• The Korean Journal of Pharmacology
• /
• v.16 no.2 s.27
• /
• pp.9-14
• /
• 1980

The influence of penicillin G infusion(7.5 units/min/kg) on the diuretic action of furosemide$(250{\mu}g/kg)$ in rabbits was studied to investigate the drug interaction between penicillin G and furosemide. The results were as follows: 1) There was no significant change in renal function in the penicillin G infused rabbits compared with the normal ratbit. 2) In comparison with the control group, a significant increase in ${\triangle}U_{flow},\;{\triangle}U_{Na}V,\;{\triangle}U-kV\;and{\triangle}U_{cl}V$ was noted by 30 minutes following the administration of furosemide in the penicillin G infused group. There was no significant difference in ${\triangle}C_{In},\;{\triangle}C_{PAH}$ between the two groups and ${\triangle}Na^+$ reabsorption rate was significantly decreased in the latter. The potentiating effect of penicillin G on the diuretic action of furosemide should be due to the increased luminal concentration of free form of furosemide, and it may be related to the competitive inhibition of plasma protein binding between the two drugs.

• Korean Journal of Clinical Pharmacy
• /
• v.15 no.1
• /
• pp.50-54
• /
• 2005

The purpose of this study is to investigate the effect of aspirin on the pharmacokinetics of pranoprofen by oral coadministration of pranoprofen (5 mg/kg) with aspirin (5, 10 and 20 mg/kg) in Sprague-Dawley rats. After oral coadministration of pranoprofen with aspirin, the area under the plasma concentration-time curves (AUC) of pranoprofen was increased significantly by 10 mg/kg (p<0.05) and 20 mg/kg (p<0.01) of aspirin coadministration, and peak concentrations ($C_{max}$) of pranoprofen was increased significantly by coadministration of 20 mg/kg aspirin (p<0.05) compared to pranoprofen alone. Relative bioavailabilities (RB${\%}$) of pranoprofen in coadmistration were higher (from 1.42 to 1.67 fold) than control. The half-lives ($t_{1/2}$) of pranoprofen in coadministration were increased significantly (p<0.05) by 20-mg/kg aspirin. Based on these results, we might be considered that the pharmacokinetics of pranoprofen would be affected by coadministration of aspirin, by inhibit its metabolism in the liver and the tubular secretion of the kidney with the same acidic property. It should take into consideration in dosage regimen of pranoprofen when coadministration of pranoprofen with aspirin in treatment of rheumatoid arthritis.

• The Journal of Korean Medicine
• /
• v.26 no.2 s.62
• /
• pp.195-200
• /
• 2005

Objecitves: Peel of Citrus unshiu (Rutaceae) has been used in traditional herbal prescriptions. Hesperidin and naringin contents of Citri Unshii Pericarpium were determined and compared to herbal prescriptions. Then, the different extractions from prescriptions are explained with traditional herbal theories. Methods: The herb and herbal prescriptions were extracted in boiled water. A quantitative analysis was made of hesperidin and naringin using HPLC with-reversed-phase CIS column and a UV detector at 204nm. Elution was carried out at 1.0ml/min with $38\%$ methanol. Results and Conclusions: The extract of Citri Unshii Pericarpium for 180 min was the better method for extracting naringin and hesperidin. The flavonoid contents in remedies are different among several traditional herbal prescriptions. The reason for the difference can be explained with traditional drug interaction theories.

• Journal of Korean Traditional Oncology
• /
• v.20 no.1
• /
• pp.11-21
• /
• 2015

Objectives : The cancer incidence and cancer burden is increasing. In addition, the use of botanical agents in cancer care is increasing. This article aims to review a research strategy for botanical agents. Methods : The clinical studies of anticancer botanical agents and the papers about clinical research methodology of botanical agents were reviewed. Results : In phase I study, safety confirmation, optimal dose determination and drug interaction study are important. Most botanical agents have low toxicity and some have non-monotone dose response. Therefore, dose-response curve must be evaluated separately from the dose-toxicity curve to determine optimal dose. Although anticancer botanical agents can't shrink tumor size rapidly, they do extend survival. So, in phase II study, response should be evaluated by the survival. Conclusions : Clinical research of botanical agents in cancer is different from traditional methods and strategies. Considering the characteristics of botanical agents and experimental mechanism is necessary in conducting botanical based clinical trials.

• Biomolecules & Therapeutics
• /
• v.21 no.5
• /
• pp.343-348
• /
• 2013

We investigated the inhibitory effects of hesperidin on melanogenesis. To find melanosome transport inhibitor from natural products, we collected the structural information of natural products from Korea Food and Drug Administration (KFDA) and performed pharmacophore-based in silico screening for Rab27A and melanophilin (MLPH). Hesperidin did not inhibit melanin production in B16F10 murine melanoma cells stimulated with ${\alpha}$-melanocyte stimulating hormone (${\alpha}$-MSH), and also did not affect the catalytic activity of tyrosinase. But, hesperidin inhibited melanosome transport in melanocyte and showed skin lightening effect in pigmented reconstructed epidermis model. Therefore, we suggest that hesperidin is a useful inhibitor of melanosome transport and it might be applied to whitening agent.

