Controlled Release Matrix Tablets of Olanzapine: Influence of Polymers on the In Vitro Release and Bioavailability.
Summary of "Controlled Release Matrix Tablets of Olanzapine: Influence of Polymers on the In Vitro Release and Bioavailability."
Controlled-release (CR) tablet formulation of olanzapine was developed using a binary mixture of Methocel(R) K100 LV-CR and Ethocel(R) 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(R) 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(R) and 60% Ethocel(R) (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 degrees 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.
Affiliation
Department of Pharmacy, University of Peshawar, Peshawar, 25120 N.W.F.P, Pakistan, amir_badshah@upesh.edu.pk.
Journal Details
This article was published in the following journal.
Name: AAPS PharmSciTech
ISSN: 1530-9932
Pages:
Links
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/20824513
- DOI: http://dx.doi.org/10.1208/s12249-010-9510-0
Medical and Biotech [MESH] Definitions
Tablets, Enteric-coated
Tablets coated with material that delays release of the medication until after they leave the stomach. (Dorland, 28th ed)
Matrix Metalloproteinases, Membrane-associated
Matrix metalloproteinases that are associated with the CELL MEMBRANE, either through transmembrane domains or GLYCOSYLPHOSPHATIDYLINOSITOL ANCHORS. Membrane-type matrix metalloproteinases may act within the pericellular environment to influence the process of CELL MIGRATION.
Excipients
Usually inert substances added to a prescription in order to provide suitable consistency to the dosage form. These include binders, matrix, base or diluent in pills, tablets, creams, salves, etc.
Drug Carriers
Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers.
Delayed-action Preparations
Dosage forms of a drug that act over a period of time by controlled-release processes or technology.
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