title: A Novel Approach to Flurbiprofen Pulsatile Colonic Release: Formulation and Pharmacokinetics of Double-Compression-Coated Mini-Tablets.
abstract: A significant plan is executed in the present study to study the effect of double-compression coating on flurbiprofen core mini-tablets to achieve the pulsatile colonic delivery to deliver the drug at a specific time as per the patho-physiological need of the disease that results in improved therapeutic efficacy. In this study, pulsatile double-compression-coated tablets were prepared based on time-controlled hydroxypropyl methylcellulose K100M inner compression coat and pH-sensitive Eudragit S100 outer compression coat. Then, the tablets were evaluated for both physical evaluation and drug-release studies, and to prove these results, in vivo pharmacokinetic studies in human volunteers were conducted. From the in vitro drug-release studies, F6 tablets were considered as the best formulation, which retarded the drug release in the stomach and small intestine (3.42 ± 0.12% in 5 h) and progressively released to the colon (99.78 ± 0.74% in 24 h). The release process followed zero-order release kinetics, and from the stability studies, similarity factor between dissolution data before and after storage was found to be 88.86. From the pharmacokinetic evaluation, core mini-tablets producing peak plasma concentration (C max) was 14,677.51 ± 12.16 ng/ml at 3 h T max and pulsatile colonic tablets showed C max = 12,374.67 ± 16.72 ng/ml at 12 h T max. The area under the curve for the mini and pulsatile tablets was 41,238.52 and 72,369.24 ng-h/ml, and the mean resident time was 3.43 and 10.61 h, respectively. In conclusion, development of double-compression-coated tablets is a promising way to achieve the pulsatile colonic release of flurbiprofen.
authors.affiliation: Department of Pharmacy, College of Medical and Health Sciences, Wollega University, Post Box No: 395, Nekemte, Ethiopia. vemulasatish15@gmail.com.|Department of Pharmaceutics, Chaitanya College of Pharmaceutical Sciences, Hanamkonda, Warangal, Telangana, 506001, India. vemulasatish15@gmail.com.|Department of Pharmaceutics, Jangaon Institute of Pharmaceutical Sciences, Yeshwanthapur, Jangaon, Warangal, Telangana, 506167, India. vemulasatish15@gmail.com.
authors.forename: Sateesh Kumar
authors.initials: SK
authors.lastname: Vemula
mesh_terms: D000328:Adult; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003106:Colon / Q000378:metabolism*; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems / Q000379:methods; D065546:Drug Liberation; D005079:Excipients / Q000737:chemistry; D005480:Flurbiprofen / Q000737:chemistry* / Q000493:pharmacokinetics*; D005753:Gastric Mucosa / Q000378:metabolism; D006801:Humans; D065347:Hypromellose Derivatives / Q000737:chemistry; D007421:Intestine, Small / Q000378:metabolism; D011108:Polymers / Q000737:chemistry; D013608:Tablets, Enteric-Coated / Q000737:chemistry* / Q000493:pharmacokinetics*
chemical_list: D003692:Delayed-Action Preparations; D005079:Excipients; D011108:Polymers; D013608:Tablets, Enteric-Coated; D065347:Hypromellose Derivatives; D005480:Flurbiprofen
keywords: core mini-tablets; double-compression coating; inner compression coat; outer compression coat; similarity factor