• Biomolecules & Therapeutics
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• v.4 no.4
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• pp.301-309
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• 1996

LBD-001, a recombinant human interferon ${\gamma}$ produced by genetically engineered yeast as a host system, was intravenously administered to pregnant female rats (Sprague-Dawley) from day 7 to 17 of gestation at dose levels of 0.35$\times$10$^{6}$ , 0.69$\times$10$^{6}$ , and 1.38$\times$10$^{6}$ I.U./kg/day. As the control groups, hydrocortisone sodium succinate (5 or 10 mg/kg/day) was also similarly administered. Teratological effects of the test agents on fetuses and development of offsprings (F1 rats) were investigated. (1) No significant changes by the treatment of LBD-001 were observed in body weight, food and water consumption, feeding and nursing behaviors, and autopsy of pregnant or lactating mother rats. However, in hydrocortisone sodium succinate (10 mg/kg/day)-treated group, significant decreases of body weight on day 16, 18, and 20 of gestation and food consumption on day 20 of gestation and outstanding atrophy of thymus and adrenals were observed in two rats autopsied on day 20 of gestation. (2) No significant changes in resorption rate, skeletal or visceral development of fetuses, and physical or sensory development of offsprings (Fl) by the treatment of LBD-001 were detected. In hydrocortisone sodium succinate (10 mg/kg/day)-treated group, however, there were significant decreases of body weight of fetuses, delay of ossification, temporary delay of body weights of offsprings (F1) on day 1 and 3 of lactation, and increased tendency of stillborn rate and malformation rate of bone. The results show that LBD-001 at the dose of 1.38$\times$10$^{6}$ I.U./kg/day or less is not teratogenic in organogenesis of fetuses and the development of offsprings (F1). Meanwhile, hydrocortisone sodium succinate (10 mg/kg/day) seems to delay ossification of fetuses and temporarily retard the development of offsprings (Fl).

• Biomolecules & Therapeutics
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• v.25 no.6
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• pp.648-658
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• 2017

7-O-Succinyl macrolactin A (SMA) exerts several pharmacological effects including anti-bacterial, anti-inflammation, and anti-cancer activities. Recently, SMA has been extensively evaluated as an anti-cancer drug. Thus, the objectives of the present study were to characterise the pharmacokinetics of SMA via both non-compartmental and compartmental analysis in mice, rats, and dogs, and to derive an appropriate first-in-man dose based on allometric scaling of the animal data. The time courses of plasma SMA concentrations after intravenous administration to rats and dogs were analysed retrospectively, as were data collected after intraperitoneal SMA injection in mice. Pharmacokinetic parameters were estimated via both noncompartmental and compartmental analysis, and were correlated with body weight and/or the potential maximum life-span. The clearance and distribution volume of SMA in humans were predicted, and a first-in-man dose proposed. A two-compartment model best described the time courses of SMA plasma concentrations after a saturation elimination process was applied to fit the dataset obtained from rats. Incorporation of the maximum potential life-span during allometric scaling was required to improve the estimation of human clearance. The SMA clearance and the distribution volume in the steady state, in a 70-kg adult male, were estimated to be 30.6 L/h and 19.5 L, respectively. To meet the area under the curve (AUC) required for anti-tumour activity, a dose of 100 mg (~1.5 mg/kg) was finally proposed as the first dose for a 70-kg human. Although toxicological profiles derived from non-clinical studies must be considered before any final decision is made, our work will facilitate clinical studies on SMA.

• The Korean Journal of Nuclear Medicine
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• v.28 no.2
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• pp.214-219
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• 1994

The purpose of this study is to evaluate thallium scanning as a potential test in differentiating malignant from benign lesions of breast. Thirty-one female patients underwent thallium scan of the breast. After intravenous injection of 74-111 MBq(2-3 mCi)of thallium-201, anterior and lateral images were obtained. We compared thallium scans with pathological results. Of 11 patients with breat cancers, 10 cases(90.9%) were detected using thallium scan. Thallium scan obtained in one patient who had breast cancer but received several cycles of chemotherapy did not show thallium uptake. The smallest detectable cancer was 1.5cm in diameter. In contrast, there is no thallium accumulation in breasts of 17 of 20 patients with benign disease(85%). Three cases of 13 fibrocystic disease show thallium uptake in their breast. In conclusion, thallium scan is an effective test in differentiating benign from malignant lesion.

