Partition coefficients (n-octanol/water) of N-butyl-p-aminobenzoate and other local anesthetics measured by reversed-phase high-performance liquid chromatography

被引:44
作者
Grouls, RJE
Ackerman, EW
Korsten, HHM
Hellebrekers, LJ
Breimer, DD
机构
[1] CATHARINA HOSP,DEPT ANESTHESIOL,EINDHOVEN,NETHERLANDS
[2] UNIV UTRECHT,FAC VET MED,DEPT CLIN SCI COMPAN ANIM,UTRECHT,NETHERLANDS
[3] UNIV UTRECHT,FAC VET MED,DEPT ANESTHESIOL,UTRECHT,NETHERLANDS
[4] CTR BIOPHARMACEUT SCI,LEIDEN,NETHERLANDS
来源
JOURNAL OF CHROMATOGRAPHY B | 1997年 / 694卷 / 02期
关键词
partition coefficient; methyl-p-aminobenzoate; benzocaine; procaine; N-butyl-p-aminobenzoate; mepivacaine; prilocaine; lidocaine; bupivacaine; etidocaine; tetracaine; oxubuprocaine;
D O I
10.1016/S0378-4347(97)00207-7
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
For the determination of the logarithmic partition coefficients between n-octanol and water (log P-o/w) of local anesthetics, the pH of the aqueous phase needs to be adjusted to high values to ensure that the local anesthetics are in the unionized form. Using the shake-flask or the stir-flask method, this high pH may catalyze hydrolysis, leading to increasing amounts of impurities in time. These impurities exclude non-selective quantification methods Like UV spectrometry and require repetitive quantitative analysis of both liquid phases resulting in a tedious and time-consuming method. A rapid reversed-phase HPLC method was developed to measure log P-o/w of the local anesthetics N-butyl-p-aminobenzoate, methyl-p-aminobenzoate, benzocaine, procaine, mepivacaine, prilocaine, lidocaine, bupivacaine, etidocaine, tetracaine and oxubuprocaine. (C) 1997 Elsevier Science B.V.
引用
收藏
页码:421 / 425
页数:5
相关论文
共 31 条
[1]   NOVEL, HIGHLY DEACTIVATED REVERSED-PHASE FOR BASIC COMPOUNDS [J].
ASCAH, TL ;
FEIBUSH, B .
JOURNAL OF CHROMATOGRAPHY, 1990, 506 :357-369
[2]   MOLECULAR MECHANISMS OF LOCAL-ANESTHESIA - A REVIEW [J].
BUTTERWORTH, JF ;
STRICHARTZ, GR .
ANESTHESIOLOGY, 1990, 72 (04) :711-734
[3]  
CIOVINO BG, 1976, LOCAL ANESTHETICS ME
[4]   STUDY OF THE LIPOPHILICITY OF ORGANIC-BASES BY REVERSED-PHASE LIQUID-CHROMATOGRAPHY WITH ALKALINE ELUENTS [J].
DEBIASI, V ;
LOUGH, WJ ;
EVANS, MB .
JOURNAL OF CHROMATOGRAPHY, 1986, 353 :279-284
[5]   HYDROPHOBICITY ESTIMATIONS BY REVERSED-PHASE LIQUID-CHROMATOGRAPHY - IMPLICATIONS FOR BIOLOGICAL PARTITIONING PROCESSES [J].
DORSEY, JG ;
KHALEDI, MG .
JOURNAL OF CHROMATOGRAPHY A, 1993, 656 (1-2) :485-499
[6]  
GLYN GL, 1972, J PHARM SCI, V61, P838
[7]   MULTIVARIATE METHODS TO EVALUATE THE ROLE OF MIXED SUPPORTS IN REVERSED-PHASE THIN-LAYER CHROMATOGRAPHY [J].
GULLNER, G ;
CSERHATI, T ;
BORDAS, B ;
VALKO, K .
JOURNAL OF LIQUID CHROMATOGRAPHY, 1989, 12 (06) :957-978
[8]  
KALISZAN R, 1986, CRC CR REV ANAL CHEM, V16, P323, DOI 10.1080/10408348608085547
[9]  
KALISZAN R, 1988, CHROMATOGRAPHIA, V15, P5
[10]   LONG-LASTING EPIDURAL SENSORY BLOCKADE BY N-BUTYL P-AMINOBENZOATE IN THE DOG - NEUROTOXIC OR LOCAL-ANESTHETIC EFFECT [J].
KORSTEN, HHM ;
HELLEBREKERS, LJ ;
GROULS, RJE ;
ACKERMAN, EW ;
VANZUNDERT, AAJ ;
VANHERPEN, H ;
GRUYS, E .
ANESTHESIOLOGY, 1990, 73 (03) :491-498