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  • 1
    Electronic Resource
    Electronic Resource
    Preparation and properties of the immunoconjugate composed of anti-human colon cancer monoclonal antibody and mitomycin C-dextran conjugate (1992)
    s.l. : American Chemical Society
    Bioconjugate chemistry 3 (1992), S. 132-137 
    Details
    ISSN: 1520-4812
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/bc00014a007
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  • 2
    Electronic Resource
    Electronic Resource
    Effect of plasma protein binding on drug disposition in muscle tissue: Application of statistical moment analysis and network theory toin situ local single-pass perfusion system (1988)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 16 (1988), S. 129-149 
    Details
    ISSN: 1573-8744
    Keywords: local perfusion system ; statistical moment theory ; drug disposition ; rabbit muscle tissue ; mitomycin C ; lipophilic derivative ; plasma protein binding ; network theory ; single-pass system analysis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The local disposition characteristics of mitomycin C (MMC) and five lipophilic prodrugs in rabbit hind leg muscle were examined using an in situ single-pass perfusion experiment. Test compounds inputted into a perfusion line as a rectangular function (unit pulse) were perfused with or without albumin and their outflow patterns were analyzed by statistical moment analysis. In interpretation of statistical moment parameters, the well-stirred model was applied to the local perfusion system based on the plate theory of a chromatographic system and some general pharmacokinetic parameters (the disposition parameters) were derived from the moments. A new theory which elucidates the relationships among the moments for plasma protein binding, unbound (free), and total drug fraction was established based on network theory. Using this system, the following conclusions were made for mitomycin C and its five lipophilic derivatives: (i) In the absence of albumin, an increase in lipophilicity led to an increase in organ clearance and distribution volume; (ii) drug bound to albumin did not transfer to the extravascular space; (iii) in the presence of albumin, an increase in lipophilicity results in a decrease in clearance.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01062256
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  • 3
    Electronic Resource
    Electronic Resource
    Disposition Characteristics of Protein Drugs in the Perfused Rat Kidney (1993)
    Springer
    Pharmaceutical research 10 (1993), S. 823-827 
    Details
    ISSN: 1573-904X
    Keywords: protein drugs ; rat kidney perfusion ; moment analysis ; glomerular and postglomerular permselectivity ; tubular reabsorption
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The renal disposition characteristics of 111In-labeled neocarzinostatin (NCS), soybean trypsin inhibitor (STI), and superoxide dismutase (SOD) were studied in the perfused rat kidney. In a single-pass indicator dilution experiment, venous and urinary recovery profiles and tissue accumulation of proteins were determined under filtering or nonfiltering conditions. In the nonfiltering kidney perfusion experiment, no significant tissue accumulation was observed, suggesting minimal uptake from the glomerular and peritubular capillary sides. Therefore, tissue recovery corresponded to that with tubular reabsorption after glomerular filtration. The total amount of NCS or STI being filtrated through glomeruli, the sum of tissue and urinary recoveries, was similar to that of inulin, but that of SOD was about half. Similarly, the steady-state distribution volumes (V d) of NCS and STI obtained by moment analysis of their venous outflow curves were similar to that of inulin, while the V d value of SOD was significantly lower. These results suggest the restricted passage of SOD through the glomerular and postglomerular capillary wall. The tubular reabsorption ratio of proteins against the total filtrated amount decreased with an increase in the administered dose, suggesting nonlinearity of reabsorption. SOD had the largest reabsorption ratio. Thus, this experimental system is useful for quantitative analysis of renal disposition of proteins.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1018996808153
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  • 4
    Electronic Resource
    Electronic Resource
    Characterization of LLC-PK1 Kidney Epithelial Cells as an in Vitro Model for Studying Renal Tubular Reabsorption of Protein Drugs (1995)
    Springer
    Pharmaceutical research 12 (1995), S. 1968-1972 
    Details
    ISSN: 1573-904X
    Keywords: LLC-PK1 cells ; renal protein reabsorption ; protein drugs ; adsorptive endocytosis ; chemical modification of protein drug
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. The purpose of this study was to assess whether LLC-PK1 renal epithelial cells could serve as an in vitro model for studying the renal tubular reabsorption of protein drugs. Methods. The association of 111In-labeled model protein drugs, bovine serum albumin (BSA), superoxide dismutase (SOD), soybean trypsin inhibitor (STI), and [Asu1,7]-eel calcitonin (Asu-ECT), with the monolayers of LLC-PK1 renal epithelial cells was characterized under various conditions. Results. The cellular association of these proteins was temperature-dependent and varied according to the protein. Saturation kinetics were observed for STI association, with the apparent Km and Vmax values determined to be 66.3 µg/ml and 250 ng/mg protein/min, respectively. The association of STI decreased with increases in medium pH from 5.4 to 8.4 and was inhibited significantly by 2,4-dinitrophenol, sodium azide, cytochalasin B, and colchicine, suggesting that the cellular association involved endocytosis. Mutual inhibition was observed in competitive binding experiments with the four protein drugs, suggesting that they shared a common binding site on the luminal membrane of LLC-PK1 cells. Taken together, these findings show that a variety of protein drugs bind to LLC-PK1 cells in a non-specific manner and possibly undergo endocytosis, a phenomenon that is similar to in vivo proximal tubular reabsorption. Conclusions. LLC-PK1 renal epithelial cells would be a suitable model system for the study of the renal proximal tubular reabsorption of protein drugs.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1016256325921
