Development of hollow/porous calcium pectinate beads for floating-pulsatile drug delivery.
The purpose of this work was to develop hollow calcium pectinate beads for floating-pulsatile release of diclofenac sodium intended for chronopharmacotherapy. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. To overcome limitations of various approaches for imparting buoyancy, hollow/porous beads were prepared by simple process of acid-base reaction during ionotropic crosslinking. The floating beads obtained were porous (34% porosity), hollow with bulk density<1 and had Ft50% of 14-24 h. In vivo studies by gamma scintigraphy determined on rabbits showed gastroretention of beads up to 5 h. The floating beads provided expected two-phase release pattern with initial lag time during floating in acidic medium followed by rapid pulse release in phosphate buffer. This approach suggested the use of hollow calcium pectinate microparticles as promising floating-pulsatile drug delivery system for site- and time-specific release of drugs acting as per chronotherapy of diseases.
Badve
Shraddha S
SS
Department of Pharmaceutics, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Pune, India.
Sher
Praveen
P
Korde
Aruna
A
Pawar
Atmaram P
AP
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000493:pharmacokinetics; D002118:Calcium / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D019454:Chronotherapy / Q000379:methods; D019245:Compressive Strength; D003692:Delayed-Action Preparations; D004008:Diclofenac / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers; D041981:Gastrointestinal Tract / Q000000981:diagnostic imaging; D005772:Gastrointestinal Transit; D008297:Male; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D010316:Particle Size; D010368:Pectins / Q000737:chemistry*; D016062:Porosity; D011817:Rabbits; D011877:Radionuclide Imaging; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods; D013997:Time Factors
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004008:Diclofenac; D010368:Pectins; D002118:Calcium