• Journal of Pharmaceutical Investigation
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• v.22 no.2
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• pp.149-153
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• 1992

The applicability of sodium alginate as a carrier of 5-fluorouracil as an oral delivery system was investigated. Hydrophobicity of sodium alginate was controlled by introducing cetyl group to this polymer. The effects of degree of esterification for n-cetyl partial ester on the rate of release of 5-fluorouracil in artificial gastric juice and artificial intestinal juice were examined. The release rete of the drug in the gastric juice was mainly affected by the diffusion of the drug. The release rate of the drug in the intestinal juice could be controlled by the degree of esterification. The alginate matrices may be a valuable addition as the carrier of 5-fluorouracil for an oral delivery system.

• Journal of Pharmaceutical Investigation
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• v.24 no.4
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• pp.233-243
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• 1994

Precipitation was formed during the preparation of decoction from a mixture of Scutellariae Radix and Coptidis Rhizoma or Phellodendri Cortex according to the prescription of Hwang-ryean-hae-dog-tang. Baicalin and berberine were identified in coprecipitated product and these components were the active ingredients of two herbal medicine. The coprecipitated product was very slightly soluble in water and sparingly soluble in ethanol. The stoichiometric ratio of baicalin and berberine was found to be 1:1. The lipid-water partition coefficients of coprecipitated product were increased more than baicalin and berberine in chloroform, but were decreased in other organic solvents. The content of baicalin and berberine in coprecipitated product, determined by HPLC, were 23.08% and 26.75%, but the content of active ingredients in supernatant were 0.66% and 0.26%, respectively. The dissolution profile of baicalin of coprecipitated product was increased more than extract of Scutellariae Radix in artificial gastric juice, but was decreased in artificial intestinal juice. The dissolution rate of berberine of coprecipitated product was lower than extract of Coptidis Rhizoma in artificial gastric juice and intestinal juice commonly.

• YAKHAK HOEJI
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• v.30 no.3
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• pp.128-138
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• 1986

Three newly synthesized alkanol esters of d-2-(6-methoxy-2-naphthyl) propionic acid, NAPROXEN were examined for physicochemical properties and biopharmaceutical characteristics. These esters were very stable in solid state, but more than 90% of these esters were hydrolysed to the parent, naproxen in rabbit's liver hornogenates. They showed higher dissolution rate in the artificial gastric and intestinal juice, and significantly greater partition coefficient in n-octanol, when compared with naproxen. The absorption rate constants of these esters were increased, while the elimination rate constants were decreased, comparing with naproxen. The ulcerogenic doses on gastric and intestinal mucosa were increased remarkably, and the antiinflammatory dose against carrageenininduced edema on rat hind paw was decreased markedly in these esters, and thus the safety indexes of these esters were higher than that of naproxen.

• Journal of Dairy Science and Biotechnology
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• v.31 no.1
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• pp.51-58
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• 2013

Emerging studies suggest that vegetables or fruit juices deemed to be potential alternative base medium for lactic acid bacteria fermentation. Until now, limited studies have been carried out to evaluate such applications. Thus, the objective of present study is that lactic acid bacteria were evaluated for their viability at low pH, growth during storage at low temperature, and $CO_2$ formation. Furthermore, the effects of grapefruit extract with respect to cell viability, sensory ability, and organic acid production were evaluated for these strains. The probiotic properties of the strains, including acid tolerance, bile tolerance, and adhesion to human intestinal epithelial cells (HT-29 cells), prebiotic characteristics, and safety features were examined. All strains survived in MRS medium broth adjusted to pH 3.8, at $10^{\circ}C$ for 6 days, and did not produce $CO_2$ to check post fermentation. The medium of grapefruit extract fermentation by Lactobacillus plantarum CJIH 203 resulted in maximal viable counts, compared with other strains, and the extract subsequently tasted sour due to the presence of lactic acid. Lactobacillus plantarum CJIH203 was highly resistant to artificial gastric juice and intestinal juice, while Lactococcus lactis SJ09 strongly adhered to HT-29 cells. Tagatose showed the greatest ability to enhance the growth of L. plantarum SJ21, relative to the other strains. All strains were verified by safety tests such as hemolysis, gelatin hydration, and urea degradation. Therefore, these strains could be promising candidates for use in reducing excessive post-fermentation and functional products.

