In vitro and in vivo evaluation of ranitidine hydrochloride loaded hollow microspheres in rabbits.
The objective of this investigation was to develop the hollow microspheres as a new dosage form of floating drug delivery systems with prolonged stomach retention time. Hollow microspheres containing ranitidine hydrochloride (RH) were prepared by a novel solvent diffusion-evaporation method using ethyl cellulose (EC) dissolved in a mixture of ethanol and ether (6:1.0, v/v). The yield and drug loading amount of hollow microspheres were 83.21+/-0.28% and 20.71+/-0.32%, respectively. The in vitro release profiles showed that the drug release rate decreased with increasing viscosity of EC and the diameter of hollow microspheres, while increased with the increase of RH/EC weight ratio. Hollow microspheres could prolong drug release time (approximately 24 h) and float over the simulate gastric fluid for more than 24 h. Pharmacokinetic analysis showed that the bioavailability from RH-hollow microspheres alone was about 3.0-times that of common RH gelatin capsules, and it was about 2.8-times that of the solid microspheres. These results demonstrated that RH hollow microspheres were capable of sustained delivery of the drug for longer period with increased bioavailability.
Wei
Yu-meng
YM
Research Laboratory of Pharmaceutical Chemistry and Biomaterials, School of Pharmacy, Chongqing Medical University, No 1, Yixue Yuan Road, Chongqing 400016, PR China.
Zhao
Ling
L
D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002214:Capsules; D005780:Gelatin; D006635:Histamine H2 Antagonists / Q000008:administration & dosage / Q000494:pharmacology*; D008863:Microspheres; D010316:Particle Size; D011817:Rabbits; D011899:Ranitidine / Q000008:administration & dosage / Q000494:pharmacology*; D015203:Reproducibility of Results; D013499:Surface Properties
D002214:Capsules; D006635:Histamine H2 Antagonists; D011899:Ranitidine; D005780:Gelatin