title: Innovative intragastric ascaridole floating tablets: Development, optimization, and in vitro-in vivo evaluation.
abstract: Gastro-floating tablets of ascaridole, a volatile oil were developed to prolong the gastric residence time and thereby, enhance local therapeutic efficacy. The tablets were optimized and prepared by direct compression techniques using hydroxypropylmethylcellulose (HPMC K15M) and polyethylene oxide (PEO WSRN-750) as hydrophilic matrices and calcium carbonate (CaCO3) as a gas-generating agent. In vitro evaluation of the prepared tablets was performed by determining the hardness, friability, content uniformity, and weight variation. In addition, floating lag time, total floating time, and drug release behavior were evaluated. Finally, optimized tablets were subjected to stability and in vivo gamma scintigraphy studies. Results showed that the formulated tablets were white, smooth, and flat in appearance and met the Chinese Pharmacopoeia (ChP) criteria for weight variation, drug content, and friability. The tablets had satisfactory buoyancy and sustained drug release profile that followed non-Fickian kinetics. In vivo gamma scintigraphy suggests that the floating tablet did not adhere to the stomach mucous but were retained in the stomach for extended periods of 5.80±0.50h following administration, indicating that gastro retentive time of ascaridole tablets increased owing to the floating principle.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China; Department of Pharmacy, Fujian University of Traditional Chinese Medicine, Fujian 350108, PR China.
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhao
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China.
authors.forename: Baoan
authors.initials: B
authors.lastname: Gao
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China.
authors.forename: Lulu
authors.initials: L
authors.lastname: Ma
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China; Department of Pharmacy, Fujian University of Traditional Chinese Medicine, Fujian 350108, PR China.
authors.forename: Jianhao
authors.initials: J
authors.lastname: Lian
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China. Electronic address: lilideng2004@126.com.
authors.forename: Li
authors.initials: L
authors.lastname: Deng
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China; Tasly Diyi Pharmaceutical Group Co., Ltd., Jiangsu 223002, PR China. Electronic address: yjcjm@163.com.
authors.forename: Jianming
authors.initials: J
authors.lastname: Chen
mesh_terms: D000328:Adult; D002119:Calcium Carbonate / Q000737:chemistry; D002266:Carboxymethylcellulose Sodium / Q000737:chemistry; D000081005:Cyclohexane Monoterpenes; D055808:Drug Discovery; D004355:Drug Stability; D006801:Humans; D008297:Male; D039821:Monoterpenes / Q000008:administration & dosage* / Q000737:chemistry; D010545:Peroxides / Q000008:administration & dosage* / Q000737:chemistry; D012995:Solubility; D013270:Stomach; D013607:Tablets
chemical_list: D000081005:Cyclohexane Monoterpenes; D039821:Monoterpenes; D010545:Peroxides; D013607:Tablets; C043372:ascaridole; D002119:Calcium Carbonate; D002266:Carboxymethylcellulose Sodium
keywords: Ascaridole; Drug release; Evaluation; Gamma scintigraphy; Intragastric floating tablet