• Journal of Pharmaceutical Investigation
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• v.14 no.3
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• pp.105-121
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• 1984

The bioavailability of rifampicin (brand A, B and C) was studied and the dissolution by foamed plastic rotating method and basket rotating method was also investigated. The results were as follows; 1. In the case of foamed plastic rotating method, it was revealed that dissolution rate of brand C was most rapid, but in the case of basket rotating method the results revealed that brand B was most rapid. Also it was observed that the dissolution rate in artificial gastric juice was more rapid than one in artificial intestinal juice, and that Avicel added in capsule increased additively the dissolution rate, particulary brand B. 2. Relative systemic availability by urine data showed that the results from all capsules filled with brand A, B and C were identical but in the case of the ripamficin capsules filled with Avicel, the results showed that Avicel increased the availability of brand A and B. 3. Area under serum concentration curve $(0{\sim}8hrs)$ was in order of $brand\;A{\fallingdotseq}brand\;C$ > brand B, but Avicel increased significantly the AUC of brand B and showed no effect in others. 4. Relative systemic availability calculated with excreted amount of rifampicin in urine was similar in each rifampicin capsules. In rifampicin (A) and rifampicin (B), Avicel which added in capsules appeared increasing tendency in urine excretion of rifampicin, but in rifampicin (C) it did not appeared. 5. Area under serum concentration curve $(0{\sim}8hrs)$ in rifampicin capsules was in order of $rifampicin(A){\fallingdotseq}rifampicin(C)$>rifampicin(B). In rifampicin (B) with Avicel capsules, area under serum concentration curve (0-8hrs.) increased significantly and in others insignificantly.

• YAKHAK HOEJI
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• v.38 no.2
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• pp.123-130
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• 1994

Physicochemical properties and hydrolysis kinetics of new some oral cephalosporins were examined in buttered solution and human plasma or rat liver homogenate. The test cephalosporins were 7-[(Z)-2-(2-aminothiazole-4-yl)-2- methoxyiminoacetamido]-3-[4-(2-pyridyl)piperazinyl] thiocarbonylthhiomethyl-3-cephem-4-carboxylic acid (CEN1), 7-[(Z)-2-(2-aminoth iazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyrimidyl)piperazinyl]th iocarbonylthiomethyl-3-cephem-4-carboxylic acid (CEN2), pivaloyloxymethyl-7-[ (Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyridyl)piperazi nyl]thiocarbonylthiomethy1-3-cephem-4-carboxylate (CEN1P), and pivaloyloxymethyl-7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[ 4-(2-pyrimidyl)piperazinyl]thiocarbonyl-thiomethyl-3-cephem-4-carboxylate (CEN2P). The partition coefficient(Ko/w) of CEN1P, CEN2P were higher than those of CEN1, CEN2. The calculated pKa values of CEN1, CEN2, CEN1P, and CEN2P were 7.09, 7.75, 4.92, and 5.39, respectively. The hydrolysis of CEN1P and CEN2P were not depend on the composition of pH of the test medium except weak alkaline buffered solution (pH 8.00). CEN1 and CEN2 were very stable in pH 6.80 and 8.00 buffer solutions. CEN1P and CEN2P were rapidly deesterified to CEN1 and CEN2 in human plasma and in rat liver homogenate. Half-lives$(t_{1/2})$ of CEN1 and CEN2 were 3.49 and 4.93 hr in human plasma, 1.47 and 1.26 hr in rat liver homogenate, respectively.

• YAKHAK HOEJI
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• v.37 no.6
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• pp.638-646
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• 1993

