• Journal of Pharmaceutical Investigation
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• 제9권3호
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• pp.1-8
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• 1979

The main route of metabolism of isonicotinic acid hydrazid (INH) in man is its conjugation with acetyl coenzyme A to form acetyl-INH. The reaction is catalyzed by an N-acetyl transferase in the liver. The acetylated drug can be excreted by the kidney more efficiently than INH, and the biological half-life of the drug in the body depends upon how rapidly the drug can be acetylated. This report measured the concentration of INH in the blood of 147 individuals 6 hours after they received a standard dose (9.8mg/kg) and plotted the data as a frequeney distribution hiotogram. There was bimodality, with a mean for one subpopulation at approximately $0.6{\sim}0.8\;mcg/ml.$, and a mean for the other subpopulation between 2.8 and 4.0mcg/ml. As might be expected slow acetylators of INH are more likely to develop a cumulative toxicity to the drug. The principle ,toxicity to INH is a peripheral neuritis but this adverse effect can be prevented by given extra pyridoxin to the patients, and the vitamin does not alter the antitubercular activity of INH. This report carried out that pyridoxine does not alter the ratio of free INH to the total INH in blood.

• 대한한방내과학회지
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• 제39권5호
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• pp.914-928
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• 2018

Objectives: This case report examines the effects of traditional Korean medicine for unspecified tremor with xerostomia caused by psychometric drug intake. Methods: A patient who suffered from unspecified tremor with xerostomia caused by psychometric drug intake was treated with acupuncture, pharmacopuncture, and traditional Korean medicine for 30 days. We provided the patient with herbal medicines including Ondam-tang-gagam (溫膽湯加減), Pumsimgieum-gagam (忿心氣陰加減), and Hoichunyanggyeok-san-gami (回春凉隔散加味). Symptoms were charted and evaluated using the Yin-deficiency questionnaire score, Yin-deficiency scale score, dry mouth symptom questionnaire, and visual analogue scale. Results: After treatment with Korean Medicine and pharmacopuncture, the frequency and degree of tremor has decreased, and degree of Xerostomia also improved. The Scores of Yin-deficiency questionnaire score, Yin-deficiency scale score, dry mouth symptom questionnaire, and visual analogue scale were also improved. And we could see reduction in the level of distribution of gastrointestinal heat at Digital Infrared Thermal Imaging test. The patient's Symtoms (Xerostomia as well as unspecified tremor) were improved after treated with Korean Medicine and pharmacopuncture. Conclusion: Korean medicine treatments may be valuable for xerostomia caused by psychometric drug intake.

• 대한수의학회지
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• 제30권4호
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• pp.413-420
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• 1990

The present study was conducted to investigate biochemical properties and antimicrobial drug susceptibilities of 47 strains of E rhusiopathiae isolated from the cases of acute septicemic swine erysipelas in Youngnam and Kyunggi provinces during the period from June 1988 to December 1989. The isolants were identified as E rhusiopathiae on the basis of cellular and colonial morphology, and characteristic reactions in some biochemical tests. All the organisms produced hydrogen sulfide in triple sugar iron agar and showed the characteristic "pipe cleaner" type of growth in gelatin stab cultures. The majority of biochemical and cultural properties of E rhusiopathiae isolated from pigs affected with acute erysipelas were identical to those of the reference strains employed. All the isolates were highly susceptible to penicillin G, ampicillin, erythromycin (MIC:0.025~0.39IU or ${\mu}g/ml$), and moderately susceptible to oleandomycin, oxytetracycline, chloramphenicol(MIC:$0.78{\sim}25{\mu}g/ml$). Kanamycin and sulfadimethoxine showed no activity against the isolates(MIC:>$400{\mu}g/ml$). The MICs of dihydrostreptomycin presented two distribution peaks; of 47 strains, 5(10.6%) were resistant to dihydrostreptomycin (MIC:$400{\mu}g/ml$), while the majority of them were susceptible to the drug.

