title: Design and Development of Clopidogrel Bisulfate Gastroretentive Osmotic Formulation Using Quality by Design Tools.
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.
authors.affiliation: Department of Quality Assurance Techniques, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Pune, 411038, India.
authors.forename: Nilesh
authors.initials: N
authors.lastname: Desai
authors.affiliation: Department of Quality Assurance Techniques, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Pune, 411038, India. ravindrapurohit@outlook.com.
authors.forename: Ravindra
authors.initials: R
authors.lastname: Purohit
mesh_terms: D001682:Biological Availability; D000077144:Clopidogrel; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D065546:Drug Liberation; D005753:Gastric Mucosa / Q000378:metabolism*; D009995:Osmosis; D012995:Solubility; D013607:Tablets / Q000378:metabolism; D013988:Ticlopidine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism
chemical_list: D003692:Delayed-Action Preparations; D013607:Tablets; D000077144:Clopidogrel; D013988:Ticlopidine
keywords: clopidogrel bisulfate; design of experiment; gastroretentive osmotic tablet; quality by design