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  • 1
    Electronic Resource
    Electronic Resource
    In vivo and in vitro studies of the site of inhibitory action of omeprazole on adrenocortical steroidogenesis (1988)
    Springer
    European journal of clinical pharmacology 35 (1988), S. 625-629 
    Details
    ISSN: 1432-1041
    Keywords: omeprazole ; cortisol synthesis ; urinary steroid metabolites ; cholesterol cleavage inhibition ; adrenal steroidogenesis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The site of omeprazole inhibition of adrenal steroidogenesis has been sought in vivo by analyzing the patterns of urinary steroid metabolite excretion after 6 days of treatment with placebo/omeprazole. Excretion rates of androsterone, aetiocholanolone, dehydroepiandrosterone, 11 β hydroxyandrosterone, tetrahydrocortisone, tetrahydrocortisol and α cortolone were reduced, indicating a block at an early step in steroidogenesis, possibly cholesterol side-chain cleavage. In vitro studies have confirmed this finding by measuring conversion of added precursors to cortisol in isolated bovine adrenocortical cells. Cortisol synthesis from added 20 α hydroxycholesterol was inhibited by 83% in the presence of 100 µg omeprazole/ml. Conversion from pregnenolone and progesterone and their 17 α hydroxylated derivatives was inhibited by 20–40% whereas cortisol production from added 11 deoxycortisol was not affected. These data suggest that omeprazole primarily inhibits cholesterol cleavage and does not inhibit 3 β hydroxysteroid dehydrogenase, 17 α hydroxylase or 11 β hydroxylation; 21 hydroxylase activity may be marginally attenuated.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00637598
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  • 2
    Electronic Resource
    Electronic Resource
    The effects of omeprazole on endocrine function in man (1987)
    Springer
    European journal of clinical pharmacology 32 (1987), S. 423-425 
    Details
    ISSN: 1432-1041
    Keywords: omeprazole ; endocrine function ; cortisol ; 11-deoxycortisol ; FSH ; LH ; TSH ; T3 ; T4 ; testosterone ; prolactin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We have assessed the effect of omeprazole on various endocrine functions in man. Eight healthy subjects took 60 mg omeprazole or placebo daily for 1 week in a double-blind, randomized, cross-over study. On Day 7 basal concentrations of follicle-stimulating hormone (FSH), luteinising hormone (LH), prolactin, testosterone, thyroid-stimulating hormone (TSH), and serum thyroxine (T4) and tri-iodothyronine (T3) were measured, followed by the gonadotrophin response to luteinising hormone releasing hormone (LHRH) and the prolactin and TSH responses to thyrotrophin releasing hormone (TRH). There were no differences in basal or stimulated values between omeprazole and placebo. In a second study, a further 8 subjects were similarly treated, and on Day 7 serial measurements of cortisol and 11-deoxycortisol were made before and for 2.5 h after intravenous adrenocorticotrophin (ACTH). There were no differences in basal values or pattern of response to ACTH for either hormone. Omeprazole in clinical practice is unlikely to cause any significant interference in endocrine function.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00543980
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  • 3
    Electronic Resource
    Electronic Resource
    Colonic spreading of a non-chlorofluorocarbon mesalazine rectal foam enema in patients with quiescent ulcerative colitis (1995)
    Oxford, UK : Blackwell Publishing Ltd
    Alimentary pharmacology & therapeutics 9 (1995), S. 0 
    Details
    ISSN: 1365-2036
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Background: Rectal foam enemas provide for drug delivery to the distal colon for treatment of left sided ulcerative colitis. However, currently available formulations contain chlorofluorocarbons which are due to be phased out in the near future. The objective of this study was therefore to determine the degree of dispersion of a newly developed nonchlorofluorocarbon rectal foam preparation in ulcerative colitis patients. Methods: This was an open label non-controlled study of a single administration of a mesalazine foam enema (two actuations containing 2 g of mesalazine in approximately 120 mL foam) in 10 patients with quiescent ulcerative colitis. Spreading of the 99mTc-labelled foam enema was assessed over a 4-h period by the non-invasive technique of gamma scintigraphy. Results: All patients retained the enema for the full 4-h imaging period. In nine out of the 10 patients, the enema was observed to spread as far as the descending colon and on average 23% of the dose was present in the descending colon at 4 h post-dose. Conclusions: The extent of spreading observed in the study supports the use of the formulation in the treatment of left sided ulcerative colitis.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1365-2036.1995.tb00365.x
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  • 4
    Electronic Resource
    Electronic Resource
    Colonic delivery of dexamethasone: a pharmacoscintigraphic evaluation (1997)
    Oxford BSL : Blackwell Science
    Alimentary pharmacology & therapeutics 11 (1997), S. 0 
    Details
    ISSN: 1365-2036
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Background: Colonic delivery of corticosteroids may reduce the side-effects commonly associated with their use. Therefore, we tested the ability of the naturally occurring polysaccharide guar gum to deliver a corticosteroid, dexamethasone, to the colon using pharmacoscintigraphy. Guar gum is metabolized in the colon by resident bacterial enzymes to trigger drug release. Materials: Each subject (eight per group, parallel study design) was administered one of four dexamethasone (9 mg) tablet formulations, radiolabelled with 153Sm using neutron activation, under fasted conditions. One formulation was designed to release drug rapidly following ingestion while the other three formulations were designed to delay release of dexamethasone to varying degrees. Progression of the formulations down the gastrointestinal tract was followed by gamma scintigraphy. Serum concentrations were measured over time to relate disintegration profiles of the tablets with pharmacokinetic observations. Results: The immediate release formulation disintegrated in the stomach, on average, within 20  min of dosing. One of the three delayed release preparations (CD1) began to disintegrate in the small intestine 1.7±1.0 h after dosing. The second and third delayed release preparations (CD2 and CD3) did not begin to disintegrate until 5.8±2.3 and 3.6±1.6 h after dosing, respectively. All three colonic delivery preparations completely disintegrated in the colon ranging from 7.8±2.7 h (CD1) to 12.4±3.2 h (CD2) following oral administration. Pharmacoscintigraphic data indicated that 72–82% of the dexamethasone was delivered into the colon although not all the dexamethasone delivered into the colon was absorbed. Conclusions: Simple guar gum formulations are capable of delivering the corticosteroid dexamethasone to the colon of normal subjects. Locally delivered corticosteroids may be useful in the treatment of ulcerative colitis and Crohn's disease. Pharmacoscintigraphic evaluation is a useful method to discriminate between the in vivo behaviour of colonic delivery systems.