Prediction of the possibility of the second peak of drug plasma concentration time curve after iv bolus administration from the standpoint of the traditional multi-compartmental linear pharmacokinetics.

abstract：:Various novel diesters of pilocarpic acid were synthesized and evaluated as prodrug forms for pilocarpine with the aim of improving the ocular delivery characteristics of the drug. The pilocarpic acid monoesters previously studied cyclized spontaneously to pilocarpine in aqueous solution and although they showed enhan...

journal_title：Journal of pharmaceutical sciences

authors： Bundgaard H,Falch E,Larsen C,Mosher GL,Mikkelson TJ

更新日期：1986-08-01 00:00:00

abstract：:A simple enzyme immunoassay for the determination of captopril was developed. A specific antibody for captopril was produced in rabbits that were immunized with a hapten-bovine immunoglobulin G conjugate, which was prepared by using 4-(maleimidomethyl)cyclohexane carboxylic acid as a spacer group. The limit of detecti...

journal_title：Journal of pharmaceutical sciences

authors： Kinoshita H,Nakamaru R,Tanaka S,Tohira Y,Sawada M

更新日期：1986-07-01 00:00:00

abstract：:Present study aims to improve efficiency and capacity of in vivo rat pharmacokinetic studies for rapid assessment of systemic exposure (AUC and C(max)) of new chemical entities. Plasma concentration-time profiles in rats from structurally diverse compounds were extracted from the Pfizer database. AUC(0-8) was calculat...

journal_title：Journal of pharmaceutical sciences

authors： Han HK,Sadagopan N,Reichard GA,Yapa U,Zhu T,Hubbel A,Johnson K,Brodfuehrer J

更新日期：2006-08-01 00:00:00

abstract：:One of the challenges with predictive modeling is how to quantify the reliability of the models' predictions on new objects. In this work we give an introduction to conformal prediction, a framework that sits on top of traditional machine learning algorithms and which outputs valid confidence estimates to predictions ...

journal_title：Journal of pharmaceutical sciences

authors： Alvarsson J,Arvidsson McShane S,Norinder U,Spjuth O

更新日期：2021-01-01 00:00:00

abstract：:The hydrolysis of acetylcholine and acetylcholine mustard by acetylcholinesterase was compared over a substrate concentration range of 1-10 mM. Reactions were allowed to proceed for 2 min at 25 degrees. Results of these experiments reveal that the substrates have similar affinities for the enzyme, whereas the maximum ...

journal_title：Journal of pharmaceutical sciences

authors： Hudgins PM,Stubbins JF

更新日期：1975-08-01 00:00:00

abstract：:Pancreatic islet transplantation is a promising advanced therapy that has been used to treat patients suffering from diabetes type 1. Traditionally, pancreatic islets are infused via the portal vein, which is subsequently intended to engraft in the liver. Severe immunosuppressive treatments are necessary, however, to ...

journal_title：Journal of pharmaceutical sciences

authors： Scheiner KC,Coulter F,Maas-Bakker RF,Ghersi G,Nguyen TT,Steendam R,Duffy GP,Hennink WE,O'Cearbhaill ED,Kok RJ

更新日期：2020-01-01 00:00:00

abstract：:The kinetics of acetylation of alcohols by acetyl chloride and acetic anhydride, with N-methylimidazole as the catalyst, were studied in acetonitrile solution at 25 degrees; some measurements were also made with 4-dimethylaminopyridine as the catalyst. The acetic anhydride-N-methylimidazole system proceeds entirely by...

journal_title：Journal of pharmaceutical sciences

authors： Pandit NK,Connors KA

更新日期：1982-05-01 00:00:00

abstract：:The effects of permeant charge (z) on iontophoretic-enhanced transport were investigated with synthetic Nucleopore membranes and with human epidermal membranes using a four-electrode potentiostat with side-by-side diffusion cells. The modified Nernst-Planck model (Nernst-Planck theory with an additional transport term...

journal_title：Journal of pharmaceutical sciences

authors： Li SK,Ghanem AH,Peck KD,Higuchi WI

更新日期：1997-06-01 00:00:00

abstract：:Hard gelatin capsule (HGC) shells are widely used to encapsulate drugs for oral delivery but are vulnerable to gelatin cross-linking, which can lead to slower and more variable in vitro dissolution rates. Adding proteolytic enzymes to the dissolution medium can attenuate these problems, but this complicates dissolutio...

journal_title：Journal of pharmaceutical sciences

authors： Likar MD,Carroll SC,Colgan ST,Yeoh T,MacDonald BC,Johnson GM,Space JS

更新日期：2018-12-01 00:00:00

abstract：:Pretreatment with cyclosporine reportedly prolongs the effect of certain general anesthetics in humans and the sleeping time of mice after pentobarbital administration. This investigation was designed to determine the mechanism(s) of the cyclosporine-barbiturate interaction. Adult female Wistar rats received cyclospor...

