• Title/Summary/Keyword: Cmax

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Mode of Action of Water Soluble β-Glucan from Oat (Avena sativa) on Calorie Restriction Effect In-Vitro and In-Vivo Animal Models (In-Vitro, In-Vivo 동물모델에서 귀리 유래 수용성 베타-글루칸의 칼로리 제한 효과 작용기전 규명)

  • Kang, Hanna;Kim, Se-Chan;Kang, Yong Soo;Kwon, Young-In
    • The Korean Journal of Food And Nutrition
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    • v.30 no.6
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    • pp.1222-1228
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    • 2017
  • In the current study, we investigated the inhibitory activity of water soluble ${\beta}-glucan$ from oat (Avena sativa) against various digestive enzymes such as ${\alpha}-glucosidase$, sucrase, maltase and glucoamylase. Inhibition of these enzymes involved in the absorption of disaccharide can significantly decrease the post-prandial increase of blood glucose level after a mixed carbohydrate diet. The ${\beta}-glucan$ had the highest documented rate of small intestinal sucrase inhibitory activity (2.83 mg/mL, $IC_{50}$) relevant for potentially managing post-prandial hyperglycemia. Furthermore, we evaluated the effects of ${\beta}-glucan$ on the level of post-prandial blood glucose in animal model. The post-prandial blood glucose levels were tested two hours after sucrose/starch administration, with and without ${\beta}-glucan$ (100, and 500 mg/kg-body weight). The maximum blood glucose levels (Cmax) of ${\beta}-glucan$ administration group were decreased by about 23% (from $219.06{\pm}27.82$ to $190.44{\pm}13.18$, p<0.05) and 10% (from $182.44{\pm}13.77$ to $165.64{\pm}10.59$, p<0.01) in starch and sucrose loading test, respectively, when compared to control in pharmacodynamics study. The ${\beta}-Glucan$ administration significantly lowered the mean, maximum, and minimum level of post-prandial blood glucose at 30 min after meal. In view of the foregoing, it is felt that our findings suggest that ${\beta}-glucan$ from oat serves to reduce post-prandial blood glucose rise secondary to slower absorption of glucose in the small intestine, via carbohydrate hydrolyzing enzymes inhibition.

Effect of Phenobarbital on the Pharmacokinetics of Rutaecarpine and its Metabolite in Rats

  • Kim, Ju-Hyun;Lee, Sang-Kyu;Seo, Young-Min;Choi, Jae-Ho;Shin, Sil;Kang, Mi-Jeong;Kim, Dong-Hyeon;Jeong, Hye-Gwang;Jahng, Yurng-Dong;Jeong, Tae-Cheon
    • Biomolecules & Therapeutics
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    • v.16 no.3
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    • pp.215-218
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    • 2008
  • To investigate the possible interaction between rutaecarpine and phenobarbital in rats, phenobarbital in saline at 80 mg/kg was given ip to male SD rats for 3 consecutive days. Saline was given to control animals. One day after phenobarbital pre-treatment, rutaecarpine at 16 mg/kg was administered through penile vein. Blood was collected and analyzed by using HPLC. The pharmacokinetic parameters were determined with the non-compartmental model. Pre-treatment with phenobarbital significantly altered the pharmacokinetic profiles of rutaecarpine and its metabolite, 10-hydroxyrutaecarpine. The AUC of rutaecarpine was reduced to approximately 50% of control and the plasma half-life of rutaecarpine was significantly shortened when compared with control. In addition, the Cmax of 10-hydroxyrutaecarpine was increased approximately 160% of control. The AUC and the plasma half-life of 10-hydroxyrutaecarpine were decreased to 76.9% of control and to 82.7 min from 175.9 min, respectively. The results suggested that phenobarbital might accelerate the metabolism of rutaecarpine, thereby changing the pharmacokinetic parameters of rutaecarpine in male SD rats.

Classification Method for Four Types of Obesity in Women (여성 비만의 유발유형 분류방법 연구)

