• Title/Summary/Keyword: Partition coefficient ($K_d$)

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The Role of Excipients in Iontophoretic Drug Delivery: In vitro Iontophoresis of Isopropamide and Pyridostigmine through Rat Skin and Effect of Ion-pair Formation with Organic Anions

  • Shim, Chang-Koo
    • Journal of Pharmaceutical Investigation
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    • v.23 no.3
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    • pp.41-50
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    • 1993
  • The iontophoretic delivery across rat skin of quaternary ammonium salts (isopropamide: ISP, pyridostigmine: PS), which are positively charged over a wide pH range, was measured ill vitro. The study showed that: (a) iontophoresis significantly enhanced delivery of ISP and PS compared to respective passive transport; (b) delivery of ISP and PS was directly proportional to the applied continuous direct current density over the range of $0-0.69\;mA/cm^2;$ (c) delivery of ISP and PS was also proportional to the drug concentration in the donor compartment over the range of $0-2{\time}l0^{-2}M:$ (d) sodium ion in the donor compartment inhibited the drug transport possibly due to decreasing the electric transference number of the drug; (e) delivery of ISP and PS increased as the pH of the donor solution increased over the pH range 2-7 suggesting permselective nature of the epidermis, and inhibition of the transference number of the drugs by hydronium ion; (f) some organic anions such as taurodeoxycholate, salicylate and benzoate which form lipophilic ion-pair complexes with ISP inhibited the delivery of ISP. The degree of inhibition by the organic anions was linearly proportional to the extraction coefficient $(K_e)$ of ISP from the partition system with each counteranion between phosphate buffer (pH 7.4) and n-octanol. For PS, however, taurodeoxycholate, but not salicylate and benzoate inhibited the iontophoretic delivery. It suggests that not only sodium ion and hydronium ion but also the counteranions which form lipophilic ion-pairs with quaternary ammonium drugs are not favorable components in formulating the donor solution of the drugs to achieve an effective iontophoretic delivery.

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Persistence of Fungicide Pencycuron in Soils (토양 중 살균제 Pencycuron의 잔류 특성)

  • An, Xue-Hua;An, Wen-Hao;Im, Il-Bin;Lee, Sang-Bok;Kang, Jong-Gook
    • The Korean Journal of Pesticide Science
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    • v.10 no.4
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    • pp.296-305
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    • 2006
  • The adsorption and persistence of pencycuron {1-(4-chlorobenzyl) cyclopentyl-3-phenylurea} in soils were investigated under laboratory and field conditions to in order to assess the safety use and environmental impact. In the adsorption rate experiments, a significant power function of relation was found between the adsorbed amount of pencycuron and the shaking time. Within one hour following the shaking, the adsorption amounts in the SCL and the SiCL were 60 and 65% of the maximum adsorption amounts, respectively. The adsorption reached a quasi-equilibrium 12 hours after shaking. The adsorption isotherms followed the Freundlich equation. The coefficient (1/n) indicating adsorption strength and degree of nonlinearity was 1.45 for SCL and 1.68 to SiCL. The adsorption coefficients ($K_d$) were 2.31 for SCL and 2.92 to SiCL, and the organic carbon partition coefficient, $K_{oc}$, was 292.9 in SCL and 200.5 inSiCL. In the laboratory study, the degradation rate of pencycuron in soils followed a first-order kinetic model. The degradation rate was greatly affected by soil temperature. As soil incubation temperature was increased from 12 to $28^{\circ}C$, the residual half life was decreased from 95 to 20 days. Arrhenius activation energy was 57.8 kJ $mol^{-1}$. Furthermore, the soil moisture content affected the degradation rate. The half life in soil with 30 to 70% of field moisture capacity was ranged from 21 to 38 days. The moisture dependence coefficient, B value in the empirical equation was 0.65. In field experiments, the half-life were 26 and 23 days, respectively. The duration for period of 90% degradation was 57 days. The difference between SCL and SiCL soils varied to pencycuron degradation rates were very limited, particularly under the field conditions, even though the characteristics of both soils are varied.

Establishment of Analytical Method for Dichlorprop Residues, a Plant Growth Regulator in Agricultural Commodities Using GC/ECD (GC/ECD를 이용한 농산물 중 생장조정제 dichlorprop 잔류 분석법 확립)

  • Lee, Sang-Mok;Kim, Jae-Young;Kim, Tae-Hoon;Lee, Han-Jin;Chang, Moon-Ik;Kim, Hee-Jeong;Cho, Yoon-Jae;Choi, Si-Won;Kim, Myung-Ae;Kim, MeeKyung;Rhee, Gyu-Seek;Lee, Sang-Jae
    • Korean Journal of Environmental Agriculture
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    • v.32 no.3
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    • pp.214-223
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    • 2013
  • BACKGROUND: This study focused on the development of an analytical method about dichlorprop (DCPP; 2-(2,4-dichlorophenoxy)propionic acid) which is a plant growth regulator, a synthetic auxin for agricultural commodities. DCPP prevents falling of fruits during their growth periods. However, the overdose of DCPP caused the unwanted maturing time and reduce the safe storage period. If we take fruits with exceeding maximum residue limits, it could be harmful. Therefore, this study presented the analytical method of DCPP in agricultural commodities for the nation-wide pesticide residues monitoring program of the Ministry of Food and Drug Safety. METHODS AND RESULTS: We adopted the analytical method for DCPP in agricultural commodities by gas chromatograph in cooperated with Electron Capture Detector(ECD). Sample extraction and purification by ion-associated partition method were applied, then quantitation was done by GC/ECD with DB-17, a moderate polarity column under the temperature-rising condition with nitrogen as a carrier gas and split-less mode. Standard calibration curve presented linearity with the correlation coefficient ($r^2$) > 0.9998, analysed from 0.1 to 2.0 mg/L concentration. Limit of quantitation in agricultural commodities represents 0.05 mg/kg, and average recoveries ranged from 78.8 to 102.2%. The repeatability of measurements expressed as coefficient of variation (CV %) was less than 9.5% in 0.05, 0.10, and 0.50 mg/kg. CONCLUSION(S): Our newly improved analytical method for DCPP residues in agricultural commodities was applicable to the nation-wide pesticide residues monitoring program with the acceptable level of sensitivity, repeatability and reproducibility.