• 약학회지
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• 제39권4호
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• pp.411-416
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• 1995

The single-pass perfusion experiments were performed in anesthetized rats to investigate the effects of perfusates and their osmolality on the water transport and to determine the correlation between the extent of water transport and the volume change of perfusate. Phenol red was used as a nonabsorbable marker. In normal rats, when perfused at a flow rate of 0.5 ml/min, 2-(N-rnorpholino) ethanesulfonic acid (MES) and S$\phi$rensen's phosphate buffers showed minimal net water transport as 0.125 and 0.173 %/cm of intestinal length, respectively. Hypotonic perfusate of 200 mOsm/kg of water and hypertonic perfusate of 400 mOsm/kg of water generated significant water transport compared with isotonic perfusate of 300 mOsm/kg of water. There was a linear correlation between the extent of water transport and the volume change of perfusate, suggesting that the volume change can be used as a measure of water transport.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1997년도 춘계학술대회
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• pp.57-63
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• 1997

Animal and clinical investigations have shown that fluoroquinolones, new quinolone antibacterial agents (NQs), are well absorbed across the intestinal tract, with a bioavailability of 60-90% after oral administration. Although some types of carrier-mediated intestinal transport mechanisms have been reported for enoxacin (ENX), ofloxacin (OFLX) and sparfloxacin (SPFX), recent results using a human intestinal epithelial cell line, Caco-2, indicated a passive or nonsaturable transport of SPFX, one of the most hydrophobic NQs. The mechanism underlying the intestinal absorption of NQs is still largely unknown. The distribution of NQs into peripheral tissues including erythrocytes is very rapid and their tissue-to-plasma concentration ratios (Kp) are considerably larger than those of inulin (an extracellular fluid space marker), in spite of almost complete ionization of NQs at the physiological pH. Our findings suggest that OFLX and lomefloxacin (LFLX) are taken up by rat erythrocytes via a transport system common to that of a water-soluble vitamin, nicotinic acid.

• 생약학회지
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• 제24권2호
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• pp.140-152
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• 1993

This study was attempted to investigate the effect of Ganoderma lucidum extract on digestive system in experimental animals. Ganoderma lucidum water extract (GWE) was found to be promoted the charcol transport rate in the small intestine of mice. GWE exhibited the augmentation of spontaneus movement(motility) and contractile response(tension) in the ileum and colon strips of rabbit, and these action were inhibited by atropine. GWE given intraduodenaly(i.d.) exhibited the significant increase of gastric acid secretion in pylorus-ligated rats. GWE inhibited the formation of some experimental gastric ulcers(pylorus ligation ulcer i.d., indomethacin-induced ulcer p.o., i.d. and aspirin-induced ulcer p.o.) in rats, which are considered to relate to a protective action. GWE and EtOH extract(water soluble phase) were remarkably increase of bile excretion, when administration of i.d., intravenation(i.v.) and per os (p.o.) compared with normal-control group. GWE was observed antibacterial activity aginst several intestinal microoganisms and others bacteria in vitro test.

• 약학회지
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• 제49권2호
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• pp.185-191
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• 2005

The absorption of a P-gp substrate, rhodamine 123, from a liposomal dosage form was investigated across Caco-2 cell monolayers, rat intestines and rat intestinal Peyer's patches in Ussing chamber, Rhodamine 123 was incorporated into liposomes according to the standard evaporation method, which led to a production of liposomes with a mean diameter of 71.3 nm. The permeability (Papp of rhodamine 123 from a water solution across the monolayer was $2.45{\times}10^{-6}$ cm/s for $A{\leftrightarrow}B$ (apical to basal) and $14.0{\times}10^{-6}$ cm/s for $B{\leftrightarrow}A$ (basal to apical) directions, consistent with the fact that rhodamine 123 is one of the P-gp substrates. The transport of rhodamine 123 from the liposomal dosage form was much lower for both directions compared to the solution of rhodamine 123. The transport of rhodamine 123 across the rat intestine was also significantly decreased for both directions, I.e., influx and efflux, by the liposomal incorporation of the compound. The transport of rhodamine 123 across the Peyer's patch was substantially reduced by liposomal incorporation. No difference was found in the transport between the Peyer's patch and non-Peyer's patch. These observations suggest that the contribution of transport via Peyer's patches in the uptake of liposomes may be minimal, especially for rapidly absorbed compounds like rhodamine 123. Therefore, the increased absorption of P-gp substrates does not appear to be feasible by incorporating the compounds in liposomes, due to negligible involvement of Peyer's patches in the uptake of particulate dosage forms like liposomes. Liposomes may rather represent a sustained release dosage form of incorporated compounds.