  • 진승희;최경미;박영배
    • The Journal of Korean Medicine
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    • v.24 no.1
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    • pp.122-132
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    • 2003
  • Objectives: To effectively improve the treatment of obesity through oriental medicine and to prepare basic material for proper classification of different types of obesity. Methods: After deciding on four types of obesity based on 'DongYiBaoJian', a questionnaire consisting of 38 items was constructed to decide to which type an individual belonged. 212 women were asked to the complete the questionnaire. To verify that the cluster of four types of obesity was acceptable, a cluster analysis and a factor analysis were conducted as well as an evaluation on the distinction of each type. Also, a canonical discriminant analysis was done to categorize the individuals into one of four types of obesity. Results: 1. Developed a reliable questionnaire consisting of 38 items for the purpose of classifying four types of obesity. 2. Obesity types were divided into four groups. Type I was designated as GanChengPi (肝乘脾類型), Type II as PiWeiJuWang(脾胃俱旺類型), Type III as PiWeiJuXu (脾胃俱虛類型), and Type IV as Tan TanYin(痰飮類型). These types were verified and classified through the use of a cluster analysis as well as a factor analysis (p<0.05). 3. By the use of a questionnaire, four types of obesity were correctly classified with a hit ratio of 87.3%, 40.64% higher than the maximum chance criteria (Cmax) in unselected grouped. The hit ratios for obesity types I, II, III and IV were 93.3%, 93.3%, 78.6% and 50%(p<0.05). Conclusion: Further clinical research is necessary into the four types of obesity explored. By analyzing various test results, characteristics these types should be further explored.

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Optimal Sampling Times of Once Daily Gentamicin in Korean Patients with Urinary Tract Infections

  • Park, Hyo-Jung;Sohn, Kie-Ho;Choi, Kyung-Eob;Shin, Sang-Yup;Jung, Sook-In;Oh, Won-Sup;Peck, Kyong-Ran;Song, Jae-Hoon;Lee, Suk-Hyang
    • Biomolecules & Therapeutics
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    • v.11 no.3
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    • pp.178-182
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    • 2003
  • The clinical use of once daily aminoglycoside (ODA) dosing has been increased because of the potential therapeutic advantages of this dosing regimen. To evaluate the optimal sampling times of ODA dosing method in a clinical setting, the study was prospectively conducted in a total of 28 patients with UTI. All of the patients were intravenously administered gentamicin at a dose of 7 mg/kg over 60 minutes and randomly divided into two groups. Blood was collected at 0, 2, and 6 hours in Group A and at 1, 2, and 6 hours in Group B after the end of 1-hour infusion. The pharmacokinetic parameters (Ke, Vd and Cmax) obtained using the 0, 6 hour levels and 2, 6 hour levels in Group A were statistically different while those of 1, 6 hour levels and 2, 6 hour levels in Group B were similar. This finding indicated that the distributional phase of ODA is completed within 1 hour following the end of the I-hour infusion. If we are allowed to collect only two blood samples in ODA considering patients comfort and the analytical cost of drug, the first one should be drawn after 1 hour following the end of infusion to obtain adequate pharmacokinetic information.

Preparation and Bioavailability of Oriental Medicine containing Baicalin (II) : Gastro-Intestinal Absorption and Antibacterial Effect of Coprecipitated Product of Scutellariae Radix and Coptidis Rhizoma (바이칼린 함유 생약의 제제화 및 생체 이용률 (제 2보) : 황금 및 황련 공침물의 장내 흡수 및 항균 효과)

  • Yang, Jae-Heon;Kim, Dong-Su;Yoo, Hee-Doo;Lee, Nam-Hee
    • Journal of Pharmaceutical Investigation
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    • v.26 no.2
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    • pp.91-98
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    • 1996
  • Precipitation was formed during the preparation of decoction from a mixure of Scutellariae Radix and Coptidis Rhizoma or Phellodendri Cortex according to the prescription of Hwang-ryean-hae-dog-tang. Baicalin and berberine, the active ingredients of the two herbal medicine were identified in coprecipitated product. Pills were prepared using the coprecipitated product and various binders. The dissolution rate of baicalin and berberine from pills was increased in at pH1.2 when acacia or tragacanth was used. The absorption rate of baicalin from the coprecipitated product was faster than that from Scutellaria extract, but the absorption of berberine from CPP was slower in stomach, duodenum and jejunum of rats compared with Coptis extract. The time required for the maximum serum concentration (Cmax) of baicalin and berberine from CPP in mice were 150 and 200 min after oral administration, respectively. The maximum serum concentration of baicalin from CPP in mice was higher than Scutellaria extract, but the concentration of berberine was lower compared with Coptis extract. The minimum inhibitory concentration of CPP was below $50\;{\mu}g/ml$ against gram positive bacteria, and was higher than that against gram negative bacteria. The antibacterial activity of CPP was lower than that of herberine, but was more potent than Scutellaria extract. It was found that the inhibition rates of growth by CPP against S. epidermidis, K. pneumoniae, B. cereus and S.aureus were 60.0, 51.1, 45.4 and 39.9%, respectively.

