Correlations between theophylline concentrations in plasma, erythrocytes and cantharides-induced blister fluid and peak expiratory flow in asthma patients

Philip-Joët, F.; Bruguerolle, Bernard; Reynaud, M; Arnaud, A.

doi:10.1007/bf02285104

Cited by 8 publications

(2 citation statements)

References 11 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…However, cantharides blisters are formed due to chemical irritation of the skin, and blister fluid mimics inflamed tissue fluid rather than a physiological protein free fluid. In blister fluid, high protein concentrations were observed [ 7], possibly being the reason for the cumulation of protein bound drugs in blister fluid [ 17]. This cumulation led some authors to the conclusion that cantharides induced skin blisters are not representative of the peripheral compartment in the measurement of highly protein bound drugs [ 4].…”

Section: Discussionmentioning

confidence: 99%

Direct assessment of peripheral pharmacokinetics in humans: comparison between cantharides blister fluid sampling, in vivo microdialysis and saliva sampling

Brunner¹,

Schmiedberger²,

Schmid

et al. 1998

Brit J Clinical Pharma

View full text Add to dashboard Cite

Aims Skin blister fluid sampling, in vivo microdialysis and saliva sampling are commonly employed as surrogates for the measurement of drug concentrations in peripheral compartments. Although expected to exhibit comparable results, data derived from these techniques have never been directly compared. Thus, the aim of the present study was to evaluate the comparability of these techniques. Methods Paracetamol, a model drug with low protein binding, was administered to seven healthy volunteers at an oral dose of 2000 mg. Subsequently, tissue kinetics were measured simultaneously in cantharides induced skin blisters, microdialysates of subcutaneous-and skeletal muscle-tissue and saliva and compared to serum concentrations. Results Mean ratio (AUC blister /AUC serum ) was 0.88 (95% CI, 0.50-1.26), mean ratio (AUC muscle /AUC serum ) was 1.08 (0.67-1.49), mean ratio (AUC subcutaneous /AUC serum ) was 0.96 (0.41-1.51) and mean ratio (AUC saliva /AUC serum ) was 1.83 (1.39-2.27). In this study the concentration profiles after single oral administration differed among the three methods. The time course of the concentration peripheral compartment /concentration serum -ratios showed that cantharides blister and microdialysate concentrations closely paralleled serum levels. An equilibration period of less than 2 h had to be taken into account for blister measurements. In contrast, saliva concentrations were significantly higher than corresponding serum concentrations. Conclusions Skin blister sampling and microdialysis closely mirrored corresponding serum concentrations and, thus, proved to be suitable techniques for the assessment of peripheral compartment pharmacokinetics. In contrast, saliva data overestimated the corresponding serum concentrations.

show abstract

Section: Discussionmentioning

confidence: 99%

Direct assessment of peripheral pharmacokinetics in humans: comparison between cantharides blister fluid sampling, in vivo microdialysis and saliva sampling

Brunner¹,

Schmiedberger²,

Schmid

et al. 1998

Brit J Clinical Pharma

View full text Add to dashboard Cite

show abstract

“…Blister fluid sampling is a well‐established method used for examining tissue distribution of anti‐infective drugs. However, many variables potentially affect the results obtained from blister fluid sampling, including the size of the blisters [24], the degree of inflammation due to blister induction or underlying pathology [25], the timing of blister formation [26] and the possibility of protein accumulation in the blister fluid over time [27]. These variables may complicate interpretation of tissue concentration data obtained using this technique.…”

Section: Introductionmentioning

confidence: 99%

Human subcutaneous tissue distribution of fluconazole: comparison of microdialysis and suction blister techniques

Sasongko

Williams

Day

et al. 2003

Brit J Clinical Pharma

View full text Add to dashboard Cite

Aims To investigate uptake of fluconazole into the interstitial fluid of human subcutaneous tissue using the microdialysis and suction blister techniques. Methods A sterile microdialysis probe (CMA/60) was inserted subcutaneously into the upper arm of five healthy volunteers following an overnight fast. Blisters were induced on the lower arm using gentle suction prior to ingestion of a single oral dose of fluconazole (200 mg). Microdialysate, blister fluid and blood were sampled over 8 h. Fluconazole concentrations were determined in each sample using a validated HPLC assay. In vivo recovery of fluconazole from the microdialysis probe was determined in each subject by perfusing the probe with fluconazole solution at the end of the 8 h sampling period. Individual in vivo recovery was used to calculate fluconazole concentrations in subcutaneous interstitial fluid. A physiologically based pharmacokinetic (PBPK) model was used to predict fluconazole concentrations in human subcutaneous interstitial fluid. Results There was a lag-time (approximately 0.5 h) between detection of fluconazole in microdialysate compared with plasma in each subject. The in vivo recovery of fluconazole from the microdialysis probe ranged from 57.0 to 67.2%. The subcutaneous interstitial fluid concentrations obtained by microdialysis were very similar to the unbound concentrations of fluconazole in plasma with maximum concentration of 4.29 ± 1.19 m g ml -1 in subcutaneous interstitial fluid and 3.58 ± 0.14 m g ml -1 in plasma. Subcutaneous interstitial fluid-to-plasma partition coefficient (K p ) of fluconazole was 1.16 ± 0.22 (95% CI 0.96, 1.35). By contrast, fluconazole concentrations in blister fluid were significantly lower (P < 0.05, paired t-test) than unbound plasma concentrations over the first 3 h and maximum concentrations in blister fluid had not been achieved at the end of the sampling period. There was good agreement between fluconazole concentrations derived from microdialysis sampling and those estimated using a blood flow-limited PBPK model. Conclusions Microdialysis and suction blister techniques did not yield comparable results. It appears that microdialysis is a more appropriate technique for studying the rate of uptake of fluconazole into subcutaneous tissue. PBPK model simulation suggested that the distribution of fluconazole into subcutaneous interstitial fluid is dependent on tissue blood flow.

show abstract

Microdialysis in Antibiotic Research

Zeitlinger

Marchand

Couet

et al. 2012

Microdialysis in Drug Development

View full text Add to dashboard Cite

Correlations between theophylline concentrations in plasma, erythrocytes and cantharides-induced blister fluid and peak expiratory flow in asthma patients

Cited by 8 publications

References 11 publications

Direct assessment of peripheral pharmacokinetics in humans: comparison between cantharides blister fluid sampling, in vivo microdialysis and saliva sampling

Direct assessment of peripheral pharmacokinetics in humans: comparison between cantharides blister fluid sampling, in vivo microdialysis and saliva sampling

Human subcutaneous tissue distribution of fluconazole: comparison of microdialysis and suction blister techniques

Microdialysis in Antibiotic Research

Contact Info

Product

Resources

About