• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.203-203
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• 1996

It has been known that pinusolide isolated from Biota orientalis inhibits specifically [$^3$H] PAF binding to and PAF-induced aggregation of rabbit platelets in vitro. The present study was undertaken to evaluate the effects of pinusolide on hypotension and bronchoconstriction due to PAF. PAF(i.v.) in doses of 0.01 to 0.3 $\mu\textrm{g}$/kg induced a dose-dependent hypotension without tachyphylaxis in rat. Pinusolide(5～20 mg/kg, i.v.) inhibited PAF(0.03 $\mu\textrm{g}$/kg, i.v.)-induced hypotension dose-dependently, while it failed to block the hypotensive action of histamine, serotonin and acetylcholine. It inhibited bronchoconstriction and cutaneous vascular permeability induced by PAF in anesthetized guinea-pigs and rats, respectively, but it showed no inhibitory effect on the increase in bronchial resistance by histamine and acetylcholine. These results strongly suggest that in vivo pinusolide acts as a selective antagonist of PAF.

• Journal of Pharmaceutical Investigation
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• v.20 no.1
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• pp.1-5
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• 1990

Effect of an angiotensin inhibitor (AAS; loading dose of 25, 50, $100{\mu}g/kg$ and maintenance dose of 12.5, 25,$50{\mu}g/ka/hr$) on the pharmacokinetics of propranolol (4 mg/kg i.v.) was studied in rabbits. Plasma concentrations and relative bioavailability of propranolal increased upto 127-175% by AAS coinjection. The urinary excretion of propranolol decreased by AAS. Dosage regimen of propranolol should be adjusted when it is administered with AAS.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.313.2-314
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• 2003

This study was conducted to investigate the pharmacokinetic characteristics of a synthetic opioid, Tridol\ulcornerCapsule (tramadol hydrochloride from Yuhan Pharmaceutical Co., Ltd., Korea) in 24 healthy Korean volunteers after a single dose administration. The volunteers received two capsules of 50 mg dose. Plasma samples were obtained over a 24-hour interval, and tramadol concentrations were obtained over a 24-hour intervalm and tramadol concentrations were determined by validated HPLC methods with a fluorescence detector. (omitted)

• Natural Product Sciences
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• v.9 no.3
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• pp.180-182
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• 2003

In the present study the whole plant of Ammania baccifera Linn was extracted with petroleum ether, chloroform, ethyl acetate and ethanol. The extracts were vacuum dried to yield the respective petroleum ether (PEE), chloroform (CE), ethyl acetate (EAE) and ethanol extracts (EE). PEE, CE, EAE and EE were evaluated for their antipyretic and diuretic activity at 200 mg/kg dose level. Significant antipyretic activity was associated with PEE, CE, EAE and EE. CE was found to exhibit higher antipyretic activity as paracetamol at 100 mg/kg dose level. Significant diuretic activity was exhibited by EAE, EE and PEE. The present study supports the claims of Ammania baccifera mentioned in the Indian system of medicine.

• Journal of Pharmaceutical Investigation
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• v.29 no.3
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• pp.179-184
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• 1999

Phannacokinetics of epigallocatechin gallate(EGCG) was studied following i.v. bolus and oral administration in rats. The values of systemic clearance(CL) were $67.9{\pm}5.2$ and $26.5{\pm}1.4\;ml/min/kg$ following i.v. bolus administration of 1 mg and 5 mg EGCG, respectively. The values of volume of distribution at steady state (Vss) were $380{\pm}56$ and $835{\pm}84\;ml/kg$ after i.v. bolus administration of 1 mg and 5 mg EGCG, respectively. The decrease in the value of CL and the increase in the value of $V_{ss}$ as a function of EGCG dose (1 mg to 5 mg) suggest saturable mechanism(s) responsible for the distribution and elimination of EGCG. The fraction absorbed of EGCG after oral and intraduodenal administration of GTC were 13% and 22% of the dose, respectively. This result suggests a considerable degradation or elimination of EGCG in the gastrointestinal absorption after oral administration in rats.

• YAKHAK HOEJI
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• v.35 no.5
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• pp.401-415
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• 1991

Effects of quercetin on the specific and non-specific immune responses were studied in vivo. Quercetin at a dose of 2.5, 5, 10, 20 and 40 mg/kg were orally administered to ICR male mice once daily for 28 consecutive days. Cyclophosphamide was injected intraperitoneally to ICR mice with a single dose of 5 mg/kg 2 days before secondary immunization. Mice were sensitized and challenged with sheep red blood cells (S-RBC). Immune responses were evaluated by humoral and cellular immune reponses and non-specific immune response. The results of this study were summarized as followings; 1. Quercetin significantly decreased the body weight, and introduced the atrophy of liver, spleen and thymus gland dose-dependently, but increased the numbers of white blood cell. 2. Querectin significantly depressed the hemagglutination titer, Arthus reaction and hemolytic plaque forming cell. 3. Quercetin significantly depressed the delayed type hypersensitivity and rosette forming cell. 4. Quercetin at a dose of 2.5, 5 and 40 mg/kg significantly depressed phagocytic activity. 5. Quercetin at a dose of 10 and 20 mg/kg significantly increased natural killer cell activity.

