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  • 1
    Electronic Resource
    Electronic Resource
    Formation and stability of lanthanide complexes and their encapsulation into polymeric microspheres (1992)
    s.l. : American Chemical Society
    The @journal of physical chemistry 〈Washington, DC〉 96 (1992), S. 8626-8631 
    Details
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology , Physics
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/j100200a076
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  • 2
    Electronic Resource
    Electronic Resource
    Purification of Proteins Using Foam Fractionation (1997)
    Springer
    Pharmaceutical research 14 (1997), S. 1511-1515 
    Details
    ISSN: 1573-904X
    Keywords: separation ; foam fractionation ; protein purification
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purification is an important step in the production of pharmaceuticals from recombinant proteins. The characteristics of industrial-scale purification schemes, such as conventional chromatography, have a significant impact on the cost of production. Foam fractionation, a novel separation technique based upon the differences in affinities of components for the gas/aqueous interface of a foam, has the potential to be a cost-effective component in a purification scheme. This review covers some of the more recent studies in understanding the process and applications of foam fractionation in protein-containing systems with special attention to the requirements of pharmaceutical products.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1012109830424
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  • 3
    Electronic Resource
    Electronic Resource
    Drug Distribution and Biliary Excretion Pattern of a Cyclic Somatostatin Analog: A Comparison of 14C Labeled Drug and a 131I lodinated Drug Analog (1985)
    Springer
    Pharmaceutical research 2 (1985), S. 80-83 
    Details
    ISSN: 1573-904X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A cyclic somatostatin analog was compared to an iodinated analog of the same compound with respect to organ distribution and biliary excretion in the rat. The cyclic hexapeptide was radiolabeled with either 14C or 131I (tyrosine). Organ distribution of the iodinated compound as a function of time was nearly identical to that observed for the non-iodinated compound. Results indicated a rapid uptake by the liver and subsequent rapid excretion of the intact peptide in bile. Activity in other organs examined tended to fall off in a manner similar to the activity in blood with sequential samples. Because of the similarity in the in vivo behavior of the two compounds, the iodinated analog was deemed a suitable model for less invasive distribution studies, and was further examined in the dog using external gamma scintigraphy. In the unanesthetized dog the iodine activity was rapidly taken up by liver and collected in the gallbladder, thus exhibiting a similar rapid excretion pattern to that observed in the rat.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1016342812234
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  • 4
    Electronic Resource
    Electronic Resource
    Correlation of Ibuprofen Bioavailability with Gastrointestinal Transit by Scintigraphic Monitoring of 171Er-Labeled Sustained-Release Tablets (1987)
    Springer
    Pharmaceutical research 4 (1987), S. 486-489 
    Details
    ISSN: 1573-904X
    Keywords: scintigraphy ; neutron activation ; bioavailability ; ibuprofen ; sustained release ; gastrointestinal transit
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract External gamma scintigraphy was used to monitor the gastrointestinal (GI) transit of radiolabeled sustained-release tablets containing 800 mg ibuprofen in eight fasted healthy volunteers. Ibuprofen serum concentrations were determined from blood samples drawn sequentially over a 24-hr period. Serum concentrations and related parameters were correlated to the position of the dosage form in the GI tract from the scintiphotos. The sustained-release tablets were radiolabeled intact utilizing a neutron activation procedure, by incorporating 0.18% of 170Er2O3 (enriched to 〉96% 170Er) into the bulk formulation. After manufacture of the final dosage forms, the tablets were irradiated in a neutron flux (4.4 × 1013 n/cm2 · sec) for 2 min, converting the stable 170Er to radioactive 171Er (t 1/2 = 7.5 hr). Each tablet contained 50 µCi of 171Er at the time of administration. The scintigraphy studies suggested that the greatest proportion of ibuprofen was absorbed from this dosage form while the tablet was in the large bowel. The dosage forms eroded slowly in the small bowel and appeared to lose their integrity in the large bowel. In vitro studies showed only minimal effects of the neutron irradiation procedure on the dosage form performance.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1016475421474
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  • 5
    Electronic Resource
    Electronic Resource
    An in Vitro/in Vivo Correlation for the Disintegration and Onset of Drug Release from Enteric-Coated Pellets (1993)
    Springer
    Pharmaceutical research 10 (1993), S. 233-238 
    Details
    ISSN: 1573-904X
    Keywords: enteric coated ; in vitro/in vivo correlation ; targeted release ; pellet formulation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract An empirical mass-transfer model for enteric-coating dissolution that uses in vitro dissolution data to characterize the pH-dependent solubility properties of the polymer film and a mass-transfer coefficient determined from in vivo dissolution or disintegration studies is developed. Once the in vivo mass- transfer coefficient has been evaluated, it can be used in conjunction with in vitro dissolution data from other formulations to predict the in vivo time to disintegration and onset of drug release. Results of in vitro dissolution experiments using the USP basket dissolution apparatus and in vivo disintegration experiments using gamma scintigraphy with four enteric-coated pellet formulations are presented. The good agreement among the in vivo mass-transfer coefficients that were determined supports the validity of the model.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1018986827350
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  • 6
    Electronic Resource
    Electronic Resource
    Studies on the Dissolution of Drugs from Tablets using Perturbed Angular Correlation (1985)
    Springer
    Pharmaceutical research 2 (1985), S. 75-77 
    Details
