• 약학회지
• /
• 제44권5호
• /
• pp.424-431
• /
• 2000

A biopharmaceutics drug classification system for correlation between in vitro dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling the rate and extent of drug absorption. The objective of this study was to assess whether in vitro dissolution profiles of immediate-release beta-blocker tablets can be correlated with intestinal membrane permeability and/or in vivo bioavailability In vitro dissolution of the beta-blocker tablets was examined using KP VII Apparatus II methods at various pH. Intestinal membrane permeability was determined in vitro using the diffusion chamber method. Bioavailablity parameters were cited from literatures. The dissolution profiles did not accurately represent the in vivo bioavailablity However there were good correlations between intestinal membrane permeability and log P (noctanol/buffer). The correlations obtained in this study indicated that in vitro diffusion chamber method could be used to predict intestinal absorption in vivo.

• 한국생물공학회:학술대회논문집
• /
• 한국생물공학회 2005년도 생물공학의 동향(XVII)
• /
• pp.1015-1016
• /
• 2005

• 대한약학회:학술대회논문집
• /
• 대한약학회 2000년도 춘계총회 및 학술대회
• /
• pp.197.1-197.1
• /
• 2000

• 대한약학회:학술대회논문집
• /
• 대한약학회 2001년도 Proceedings of the Pharmaceutical Society of Korea
• /
• pp.242.1-242.1
• /
• 2001

• 대한약학회:학술대회논문집
• /
• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
• /
• pp.213.2-213.2
• /
• 2002

• 한국임상약학회지
• /
• 제16권2호
• /
• pp.113-122
• /
• 2006

Purpose: A retrospective study was performed to assess the efficacy and tolerance of ${\beta}-blocker$ administration in patients with heart failure and diabetes. Method: Records of 164 patients who were treated for the heart failure condition more than a year were studied retrospectively. Patients were divided into 4 groups based on their diabetes(DM) status and the administration of ${\beta}-blockers$ ($DM+{\beta}-blocker$ group: 14, DM w/o ${\beta}-blocker$: 19, No DM + ${\beta}-blocker$: 62, No DM + no ${\beta}-blocker$: 69). All patients had been receiving conventional therapy such as digoxin, ACE-I, ARB, diuretics, nitrates, aspirin, anticoagulants or lipid-lowering agents. The primary endpoints (death and hospital admission) were recorded during 1 year period and hemodynamic factors (HR, LVEF, SBP, DBP) were obtained from all patient groups before and after 12 months of ${\beta}-blocker$ treatment. To evaluate toxicity of ${\beta}-blocker$, SCr, BUN, AST, ALT and Alkaline phosphatase were obtained. Result: There were less death and hospital admission in DM + ${\beta}-blocker$ group than in DM without ${\beta}-blocker$ group (p=0.014). Relative risk of hospital admission for $DM+{\beta}-blocker$ group over no DM group was 1.17. Long term ${\beta}-blocker$ administration was associated with an improvement of heart rate in patients with DM (P< 0.02) with no significant improvement of LVEF, SBP, DBP. in DM patient. In patient without DM, ${\beta}-blocker$ was associated with improvement in LVEF, HR and DBP (P<0.01, P<0.03), but not in SBP. The incidence of toxicity was similar between the four group with no significant difference. Conculsion: Treatment of heart failure patients with ${\beta}-blocker$ appears to be beneficial in terms of hospital admission event and several hemodynamic factors. The toxicities of ${\beta}-blocker$ treatment were not significant and the treatment is generally well-tolerated in most of the heart failure patients.

• The Korean Journal of Physiology and Pharmacology
• /
• 제6권1호
• /
• pp.1-7
• /
• 2002

Congenital Long QT syndrome (LQTs) is a relatively rare pathologic disorder but results frequently in sudden cardiac death. Of the six LQTs that have been clinically described, five have been worked out for their genetic and biophysical profile. Most are generated by mutations which cause a loss of function in two delayed $K^+$ currents, $i_{Ks}\;and\;i_{Kr}.$ One syndrome is generated by mutations in the $Na^+$ channel which causes essentially a gain of function in the channel. Clinically the syndromes are characterized by slowed repolarization of the cardiac ventricular action potential and the occurrence of typical arrhythmias with undulating peaks in the electrocardiogram, called Torsade de Pointes. Arrhythmias are initiated by early or delayed afterdepolarizations and continue as reentry. Triggers for cardiac events are exercise (swimming; LQT1), emotion (arousal; LQT2) and rest/sleep (LQT3). ${\beta}-blockers$ have a high efficacy in the treatment of LQT1 and LQT2. In LQT3 their use is questionable. The study of congenital LQTsyndromes is a remarkable example of how basic and clinical science converge and take profit of each other's contribution.