• 한국식품과학회지
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• 제30권2호
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• pp.456-460
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• 1998

음용수 중에 납과 카드뮴이 오염되었을 때 치커리, 당귀, 영지버섯의 중금속의 장내 흡수억제 효과가 있는지를 알아보기 위해 장내 흡수 조건을 고려한 투과막을 이용하여 in vitro실험을 실시하였다. 납과 카드뮴이 음용수 수질기준의 10배 또는 50배로 오염된 음용수에서 단독오염의 경우 납은 치커리, 당귀, 영지버섯에서 $40{\sim}60%$의 제거효과를 보였고 카드뮴의 경우는 치커리, 당귀, 영지버섯에서 $20{\sim}40%$의 제거효과를 나타내었다. 납과 카드뮴이 혼합오염된 경우에 납은 치커리, 당귀, 영지버섯의 세 시료에서 비슷하게 $30{\sim}50%$의 제거효과를 나타냈으며 카드뮴은 $10{\sim}30%$의 제거효과를 보여주었는데 치커리, 영지버섯에 비해 당귀가 높은 제거효과를 보여주었다. 추출조건별로 비교해보면 $70^{\circ}C$, 2분 추출조건의 경우가 $95^{\circ}C$, 10분의 경우보다 더 제거효과가 높았음을 관찰할 수 있었다. 한편 여과지 및 투과막에도 상당량의 중금속이 흡착되어 제거된다는 사실을 알 수 있었는데 오염된 중금속의 농도가 높을수록, 음료 추출온도가 높을수록 더 많은 중금속이 흡착되었음을 관찰할 수 있었다. 이러한 결과는 투과막이 중금속에 흡착되기 쉬운 섬유질로 이루어져 있기 때문인 것으로 추측되며 치커리, 당귀, 영지는 음용수중에 오염된 중금속의 장내흡수 억제 효과가 있음을 알 수 있었다.

• The Korean Journal of Physiology
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• 제7권2호
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• pp.39-47
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• 1973

The influences of the acute hemorrhage on the intestinal functions were studied in the rabbits subjected to acute bleeding, amounting 1.5-2% of the body weight. The motility and the absorptive capacity of the ileum were compared before and after the bleeding. Transfusion of shed blood was also performed in order to see whether the deteriorations were reversible or not. The tension developed in the direction of the longitudinal axis of the ileum was recorded through an appropriate transducer, and the frequency of the rhythmic contraction was counted throughout the procedure. Test solution, 10ml in amount, was placed in the loop of the ileum, and the samples were drawn at zero time and at 20 minutes. Triplicated procedures were repeated on the same loop;namely, before and after bleeding and after transfusion. The test solution was composed of 200 mg% urea, 218 mEq/l of NaCl and 150 mg% of polyethylene glycol (PEG) No. 4,000 in distilled water. The latter substance was used as a marker substance for the volume change of the loop. The results obtained were as follows; 1. The motility of the ileum suffered little effects by acute hemorrhage. However, minor fluctuations were seen in the frequency of the rhythm, showing a slight tendency of decreasing rhythmicity, and it was reversed by transfusion. 2. Diminution of absorptive capacity of urea was noticed in acute hemorrhage and it was interpreted as the consequence of the secondary effect of the retardation of the active transport mechanism governing the sodium transport 3. Absorption rate of the sodium ion was dropped in the hemorrhage, suggesting the indispensable need of the blood supply. 4. Osmolarity of the luminal fluid remained higher in the case of acute hemorrhage. 5. There was a tendency of retaining more fluid in the intestinal lumen in acute hemorrhage, comparing with that observed prior to the bleeding. 6. The deteriorations in the absorptive capacity were restored by transfusion of shed blood.

