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Design and Development of Clopidogrel Bisulfate Gastroretentive Osmotic Formulation Using Quality by Design Tools

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Abstract

Clopidogrel bisulfate (CBS) is antiplatelet drug and it is becoming a drug of choice in the treatment and management of prevention of heart attacks and strokes. CBS is stable and soluble in acidic pH; therefore, retention in stomach for prolonged period appears to be beneficial for controlling the bioavailability. The gastroretentive osmotic system (GROS) facilitates prolonged retention of drug in stomach and provides zero-order drug release. A complex formulation like GROS poses many challenges, and QbD tools can help in designing robust formulation which takes all aspects of product and process development in order to deliver a robust product. The GROS was formulated in three steps: core tablet, osmotic tablet, and gastroretentive osmotic tablet. The design of experiment was used for screening and optimization of formulation and process-related parameters. The dissolution study was carried out to analyze the release pattern of tablet. The optimized batch O-4 showed cumulative drug release of 19.43, 30.49, 64.41, and 85.11% at 2, 4, 8, and 12 h which is in the range of QTPP predictions. The novel technique of GROS was implemented successfully which demonstrates robust design giving consistent and desired results.

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Acknowledgments

Nilesh S. Desai thanks University Grants Commission, India, for the financial assistance to the work in the form of UGC-BSR Project file no. 7-23/2007(BSR).

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  1. Department of Quality Assurance Techniques, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Pune, 411038, India

    Nilesh Desai & Ravindra Purohit

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  1. Nilesh Desai
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  2. Ravindra Purohit
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Correspondence to Ravindra Purohit.

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Desai, N., Purohit, R. Design and Development of Clopidogrel Bisulfate Gastroretentive Osmotic Formulation Using Quality by Design Tools. AAPS PharmSciTech 18, 2626–2638 (2017). https://doi.org/10.1208/s12249-017-0731-3

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  • DOI: https://doi.org/10.1208/s12249-017-0731-3

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