In order to clarify mechanism of the formation of cinnamaldehyde (CNA) in incubation mixtures of tranylcypromine (TCP) with rat liver microsomes, the CNA formed under various incubation conditions were analyzed. For the purpose, HPLC method of the analysis of CNA was developed. The formation of CNA was found to be dependent on the incubation time and the amounts of microsomes added. In addition, exclusion of NADPH or NADP of NADPH-generating system in incubation mixtures resulted in the formation of markedly decreased amounts of CNA to 8.5 and 2.4%, respectively, relative to the amounts formed each in a standard system. The small amounts measured were comparable to those formed by incubation without microsomes or with boiled microsomes. The results clearly suggested that CNA is a metabolic product of TCP by rat liver microsomes though further studies are needed to suggest details of the steps to the formation of CNA from TCP and of the enzymatic entities involved in the formation of CNA.

An oral adhesive tablet of acyclorir [9-(2-hydroxyethoxymethyl) guanine] for herpetic stomatitis was prepared and its physical properties were evaluated. 300 mg weighed tablets containing 30 mg of acyclovir were prepared with six kinds of polymers from direct compression, and the stickiness, fracture resistance and dissolution in pH 6.8 buffer solution were tested. HPMC and MC showed good stickiness and fracture resistance, and their dissolution rates were significantly different from each other. Three factors-HPMC:MC ratio, acyclovir content, compression force-were chosen as an important factor of manufacture and factorial analyses for these three factors were carried out. Eight kinds of formulations from different combination of three factors were prepared and tested in stickiness, fracture resistance and dissolution in pH 6.8 buffer solution. Dissolution rate was significantly affected by polymer ratio, fracture resistance was affected by compression force, and stickiness was not significantly affected by acyclovir content and polymer ratio.

An automated, simple, and reliable method was developed for determining in vitro drug release rate from transdermal delivery dosage forms. The patch is held in position in the heating block by sandwiching it between the middle plate and the bottom plate of diffusion cell. The dissolution profile of the commercially available transdermal scopolamine patch was determined over a 72-h period, and the results were compared with those obtained with other methods; paddle-over-disk method, reciprocating method, and diffusion cell method. It was demonstrated that the flow-through method is equivalent in terms of release rate profile and accumulated released drug amount over the lifetime of the dosage form tested. Also this method is simple, reliable and reproducible. Therefore, this technique can be used in a quality control for assuring product uniformity.

An efficient synthetic route to macrolide is described. Eight-membered lactone was synthesized via palladium catalyzed intramolecular alkylation of allylic carbonate in high yield.

The recombinant gamma-interferon (LBD-001) which was produced by yeast as host system was investigated on the pharmacological activities. This gamma-interferon exhibited potent inhibitory effect on adjuvant induced arthritis, but no effect on carrageenin induced paw edema in rats. It did not show any sedative, anticonvulsive, analgesic and hypothermic activities in animals. It also had no influences on isolated tracheal muscle and ileum of guinea pig, isolated uterus and fundus strip of rats, and on blood pressure and respiration in situ experiments of rabbits.

A comparison was made of the effects of selective ${\alpha_1}-adrenoceptor$ agonist phenylephrine and selective ${\alpha_2}-adrenoceptor$ agonist clonidine on endothelium-containing and endothelium-denuded rings of the rat aorta. In the case of phenylephrine, removal of endothelium increased sensitivity 2.5 fold at $EC_{50}$ level and maximum contractive response 1.4 fold. In the case of clonidine, which gave only 15% of maximum contractive response given to phenylephrine on endothelium-containing rings, removal of the endothelium increased sensitivity 5.6 fold at $EC_{50}$ level and maximum contractive response 5 fold, which was about 55% of that given by phenylephrine. In endothelium-denuded ring, phenylephrine-induced contraction tended to be more increased in tonic contraction than in phasic contraction as compared to that in endothelium-containing ring, while clonidine-induced contraction was monophasic and was increased only in tonic contraction. In the calcium-free solution or in the presence, of verapamil, contraction stimulated by clonidine was almost abolished while that stimulated by phenylephrine produced only phasic contraction. The depression of sensitivity to these agonists in rings with endothelium appeared to be due to the vasodepressor action of endothelium derived relaxing factor (EDRF), because hemoglobin, a specific blocking agent of EDRF, abolished this depression. It is unlikely that the endothelium-dependent relaxation was due to stimulation of release of EDRF, because clonidine did not produce endothelium-dependent relaxation in 5-hydroxytryptamine-precontracted ring even when its contractile action was blocked by the ${\alpha_1}-adrenoceptor$ antagonist, prazosin. When the efficacy of phenylephrine was reduced to about the initial efficacy of clonidine by pretreatment with dibenamine, the contraction-response curves for phenylephrine became very similar to the corresponding curves obtained for clonidine before receptor inactivation. In the dibenamine-treated rings, contraction of phenylephrine was abolished in calcium-free solution or in the presence of verapamil like that obtained for clonidine before receptor inactivation. These results suggest that EDRF spontaneously released from endothelium depress contraction more profoundly in a case of an agonist with low efficacy and the phenylephrine-induced contraction was totally dependent on extracellular calcium as was that obtained for clonidine when the efficacy of phenylephrine was reduced to that of clonidine by irreversible inactivation of ${\alpha_1}-adrenoceptor$ with dibenamine.

