|
KMID : 0369820060360060363
|
|
Jorunal of Korean Pharmaceutical Sciences
2006 Volume.36 No. 6 p.363 ~ p.369
|
|
|
Nasal Administration of Granisetron to Rats
|
|
Woo Jong-Soo
|
|
|
Abstract
|
|
|
|
Granisetron is a selective 5-HT3 receptor antagonist that is used therapeutically for the prevention of vomiting and nausea associated with emetogenic cancer chemotherapy. although this drug is commercially available for intravenous and oral dosage, there is a need for intranasal delivery formulations in specific patient populations in which the use of these dosage forms may be unfeasible and/or inconvenient. A rapid and specific high-performance liquid chromatography method with mass spectrometric detection(LC-MS) was developed and validated for the analysis of granisetron in plasma after nasal administration in rats. This method has been validated for concentrations ranging from 5 to 1000ng/ml with simple treatment. This technique has high level reproducibility, accuracy, and sensitivity. The method described was found to be suitable for the analysis of all samples collected during preclinical pharmacokinetic investigations of granisetron in rats after nasal administration. This study was aimed to investigate the feasibility of nasal delivery of granisetron for the elimination of vomiting. The effect of osmolarity, dosage volume at the same dose and applied dose on the nasal absorption of granisetron in rats were observed. No significant difference in the effect of osmorality and dosage volume at the same dose were observed. As the applied dose of granisetron in nasal formulation increased, the absroption increased linearly. Based on these results it appears that only the applied dose(drug mass) determined the nasal absorption of granisetron. The bioavailability of granisetron on nasal administration of 4 mg/kg appeared to be compareable to that of intravenous admigistration of the same dose. These results suggest that granisetron can be efficiently delivered nasally and the development of nasnal formulatuion will be feasible.
|
|
|
KEYWORD
|
|
|
Nasal administration, Granisetron, LC-MS, Osmolarity
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
|