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  • 5
    Electronic Resource
    Electronic Resource
    Synthesis and Pharmacokinetics of a New Liver-Specific Carrier, Glycosylated Carboxymethyl-Dextran, and Its Application to Drug Targeting (1993)
    Springer
    Pharmaceutical research 10 (1993), S. 1253-1261 
    Details
    ISSN: 1573-904X
    Keywords: drug targeting ; sugar recognition ; glycosylated dextran ; pharmacokinetics ; cytosine β-D-arabinoside
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract To develop a new carrier system for hepatic targeting, carboxymethyl-dextran (CMD) was modified with galactose and mannose residues (Gal-CMD, Man-CMD), and their disposition characteristics were studied in mice using 14C-labeled dextran. At a dose of 1 mg/kg, i.v.-injected Gal-CMD and Man-CMD rapidly accumulated in the liver parenchymal and nonparenchymal cells, respectively, because of their preferential uptake via carbohydrate receptors in these cells. Pharmacokinetic analysis revealed that their uptake rates were sufficiently large for selective drug targeting. Targeting of cytosine β-D-arabinoside (araC) was studied using Gal-CMD as a specific carrier to the hepatocytes. From the conjugate of araC with Gal-CMD, araC was released with a half-life of 36 hr in phosphate buffer (pH 7.4) and 23 hr in plasma. An in vivo biodistribution study demonstrated a disposition profile of the conjugated araC similar to that of the carrier, and selective delivery to hepatocytes of up to 80% of the dose was achieved. These findings suggest that glycosylated CMDs are carriers with a high affinity to liver parenchymal or nonparenchymal cells without any affinity to other tissues.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1018949109004
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  • 6
    Electronic Resource
    Electronic Resource
    Design for Cell-Specific Targeting of Proteins Utilizing Sugar-Recognition Mechanism: Effect of Molecular Weight of Proteins on Targeting Efficiency (1995)
    Springer
    Pharmaceutical research 12 (1995), S. 209-214 
    Details
    ISSN: 1573-904X
    Keywords: protein targeting ; sugar recognition ; pharmacokinetics ; molecular weight ; liver
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Hepatic targeting of proteins utilizing the sugar-recognition mechanism was investigated in mice after intravenous injection. Five proteins with different molecular weights, i.e., bovine γ-globulins (IgG), bovine serum albumin (BSA), recombinant human superoxide dismutase (SOD), soybean trypsin inhibitor (STI), and chicken egg white lysozyme (LZM), were modified with 2-imino-2-methoxyethyl 1-thiogalactoside to obtain galactosylated proteins (Gal-IgG, Gal-BSA, Gal-SOD, Gal-STI, and Gal-LZM). The numbers of galactose residues were 38, 20, 11, 6, and 5 for Gal-IgG, Gal-BSA, Gal-SOD, Gal-STI, and Gal-LZM, respectively. All galactosylated proteins were dose-dependently taken up by the liver and the relative amount accumulated in the liver was decreased with an increase of the administered dose. At low doses (0.05 and 0.1 mg/kg), Gal-IgG, Gal-BSA, and Gal-SOD could be taken up by the liver up to more than 70–80% of dose within 10 min after intravenous injection, but the maximum amounts accumulated in the liver were approximately 40 and 30% of the dose for Gal-STI and Gal-LZM, respectively. Pharmacokinetic analysis revealed that the hepatic uptake clearance (CLliver) was quite different around the molecular weight of 32 kDa and correlated with the amount delivered to the liver; Gal-IgG, Gal-BSA, and Gal-SOD has a large CLliver that is close to the hepatic plasma flow rate (85 ml/hr), whereas those of Gal-STI and Gal-LZM were approximately 10 ml/hr at low doses. As for the total amount accumulated in the liver, high glomerular filtration rate of Gal-STI and Gal-LZM was also shown to cause insufficient delivery to the liver apart from being caused by their low CLliver.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1016222808484
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  • 7
    Electronic Resource
    Electronic Resource
    Statistical moments and disposition parameters in a local perfusion system under mammillary nonequilibrium condition (1990)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 18 (1990), S. 449-458 
    Details
    ISSN: 1573-8744
    Keywords: statistical moment analysis ; nonequilibrium condition ; local perfusion system ; two-compartment perfusion model ; peripheral elimination ; dispersion ratio ; steady state distribution volume ; mean elimination time ; intrinsic clearance
