• 약학회지
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• 제46권6호
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• pp.392-397
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• 2002

A simple and sensitive high performance liquid chromatographic method to quantitate ursodeoxycholic acid in crude drug pharmaceuticals was investigated. Ursodeoxycholic acid react with 2-bromoacetyl-6-methoxynaphthalene (Br-AMN) in the presence of triethylamine to form highly fluorescent derivative. The derivatization procedure was performed at 7$0^{\circ}C$ and completed within 30 min. The optimal wavelength of the fluorescence detector are λ$_{ex}$=300 nm and λ$_{em}$ = 460 nm. The LOD of the ursodeoxycholic acid was 25 ng/mι based on the S/N =3, and the LOQ was 80 ng/mι based on S/N = 10. Crude drug pharmaceuticals pretreated by solid phase extraction (Sep-pak $C_{18}$ cartridge) which were shown very good separation and recovery values for the compound.d.

• 한국식품위생안전성학회지
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• 제9권2호
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• pp.75-80
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• 1994

The effects of ursodeoxycholic acid (UDCA) were studied on the hepatotoxicity induced by several hepatotoxicants such as carbonte trachloride, thioacetamide and 1-naphthylisothiocyanate in ICR male mice. UDCA (50 mg/kg, 100 mg/kg) decreased the elevated serum bilirubin in carbon tetrachloride intoxicated mice, the elevated serum AST, alkaline phosphatase in thioacetamide intoxicated mice, the elevated serum AST and bilirubin in 1-naphthylisothiocyanate intoxicated mice.

• 생약학회지
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• 제48권1호
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• pp.10-17
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• 2017

Ursi Fel's component ursodeoxycholic acid (UDCA), a traditional medicine, is used for the treatment of hepatic diseases. UDCA derivatives prepared by conjugation with antioxidant moiety such as maltol, sesamol, eugenol, mesitol and 3,4-(methylenedeoxy)aniline were expected to have various biological activity caused by synergistic effect of UDCA. Therefore, in this study, it was conducted the study of the manufacture of the UDCA derivatives and their biological activity. As a result, UDCA derivatives showed weak antioxidant activity in TBA method in vitro compared to original agents. SJ-505, SJ-502 and SJ-504 showed the effect of reducing ALT, AST, sorbitol dehydrogenase and ${\gamma}-glutamyltransferase$ in $CCl_4-induced$ liver injury experiment in vivo, even if the effects are weaker than UDCA and silymarin of the control group.

• Biomolecules & Therapeutics
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• 제2권3호
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• pp.213-222
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• 1994

The acute tonicity of DWP305 (Ursodeoxycholic acid : Silymarin : Fursulthiamine : Riboflavin tetrabutyrate=1: 1 : 0.1 : 0.05) was evaluated in both sexes of Sprague-Dawley rats, 6weeks old by the oral route of administration. DWP305 was not considered to induce any toxic effect on the rats in mortalities, clinical findings, body weights and gross findings. It is suggested that LD$_{50}$ value in rats would be above 5 g/kg in the oral administration. Subacute toxicity of DWP305 was examined in Sprague-Dawley rats. Four groups of rats were administered orally at doses of 0, 0.32, 0.8, and 2.0 g/kg/day of DWP305 for one month. Any significant toxic clinical symptom was not observed in the treated rats during the experimental period. Macroscopic examination on the organs of tested animals showed no abnormal findings. On autopsy, no significant changes were found in organs examined. Maximum tolerated dose of DWP305 for the rat was estimated to be above 2 g/kg in this study.y.

• Biomolecules & Therapeutics
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• 제10권1호
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• pp.1-6
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• 2002

The particle size of medicinal materials is an Important physical property that affects the phar-maceutical behaviors such as dissolution, chemical stability, and bioavailability of solid dosage forms. The size reduction of raw medicinal powder is needed to formulate insoluble drugs or slightly soluble medicines and to improve the pharmaceutical properties such as the solubility, the pharmaceutical mixing, and the dispersion. The objective of the present study is to evaluate physiological activity of amorphous and nano-particle prep-arations of insoluble drug, ursodeoxycholic acid (UDCA), which were made by three types of fine grinding mills. The change of physical properties of ground UDCA was conformed by Mastersiger microplus and X-ray diffraction. We have investigated hepatoprotective effects of the nano-particle preparations of UDCA by plan-etary mill, vibration rod mill and jet mill in $CCI_4$-induced oxidatively injured mouse liver. The results showed that nano-particle preparations of UDCA all decreased reactive oxygen sepecies generation and lipid peroxi-dation in $CCI_4$-induced oxidative stress mice. Among them, nano-particle preparations by vibration rod mill and jet mill showed more significantly hepatoprotective effects compared to intact UDCA and planetary mill-ground UDCA. These results suggest that ground UDCA with vibration rod mill and jet mill shows a high amorphous state and the improved dissolution.