• The Korean Journal of Physiology
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• 제7권1호
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• pp.23-31
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• 1973

Numerous factors concern with the absorption of substances through the membrane of the gastrointestinal tract. To simplify the experimental condition, present work has been restricted to observe the disappearance rate of substance from the intestinal loop which was made in the jejunum, 70 cm apart from the pylorus of the adult rabbit. The purpose of the study is to clarify the absorption of urea through the jejunal wall is solely attributable to the concentration difference between the luminal fluid and plasma, and to observe the effect of adding red pepper upon the rate of absorption. The rabbits were anesthetized with nembutal, 35mg/kg I.V. Jejunal loop was made by ligating at 2 spots, 70 cm and 80cm apart from the pylorus. After rinsing with normal saline solution through the polyethylene tubing inserted from the end of the loop, 8 ml of test solution was placed through the same tubing. The test solution contained 200 mg% of urea and 150mg% of polyethylene glycol(M.W. 4,000) in normal saline solution. Right after placing the test solution the first specimen was taken through the tubing, and successive samplings were performed at 5, 10, 20, and 30 minutes. Logarithm of the difference of urea concentration between the luminal fluid and plasma was plotted against time elapsed after the onset of the experiment. If straight line is revealed, it would verify the nature of transport mechanism as diffusion, obeying the Fick's principle. The concentration of polyethylene glycol (PEG) was also measured in order to examine the change in the volume. PEG was used as the marker substance because it is not absorbable in the intestinal tract. Consequently the concentration of PEG relates inversely to the volume of the loop. Instantaneous concentration of urea in the loop times the volume will give the amount of urea remaining in the luminal fluid. The change in the amount of any substance is directly relate to the volume of the compartment and differs from the change in the concentration which is independent of the volume. After completion of the experiment without red pepper, it was added in the test solution and was centrifuged after thorough mixing. Supernatant of the mixture was placed in the loop and similar sampling were performed with the same time intervals that of previous run in order to observe the effects of the red pepper on the passive transport of the water soluble small substance, urea. The results obtained were as follows: 1. Logarithm of the concentration difference of urea between the luminal fluid and plasma was diminished exponentially as time elapsed. The decay constant in the experiment without red pepper was 0.0563/min. By adding red pepper in the test solution as much as the concentration rose to 4,000 mg% and 8,000 mg%, the decay constants were lowered to 0.0493/min and to 0.0506/min, respectively. The time interval by which the concentration difference dropped to one half of the initial value was prolonged. Without red pepper the half concentration time was 13.30 minutes, and by adding extract of red pepper, 15.31 minutes and 15.71 minutes were revealed. 2. The profile of the diminishing rate of tile amount of urea was quite different from that of the concentration because of the change in the volume of the loop during the observed period. 3. By adding the extract of red pepper, it slowed down the rate of absorption of urea in the intestinal loop, suggesting an increase in the diffusional barrier. 4. Larger dosage of red pepper brought an increase in the secretion of intestinal fluid with concomitant expansion of the luminal volume, and the retardation of the absorption of urea was noticed. This effect was largely dependent on the sensitivity of the individual animal to the red pepper, extract. The amount of urea remained after 10 minutes interval was 55.5% of the initial amount in the experiment without red pepper. On the other hand it was not consistent after administration of red pepper, showing 50.6% and 66.5% of the initial figures by adding 400 mg and 800 mg of red pepper in the test solution, respectively. It was postulated that symptom of diarrhea often encountered by taking a hot (red pepper) food might be attributable to the increase of secretion and the retardation of absorption in the intestinal tract.

