Pharmacokinetics and brain penetration study of chlorogenic acid in rats

1. The present study is designed to investigate the brain distribution and plasma pharmacokinetics profiles of chlorogenic acid (CGA) after intranasal administration in Charles–Foster rats to evaluate whether the CGA molecules are transported directly via the nose-to-brain path.

2. The CGA is administered intravenously (IV) and intranasally (IN) at the dose of 10?mg/kg. Further, its concentration in the plasma, cerebrospinal fluid (CSF) and the whole brain is analyzed by HPLC-UV method.

3. The study observes that CGA is rapidly absorbed in plasma with t_max of 1?min similar to IV route after IN administration. The peak plasma concentration and AUC_0–24 are higher by 3.5 and 4.0 times respectively in IV administration, compared to IN delivery that represents the significant less systemic exposure of CGA in IN route.

4. However, the concentration of CGA in the brain is 4, 6.5, 5.3, 5.2 and 4.5 times higher at 30, 60, 120, 240 and 360?min, respectively in IN administration compared to IV administration. The exposure of CGA in the brain after IN administration (AUC_{brain, IN}) was significantly greater (4 times) as compared to the exposure of CGA in the brain (AUC_{brain, IV}) after IV administration reflecting significant brain uptake of CGA through nasal route. Therefore, IN delivery of CGA can be a promising approach for the treatment of stroke and neurodegenerative disorders.     

《医用有机化学》课程中进行德育渗透

教学与德育有机融会贯通,是当前教育领域的共识。医学本科生秉承"以德载医"的精神,肩负"治病救人"的重任,因此德育教育在整个医学教学中占有重要的地位。《医用有机化学》教材中含有丰富的德育内容,高校教师传授专业知识的同时,在教学过程中巧妙的穿插辩证唯物主义、爱国主义和社会责任感的思政教育,可以帮助学生们树立正确的世界观和人生观。文章以医用有机化学课程为例,主要从教师的自身道德素养、德育在教学过程中的具体实践和德育实施过程中需要注意的问题三方面进行阐述,充分将新时代新理念融入大纲、教案和课堂中,化"知识"为"智慧",变"文化"为"品格",充分发挥医用有机化学课程的德育功能。     

中药透皮吸收促进剂的研究进展

中药透皮吸收促进剂具有起效快、效果好、副作用小、无污染等优点,总结近年来常用中药透皮吸收促进剂的研究进展,中药透皮吸收促进剂主要包括单一中药透皮吸收促进剂和含中药PE多元透皮吸收促进剂,并对存在的问题及今后的研究前景进行了思考和展望。     

Interactions of small polypeptides with dimyristoylphosphatidylcholine monolayers: effect of size and hydrophobicity

The effects of size and hydrophobicity of small (molecular weights below 2,000) polypeptides on their predominantly hydrophobic interactions with a neutral phospholipid monolayer were studied. The changes in surface pressure were determined when various concentrations of Gly, Gly-Gly-Gly, -Ala, -Ala- -Ala- -Ala, -Ala-Gly-Gly-Gly-Gly, -Phe- -Leu- -Glu- -Glu- -Leu, adrenocorticotropic hormone fragments 1–10 (ACTH-(1–10)), porcine β-lipotropin, -endorphin and human fibrinopeptide A were injected under dimyristoylphosphatidylcholine (DMPC) monolayers at an initial surface pressure of 10 dyne/cm. In all cases, when peptides with the same number of residues are compared, the concentration needed to increase the surface pressure of the film by 1 dyne/cm was inversely related to its hydrophobicity. A reasonably good correlation was found to exist between the calculated free energy of transfer of a polypeptide from ethanol to water (a measure of its hydrophobicity) and its ability to increase the surface pressure of the DMPC film (a measure of the extent of its interaction with the neutral lipid monolayer).     

新型经皮渗透促进剂的研究进展

介绍国内外近年来报道的新型经皮渗透促进剂的研究与开发进展,重点介绍若干具代表性的新合成的化合物以及新发现的天然产物,包括内酰胺类、糖苷类、氨基酸衍生物、聚合物、挥发油和酶类等,为合成和发现更加安全、高效的促渗剂提供线索.     

