title: Design and evaluation of polymeric coated minitablets as multiple unit gastroretentive floating drug delivery systems for furosemide.
abstract: A gastro retentive floating drug delivery system with multiple-unit minitablets based on gas formation technique was developed for furosemide. The system consists of core units (solid dispersion of furosemide:povidone and other excipients), prepared by direct compression process, which are coated with two successive layers, one of which is an effervescent (sodium bicarbonate) layer and other one an outer polymeric layer of polymethacrylates. The formulations were evaluated for pharmacopoeial quality control tests and all the physical parameters evaluated were within the acceptable limits. Only the system using Eudragit RL30D and combination of them as polymeric layer could float within acceptable time. The time to float decreased as amount of the effervescent agent increased and, when the coating level of polymeric layer decreased. The drug release was controlled and linear with the square root of time. By increasing coating level of polymeric layer decreased the drug release. The rapid floating and the controlled release properties were achieved in this present study. The stability samples showed no significant change in dissolution profiles (f(2) = 81). The in vivo gastric residence time was examined by radiograms and it was observed that the units remained in the stomach for about 6 h.
authors.affiliation: Centre for Biopharmaceutics and Pharmacokinetics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal 506 009, Andhra Pradesh, India. mekalingam@gmail.com
authors.forename: Lingam
authors.initials: L
authors.lastname: Meka
authors.forename: Bhaskar
authors.initials: B
authors.lastname: Kesavan
authors.forename: Venkatasimhadri Naidu
authors.initials: VN
authors.lastname: Kalamata
authors.forename: Chandra Mohan
authors.initials: CM
authors.lastname: Eaga
authors.forename: Suresh
authors.initials: S
authors.lastname: Bandari
authors.forename: Venkateswarlu
authors.initials: V
authors.lastname: Vobalaboina
authors.forename: Madhusudan Rao
authors.initials: MR
authors.lastname: Yamsani
mesh_terms: D000328:Adult; D004232:Diuretics / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D004339:Drug Compounding; D016503:Drug Delivery Systems / Q000379:methods*; D005665:Furosemide / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D005753:Gastric Mucosa / Q000378:metabolism; D006801:Humans; D008297:Male; D011109:Polymethacrylic Acids / Q000737:chemistry; D011859:Radiography; D017693:Sodium Bicarbonate / Q000737:chemistry; D012995:Solubility; D013270:Stomach / Q000000981:diagnostic imaging; D013608:Tablets, Enteric-Coated / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D013997:Time Factors; D014961:X-Ray Diffraction
chemical_list: D004232:Diuretics; D011109:Polymethacrylic Acids; D013608:Tablets, Enteric-Coated; C030613:polymethacrylic acid; D005665:Furosemide; D017693:Sodium Bicarbonate