Abstract：
:The placental and nonplacental clearances of metoclopramide were studied in nine chronically instrumented, near-term pregnant sheep using a two-compartment open model. Metoclopramide was administered to the ewe and fetus on separate occasions as an initial iv bolus loading dose followed by a constant-rate infusion, with steady-state maternal and fetal plasma concentrations being obtained by 45 min. Following the maternal infusions, metoclopramide reached average steady-state concentrations of 50.0 +/- 20.2 ng/mL in the ewe and 27.1 +/- 8.6 ng/mL in the fetus, with a mean fetal-to-maternal concentration ratio of 0.57 +/- 0.14. The ability of the fetus to eliminate metoclopramide by nonplacental routes appears to be responsible for this ratio being less than unity, rather than differential protein binding and ion-trapping effects. Mean steady-state concentrations were 13.8 +/- 4.5 and 253.7 +/- 92.1 ng/mL in the ewe and fetus, respectively, after fetal drug administration. Metoclopramide was bound significantly less to fetal (39.5 +/- 8.9%) than to maternal (49.5 +/- 7.9%) plasma proteins, with values similar to that reported for humans (approximately 40%). Clearance of metoclopramide across the placenta from the fetus to the ewe (6.2 +/- 2.4 L/h/kg) was significantly greater than that in the reverse direction (4.3 +/- 1.3 L/h/kg) and accounted for approximately 80% of total fetal drug elimination. This may be explained by the higher percentage of fetal cardiac output to the placenta and the flow-limited transfer of this compound.(ABSTRACT TRUNCATED AT 250 WORDS)
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Riggs KW,Rurak DW,Taylor SM,McErlane BA,McMorland GH,Axelson JEdoi
10.1002/jps.2600791204subject
Has Abstractpub_date
1990-12-01 00:00:00pages
1056-61issue
12eissn
0022-3549issn
1520-6017pii
S0022-3549(15)48446-1journal_volume
79pub_type
杂志文章abstract：:Variability in the time to crystallization is a major technical and economic hurdle in using amorphous solids in dosage forms. It is hypothesized that amorphous solids "age", and that the older they are, the more relaxed they are and the higher the probability of crystallization. At present, there is no method that al...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10404
更新日期：2003-07-01 00:00:00
abstract：:The application of a stable isotope coadministration technique for estimating the fraction (fm) of imipramine (IP) that is converted to desipramine (DMI) is described. Four healthy male subjects received 25 mg of IP-d4 hydrochloride orally with 25 mg of DMI hydrochloride. The plasma concentrations of IP-d4, DMI-d4, an...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600790203
更新日期：1990-02-01 00:00:00
abstract：:A general spectroscopic method is described that might be applied to validating amino acid sequences in peptides and protein fragments with a view to it becoming a routine procedure with which to characterize biotechnology drug products. The tripeptides are the L-enantiomers of GGA, GGH, GGI, GGL, GGF, GHG, LGG, and Y...
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pub_type： 杂志文章
doi：10.1021/js980393o
更新日期：1999-07-01 00:00:00
abstract：:A rapid, sensitive, and specific determination of ketoprofen in human and animal deproteinized body fluids by reversed-phase high-pressure liquid chromatography is presented. The acid is detectable in amounts as low as 0.1 microgram/ml. Limits of error are in the range of +/- 5.1% of the sample mean. ...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600680330
更新日期：1979-03-01 00:00:00
abstract：:The solubility of a series of compounds was determined in a wide polarity spectrum of normal aliphatic alcohols over a limited temperature range. The solutes chosen were the methyl through n-butyl p-hydroxybenzoates, several of these being useful preservatives. Solubility profiles were determined for these compounds, ...
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更新日期：1977-01-01 00:00:00
abstract：:The area under the plasma concentration-time curve (AUC) was measured after an intravenous injection of sodium salicylate and after intragastric administration of aspirin, using either an intermittent sampling and the trapezoid rule (AUC-trapezoid) or the recently introduced constant blood withdrawal method (AUC-integ...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600670644
更新日期：1978-06-01 00:00:00
abstract：:Pharmaceutical cocrystals have garnered significant interest as potential solids to address issues associated with formulation development of drug substances. However, studies concerning the understanding of formulation behavior of cocrystals are still at the nascent stage. We present results of our attempts to evalua...
