Methocel K15M based tablet matrices of those proposed formulations were carried out in the simulated gastric medium (pH 1.3) for first two hours and then in the simulated intestinal medium (pH 6.8) for 8 hours using USP dissolution apparatus II. The formulation F-5 (40%) and F-6 (45%) met the optimum release rate of esomeprazole for 10h period of in vitro dissolution study. The release kinetics of formulation F-5 and F-6 very closely followed Higuchi kinetic order than first order and zero order kinetics. Similarly Methocel K100 LVCR was used to develop matrix builder in another seven proposed formulations (F8-F14). It was found that formulations F-11 (35%), F-12 (40%) and F-13 (45%) met the desired release rate of esomeprazole for 10h period. The release kinetics of formulation F-11, F-12 and F-13 followed Higuchi kinetic order. Between these two polymers, Methocel K100 LVCR showed better release retardant effect than Methocel K15M. Key words: Esomeprazole, Direct compression, Controlled release, Methocel K15M and Methocel K100 LVCRDOI = 10.3329/dujps.v7i1.1216 Dhaka Univ. J. Pharm. Sci. 7(1): 39-45, 2008 (June) Â

Commercially available four national and four international brands of esomeprazole magnesium sustained release matrix tablets were studied in simulated gastric medium (pH 1.2) for 2 hours and simulated intestinal medium (pH 6.8) for 8 hours time period using USP reference dissolution apparatus. All the national and international brands complied with the USP in-vitro dissolution specifications for drug release in simulated gastric medium. However, one of the national brands (Code: MP-1) and one of the international brands (MP-7) failed to fulfill the official requirement of 80% drug release within 8th hour in simulated intestinal medium. Drug release of that national and international brand were 70.49% and 67.05% respectively within the specified time period, however one national brand (Code: MP-4) released 103.46 % drug within 8th hour in intestinal medium. Drug release profiles were analyzed for zero order, first order and Higuchi equation to reveal the release kinetics perspective of esomeprazole magnesium sustained release matrix tablets. It was found that zero order release kinetics was the predominant release mechanism than first order and Higuchi release kinetics for those brands (Code: MP-2, MP-3, MP-4, MP-5, MP-6 and MP-8) which complied with the USP in vitro dissolution specification for drug releases. On the other hand, first order release kinetics was predominant for one national and also one international non compliant brands (Code: MP-1 and MP-6). Key Words: In vitro dissolution; Sustained release; Market preparations; Kinetic analysis; Esomeprazole; National brand; International brand. DOI: 10.3329/sjps.v2i1.5812Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 27-31

The main aim of present investigation was to study the dissolution pattern of most commercially available formulations of Esomeprazole in Bangladesh. Commercially available ten national brands and originator brand of esomeprazole magnesium trihydrate tablets were studied in simulated gastric medium (pH 1.2) for first 15 minutes and simulated intestinal medium (pH 6.8) for next 30 minutes time period using USP reference dissolu-tion apparatus (Type II). No brands met the dissolution pattern like the originator brand (E1). But three brands (E3, E6 and E7) were found to be very close to it in terms of dissolution pattern. One brand E11 was found to be sub-standard compared to originator one. Drug release profiles were analyzed for zero order, first order and Higuchi equation to reveal the release kinetics perspective of Esomeprazole magnesium trihydrate enteric coated tablets. It was found that first order kinetics was predominant for E1 (Originator Brand). Zero order and Higuchi release kinetics was predominant release mechanism than first order release kinetics for E2, E4 and E11. First order release kinetics was predominant for rest of the brands (E3, E5, E6, E7, E8, E9 and E10). It was found that drug release of those brands followed moderately diffusion method and concentration dependant from the dosage form. Among all of these locally manufactured Esomeprazole brands E3, E6 and E7 showed compatible dissolution pattern and release kinetics compared with the originator brand. Key words: In vitro dissolution; Market preparations; Kinetics study; Esomeprazole; National brand; Originator brand. DOI: http://dx.doi.org/10.3329/sjps.v4i1.8875 SJPS 2011; 4(1): 79-83

A bioequivalence study for the selection of the alternative and feasible mode of administration of esomeprazole pellets suspended in some common soft liquid foods has been done. 20 mg of four different brands esomeprazole pellets suspended in yogurt, orange juice, apple juice and milk were analyzed in the gastric environment using dissolution tester and high performance liquid chromatography. The release of the esomeprazole active was found more the 90% using these liquid foods except milk. The optimal release of the active was found in the system of apple juice (97.06%). Administration of the esomeprazole pellets suspending in apple juice may be a practical alternative for patients who cannot swallow an intact capsule. Keywords: Bioequivalence, Esomeprazole pellets, Soft foods, Gastric environment, Dissolution. DOI: 10.3329/diujst.v4i2.4368 Daffodil International University Journal of Science and Technology Vol.4(2) 2009 pp.59-61