Comparative Pharmacokinetic Studies of Borneol in Mouse Plasma and Brain by Different Administration

来源 :2012年全国中药注射剂安全性评价及质量控制学术研讨会 | 被引量 : 0次 | 上传用户:chunya88
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  Borneol, a monoterpenoid alcohol, is used widely, particularly in combined formulas for preventing and curing cardiovascular and cerebrovascular diseases in traditional Chinese medicine.In order to understand the blood and brain pharmacokinetics after intravenous, intranasal and oral administration and to investigate the superiority and feasibility of intranasal administration, a simple gas chromatographic (GC) method with flame ionization detection (FID) was developed for the determination of bomeol.The blood samples and brain were collected at 1, 3, 5, 10, 20, 30, 60, 90, 120 min after intravenous, intranasal and oral administration of borneol as a dosage of 30.0 mg/kg.Sample preparations were carried out by liquid-liquid extraction with an intemal standard solution of octadecane.The pharmacokinetic parameters were calculated by the software of Kinetica.The calibration curves were good linear in the range of 0.1 1~ 84.24 μg/mL and 0.16~63.18 μg/g for bomeol in plasma and brain, respectively.The methodological and extraction recoveries were both in the range of 85%~115%.The intra-day and inter-day variability for plasma and brain samples were ≤ 5.00% RSD.The absolute bioavailability F of intranasal and oral administration was 90.68% and 42.99%.The relative brain targeted coefficient Re of intranasal and oral administration was 68.37% and 38.40%.The GC-FID method developed could be applied to determination and pharmacokinetic study.The borneol of injection was distributed and metabolized fast without absorption process.The borneol of oral administration was distributed slowly than injection and nasal administration and had a lower absolute bioavailability.Nasal administration which was fast to blood, easy to use and the greatly improving safety than injection, was worthy of further development of encephalopathy treatment route for traditional Chinese medicine administration.
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