journal_title：Journal of pharmaceutical sciences

authors： Hoffman A,Levy G

更新日期：1990-01-01 00:00:00

abstract：:A sensitive, specific and reproducible high-performance liquid chromatographic procedure, using the normal phase and radial compression system, is described for the simultaneous determination of corticosterone, hydrocortisone, and dexamethasone in plasma, with prednisolone as the internal standard. Samples were extrac...

journal_title：Journal of pharmaceutical sciences

authors： Alvinerie M,Toutain PL

更新日期：1982-07-01 00:00:00

abstract：:Various neutral, cationic, and anionic chemicals contained in hair care products can be absorbed into hair fiber to modulate physicochemical properties such as color, strength, style, and volume. For environmental safety, there is also an interest in understanding hair absorption to wide chemical pollutants. There hav...

journal_title：Journal of pharmaceutical sciences

authors： Li L,Yang S,Chen T,Han L,Lian G

更新日期：2018-04-01 00:00:00

abstract：:Repetitive administration is routinely used to maintain therapeutic drug levels, but previous studies have documented an accelerated blood clearance of some lipid-based delivery systems under these conditions. To assess the effect of repetitive administration, non-PEGylated lipoplexes (+/-0.5) were administered 4 time...

journal_title：Journal of pharmaceutical sciences

authors： Betker JL,Anchordoquy TJ

更新日期：2017-03-01 00:00:00

abstract：:The bioavailability of three different brands and three different dosage forms of doxycycline was studied in normal subjects. Single doses, equivalent to 200 mg of doxycycline, were administered to six subjects in a crossover design as the innovator's intravenous solution given orally (Treatment A), the innovator's ca...

journal_title：Journal of pharmaceutical sciences

authors： Antal EJ,Jaffe JM,Poust RI,Colaizzi JL

更新日期：1975-12-01 00:00:00

abstract：:The objective of this study is to understand the underlying mechanisms responsible for the superior stability of indomethacin (INM)-Eudragit® E PO (E PO) system by exploring the miscibility and intermolecular interactions through the combination of thermal, rheological, and spectroscopic analysis. The zero shear-rate ...

journal_title：Journal of pharmaceutical sciences

authors： Liu H,Zhang X,Suwardie H,Wang P,Gogos CG

更新日期：2012-06-01 00:00:00

abstract：:A theoretical investigation has been conducted to understand the deconvolution method used for evaluating the in vivo release rate of an oral controlled-release product from the plasma drug concentration versus time profile. The theory is based on well-accepted pharmacokinetic compartmental models. The cumulative amou...

journal_title：Journal of pharmaceutical sciences

authors： Hwang SS,Bayne W,Theeuwes F

更新日期：1993-11-01 00:00:00

abstract：:Packing behavior and flowability of particulate material have long been acknowledged as important parameters for the processing of pharmaceutical materials. When properly understood, these properties can provide insight into weight uniformity, tableting performance and process design. The aim of this study was to meas...

journal_title：Journal of pharmaceutical sciences

authors： Sandler N,Wilson D

更新日期：2010-02-01 00:00:00

abstract：:A series of N1-p-chlorophenyl-N5-alkylbiguanides were synthesized as potential inhibitors of dental plaque. Partition coefficients and pKa values were determined by standard methods. Biological activity was evaluated against Streptococcus mutans, a pure strain of plaque-forming bacteria. All compounds were compared to...

journal_title：Journal of pharmaceutical sciences

authors： Warner VD,Lynch DM,Ajemian RS

更新日期：1976-07-01 00:00:00

abstract：:This work reports the measurement of the partition rate of a model drug, ibuprofen (IBU), from aqueous solutions into octanol in the absence and presence of common pharmaceutical excipients including glucose, lactose, maltoheptaose, hydroxypropyl methylcellulose, polyvinylpyrrolidone, polyvinylpyrrolidone-vinyl acetat...

journal_title：Journal of pharmaceutical sciences

authors： Xu H,Wang W,Shi Y,Gao P

更新日期：2019-01-01 00:00:00

abstract：:The major objective of this study was to investigate and characterize the solution properties of cromolyn sodium (in D(2)O or D(2)O/H(2)O phosphate buffer at pH 7.5) using nuclear magnetic resonance (NMR) spectroscopy. The self-association of cromolyn molecules was examined primarily via one-dimensional (1)H and (13)C...

