Abstract:
:Bouvardin is a cyclic hexapeptide antitumor agent which undergoes two major microbial transformation reactions. Screening with 220 cultures revealed 17 different strains capable of producing O-desmethylbouvardin in good yield. O-Desmethylbouvardin was isolated and characterized from preparative scale incubations with Streptomyces rutgersensis NRRL B-1256. Four aspergilli and one streptomycete formed bouvardin catechol when O-desmethylbouvardin was used as substrate. Bouvardin catechol was isolated and characterized from a preparative scale incubation with Aspergillus ochraceous UI 398.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Petroski RJ,Bates RB,Linz GS,Rosazza JPdoi
10.1002/jps.2600721114subject
Has Abstractpub_date
1983-11-01 00:00:00pages
1291-4issue
11eissn
0022-3549issn
1520-6017pii
S0022-3549(15)44872-5journal_volume
72pub_type
杂志文章abstract::High-throughput lyophilization process was designed and developed for protein formulations using a single-step drying approach at a shelf temperature (Ts) of ≥40°C. Model proteins were evaluated at different protein concentrations in amorphous-only and amorphous-crystalline formulations. Single-step drying resulted in...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2018.11.021
更新日期:2019-04-01 00:00:00
abstract::The anticonvulsant and CNS-depressant activities of 16 commercially available antiepileptics were subjected to regression analysis. For the maximal electroshock seizure test and pentylenetetrazol seizure threshold test, good correlations were obtained only after diazepam, clonazepam, and carbamazepam were deleted; for...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600680418
更新日期:1979-04-01 00:00:00
abstract::Water evaporation rates were measured from thin samples of a model layered structure of stratum corneum lipids with 32% water. A model with only free fatty acids present gave the lowest evaporation rates, while a model with only oleic acid gave values approximately 50% higher. Using the total lipid spectrum of stratum...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600780808
更新日期:1989-08-01 00:00:00
abstract::Currently, conjunctivitis is treated by frequent high dose administration of sparfloxacin eye drop solution. However, the eye drops are inconvenient because of low bioavailability, short ocular drug residence time, and need of frequent instillation, which lead to patient noncompliance affecting the routine life style ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2020.02.008
更新日期:2020-06-01 00:00:00
abstract::First-order rate constants (k) were determined for the hydrolysis of ceftazidime in the pH range of 0.5 to 8.5 at 45, 55, and 65 degrees C by a stability-indicating HPLC assay. In the absence of buffer effects, the pH-rate expression was k = kH1f1(aH+) + kH2f2(aH+) + kH3f3(aH+) + kSf3 + kOHf3(aOH-), where KH and KOH a...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600840504
更新日期:1995-05-01 00:00:00
abstract::This study is to prepare and evaluate Pluronics-modified mixed micelle (MM) to deliver polyphenolic myricetin (MYR) across the blood-brain barrier. MYR has been proven to be an effective anticancer agent against glioblastoma cells in our previous studies. However, the poor solubility of MYR limits its access to the br...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2016.01.016
更新日期:2016-04-01 00:00:00
abstract::Different approaches for the colorimetric determination of acetaminophen, based on its coupling with diazotized o-nitroaniline, are described. Copper(II) chelation with the coupled compound makes the method highly selective. Sensitivity is increased when the acetaminophen assay is carried out indirectly through the de...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600680626
更新日期:1979-06-01 00:00:00
abstract::Central-nervous-system, physiologically based pharmacokinetic (PBPK) models predict exposure profiles in the brain, that is, the rate and extent of distribution. The current work develops one such model and presents improved methods for determining key input parameters. A simple linear regression statistical model est...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2015.12.005
更新日期:2016-02-01 00:00:00
abstract::The single pass mean residence time in peripheral tissues, tp1, is a characteristic constant of linear pharmacokinetic systems and nonlinear systems with linear distribution kinetics. It is descriptive of distribution kinetics in such systems and is not dependent on elimination kinetics as are other related parameters...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600751202
更新日期:1986-12-01 00:00:00
abstract::A GLC method for determining theophylline, hydroxyethyltheophylline, and diphenylpyraline hydrochloride is presented. The method permits the separation and quantitative determination of the therapeutically active ingredients with a single injection in an overall time of approximately 2.5 hr. ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600680438
更新日期:1979-04-01 00:00:00
abstract::The combined clearance of endogenous 6β-hydroxycortisol and 6β-hydroxycortisone is suggested biomarker for in vivo cytochrome P450 3A (CYP3A) activity. We aimed to determine whether the combined clearance of these two markers together with information of biopharmaceutics classification system (BCS) of drugs could be u...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.24566
更新日期:2015-10-01 00:00:00
abstract::Many active pharmaceutical ingredients exhibit a needle-like (acicular) crystal habit, which can significantly complicate their downstream processing. In this study, the acicular crystal habit of a model active pharmaceutical ingredient, 5-aminosalicylic acid (5-ASA), was modified by addition of selected organic solve...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2017.12.005
更新日期:2018-04-01 00:00:00
abstract::The stereoselective pharmacokinetics of suprofen enantiomers has been studied in humans by means of stable isotope-labeled pseudoracemate-diastereomer methodology. After a single oral dose of a near equimolar mixture of unlabeled-(R)-(-)- and [2H3]-(S)-(+)-suprofen [or unlabeled-(S)- and [2H3]-(R)-suprofen] to three h...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600801116
更新日期:1991-11-01 00:00:00