• Journal of Pharmaceutical Investigation
• /
• v.41 no.6
• /
• pp.323-329
• /
• 2011

In order to develop new protein carrier replacing poly(DL-lactic acid-co-glycolic acid) (PLGA) microspheres, succinylated pullulan acetate (SPA) was investigated to fabricate a long term protein delivery carrier. SPA microspheres loaded with lysozyme (Lys) as a model protein drug were prepared by a water/oil/water (W/O/W) double emulsion method. An acidity test of SPA copolymers after hydrolysis was performed to estimate the change of protein stability during releasing proteins from the microspheres. There was no pH change of SPA copolymers, but pH of PLGA polymers after hydrolysis was significantly decreased to around pH 2, indicating that the long-term stability of proteins released from SPA microspheres can be guaranteed. Loading efficiency of proteins into SPA microspheres was three times higher than those into conventional PLGA microspheres, indication of inducing stronger charge interaction between proteins and succinyl groups in SPA microspheres. Although initial burst behaviors were monitored in Lys-loaded SPA microspheres due to relatively strong hydrophilic succinyl segments in SPA microspheres, initial burst issues would be circumvented if the ratio of charge density of succinyl moieties and hydrophobic acetate groups is harmonically controlled. Therefore, in this study, a new attempt of protein delivery system was made and functional SPA was successfully confirmed as a new protein carrier.

• Journal of Pharmaceutical Investigation
• /
• v.36 no.3
• /
• pp.157-160
• /
• 2006

This study investigated the effect of clarithromycin on the pharmacokinetics of ambroxol in rats. The pharmacokinetic parameters of ambroxol in rats were determined after the oral administration of ambroxol (12 mg/kg) in the presence or absence of clarithromycin (5 or 10 mg/kg). Compared with the control (given ambroxol alone), coadministration of clarithromycin significantly (p<0.05 at 5 mg/kg; p<0.01 at 10 mg/kg) increased the area under the plasma concentration-time curve (AUC), peak plasma concentrations $(C_{max})$ and absorption rate constant $(K_a)$ of ambroxol. Clarithromycin increased the AUC of ambroxol in a dose dependent manner within the dose range of 5 to 10 mg/kg. The absolute bioavailability (AB%) of ambroxol in the presence of clarithromycin was significantly higher than that of the control (p<0.05 at 5 mg/kg; p<0.01 at 10 mg/kg), and the relative bioavailability (RB%) of ambroxol with clarithromycin was increased by 1.32-to 1.71-fold. However, there were no significant changes in time to reach peak concentration $(T_{max})$ and terminal half-life $(T_{1/2})$ of ambroxol in the presence of clarithromycin. Coadministration of clarithromycin enhanced the bioavailability of ambroxol, which may be due to the inhibition of intestinal and hepatic metabolism of ambroxol by CYP 3A4. Further studies for the potential drug interaction are necessary since ambroxol is often administrated concomitantly with clarithromycin in humans.

• CELLMED
• /
• v.5 no.4
• /
• pp.27.1-27.6
• /
• 2015

Literatures and experimental studies have shown that Prunella has an effect on anti-hypertension, however, its components are complicated, so that it is still difficult to clear the specific roles of its various components in blood pressure regulation in. So we decide to systematically study the anti-hypertension mechanism of Prunella. We integrated multiple databases and constructed molecular interaction network between the chemical constituents of Prunella Vulgaris and hypertension based on entity grammar systems model. The network has 262 nodes and 802 edges. Then we infer the interactions between chemical compositions and disease targets to clarify the anti-hypertension mechanism. Finally, we found Prunella could influence hypertension by regulating apoptosis, cell proliferation, blood vessel development and vasoconstriction, etc. Thus this study provides reference for drug development and compatibility, and also gives guidance for health care at a certain extent.

• Journal of Pharmaceutical Investigation
• /
• v.32 no.4
• /
• pp.327-330
• /
• 2002

Alginate based polymeric matrices were designed for controlled release and stabilization of cefaclor in gastrointestinal fluid. Cefaclor is known to be acid stable and subjected to be degraded at neutral and alkaline pHs. In order to achieve an effective release profile of cefaclor in gastrointestinal tract, a particular strategy in dosage form design should be required from the view point of maintaining its activity. The amphiphilic nature of cefaclor allowed its controlled release using ionic polymers based on ionic interaction between the drug and polymers. The thrust of this study was to develop a technique that delivers cefaclor keeping effective release rate in the intestinal tract. Considering the fast degradation of cefaclor in the intestinal fluid, the matrices were designed to release surplus amount of cefaclor. The alginate based matrices demonstrated increase in release rate in the simulated intestinal fluid, which was favorable to compensate the degraded portion of cefaclor. In addition, stabilization of cefaclor in the intestinal fluid was obtained by employing citric acid that provides an local acidic environment. The matrices might be valuably used for the development of an oral cefaclor dosage form.

• Journal of Microbiology and Biotechnology
• /
• v.11 no.3
• /
• pp.463-468
• /
• 2001

Cyclosophoraoses are a class of unbranced cyclic-(1longrightarrow2)-${\beta}$-D-glucans found in the Rhizobium species. Their unique cyclic structures and high solubility make them potent for inclusion complexation as a host for an insoluble guest molecule. A family of neutral cyclosophoraoses (DP 17-27) isolated from Rhizobium meliloti 2011 was used as a host for inclusion complexation with an insoluble guest drug, indomethacin. A high performance liquid chromatographic analysis indicated that the inclusion complexation of cyclosophoraoses greatly ehanced the solubility of indomethacin compared with ${\beta}$-cyclodextrin. The estimated value of the association constant of the complex in water for $\beta$-cyclodextrin and cyclosophoraoses was $523M^{-1} and 17,570M^{-1}$, respectively. NMR spectroscopy showed that the inclusion complex was characterized by the interaction of the indole ring moiety of indomethacin with the cavity of cyclosophoraoses.