Design and in vitro characterization of buccoadhesive tablets of timolol maleate

Design and in vitro characterization of buccoadhesive tablets of timolol maleate

Abstract Objective: The purpose of this work was to develop and evaluate buccoadhesive tablets of timolol maleate (TM) due to its potential to circumvent the first-pass metabolism and to improve its bioavailability. Methods: The tablets were prepared by direct compression using two release modifying...

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Bibliographic Details
Published in:Drug development and industrial pharmacy Vol. 40; no. 5; pp. 680 - 690
Main Authors: Gaikwad, Sachin S., Thombre, Shital K., Kale, Yogesh K., Gondkar, Sheetal B., Darekar, Avinash B.
Format: Journal Article
Language:English
Published: England Informa Healthcare USA, Inc 01-05-2014
Taylor & Francis
Subjects:
Acrylates - chemistry
Adhesiveness
Administration, Buccal
Alginates - chemistry
Biological Availability
Buccal
Calorimetry, Differential Scanning
Chemistry, Pharmaceutical
compatibility
Drug Delivery Systems
drug release
Drug Stability
DSC
entrapments
Excipients - chemistry
FTIR
Glucuronic Acid - chemistry
Hexuronic Acids - chemistry
Humans
P-XRD
Powder Diffraction
Spectroscopy, Fourier Transform Infrared
swelling index
Tablets
Timolol - administration & dosage
Timolol - pharmacokinetics
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Summary:Abstract Objective: The purpose of this work was to develop and evaluate buccoadhesive tablets of timolol maleate (TM) due to its potential to circumvent the first-pass metabolism and to improve its bioavailability. Methods: The tablets were prepared by direct compression using two release modifying polymers, Carbopol 974P (Cp-974p) and sodium alginate (SA). A 32 full factorial design was employed to study the effect of independent variables, Cp-974p and SA, in various proportions in percent w/w, which influences the in vitro drug release and bioadhesive strengths. Physicochemical properties of the drug were evaluated by ultraviolet, Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder X-ray diffraction (P-XRD). Tablets were evaluated for hardness, thickness, weight variation, drug content, surface pH, swelling index, bioadhesive force and in vitro drug release. Results: The FTIR and DSC studies showed no evidence of interactions between drug, polymers and excipients. The P-XRD study revealed that crystallinity of TM remain unchanged in optimized formulation tablet. Formulation F9 achieves an in vitro drug release of 98.967% ± 0.28 at 8 h and a bioadhesive force of 0.088 N ± 0.01211. Conclusion: We successfully developed buccal tablet formulations of TM and describe a non-Fickian-type anomalous transport as the release mechanism.
Bibliography:ObjectType-Article-1
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ISSN:0363-9045
1520-5762
DOI:10.3109/03639045.2014.892955