• Journal of the Korea Society of Computer and Information
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• v.12 no.2 s.46
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• pp.123-130
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• 2007

The aim of this study was to propose a fusion and registration method with heterogeneous small animal acquisition system in small animal in-vivo study. After an intravenous injection of $^{18}F$-FDG through tail vain and 60 min delay for uptake, mouse was placed on an acryl plate with fiducial markers that were made for fusion between small animal PET (microPET R4, Concorde Microsystems, Knoxville TN) and Discovery LS CT images. The acquired emission list-mode data was sorted to temporally framed sinograms and reconstructed using FORE rebining and 2D-OSEM algorithms without correction of attenuation and scatter. After PET imaging, CT images were acquired by mean of a clinical PET/CT with high-resolution mode. The microPET and CT images were fusion and co-registered using the fiducial markers and segmented lung region in both data sets to perform a point-based rigid co-registration. This method improves the quantitative accuracy and interpretation of the tracer.

• Korean Journal of Pharmacognosy
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• v.40 no.2
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• pp.128-136
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• 2009

This study was carried out to investigate the antidiabetic and antioxidative effect of Lycii fructus in the Streptozotocin(STZ)-induced diabetic rats. The effective fractions were prepared as a form of organic solvents of $CH_{3}(CH_{2})_{4}CH_{3}$ $CHCI_{3}$, EtOAc, BuOH and $H_{2}O$ fractions prepared from the EtOH extract of Lycii fructus and The diabetes were induced by an tail-intravenous injection of STZ with a dose of 45 mg/kg dissolved in citrate buffer. The various fractions of Lycii fructus were orally administrated once a day for 7 days. The contents of serum glucose, and triglyceride in the $CHCI_{3}$ fraction and hepatic lipid peroxidation in the EtOAc, BuOH and $H_{2}O$ fractions treated rats were significantly decreased when compared to those of the STZ-control group In addition, an activity of hepatic GST in the BuOH fraction treated rats was significantly increased compared to that of the STZ-control group. whereas, activities of hepatic catalase, GSH-Px in the BuOH fraction treated rats were significantly decreased compared to those of the STZ-control group. Meanwhile, The content of hepatic glycogen and avtivity of hepatic glucokinase in $CHCI_{3}$ fraction treated rats were significantly increased, but activity of glucose-6-pase was significantly decreased in the $CHCI_{3}$ fraction treated rats. In conclusion, these results indicated that the BuOH fraction of Lycii fructus was effective for the antioxidation, and also the $CHCI_{3}$ fraction of Lycii fructus was effective for the antidiabetes in the STZ-induced diabetic rats.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1998.11a
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• pp.154-155
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• 1998

Taurine, 2-aminoethanesulfonic acid is widely distributed in animal tissues and has a variety of biological activities. A recent worldwide study demonstrated beneficial effects of taurine on aging and age-associated disorders. In general, taurine levels in the brain decrease when an animal is subjected to pathologic conditions such as ischemia-anoxia and seizure. But taurine levels tend to increase in the brain in hypertention. In the present study, the blood-brain barrier BBB) transport of [$^3$H]taurine was compared between spontaneously hypertensive rats (SHR) and normotensive Sprague-Dawley rats (SD) using Internal artery carotid perfusion (ICAP) at a rate of 4$m\ell$/min for 10, 15 and 30 second. Calculated V$\_$D/, volume of distribution in brain, and PS, the permeability surface area product of [$^3$H]taurine through the BBB in SHR was a little lower than that in SD. PS for 15s is more higher than that of other seconds in both of them. It could be followed by taurine efflux back into blood after 15s. We also obtained pharmacokinetic parameters using intravenous injection of plasma volume marker, [$\^$14/C]sucrose and [$^3$H] taurine. PS value of [$^3$H]taurine in SHR (16.1 ${\pm}$ 2.9 ${\times}$ 10$\^$-3/ $m\ell$/min/g) was significantly higher than that in SD (7.4 ${\pm}$ 0.8 ${\times}$ 10$\^$-3/ $m\ell$/min/g). There is also significant difference for %ID/g in brain between SHR (0.195 ${\pm}$ 0.031) and SD (0.058 ${\pm}$ 0.003).

• Biomolecules & Therapeutics
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• v.5 no.4
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• pp.369-375
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• 1997

General pharmacological effects of SB-31$^{R}$, the extracts of Pulsatilla koreana, were investigated in mice, rats and guinea-pigs. Intravenous injection of SB-31 (3 and 6 ml/kg) produced almost no effect on central nervous system no effects on the general symptom and behaviors of mice, spontaneous locomotor activity, pentobarbital- induced sleeping time , rotared performance , electroshock and pentylenetertrazole -induced seizures, acetic acid-induced writhing and normal body temperature in mice. SB-31 showed little effects on the spontaneous movement of the isolated ileum and contraction induced by agonists in isolated ileum, suggesting no influence on autonomic nervous system. Administration of SB-31 also did not show any effect on blood pressure in conscious rats. However, a slight decrease in heart rate was observed at high doses (6 and 10 ml/kg) of SB-31 in conscious rats. Similarly, a slight increase in respiratory rate was observed at 6 m1/kg of SB-31 in anesthetized rats. SB-31 did not produce any effect at the dose of 3 ml/kg, but showed a tendency to increase the urinary volume at 6 ml/kg, and produced a decrease in urinary excretions of N $a_{+}$and $K_{+}$at 6 ml/kg. However, transport capacity within the gastrointestinal tract and the secretion of the gastric juice were not influenced by 6 ml/kg of SB-31. In conclusion, these results suggest that SB-31 did not pro-duce any acute effects on the central nervous system, autonomic nervous system, respiratory and circulatory systems, digestive system and kidney function at the dose of below 3 ml/kg.ml/kg.

