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  • 1
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Annals of the New York Academy of Sciences 446 (1985), S. 0 
    ISSN: 1749-6632
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Natural Sciences in General
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1573-904X
    Keywords: hydroxypropylmethylcellulose ; propylthiouracil ; sustained release ; in vitro release ; bioavailability in dogs and pigs
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A hydrophilic matrix tablet containing 300 mg of propylthiouracil was formulated with several types of hydroxypropylmethylcellulose. The influence of polymer and drug granule particle size, polymer concentration, crystallinity and geometry of the polymer particles, the polymer incorporation outside or inside the granule, addition of a filler and tablet hardness were studied. Polymer concentration, polymer particle size and geometry, filler addition and type of the filler used had a major influence on in vitro drug dissolution profiles. The bioavailability of propylthiouracil in dogs from the hydrophilic matrices investigated was low, because of the short gastro-intestinal transit times of the matrix tablets in the dogs. The matrix tablets reached the colon in fasted dogs within 2–3 hours after administration. The results indicated the poor predictability of bioavailability experiments in dogs with hydrophilic matrices. Although the bioavailability data in pigs seemed promising, a transit time study revealed a long stomach residence time of the matrix tablets in pigs. These data suggested that pigs are an inappropriate animal model for bioavailability studies of erodible matrix tablets.
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 13 (1996), S. 146-150 
    ISSN: 1573-904X
    Keywords: freeze-drying ; protein ; maltodextrins ; PEG
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. Maltodextrins, partially hydrolysed starches, were evaluated as potential lyoprotectants and the effect of combinations of maltodextrins and PEG 8000 on the protection of lactate dehydro genase (LDH) was examined. Methods. LDH activity assays were performed immediately before freezing and after reconstitution. The activity recovery was used as the parameter to evaluate the lyoprotectants. Differential Scanning Calorimetry (DSC) was used to measure the glass transition temperature (Tg′) of the solutions. DSC and X ray diffraction were used to characterise the freeze-dried products. Results. Maltodextrins were found to protect LDH againt inactivation during freeze-drying. The lyoprotection obtained by these maltodextrins is dependent on their D.E. value and the concentration used. The maltodextrin formulations performed as good or better than those containing sucrose and maltose, depending on the concentration used. Freeze dried cakes of maltodextrin formulations were amorphous. In the case of low D.E. maltodextrins, lyoprotection was improved by the addition of PEG 8000 as a cryoprotectant. Conclusions. Maltodextrins could be considered as potential lyoprotectants in lyophilization of proteins.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1573-904X
    Keywords: HCT ; hydroflumethiazide ; cyclodextrins
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 13 (1996), S. 1228-1232 
    ISSN: 1573-904X
    Keywords: bioadhesion ; buccal absorption ; testosterone ; dog model ; bioavailability ; in vitro bioadhesion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. As the oral bioavailability of testosterone is very low because of its high first pass effect, buccal administration might present a viable alternative. In this study a buccal bioadhesive tablet was used in order to sustain the delivery and bypass the liver. Methods. Testosterone and testosterone acetate, propionate, enanthate and decanoate were investigated. The influence of the concentration of testosterone (10–50%) and testosterone esters (30%) on in vitro bioadhesion was investigated. The absolute (IV) and relative (oral) bioavailability of 60 mg testosterone or an equivalent amount of testosterone ester was determined in castrated male dogs. Results. Both the in vitro detachment force and the work of adhesion decreased gradually with an increasing amount of testosterone and for an increasing chain length of the esters, except in the case of testosterone enanthate. The in vivo results revealed that the bioavailability of testosterone was significantly higher (p 〈 0.05) than that of the esters, which is probably due to the lower solubility of the esters. The mean absolute bioavailability of testosterone from the bioadhesive tablet was 14.1%, while the mean relative bioavailability was 1370%. The buccal administration of testosterone via the bioadhesive tablet allowed the maintenance of the plasma level at above 3 ng/ml for 15 to 24 h. Conclusions. Buccal absorption of testosterone was significantly higher than that of its esters.
