Controlled-release effervescent floating matrix tablets of ciprofloxacin hydrochloride: Development, optimization and in vitro–in vivo evaluation in healthy human volunteers

• Published in: European journal of pharmaceutics and biopharmaceutics Vol. 74; no. 2; pp. 332 - 339
• Main Author: Tadros, Mina Ibrahim
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 01.02.2010; Elsevier
• Subjects: Abdominal X-ray imaging; Adult; Alginates - chemistry; Alginates - pharmacokinetics; Barium Sulfate - pharmacokinetics; Biological and medical sciences; Calcium Carbonate - chemistry; Chemical Phenomena; Ciprofloxacin - pharmacokinetics; Ciprofloxacin hydrochloride; Contrast Media - pharmacokinetics; Delayed-Action Preparations - administration & dosage; Delayed-Action Preparations - chemical synthesis; Delayed-Action Preparations - chemistry; Delayed-Action Preparations - pharmacokinetics; Drug Compounding - methods; Drug Stability; Floating gastroretentive tablets; Gas former; General pharmacology; Glucuronic Acid - chemistry; Glucuronic Acid - pharmacokinetics; Hexuronic Acids - chemistry; Hexuronic Acids - pharmacokinetics; Humans; Hypromellose Derivatives; Male; Medical sciences; Methylcellulose - analogs & derivatives; Methylcellulose - chemistry; Methylcellulose - pharmacokinetics; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Radiography, Abdominal; Release-retarding polymers; Sodium Bicarbonate - chemistry; Stomach - diagnostic imaging; Stomach - metabolism; Tablets - administration & dosage; Tablets - chemical synthesis; Tablets - chemistry; Tablets - pharmacokinetics; Time Factors; Abdominal X-ray imaging; Gas former; Ciprofloxacin hydrochloride; Release-retarding polymers; Floating gastroretentive tablets; Human; Evaluation; Pharmaceutical technology; Healthy subject; Controlled release form; Polymer; X ray; Effervescent form; In vitro; Matrix tablet; Optimization; In vivo; Fluoroquinolone derivatives; Dosage form; Medical imagery; Antibacterial agent; Ciprofloxacin; Quinolone derivatives; Release
• ISSN: 0939-6411; 1873-3441; 1873-3441
• DOI: 10.1016/j.ejpb.2009.11.010

Ciprofloxacin hydrochloride has a short elimination half-life, a narrow absorption window and is mainly absorbed in proximal areas of GIT. The purpose of this study was to develop a gastroretentive controlled-release drug delivery system with swelling, floating, and adhesive properties. Ten tablet formulations were designed using hydroxypropylmethylcellulose (HPMC K15M) and/or sodium alginate (Na alginate) as release-retarding polymer(s) and sodium bicarbonate (NaHCO 3) or calcium carbonate (CaCO 3) as a gas former. Swelling ability, floating behaviour, adhesion period and drug release studies were conducted in 0.1 N HCl (pH 1.2) at 37 ± 0.5 °C. The tablets showed acceptable physicochemical properties. Drug release profiles of all formulae followed non-Fickian diffusion. Statistical analyses of data revealed that tablets containing HPMC K15M (21.42%, w/w), Na alginate (7.14%, w/w) and NaHCO 3 (20%, w/w) (formula F7) or CaCO 3 (20%, w/w) (formula F10) were promising systems exhibiting excellent floating properties, extended adhesion periods and sustained drug release characteristics. Both formulae were stored at 40 °C/75% RH for 3 months according to ICH guidelines. Formula F10 showed better physical stability. Abdominal X-ray imaging of formula F10, loaded with barium sulfate, in six healthy volunteers revealed a mean gastric retention period of 5.50 ± 0.77 h.