• The Korean Journal of Nuclear Medicine
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• v.20 no.1
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• pp.25-31
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• 1986

This study was performed to establish normal hepatoscintiangiographic(HSA) pattern of hepatic blood flow and to investigate dynamic differential HSA findings of primary and metastatic carcinomas and abscess of the liver. HSA was carried out after intravenous bolus injection of 10 mCi of Tc-99m-phytate by obtaining sequential anterior images of 1-second exposure for 16 seconds. Observations included (1) baseline study of normal hepatic blood flow pattern by correlating with contrast angiogram, (2) time sequence phasing of normal HSA, and (3) analysis of altered patterns in primary and metastatic carcinomas and abscesses of the liver. Materials consisted of 20 normal subjects, 28 primary hepatocellular carcinomas, 16 metastatic carcinomas and 7 liver abscesses. Results were: (1) Normal HSA demonstrated 3 distinct phases of arterialization(AP), of arterial hepatogram(AHP), and of portal venous hepatogram(PVHP). The means of each phase were 5.3, 6.3 and 8.3 seconds, respectively. Portal vein could be seen in all but one of 20 normal subjects. (2) Pattern changes in diseases groups were early start of AP in carcinomas and very early start of AP in abscesses. AP became prolonged in all disease group. (3) Distinction between AHP was sharp in metastasis and abscesses but un sharp in primary hepatoma. Cold area or areas became vascularized in primary hepatoma but not in abscess. Cold areas of metastasis were inhomogeneously vascularized in late AP and throughout AHP and became relatively vascular as PVHP began. The cold area of abscess showed rim enhancement during AH and APH. These differences in HSA pattern were very useful in differential diagnosis of the diseases studied.

• The Korean Journal of Pain
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• v.8 no.1
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• pp.37-42
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• 1995

The intermittent injection of analgesics is a inadquate method for postoperative pain control. Recently a non-electroic, disposable and portable infusor (Boxter Two Day $Infusor^R$) has been developed which can deliver analgesics with 2 ml/h speed continuousely. The present study examined the effects of three methods of pain management on recovery in 306 patients undergoing elective surgery in Wonkwang University Hospital. Group 1 (n=106) received i.m. $Valentac^R$ on a PRN basis. Group 2 (n=100), initial 2 mg of bolus morphine was followed by 48 mg of continuous infusion. Group 3 (n=100), initial 2 mg of morphine followed by morphine 18 mg-ketorolac 120 mg. We evaluated an analgesic efficacy with NRS (numerical rating scale) at 12, 24, 36, 48, 60 and 72 hours after the operation. The side effects (nausea, vomiting, pruritus, sedation and respiratory depression) were evaluated. In group 1, we asked major concern before operation and efficacy of pain control with pain severity (no pain, mild pain, moderate pain, sever pain). The results were as follows: 1) Major concern before operation is pain (40%). 2) 53% of patients suffered pain in group 1. 3) Morphine and morphine-ketorolac infusion groups were superior to the i. m. ($Valentac^R$) group with respect to postoperative analgesia. 4) In group 3 (morphine-ketorolac), there was no pruritus and mild nausea and vomiting.

• Journal of Pharmaceutical Investigation
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• v.24 no.3
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• pp.131-137
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• 1994

Drug delivery system by the use of red blood cells was established to sustain the release of drugs in the circulatory system by the intravenous injection. The entrapment method by the preswelling technique was re-examined and evaluated for searching the new entrapping conditions without hemolysis. The addition of 4 volume of $0.6{\times}\;hank's$ balanced salt solution (HBSS) into 1 volume of 50% red blood cells suspension did not induce the hemolysis and change the hematocrit level in this experimental condition (within 15 min). Most of daunorubicin could be entrapped into red blood cells within 15 min. While the intracellular adenosine triphosphate (ATP) level followed by the entrapment was reduced to 86% of normal ATP level, the membrane fluidity and the shape factor of red blood cells were not altered. The release rate of daunorubicin from red blood cells was affected by the hemolysis under this condition. To maintain the intracellular ATP in red blood cells, the new reaction buffer was made With the addition of ATP and sodium pyruvate during the entrapment procedure because the hemolysis during the release test would reflect the loss of intracellular ATP that might result in the decrease of the viability in vivo. The addition of ATP raised the intracellular ATP level, which protect the hemolysis during the release test.