• Archives of Pharmacal Research
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• 제28권8호
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• pp.988-994
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• 2005

The purpose of the present study was to prepare multivesicular liposomes with a high drug loading capacity and to investigate its potential applicability in the oral delivery of a peptide, human epidermal growth factor (rhEGF). The multivesicular liposomes containing rhEGF was prepared by a two-step water-in-oil-in-water double emulsification process. The loading efficiency was increased as rhEGF concentration increased from 1 to 5mg/mL, reaching approximately $60\%$ at 5 mg/mL. Approximately $47\%$ and $35\%$ of rhEGF was released from the multivesicular liposomes within 6 h in simulated intra-gastric fluid (pH 1.2) and intra-intestinal fluid (pH 7.4), respectively. rhEGF-loaded multivesicular liposomes markedly suppressed the enzymatic degradation of the peptide in an incubation with the Caco-2 cell homogenate. However, the transport of rhEGF from the multivesicular liposomes to the basolateral side of Caco­2 cells was two times lower than that of the rhEGF in aqueous solution. The gastric ulcer healing effect of rhEGF-loaded multivesicular liposomes was significantly enhanced compared with that of rhEGF in aqueous solution; the healing effect of the liposomes was comparable to that of the cimetidine in rats. Collectively, these results indicate that rhEGF-loaded multivesicular liposomes may be used as a new strategy for the development of an oral delivery system in the treatment of peptic ulcer diseases.

• Molecular & Cellular Toxicology
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• 제4권1호
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• pp.52-60
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• 2008

In order to investigate whether the particles reduced to almost nano grade might affect the chemical and physical properties of organic materials, whole Korean Black-Red Ginseng was pulverized into almost nano size and then ginsenosides, minerals, carbohydrates, lipids and proteins in the ultrafine particles were compared with those in the regular particles as control. The mean size of the ultrafine particles was in the 350 nm range, while that of the regular particles was $127{\mu}m$. More ginsenosides, minerals, carbohydrates, lipids and proteins were detected in the ultrafine particles than in the regular particles. Interestingly, more lipids from the ultrafine particles dissolved in the water than those from the regular particles in the ethanol. Absorption and transport of carbohydrate, lipid or antioxidant activity across the intestinal wall using everted intestine sacks of mice was also enhanced by particle size reduction at the almost nano scale. More cytotoxic effect against hepatoma cell growth by ultrafine particles was also found. These results could be used as the basic data for the understanding and evaluation of the effects of organic nanomaterials on the human health.

• 생약학회지
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• 제34권1호통권132호
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• pp.45-54
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• 2003

We have conducted to characterize the physico-chemical change and pharmacological transformation of traditional herbal medicines by means of processing. Processed Gardeniae Fructus was prepared by heating of fruit of Gardenia jasminoides(GF) for $30{\sim}50\;minute$ in the roster designed for herb processing. The contents of drying loss, water extract, diluted ethanol extract, ether extract and geniposide in non-processed GF and processed GF were examined. The contents of drying loss, water extract and geniposide in processed GF showed a decrease as compared with those of non-processed GF, however the contents of dilute ethanol and ether extract showed a increase as compared with those of non-processed GF. The rate of decrease/increase of those index were in proportion to heating time. And, biological activities of methanol extract of non-processed GF and processed GF were investigated. DPPH scavenging effects and inhibitory effect of xanthine oxidate and hemolysis of processed GF exhibited more effective than those of non-processed GF in vitro. Accelerating effect of large intestinal transport and purgative action of non- processed GF were discriminated by processing of GF. Methanol extracts of non-pro- cessed GF and processed GF showed the protective effects against the hepatotoxicity induced by ${\alpha}-naphthylisothiocyanate$ in rats. These results suggested that the transformation of biological activities of GF by means of processing may be due to the physico-chemical change of the constituents in GF by heating.