Synthesis and characterization of surface-hydrophobic ion-exchange microspheres and the effect of coating on drug release rate.

abstract：:Literature data pertaining to the decision to allow a waiver of in vivo bioequivalence testing for the approval of immediate-release (IR) solid oral dosage forms containing efavirenz as the only active pharmaceutical ingredient (API) are reviewed. Because of lack of conclusive data about efavirenz's permeability and i...

journal_title：Journal of pharmaceutical sciences

authors： Cristofoletti R,Nair A,Abrahamsson B,Groot DW,Kopp S,Langguth P,Polli JE,Shah VP,Dressman JB

更新日期：2013-02-01 00:00:00

abstract：:A simple, reliable, and user friendly system was established to cultivate Caco-2 cell monolayer for epithelial transport studies. After an initial growth period of 1 week in a CO(2) incubator, Caco-2 cells were cultivated in an automated continuous perfusion system (Minucells and Minutissue, Germany). Medium was const...

journal_title：Journal of pharmaceutical sciences

authors： Masungi C,Borremans C,Willems B,Mensch J,Van Dijck A,Augustijns P,Brewster ME,Noppe M

更新日期：2004-10-01 00:00:00

abstract：:A high-performance liquid chromatographic (HPLC) method for the simultaneous determination of pralidoxime chloride (I) and its major decomposition products in an injectable formulation is described. I and its decomposition products were detected and quantitated by their UV absorbances at 270 nm, after being separated ...

journal_title：Journal of pharmaceutical sciences

authors： Prue DG,Johnson RN,Kho BT

更新日期：1983-07-01 00:00:00

abstract：:Resveratrol trimethyl ether (trans-3,5,4'-trimethoxystilbene, RTE) is a naturally occurring and pharmacologically active resveratrol derivative. To evaluate its suitability as a drug candidate, a pharmacokinetic study was carried out in Sprague-Dawley rats with the emphasis to identify the impact of aqueous solubility...

journal_title：Journal of pharmaceutical sciences

authors： Lin HS,Ho PC

更新日期：2011-10-01 00:00:00

abstract：:In the present study, a previously described sulfenamide prodrug of a basic antidiabetic drug, metformin, was evaluated further. This sulfenamide prodrug was designed to improve the permeability and consequently the oral absorption and bioavailability (F) of the highly water-soluble metformin. Bioactivation of the pro...

journal_title：Journal of pharmaceutical sciences

authors： Huttunen KM,Leppänen J,Vepsäläinen J,Sirviö J,Laine K,Rautio J

更新日期：2012-08-01 00:00:00

abstract：:The axial and radial tensile strengths were compared to the hardness of compressed tablets containing various concentrations of lubricants. Since radial tensile strength measurement considers the thickness of a tablet, and only tensile stress and axial tensile strength express the strength in the direction in which ca...

journal_title：Journal of pharmaceutical sciences

authors： Jarosz PJ,Parrott EL

更新日期：1982-06-01 00:00:00

abstract：:To design safe, efficient synthetic gene therapy vectors, it is desirable to understand the intracellular mechanisms that facilitate their delivery from the cell surface to the nucleus. Elements of the cytoskeleton and molecular motor proteins are known to play a pivotal role in most intracellular active transport pro...

journal_title：Journal of pharmaceutical sciences

authors： Drake DM,Pack DW

更新日期：2008-04-01 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

authors： Risaliti L,Ambrosi M,Calamante M,Bergonzi MC,Lo Nostro P,Bilia AR

更新日期：2020-10-01 00:00:00

abstract：:Both developing (Days --1-+12 relative to inoculation) and established (Days +18-+29) stages of Mycobacterium butyricum adjuvant-induced polyarthritis in rats were treated orally with cryogenine (100 mg/kg/day), a prototype anti-inflammatory (phenylbutazone, 100 mg/kg/day), or a prototype immunosuppressive (cyclophosp...

journal_title：Journal of pharmaceutical sciences

authors： Watson WC,Malone MH

更新日期：1977-09-01 00:00:00

abstract：:The metabolism of tocainide, an experimental antiarrhythmic drug, was studied in humans. Urinary excretion of unchanged drug was 28-55% in 24 hr after oral dosing. Urine hydrolysis with hydrochloric acid or beta-glucuronidase increased tocainide recovery to 55-79%. Saccharo-1,4-lactone inhibited the beta-glucuronidase...

