灯盏花素经鼻给药吸收特性研究

目的研究灯盏花素的离体、在体经鼻吸收特性,为灯盏花素的鼻腔给药制剂设计提供依据。方法采用V-C扩散池,以新鲜犬鼻黏膜为渗透屏障,以含灯盏花乙素0.25、0.50、1.25 mg/mL的灯盏花素PBS液(pH 6.5)为释放液,以空白PBS为接收液,进行渗透试验;采用大鼠鼻腔循环灌流法,以1.01、1.70、4.48 mg/mL灯盏花素PBS溶液(pH 6.5)作为鼻腔循环液,HPLC法测定灯盏乙素,进行在体鼻黏膜吸收试验。结果灯盏花素高、中、低质量浓度组的犬鼻黏膜渗透系数分别为3.6×10-5、1.272×10-3、1.856×10-3cm/min(n=3)。随着灯盏花素的质量浓度增加,其渗透系数呈剂量依赖性增加;高、中、低质量浓度灯盏花素的大鼠在体吸收速度常数分别为4.5×10-3、2.3×10-3、1.7×10-3min-1,随质量浓度的增加,鼻黏膜吸收量逐渐增加,但其吸收速度常数较小。结论灯盏花素可经鼻吸收,质量浓度对其吸收的影响较大,适合制备成经鼻给药的新制剂。

磷酸川芎嗪脂质体大鼠在体鼻黏膜吸收研究

目的研究磷酸川芎嗪脂质体的鼻黏膜吸收特性。方法采用大鼠在体鼻腔循环灌流法,考察循环液流速、药物浓度对磷酸川芎嗪脂质体鼻黏膜吸收的影响,并对磷酸川芎嗪脂质体和磷酸川芎嗪溶液的鼻黏膜吸收进行比较。结果在流速为1.2～2.4mL/min范围内,磷酸川芎嗪脂质体鼻黏膜吸收速率常数随流速的增加而增加;在浓度为0.245～0.98mg/mL范围内,鼻黏膜吸收速率常数随浓度的增加而增加。与同浓度的磷酸川芎嗪溶液比较,脂质体吸收更快,鼻黏膜经时吸收量更高。结论磷酸川芎嗪脂质体比磷酸川芎嗪溶液鼻黏膜吸收更加完全。

磷酸川芎嗪脂质微球在大鼠鼻黏膜吸收的特性

目的研究磷酸川芎嗪(tetramethylpyrazine phosphate,TMPP)脂质微球在大鼠鼻黏膜吸收的特性。方法采用大鼠鼻腔循环灌流法,考察循环液流速、TMPP溶液浓度、TMPP脂质微球浓度对鼻黏膜吸收的影响,并对TMPP脂质微球和TMPP溶液的鼻吸收水平进行比较。结果在流速为2.0ml/min时,TMPP脂质微球鼻黏膜吸收速率常数有最大值;在浓度为0.25～1.0mg/ml范围内,TMPP溶剂的鼻黏膜吸收速率常数随浓度变化趋势不明显;而TMPP脂质微球的鼻黏膜吸收速率常数随浓度的增大而减小,与同浓度TMPP溶液比较,TMPP脂质微球吸收更快,鼻黏膜随时间延长吸收量更高。结论将TMPP制备成脂质微球能促进药物在鼻黏膜的吸收。

石杉碱甲的大鼠鼻黏膜吸收研究

目的研究治疗早老性痴呆症药物石杉碱甲的鼻黏膜吸收特性。方法采用石杉碱甲进行大鼠鼻腔灌流实验,测定循环液中药物浓度。结果随着石杉碱甲的浓度增加（0.125~0.75mg/mL）,其吸收速度呈线性增加（r=0.995）。在pH值5.5-7.5内,随pH值的升高,其吸收速度增加。结论石杉碱甲的鼻黏膜吸收良好,其吸收程度与药液的浓度和pH值有较好的相关性。

可吸收内置夹板在单侧唇裂鼻畸形早期整复中的应用

单侧唇裂整复术后常表现为患侧鼻翼软骨塌陷、患侧鼻小柱过短等继发鼻畸形。作者在唇裂整复术中采用可吸收的鼻内置夹板,保护支撑患侧鼻翼软骨,以防因瘢痕挛缩而造成的鼻继发畸形的可能。 材料和方法 选用的可吸收内置夹板为无孔隙的聚乙二醇酸/聚乳酸共聚物,它是一种安全可靠,可缓慢吸收的生物替代材料。

中药挥发油对水蛭素经鼻给药的影响研究

目的以水蛭素为模型药物,探讨中药挥发油对蛋白/多肽类药经鼻黏膜吸收的影响,并考察中药挥发油的鼻纤毛毒性。方法用离体蟾蜍上颚黏膜模型,评价水蛭素及中药挥发油的鼻纤毛毒性;以同位素示踪法测定水蛭素,以离体猪鼻黏膜Valia-Chien水平扩散池法与在体大鼠鼻腔灌流实验,考察部分中药挥发油对水蛭素透鼻黏膜吸收的影响。结果离体实验结果表明,3%冰片和3%薄荷油对水蛭素鼻黏膜吸收促进作用较显著;在体实验结果表明,3%冰片和3%薄荷油组水蛭素的血药浓度显著高于阴性对照组,3%冰片和3%薄荷油组水蛭素的肾脏分布显著高于阴性对照组及其他实验组。纤毛毒性实验结果显示,中药挥发油对离体蟾蜍上颚黏膜纤毛影响由小到大的顺序为:1%冰片<1%薄荷油<3%冰片<1%石菖蒲油<1%细辛油<5%冰片<3%石菖蒲油<5%细辛油<5%薄荷油<5%石菖蒲油<3%细辛油<3%薄荷油。结论3%薄荷油和3%冰片对水蛭素透鼻黏膜吸收有较显著促进作用;中药挥发油对离体蟾蜍上颚黏膜纤毛均有不同程度的影响,但纤毛运动相对百分率大于60%,毒性较小。