Differential Stripping: Determination of the Amount of Topically Applied Substances Penetrated into the Hair Follicles

The determination of penetration pathways of topically applied substances into the skin is the subject of several investigations. Recently, follicular penetration has become a major focus of interest. To date, a direct, non-invasive quantification of the amount of topically applied substance penetrated into the follicles had not been possible. The development of such a method was the aim of this study. Therefore, the advantages of both stripping techniques, tape stripping and cyanoacrylate skin surface biopsy, were combined and evaluated. Tape stripping was used to remove the part of the stratum corneum that contained the topically applied dye. Subsequently, the follicular contents were ripped off by cyanoacrylate skin surface biopsy. The combined method termed "differential stripping" was evaluated in vitro and in vivo , and the amount of topically applied fluorescent dye penetrated into the hair follicles was quantified after different penetration times. After 30 min, 5% of the recovered concentration of sodium fluorescein was found in the follicular infundibula, where it was still detectable after 48 h. Altogether, the results of this investigation revealed that differential stripping is a new method that can be used to study the penetration of topically applied substances into the follicular infundibula non-invasively and selectively.     

Penetration of fusidic acid and rifampicin into cerebrospinal fluid in low-grade inflammatory meningitis caused by Staphylococcus epidermidis

Cerebrospinal fluid (CSF) concentration-time curves of rifampicin and fusidic acid were studied in a patient with post-operative meningitis caused by Staphylococcus epidermidis. The patient was treated with this combination of antimicrobial agents because of a severe hypersensitivity reaction to vancomycin. Peak CSF concentrations of rifampicin exceeded the MIC by > 60-fold, while those of fusidic acid just reached the MIC. CSF concentrations of fusidic acid were relatively stable within the range reported for patients with uninflamed meninges, but serum levels were surprisingly low. An increase in the metabolism of fusidic acid induced by rifampicin cannot be excluded.     

头低位限制活动对家兔主要脏器微血管壁通透性的影响

本文报导了用40只白色短毛家兔所做的动物模拟失重实验,得出各脏器微血管通透性的动态反应曲线。并用微循环研究方法,分析了模拟失重时各脏器微血管功能状态与微血管通透性之间的关系;阐述了各脏器微循环功能变化特点;并对变化机理作了初步探讨。     

Staple penetration and staple histological response for attaching an epimysial electrode onto the abdominal surface of the diaphragm using a laparoscopic approach

Background: Laparoscopic stapling was found to be a viable option for attaching epimysial electrodes onto the abdominal surface of the diaphragm. Stapling was preferable to suturing due to its simplicity and speed. Methods: Of the two staplers tested in this study, the Ethicon Endopath was preferred over the Autosuture Endo Hernia because the staples did not penetrate the diaphragm when an electrode tab thickness greater than 0.75 mm was used. Results: The thickness of the electrode tab was an important factor in determining staple penetration but large variation in penetration depth indicated that other factors may also play a role. An electrode tab thickness of 1.0–1.25 mm was suggested to minimize the risk of diaphragm perforation. Conclusions: The histological reaction to staples implanted up to 14 months was unremarkable, reflecting the safety of laparoscopic staples for permanently anchoring electrodes on the diaphragm. Received: 2 April 1996/Accepted: 12 June 1996     

人精子穿卵改良试验对不同生育状态男子生育力测定的价值

目的　本研究用一种经改良的人精子穿卵试验 (SPA)处理人精子 ,以探讨一种更简便、快速、经济 ,适合一般实验室要求的方法。方法　将精子体外获能液用磷酸氢二钠把pH值调理至 8.2± 0 .2 ;用普通隔水式恒温培养箱进行培养 ;对 75例不同生育状态男子生育力进行测定 (其中 2 5例有生育力男子 ;2 5例“原因不明”不育男子 ;及 2 5例输精管吻合术后 )。结果　 3种不同生育状态男子的SPA值分别是 (4 7.12± 9.92 ) % ;(2 1.73± 9.91) % ,及 (2 8.0 4± 9.91) %。前两者在统计学上有显著差异 ,(P<0 .0 1) ;后两者在统计学上无明显差异 (P >0 .0 5 )。结果表明经用改良的精子获能液并在普通恒温培养箱培养后精子的活率和活力都有较大的提高 ,这有利于精子的长期获能及提高精子的穿透能力。结论　本研究提示改良后的人精子穿卵试验处理精子确实更简便、快速、经济 ,适合一般实验室要求 ,便于推广。