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  • 1
    Electronic Resource
    Electronic Resource
    s.l. : American Chemical Society
    The @journal of organic chemistry 40 (1975), S. 385-386 
    ISSN: 1520-6904
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1573-904X
    Keywords: Peyer’s patches ; absorption ; degradation ; polypeptide ; dipeptide ; endocytosis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The permeability of peptides across rabbit jejunal epithelium (JE) and Peyer’s patches (PP) was compared. Kyotorphin (L-tyrosyl-L-arginine) was almost completely hydrolyzed during its membrane transport in both PP and JE, but [D-Arg2] Kyotorphin (L-tyrosyl-D-arginine) was less hydrolyzed in PP than in JE. Since the permeability of intact [D-Arg2] Kyotorphin was almost equal in PP and JE, no superiority of PP to JE was found for dipeptide transport. More intact fluorescein isothiocyanate (FITC)-labeled bovine serum albumin (FITC-BSA) and concanavalin A (FITC-Con A) were transported in PP than in JE. At both absorption sites, the transport of the intact FITC-Con A was superior to that of the intact FITC-BSA. Colchicine significantly reduced the total transport of the intact and degradation forms of both peptides and the reduction ratio was greater in PP than in JE. Accordingly, it was suggested that PP can be used as prominent absorption sites for polypeptides since they have lower peptidase activity and higher endocytosis activity than JE.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1573-904X
    Keywords: granulocyte colony-stimulating factor (rhG-CSF) ; recombinant human granulocyte-CSF ; nasal absorption in rats ; bioavailability ; leukocyte number
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Nasal absorption of recombinant human granulocyte colony-stimulating factor (rhG-CSF) was examined in the rat. The relative bioavailability of rhG-CSF for subcutaneous administration was ∼2%, as evaluated from the immunologically active rhG-CSF concentration in rat plasma and the area under the curve (AUC) of the plasma rhG-CSF concentration versus time for 8 hr. Pharmacological availability relative to subcutaneous administration was determined from the increase in total blood leukocyte numbers. The pharmacological availability was 5–10%, determined from the AUC for the increased ratio of total leukocyte numbers versus time for 48 hr; it was slightly dependent on the pH and the osmotic pressure of the dosing solution. Accordingly, the plasma concentration of rhG-CSF did not always reflect its pharmacological effects. Relative bioavailability and pharmacological availability were increased about 23 times and 3 times, respectively, by polyoxyethylene 9-lauryl ether (Laureth-9), but no increase in availability occurred with sodium glycocholate. The increase in total leukocyte numbers was maintained during multiple rhG-CSF dosing, and the addition of Laureth-9 further increased the pharmacological effects of this agent. This study indicates that nasal administration of rhG-CSF is an effective parenteral administration route.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 5 (1988), S. 341-346 
    ISSN: 1573-904X
    Keywords: colonic absorption ; absorption promoter ; cefmetazole ; inulin ; pore radius ; paracellular route
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Colonic absorption of poorly absorbable cefmetazole was shown to increase considerably by the addition of 1% sodium caprate, sodium laurate, and mixed micelles composed of sodium oleate and sodium taurocholate. At 0.25%, their effects were weaker but still significant. Colonic absorption of inulin was also increased by the promoters at a concentration of 0.25%. These results suggest that there is a common route between inulin and cefmetazole absorption, i.e., the paracellular route. Sodium taurocholate, sodium caprylate, and EDTA disodium salts (EDTA-2Na) at 1% enhanced cefmetazole absorption less than caprate, laurate, or mixed micelles, but no such effect was found at 0.25%. The colonic pore radius was determined from the equivalent pore theory using an everted sac procedure. Caprate, laurate, and mixed micelles at 0.25% caused this radius to increase significantly, thus making it possible for inulin to permeate the everted sac from the mucosal to the serosal side. The effects of taurocholate, caprylate, and EDTA-2Na for increasing colonic pore sizes and the degree of inulin permeation were less than those of caprate, laurate, or mixed micelles. The change in the paracellular route is thus considered to result from the increase in pore size.
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1546-1696
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Process Engineering, Biotechnology, Nutrition Technology
    Notes: [Auszug] We describe the generation of transgenic silkworms that produce cocoons containing recombinant human collagen. A fusion cDNA was constructed encoding a protein that incorporated a human type III procollagen mini-chain with C-propeptide deleted, a fibroin light chain (L-chain), and an enhanced green ...
    Type of Medium: Electronic Resource
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  • 6
    ISSN: 1436-2813
    Keywords: carcinosarcoma ; polypoid carcinoma ; esophagus
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Among 137 cases of esophageal neoplasms surgically treated at Kobe City General Hospital from 1983 to 1990, there were two patients with a huge polypoid lesion identified as carcinosarcoma by light microscopic examination, both of whom underwent radical resection and esophagogastrostomy. Microscopic examination of the resected specimens revealed the tumors to be composed of carcinomatous and sarcomatous elements. Additional immunohistochemical examination disclosed keratin-positive cells in the carcinomatous element and vimentin-positive cells in the sarcomatous element. In case 1, keratin-positive cells were also found in the sarcomatous element, which suggested that the sarcomatous cells were derived from epithelial cells. Despite the huge size of the tumors, the depth of invasion to the esophageal wall was limited to the mucosal layer in case 1 and the submucosal layer in case 2, and there has been no evidence of recurrence in either case since surgery.
