摘要:

AbstractA simple, rapid, and sensitive procedure is described for the determination of Fendosal in plasma. After extraction of Fendosal from buffered plasma, the drug is determined by measurement of the fluorescence induced by irradiation with short‐wave ultra‐violet (UV) light. The complete procedure can be completed in less than 2 h; one technician can perform up to 50 assays in one working day. The limit of detection corresponds to 0–1 μg ml−1plasma. Drug concentration and induced fluorescence were linearly related over the concentration range 0

ISSN:0142-2782    

DOI:10.1002/bdd.2510010302

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

AbstractA single oral dose of the diuretic chlorthalidone (100 or 200 mg) was given to six cholecystectomized patients with T‐tube drainage of the common bile duct, and the 24 h bile and urine were collected during 3–7 days. Urinary recovery of chlorthalidone was 23–27 per cent of the dose, which is in the range of that in healthy volunteers. Chlorthalidone concentration in bile was 11–44 times lower than urine concentration in corresponding periods, and biliary recovery was only 0·6–1·4 per cent of the dose. When compared from equal periods of sampling of bile and urine, the same relative amount of drug was found in bile, whether the 100 or 200 mg dose had been given (viz., a fraction of 2·5–4·7 per cent and 2·5–5·7 per cent of corresponding urinary amounts respectively). It was concluded that excretion into bile constitutes only a minor route of elimination for unchanged chlorthalidone. Bile samples treated with glucuronidase and sulphatase showed no increase of chlorthalidone concentration. The open acid analogue of chlorthalidone, 3‐(4‐chloro‐3‐sulphamoylbenzoyl)‐benzoic acid, was apparently not formed as a human metabolite, as evidenced by gas chromatographic an

ISSN:0142-2782    

DOI:10.1002/bdd.2510010303

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

ISSN:0142-2782    

DOI:10.1002/bdd.2510010304

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

AbstractA determinant solution for the infinity values of multi‐exponential equations using the Guggenheim method of equal time intervals is demonstrated. The resultant solution is independent of the rate constants and can be applied using data in the early non‐log‐linear phase of the process. The minimum number of data points needed for an nth exponential equation is (2

ISSN:0142-2782    

DOI:10.1002/bdd.2510010305

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

AbstractChlorodesmethyldiazepam (I) concentrations were followed for 72 h in the plasma of four volunteers given 2 mg of the drug orally. The drug appears to be well absorbed, reaching peak plasma levels of 20–30 ng ml−11–2 h after administration; 72 h after administration, plasma concentrations are still measurable (5 ng ml−1).The analytical method involved a single extraction of I from the plasma into benzene followed by centrifugation, evaporation, and gas‐chromatographic analysis of th

ISSN:0142-2782    

DOI:10.1002/bdd.2510010306

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

AbstractDisplacement of cephazolin, a highly protein‐bound β‐lactam antibiotic, by sulpha‐phenazole was studiedin vitroandin vivo. In vitro, the sulphonamide was effective in displacing the antibiotic from its binding sites at the concentration 100–1000 μmol I−1.In vivo, both the serum and the tissue fluid concentration of free cephazolin increased significantly in rats concomitantly treated with sulp

ISSN:0142-2782    

DOI:10.1002/bdd.2510010307

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

AbstractThe pharmacokinetics of an intravenous injection of disopyramide was studied in five normal subjects and six patients with varying degrees of renal impairment. The elimination rate constant (β) was related to the endogenous creatinine clearance (Clcr). However, a decrease in β was not observed until the Clcrwas reduced below 40 ml min−1. Below 40 ml min−1a linear relationship existed between β and Clcr. Similarly, the plasma elimination half‐life (t½β) showed a significant increase when the Clcrwas less than 30 ml min−1. Hence, dosage modification for disopyramide is necessary only when renal function is severely impaired. Overall, the apparent volume of distribution in patients with renal insufficiency was reduced to two‐thirds of that in normal subjects. Therefore, in patients with Clcrless than 40 ml min−1both the loading and maintenance dose of disopyramide s

ISSN:0142-2782    

DOI:10.1002/bdd.2510010308

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

AbstractConcentrations of the vasodilator isosorbide dinitrate (ISDN) in human plasma can be measured with good sensitivity (about 0·2–0·5 ng ml−1) using electron‐capture gas chromatography after a one‐stage extraction. The mean recovery of ISDN from plasma was 83 per cent ± 9 standard deviation (S.D.). The precision of the method for the measurement of ISDN in plasma ranged from ± 14 per cent at 1 ng ml−1to ± 7 per cent at 5 ng ml−1to ± 4 per cent at 50 ng ml−1. The 95 per cent confidence limits of the least‐squares regression calibration line forced through the origin were ± 100 per cent at 1 ng ml−1, ± 11 per cent at 10 ng ml−1, and ± 8 per cent at 30 ng ml−1. The method has been used to assay many samples withdrawn after doses of drug at therape

ISSN:0142-2782    

DOI:10.1002/bdd.2510010309

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

AbstractPlasma concentrations of isosorbide dinitrate have been measured after intravenous infusion of drug at a rate of 5·0 mg h−1for 150 min and after single equal oral doses of 12·5 mg of drug in solution to two normal human subjects. During the infusion, uneven plateau concentrations were approached after 30 min. The calculated average steady‐state plasma levels were 258 ng ml−1and 514 ng ml−1in the two subjects respectively. The half‐life of elimination of isosorbide dinitrate after termination of the infusion was 9–10 min. After oral doses, peak plasma levels of 26·6 ng ml−1and 12·7 ng ml−1occurred at 10 min and 20 min in the two subjects respectively. The terminal half‐life of drug after the oral doses was much longer than the elimination half‐life (about 10 min), and was associated with the absorption phase. Fairly good agreement was obtained between the observed concentrations and those predicted by a one‐compartment open model.The systemic availability of isosorbide dinitrate after the oral doses was up to only 3 per cent of the equal doses infused, indicating that presystemic elimination processes accounted for very large proportions of the oral doses. The systemic clearances of drug after infusion of 0·32 1 min−1and 0·161 min−1were unexpectedly low for a drug of repor

ISSN:0142-2782    

DOI:10.1002/bdd.2510010310

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

ISSN:0142-2782    

DOI:10.1002/bdd.2510010311

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY