OBJECTIVETo investigate the distribution of antimicrobial agent STR-1 of nanometer level which was incorporated with ball-grinding method in the polymethylmethacrylate (PMMA) denture base, and to study the release mode of silver ions from the base.

METHODSThe distribution of the antimicrobial agent in the PMMA denture base containing STR-1 at concentrations of 0 g/L, 5 g/L, and 10 g/L was examined with scanning electronic microscopy. Then, PMMA resin bases containing STR-1 at the three concentrations were respectively immersed in artificial saliva at 37 degrees C for 54 days. The release of silver ions from the resin bases was surveyed with inductively coupled plasma-mass spectroscopy (ICP-MS) every 24 hours.

RESULTSThe antimicrobial agent incorporated by ball-grinding method was even-distributed with individual particles of nanometer level in the PMMA resin base. The release of silver ions from the PMMA resin with antimicrobial agent was extremely slow during the test, a very small fraction of the silver ions released. At the beginning of the test, the release speed was extremely slow, the speed increased rapidly in the middle of the test, and at the end of the test, the speed returned to slow and steady. The cumulative release curve of silver ions was of "S" type.

CONCLUSIONSSTR-1 can be even-distributed in the denture base, and the silver ions release from the base with extremely slow speed. It also indicates that biological safety and long-term antimicrobial efficacy of denture base containing silver-supported antimicrobial agents of nanometer level are possibly obtained based on their slow release of silver ions.

Anti-Infective Agents ; pharmacokinetics ; Dental Materials ; chemistry ; Denture Bases ; Denture, Partial ; Ions ; pharmacokinetics ; Materials Testing ; Nanostructures ; Polymethyl Methacrylate ; chemistry ; Silver ; pharmacokinetics

BACKGROUND: Interest in pharmacist participation in the multidisciplinary intensive care team is increasing. However, studies examining pharmacist interventions in the medical intensive care unit (MICU) are limited in Korea. The aim of this study was to describe the current status of pharmacist interventions and to identify common pharmacologic problems requiring pharmacist intervention in the MICU. METHODS: Between September 2013 and August 2014, a retrospective, observational study was conducted in the 22-bed MICU at a university hospital. Data were obtained from two trained pharmacists who participated in MICU rounds three times a week. In addition to patient characteristics, data on the cause, type, related drug, and acceptance rate of interventions were collected. RESULTS: In 340 patients, a total of 1211 pharmacologic interventions were performed. The majority of pharmacologic interventions were suggested by pharmacists at multidisciplinary rounds in the MICU. The most common pharmacologic interventions were adjustment of dosage and administration (n = 328, 26.0%), followed by parenteral/enteral nutritional support (n = 228, 18.1%), the provision of drug information (n = 228, 18.1%), and advice regarding pharmacokinetics (n = 118, 9.3%). Antimicrobial agents (n = 516, 42.6%) were the most frequent type of drug associated with pharmacist interventions. The acceptance rate of interventions was 84.1% with most accepted by physicians within 24 hours (n = 602, 92.8%). CONCLUSIONS: Medication and nutritional problems are frequently encountered pharmacotherapeutic problems in the MICU. Pharmacist interventions play an important role in the management of these problems.
Anti-Infective Agents ; Humans ; Critical Care ; Intensive Care Units* ; Korea ; Nutritional Support ; Observational Study ; Pharmacists* ; Pharmacokinetics ; Retrospective Studies

BACKGROUND: Interest in pharmacist participation in the multidisciplinary intensive care team is increasing. However, studies examining pharmacist interventions in the medical intensive care unit (MICU) are limited in Korea. The aim of this study was to describe the current status of pharmacist interventions and to identify common pharmacologic problems requiring pharmacist intervention in the MICU. METHODS: Between September 2013 and August 2014, a retrospective, observational study was conducted in the 22-bed MICU at a university hospital. Data were obtained from two trained pharmacists who participated in MICU rounds three times a week. In addition to patient characteristics, data on the cause, type, related drug, and acceptance rate of interventions were collected. RESULTS: In 340 patients, a total of 1211 pharmacologic interventions were performed. The majority of pharmacologic interventions were suggested by pharmacists at multidisciplinary rounds in the MICU. The most common pharmacologic interventions were adjustment of dosage and administration (n = 328, 26.0%), followed by parenteral/enteral nutritional support (n = 228, 18.1%), the provision of drug information (n = 228, 18.1%), and advice regarding pharmacokinetics (n = 118, 9.3%). Antimicrobial agents (n = 516, 42.6%) were the most frequent type of drug associated with pharmacist interventions. The acceptance rate of interventions was 84.1% with most accepted by physicians within 24 hours (n = 602, 92.8%). CONCLUSIONS: Medication and nutritional problems are frequently encountered pharmacotherapeutic problems in the MICU. Pharmacist interventions play an important role in the management of these problems.
Anti-Infective Agents ; Humans ; Critical Care ; Intensive Care Units ; Korea ; Nutritional Support ; Observational Study ; Pharmacists ; Pharmacokinetics ; Retrospective Studies