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Studies of Pharmacological Activity on New Oral Cephalosporins (새로운 경구용 세팔로스포린의 약효평가)

  • La, Sung-Bum;Kim, Wan-Joo;Jee, Ung-Kil
    • YAKHAK HOEJI
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    • v.38 no.2
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    • pp.140-148
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    • 1994
  • ${\beta}-Lactamase$ stability, chemotherapeutic activity, and pharmacokinetics of 7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyridyl)piperazinyl]thiocarbonylthiomethyl-3-cephem-4-carboxylic acid(CEN1), 7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyrimidyl)piperazinyl]thiocarbonylthiomethyl-3-cephem-4-carboxylic acid(CEN2), pivaloyloxymethyl-7-[(Z)-2-(2-aminothizaole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyridyl)piperazinyl]thiocarbonyl-thiomethyl-3-cephem-4-carboxylate(CEN1P), and pivaloyloxymethyl-7-{(Z)--2-(2-aminothizaole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyridyl)piperazinyl]thiocarbonyl-thiomethyl-3-cephem-4-carboxylate(CEN2P) were examined. CEN1, CEN2, CEN1P, and CEN2P were very stable to the ${\beta}-lactamase$ obtained from three strains(Enterobacter cloacae P99, Escherichia coli TEM, and Citrobacter freundii). Chemotherapeutic activities$(ED_{50})$ of CEN2 and CEN2P against experimental systemic infections due to Streptococcus pyogenes 77A and Escherichia coli 078 were superior to those of CEN1 and CEN1P, respectively. The $ED_{50}$ values of CEN1, CEN2 were 5.82 mg/kg, 0.89 mg/kg(s.c., S. pyogenes 77A) while those of CEN1P, CEN2P were 14.56mg/kg, 6.40mg/kg(p.o., S. pyogenes 77A), respectively. The pharmacokinetics of CEN1, CEN2, CEN1P, and CEN2P were investigated in mice and rats. In mice, peak blood levels of $1.25\;{\mu}g/ml$ were recorded within 20 min after oral administration of a single dose equivalent to 40 mg/kg CEN1P. Cmax of CEN1P was much higher than that of CEN1 in mice and rats. Oral absorption of CEN2P was much higher than that of CEN2.

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In Vivo Antitumor Activities and Pharmacokinetics of DW2282 Depending on Vehicles (DW2282의 용매의존성 항암효과 및 약동력학)

  • Moon, Eun-Yi;Choi, Chung-Ha;Seong, Seung-Kyoo;Lee, Jin;Ryu, Jei-Man;Lee, Moon-Sun;Jung, Sang-Hun;Chung, Yong-Ho;Lee, Dog-Keun;Yoon, Sung-June
    • Biomolecules & Therapeutics
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    • v.6 no.4
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    • pp.395-399
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    • 1998
  • DW2282, (S)- (+)-4-phenyl -1-[N-(4-am mob enzoyl) -indolin-5- sulfonyl]-4,5- dihydro-2-imidazolone hydrochloride, is a novel anticancer agent thought to have an unique mechanism of action on the inhibition of tumor growth. In this study, we estimated in vivo antitumor activities and pharmacokinetics of Dw2282 depending on various vehicles. The inhibition rate of tumor growth was increased by 50, 100 and 200 mg/kg of Dw2282 in a dose-dependent manner. When Dw2282 dissolved in 4 sorts of vehicles was orally single dosed to rats at 50 mg/kg, Cmax of Dw2282 in 0.5% CMC.Na was a half as high as those in PG, PG+CP and PG+CP+DW. When Dw2282 was orally administered to mice for 5 days, antitumor activity of 130 mg/kg suspended in 0.5% CMC.Na was as effective as that of 65 mg/kg dissolved in the rest of vehicles. Taken together, it is thought that antitumor activities of Dw2282 are resulted from the absorption extent of it and related to the vehicle used.

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Effect of Gongjindon a Traditional Korean Polyherbal Formula, on the Pharmacokinetics Profiles of Donepezil in Male SDRats (1) -Single Oral Combination Treatment of Donepezil 10mg/kg with Gongjindan 100mg/kg within 5 min-