• Journal of Chest Surgery
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• 제21권1호
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• pp.109-115
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• 1988

With the decreasing incidence of new cases and the highly effective results with antituberculous drug therapy, there is a marked decline in the need for surgery which was formerly such an important part in the successful program of management of this disease. During the period of two years and a half from Jun. 1984 to Dec. 1986, this study represents an analysis of 163 cases of several surgical management for eventual control of pulmonary tuberculosis at National Kon-ju tuberculosis Hospital. 1. Mode of surgical treatment was: Resection; 123 cases [Pneumonectomy: 83, lobectomy: 35, lobectomy plus segmentectomy; 4 segmentectomy: 1], thoracoplasty: 20 and others: 20. 2. Age distribution ranged 16and 68 with average of 34 years. Male and female ratio was 1.2: 1. 3. Surgical indications were: totally destroyed lung; 64, Destroyed lobe of segment; 13, cavity positive sputum; 10, cavity c negative Sputum; 6, Bronchostenosis c atelectasis; 2, empyema c or s BPF; 46, Aspergilloma; 8, Questions of Associated tumor; 4 and other 5. 4. Incidence of Complications was 10.4% and the mortality was 5.5 percent. The cause of mortality were analyzed. The main causes of death were respiratory insufficiency; 4, fulminant hepatitis; 1, hemorrhage; 1 and unknown; 1 in pneumonectomy, and asphyxia; 1 in lobectomy and sepsis; 1 in other procedure. 5. Conversion rare of positive sputum to negative state related to resectional surgery was 91.5%. In pneumonectomy, drug resistant group preoperatively showed 88.1% conversion rate postoperatively and drug sensitive group showed that 100% conversion rate. In lobectomy, both drug resistant and sensitive groups showed that 100% conversion rate postoperatively.

• Archives of Pharmacal Research
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• 제19권1호
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• pp.30-35
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• 1996

Poly(l-lactic acid)(PLLA) microspheres loaded with ampicillin sodium (AMP-Na_, .betha.-lactam antibiotic, were prepared by a w/o/w multiple emulsion-solvent evaporation method. The amounts of each component in three phases (inner water phase, organic phase, and outer water phase) wre carefully examined in the preparation of PLLA microspheres. The stirring rate, another preparation parameter, was also investigated for study on the effect of mechanical stress on the drug loading and morphology of PLLA microspheres. Most of the preparation parameters had a great influence on the drug loading, surface morphology and size distribution of PLLA microspheres. PLLA microspheres with 15.89 w/w% drug loading were subjected to the in vitro release experimet. The release of ampicillin sodium was constant at a rate of 1.68 $mug/ml/day$ per 1 mg of microspheres for 18 days initial burst effect.

• Macromolecular Research
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• 제11권5호
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• pp.382-386
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• 2003

Reductive amination of N-succinyl-chitosan (1) and lactose using sodium cyanoborohydride in 1/15 M phosphate buffer (pH 6.0) for 6 d was suitable for the preparation of lactosaminated N-succinyl-chitosan (2). At 8, 24 and 48 h after i.v. administration of fluorescently labeled 1 (1') or 2 (2'), Peyer's patch, mesenteric lymph nodes, testes, prostate, preputial grand, intestine (small intestine plus cecum), femoral muscle, backbone and peritoneum were taken. Peyer's patch and mesenteric lymph nodes were put together as lymph nodes. Over 10% of dose/g tissue was distributed to the prostate and lymph nodes at 48 h post-administration in both l' and 2'.2' was easily distributed into not only the liver but also prostate, intestine, preputial gland and lymph nodes. Although galactose receptors are known to exist not only on the liver parenchymal cells but also on prostate and testes, the selective distribution of 2' into the prostate and the testes were not observed clearly. This study suggested that 1 and 2 should have possibilities for both the prevention and cure of lymph node metastasis as drug carriers.

