title: Preparation of a matrix type multiple-unit gastro retentive floating drug delivery system for captopril based on gas formation technique: in vitro evaluation.
abstract: A gastro retentive floating drug delivery system with multiple-unit minitab's based on gas formation technique was developed in order to prolong the gastric residence time and to increase the overall bioavailability of the drug. The system consists of the drug-containing core units prepared by direct compression process, which are coated with three successive layers of an inner seal coat, effervescent layer (sodium bicarbonate) and an outer gas-entrapped polymeric membrane of an polymethacrylates (Eudragit RL30D, RS30D, and combinations of them). Only the system using Eudragit RL30D and combination of them as a gas-entrapped polymeric membrane could float. The time to float decreased as amount of the effervescent agent increased and coating level of gas-entrapped polymeric membrane decreased. The optimum system floated completely within 3 min and maintained the buoyancy over a period of 12 h. The drug release was controlled and linear with the square root of time. Increasing coating level of gas-entrapped polymeric membrane decreased the drug release. Both the rapid floating and the controlled release properties were achieved in the multiple-unit floating drug delivery system developed in this present study. The analysis of the parameter dissolution data after storage at 40 degrees C and 75% RH for 3 months showed, no significant change indicating the two dissolution profiles were considered to be similar (f2 value is more than 50).
authors.affiliation: Novel Drug Delivery Systems Laboratory, University College of Pharmaceutical Sciences, Kakatiya University, Warangal 506009, 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: Krishna Mohan
authors.initials: KM
authors.lastname: Chinnala
authors.forename: Venkateswarlu
authors.initials: V
authors.lastname: Vobalaboina
authors.forename: Madhusudan Rao
authors.initials: MR
authors.lastname: Yamsani
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry; D000284:Administration, Oral; D000806:Angiotensin-Converting Enzyme Inhibitors / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D002214:Capsules; D002216:Captopril / Q000008:administration & dosage / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004339:Drug Compounding; D004355:Drug Stability; D005740:Gases; D005746:Gastric Emptying; D005753:Gastric Mucosa / Q000378:metabolism; D006801:Humans; D006813:Humidity; D007700:Kinetics; D008567:Membranes, Artificial; D011108:Polymers / Q000737:chemistry; D011109:Polymethacrylic Acids / Q000737:chemistry*; D017693:Sodium Bicarbonate / Q000737:chemistry*; D012995:Solubility; D013607:Tablets; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature
chemical_list: D000180:Acrylic Resins; D000806:Angiotensin-Converting Enzyme Inhibitors; D002214:Capsules; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005740:Gases; D008567:Membranes, Artificial; D011108:Polymers; D011109:Polymethacrylic Acids; D013607:Tablets; C050528:Eudragit RS; C058665:Eudragit RL; D017693:Sodium Bicarbonate; D002216:Captopril