BACKGROUNDBacterial infection can pose a substantial diagnostic dilemma. (99m)Tc-labeled ciprofloxacin (CPF) was developed as a biologically active radiopharmaceutical to diagnose infection. In the present research, we studied the biodistribution and imaging properties of infection tracer (99m)Tc-CPF in a mouse model of infection.

METHODSCPF was labeled with (99m)Tc and the radiochemical purity and labeling rate were measured. A mouse model of infection was established. We then determined the biodistribution of (99m)Tc-CPF and conducted the whole body scintigraphy of the animal model.

RESULTS(99m)Tc-Ciprotech was stable for at least 6 hours at room temperature. The labeling rate of CPF by (99m)Tc was over 90%. Clearance of radioactivity mainly occurred in the liver and kidney, and the clearance from blood was rapid. Both biodistribution and imaging results showed higher uptake of (99m)Tc-CPF at sites of infection. The infectious tissue/normal tissue ratio peak was 4.30 at 4 hours after injection.

CONCLUSIONS(99m)Tc-CPF is a sensitive radiopharmaceutical for scintigraphy of infectious lesions and it is easy to prepare.

Animals ; Anti-Infective Agents ; chemistry ; pharmacokinetics ; Bacterial Infections ; diagnosis ; Ciprofloxacin ; chemistry ; pharmacokinetics ; Disease Models, Animal ; Isotope Labeling ; methods ; Mice ; Mice, Inbred BALB C ; Organotechnetium Compounds ; chemistry ; Tissue Distribution

Ofloxacin was administered to six male goats intravenously (5 mg/kg) to determine its kinetic behavior, tissue residue, in vitro plasma protein binding and to compute a rational dosage regimen. The concentration of ofloxacin in plasma and tissue samples collected at prescheduled time were estimated by using HPLC. The pharmacokinetic parameters were determined by non-compartmental model and plasma protein binding was estimated by equilibrium dialysis technique. The therapeutic concentration (> or = 0.5 microgram/ml) was maintained up to 36 h and the initial concentration at 2.5min (14.76 +/- 0.47 microgram/ml) declined to 0.05 +/- 0.03 microgram/ml at 96 h with a secondary peak (0.64 +/- 0.15 microgram/ml) at 24 h. The mean AUC, AUMC, t1/2, MRT, Cl and Vd were calculated to be 58.94 +/- 19.43 microgram h/ml, 1539.57 +/- 724.69 microgram h2/ml, 15.58 +/- 1.87 h, 22.46 +/- 2.71 h, 135.60 +/- 31.12 ml/h/kg and 2.85 +/- 0.74 L/kg respectively. Significantly high concentration of drug was detected in different tissues after 24 h of intravenous dosing of 5mg/kg, at 24 h interval for 5 days. The in vitro plasma protein binding of ofloxacin was found to be 15.28 +/- 0.94%. Based on these kinetic parameters, a loading dose of 5mg/kg followed by the maintenance dose of 3mg/kg at 24 h dosing interval by intravenous route is recommended.
Animals ; Anti-Infective Agents/*pharmacokinetics ; Blood Proteins/*metabolism ; Chromatography, High Pressure Liquid/veterinary ; Goats/*metabolism ; Male ; Ofloxacin/*pharmacokinetics ; Protein Binding ; Tissue Distribution

AIMTo develop a sensitive and rapid HPLC method for the determination of tanshinone IIA (TS) in rat plasma and to study its pharmacokinetics in rats.

METHODSTS and 4-chlorodiphenyl (internal standard) were extracted from plasma with ethyl acetate. After liquid-liquid extraction, the sample was analyzed by HPLC with YMC C18 column (5 microns, 150 mm x 3.0 mm ID). The mobile phase consisted of acetontrile-water-acetic acid (74:26:1) at the flow rate of 0.3 mL.min-1, the UV detection wave length was 270 nm.