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Application of the statistical moment analysis to the local organ perfusion system leads moment parameters (moments) from the venous outflow concentration-time curve (dilution curve) of drug after its intraarterial bolus injection. By introducing the chromatographic concept and the network theory, we had defined the disposition parameters such as steady state distribution volume, mean elimination time, and intrinsic clearance from moments based on the well-stirred model. In this paper, discussion was expanded to general two-compartment organ perfusion models and the meanings of these disposition parameters in them were investigated. The relationship between compartmentally defined microconstants and moments-oriented disposition parameters was examined and the effect of the nonequilibrium (mainly peripheral elimination) condition on the latter was discussed. The possible utility of the disposition parameters as noncompartmental indications of drug disposition characteristics was suggested.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01061704
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  • 8
    Electronic Resource
    Electronic Resource
    An application of water-in-oil and gelatin-microsphere-in-oil emulsions to specific delivery of anticancer agent into stomach lymphatics (1977)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 5 (1977), S. 241-255 
    Details
    ISSN: 1573-8744
    Keywords: drug delivery system for cancer chemotherapy ; anticancer agent ; water-in-oil emulsion ; microsphere-in-oil emulsion ; stomach wall ; improvement of availability in the lymphatics ; prolonged release ; reduction of adverse effect ; adjuvant chemotherapy
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The efficiency of water-in-oil (W/O) and gelatin-microsphere-in-oil (W/O-G) emulsions as drug delivery systems for achieving specificity into lymphatics was evaluated in the rat stomach. Following injection into the stomach wall, radioactivities of 131 I-labeled o-iodohippuric acid (IH, watersoluble model compound) and [ 14 C]tripalmitin (TP, tracer of oil) in blood, regional lymph nodes, thoracic lymph, and stomach were determined. Since increased transfer of TP indicated the facilitation of lymphatic transport of IH following injection of W/O and W/O-G emulsions, the existence of a special transport mechanism through which drug and oil are delivered together was confirmed for this injection site. W/O and W/O-G emulsions increased the concentration-time curve (AUC) of IH in the regional lymph nodes (1.7 and 5.5 times that of aqueous solution injection, respectively), so the improvement of bioavailability was accomplished. In addition, a prolonged release of IH and decrease of its maximum blood concentration were obtained following injection of W/O-G emulsion. These results suggest that W/O and W/O-G emulsions satisfy many of the criteria of an ideal drug delivery system for cancer chemotherapy. An abundant supply of lymphatic vessels in the stomach wall exhibited the efficiency of these delivery systems more clearly than did thigh muscle.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01065398
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  • 9
    Electronic Resource
    Electronic Resource
    Role of intramuscular administration of water-in-oil emulsions as a method for increasing the delivery of anticancer to regional lymphatics (1977)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 5 (1977), S. 225-239 
    Details
    ISSN: 1573-8744
    Keywords: drug delivery system ; anticancer agent ; water-in-oil emulsion, gelatincontaining water-in-oil emulsion ; intramuscular injection ; lymph nodes ; enhanced delivery into the lymphatic system ; sustained release
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Further work was undertaken to clarify the mechanism of enhanced delivery of anticancer agents into rat lymph nodes by water-in-oil (W/O) emulsions. Radiolabeled [ 131 I] iodohippuric acid (IH, watersoluble model compound) and [ 14 C]tripalmitin (TP, tracer of oil) were administered intramuscularly, and radioactive concentrations in blood, lymph nodes, and muscles were determined. Also, a new type of emulsion, gelatin-containing W/O (W/O-G) emulsion, was manufactured to be used as a delivery system for the anticancer agents. It was found that the rate of transfer of TP into lymph nodes was enhanced in the following order: oil, oil-in-water (O/W) emulsion, W/O emulsion, and W/O-G emulsion. The transfer of IH into lymph nodes was enhanced more effectively by W/O-G emulsion. The results of this study suggest the existence of a special transport mechanism through which drug and oil are delivered together.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01065397
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  • 10
    Electronic Resource
    Electronic Resource
    A new method for assessment of drug disposition in muscle: Application of statistical moment theory to local perfusion systems (1985)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 13 (1985), S. 609-631 
    Details
    ISSN: 1573-8744
    Keywords: local perfusion system ; statistical moment theory ; drug disposition ; rabbit muscle tissue ; mitomycin C ; lipophilic derivative ; tissue distribution ratio ; mean elimination time ; dispersion ratio
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A new experimental system is used to determine exact information concerning local drug disposition. Rabbit hind leg is perfused in situusing a single-pass technique, and outflow curves of drugs are analyzed using statistical moment theory. By the introduction of Chromatographic concepts and the application of the well-stirred model to the local perfusion system, physiologically and/or physicochemically meaningful parameters are derived from the first three moments. Moreover, in the assessment, drug disposition is divided into elimination and distribution. The elimination process is also evaluated with respect to rate and extent. This system is used to elucidate the disposition characteristics of mitomycin C and its lipophilic derivative nonyloxycarbonyl mitomycin C.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01058904
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