journal_title：Journal of pharmaceutical sciences
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abstract：:Two nonporous and three porous amorphous silicas were used as dispersion media to convert corticoid solutions into free-flowing powders. The corticoids (prednisone, prednisolone, and hydrocortisone) were dissolved in N,N-dimethylacetamide-polyethylene glycol 400 (7:3 v/v) and their 10% (w/v) solutions were mixed with ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600730330
更新日期：1984-03-01 00:00:00
abstract：:The physical state of a dosage form, crystalline versus amorphous, is critical in determining its solid-state physical and chemical properties. This minireview describes the physics associated with the preparation and storage of amorphous solids including a review of the common theories of the glass transition and rel...
journal_title：Journal of pharmaceutical sciences
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journal_title：Journal of pharmaceutical sciences
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doi：10.1021/js960196u
更新日期：1997-05-01 00:00:00
abstract：:Porcine gelatins have been widely used as stabilizers of macromolecular based pharmaceuticals but the mechanism by which they stabilize has not been precisely established. Their variability and immunogenicity, however, make them less than ideal excipients. In this work, we take advantage of the availability of recombi...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.20980
更新日期：2007-12-01 00:00:00
abstract：:Oxidation of 7,8-dimethoxy-1,2,3,4-tetrahydroisoquinoline with potassium permanganate in acetone afforded 7,8-dimethoxy-3,4-dihydroisoquinoline as the primary product. Hence, oxidation of the appropriate secondary nonphenolic 7,8-dioxygenated tetrahydroisoquinoline alkaloid is thus a facile method for the generation o...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600731137
更新日期：1984-11-01 00:00:00
abstract：:6-Chloro-9-[2-(6-methyl-3-pyridyl)ethyl]-1,2,3,4-tetrahydrocarbazole-2-carboxylic acid hydrochloride lowered serum cholesterol, triglyceride, phospholipid, and free fatty acid levels in normal rats. The compound appeared to have a low toxicity and to be well tolerated in mice, adult and neonatal rats, and rabbits. At ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600660311
更新日期：1977-03-01 00:00:00
abstract：:Adsorption of proteins to solid-fluid interfaces is often empirically found to promote formation of soluble aggregates and larger, subvisible, and visible particles, but key stages in this process are often difficult to probe directly. Aggregation mediated by adsorption to water-silicon oxide (SiOx) interfaces, akin t...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24429
更新日期：2015-06-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1016/j.xphs.2020.02.008
更新日期：2020-06-01 00:00:00
abstract：:This work investigates the use of spray freeze-drying (SFD) to produce protein loaded particles suitable for epidermal delivery. In the first part of the study, the effects of formulation and process conditions on particle properties are examined. Aqueous solutions of trehalose produce SFD particles in the size range ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10204
更新日期：2002-10-01 00:00:00
abstract：:A rapid, simple, and accurate high-performance liquid chromatographic procedure using an amino-bonded microparticulate column is reported for the determination of chlorpromazine hydrochloride (I) and its two oxidation products, the sulfoxide (II) and the sulfone (III), in commercially available pharmaceutical dosage p...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600690217
更新日期：1980-02-01 00:00:00
abstract：:The distribution of zidovudine (AZT) between plasma, brain extracellular fluid (ECF), and cerebrospinal fluid (CSF) was investigated in a crossover design study (n = 5) in unanesthetized rabbits. Drug was administered by intravenous (iv) and intracerebroventricular (icv) infusions at the same infusion rate (1.5 mg/h.k...
journal_title：Journal of pharmaceutical sciences
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更新日期：1995-07-01 00:00:00
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更新日期：1985-08-01 00:00:00
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更新日期：1989-04-01 00:00:00
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更新日期：2002-07-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600670108
更新日期：1978-01-01 00:00:00
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更新日期：2015-02-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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更新日期：1993-05-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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更新日期：2013-11-01 00:00:00
abstract：:A high-performance liquid chromatographic method has been developed for the simultaneous determination of azobenzene and hydrazobenzene in phenylbutazone and sulfinpyrazone raw materials and formulations. The drug raw material or formulation is shaken with 1N NaOH and n-hexane and centrifuged. The n-hexane layer is in...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600721032
更新日期：1983-10-01 00:00:00
abstract：:Apparent micellar molecular weights were determined with the antibiotic fusidate sodium by ultracentrifugation in varying counterion concentrations (Na+). The effects of buffer salts, pH, sodium chloride concentration, and drug concentration were studied. The results strongly support the concept of the formation of pr...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600640536
更新日期：1975-05-01 00:00:00