    Type of Medium: Electronic Resource
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  • 7
    ISSN: 1573-2568
    Keywords: RAT COLON ; HUMAN COLON ; SODIUM CAPRATE ; PALMITOYLCARNITINE ; PERIJUNCTIONAL ACTOMYOSIN RING
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract We examined the enhancing action of sodiumcaprate and palmitoylcarnitine on the permeability offluorescein isothiocyanate dextran 4000 as aparacellular permeant compound in isolated rat and humancolon samples using the Ussing-type chamber method.In the absence of an enhancer, the permeation clearanceof fluorescein isothiocyanate dextran 4000 was notsignificantly different in the rat and human colons, but the electric membrane resistance wassmaller in the rat colon than in the human colon. Sodiumcaprate and palmitoylcarnitine increased permeationclearance and decreased electric membrane resistance in both types of colonic membrane, showing thatthe rat colon can be used as a model of the human colonfor studies of enhancer effects. A calmodulin antagonistsignificantly inhibited the action of sodium caprate in both colonic membranes. However, ittended to promote the effects of palmitoylcarnitine onpermeation clearance and electric membrane resistance.These results suggest that sodium caprate induces the contraction of the perijunctionalactomyosin ring to widen the tight junction and that themechanism of palmitoylcarnitine is different from thatof sodium caprate in the human colon, as reportedpreviously for Caco-2 cell monolayers.
    Type of Medium: Electronic Resource
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  • 8
    ISSN: 1573-5117
    Keywords: marine rotifer ; EFA enrichment ; freshwater Chlorella ; high density culture
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract High density cultured marine rotifer (Brachionusrotundiformis) fed on freshwater Chlorella wascultured secondarily with an emulsion of ethyl esters(65% DHA, 15% EPA) for EFA-enrichment, with orwithout freshwater Chlorella. Culture tanks (30 l, 20 lworking volume) set in a water bath (24 °C)were continuously supplied with air (2.50 lm−1) or high-purity oxygen gas (1.25 lm−1). Samples for fatty acid compositionanalysis were collected at 0, 6, 12, and 24 hoursafter the inoculation of rotifer, followed by themonitoring of rotifer density, DO, NH4-N and pH.The n-3 HUFA content plateaued at 6 hours afterthe onset of the secondary culture and no significantdifferences were observed afterwards, regardless ofthe aeration methods. The HUFA content increased withdecreasing amounts of Chlorella added. Thehighest content (ca 3.5% on a dry basis) was notedin non-Chlorella feeding groups. When largeamounts of Chlorella were fed, the DO of culturewater drastically decreased and the NH4-Nconcentration increased. The results from theexperiment indicate that the presence of Chlorella cells greatly affect the HUFA intake ofrotifers during the secondary culture process. Alsothe supply of high-purity oxygen gas was effective forpreventing a culture crash of rotifers during EFAenrichment.
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    Journal of pharmacokinetics and pharmacodynamics 6 (1978), S. 327-337 
    ISSN: 1573-8744
    Keywords: in vitro andin vivo correlation ; microsomal oxidation of drugs ; nonlinear pharmacokinetics ; physiological pharmacokinetics ; tissue distribution ; distribution volume ; ethoxybenzamide ; Michaelis-Menten parameters
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract In vitroand in vivocorrelations of the microsomal oxidation of drugs were examined, using ethoxybenzamide as a model drug. Ethoxybenzamide disappearance time course from rat plasma in vivowas analyzed by a two-compartment model assuming a Michaelis-Menten type elimination process. Ethoxybenazmide oxidation in vitrowas measured by the appearance rate of salicylamide in rat liver microsomal suspension. Parameters obtained were Vmax=3.46 and 3.77 μmoles/min/kg body weight and Km=0.378 and 0.192mM, in vitroand in vivo,respectively.
    Type of Medium: Electronic Resource
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  • 10
    ISSN: 1573-904X
    Keywords: colonic absorption ; absorption promoter ; transcellular route ; fluorescence polarization ; membrane perturbation ; sodium caprate
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The effects of sodium caprate and sodium caprylate on transcellular permeation routes were examined in rats. The release of membrane phospholipids was significantly increased only by caprate, while protein release did not change from the control in the presence of caprate or caprylate, indicating that the extent of membrane disruption was insufficient to account for enhanced permeation. Using brush border membrane (BBM) vesicles prepared from colon, with their protein and lipid component labeled by fluorescent probes, the perturbing actions of caprate and caprylate toward the membrane were examined by fluorescence polarization. Caprate interacted with membrane protein and lipids, and caprylate mainly with protein, causing perturbation to the membrane. The release of 5(6)-carboxyfluorescein previously included in BBM vesicles was increased by caprate but not by caprylate. These results suggest that caprate enhances permeability via the transcellular route through membrane perturbation.
    Type of Medium: Electronic Resource
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