Abstract：
:The fungal microorganism Cunninghamella echinulata was utilized to para-hydroxylate the synthetic substrate (+/-)-1-isopropylamino-3-phenoxy-propan-2-ol (1). The resulting product, (+/-)-1-(4-hydroxyphenoxy)-3-isopropylamino-propan-2-ol, or (+/-)-prenalterol, (2) was formed in greater than 85% yield. Extracts from incubates were derivatized with trifluoroacetic anhydride and the concentrations of 1 and 2 were determined by GC on a fused silica methyl silicone capillary column with nitrogen-phosphorus detection. At substrate concentrations of 100 and 200 mg/L, the biotransformation proceeds with apparent first-order kinetics. With higher concentrations, the kinetics of prenalterol formation and substrate uptake appear to be nonlinear with a Km value of 427.8 micrograms/mL and a Vmax value of 232.3 micrograms/mL/d. This suggests that the biotransformation may proceed through a single-capacity limited pathway. The microbial product was isolated and identified as (+/-)-prenalterol by comparison (mp, IR, MS, 1H NMR) with an authentic specimen.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Pasutto FM,Singh NN,Jamali F,Coutts RT,Abuzar Sdoi
10.1002/jps.2600760220subject
Has Abstractpub_date
1987-02-01 00:00:00pages
177-9issue
2eissn
0022-3549issn
1520-6017pii
S0022-3549(15)47351-4journal_volume
76pub_type
杂志文章abstract：:Regular insulin, NPH insulin, glargine insulin, calcitonin, and human growth hormone were administered to rats nasally with 0.125% tetradecyl-beta-D-maltoside (TDM), or at various times after TDM treatment. Absorption of all five peptides was enhanced initially and diminished in a time-dependent manner as the interval...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21977
更新日期：2010-04-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600740819
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pub_type： 杂志文章
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更新日期：2015-04-01 00:00:00
abstract：:A mathematical model based on convective diffusion was developed to describe the rate of dissolution form the surface of a compressed compact. Experimental studies were carried out to test the model. The basic experimental apparatus consisted of a modified rotating-filter-stationary basket dissolution test apparatus. ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600640407
更新日期：1975-04-01 00:00:00
abstract：:The capacity factors of several penicillins and cephalosporins, as well as those of 7-aminocephalosporanic acid, 6-aminopenicillanic acid, and 7-aminodeacetoxycephalosporanic acid, were determined at pH 2.5-7.5 with different methanol concentrations in the mobile phase. The influence of ionic strength on activity fact...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600690506
更新日期：1980-05-01 00:00:00
abstract：:The objective of this study was to examine the ocular absorption behavior of an amphiphilic prodrug after instillation onto the cornea of rabbits. A micellar solution of O-palmitoyl tilisolol (PalTL), an amphiphilic prodrug, was prepared. After instillation of tilisolol (TL) and PalTL, the drug concentrations in the t...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.1162
更新日期：2001-12-01 00:00:00
abstract：:Electron micrographs of Pseudomonas aeruginosa grown in nutrient broth or broth containing subinhibitory concentrations of benzalkonium chloride indicate that benzalkonium chloride at 50 and 100 mug/ml strips off the outer cell membrane. Cells grown in the presence of edetate disodium, 50-100 mug/ml had convoluted sur...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600650115
更新日期：1976-01-01 00:00:00
abstract：:Spray-dried dispersions (SDDs) are an important technology for enhancing the oral bioavailability of poorly water-soluble drugs. To design an effective oral SDD formulation, the key rate-determining step(s) for oral drug absorption must be understood. This work combined in vivo and in vitro tests with in silico modeli...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2018.09.031
更新日期：2019-01-01 00:00:00
abstract：:Crystallization of drugs in metastable, supersaturated adhesive polymeric matrices in transdermal drug delivery devices can be avoided by determination of the solubility of the drug in the adhesive polymer. A novel method is described to determine the solubility of the drug in polymeric matrices. Unlike existing metho...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.20122
更新日期：2004-08-01 00:00:00
abstract：:Literature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate-release, solid oral dosage forms containing enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhi...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
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更新日期：2017-08-01 00:00:00
abstract：:Despite being a major breakthrough in multiple myeloma therapy, carfilzomib (CFZ, a second-generation proteasome inhibitor drug) has been largely ineffective against solid cancer, possibly due to its pharmacokinetic drawbacks including metabolic instability. Recently, quinic acid (QA, a low-affinity ligand of selectin...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2020.01.008
更新日期：2020-04-01 00:00:00
abstract：:In this study the relationships between previously reported connectivity indices described by Kier and Hall and steric contributions to the rate constants for several series of reactions are examined. Rate data were examined for four different series of reactions, which were chosen to represent a range of different re...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600731038
更新日期：1984-10-01 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, ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600660110
更新日期：1977-01-01 00:00:00
