Abstract：
:The intrinsic absorption of salbutamol in different intestinal segments of the rat was measured and related with the corresponding intestinal P-glycoprotein (P-gp) expression levels. The apparent absorption rate constants (k(a), h(-1)) observed in each fraction by means of the "in situ" rat gut absorption method after perfusion of a 0.29-mM isotonic solution of salbutamol were used as absorption indexes. In a separate series of studies, a semiquantitative analysis of the mRNA expression of P-gp by means of polymerase chain reaction and Western blot with an antibody raised against the P-gp were also performed. The "in situ" k(a) values determined in the different segments (h(-1)) showed that the absorption is not homogeneous along the intestinal tract, that is, 0.499 +/- 0.054 for colon, 0.474 +/- 0.052 for the proximal segment, 0.345 +/- 0.014 for the mean, and 0.330 +/- 0.023 for the distal fraction. Addition of verapamil to the perfusion fluid did provide a better absorption of salbutamol in the distal segment. The analysis of the mRNA expression and levels of P-gp showed that the enzyme content in each section of the intestine was inversely related to salbutamol absorption.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Valenzuela B,Nácher A,Ruiz-Carretero P,Martín-Villodre A,López-Carballo G,Barettino Ddoi
10.1002/jps.20071subject
Has Abstractpub_date
2004-06-01 00:00:00pages
1641-8issue
6eissn
0022-3549issn
1520-6017pii
S0022-3549(16)31528-3journal_volume
93pub_type
杂志文章abstract：:Sucrose fatty acid esters are increasingly used as excipients in pharmaceutical products, but few data are available on their toxicity profile, mode of action, and efficacy on intestinal epithelial models. Three water-soluble sucrose esters, palmitate (P-1695), myristate (M-1695), laurate (D-1216), and two reference a...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600720609
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doi：10.1002/jps.2600711206
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doi：10.1002/jps.20883
更新日期：2007-11-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600650117
更新日期：1976-01-01 00:00:00
abstract：:A combination of coformer screening and modeling, followed by characterization using calorimetry, structure elucidation, and solubility led to the identification of novel crystalline forms of the hepatitis C protease inhibitor, telaprevir. The lead crystalline form, a cocrystalline solid of telaprevir with 4-aminosaly...
journal_title：Journal of pharmaceutical sciences
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更新日期：2015-10-01 00:00:00
abstract：:Two novel series of benzimidazole derivatives bearing structural modifications of certain drugs were prepared for evaluation for potential anticancer activity. The first series was a group of alkylating agents, and the second series was a variety of 4-substituted-1-thioacetyl-3-thiosemicarbazides. The tests of some re...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600691130
更新日期：1980-11-01 00:00:00
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doi：10.1021/js980070s
更新日期：1998-11-01 00:00:00
abstract：:The purpose of this study was to investigate the phase-sensitive delivery systems (D,L-polylactide in triacetin) for controlled delivery of insulin at basal level. The effect of varying concentration of zinc, polymer, and insulin on the in vitro release of insulin was evaluated. Stability of released insulin was inves...
journal_title：Journal of pharmaceutical sciences
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abstract：:Evidence is provided for the existence of a second discrete chemical form of meropenem at clinically relevant concentrations prepared from the marketed formulation of the drug. Proton and carbon-13 NMR spectra in D2O, coupled with tandem mass spectroscopy (MS/MS) and cross polarization/magic angle spinning (CP-MAS) NM...
journal_title：Journal of pharmaceutical sciences
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doi：10.1021/js970370u
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abstract：:Three analogs of thyroliberin (I) were prepared. These compounds, N-m-chloroacetylbenzoyl-phenylalanyl-prolineamide (VIa), N-p-chloroacetylbenzoyl-phenylalanyl-prolineamide (VIb) and N-chloroacetyl-alanyl-phenylalanyl-prolineamide (IX), were designed as potential I antagonist affinity labels. However, no significant a...
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doi：10.1002/jps.2600710928
更新日期：1982-09-01 00:00:00
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pub_type： 临床试验,杂志文章
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abstract：:A series of gem-cichlorocyclopropyl and cyclopropyl analogs of stilbene congeners was synthesized and examined for estrogenic and antiestrogenic activity using the uterotropic assay in the immature mouse. The relative receptor affinity in vitro was determined by measuring [3H]estradiol displacement from the rat uterin...
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doi：10.1002/jps.2600711012
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abstract：:Cephalosporins are among the most frequently used broad-spectrum antimicrobial agents. Ceftazidime is a semisynthetic β-lactam antibiotic for parenteral administration widely used in the clinical practice, which has been categorized as a third-generation cephalosporin antibiotic. This drug crystallizes as a pentahydra...
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abstract：:A series of 1-(substituted benzyl)-3,4,5,6-tetrahydro-2(1H)-pyrimidones was synthesized primarily by catalytic hydrogenation of the corresponding 1-(substituted benzyl)-2(1H)-pyrimidone. The pharmacological evaluation of these compounds in mice revealed a unique profile that included evidence of CNS stimulation and de...
journal_title：Journal of pharmaceutical sciences
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更新日期：1980-10-01 00:00:00
abstract：:Phenylpropanolamine was determined by measuring its fluorescent fluorescamine derivative. The method is rapid, sensitive, and easily automated. Statistics are presented for an effervescent cold product, and recovery data are presented for other commercially available products. ...
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doi：10.1002/jps.2600671137
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abstract：:Coralyne analogues, isomers, and related alkaloids were examined as inhibitors of reverse transcriptase of RNA tumor viruses in the presence of polyriboadenylic acid-oligodeoxythymidylic acid (Poly rA.oligo dT), polydeoxyadenylic acid-oligodeoxythymidylic acid (Poly dA.oligo dT), polyribocytidylic acid-oligodeoxyguany...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600740819
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abstract：:A method for the measurement of a potential diuretic-antihypertensive agent, (+/-)-[[6,7-dichloro-2-(4-fluorophenyl)-2-methyl-1-oxo-5-indanyl] oxy]acetic acid, in biological fluids is described. The procedure involves the addition of a related internal standard to the specimens followed by extraction of the acids into...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600730234
更新日期：1984-02-01 00:00:00
abstract：:The crystal structure of the common therapeutic agent, the pentahydrated sodium salt of L-thyroxine hormone (3-[4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl]-L-alanine), has been determined and discussed in relation to the drug's stability. The stoichiometry and absolute configuration (-)-C(8)S-[C15H10I4NO4]-.Na+....
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doi：10.1002/jps.20155
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journal_title：Journal of pharmaceutical sciences
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