Abstract：
:3-N-(1',8'-Naphthalimido)propionic acid was synthesized and shown to effectively lower both serum cholesterol and triglyceride levels in rats and mice. In hyperlipidemic mice, serum lipid levels were lowered significantly, approaching normal levels of cholesterol and below normal levels of triglyceride. The serum lipid levels were reduced due to accelerated clearance of cholesterol via the biliary route as well as a lowering of available acetyl CoA in the cytoplasm for liver de novo cholesterol and triglyceride syntheses. The liver regulatory enzyme of fatty acid and triglyceride syntheses were depressed by drug treatment. Significant reduction of liver lipids as well as the lipid content of the lipoprotein fractions were observed. The agent possessed a safe therapeutic index when used as a hypolipidemic agent.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Hall IH,Chapman JM Jr,Voorstad PJ,Cocolas GHdoi
10.1002/jps.2600730724subject
Has Abstractpub_date
1984-07-01 00:00:00pages
956-61issue
7eissn
0022-3549issn
1520-6017pii
S0022-3549(15)46224-0journal_volume
73pub_type
杂志文章abstract：:Capillary gas chromatography using an open tubular fused silica column and NP-FID was applied to the simultaneous analysis of the antihistamine, carbinoxamine, and the antitussive, hydrocodone, in human serum. Carbinoxamine and hydrocodone were extracted into methylene chloride-2-propanol (9:1) under alkaline conditio...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600721126
更新日期：1983-11-01 00:00:00
abstract：:Biopharmaceuticals represent an important and growing class of medicines. Immunogenic responses to biopharmaceuticals in patients can sometimes result in reduced safety and efficacy. Although multiple factors are known to influence immunogenicity, our understanding of the complex underlying mechanisms remains imperfec...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23247
更新日期：2012-10-01 00:00:00
abstract：:The bioavailability of single lots of 250-mg ampicillin capsules, available from 17 distributors and/or manufactures, was determined. Each product was evaluated in terms of the serum ampicillin levels achieved at 1, 2, 3, 4, 6, and 8 hr postadministration, the peak serum levels, the time of peak serum level, and the a...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600650505
更新日期：1976-05-01 00:00:00
abstract：:The aim of the study was to determine and compare the degree of swelling and the swelling kinetics of poly(ethylene oxide) (PEO) hydrophilic matrix tablets without any additives for matrixes with different molecular weight polydispersities. A wide range of "mixed" polydisperse PEO tablets were obtained by mixing two P...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21892
更新日期：2010-03-01 00:00:00
abstract：:Since its inception in the 1930s, disintegration testing has become an important quality control (QC) test in pharmaceutical industry, and disintegration test procedures for various dosage forms have been described by the different pharmacopoeias, with harmonization among them still not quite complete. However, becaus...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
doi：10.1002/jps.24303
更新日期：2015-09-01 00:00:00
abstract：:Preliminary studies indicate that it may be possible to differentiate the effects of a nephrotoxic substance from those of diuretic agents by the measurement of both urine and plasma osmolarity. The nephrotoxic substance, mercuric chloride, decreases urinary osmolality and increases plasma or serum osmolality. The diu...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600660411
更新日期：1977-04-01 00:00:00
abstract：:The aim of this study was to evaluate a strategy based on static and dynamic physiologically based pharmacokinetic (PBPK) modeling for the prediction of metabolite and parent drug area under the time-concentration curve ratio (AUCm/AUCp) and their PK profiles in humans using in vitro data when active transport process...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2017.03.032
更新日期：2017-09-01 00:00:00
abstract：:A GLC method for the determination of valproic acid and ethosuximide in plasma was developed. The procedure involved a single solvent extraction of drugs from acidified plasma samples, followed by a GLC injection of the unconcentrated organic phase. This rapid, sensitive, specific, and reproducible method has been use...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600710126
更新日期：1982-01-01 00:00:00
abstract：:The present study was carried out to investigate the blood-to-retina transport of nicotine across the inner blood-retinal barrier (BRB). Using the in vivo vascular injection method, the blood-to-retina influx clearance of nicotine across the BRB was determined as 131 μL/(min?g retina), which is much higher than that o...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24453
更新日期：2015-09-01 00:00:00
abstract：:The diterpene esters, genkwadaphnin and yuanhuacine, have been shown to possess significant antileukemic activity in the P-388 screen. The major metabolic effects of the diterpene esters were on DNA and protein synthesis. The effects on DNA synthesis in vitro were evoked at a lower concentration than that required for...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600711120
更新日期：1982-11-01 00:00:00
abstract：:Foam granulation is a relatively newer wet granulation process whereby foamed binder solutions are added to powders in a mixer. It is essential to understand the effect of powder substrate on foam drainage and half-life, which are relevant to nucleation and agglomeration during foam granulation. Hydroxypropyl methylce...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23053
更新日期：2012-04-01 00:00:00
abstract：:The solubilization of five model hydrophobic drugs by a series of micelle-forming, water-soluble methoxy poly(ethylene glycol)-block-polycaprolactone diblock copolymers (MePEG-b-PCL) with varying methoxy poly(ethylene glycol) (MePEG) and polycaprolactone (PCL) block lengths was investigated. Variation of the feed weig...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21037
更新日期：2008-03-01 00:00:00
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
pub_type： 杂志文章
doi：10.1002/jps.2600740819
更新日期：1985-08-01 00:00:00