abstract：:The role of particle size and surface modification on biodistribution of nanocarriers is widely reported. We report for the first time the role of nanoparticle shape on biodistribution. Our study demonstrates that irregular shaped polymer lipid nanoparticles (LIPOMER) evade kupffer cells and localize in the spleen. We...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.22052
更新日期：2010-06-01 00:00:00
abstract：:Flumizole is a potent anti-inflammatory agent in animal models with an inhibitory activity severalfold that of indomethacin in rat foot edema and prostaglandin synthetase tests. The drug was well absorbed from the GI tract when administered in the solution used in pharmacological assays. However, markedly poorer absor...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600640909
更新日期：1975-09-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2017.11.005
更新日期：2018-03-01 00:00:00
abstract：:Two types of drug release mechanisms-matrix controlled (Q - t1/2 relationship) and partition controlled (Q - t relationship)-were reported previously. The dependency of the transition between these two processes on the solution solubility of drug is now analyzed. Mathematical expressions are derived to treat the syste...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600641011
更新日期：1975-10-01 00:00:00
abstract：:The challenge of defining the concentration of unbound drug at the lung target site after inhalation limits the possibility to optimize target exposure by compound design. In this study, a novel rat lung slice methodology has been developed and applied to study drug uptake in lung tissue, and the mechanisms by which t...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24575
更新日期：2016-02-01 00:00:00
abstract：:The purpose of this study was to elucidate the effect of heat treatment on the miscibility of multiple concentrated solutes that mimic biopharmaceutical formulations in frozen solutions. The first heating thermal analysis of frozen solutions containing either a low-molecular-weight saccharide (e.g., sucrose, trehalose...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.22706
更新日期：2011-12-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600690318
更新日期：1980-03-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670122
更新日期：1978-01-01 00:00:00
abstract：:The influence of various test meals and coadministered water volumes on erythromycin stearate bioavailability from orally dosed film-coated tablets was studied in healthy human subjects. Serum erythromycin levels were uniformly reduced by all test meals, with the reduction in mean peak serum levels varying from 47 to ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670608
更新日期：1978-06-01 00:00:00
abstract：:A modified NF method for the quantitative determination of pentaerythritol tetranitrate is reported. A solution of powder is made directly from the dosage form in glacial acetic acid and is then reacted with phenoldisulfonic acid TS. The proposed method saves approximately 75% of the time required with the NF method. ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670543
更新日期：1978-05-01 00:00:00
abstract：:The present study was conducted to investigate the impact of drying method and formulation on the storage stability of IgG1. Formulations of IgG1 with varying levels of sucrose with and without surfactant were dried by different methods, namely freeze drying, spray drying, and foam drying. Dried powders were character...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20859
更新日期：2007-08-01 00:00:00
abstract：:It is now becoming apparent that a common pathway of protein aggregation involves the unimolecular structural rearrangement from the native state to a slightly expanded aggregation-competent species. It is the goal of this study to understand the aggregation and the effects of buffer on the stability of IFN-tau. In th...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20471
更新日期：2006-06-01 00:00:00
abstract：:Plasma levels were determined frequently after single doses of perfluorooctyl bromide were administered to beagle dogs at doses of either 30.8 g/kg po or 3.9 g/kg intratracheally. The apparent first-order half-life during the terminal elimination phase was about 1 day after oral medication and about 7 days after intra...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670751
更新日期：1978-07-01 00:00:00
abstract：:Vehicle effects may be caused by thermodynamic effects and by specific (penetration enhancing) effects. To investigate the effects of various lipophilic vehicles on drug penetration, an in vivo permeability study was conducted with methyl nicotinate as the model drug. The drug was dissolved in the respective vehicles ...
journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章
doi：10.1002/jps.2600840214
更新日期：1995-02-01 00:00:00
abstract：:Controlled-release delivery of 6-beta-naltrexol (NTXOL), the major active metabolite of naltrexone, via a transdermal patch is desirable for treatment of alcoholism. Unfortunately, NTXOL does not diffuse across skin at a therapeutic rate. Therefore, the focus of this study was to evaluate microneedle (MN) skin permeat...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.22083
更新日期：2010-07-01 00:00:00
abstract：:SPRYCEL® (Dasatinib) is a Biopharmaceutical Classification System II weakly basic drug that exhibits strong pH-dependent solubility. Dasatinib is currently presented in 2 drug product formulations as an adult immediate release tablet and a pediatric powder for oral suspension. A bioequivalence study comparing the form...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2018.11.005
更新日期：2019-01-01 00:00:00
abstract：:Ascorbic acid has a unique role in the prevention and treatment of a large number of chronic diseases, including skin disorders but it can hardly penetrate the skin due to its solubility in water and its high instability. This study explored the formation of phosphatidylcholine-based vesicles upon addition of ascorbyl...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2020.06.017
更新日期：2020-10-01 00:00:00
