No abstract available.
Pharmacokinetics*

No abstract available.
Nortriptyline* ; Pharmacokinetics*

No abstract available.
Humans* ; Pharmacokinetics*

The aim of this research is to investigate the mechanism and kinetics of drug release from the core and coated pellets containing sodium diclofenac. Avicel was found to be a good excipient to prepare matrix-type pellets. The drug release could be sustained up to 12 hours. the rate of drug release was fit to Higuchi's model. The microphotograph revealed that the drug release was controlled by the diffusion from the isoluble matrix. The drug release was sustained up to 24 hours. The rate of drug release was fit to Higuchi's model, too. The mechanism of drug release was determined to be the diffusion from insoluble matrix and through the insoluble membrane.
Diclofenac ; Pharmacokinetics

The study was carried out on 30 healthy volunteers (16 males, 14 females), aged 21-40. Cyclosporine A (CsA), Neoral®, dosage of 2 mg/kg body weight (rounded nearest to 25 mg), was given at hours as 0 (starting time), 12, and 24. The blood samples were collected at hours 0, 2, 4, 6, 8, 12 (before the 2nd dose), 24 (before the 3rd dose) and 36. The CsA concentrations were measured with fluorescence polarization immunoassay (FPIA) with the TDx analyser, Abbott. Results: Pharmacokinetics of CsA, oral micro-emulsion, in Vietnamese volunteers have the characteristics: Cmax = 763 ± 241 ng/ml, Cmin = 358 ± 104 mg/ml/mg/kg, tmax = 2.3 ± 1.1 h, AUC 0-4 = 1756 ± 561 ng.h/ml, AUC0-4 /dose/kg = 827 ± 250 ng.h/ml/mg/kg, AUCinf = 3725 ± 983 ng.h/ml, AUCinf/dose/kg = 1756 ± 433 ng.h/ml/mg/kg, t1/2 = 4.1 ± 1.2, Cl/F = 30.5 ± 6.9 L/h. The inter-individual variation in pharmacokinetics is presented with the coefficient of variations (CVs) of Cmax, AUC 0-4, AUCinf as 31.6%, 31.9% and 26.4%, respectively. The concentration of C2 has an important linear relationship with AUC0-4 (r = 9.987, p <0.0005), inversely there is no linear relation between C12 (the trough C0: before 2nd dose of CsA) (r = -0.189, p= 0.32). Cmax/dose/kg, AUC0-4/dose/kg and AUCinf/dose/kg in female volunteers were lower than those in male volunteers (p<0.005)
Pharmacokinetics ; Cyclosporine

This study introduced Macrolid antibiotic class including effects, classification, pharmacokinetics, indication of treatment, and future prospects
Macrolides ; Pharmacokinetics

OBJECTIVETo investigate the relationship of properties and drug release rate of hot melt pressure sensitive adhesive (HMPSA), and to provide a recommendation of preparing and selecting of HMPSA for transdermal use.

METHODHMPSA with different properties were prepared using styrene-isoprene-styrene triblock copolymer as main material, and the tacks, adhesions and cohesions were determined. Drug-in-adhesive type patches were prepared using alpha-asarone as model drug, and the drug release rates were investigated on single chamber diffusion cells using 60% ethanol solution as release media.

RESULTThe prepared HMPSAs had different tacks, adhesions and cohesions. The drug release rates of HMPSA patches were related to the cohesions. The release rate decreased when the cohesion increased.

CONCLUSIONThe HMPSA with appropriate cohesion should be selected when preparing patches to balance the drug release rate and patch property.

Ganoderic acid(GA) is one of main bioactive components produced by Ganoderma lucidum,which a traditional Chinese herbal medicine and a kind of tracyclic triterpene lanosterol derivatives with highly oxidized structure. It has a variety of important pharmacological activities,such as anticancer,immunoregulation,anti-oxidation,anti-diabetes and anti-HIV. At present,the studies of GA mainly focus on biosynthesis,fermentation control,isolation and purification,structure identification and pharmacological effects.However,there are a fewer pharmacokinetic studies of GA,although it is closely related to the clinical application. Recent studies have shown that GA can be absorbed rapidly by gastrointestinal tract and distributed in various tissues and organs after oral intake. GA is metabolized by liver at phase Ⅰ and phase Ⅱ,and then mainly excreted by bile. In this paper,the pharmacokinetic characteristics of GA and its absorption,distribution,metabolism and excretion(ADME) will be systematically summarized,in order to provide scientific basis for the application and development studies of Ganoderma triterpenoid drugs and their rational clinical use.
Humans ; Lanosterol ; pharmacokinetics ; Reishi ; chemistry ; Triterpenes ; pharmacokinetics

BACKGROUNDPrevious studies have suggested that nomogram can simplize complicated calculations of several variables. A simple nomogram was constructed to estimate absorption rate coefficient (k(a)) by using the peak time (tpeak) and the elimination rate coefficient (k(e)) of drugs administered orally.

METHODSThe nomogram was based on the plasma concentration-time (C-T) curve equation and the function relation between t(peak), k(a) and k(e). A mathematical analysis was presented for the construction of single chart nomogram. To check the degree of accuracy of the developed nomogram, we used it to analyze retrospective profiles of 46 drugs and compared the ka values obtained graphically and those calculated by numerically solving the descriptive equation. In addition, we measured the carbocisteine concentration of 18 healthy volunteers by HPLC with fluorescence detection. To analyze performance error, the measured carbocisteine concentrations were compared with predicted concentrations by the ka obtained from the nomograms along with the other pharmacokinetic parameters.

RESULTSThe estimated of k(a) values from nomograms were in very close proximity with the numerical values. The performance error was as follows: median performance error (MDPE) and median absolute performance error (MDAPE) were 1.32% and 18.15%, respectively.

CONCLUSIONSThe developed nomogram is accurate and reliable. The size of performance error meets the demand of clinical pharmacokinetics. Therefore, the nomograms can offer another convenient and easy method for rational individualized dosage regimens.

A sensitive liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was applied for the quantification of each component: tetrahydropalmatine (THP), dehydrocorydaline (DHC), salvianolic acid B (SAB), ginsenoside Rg1, Re, Rb1 and Rd in the Chinese herbal component SSTG (Shuangshentongguan) with different combinations. The pharmacokinetic data were analyzed with WinNonlin 5.2 software. The results showed that combination can increase the THP AUC value while the AUC values of SAB, ginsenoside Rg1, Re, Rb1 and Rd were reduced. These results showed significant differences. The AUC value of ginsenoside Rb1 was increased when combined with Danshen or Yanhusuo, but reduced when combined with Danshen and Yanhusuo. The DHC concentration in serum was too low to be determined.
Benzofurans ; pharmacokinetics ; Drug Combinations ; Drugs, Chinese Herbal ; pharmacokinetics ; Ginsenosides ; pharmacokinetics ; Phenanthrolines ; pharmacokinetics