abstract：:High protein concentration formulations are required for low-volume administration of therapeutic antibodies targeted for subcutaneous, self-administration by patients. Ultra-high concentrations (≥150 mg/mL) can lead to dramatically increased solution viscosities, which in turn can lead to stability, manufacturing, an...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2017.06.017
更新日期：2017-11-01 00:00:00
abstract：:The reactions of omeprazole, a potent proton pump inhibitor (PPI), were investigated in the absence of a nucleophile. Reactions were monitored, using differential pulse polarography (DPP) at the static mercury drop electrode (SMDE), in solutions buffered to pH values ranging from 2.0 to 8.0. The fast, sensitive, and s...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20546
更新日期：2006-02-01 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
pub_type： 杂志文章
doi：10.1016/j.xphs.2017.09.013
更新日期：2018-02-01 00:00:00
abstract：:TLC analysis of extracts of Pilosocereus maxonii (Rose) Byles and Rowley detected six identifiable alkaloids. Preparative TLC aided in the crystallization of the hydrochlorides of N-methyl-3,4-dimethoxyphenethylamine, N-methyl-3-methoxytyramine, and N,N-dimethyl-3-methoxytyramine. Traces of 3,4-dimethoxyphenethylamine...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600661037
更新日期：1977-10-01 00:00:00
abstract：:A pharmacokinetic model that permits prediction of aqueous humor pilocarpine levels following topical application to rabbit eyes was developed. The model is able to account for changes in both instilled solution volume and drug concentration. The model, although simplified, relies mainly on experimentally verifiable a...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670507
更新日期：1978-05-01 00:00:00
abstract：:Daunorubicin (DAUN) and doxorubicin (DOX) are used to treat a variety of cancers. The use of DAUN and DOX is hampered by the development of cardiotoxicity. Clinical evidence suggests that patients with leukemia and Down syndrome are at increased risk for anthracycline-related cardiotoxicity. Carbonyl reductases and al...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2016.03.013
更新日期：2016-06-01 00:00:00
abstract：:Allopurinol exhibits good bioavailability (78-90%) after administration of oral dosage forms to humans and rabbits; however, it is not absorbed rectally from any of the dosage forms to any significant extent. Oral administration of allopurinol in a polyethylene glycol suspension, to which allopurinol may be reversibly...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600750314
更新日期：1986-03-01 00:00:00
abstract：:A procedure is described for the analysis of urushiol content of pharmaceutical preparations containing extracts of poison ivy (Toxicodendron radicans) and poison oak (T. diversilobum) in vegetable oils. The procedure involves extraction of the urushiols from the oily solutions using 90% methanol in water followed by ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600690530
更新日期：1980-05-01 00:00:00
abstract：:A method for the determination of sematilide levels in human plasma is described. After the addition of an internal standard, plasma samples are adjusted to pH 8.5 and extracted with a solution of 7.5% isopropanol in methylene chloride. Separation from co-extracted matrix constituents is performed by reversed-phase HP...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600800214
更新日期：1991-02-01 00:00:00
abstract：:A kinetic dialysis technique together with a radiolabeled chenodeoxycholate (CDC) was used to determine the existence of a relationship between the monomer concentration of CDC and the total CDC concentration in different CDC solutions containing 1 or 5 mM sulfobutylether (SBE)-β-cyclodextrin. On the basis of the natu...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23231
更新日期：2012-08-01 00:00:00
abstract：:The inhibitory effect of dioctyl sodium sulfosuccinate of hog pepsin activity was investigated over the pH 1.5-3.0 range. The inhibitory effect was studied using a natural substrate, hemoglobin, and a synthetic substrate, N-acetyl-L-phenylalanyl-L-diiodotyrosine. The mechanistic studies revealed that a substrate-inhib...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600650914
更新日期：1976-09-01 00:00:00
abstract：:A rapid, sensitive, and accurate reversed-phase HPLC method has been developed for the analysis and quantification of pharmaceutical formulations containing tyrothricin (1), an antibiotic used in antiseptic buccal compressed tablets for local application. The assay has been carried out under isocratic conditions, usin...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600830815
更新日期：1994-08-01 00:00:00
abstract：:To evaluate oral mucosal absorption of drugs in dogs, a newly designed in situ perfusion system with a circulating perfusion chamber was developed. The utility of the perfusion system was investigated by using three drugs: salicylic acid (SA), sulfadimethoxine (SM), and diltiazem (DIL). The oral mucosal absorption of ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600791103
更新日期：1990-11-01 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：:Virtually all biological variables, including those affected by drugs, are subject to adaptive self regulation. In the description of the pharmacodynamics (PD) of drugs, it may be necessary to consider the endogenous control system (ECS) as an integral part of the PD. A PDECS model based on system analysis principles ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600820310
更新日期：1993-03-01 00:00:00
abstract：:A rotating-basket apparatus for dissolution testing of veterinary bolus tablets was designed and constructed. Sulfamethazine boluses containing different disintegrating agents were evaluated in vitro and by blood level data following administration to cattle. The dissolution t50 and various pharmacokinetic parameters ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600651231
更新日期：1976-12-01 00:00:00
abstract：:Selected synthetic luteinizing hormone releasing hormone preparations were assayed, and their potencies were determined relative to one sample utilizing primary cultures of enzymatically dispersed rat anterior pituitary cells. Preliminary cell culture experiments indicated that luteinizing hormone releasing hormone ha...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600660319
更新日期：1977-03-01 00:00:00