基于单向灌流法的艾片大鼠在体鼻黏膜吸收研究

目的:研究艾片的大鼠在体鼻黏膜吸收影响因素。方法:运用单向灌流模型、采用GC对艾片中有效成分龙脑进行检测,分别研究药物质量浓度、灌流速度、pH对艾片吸收的影响。结果:灌流速度对艾片的吸收速率常数(Ka)有显著性影响;药物质量浓度和pH对Ka无显著性影响。结论:艾片的鼻黏膜吸收良好,艾片的吸收速率不受药物质量浓度的影响,其在鼻腔按照一级被动方程进行吸收。

醒脑静不同制剂给大鼠鼻单向灌流后龙脑和麝香酮吸收比较研究

目的比较醒脑静不同制剂给大鼠鼻单向灌流后其有效成分龙脑和麝香酮吸收特征。方法采用大鼠在体鼻单向灌流模型,GC法测定灌流液中龙脑和麝香酮的量,比较醒脑静滴鼻液与醒脑静微乳中龙脑和麝香酮在大鼠鼻腔的吸收。结果醒脑静滴鼻液中龙脑吸收速率常数(Ka)为(1.00±0.02)min 1,醒脑静微乳中龙脑Ka为(0.76±0.03)min 1;醒脑静滴鼻液中麝香酮Ka为(0.76±0.02)min 1,醒脑静微乳中麝香酮Ka为(0.58±0.10)min 1。结论醒脑静滴鼻液中龙脑和麝香酮在鼻腔的吸收均较醒脑静微乳快。

Influence of pH Environment on Nasal Absorption of Meptazinol Hydrochloride

Aim To investigate the relationship between pH environment of meptazinolhydrochloride (MEP) and its nasal absorption. Methods In situ nasal peifusion was performed to studythe effect of pH environment on the nasal absorption. Its effect on the transport from nose tobrain was further researched by in vivo experiment. Results In in situ perfusion experiment, thenasal absorption of MEP in basic environment was significantly higher than that in acid condition,but the difference was not observed in in vivo experiment. Conclusion The pH environment ofmeptazinol hydrocloride in formulation cannot be regarded as an important factor influencing nasalabsorption and transport from nose to brain.

水蛭素鼻腔给药的影响因素研究

目的:探讨蛋白多肽类中药水蛭素的经鼻吸收特性及其影响因素。方法:用离体蟾蜍上颚黏膜模型,评价水蛭素的鼻纤毛毒性;采用Valia-Chien水平扩散池实验与在体大鼠鼻腔灌流实验,观察水蛭素鼻腔给药的吸收特性以及药物浓度、pH值等因素对吸收的影响。结果:Valia-Chien水平扩散池实验和在体大鼠鼻腔灌流实验显示水蛭素能够透过鼻黏膜吸收;介质pH值、药物浓度等因素均能影响水蛭素的吸收,但水蛭素的浓度与渗透系数、吸收速度间线性关系不明显,水蛭素浓度为0.6mg.mL-1时,鼻黏膜吸收较好。结论:水蛭素对离体蟾蜍上颚黏膜纤毛影响较小,并且能透过鼻黏膜吸收;药物的浓度和介质的pH值对鼻黏膜的吸收均有影响。

Influence of intranasal medication on the structure of the nasal mucosa

OBJECTIVE: To study the influence of intranasal medication on the structure, pathology and reversibility of the nasal mucosa to provide a basis for the feasibility of intranasal route of drug administration. METHODS: Nasal drops of gentamicin were placed in the nasal cavity of rabbits for 3, 5, 7, 14 and 28 days. After that, the drops were stopped and drugs protecting the nasomucosa were used for one and three weeks. After being sacrificed over time, the nasomucosa of the rabbit was observed under optical and electron microscopes. RESULTS: Damage to the nasal mucosa appeared to different extents with prolonged use of nasal drops. Within 3 - 7 days of applying the drug, damages to the nasal mucosa gradually appeared, and after two and four weeks, were most serious. After stopping the drug, the nasal mucosa was gradually restored. CONCLUSION: Damages of drugs to the nasal mucosa could be restored. The intranasal route of drug administration would be feasible and clinically applicable.

Influence of intranasal medication on the structure of the nasal mucosa

To study the influence of intranasal medication on the structure, pathology and reversibility of the nasal mucosa to provide a basis for the feasibility of intr anasal route of drug administration Methods Nasal drops of gentamicin were placed in the nasal cavity of rabbits for 3, 5, 7 , 14 and 28 days After that, the drops were stopped and drugs protecting the nasomucosa were used for one and three weeks After being sacrificed over t ime, the nasomucosa of the rabbit was observed under optical and electron micros copes Results Damage to the nasal mucosa appeared to different extents with prolonged use of nasal drops Within 3-7 days of applying the drug, damages to the nasal mucosa gradually appeared, and after two and four weeks, were most serious After stop ping the drug, the nasal mucosa was gradually restored Conclusion Damages of drugs to the nasal mucosa could be restored The intranasal rou te of drug administration would be feasible and clinically applicable