Preparation and evaluation of novel metronidazole sustained release and floating matrix tablets.
In the present study, metronidazole was used for preparing floating dosage forms that are designed to retain in the stomach for a long time and have developed as a drug delivery system for better eradication of Helicobacter Pylori in peptic ulcer diseases. For this means, various formulations were designed using multi-factorial design. HPMC, psyllium and carbopol in different concentrations were used as floating agents, and sodium bicarbonate was added as a gas-forming agent. Hardness, friability, drug loading, floating ability and release profiles as well as kinetics of release were assessed. Formulations containing HPMC as filler showed prolonged lag times for buoyancy. Adding psyllium to these formulations had reduced relative lag times. Overall, selected formulations were able to float immediately and showed buoyancy for at least 8?h. Meanwhile, sustained profiles of drug release were also obtained. Kinetically, among the 10 assessed models, the release pattern of metronidazole from the tablets fitted best to Power law, Weibull and Higuchi models in respect overall to mean percentage error values of 3.8, 4.73 and 5.77, respectively, for calcium carbonate-based tablets and, 2.95, 6.39 and 3.9, respectively, for calcium silicate-based tablets. In general, these systems can float in the gastric condition and control the drug release from the tablets.
Asnaashari
Solmaz
S
Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz 51664, Iran.
Khoei
Nazaninossadat Seyed
NS
Zarrintan
Mohammad Hosein
MH
Adibkia
Khosro
K
Javadzadeh
Yousef
Y
D000465:Algorithms; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003692:Delayed-Action Preparations / Q000008:administration & dosage*; D005079:Excipients / Q000737:chemistry; D006244:Hardness; D016480:Helicobacter pylori; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D008795:Metronidazole / Q000008:administration & dosage* / Q000493:pharmacokinetics; D011620:Psyllium; D017693:Sodium Bicarbonate; D012995:Solubility; D013270:Stomach; D013607:Tablets
D000890:Anti-Infective Agents; D003692:Delayed-Action Preparations; D005079:Excipients; D013607:Tablets; D008795:Metronidazole; D065347:Hypromellose Derivatives; D011620:Psyllium; D017693:Sodium Bicarbonate; D008747:Methylcellulose