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김수경,권지윤 대한생물치료정신의학회 2003 생물치료정신의학 Vol.9 No.1
선택적 세로토닌 재흡수 억제제(selective serotonin reuptake inhibitors : SSRIs)에 속하는 우울증 치료제들이 TCA나 heterocyclic 항우울제(제2 세대 및 제3세대 약물) 등과 같은 우울증 치료제에 비하여 전반적으로 효과가 우수하지는 않지만 독성이 적기 때문에 1990년 이후부터 널리 사용되어 왔다. 우울증이 단일증상으로 나타날 수도 있지만 여러 가지 질병과 복합되어 있는 경우에 우울증치료제는 흔히 다른 약물과 병합요법으로 사용된다. 따라서 SSRIs계 약물과 병합 투여에 의하여 나타날 수 있는 약력학 및 약동학적 약물상호작용을 고려하여 치료에 임하는 것이 매우 중요하다. SSRIs계 약물은 선택적으로 serotonergic transmission에 영향을 미치는 약리작용을 갖고 있기 때문에 약력학적 약물상호작용은 그리 광범위하게 나타나지 않지만 교감신경 효현제 또는 일부 발효식품이나 타이라민이 함유된 음료 등과 병합 투여했을 경우 고혈압의 위험이 초래될 수 있으며 매우 위험한 상호작용으로 세로토닌 증후군(serotonin syndrome)이 나타날 수 있다. 이 증후군은 고열, 근육경직, 간대성근경련 등을 포함하는 급격한 증상으로 때로는 사망을 초래할 수도 있기 때문에 반드시 유념해야 할 상호작용이다. SSRIs계 약물은 cytochrome P450(CYP) 효소계를 다양하게 억제하므로 이들 약물에 의한 약동학적 약물 상호작용은 광범위하게 여러 종류의 약물에서 나타날 수 있다. 특히 fluoxetine과 paroxetine은 CYP2D6를 강력하게 억제하고 fluvoxamine은 CYP3A4를 강력하게 억제하므로 이 효소계를 대사과정에서 이용하는 약물들과 병용할 때에는 특별한 주의가 필요하다. 그러나 SSRIs계 약물 중에서 citalopram이나 sertraline은 serotonin에 대한 선택성이 보다 우수하면서도 CYP에 대한 억제작용이 미약하여 약동학적 상호작용이 적게 나타나므로 이 점에 있어서 병합요법제로 비교적 안전하게 선택되고 있다. Since the 1990s, selective serotonin reuptake inhibitors(SSRIs) have been increasingly to treat depression because of their relatively fewer adverse effects and lower toxicity than older compounds such as tricyclic antidepressants(TCAs) and monoamine oxidase inhibitors(MAOIs). Polyharmacy, by several factors such as diseases, genetic constitution, diet, and age-related physiological changes may induce drug interactions predisposed to adverse effects. SSRIs have a low potential for pharmacodynamic drug interactions because they have more selective mechanism of action than older antidepressants. However, a serious pharmacodynamic drug interaction with SSRIs, serotonin levels. SSRIs can have potential pharmacokinetic interactions due to their seletive inhibitory action on cytochrome P450(CYP) isoenzymes, especially fluoxetine, paroxetine, paroxetine,and fluvoxamine. Therefore, these agents should be closely monitored or avoided in patients treated with substrates of the same isoenzyme. However, citalopram and sertraline have less inhibitory effects on different CYP drug metabolizing enzymes and offer more favorable drug interacton profile. This review provides evidence of potential drug ineractions of individual SSRIs. This study may help to guide safe and efficacious care to patients.
정용진,서권일,이기동,윤광섭,강미정,김광수 동아시아식생활학회 1998 동아시아식생활학회지 Vol.8 No.1
To utilize deteriorated sweet persimmon effectively, response surface methodology(RSM) was used to determine the optimal vinegar fermentation conditions and monitored by a divided two stage fermentation. The optimum conditions for maximum alcohol content were obtained when the first stage (alcohol fermentation) was carried out with an initial sugar concentration of 18.5°Brix, agitation rate of 140.8 rpm, fermentation time of 127.6 hr. When sugar concentration was 14°Brix, maximum alcohol content(7.1%) was predicted at fermentation conditions of 160 rpm in agitation rate, 140 hr in fermentation time. The optimum conditions for maximum acidity were obtained when second stage(vinegar fermentation) was carried out 249.5 rpm in agitation rate, 148.8 hr in fermentation time. Predicted values at the optimum conditions were similar to experimental values.
Gee-youn Kwon,Soo-kyung Kim 대한생리학회-대한약리학회 2001 The Korean Journal of Physiology & Pharmacology Vol.5 No.6
<P> The existence of opioid receptors in mammalian cerebellum except human, has not been clearly understood. In the present study, we found that NPY was inducible by morphine in the mouse cerebellar granular and Purkinje cell layers. We performed in situ RT-PCR and immunohistochemistry to characterize the NPY expression. The increase of NPY gene expression by morphine (30 mg/kg, i.p.) was inhibited by pretreatment with not only naloxone (100 mg/kg, i.p.) but also a noncompetitive NMDA antagonist, MK-801 (0.3 mg/kg, i.p.). The competitive NMDA antagonist, AP-5 (0.9 mg/kg, i.p.) slightly attenuated the increased NPY expression by morphine. Also, the finding similar to morphine was shown by NMDA (70 mg/kg, i.p.) treatment. Our results indicate that NPY was inducible by morphine and this might reflect activation of NMDA receptors in granule cells that relay mossy fiber inputs to Purkinje cells <I>via</I> parallel fibers.