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  • 6
    ISSN: 1573-904X
    Keywords: miconazole ; buccal bioadhesive ; slow release ; in vitro/in vivo correlation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract An in vitro–in vivo correlation study was performed on the bioadhesive properties of three buccal formulations based on modified starch (drum-dried waxy maize)/polyacrylic acid mixtures. Mixtures containing 10 mg miconazole nitrate, characterized by a different in vitro detachment force and work of adhesion, were evaluated for their bioadhesive properties in human volunteers. The results obtained showed that no significant difference could be seen among the formulations in vivo. The in vitro method showed no significant influence of miconazole nitrate on the bioadhesion properties of the polymers, while the in vivo adhesion time of the pure polymer mixtures was significantly higher than for the polymers containing miconazole. The results from the in vitro method thus did not correlate well with the in vivo data. The in vitro method provided information only on the initial bioadhesion and no correlation could be made with the residence time of the tablet in the oral cavity.
    Type of Medium: Electronic Resource
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  • 7
    ISSN: 1573-904X
    Keywords: absorption enhancers ; ciliotoxicity ; rotifers ; cyclodextrins ; bile salts ; phosphatidylcholine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 16 (1999), S. 1240-1244 
    ISSN: 1573-904X
    Keywords: mucosal toxicity ; screening ; absorption enhancers ; drugs
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. The objective of this study was to develop a simple alternative test using naked snails (slugs) for screening the irritating potency of chemicals on mucosal surfaces. Methods. The effect of various absorption enhancers and two β-blocking agents on the mucosal tissue was determined from the total protein and lactate dehydrogenase released from the foot mucosa after treatment. Additionally, mucus production and reduction in body weight of the slugs caused by the treatment were measured. Results. According to the effects on the mucosal epithelium of the slugs the following rank order of increasing toxicity was established: PBS, HP-β-CD (5%), β-CD (1.8%) and oxprenolol hydrochloride (1 %) 〈 DDPC (l%) 〈 STDHF (l%) 〈 BAC (l%), SDC (l%) and propranolol hydrochloride (1 %). The results of the present study are in agreement with other studies using the same compounds on other models. Conclusions. The results of this study indicated the mucosa of slugs can serve as a primary screening tool for the evaluation of chemicals on mucosal surfaces. By simply measuring mucus production and weight loss reliable toxicity information can be obtained. This demonstrates rapid screening tests can be carried out using simple toxicity endpoints.
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  • 9
    ISSN: 1546-1696
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Process Engineering, Biotechnology, Nutrition Technology
    Notes: [Auszug] Genetically modified Lactococcus lactis secreting interleukin 10 provides a therapeutic approach for inflammatory bowel disease. However, the release of such genetically modified organisms through clinical use raises safety concerns. In an effort to address this problem, we replaced ...
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  • 10
    Electronic Resource
    Electronic Resource
    New York, NY [u.a.] : Wiley-Blackwell
    Biotechnology and Bioengineering 42 (1993), S. 381-386 
    ISSN: 0006-3592
    Keywords: alginate ; polylysine ; microcapsules ; optimization ; cut-off ; FITC-dextran ; FITC-polylysine ; Chemistry ; Biochemistry and Biotechnology
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Biology , Process Engineering, Biotechnology, Nutrition Technology
    Notes: Mammalian cells encapsulated in alginate-polylysine microcapsules are used as artificial organs in cancer research and in biotechnology. These applications require microcapsules with a reproducible mol. wt. cut-off. The high cost of the polycation, polylysine, requires an efficient preparation procedure. This article shows that the overall reported contact time of 5 minutes at ambient conditions should be increased several times in order to reach a maximal binding between the calcium alginate beads and 0.1% (w/v) polylysine solutions. An increase of the polylysine concentration from 0.0125% to 0.8% (w/v) resulted in a faster maximal binding, but the amount of polylysine bound increased also. Immersion of calcium alginate beads with a diameter of 750 μm, prepared from 1 mL alginate, in 30 mL of a 0.8% (w/v) polylysine solution, resulted in a polylysine spill of more than 89%. The time required to reach a maximal binding was related to the reaction temperature. The interaction zone between calcium alginate beads and fluorescein isothiocyanate-labeled polylysine solutions was visualized with a confocal laser scanning microscope as a function of time. Microcapsules, prepared at 40°C with 0.1% (w/v) polylysine solutions with mol. wts. between 12 and 249.2 kD, were permeable for fluorescein isothiocyanate-labeled dextran, mol. wt. 4.7, but not for 40.5 kD. Higher polylysine concentrations resulted in a membrane with a mol. wt. cut-off lower than 4.7 kD. © 1993 John Wiley & Sons, Inc.
    Additional Material: 5 Ill.
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