journal_title：Journal of pharmaceutical sciences

authors： Elvin AT,Keenaghan JB,Byrnes EW,Tenthorey PA,McMaster PD,Takman BH,Lalka D,Manion CV,Baer DT,Wolshin EM,Meyer MB,Ronfeld RA

更新日期：1980-01-01 00:00:00

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

authors： Hoffman DJ,Leveque MJ,Thomson T

更新日期：1983-11-01 00:00:00

abstract：:Nitroglycerin is rapidly lost from solution when incubated with red blood cells or whole blood. The assumption that the loss is enzymatic in nature may not be true, since no major metabolite is detected during this incubation. Explanation on the basis of a chemical reaction is also difficult, since the products of the...

journal_title：Journal of pharmaceutical sciences

authors： Sokoloski TD,Wu CC,Wu LS,Burkman AM

更新日期：1983-04-01 00:00:00

abstract：:The objective of this study was to generate a water-soluble thiolated chitosan to enable the permeation-enhancing effect of chitosan at pH of at least 5.5 without losing the advantages of improved mucoadhesive properties. Therefore, the thiol-bearing polyoxyethylene ligand {O-(3-carboxylpropyl)-O'-[2-[3-mercaptopropio...

journal_title：Journal of pharmaceutical sciences

authors： Hauptstein S,Bonengel S,Griessinger J,Bernkop-Schnürch A

更新日期：2014-02-01 00:00:00

abstract：:The correlation between dynamic surface properties of drug molecules and drug absorption in two common in vitro models of the intestinal wall (Caco-2 monolayers and rat intestinal segments) has been investigated. A homologous series of beta-adrenoreceptor antagonists were used as model compounds. Dynamic molecular sur...

journal_title：Journal of pharmaceutical sciences

authors： Palm K,Luthman K,Ungell AL,Strandlund G,Artursson P

更新日期：1996-01-01 00:00:00

abstract：:Paclitaxel and other taxanes have complex structures including the presence of numerous hydrolytically sensitive ester groups and a chiral center that readily undergoes epimerization thus making their kinetics complex. The present study attempts to understand the mechanism of epimerization at the 7-position of paclita...

journal_title：Journal of pharmaceutical sciences

authors： Tian J,Stella VJ

更新日期：2008-03-01 00:00:00

abstract：:We have shown that adsorbability of local anesthetics onto activated carbon, expressed by the partition coefficients at infinite dilution, correlated well with the pharmacological activity. However, there is no parameter that can singly express the tendency to be adsorbed. Adsorbability is a loosely defined term and i...

journal_title：Journal of pharmaceutical sciences

authors： Abe I,Kamaya H,Ueda I

更新日期：1990-04-01 00:00:00

abstract：:The aim was to study a new method of dissolution in vitro, the "Bio-Dis" apparatus, and to compare it with the classical rotating bottle method. Several theophylline controlled-release drug dosage forms were studied. Dissolution testing was performed in increasing pH in standard conditions and after treatment with pea...

journal_title：Journal of pharmaceutical sciences

authors： Esbelin B,Beyssac E,Aiache JM,Shiu GK,Skelly JP

更新日期：1991-10-01 00:00:00

abstract：:A procedure for the quantitative determination of adinazolam in plasma was developed. The drug, an N-demethylated metabolite, and an internal standard were extracted from basified plasma into ethyl acetate. After evaporation, the residue was dissolved in toluene which was washed with sodium hydroxide. The toluene was ...

journal_title：Journal of pharmaceutical sciences

authors： Peng GW

更新日期：1984-08-01 00:00:00

abstract：:Mycophenolate mofetil (MPM), a new immunosuppressant, is the morpholinoethyl ester of mycophenolic acid (MPA). The distribution in blood and pharmacokinetics of MPA after administration of MPM were examined. The plasma to erythrocyte concentration ratio was low (0.10-0.15). MPA existed in rat plasma as the highly boun...

journal_title：Journal of pharmaceutical sciences

authors： Sugioka N,Koyama H,Ohta T,Kishimoto H,Yasumura T,Takada K

更新日期：1996-03-01 00:00:00

abstract：:Accurate prediction of target occupancy facilitates central nervous system drug development. In this review, we discuss the predictability of serotonin transporter (SERT) occupancy in human brain estimated from in vitro Ki values for human SERT and plasma concentrations of unbound drug (Cu,plasma), as well as the impa...

