Dissolution characteristics of indomethacin (IMC) from hydrophobic polymer solid dispersions were investigated. IMC-polyvinyl chloride (PVC) and IMC-ethylcellulose (EC) solid dispersions were prepared. The dissolution patterns of pure IMC, IMC-PVC and IMC-EC solid dispersions prepared at various ratios (1:1, 1:3, 1:5, 1:9 and 1:19 w/w), and those of corresponding physical mixtures were compared. It was found that the dissolution rates of IMC from solid dispersions with PVC or EC decreased in the order of 1:1>1:3>1:5>1:9>1:19 as the drug to polymer ratios decreased. Also the dissolution rates of IMC from EC solid dispersions increased according to flow rate, but PVC solid dispersions were not affected significantly. After all, PVC and EC matrices could be applied in sustained-release preparation of IMC.

Complex formation of water-soluble polyparacyclophanes bearing two diphenylmethane or two diphenyl ether skeletons with l-anilinonaphthalene-8-sulfonate (ANS) and 2-p-toluidinylnaphthalene-6-sulfonate (TNS) was investigated quantitatively to develop useful host compounds comparing with in aqueous solution. Benesi-Hildebrand type analysis of the fluorescent intensity showed that the dissociation constants (Kd) of paracyclophane-ANS complexes were for 1,6,20,25-tetraaza[6.1.6.1]paracyclophane(CPM 44) and for 1,7,21,27-tetraaza[7.1.7.1]paracyclophane (CPM 55), and those of paracyclophane-TNS complexes were for CPM 44 and for CPM 55, in 1:1 molar ratio. On the other hand, the Kd values of 1,7,21,27-tetraaza-14,34-dioxa[7.1.7.1]paracyclophane (CPE 55)-ANS, 1,8,22,29-tetraaza-15,36-dioxa[8.1.8.1]paracyclophane (CPE 66)-ANS, CPE 55-TNS, CPE 66-TNS complexes were , , and , respectively. On the contrary, the Kd values of , , and complexes were found to be , , and , respectively. These results mean that the complexation of CPMs with ANS or TNS is by 5.6-1,975 fold stronger than that for , and the complex formation of CPEs with ANS or TNS is nearly same as or somewhat stronger than that for . From the Kd values determined at different temperatures, thermodynamic parameters were calculated and the complexation was found to be a spontaneous exothermic reaction. The effects of pH on Kd values of CPM 44-ANS, and CPM 55-ANS complexes were negligible in the range of pH 1.2-1.8. However, the Kd values of these complexes increased significantly with increasing ionic strength.

The proteolytic enzyme extracted from Neungee [Sarcodon aspratus (Berk.) S. Ito] was purified by using Tris-acryl CM-cellulose column chromatography and chromatofocusing. The specific activity of the purified enzyme increased 15.8 times as compared with that of the crude enzyme. The enzyme was homogeneous on polyacrylamide gel electrophoresis and stable at pH values ranging from 4.0 to 10.8. The enzyme activity remained unchanged when the mushroom and the purified enzyme were stored for 3 years and 6 months at 4°C, respectively. The enzyme was found to be an endogeneous protease.

The multilayered monolithic type transdermal delivery device has been designed and analyzed by a numerical analysis. The device consists of three layered polymer matrices which posess the different diffusion parameters, respectively. The purpose of this study was to design an ideal transdermal drug delivery device which is capable of initial burst and zero order release later on. Numerical modelings were simulated for a dispersed and a dissolved multilayered monolithic system. The results showed that the dispersed multilayered monolithic system could meet the requirements for an ideal transdermal delivery device.

The study was performed to compare the dissolution, diffusion and absorption characteristics using Sartorius dissolution and absorption simulator and in vivo bioavailability of commercially available rifampicin capsules. Both brands C and F showed similar dissolution patterns and absorption properties through artificial gastric barrier in Sartorius simulator. Diffusion rate constants through the membrane of brands C and F were and , respectively. Rifampicin capsules were administered orally to six fasted healthy volunteers according to cross-over design. The pharmacokinetic parameters between brands C and F, maximum plasma drug concentration, the time to reach , absorption rate constant and area under the curve , elimination rate constant, and amount of drug excreted in urine were 6.11 and , 2.71 and 1.52 hr, 0.6371 and , 57.84 and , 0.1891 and , 119.98 and 119.93 mg, respectively. On the basis of experimental results, it was concluded that the bioavailability of brand C rifampicin capsules was almost the same as that of brand F rifampicin capsules.

In order to develop a pediatric liquid preparation with sustained release properties, dextromethorphan hydrobromide (DEXT) was complexed with strong cation exchange resin (CG 120) and the-complex was coated with Eudragit RS using a phase separation method by non-solvent addition. The effect of pH, ionic strength of the release medium and drug/resin ratio on the release rate of DEXT was studied. The release rate of free drug from the uncoated complex, and coated complexes with 9.5 and 18.5% Eudragit RS in artificial gastric juice were measured. The release rate from the uncoated complex was faster with higher pH, higher ionic strength of the release medium and higher drug/resin ratio. The release rate from the coated complex could be controlled by the amount of coating material, and the surface after release did not rupture into.

Solid dispersion of fenticonazole nitrate (FN) with poloxamer 407, polyethylene glycol 6000, povidone (K-90) were prepared by the solvent method. To characterize the state of the drug in solid dispersions, the x-ray diffractometry and differential scanning calorimetry were carried out. The identification of these systems suggested that FN in the poloxamer 407 system remained in crystalline state, and the drug in the PVP system was amorphous. A marked increase in the dissolution rate of FN was attained by dispersing the drug in the hydrophilic polymers used, and the dispersion with poloxamer 407 was superior to the other two carriers in releasing the drug into solution.