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KMID : 0043320100330050691
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Archives of Pharmacal Research
2010 Volume.33 No. 5 p.691 ~ p.696
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The In Situ and In Vivo Study on Enhancing Effect of Borneol in Nasal Absorption of Geniposide in Rats
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Zhai Yongsong
Lu Yang
Chen Xiaolan
Du Shouying
Wu Qing
Yao Zongling
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Abstract
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The objective of this research was to study the in situ and in vivo nasal absorption of Geniposide (Ge) co-administered with borneol. A rat in situ nasal perfusion technique with a novel volumeadjusted calculation was used to examine the absorption rate and extent of Ge. The influence of different experimental conditions such as purity of extract, drug concentration, co-administration with synthetic borneol or natural borneol were also investigated. Results indicated nasal absorption of Ge was primarily by passive diffusion that resembled first order kinetics. Following co-administration with borenol, the drug absorption was increased by 1.4 and 1.7 folds for natural borneol and synthetic borneol , respectively. However, the effect of other factors on drug absorption was not significant. In addition, it was also observed that there is a positive correlation between the absorption of water and Ge by the nasal route. In vivo studies carried out in rats where Ge was co-administered with NB and the pharmacokinetic profile obtained following intranasal administration were compared with those after intravenous administration. The bioavailability of Ge by intranasal was 101.5% and Tmax was 2.04 ± 0.64 min. MRT was 218.7 ± 74.1 min and 44.4 ± 8.9 min for intranasal and intravenous, respectively. Combined with the borneol, Ge can be promptly and thoroughly absorbed intranasally in rats.
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KEYWORD
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Geniposide, Nasal absorption, Borneol, Enhancement, Pharmacokinetics
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