Novel sustained release, swellable and bioadhesive gastroretentive drug delivery system for ofloxacin.
Oral sustained release gastroretentive dosage forms offer many advantages for drugs having absorption from upper gastrointestinal tract and improve the bioavailability of medications that are characterized by a narrow absorption window. A new gastroretentive sustained release delivery system was developed with floating, swellable and bioadhesive properties. All these properties were optimized and evaluated. Various release retarding polymers like psyllium husk, HPMC K100M and a swelling agent, crosspovidone in combinations were tried and optimized to get the release profile for 24 h. Formulations were evaluated for in vitro drug release profile, swelling characteristics and in vitro bioadhesion property. The in vitro drug release followed Higuchi kinetics and the drug release mechanism was found to be of anomalous or non-Fickian type. For the developed formulation, the value of n was found to be 0.5766 while for the marketed formulation the value was 0.5718 indicating the anomalous transport. The high water uptake leading to higher swelling of the tablet supported the anomalous release mechanism of ofloxacin. The similarity factor f2 was found to be 91.12 for the developed formulation indicating the release was similar to that of the marketed formulation (Zanocin OD). The swelling properties were increased with increasing crosspovidone concentration and contributed significantly in drug release from the tablet matrix. The bioadhesive property of the developed formulation was found to be significant (P < 0.005) in combination as compared to HPMC K100M and psyllium husk alone.
Chavanpatil
Mahesh D
MD
Mumbai University Institute of Chemical Technology, Pharmaceutical Sciences Division, Near Nathalal Parikh Marg, Matunga, Mumbai 400019, India. mcp_112000@rediffmail.com
Jain
Paras
P
Chaudhari
Sachin
S
Shear
Rajesh
R
Vavia
Pradeep R
PR
D000284:Administration, Oral; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000737:chemistry*; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D066298:In Vitro Techniques; D015242:Ofloxacin / Q000008:administration & dosage* / Q000737:chemistry*; D011817:Rabbits; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D013270:Stomach / Q000502:physiology*; D013607:Tablets; D014014:Tissue Adhesives / Q000737:chemistry*; D014867:Water / Q000737:chemistry
D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D012997:Solvents; D013607:Tablets; D014014:Tissue Adhesives; D014867:Water; D015242:Ofloxacin