Neuroprotection of Lithium is Associated with Inhibition of Bax Expression and Caspase 8 Activation
Gee-youn Kwon,Soo-kyung Kim 대한생리학회-대한약리학회 2001 The Korean Journal of Physiology & Pharmacology Vol.14 No.5
<P> Neuroprotective properties of lithium were investigated by using <I>in vivo</I> NMDA excitotoxicity model. The appearance of TUNEL positive cells was prominent within 24 h of NMDA (70 mg/kg, i.p.) injection in the regions of the cortex, hippocampal formation, and thalamus of mouse cerebrum. NMDA treatment resulted in the extensive enhancement of Bax immunoreactivity in the cortical and hippocampal regions. NMDA also increased the immunoreactivity of caspase 8 in the similar regions of the mouse cerebrum. However, the increased immunoreactivity of Bax and caspase 8 were dramatically attenuated by chronic lithium pretreatment (lithium chloride, 300 mg/kg/d, i.p. for 7∼10 days). At the same time, lithium ion blocked the appearance of TUNEL positive cells, and the morphological assessment indicated an effective neuroprotection by lithium against NMDA excitotoxicity. Although the exact action mechanism of lithium is not straightforward at this time, we propose that the inhibition of Bax and caspase cascade is involved in the neuroprotective action of lithium.
( Youn Gee Seo ),( Dong Wuk Kim ),( Abid Mehmood Yousaf ),( Jong Hyuck Park ),( Pahn Shick Chang ),( Hyung Hee Baek ),( Soo Jeong Lim ),( Jong Oh Kim ),( Chul Soon Yong ),( Han Gon Choi ) 영남대학교 약품개발연구소 2015 영남대학교 약품개발연구소 연구업적집 Vol.25 No.-
To develop a novel self-nanoemulsifying drug delivery system (solid SNEDDS) with better oral bioavailability of tacrolimus, the solid SNEDDS was obtained by spray-drying the solutions containing the liquid SNEDDS and colloidal silica. Its reconstitution properties were determined and correlated to solid state characterisation of the powder. Moreover, the dissolution and pharmacokinetics in rats was done in comparison to the commercial product. Among the liquid SNEDDS formulations tested, the liquid SNEDDS comprised of Capryol PGMC, Transcutol HP and Labrasol (10:15:75, v/v/v) presented the highest dissolution rate. In the solid SNEDDS, this liquid SNEDDS was absorbed in the pores and attached onto the surface of the colloidal silica. Drug was present in the amorphous state in it. The solid SNEDDS with 5% w/v tacrolimus produced the nanoemulsions and improved the oral bioavailability of tacrolimus in rats. Therefore, this solid SNEDDS would be a potential candidate for enhancing the oral bioavailability of tacrolimus.
( Youn Gee Seo ),( Dong Wuk Kim ),( Woo Hyun Yeo ),( Thiruganesh Ramasamy ),( Yu Kyoung Oh ),( Young Joon Park ),( Jung Ae Kim ),( Dong Hoon Oh ),( Sae Kwang Ku ),( Jin Ki Kim ),( Chul Soon Yong ),( J 영남대학교 약품개발연구소 2013 영남대학교 약품개발연구소 연구업적집 Vol.23 No.0
PURPOSE: To investigate the potential of thermosensitive and biadhesive nanomicelles in improving the bioavailability of docetaxel (DCT) and its chemotherapeutic effect. METHOD: DCT-loaded nanomicelles were prepared by emulsufication and characterized in terms of physico-chemical and visco-elastic parameters. The optimzed formulation was evaluated for in vivo localization, pharmacokinetic and anti-tumor efficacy. RESULTS: The hydrodynamic size of DCT-loaded nanomicelles was approximately 13 nm and thenanomicelles exhibited a sufficient gelation strength (9250 mPa·s) and bioadhesive force (2100 dyn/cm²) to be retained in the upper part of rectum. We observed a high rectal bioavailability of 29% DCT compared to that following oral administration in rats, as it successfully evaded the multidrug efflux transporters and hepatic first-pass metabolism. Plasma concentration around ∼50 ng/mL was maintained throughout the study period (12 h) while Taxotere® attained subtherapeutic range within 4 h of drug administration. Results also revealed that the rectally administered DCT-loaded nanomicellesexhibited a significant anti-tumor effect (200 mm³) with a reduced toxicity profile when compared to orally administered DCT (950 mm³). Furthermore, histological study showed that the rectal mucosa was completely intact with no signs of irritation upon treatment with DCT-loaded nanomicelles. CONCLUSIONS: Taken together, our novel thermosensitive and biadhesive nanomicellesdemonstrated the ability to improve the bioavailability and chemotherapeutic potential of DCT in vivo. To the best of our knowledge, this is the first report describing the rectal delivery of DCT-loaded nanomicelles.