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Enhanced dissolution rates of piroxicam from the ground mixtures with chitin or chitosan
Koh, Ik-Bae,Shin, Sang-Chul,Lee, Yong-Bok The Pharmaceutical Society of Korea 1986 Archives of Pharmacal Research Vol.9 No.1
To increase the dissolution rate of piroxicam, chitin and chitosan which are widely occurring biodegradable natural materials were used as drug carriers. The ground mixtures of piroxicam with chitin or chitosan were prepared by grinding in a ball mill. The dissolution rates of piroxicam from the ground mixtures were enhanced markedly than that from the physical mixtures or from intact piroxicam. The X-ray diffraction peaks disappeared in the ground mixture indicating the production of the amorphous form. The comparison of infrared spectra of the physical mixture and the ground minture showed an interaction such as association between the functional groups of piroxicam and chitin or chitosan in the molecular level. The weight losses in TGA curves shoed all the same patterns. However, in the ground mixture by DTA curve, the undothermic peak due to the fusion of piroxicam was disappeared indicating the different thermal property.
Koh,Ik Bae,Kim,Ok Seon,Lee,Yong Bok,Oh,In Joon,Lee,Yeong Woo 한국약제학회 1994 Journal of Pharmaceutical Investigation Vol.24 No.3
We have studied the iron uptake by the purified brush-border membrane vesicles (BBMVs) to determine the effect of fructose on the absorption of iron. BBMVs were prepared by the modified calcium precipitation method. The degree of purification was routinely assessed by the marker enzyme, alkaline phosphatase, and the functional integrity was tested by D-[1-³H]glucose uptake. The appearance of membrane vesicles was shown by transmission electron microscopy (TEM). The uptakes of complexes of labeled iron [^(59)Fe] with fructose and ascorbate were measured with a rapid filtration technique. The uptake rate and pattern of the two iron-complexes, Fe(III)-fructose and Fe(III)-ascorbate, were also observed. A typical overshooting uptake of D-glucose was observed with peak value of 2∼3 times higher concentration than that at equilibrium. This result was similar to other studies with BBMVs. TEM showed that the size of BBMVs was uniform and we can hardly find any contaminants. Fe(III)-fructose has the higher value of Vmax and the lower value of Km than those of Fe(III)-ascorbate, respectively. It may be concluded that D-fructose is more effective in promoting the iron absorption than ascorbate.
Enhancement of Dissolution Properties of Ketoprofen from Ground Mixtures with Chitin or Chitosan
Koh, Ik Bae,Shin, Sang Chul,Lee, Youg Bok 한국약제학회 1986 Journal of Pharmaceutical Investigation Vol.16 No.1
The ground mixtures of ketoprofen with chitin or chitosan were prepared by grinding in a ball mill to increase the dissolution rate. The ground mixture showed a faster and more enhanced dissolution rate than the physical mixture or intact ketoprofen. The X-ray diffraction peaks indicated the production of the amorphous form of ketoprofen in the ground mixture. An interaction, in the ground mixture, such as association between the functional groups of ketoprofen and chitin or chitosan might occur in the molecular level. The endothermic peak due to the fusion of ketoprofen disappeared in the ground mixture indicating the different thermal property. The co-grinding technique with chitin or chitosan provided a promising way enhancing the dissolution rate of practically insoluble drug.
그리세오풀빈-페노바르비탈 상호작용(I) -페노바르비탈 전처리 Rat에 있어서 그리세오풀빈의 생체내 동태-
고익배(Ik Bae Koh),신상철(Sang Chul Shin),이용복(Yong Bok Lee) 대한약학회 1986 약학회지 Vol.30 No.6
Effects of phenobarbital on the pharmacokinetics of griseofulvin were studied in rats. Phenobarbital was administered orally for five days at the dose of 75mg/kg/day. Absolute bioavaiability of oral griseofulvin was significantly(p<0.005) reduced but total clearance(CLs) was not changed by phenobarbital pretreatment. Absorption rate constant(Ka) and maximum plasma concentration(Cmax) were significantly(pmax) of griseofulvin was significantly(p<0.05) increased by phenobarbital pretreatment. Changed pharmacokinetics of griseofulvin seemed not to be due to induced enzyme activity by phenobarbital but to reduced GI absorption of griseofulvin.
고익배,이용복 한국약제학회 1987 Journal of Pharmaceutical Investigation Vol.17 No.1
Effects of phenobarbital pretreatment on the pharmacokinetics of enterohepatic recirculating griseofulvin were investigated by comparing normal to bile duct cannulated rats and also the effects of enhanced endogeneous bile flow on the absorption of griseofulvin were studied by means of in situ recirculation method in phenobarbital-pretreated rats. Phenobarbital was administered orally for five days at the dose of 75 ㎎/㎏/day. The influence of phenobarbital pretreatment on the absorption rate constant, area under the plasma concentration-time curve, maximum plasma concentration of orally administered griseofulvin was not found in bile duct cannulated rats. Decreased absorption clearance and apparent partition coefficient of griseofulvin in accordance with the amount of endogeneous bile juice seemed to be due to the decrease of thermodynamic activity of griseofulvin as bile forms the micelle with griseofulvin.
총수담관 결찰에 의한 간외 담즙분비정체가 흰쥐의 간기능에 미치는 영향에 대한 약물속도론적 분석
고익배,이용복,나은영,주은희,정숙진 한국약제학회 1995 Journal of Pharmaceutical Investigation Vol.25 No.3
In order to examine the effect of extrahepatic cholestasis induced by common bile duct ligation on the hepatic function, the pharmacokinetics of antipyrine and d-propranolol were investigated in rats. In addition, in an attempt to observe the degree of direct hepatic injury, light and electron microscopic observations and conventional pathologic test using serum were performed. Five days after common bile duct ligation, antipyrine(15 ㎎/㎏) and d-propranolol(3 ㎎/㎏) were intravenously administrated to the rats, respectively. The total clearances of antipyrine and d-propranolol were significantly(p<0.05) decreased. Because hepatic clearance of antipyrine poorly extracted by the liver and that of d-propranolol highly extracted by the liver are respectively dependent on the hepatic intrinsic clearance and the hepatic blood flow, it may be concluded that extrahepatic cholestasis following five days after common bile duct ligation decreased the hepatic intrinsic clearance and the hepatic blood flow. SGPT, SGOT, cholesterol, bilirubin(total bilirubin. direct bilirubin) and alkaline phosphatase were significantly increased(p<0.05). The proliferation of bile ducts was prominent, and degeneration and necrosis of hepatocytes were observed by light microscope. Also, ultrastructurally, bile canaliculi were containing the amorphous materials and losing microvilli. and SER and RER in hepatocytes were dilated and vacuolated.