Earticle

Folates are involved in a variety of important biosynthesis by way of donating one carbon unit. Since folate metabolism was well understood a number of antifol have been developed. Among these antifols, aminopterin was first used in the treatment of childhood leukemia. However due to its toxicity and purity problems. it was immediately replaced by another antifols. methotrexate (MTX). MTX is shown to be active against various malignancies including leukemia breast cancer, osteogenic sarcoma, and head and neck cancer. Clinically, MTX therapy is divided into 3 categories. depeding on the dose administered; low-dose is defined as doses < intermediate-dose as doses and < and high-dose as doses . Leucovorin should be administered to minimize MTX toxicities when MTX doses are greater than . The clinical pharmacokinetics (ADME) of MTX is discussed in this text.

Inclusion complexes of piroxicam with were prepared and suspended to enhance the bioavailability of piroxicam. A quantitative analysis was employed HPLC for the determination of piroxicam in the rabbit serum after a single oral dose in suspension of piroxicam and each of inclusion complexes of piroxicam with , respectively. The bioavailability and serum level of piroxicam exhibited the highest in piroxicam clathrated than both piroxicam and the other complexes administered. and the total area under the curve of serum concentration versus time for their inclusion complexes were larger than that of piroxicam.

This study was attempted to investigate the dissolution rate and bioavailability of commercially available furosemide preparations. A. B. and C. The dissolution test was conducted in an artificial gastric juice using the basket method. and furosemide (40 mg) was administered orally to 8 normal volunteers by cross-over design. The results were as follows: the AUC and dissolution rate in 100 min () were higher in order of preparations. A > C > B. But the peak concentration. time to reach peak concentration , and mean dissolution time (MDT) were in order of preparations. C > A > B. There were significantly linear correlations between the AUC and the , and between the and the MDT. From the results of this experiment. it can be concluded that commercially available preparations bioavailability of furosemide, which may be predicted from the dissolution rate.

The sustained-release beads containing terbutaline sulfate (TBS) were prepared by rotogranulation method. The drug was dusted on the non-pareil seeds in a CF-granulator. The sustained-release beads were obtained by coating the active beads with ethylcellulose or , using in any case the same granulator employed for active beads preparation. The release characteristics of sustained-release beads were examined in vitro by rotating basket method applied to durules which is a sustained-release TBS matrix tablet. The release of terbutaline from the beads in vitro was first-order, and the release rate was dependent on both the coat weight ratio and membrane hydrophilicity. Both surfaces of the beads before and after dissolution were smooth. The drug release pattern from the beads could be thought the diffusion through the polymer membrane. The release rate and the surface of the beads stored for 3 years at room temperature were the same with those of the initial beads.

Tobramycin is one of the most frequently selected agents for pharmacokinetic drug monitoring because of its narrow therapeutic index and essential role for the management of serious infections, especially gram-negative infections. Its pharmacokinetic parameters are dependent on race, sex, age, ideal body weight. disease states, and etc. Therefore, to schedule the dosing of tobramycin, the individual pharmacokinetic parameters such as half-life and volume of distribution are needed. However, these pharmacokinetic parameters have never been reported in Koreans. The purposes of this study were to evaluate the volume of distribution of tobramycin in cancer patients who had normal renal function, to compare the mean values of Vd reported in the literature, and to compare the measured half-life with the expected half-life based on ABW, LBW, and IBW, respectively. Venous blood samples were collected just before and thirty minutes after dosing during steady state. Serum tobramycin concentrations were determined by (fluorescence immunoassay). IBW were measured by the method of Devine: and LBW were measured by the method of Hallynck. Creatinine clearances (CLcr) of the patients were estimated using the Cockcroft and Gault equation. Elimination rate constants (kel) were determined using the Welling and Craig equation. Infusion rate (ko), volume of distribution (Vd), and half-life were determined using the Saw chuk and Zaske equation. The volume of distribution Was greater than the Schentag's study (0.26 vs 0.33 l/kg), but the half-life was similar to the Levy's study. The predicted half-lives based on IBW were the closest to actual half-lives (1.85 vs 2.01 hr).