    ISSN: 1573-904X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The perturbed angular correlation (P.A.C.) technique was used to assess the dissolution of drugs coprecipitated with [111In]indium chloride in tablets in vitro. The amount of drug in solution was monitored simultaneously with the amount of radioactivity in solution and these were correlated to the anisotropy values obtained by P.A.C. measurements. The results indicated that the rate of drug dissolution paralleled the change in measured anisotropy of the system. Thus, the measurement of anisotropic changes in drug-indium complexes by P.A.C. is a reliable indicator of drug dissolution and can provide meaningful dissolution data for noninvasive in vivo studies.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1016338611325
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  • 7
    Electronic Resource
    Electronic Resource
    The Effect of Food on Gastrointestinal (GI) Transit of Sustained-Release Ibuprofen Tablets as Evaluated by Gamma Scintigraphy (1990)
    Springer
    Pharmaceutical research 7 (1990), S. 304-307 
    Details
    ISSN: 1573-904X
    Keywords: scintigraphy ; neutron activation ; bioavailability ; ibuprofen ; sustained release ; food effect ; gastrointestinal transit
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The GI transit of radiolabeled sustained-release ibuprofen 800-mg tablets in eight healthy, fed volunteers was monitored using external gamma scintigraphy. Ibuprofen serum concentrations were determined from blood samples drawn over 36 hr following dosing. Sustained-release ibuprofen tablets containing 0.18% of 170Er2O3 (〉96% 170Er) in the bulk formulation were manufactured under pilot-scale conditions and were radiolabeled utilizing a neutron activation procedure which converted stable 170Er to radioactive 171Er (t 1/2 = 7.5 hr). At the time of dosing, each tablet contained 50 µCi of 171Er. Dosage form position was reported at various time intervals. In five subjects the sustained-release tablet remained in the stomach and eroded slowly over 7–12 hr, resulting in gradual increases in small bowel radioactivity. In the remaining three subjects, the intact tablet was ejected from the stomach and a gastric residence time of approximately 4 hr was measured. This is in marked contrast to a previous study conducted in fasted volunteers in which gastric retention time ranged from 10 to 60 min. Differences in GI transit between fed and fasted volunteers had little effect on ibuprofen bioavailability. AUC and T max were unaltered and C max was increased by 24%, which is in agreement with results from a previous, crossover-design food effect study.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015842600189
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  • 8
    Electronic Resource
    Electronic Resource
    Noninvasive in Vivo Percutaneous Absorption Measurements Using X-Ray Fluorescence (1992)
    Springer
    Pharmaceutical research 9 (1992), S. 1410-1414 
    Details
    ISSN: 1573-904X
    Keywords: percutaneous absorption ; topical delivery ; X-ray fluorescence spectrometry ; 5-iodouracil
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract X-ray fluorescence (XRF) has been used to determine in vivo the percutaneous absorption of 5-iodouracil (5IU) in dimethyl sulfoxide (DMSO) on female Sprague-Dawley rats. An average absorption rate constant of 122 ± 34 µg/cm2-hr was obtained from the XRF measurements on four rats. A comparative study was performed with radiolabeled (125I) 5IU in which the absorption rate constant was determined to be 126 ± 20 µg/cm2-hr. The XRF system described provides a simple, noninvasive means of measuring the percutaneous absorption rate of select compounds by the surface disappearance method.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015850627370
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  • 9
    Electronic Resource
    Electronic Resource
    Poly(L-lactic Acid) Microspheres Containing Neutron-Activatable Holmium-165: A Study of the Physical Characteristics of Microspheres Before and After Irradiation in a Nuclear Reactor (1992)
    Springer
    Pharmaceutical research 9 (1992), S. 149-154 
    Details
    ISSN: 1573-904X
    Keywords: acetylacetone ; holmium ; microspheres ; nuclear reactor ; poly-L-lactic acid
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The solvent evaporation technique was employed to prepare poly(L-lactic acid) (PLA) microspheres with 165Ho acetylacetonate (Ho-AcAc). Particle size, percentage Ho-165, percent residual solvent, and retentive ability of the spheres were found to be strongly affected by preparatory conditions. Differential scanning calorimetry (DSC) thermograms suggested that the Ho-AcAc existed in the PLA matrix as a molecular dispersion. High neutron flux irradiations of the PLA spheres in a nuclear reactor produced Ho-166, a therapeutic radionuclide that emits high-energy negatrons (E max = 1.84 MeV; half-life = 26.9 hr). The gamma radiation dose (53– 75 Mrad) from the core of the reactor provided an overkill of all bioburdens in the PLA spheres. Gel permeation chromatography (GPC) analysis showed that these irradiations caused a reduction in PLA molecular weight. Infrared spectra, 13C NMR spectra, 1H NMR spectra, and DSC thermograms further confirmed the presence of lower molecular weight PLA but proved the overall maintenance of PLA structure.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1018908600711
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  • 10
    Electronic Resource
    Electronic Resource
    Radiolabeling of Intact Dosage Forms by Neutron Activation: Effects on In Vitro Performance (1987)
    Springer
    Pharmaceutical research 4 (1987), S. 524-526 
    Details
    ISSN: 1573-904X
    Keywords: neutron activation ; barium-138 ; erbium-170 ; samarium-152 ; tablet hardness ; tablet disintegration ; radiolabeling
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Compressed tablets containing various quantities of stable isotopes of Ba, Er, and Sm for use in neutron activation studies were evaluated for the effect of stable isotope incorporation on tablet hardness and disintegration times. At concentrations likely to be used in scintigraphic studies employing neutron activation as a radiolabeling method, no significant effect on in vitro parameters were observed. While the incorporation of stable isotopes influenced tablet hardness to a greater degree than disintegration time, irradiation of tablets in a neutron flux of 4.4× 1013 n/cm2 sec had a direct effect on tablet disintegration time. Thus, future neutron activation studies should focus on minimizing the amount of stable isotope to be incorporated with the formulation while using the shortest feasable irradiation time.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1016491925109
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