RESULTSThe calibration curve was linear (r = 0.9981) in the range from 0.05 to 6.40 mg.L-1. The lowest detectable concentration was 0.05 mg.L-1. The recoveries at the concentration of 0.05, 1.60 and 6.40 mg.L-1 were 98.9%, 102.1% and 100.4%, respectively. The inter- and intra-day RSDs were all less than 5%.

CONCLUSIONThis method is proved to be rapid, precise and reliable enough to be applied to the pharmacokinetics studies of TS in rats after a single dose of 15 mg.kg-1 by oral administration.

Animals ; Anti-Infective Agents ; blood ; pharmacokinetics ; Area Under Curve ; Chromatography, High Pressure Liquid ; methods ; Diterpenes, Abietane ; Drug Stability ; Male ; Phenanthrenes ; blood ; pharmacokinetics ; Random Allocation ; Rats ; Rats, Sprague-Dawley

AIMTo establish a method for determineation of the concentration of ofloxacin in human fallopian tube, uterus and serum.

METHODSThe separation was performed on a Spherisob C18 column (Hypersil, 250 mm x 4.6 mm ID, 5 microns) with a mobile phase of acetonitrile-0.01 moL.L-1 potassium dihydrogen phosphate-0.5 mol.L-1 tetrabutylammonium bromide (9:91:4, pH 2.5). The flow rate was 1.0 mL.min-1 and detection was at 294 nm. The samples were homogenated or ground to powder after freezing with liquid nitrogen. 1% triton-100 and certain volume of ethylacetate-isopropanol (10:1) were added, shaken and centrifuged. Then the entire organic layer was transferred to a tube and vacuum dried. The residue was reconstituted in the mobile phase for HPLC.

RESULTSThere was a linear relationship between the peak area ratio and the ofloxacin concentration over the range of 0.2-8.0 micrograms.mL-1. The limits of detection was 40 ng.mL-1. Using this method to determine the ofloxacin concentrations in relevant organs as well as in the plasma of patients of the Department of Gynecology, and achieved satisfactary results.

CONCLUSIONThe method can be applied to assay the ofloxacin concentration in human tissues. Ofloxacin was well distributed in woman fallopian tube, uterus and serum after single oral administration.

Adolescent ; Adult ; Anti-Infective Agents ; analysis ; pharmacokinetics ; Chromatography, High Pressure Liquid ; Fallopian Tubes ; metabolism ; Female ; Humans ; Ofloxacin ; analysis ; blood ; pharmacokinetics ; Tissue Distribution ; Uterus ; metabolism

OBJECTIVETo prepare the controlled-release delivery gutta-percha points containing metronidazole compound (CDGMC) and to determine its release rate in vitro.

METHODSThe drug points were made by using compound drugs and gutta-percha as a carrier, and CDGMC were prepared followed by enveloping a release membrane outward. The best formula was selected according to the release parameters of the drugs extracted in the release experiments in vitro. The CDGMC were placed into the extracted teeth after root canals were routinely prepared. The non-drug CDGMC was used as the control. The absorbency of the drugs in normal saline (37 degrees C, pH 7.4) was determined timely. The percentage of release and cumulated release of the drugs were calculated according to the concentrations of drugs in medium.

RESULTSThe in vitro experiments showed that this system contained 1,880 micrograms of metronidazole and 267 micrograms of ciprofloxacin. The experiments in healthy single root canal showed that the drug release amounts around the perioapical area were metronidazole 88.54 micrograms/ml and ciprofloxacin 9.05 micrograms/ml in 10 days.

CONCLUSIONCDGMC can continuously release effective drug concentrations more than 10 days and could be considered as an ideal method for clinical application.

Anti-Infective Agents, Local ; administration & dosage ; pharmacokinetics ; Ciprofloxacin ; administration & dosage ; pharmacokinetics ; Delayed-Action Preparations ; chemical synthesis ; pharmacokinetics ; Dental Pulp Cavity ; drug effects ; metabolism ; Drug Delivery Systems ; Gutta-Percha ; Humans ; Metronidazole ; administration & dosage ; pharmacokinetics ; Root Canal Therapy ; methods