  • Chung, Dae-Kyoo;Kwon, Oh-Dae;Park, Soo-Jin;Lee, Young-Joon;Ku, Sae-Kwang
    • Journal of Society of Preventive Korean Medicine
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    • v.17 no.1
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    • pp.77-88
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    • 2013
  • Objectives : This study was aim to evaluate effects of pharmacodynamics and toxicity in combination therapy of donepezil with Gongjindan. Methods : After 10mg/kg of donepezil treatment, Gongjindan 100mg/kg was administered within 5 min. The plasma were collected at 30min before administration, 30min, 1, 2, 3, 4, 6, 8 and 24hrs after end of Gongjindan treatment, and plasma concentrations of donepezil were analyzed using LC-MS/MS methods. PK parameters of donepezil were analysis as compared with donepezil single administered rats. Results : Gongjindan markedly inhibited the absorption of donepezil regardless of sample time, from 30min to 8hrs after end of co-administration comparing with donepezil single treated rats. Especially the absorption of donepezil was significantly decreased at 2hrs after co-administration as compared with donepezil single treated rats, in the present study. Accordingly, the Cmax(-27.76%), $AUC_{0-t}$(-27.22%) and $AUC_{0-inf}$(-26.54%) of donepezil in co-administered rats were significantly decreased as compared with donepezil single treated rats, respectively. Conclusions : Based on the results of the present study, co-administration of Gongjindan decreases the oral bioavailability of donepezil by inhibiting the absorption. It is considered that the more detail pharmacokinetic studies should betested to conclude the effects of Gongjindan on the pharmacokinetics of donepezil, when they were co-administered, like the effects after co-administration with reasonable intervals considering the Tmax of donepezil and after repeated co-administrations.

Palmitoylpolysaccharide-coated Liposomes As A Potential Oral Drug Carrier (경구용 약물수송체로서의 팔미토일 치환 다당체로 코팅된 리포좀)

  • Hahn, Yang-Hee;Yi, Jung-Woo;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.24 no.2
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    • pp.73-83
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    • 1994
  • Applications of liposomes as a drug carrier for the oral delivery of poorly-absorbable macromolecular drugs have been limited, because of their instability in gastrointestinal environments including pH, bile salts, and digestive enzymes. Two polysaccharides, dextran(DX) and pullulan(PL), were introduced to the preformed liposomes in order to enhance the stability. Palmitoyl derivatives of polysaccharides, palmitoyldextran(PalDX) and palmitoylpullulan(PalPL), were synthesizd and introduced to the liposomes during preparation for the same purpose of stability. The effects of these polysaccharides coating were evaluated basically by physical properties of particle size distribution and optical microscopy, then compared with uncoated liposomes by the observations of both in vitro stability and in vovo absorption characteristics. The geometric mean diameters of polysaccharide-coated liposomes were greater than that of uncoated liposome, showing the outermost polysaccharide-coated layer under the optical microscopy. In vitro stabilities of uncoated or polysaccharides-coated liposomes were measured by turbidity changes in various pH buffer solutions containing sodium choleate as bile salts. While uncoated liposome was very sensitive to bile salts, polysaccharides-coated liposomes were stable in relatively higher concentrations of sodium choleate, giving the results of better stability of PalDX- and PalPL-coated liposomes than that of DX- and PL-coated liposomes. After liposomal encapsulation of acyclovir(ACV), an antiviral agent as a model drug, it has been administered orally to rats as dose of ACV 40 mg/kg. Plasma concentrations of ACV were assayed by HPLC and analyzed by model-independent pharmacokinetics. Pharmacokinetic parameters of Cmax, tmax, and [AUC] have been compared.

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Tandem Mass Spectrometry for the Quantification and Bioavailability Test of Nicorandil in Human Plasma (Tandem Mass를 이용한 혈중 니코란딜의 정량법 개발 및 생체이용률시험)

  • Moon Chul-Jin;Lee Eun-Hee;Yang Song-Hyun;Moon Hae-Ran
    • YAKHAK HOEJI
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    • v.49 no.3
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    • pp.225-229
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    • 2005
  • A rapid, sensitive and selective tandem mass spectrometric method (LC-MS/MS) for the quantitation of nicorandil in human plasma was developed. A bioavailability study of Sigmat tablet (5 mg nicorandil, Choongwae Co.) was per-formed using the validated LC-MS/MS method. The dose of 5 fig of nicorandil (1 tablet) was orally administered to 9 healthy Korean subjects. After administration, blood was taken at 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, and 24 hour. The validation data were as follows; the standard curve was linear ($r^2$=0.999) over the concentration range of $0.5\~200.0 ng/ml$. The coefficient of variation for intra- and inter-day assay were $3.55\~7.44$, and $2.17\~9.102\%$, respectively. The lower limit of quantification for nicorandil was 0.5 ng/ml. The pharmacokinetic parameters obtained were as follows; $AUC_t$ was 145.9$\pm$83.0 ng-hr/ml, Cmax was 83.8$\pm$32.2 ng/ml, $C_{max}$ was 0.42$\pm$0.13 hr, $K_e$ was 0.56$\pm$0.23 l/hr, and $t_{l/2}$ was 1.42$\pm$0.52 hr. Based on the validated analytical method and pharmacokinetic parameters, a standard guideline of the bioavailability test of nicorandil dos-age forms was prepared successfully and could be used for the bioequivalence test of nicorandil preparation.