• Journal of Chest Surgery
• /
• 제48권3호
• /
• pp.220-224
• /
• 2015

A patient presented with loss of consciousness and conversion. During an exercise test, catecholaminergic polymorphic ventricular tachycardia (CPVT) resulted in cardiac arrest. He started taking medication (a beta-blocker and flecainide) and an implantable cardioverter defibrillator (ICD) was inserted, but the ventricular tachycardia did not resolve. Left cardiac sympathetic denervation (LCSD) was then performed under general anesthesia, and the patient was discharged on the second postoperative day without complications. One month after the operation, no shock had been administered by the ICD, and an exercise stress test did not induce ventricular tachycardia. Although beta- blockers are the gold standard of therapy in patients with CPVT, thoracoscopic LCSD is safe and can be an effective alternative treatment option for patients with intractable CPVT.

• The Korean Journal of Physiology
• /
• 제19권2호
• /
• pp.101-111
• /
• 1985

Transient inward current (TI) was studied by the two micro-electrode voltage clamp technique in the sinoatrial node of the rabbit. The author confirmed that in $10^{-6}$ M ouabain TI was found in the SA node and investigated the effects of ions, $(Na^+,\;K^+,\;Ca^{2+})$, $\beta-agonist$ (isoprenaline), local anesthetics (quinidine, lidocaine) and Ca-blockers ($Co^{2+}$, verapamil, diltiazem) on the TI recorded during depolarizing voltage clamp pulses to -40 and -20 mV. The results obtained were as follows ; 1) $10^{-6}M$ ouabain increased the frequency of sinus action potential and decreased the amplitude, especially overshoot of action potential. TI was induced by the depolarizing voltage clamp Pulses and the magnitude of the slow inward current (isi) decreased and the time course was slowed by the same depolarizing pulses. 2) 30% $Na^{+}$ and 24mM $K^+$ decreased by $10^{-6}M$ ouabain and 6 mM $Ca^{2+}$ and $10^{-7}M$ isoprenaline increased TI, $i_{si}$ and current oscillations. 3) Quinidine $(5\times10^{-7}M)$ reduced TI and $i_{si}$ but lidocaine $(10^6\;-10^5M)$ didn't reduced or increase TI. Current oscillations increased and isi decreased by lidocaine. 4) Ca-blockers decreased the amplitude and the frequency of sinus action potential. TI and $i_{si}$ decreased significantly but were not abolished completely at the concentrations used in this experiment. Verapamil and diltiazem had inhibitory action on TI in $2\times10^{-7}M$ concentration and showed very slow recovery after wasting out with normal Tyrode solution.

• Journal of Gastric Cancer
• /
• 제13권3호
• /
• pp.172-178
• /
• 2013

Purpose: The aims of this study were as follow: 1) to de scribe the expression status of estrogen receptor-${\alpha}$ and -${\beta}$ mRNAs in five gastric carcinoma cell lines; 2) to evaluate in vitro the effects of $17{\beta}$-estradiol and estrogen receptor antagonists on the proliferation of the cell lines. Materials and Methods: Detection of estrogen receptor-${\alpha}$ and estrogen receptor-${\beta}$ mRNA in five human gastric cancer cell lines (AGS, KATO III, MKN28, MKN45 and MKN74) was made by the reverse transcription-polymerase chain reaction system. To evaluate the effect of $17{\beta}$-estradiol and estrogen receptor antagonists on the proliferation of gastric cancer cell line, the cell lines which expressed both es trogen receptors were chosen and treated with $17{\beta}$-estradiol and estrogen receptor antagonists (methyl-piperidino-pyrazole and pyrazolo [1,5-a] pyrimidine). Cell proliferation was assessed with the methylthiazol tetrazolium test. Results: Estrogen receptor-${\alpha}$ and estrogen receptor-${\beta}$ mRNAs were expressed in three (KATO III, MKN28 and MKN45) and all of the five gastric cancer cell lines, respectively. At higher concentrations, $17{\beta}$-estradiol inhibited cell growth of MKN28, MKN45 and KATO III cell lines. Neither estrogen receptor-${\alpha}$ nor estrogen receptor-${\beta}$ antagonist blocked the anti-proliferative effect of $17{\beta}$-estradiol. Conclusions: Our results indicate that estrogen receptor-${\beta}$ mRNAs are preferentially expressed in gastric cancers and also imply that hormone therapy rather than estrogen receptor blockers may be a useful strategy for the treatment of estrogen receptor-${\beta}$ positive gastric cancer. Its therapeutic significance in gastric cancer are, however, limited until more evidence of the roles of estrogen receptors in the gastric cancer are accumulated.