The present study is aimed to investigate the in vitro metabolic interconversion between baicalin (BG) and baicalein (B) in rat liver, kidney, intestine and bladder. BG and B were separately incubated with rat hepatic, renal, and intestinal microsomes, as well as bladder homogenates, for 30 min. The metabolites were identified and quantified by HPLC and metabolic kinetic parameters were obtained by fitting the data to the Michaelis-Menten equation. In hepatic microsomes, renal microsomes and bladder homogenates, but not in intestinal microsomes, BG was transformed into B, the hydrolysis metabolite of BG, with K(m) values being (44.65 +/- 6.01), (92.73 +/- 11.41), (74.60 +/- 3.68) micromol x L(-1), respectively, and V(max) values being (12.32 +/- 0.56), (3.30 +/- 0.18), (5.93 +/- 0.12) micromol x min(-1) x g(-1) (protein), respectively. In incubations with hepatic, renal, and intestinal microsomes and bladder homogenates, B was also transformed into BG, the glucuronidation metabolite of B, with K(m) values being (67.46 +/- 10.49), (226.7 +/- 71.59), (177.3 +/- 35.85), and (18.33 +/- 2.53) micromol x L(-1), respectively, and V(max) values being (14.74 +/- 0.97), (5.91 +/- 1.03), (38.14 +/- 3.60), and (1.22 +/- 0.05) micromol x min(-1) x g(-1) (protein), respectively. The results showed that the activity of UDP-glucuronosyltranferase (UGT) in intestinal microsomes was the highest among the four organs, and the activities of UGT were higher than that of glucuronidase (GUS) in hepatic, renal and intestinal microsomes, but the activity of GUS was higher than that of UGT in bladder homogenates.
Animals ; Anti-Infective Agents ; pharmacokinetics ; Antioxidants ; pharmacokinetics ; Biotransformation ; Flavanones ; pharmacokinetics ; Flavonoids ; pharmacokinetics ; Glucuronidase ; metabolism ; Glucuronosyltransferase ; metabolism ; Hydrolysis ; Intestines ; enzymology ; metabolism ; Kidney ; enzymology ; metabolism ; Liver ; enzymology ; metabolism ; Male ; Microsomes ; enzymology ; metabolism ; Rats ; Rats, Sprague-Dawley ; Urinary Bladder ; enzymology ; metabolism

Cymbopogon citratus is a widely distributed perennial herb belonging to the Poaceae family and has been extensively consumed for its medicinal, cosmetic, and nutritional effects for centuries. A large number of reports have been published describing the pharmacological, biological, and therapeutic actions of this herb. In this review, we summarized the literatures on related studies (up to January, 2014) that highlighted the pharmacologic and biological effects of the major phytochemicals isolated from C. citratus extracts and its essential oil. The components of the essential oils found in C. citratus have a similar pharmacokinetic properties, including absorption, distribution, metabolism, and excretion. They are quickly absorbed following oral, pulmonary, and dermal administration. Based on the published reports, it can also be inferred that, after absorption from the small intestine, some phytochemicals in C. citratus can undergo oxidation, glucuronidation, sulfation, and/or O-methylation. Excretion is through urine, feces and/or expired volatiles. The biotransformation reactions of C. citratus bioactive constituents are essential for its relatively safe consumption and therapeutic applications. The data available so far warrant further studies evaluating C. citratus pharmacokinetics. Reliable pharmacokinetic data in humans would be critical for a better understanding of the the systemic handling of C. citratus.
Animals ; Anti-Infective Agents ; pharmacokinetics ; pharmacology ; therapeutic use ; Anti-Inflammatory Agents ; pharmacokinetics ; pharmacology ; therapeutic use ; Anti-Obesity Agents ; pharmacokinetics ; pharmacology ; therapeutic use ; Antineoplastic Agents ; pharmacokinetics ; pharmacology ; therapeutic use ; Antioxidants ; pharmacokinetics ; pharmacology ; therapeutic use ; Central Nervous System Agents ; pharmacokinetics ; pharmacology ; therapeutic use ; Cymbopogon ; Ethnopharmacology ; Hematologic Agents ; pharmacokinetics ; pharmacology ; therapeutic use ; Humans ; Hypoglycemic Agents ; pharmacokinetics ; pharmacology ; therapeutic use ; Male ; Mice ; Oils, Volatile ; pharmacokinetics ; pharmacology ; therapeutic use ; Plant Extracts ; pharmacokinetics ; pharmacology ; therapeutic use ; Plant Oils ; pharmacokinetics ; pharmacology ; therapeutic use ; Rats, Inbred F344 ; Urological Agents ; pharmacokinetics ; pharmacology ; therapeutic use