• Molecular & Cellular Toxicology
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• 제1권1호
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• pp.40-45
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• 2005

Ursodeoxycholic acid (UDCA) has long been used as an adjuvant or first choice of therapy for liver disease. Commonly, UDCA has been reported to play a role in improving hyperbilirubinemia and disorder of bromsulphalein. More commonly, UDCA has been used in reducing the rate of cholesterol level in bile juice that can cause cholesterol stone. The effects on the promotion of bile acid release that leads an excretion of toxic materials and wastes produced in liver cells as well as various arrays of liver disease such as hepatitis. Other than already reported in clinical use, immunosuppressive effect has been studied, especially in transplantation. In the study, we hypothesized that UDCA might have a certain role in anti-inflammation through a preventive effect of pro-inflammatory potentials in the brain macrophages, microglia. We found that the treatment of $200\;{\mu}g/ml$ UDCA effectively suppressed the pro-inflammatory mediators (i.e. nitric oxide and interleukin-$1{\beta}$) in rat microglia compared to comparators. Interestingly, RT-PCR analysis suggested that UDCA strongly attenuated the expression of $IL-1{\beta}$ that was comparable with cyclosporine A at 48 h incubation. Conclusively, we found that UDCA may playa cytoprotective role in microglial cells through direct or indirect pathways by scavenging a toxic compound or an anti-inflammatory effect, which are known as major causes of neurodegenerative diseases.

• 약학회지
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• 제38권1호
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• pp.78-85
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• 1994

From phase solubility studies bile acids and bile salts were found to form stable inclusion complexes with ${\beta}-cyclodextrin$ in aqueous solution. Stability constant of bile acids were larger than that of bile salts. Phase solubility diagrams of most bile acids showed Higuchi's $A_I$ type but lithocholic acid showed $B_S$ type. Not only the solubility of bile acids but also that of ${\beta}-cyclodextrin$ increased, especially in cases of cholic acid and ursodeoxycholic acid. Solubility increase of bile acids from their ${\beta}-cyclodextrin$ inclusion complex followed the order : cholic acid>ursodeoxycholic acid>chenodeoxycholic acid>deoxycholic acid>lithocholic acid. It seems that solubility of inclusion complexes was directly related with the hydrophilicity of bile acids.

• Journal of Periodontal and Implant Science
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• 제29권2호
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• pp.325-333
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• 1999

The antibacterial efficacy of a mouthrinse(Denta Gargle) containing CPC(cetylpyridinium chloride), NaF and UDCA(ursodeoxycholic acid), on major periodontopathogens, was in vitro examined and compared with that of Listerine by a broth dilution method. The bacteria tested were Actinobacillus actinomycetemcomitans, Bacteroides forsythus, Fusobacterium nucleatum subsp. vincentii, Prevotella intermedia, Porphyromonas gingivalis and Treponema denticola. The growth of all the bacteria were completely inhibited by a 1-min exposure to the both mouthrinses. When diluted at 1:5 or more, all bacteria analyzed but P. intermedia were not inhibited by Listerine. In contrast, Denta Gargle showed highly increased maximum inhibitory dilutions(MID) against all periodontopathogens included in this study, with MIDs ranging from 5-fold(F. nucleatum) to 160-fold dilutions(P. intermedia). The MIDs against A. actinomycetemcomitans, B. forsythus, P. gingivalis and T. denticola. were 1:40, 1:80, 1:80 and 1:80, respectively.

• 약학회지
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• 제38권4호
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• pp.372-378
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• 1994

Choleretic effect and absorption of ursodeoxycholic acid (UDCA) in rats were studied using UDCA alone and it's ${\beta}-cyclodextrin$ $({\beta}-CyD)$ inclusin complex (UDCA-IC). In spite of increase in solubility and dissolution rate, absorption of UDCA-IC was decreased compared with UDCA alone. Choleretic effect of UDCA-IC was also decreased. It looks that UDCA forms stronger inclusion complex with ${\beta}-CyD$ than any other drug or organic biological material. From this study, it was suggested that UDCA might be used as a new potential competing agent when inclusion complexes of drugs with ${\beta}-CyD$ were administered for the improvement of poor bioavailability.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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• pp.199-199
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• 1998

In this study, the effects of ursodeoxycholic acid (UDCA) on ischemia/reperfusion injury were investigated on retrograded aortic perfusion model. Hearts from Sprague-Dawley rats were perfused with oxygenated Krebs-Henseleit solution (pH 7.4, 37) on a Langendorff apparatus. After equilibration, hearts were treated with ursodeoxycholic acid 10, 20, 40 and 800 M or vehicle (0.04% DMSO) for 10 min before the onset of ischemia. Following 25 min of global ischemia, ischemic hearts were reperfused and allowed to recover for 30 min. The physiological (i.e. heart rate, left ventricular diastolic pressure, coronary flow and time to contracture formation) and biochemical (lactate dehydrogenase, LDH) endpoints were evaluated. In vehicle group, time to contracture formation (TTC) value was 19.5 min during ischemia, LVDP was 20.8 mmHg at the endpoint of reperfusion and LDH activity in reperfusate was 59.7 U/L. Cardioprotective effects of UDCA following ischemia/reperfusion consisted of a reduced TTC (EC$\_$25/ = 16.10 M), reduced LDH release and enhanced recovery of contractile function during reperfusion. Especially, the treatments of UDCA 80 M remarkably increased LVDP (68.1 mmHg) and reduced LDH release (33.2 U/L). Our findings suggest that UDCA ameliorates ischemia/reperfusion-induced myocardial damage, in agreement with physiological and biochemical parameters.