• Archives of Pharmacal Research
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• v.21 no.3
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• pp.223-230
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• 1998

The effect of an ethanolic extract of the plant Trianthema portulacastrum L. on the $CCI_4$-induced chronic hepatocellular damage of Swiss albino mice has been investigated. The normal mice received olive oil (0.2 ml/mouse) for five weeks. The $CCI_4$ control mice, on the other hand, received $CCI_4$ (0.05 ml/mouse) in olive oil for five weeks. The extract was administered at the dose of 100 mg/kg or 150 mg/kg for five weeks by gastric intubation in addition to $CCI_4$ treatment. The $CCI_4$ administraction alone caused hepatocellular necrosis, severe anemia, leucopaenia, lymphocytopaenia, neutrophilia, eosinophilia and haemoglobinaemia along with the alterations of plasma albumin and globulin. The administration of plant extract (at 100 or 150 mg/kg) restored the $CCI_4$-induced alterations of the haematological parameters to the normal level. The extract of T. portulacastrum elicited a marked protection against $CCI_4$-induced hepatotoxicity as indicated by the several haematological parameters, related indices of formed elements, and different fractions of plasma protein. We also observed the dose-dependent antihepatotoxic effect of the extraction on these mice. The 150 mg/kg of extract was found to be more effective in normalizing the toxic effects of $CCI_4$ on the above parameters of mice. These results suggest that the hepatoprotective effect of T. poltulacastrum could be caused by its critical involvement in modulating several factors associated with erythropoiesis, and the boosting of general immunity of the host.

• The Korea Journal of Herbology
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• v.32 no.4
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• pp.39-46
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• 2017

Objectives : This study aims to provide basic data about Portulacae Herba (PH) extracts as natural antioxidants by considering diverse antioxidant activities of PH depending on solvents. Methods : The samples of PH were pulverized, and A hot water and a 70% EtOH were stir-extracted for two hours three times repeatedly in a water bath with a temperature of 95 degrees and at room temperature respectively to measure 7 kinds of antioxidant activities. Results : There were significant differences in total phenol content, because the total phenol content of the 70% EtOH extract was higher than the hot water extract's, and the total flavonoid content of the 70% EtOH extract($4.40{\mu}g/mg$) was nearly 3.8 times higher than the hot water extract's($1.16{\mu}g/mg$). DPPH and ABTS radical scavenging activities were 70% EtOH extract showed a little higher activity than the hot water extract, and at a concentration of $500{\mu}g/mg$, the highest scavenging activity was found in the 70% EtOH extract, not in the control group. Hydroxyl radical and $Fe^{2+}$ chelatingactivities were slightly higher in hot water extract than in 70% EtOH extract, and increased in a dose-dependent manner. Nitrite scavenging activities increased dose-dependently in the hot water and the 70% EtOH extract, regardless of the pH level, and scavenging activity of the 70% EtOH extract was higher at pH 1.2 than at pH 3.0. Conclusions : In conclusion, it is thought that PH hot water and 70% EtOH extract have antioxidant activities, and can be used as natural antioxidants in future.

• Journal of Pharmaceutical Investigation
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• v.37 no.2
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• pp.119-126
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• 2007

Tablet splitting is used in pharmacy practice to adjust the dose to be administered. However, it also causes several problems such as undesirable effect for sustained release or enteric-coated dosage form, inaccuracy of dose, and pharmacist's safety by splitting hazardous drugs. This study investigated the current status of oral dosage form splitting for patients older than 19 years by analyzing Korea National Health Insurance Claims Database. Out of oral solid drugs prescribed (N=1,486,584) 9.8% of them included tablets (or capsules) split. There were some splitting cases even in sustained release (4.9%), enteric-coated forms (1.3%) and hazardous drugs (2.7%) that were selected by NIOSH (The National Institute for Occupational Safety and Health). The most frequently split drugs were antihistamines, neuropsychotics and steroids. In case of digoxin and warfarin, unit doses in a domestic market were not diverse compared to foreign markets. Guidelines for splitting oral solid dosage forms, approval of diverse doses and conducting dose-response studies for the commonly splitting ingredients on Korean people are needed for the saff and effective use of oral solid drugs.

• Journal of Pharmaceutical Investigation
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• v.41 no.6
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• pp.347-354
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• 2011

Repeated oral administration of loxoprofen can induce many side effects such as gastric disturbances and acidosis. Therefore, we considered alternative routes of administration for loxoprofen to avoid such adverse effects. The aim of this study was to develop an ethylene-vinyl acetate (EVA) matrix system containing a permeation enhancer for enhanced transdermal delivery of loxoprofen. The EVA matrix containing loxoprofen was fabricated and the effects of drug concentration, temperature, enhancer and plasticizer on drug release were studied from the loxoprofen-EVA matrix. The solubility of loxoprofen was highest at 40% (v/v) PEG 400. The release rate of drug from drug-EVA matrix increased with increased loading dose and temperature. The release rate was proportional to the square root of loading dose. The activation energy (Ea), which was measured from the slope of log P versus 1000/T, was 5.67 kcal/mol for a 2.0% loaded drug dose from the EVA matrix. Among the plasticizer used, diethyl phthalate showed the highest release rate of loxoprofen. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the greatest enhancing effect. In conclusion, for the enhanced controlled transdermal delivery of loxoprofen, the application of the EVA matrix containing plasticizer and penetration enhancer could be useful in the development of a controlled drug delivery system.