abstract::Development of high-throughput release and characterization assays is critical for the effective support of the rapidly growing biologics pipeline for biotherapeutics. Clipping of polypeptide chains is commonly monitored during process optimization, formulation development, and stability studies. A reduced capillary e...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.22710
更新日期:2011-12-01 00:00:00
abstract::Recent oxidation events on monoclonal antibody candidates prompted us to investigate the mechanism of oxidation of Met, Trp, and His residues and to search for suitable stabilizers. By using parathyroid hormone (1-34), PTH, as a model protein and various oxidants, aided by liquid chromatography, peptide mapping, and m...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.21746
更新日期:2009-12-01 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 antifungal drug, 5-fluorocytosine (FC), is marketed as a capsule (250 or 500 mg strength) instead of the preferred tablet dosage form. Through systematic characterization of solid-state properties, including mechanical properties, we identify tabletability and poor physical stability of FC as the problems that lik...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23876
更新日期:2014-04-01 00:00:00
abstract::The effects of physical aging and antiplasticization on the water transport properties of glassy cellulose acetate film-coated tablets were investigated. The gradual approach toward thermodynamic equilibrium during physical aging decrease the free volume of the polymers. This decrease in free volume is accompanied by ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600830337
更新日期:1994-03-01 00:00:00
abstract::Quantification of protein binding of new chemical entities is an important early screening step during drug discovery and is of fundamental interest for the estimation of safety margins during drug development. In this publication, we describe the development of a new high-throughput assay for the determination of the...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.10588
更新日期:2004-04-01 00:00:00
abstract::Hydrolytic degradation products of cefdinir were studied in acidic (pH 1), neutral (pH 6), and basic (pH 9) solutions. Seven major degradation products were isolated by preparative and/or high-performance liquid chromatography and characterized by UV, IR, 1H-NMR, and mass spectra. To clarify degradation pathways in ea...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js950446r
更新日期:1996-09-01 00:00:00
abstract::Cationic antimicrobial peptides are good candidates for new diagnostics and antimicrobial agents. They can rapidly kill a broad range of microbes and have additional activities that have impact on the quality and effectiveness of innate responses and inflammation. Furthermore, the challenge of bacterial resistance to ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章,评审
doi:10.1002/jps.21034
更新日期:2008-05-01 00:00:00
abstract::Employing the roots of Iris missouriensis, two known triterpenes, iso-iridogermanal and zeorin, were isolated and identified. As presently reported, they were found to demonstrate cytotoxic activity toward cultured P-388 cells (ED50 = 0.1 and 1.1 microgram/mL, respectively). Additionally, a new triterpene that demonst...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600750324
更新日期:1986-03-01 00:00:00
abstract::The objective of the present study was to investigate the iontophoretic transport behavior across multiple membranes of different barrier properties. Spectra/Por(R) (SP) and Ionac membranes were the synthetic membranes and sclera was the biomembrane in this model study. The barrier properties of SP membranes were dete...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.21231
更新日期:2008-01-01 00:00:00
abstract::Solid samples of 1-hydroxymethyl- and 1,5-dihydroxymethylallopurinol, 1-hydroxymethylglutethimide, and 1-hydroxymethylphenobarbital were prepared, and equilibrium constants for their formation from formaldehyde and allopurinol, glutethimide, or phenobarbital were calculated. The N-hydroxymethyl derivatives had higher ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600700804
更新日期:1981-08-01 00:00:00
abstract::Plasma and various organ concentrations of canrenone, canrenoate, and total 3H-activity were measured following single doses of 20 mg of 3H-canrenoate/kg iv to rabbits. Organs studied included heart, lungs, brain, kidneys, liver, adrenal glands, and spleen. Canrenoate was shown to be in rapid equilibrium with canrenon...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600660237
更新日期:1977-02-01 00:00:00
abstract::The stereochemistries of geometric isomers of 4-(2-bromo-1,2-diphenylvinyl)phenol, 4-(2-bromo-1,2-diphenylvinyl)anisole, and 2-[p-(2-bromo-1,2-diphenylvinyl)phenoxy]triethylamine were determined by conversion of the phenolic analog to the ethers and subsequent comparison of physical properties with those of 2-[p-(2-ch...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600651036
更新日期:1976-10-01 00:00:00
abstract::A crude chloroform-soluble fraction of the ethanol extract of the leaves of Bursera klugii showed activity against two test systems, the P-388 lymphocytic leukemia (3PS) and the human epidermoid carcinoma of the nasopharynx (9KB). The PS activity was due to two constituents, sapelins A and B. ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600660645
更新日期:1977-06-01 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::Understanding the coating unit operation is imperative to improve product quality and reduce output risks for coated solid dosage forms. Three batches of sustained-release tablets coated with the same process parameters (pan speed, spray rate, etc.) were subjected to terahertz pulsed imaging (TPI) analysis followed by...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.21766
更新日期:2009-12-01 00:00:00
abstract::Hydrogen triiodide adducts were prepared from N,N-dimethylacetamide, N-alkylpyrrolidone derivatives, and polyvinylpyrrolidone, and their structures were investigated by IR spectra and X-ray structure analyses and compared with the structure of povidone-iodine USP. The results suggest that the iodine in povidone-iodine...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600681211
更新日期:1979-12-01 00:00:00