journal_title：Journal of pharmaceutical sciences

authors： Yahata M,Chiba K,Watanabe T,Sugiyama Y

更新日期：2017-09-01 00:00:00

abstract：:This study compares one of the previously studied formulations with commercial amoxicillin capsules. The results indicate that the percentage of the dose absorbed is similar in both formulations; nevertheless, the amoxicillin capsules present a higher absorption rate. The in vivo--in vitro correlations in terms of res...

journal_title：Journal of pharmaceutical sciences

authors： Llabrés M,Vila JL,Martínez-Pacheco R

更新日期：1982-08-01 00:00:00

abstract：:A modified electron-impact GLC-selected ion monitoring mass spectrometric method for captopril is described. Positive chemical ionization GLC-selected ion monitoring and direct chemical ionization confirms the specificity of this procedure for captopril and establishes the chemical ionization techniques as potential a...

journal_title：Journal of pharmaceutical sciences

authors： Cohen AI,Devlin RG,Ivashkiv E,Funke PT,McCormick T

更新日期：1982-11-01 00:00:00

abstract：:Complexation of ferrous cytochrome P450 by metabolic intermediates formed during NADPH-catalyzed metabolism of compounds structurally related to orphenadrine was studied. This so-called metabolic intermediate complexation was determined in rat liver microsomes, obtained from phenobarbital-pretreated rats, at 455 nm us...

journal_title：Journal of pharmaceutical sciences

authors： Bast A,Savenije-Chapel EM,Noordhoek J

更新日期：1984-07-01 00:00:00

abstract：:This paper describes the synthesis and characterization of cationic copolymers with different macromolecular architecture and drug delivery properties of the corresponding dexamethasone sodium phosphate (DSP)-loaded systems. Copolyelectrolytes comprising poly[2-(acryloyloxy)ethyl] trimethylammonium chloride (PAETMAC) ...

journal_title：Journal of pharmaceutical sciences

authors： Georgieva D,Kostova B,Ivanova S,Rachev D,Tzankova V,Kondeva-Burdina M,Christova D

更新日期：2014-08-01 00:00:00

abstract：:Though there is an advantage in using the higher solubility amorphous state in cases where low solubility limits absorption, physical instability poses a significant barrier limiting its use in solid oral dosage forms. Unlike chemical instability, where useful accelerated stability testing protocols are common, no met...

journal_title：Journal of pharmaceutical sciences

authors： Bhugra C,Pikal MJ

更新日期：2008-04-01 00:00:00

abstract：:Vaults, at 13 MDa, are the largest ribonucleoprotein particles known. In vitro, expression of the major vault protein (MVP) alone in Sf9 insect cells results in the production of recombinant particles with characteristic vault structure. With the ultimate goal of using recombinant vaults as nanocapsules for the delive...

journal_title：Journal of pharmaceutical sciences

authors： Esfandiary R,Kickhoefer VA,Rome LH,Joshi SB,Middaugh CR

更新日期：2009-04-01 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

authors： Luo X,Zheng L,Cai N,Liu Q,Yang S,He X,Cheng Z

更新日期：2015-10-01 00:00:00

abstract：:The use of intravascular tyrosine (TYR) to enhance catecholamine release in hemorrhagic shock and other cardiovascular diseases, or as a constituent of nutrient mixtures used for total parenteral nutrition, is limited by the unusually poor solubility of the amino acid in water. We have thus examined the ability of var...

journal_title：Journal of pharmaceutical sciences

authors： Maher TJ,Kiritsy PJ,Moya-Huff FA,Casacci F,De Marchi F,Wurtman RJ

更新日期：1990-08-01 00:00:00

abstract：:At low protein concentrations (c2), non-native protein aggregation rates are known to be sensitive to changes in conformational stability and "weak" or "colloidal" protein-protein interactions. Protein-protein interactions are also known to be strong functions of c2. In the present work, protein-protein interactions a...

journal_title：Journal of pharmaceutical sciences

authors： Ghosh R,Calero-Rubio C,Saluja A,Roberts CJ

更新日期：2016-03-01 00:00:00

abstract：:The solubility of ergotamine tartrate in aqueous solutions of tartaric acid, citric acid, hydrochloric acid, and caffeine and the dissolution rate of ergotamine tartrate in aqueous mixtures containing hydrochloric acid, caffeine, citric acid, or sodium acetate were studied. The Noyes-Whitney model of dissolution is us...

journal_title：Journal of pharmaceutical sciences

authors： Anderson JR,Pitman IH

更新日期：1980-07-01 00:00:00