• 약학회지
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• 제57권6호
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• pp.412-419
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• 2013

Drug discovery and development processes are time consuming and costly endeavors. It has been reported that on average it takes 10 to 15 years and costs more than $ 1billion to bring a molecule from discovery to market. Compounds fail for various reasons but one of the significant reasons that accounts for failures in clinical trials is poor prediction/understanding of pharmacokinetics and drug metabolism in human. In an effort to improve the number of compounds that exhibit optimal absorption, distribution, metabolism, elimination (ADME), and pharmacokinetic properties in human, drug metabolism, pharmacokinetic scientists have been continually developing new technologies and compound screening strategies. Over the last few years, accelerator mass spectrometry (AMS) and its applications to preclinical/clinical pharmacokinetics and ADME studies have significantly increased, particularly for new chemical/biological entities that are difficult to support with conventional radiolabel studies. In this review, the application of AMS for micro-dosing, micro-tracer absolute bioavailability, mass balance and metabolite profiling studies will be discussed.

• 한국한의학연구원논문집
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• 제15권3호
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• pp.53-61
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• 2009

Oxytocin(OT), classically known to stimulate labour and milk ejection, contributes to play an important role in a wide range of behavioral effects including drug addiction. An increasing body of evidence suggests that OT ameliorates acute and long-term effects of commonly used drugs by means of interacting with the mesolimbic dopamine system. Mesolimbic dopamine system is thought to play a major role in the reinforcing properties of drug abuse. Oxytocin receptors in the nucleus accumbens(NAc) and ventral tegmental area(VTA) have been implicated in the regulation of reinforcing effects in abused drugs. In the same way acupuncture may attenuate the reinforcing effects of abused drugs in the NAc and VTA. We have an interest in similar liaison between the substrates of acupuncture and drug addiction that may involve OT. Here, we described the possibility that acupuncture modulates the reinforcing and sensitizing properties of abused drugs in the dopaminergic system via the regulation of activities in the oxytocinergic system. The elements in this paper are summarized as follows : neuroanatomical studies of oxytocinergic innervation and distribution of oxytocin receptors; experiments related to the methamphetamine, cocaine, morphine and ethanol; experiments related to the oxytocin and acupuncture.

• Archives of Pharmacal Research
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• 제29권7호
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• pp.605-616
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• 2006

A wide variety of drugs and endogenous bioactive amines are organic cations (OCs). Approximately 40% of all conventional drugs on the market are OCs. Thus, the transport of xenobiotics or endogenous OCs in the body has been a subject of considerable interest, since the discovery and cloning of a family of OC transporters, referred to as organic cation transporter (OCTs), and a new subfamily of OCTs, OCTNs, leading to the functional characterization of these transporters in various systems including oocytes and some cell lines. Organic cation transporters are critical in drug absorption, targeting, and disposition of a drug. In this review, the recent advances in the characterization of organic cation transporters and their distribution in the small intestine are discussed. The results of the in vitro transport studies of various OCs in the small intestine using techniques such as isolated brush-border membrane vesicles, Ussing chamber systems and Caco-2 cells are discussed, and in vivo knock-out animal studies are summarized. Such information is essential for predicting pharmacokinetics and pharmacodynamics and in the design and development of new cationic drugs. An understanding of the mechanisms that control the intestinal transport of OCs will clearly aid achieving desirable clinical outcomes.

• The Korean Journal of Physiology and Pharmacology
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• 제25권6호
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• pp.545-553
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• 2021

Fixed-dose combinations development requires pharmacokinetic drugdrug interaction (DDI) studies between active ingredients. For some drugs, pharmacokinetic properties such as long half-life or delayed distribution, make it difficult to conduct such clinical trials and to estimate the exact magnitude of DDI. In this study, the conventional (non-compartmental analysis and bioequivalence [BE]) and model-based analyses were compared for their performance to evaluate DDI using amlodipine as an example. Raw data without DDI or simulated data using pharmacokinetic models were compared to the data obtained after concomitant administration. Regardless of the methodology, all the results fell within the classical BE limit. It was shown that the model-based approach may be valid as the conventional approach and reduce the possibility of DDI overestimation. Several advantages (i.e., quantitative changes in parameters and precision of confidence interval) of the model-based approach were demonstrated, and possible application methods were proposed. Therefore, it is expected that the model-based analysis is appropriately utilized according to the situation and purpose.