A cepfialosporin with an aminothiazoiylmethoxyimino-type side chain at the 7 position and bicyclic quinolone dithicarbamate at the 3' position was synthesized. It has broad and potent antivacterial activity in vitro. The antibacterial spectrum reflects contributions of both the cephalosporin moiety and the quinolone moiety. Thus, this compound was named DACD implying a dualaction cephalosporin derivative. In this paper, the physicochemical proper-ties (lipid-water partition, pKa), stability and pharmacokinetics of DACD were determined and compared with cefotaxime 3'-norfloxacin dithiocarbamate (CENO). Stability tests were studied in pH 1.20, 6.80 and 8.00 buffers and in the presence of AB type human plasma, rat liver homogenate and its .betha.-lactamase. The pharmacokinetic parameters of DACD were evaluated in mice after a single intravenous dose of 40 mg/kg. The results are as follows. The lipid-water partition coefficient of DACD was higher than that of CENO. The calculated pKa values of CENO and DACD, were 6.82$\pm$0.03, 7.53$\pm$0.21, respectively. In the hydrolysis test, half-lives (t$^{1/2}$) of CENO and DACD was 66.0 hr and 80.0 hr in pH 6.80 buffer, 190 hr and 91.4 hr in pH 8.00 buffer. CENO and DACD were rapidly hydrolyzed in human plasma and in rat liver hornogenate. Half-lives (t$_{1/2}$ of CENO and DACD were 1.29 hr and 1.15 hr in hyman plasma, 0.62 hr and 0.71 hr rat liver homogenate. In $\beta$-lactamase stability test, CENO and DACD were very stable to the .betha.-lactamases obtained from three different strains. Half-life (t$_{1/2}$) and areas under the curve (AUC) in mice were 2.33 hr and 15.97 (mg.h/1), respectively.

• Journal of Pharmaceutical Investigation
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• v.17 no.2
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• pp.79-88
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• 1987

In order to reduce gastric irritation of iron preparations, one prodrug, glycine complex of ferrous fumarate, was synthesized, identified, examined for physico-chemical properties and compared with ferrous fumarate, ferrous sulfate and ferroglycine sulfate. That novel ferroglycine fumarate (FGF) resulted in higher dissolution rate in water, artificial gastric and intestinal juice. The absorption rate constants $(K_a)$ in rat of FGF was greater and ulcerogenic dose on stomach was increased remarkably than those of iron parent materials and ferroglycine sulfate.

• Journal of Microbiology and Biotechnology
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• v.28 no.6
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• pp.883-892
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• 2018

Probiotics, including Enterococcus faecium, confer a health benefit on the host. An Enterococcus strain was isolated from healthy chicken cecum, identified as E. faecium by 16S rDNA gene sequence analysis, and designated as E. faecium L11. To evaluate the potential of E. faecium L11 as a probiotic, the gastrointestinal tolerance, immunomodulatory activity, and lifespan extension properties of the strain were assayed. E. faecium L11 showed >66% and >62% survival in artificial gastric juice (0.3% pepsin, pH 2.5) and simulated small intestinal juice (0.5% bile salt and 0.1% pancreatin), respectively. Heat-killed E. faecium L11 significantly (p < 0.05) increased immune cell proliferation compared with controls, and stimulated the production of cytokines (IL-6 and $TNF-{\alpha}$) by activated macrophages obtained from ICR mice. In addition, E. faecium L11 showed a protective effect against Salmonella Typhimurium infection in Caenorhabditis elegans. In addition, feeding E. faecium L11 significantly (p < 0.05) extended the lifespan of C. elegans compared with the control. Furthermore, genes related to aging and host defense were upregulated in E. faecium L11-fed worms. In conclusion, E. faecium L11, which prolongs the lifespan of C. elegans, may be a potent probiotic supplement for livestock.

• YAKHAK HOEJI
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• v.45 no.5
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• pp.536-544
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• 2001

increase the viability of oral typhoid vaccine during the passage through the castro-intes-tidal tract, numerous attempts have been made including the vaccine coating. However problems such as high death rate during the coating process and its instability in the gastric juice still remain to be solved. In this study, the oral vaccine was made as the micro-enteric beads by adding Salmomella typhi Ty21a cells to sodium alginate solution and spraying onto calcium chloride solution (ionotropic relation method). The vaccine showed more than 90% of its original viability after treating it for 1 hour in the artificial gastric juice (37$^{\circ}C$, 300 rpm). The clearance rate of the Ty21a in the liver and spleen of the mice orally administrated with coated Ty21a was similar to that of the mice intraperitoneally administrated with uncoated Ty21a. The peripheral blood lymphocytes (PBL) isolated from the mice orally administered with this vaccine produced 15.5 fold higher specific IgA antibody titer than that from the control mice administerd with saline solution. furthermore, the mice treated with the coated Ty21a had higher survival rates (50~87%) than the control mice treated with saline solution (0~10%) in the intraperitoneal challenge test with wild type S. typhi Ty21a cells. These results suggest that the alginate-based coating technique is effective to protect live Ty21a from acidic environments, and produces better intestinal immune responses thereby providing a potentially excellent oral typhoid vaccine.