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Controlled release matrix tablets of olanzapine: influence of polymers on the in vitro release and bioavailability.
AAPS PharmSciTech. 2010 Sep; 11(3):1397-404.AP

Abstract

Controlled-release (CR) tablet formulation of olanzapine was developed using a binary mixture of Methocel® K100 LV-CR and Ethocel® standard 7FP premium by the dry granulation slugging method. Drug release kinetics of CR tablet formulations F1, F2, and F3, each one suitably compressed for 9-, 12-, and 15-kg hardness, were determined in a dissolution media of 0.1 N HCl (pH 1.5) and phosphate buffer (pH 6.8) using type II dissolution apparatus with paddles run at 50 rpm. Ethocel® was found to be distinctly controlling drug release, whereas the hardness of tablets and pH of the dissolution media did not significantly affect release kinetics. The CR test tablets containing 30% Methocel® and 60% Ethocel® (F3) with 12-kg hardness exhibited pH-independent zero-order release kinetics for 24 h. In vivo performance of the CR test tablet and conventional reference tablet were determined in rabbit serum using high-performance liquid chromatography coupled with electrochemical detector. Bioavailability parameters including C(max), T(max), and AUC(0-48 h) of both tablets were compared. The CR test tablets produced optimized C(max) and extended T(max) (P < 0.05). A good correlation of drug absorption in vivo and drug release in vitro (R(2) = 0.9082) was observed. Relative bioavailability of the test tablet was calculated as 94%. The manufacturing process employed was reproducible and the CR test tablets were stable for 6 months at 40 ± 2°C/75 ± 5% relative humidity. It was concluded that the CR test tablet formulation successfully developed may improve tolerability and patient adherence by reducing adverse effects.

Authors+Show Affiliations

Department of Pharmacy, University of Peshawar, Peshawar, 25120 N.W.F.P, Pakistan. amir_badshah@upesh.edu.pkNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

20824513

Citation

Badshah, Amir, et al. "Controlled Release Matrix Tablets of Olanzapine: Influence of Polymers On the in Vitro Release and Bioavailability." AAPS PharmSciTech, vol. 11, no. 3, 2010, pp. 1397-404.
Badshah A, Subhan F, Rauf K. Controlled release matrix tablets of olanzapine: influence of polymers on the in vitro release and bioavailability. AAPS PharmSciTech. 2010;11(3):1397-404.
Badshah, A., Subhan, F., & Rauf, K. (2010). Controlled release matrix tablets of olanzapine: influence of polymers on the in vitro release and bioavailability. AAPS PharmSciTech, 11(3), 1397-404. https://doi.org/10.1208/s12249-010-9510-0
Badshah A, Subhan F, Rauf K. Controlled Release Matrix Tablets of Olanzapine: Influence of Polymers On the in Vitro Release and Bioavailability. AAPS PharmSciTech. 2010;11(3):1397-404. PubMed PMID: 20824513.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Controlled release matrix tablets of olanzapine: influence of polymers on the in vitro release and bioavailability. AU - Badshah,Amir, AU - Subhan,Fazal, AU - Rauf,Khalid, Y1 - 2010/09/08/ PY - 2010/02/09/received PY - 2010/08/12/accepted PY - 2010/9/9/entrez PY - 2010/9/9/pubmed PY - 2011/3/8/medline SP - 1397 EP - 404 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 11 IS - 3 N2 - Controlled-release (CR) tablet formulation of olanzapine was developed using a binary mixture of Methocel® K100 LV-CR and Ethocel® standard 7FP premium by the dry granulation slugging method. Drug release kinetics of CR tablet formulations F1, F2, and F3, each one suitably compressed for 9-, 12-, and 15-kg hardness, were determined in a dissolution media of 0.1 N HCl (pH 1.5) and phosphate buffer (pH 6.8) using type II dissolution apparatus with paddles run at 50 rpm. Ethocel® was found to be distinctly controlling drug release, whereas the hardness of tablets and pH of the dissolution media did not significantly affect release kinetics. The CR test tablets containing 30% Methocel® and 60% Ethocel® (F3) with 12-kg hardness exhibited pH-independent zero-order release kinetics for 24 h. In vivo performance of the CR test tablet and conventional reference tablet were determined in rabbit serum using high-performance liquid chromatography coupled with electrochemical detector. Bioavailability parameters including C(max), T(max), and AUC(0-48 h) of both tablets were compared. The CR test tablets produced optimized C(max) and extended T(max) (P < 0.05). A good correlation of drug absorption in vivo and drug release in vitro (R(2) = 0.9082) was observed. Relative bioavailability of the test tablet was calculated as 94%. The manufacturing process employed was reproducible and the CR test tablets were stable for 6 months at 40 ± 2°C/75 ± 5% relative humidity. It was concluded that the CR test tablet formulation successfully developed may improve tolerability and patient adherence by reducing adverse effects. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/20824513/Controlled_release_matrix_tablets_of_olanzapine:_influence_of_polymers_on_the_in_vitro_release_and_bioavailability_ L2 - https://dx.doi.org/10.1208/s12249-010-9510-0 DB - PRIME DP - Unbound Medicine ER -