Three sugar glass dispersions of sulfamerazine were prepared using dextrose, galactose and sucrose as the carriers, with the ratio of the drug to the carrier was 1:9. The chemical stability of sulfamerazine in the glass dispersion system was studied using TLC. TLC revealed no additional spot and there was good correspondence with the Sulfamerazine itself. While time required to dissolve 50%($T_{50%}$) of sulfamerazine powder was 390 min that of dextrose glass dispersion system was 1.5 min. and galactose system was 4.0 min. in distilled water. 23) $T_{50%}$ of physical mixture with dextrose, galactose and sucrose were 26.4 min., 26.5 min., and 26.0 min. respectively in distilled water. $T_{50%}$ of control was 54 min. and those of all of the glass dispersion systems were within 1 min. in 0.1N HCl. The dissolution rates of sulfamerazine from sugar glass dispersion system in distilled water was greater than that in 0.1N HCl.

Microencapsulation of nalidixic acid using Eudragit RL, a methacrylic acid copolymer was investigated. Microcapsules were prepared by dispersing the drug solution in liquid paraffing using aluminium tristearate as dispersing agent. The preparation of the microcapsules showed high reprodulibility in particle size, shape and the drug content. The dissolution rates of Nalidixic acid from the these microcapsules considerably decreased as compared with that from Nalidixic acid powder and Nalidixic acid-Eudragit RL solid dispersions. The release of Nalidixic acid increased with increasing percentage of aluminium tristearate added to the microcapsules.

Total suspended particles were collected and size-fractionated by an Andersen high-volume air sampler at Chungang University located near the Han River, Seoul, Korea, during the period form March, 1986 to August, 1986 and from March, 1987 to February, 1988. The concentrations and the particle size distributions of anions such as chloride, nitrate and sulfate were determined by ion chromatography. The averages of concentrations were $125.43\;{\mu}g/m^3$ in 1986 and $189.19\;{\mu}g/m^3$ in 1987 for total suspended particles (TSP), $2.12\;{\mu}g/m^3$ in 1986 and $4.14\;{\mu}g/m^3$ in 1987 for chloride, $4.39\;{\mu}g/m^3$ in 1986 and $5.95\;{\mu}g/m^3$ in 1987 for nitrate and $11.98\;{\mu}g/m^3$ in 1986 and $19.29\;{\mu}g/m^3$ in 1987 for sulfate. Size distribution of TSP was found to be generally bimodal. Chloride exhibited a seasonal variation in the distribution; fine particles were predominant in the winter whereas the concentration of coarse ones was almost same through four seasons. Nitrate showed a distribution similar to that of chloride. Such variation was less significant for sulfate. For chloride and nitrate, the relationship between the monthly averaged distribution pattern and air temperature was analyzed in terms of fine fraction (FF). The FF decreased with increasing air temperature.

A new synthetic method for bufexamac, which is a potent anti-inflammatory agent, was described. Friedel-Crafts reaction of butoxybenzene (2) with ethyl ${\alpha}-chloro-{\alpha}-(methylthio)acetate$ (1) gave ethyl 2-methylthio-2-(p-butoxyphenyl) acetate (3). Ethyl 2-(p-butoxyphenyl)acetate (4) was prepared by desulfurization of compound (3) with zinc dust-acetic acid. Bufexamac (5) could be easily synthesized by treatment of compound (4) with hydroxylamine HCl.

An ion chromatographic method based on indirect photometric detection of UV transparent anions was developed. Separation of anion was accomplished on strong anion exchange column (Waters SAX) using UV detector at 254 nm. Among examined UV-active additives (Dns-H, Dns-glu, Dnsser, Dns-val), Dns-glu showed the highest sensitivity. Studies on the effects of the pH and ionic strength of eluent revealed that the increase of pH and ionic strength of the eluent decreased capacity factor. The best eluent for the separation of acetate, fluoride, chloride, nitrate and bromide was $1\;{\times}\;10^{-4}M$ Dns-glu in 5 mM phosphate buffer (pH 6.30). The detection limit of chloride ion was 2.1 ng in this condition.