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1046/j.1365-2036.1997.93265000.x
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  • 5
    Electronic Resource
    Electronic Resource
    The Effects of Thyroidectomy on the Mineralocorticoid Response to Aldosterone in Male Adrenalectomized Rats (1984)
    Oxford, UK : Blackwell Publishing Ltd
    Annals of the New York Academy of Sciences 435 (1984), S. 0 
    Details
    ISSN: 1749-6632
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Natural Sciences in General
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1749-6632.1984.tb13759.x
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  • 6
    Electronic Resource
    Electronic Resource
    Spreading and Retention of Vaginal Formulations in Post-Menopausal Women as Assessed by Gamma Scintigraphy (1997)
    Springer
    Pharmaceutical research 14 (1997), S. 1073-1078 
    Details
    ISSN: 1573-904X
    Keywords: vaginal delivery ; gamma scintigraphy ; bioadhesion ; pessary ; post-menopausal women
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. In this paper we report on the first scintigraphic evaluation of vaginal dosage forms in post-menopausal women. To date, almost nothing is known about the in vivo performance of pharmaceutical formulations in the human vagina, which is a major deficiency in the rational design of drug delivery systems for both existing and new indications. Methods. The vaginal spreading and clearance of a radiolabelled pessary formulation and Replens® (polycarbophil) gel, was assessed in six healthy, post-menopausal female volunteers over a six hour period using the technique of gamma scintigraphy. Results. In five out of the six subjects studied, clearance of the two formulations exhibited very little intra-subject variation. However, there was considerable inter-subject variability in clearance; in Subject 5 circa 80% of the products were retained whilst in Subject 2 less than 2% was present at the end of the six hour imaging period. Importantly, there was no evidence to suggest that either of the formulations dispersed material beyond the cervix, into the uterus, in any of the subjects studied. Conclusions. The lack of significant retention of these products in most of the volunteers has obvious implications for the delivery of therapeutic agents. This study shows that gamma scintigraphy is an invaluable technique with which to assess novel formulations aimed at optimising retention in the vagina for topical or systemic drug delivery.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1012113714552
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  • 7
    Electronic Resource
    Electronic Resource
    The Use of Pharmacoscintigraphy to Elucidate Food Effects Observed with a Novel Protease Inhibitor (Saquinavir) (1998)
    Springer
    Pharmaceutical research 15 (1998), S. 417-422 
    Details
    ISSN: 1573-904X
    Keywords: saquinavir ; protease inhibitor ; gastrointestinal tract ; food effects ; pharmacoscintigraphy
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To evaluate mechanistically the effect of food on the absorption and gastrointestinal transit of the protease inhibitor saquinavir. Methods. Pharmacoscintigraphic investigation in eight healthy volunteers. Results. Gastric emptying occurred rapidly in the fasted state with some capsules leaving the stomach prior to disintegration. Unmeasur-able plasma concentrations were observed in several subjects when dosed under fasted conditions. Following post-prandial administration the radioactive marker became re-distributed within the stomach contents and consequently slower gastric emptying resulted. Plasma concentrations under fed conditions were measurable up to 12 hrs after administration in seven of the eight subjects. Six of the eight plasma profiles showed secondary peaks at c. 4 hours post-dose; two of which coincided with the gastrocolonic response following ingestion of lunch. Conclusions. Bioavailability of saquinavir is significantly improved in the presence of food. Emptying of intact capsules in the fasted state may further reduce bioavailability. In the fed state, capsules disintegrate rapidly and gastric emptying is prolonged which may improve exposure of the drug to target absorption sites. Saquinavir may be absorbed from the colon. Second peaks in the absorption profile can only be attributed to gastrocolonic response following ingestion of a meal in some cases. Increased absorption is more likely to be due to an increase in dissolved drug being available for absorption due to general increased motility and secretion stimulated by ingestion of a meal.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1011972230829
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    Paper (German National Licenses)
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  • 8
    Electronic Resource
    Electronic Resource
    Captopril (SQ 14225) depresses drinking and aldosterone in rats lacking vasopressin (1979)
    [s.l.] : Nature Publishing Group
    Nature 281 (1979), S. 569-570 
    Details
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] DI rats drink approximately eight times more water than normal animals6'7, and in the present experiments each drank about 80 ml per 100 g body weight per 24 h during the initial 3-day control observation period. When the orally active SQ 14225 was introduced into the water (SOmgl"1), the drinking ...
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1038/281569a0
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