Borneol,a novel agent that improves central nervous system drug delivery by enhancing blood–brain barrier permeability

The clinical application of central nervous system (CNS) drugs is limited by their poor bioavailability due to the blood–brain barrier (BBB). Borneol is a naturally occurring compound in a class of ‘orifice-opening’ agents often used for resuscitative purposes in traditional Chinese medicine. A growing body of evidence confirms that the ‘orifice-opening’ effect of borneol is principally derived from opening the BBB. Borneol is therefore believed to be an effective adjuvant that can improve drug delivery to the brain. The purpose of this paper is to provide a comprehensive review of information accumulated over the past two decades on borneol’s chemical features, sources, toxic and kinetic profiles, enhancing effects on BBB permeability and their putative mechanisms, improvements in CNS drug delivery, and pharmaceutical forms. The BBB-opening effect of borneol is a reversible physiological process characterized by rapid and transient penetration of the BBB and highly specific brain regional distribution. Borneol also protects the structural integrity of the BBB against pathological damage. The enhancement of the BBB permeability is associated with the modulation of multiple ATP-binding cassette transporters, including P-glycoprotein; tight junction proteins; and predominant enhancement of vasodilatory neurotransmitters. Systemic co-administration with borneol improves drug delivery to the brain in a region-, dose- and time-dependent manner. Several pharmaceutical forms of borneol have been developed to improve the kinetic and toxic profiles of co-administered drugs and enhance their delivery to the brain. Borneol is a promising novel agent that deserves further development as a BBB permeation enhancer for CNS drug delivery.     

气相色谱法测定辛香止痛散中薄荷脑和冰片含量

采用气相色谱法测定辛香止痛散中薄荷脑、冰片的含量。色谱条件为１０％ＰＥＧ－２０ＭＣｈｒｏｍｏｓｏｒｂＷＡＷＤＭＣＳ（６０～８０目），２ｍ×３ｍｍ玻璃柱，柱温和检测器（ＦＩＤ）温度分别为１１５℃，２００℃。样品用乙酸乙酯萃取，采用内标法定量。结果薄荷脑与冰片在０．６～１．６ｍｇ／ｍｌ呈良好线性，ｒ＝０．９９９９，ＲＳＤ≤１．０％。     

气相色谱法测定镇江膏药中冰片和薄荷脑的含量

建立了镇江膏药中冰片和薄荷脑的气相色谱测定方法。色谱固定液为１５％ＰＥＧ，两者回收率分别为９８．８０％和１０１．３％。样品直接溶于石油醚中，经过滤后进行分析，对１３个批号样品的测定结果说明该方法适于镇江膏药中冰片和薄荷脑的质量控制。     

合成冰片与松节油中■-蒎烯的GLC分析

本文初步建立了松节油中(?)-蒎烯以及合成冰片的气相色谱分析方法。在5％DNP柱上,采用内标法(平均CV=1.24％,回收率99.18％,CV=0.7％)和外标法(平均CV<1％);在5％DEGS柱上,采用面积归一化法(平均CV<1％)测定(?)-蒎烯。在5％DEGS柱上,采用面积归一化法测定合成冰片。其中的两种组分(龙脑和异龙脑)测定结果变异系数(CV)均小于1％。色谱条件为:固定液涂布量5％,载体Chromosorb W AW—DMCS 0/100,检测器FID或TCD,载气氮气～20ml/分,柱温分别为115°或140℃。     

中药冰片的本草学考证

从本草学的角度对中药冰片进行分析考证,按冰片名称、原植物、性味、主治4个方面分别论述,对天然冰片进一步研究的必要,对其发展研究进行考证也有一定现实意义。     

张景岳《新方八阵》之锡灰、脑荷药物考

对张景岳《新方八阵》中的几味在中药材标准和权威药学典籍中没有明确记载的药物进行了引据考证,以便为其以后的研究提供文献依据;通过考证历代本草对"锡灰""、脑荷"的记载,并对其加以比较、分析后,认为《新方八阵》所记载的中药"锡灰"为铅灰,"脑荷"应该是指苏州龙脑薄荷。     

冰麝消痛膏的薄层色谱鉴别研究

[目的]制定冰麝消痛膏的薄层色谱鉴别方法。[方法]利用薄层色谱法对处方中冰片、血竭进行鉴别。[结果]供试品与对照品(药材)色谱相对应的位置上显相同颜色的斑点,阴性样品无干扰。[结论]此法可用于冰麝消痛膏的定性鉴别。     

艾片的体外黏膜渗透性及影响因素研究

目的:考察艾片的体外黏膜渗透性及影响因素。方法:选择离体牛蛙腹皮为渗透模型,采用改良的Franz扩散池进行体外黏膜实验;GC测定艾片中龙脑的含量,研究接收液的不同pH值、温度、搅拌速度及药物浓度对艾片体外黏膜渗透的影响。结果:搅拌速度对艾片的渗透有一定的影响;而接收液的pH值、温度及药物浓度对艾片的渗透无影响。艾片黏膜渗透性良好,累积渗透率与时间符合一级吸收过程。结论:离体牛蛙腹皮可作为艾片的体外黏膜渗透性研究的实验模型。     

龙脑樟枝叶中挥发油化学成分GC-MS分析

目的:研究龙脑樟Cinnamomum caraphora(L.)Presl枝叶中挥发油的化学成分。方法:采用水蒸气蒸馏法提取龙脑樟枝叶挥发油,用气相色谱-质谱联用技术分析提取物,利用峰面积归一化法确定挥发性组分的相对含量。结果:首次从挥发油中鉴定出了34个化学成分,占挥发油总量的98.53%,其中龙脑的含量最高,达到67.17%。结论:新鲜龙脑樟枝叶中龙脑含量很高,可以作为提取天然冰片的良好资源。     

冰片及其制剂对大鼠胃粘膜刺激作用的研究

目的研究冰片及其制剂对大鼠胃粘膜的刺激作用。方法采用雄性Wistar大鼠,灌胃给药,剂量80mg·kg-1,连续给药7d,按Guth标准评估溃疡指数。结果和空白组相比,冰片组溃疡指数有显著性差异,各制剂组溃疡指数和冰片组相比有显著性差异。结论冰片能够对雄性大鼠胃粘膜造成刺激,形成损伤,冰片制剂能够在一定程度上减轻这种刺激。