scholarly journals SCREENING OF BLOOD-BRAIN BARRIER PENETRATION USING THE IMMOBILIZED ARTIFICIAL MEMBRANE PHOSPHATIDYLCHOLINE COLUMN CHROMATOGRAPHY AT THE PHYSIOLOGICAL PH

2013 ◽  
Vol 82 (2) ◽  
pp. 55-62 ◽  
Author(s):  
Jana Žďárová Karasová ◽  
Daniel Jun ◽  
Kamil Kuča
Keyword(s):  
Blood Brain Barrier ◽  
Column Chromatography ◽  
Brain Barrier ◽  
Artificial Membrane ◽  
Immobilized Artificial Membrane ◽  
Blood Brain ◽  
Barrier Penetration

scholarly journals Rapid Screening of Blood-Brain Barrier Penetration of Drugs Using the Immobilized Artificial Membrane Phosphatidylcholine Column Chromatography

2005 ◽  
Vol 11 (1) ◽  
pp. 13-20 ◽  
Author(s):  
Chi Ho Yoon ◽  
Soo Jin Kim ◽  
Beom Soo Shin ◽  
Kang Choon Lee ◽  
Sun Dong Yoo
Keyword(s):  
Blood Brain Barrier ◽  
Prediction Method ◽  
Brain Barrier ◽  
Rapid Screening ◽  
Artificial Membrane ◽  
Immobilized Artificial Membrane ◽  
Blood Brain ◽  
Cns Penetration

The chromatographic capacity factors (kIAM) of 23 structurally diverse drugs were measured by the immobilized artificial membrane (kIAM) phosphatidylcholine chromatography for the prediction of blood-brain barrier (BBB) penetration. The kIAM was determined using themobile phase consisting of acetonitrile:DPBS (20:80 v/v) and corrected for the molar volume of the solutes (kIAM/MWn). The correlation between kIAM/MWn and CNS penetration was highest when measured at pH 5.5 with the power function of n = 4. This in vitro predictionmethod was validated with 7 newly synthesized PDE-4 inhibitors. The relationship between in vivo plasma-to-brain concentration ratios and in vitro CNS penetration was excellent ( r= 0.959). The developed in vitro prediction method may be used as a rapid screening tool for BBB penetration of drugs with passive transport mechanism, with high success, low cost, and reproducibility.

scholarly journals Association Between Vancomycin Blood Brain Barrier Penetration and Clinical Response in Postsurgical Meningitis

2017 ◽  
Vol 20 ◽  
pp. 161 ◽  
Author(s):  
Qing Wang ◽  
Si Chen ◽  
Yan-Gang Zhou ◽  
Ping Xu ◽  
Yi-Ping Liu ◽  
...  
Keyword(s):  
Cerebrospinal Fluid ◽  
Clinical Response ◽  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Serum Samples ◽  
Cell Counts ◽  
Blood Cell Counts ◽  
Blood Brain ◽  
Barrier Penetration ◽  
White Blood Cell Counts

PURPOSE: This study investigated the association between vancomycin blood brain barrier penetration and clinical response in patients with postsurgical meningitis. METHODS: Adult patients with postsurgical meningitis were recruited. Eligible patients received vancomycin 500 mg every 6 h for at least 5 days. On day 3 or 4, cerebrospinal fluid (CSF) and simultaneous serum samples were obtained to determine CSF minimum concentrations (Cmin), serum Cmin and CSF to serum Cmin ratio. RESULTS: Twenty-two patients (14 men and 8 women; mean age of 52.6± 12.1 years) were recruited. The vancomycin Cmin was 3.63 ± 1.64 mg/L in CSF and 13.38 ± 5.36 mg/L in serum, with the CSF to serum Cmin ratio of 0.291 ± 0.118. The Cmin in serum and in CSF showed a significant correlation (p=0.005, r =0.575). The vancomycin CSF Cmin had a significant correlation with the decline of white blood cell counts (WBCs) in CSF (p=0.003, r =0.609). CSF Cmin, serum Cmin and CSF to serum Cmin ratio all showed no significant correlation with clinical response (p=0.335, 0.100, 0.679, respectively). CONCLUSIONS: There was a positive correlation between serum Cmin and CSF Cmin. However, only CSF Cmin is positively correlated with WBCs improvement in CSF. All other parameters such as serum Cmin, CSF Cmin and CSF to serum Cmin ratio had no correlation with clinical response. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

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