journal_title：Journal of pharmaceutical sciences

authors： Ding X,Stringfellow TC,Robinson JR

更新日期：2004-05-01 00:00:00

abstract：:Nicotine is absorbed from the lungs into the systemic circulation during cigarette smoking. However, there is little information concerning the transport mechanism of nicotine in alveolar epithelial cells. In this study, we characterized the uptake of nicotine in rat primary cultured type II (TII) and transdifferentia...

journal_title：Journal of pharmaceutical sciences

authors： Takano M,Nagahiro M,Yumoto R

更新日期：2016-02-01 00:00:00

abstract：:A α-helical GALA peptide (WEAALAEALAEALAEHLAEALAEALEALAA) has been found to possess dual functions: a pH-dependent inducer of endosomal escape, and a ligand that targets lung endothelium. In the present study, the flexibility of GALA was improved by modifying the edge with polyethylene glycol linker, to increase lung-...

journal_title：Journal of pharmaceutical sciences

authors： Santiwarangkool S,Akita H,Nakatani T,Kusumoto K,Kimura H,Suzuki M,Nishimura M,Sato Y,Harashima H

更新日期：2017-09-01 00:00:00

abstract：:To estimate the feasibility of novel containers for drugs, poly(ethylene oxide)-poly(beta-benzyl L-aspartate) (PEO-PBLA) micelles were prepared by dialysis against water using different solvents. The solvent selected is very important because it drastically affects the stability of polymeric micelles. The critical mic...

journal_title：Journal of pharmaceutical sciences

authors： La SB,Okano T,Kataoka K

更新日期：1996-01-01 00:00:00

abstract：:In an attempt to explain the mechanism of protein stabilization conferred by detergents, we investigated the effect of Tween 80 on aggregation of bovine serum albumin (BSA) using circular dichroism (CD) and native gel electrophoresis. CD thermal scans showed that BSA denatures at about 54 degrees C in 20 mM Tris, pH 7...

journal_title：Journal of pharmaceutical sciences

authors： Arakawa T,Kita Y

更新日期：2000-05-01 00:00:00

abstract：:Progesterone release from monolithic devices prepared from various copolymers of poly(hydroxyethyl methacrylate) and poly(methoxyethoxyethyl methacrylate) or poly(methoxyethyl methacrylate) was examined. In general, plots of the fraction of drug released versus (time)1/2 were linear during the early stages of drug rel...

journal_title：Journal of pharmaceutical sciences

authors： Song SZ,Cardinal JR,Kim SH,Kim SW

更新日期：1981-02-01 00:00:00

abstract：:Phenytoin has been decreasingly used because of the high interindividual variability in drug concentration and the narrow therapeutic window. Despite such drawbacks, phenytoin is still essential as a second-line therapy for status epilepticus when patients are resistant to benzodiazepines. This study aimed to develop ...

journal_title：Journal of pharmaceutical sciences

authors： Guk J,Lee SG,Chae D,Kim JH,Park K

更新日期：2019-08-01 00:00:00

abstract：:Although PEGylation of biologics is currently the gold standard for half-life extension, the technology has a number of limitations, most importantly the non-biodegradability of PEG and the extremely high viscosity at high concentrations. HESylation is a promising alternative based on coupling to the biodegradable pol...

journal_title：Journal of pharmaceutical sciences

authors： Liebner R,Meyer M,Hey T,Winter G,Besheer A

更新日期：2015-02-01 00:00:00

abstract：:Dissolution testing is routinely conducted in the pharmaceutical industry to provide in vitro drug release information for quality control purposes. The most common dissolution testing system for solid dosage forms is the United States Pharmacopeia (USP) Dissolution Testing Apparatus 2. This apparatus is very sensitiv...

journal_title：Journal of pharmaceutical sciences

authors： Wang Y,Armenante PM

更新日期：2012-02-01 00:00:00

abstract：:The synthesis of diazoketone analogs of amino acids and associated problems were investigated with N-phthaloyl-DL-alanine serving as a model. The carboxyl was activated by conversion to the acid chloride or, under mild conditions, to the mixed anhydride obtained with ethyl chloroformate or dicyclohexylcarbodiimide; th...

journal_title：Journal of pharmaceutical sciences

authors： Paul B,Korytnyk W

更新日期：1978-05-01 00:00:00

abstract：:Uptake of the fluorescent probe, 1-anilino-8-naphthalene-sulfonate (I) into isolated rat liver cells was studied using both fluorescence and filtration methods. The time course of the fluorescence enhancement of I after addition to the isolated liver cells was analyzed in terms of rapid, medium, and slow phases. The s...

journal_title：Journal of pharmaceutical sciences

authors： Sugiyama Y,Kimura S,Lin JH,Izukura M,Awazu S,Hanano M

更新日期：1983-08-01 00:00:00