Solubility advantage of amorphous pharmaceuticals, part 3: Is maximum solubility advantage experimentally attainable and sustainable?

abstract：:The absorption of triazolam from pelleted drug-diet mixtures by mice under steady-state conditions was determined for doses up to 150 mg/kg/day by measuring alpha-hydroxytriazolam, the principal urinary metabolite of triazolam in the mouse, in urine samples collected over a 24-hour period. Following beta-glucuronide g...

journal_title：Journal of pharmaceutical sciences

authors： Adams WJ,Bombardt PA,Code RA

更新日期：1983-10-01 00:00:00

abstract：:Terbinafine is an allylamine antifungal agent that is highly lipophilic and keratophilic. The aim of this study was to investigate terbinafine distribution in peripheral and visceral tissues after intravenous administration to rats. Terbinafine, 6 mg/kg, was administered to 33 male Sprague-Dawley rats via a jugular ve...

journal_title：Journal of pharmaceutical sciences

authors： Hosseini-Yeganeh M,McLachlan AJ

更新日期：2001-11-01 00:00:00

abstract：:A method was developed for the baseline separation of common free bile acids by supercritical fluid chromatography. A phenylbonded silica column, with UV detection at 210 nm, and carbon dioxide modified with methanol as the mobile phase were used. The influence of the stationary phase, modifier concentration, temperat...

journal_title：Journal of pharmaceutical sciences

authors： Scalia S,Games DE

更新日期：1993-01-01 00:00:00

abstract：:(14)N nuclear quadrupole resonance (NQR) in two known polymorphs of famotidine was measured. At room temperature, seven quadrupolar sets of transition frequencies (ν(+), ν(-), and ν(0)) corresponding to seven different nitrogen sites in the crystal structure of each of the two polymorphs were found. This confirms the ...

journal_title：Journal of pharmaceutical sciences

authors： Luźnik J,Pirnat J,Jazbinšek V,Lavrič Z,Žagar V,Srčič S,Seliger J,Trontelj Z

更新日期：2014-09-01 00:00:00

abstract：:The poor membrane permeability and oral bioavailability of the iron chelating agent deferoxamine (DFO) mesylate result from the low octanol/water partition coefficient and high aqueous solubility. With the ultimate aim to improve biomembrane permeability while retaining the iron-binding ability of DFO, a series of mor...

journal_title：Journal of pharmaceutical sciences

authors： Ihnat PM,Vennerstrom JL,Robinson DH

更新日期：2000-12-01 00:00:00

abstract：:The plasma nitroglycerin levels obtained after intracardial (0.7 mg/kg), oral (7 mg/kg), and topical (7--14 mg/kg) doses of nitroglycerin in rats are reported. Nitroglycerin followed essentially one-compartment kinetics after intracardial administration, showing a mean half-life of about 4 min and a mean apparent volu...

journal_title：Journal of pharmaceutical sciences

authors： Yap PS,Fung HL

更新日期：1978-04-01 00:00:00

abstract：:The elementary osmotic pump is a new delivery system for drugs or other active agents; it delivers the agent by an osmotic process at a controlled rate. Control resides in the: (a) water permeation characteristics of a semipermeable membrane surrounding the formulated agent, and (b) osmotic properties of the formulati...

journal_title：Journal of pharmaceutical sciences

authors： Theeuwes F

更新日期：1975-12-01 00:00:00

abstract：:Naltrexone (NTX) is an opioid antagonist used for treatment of narcotic dependence and alcoholism. Transdermal naltrexone delivery is desirable to help improve patient compliance. The purpose of this study was to increase the delivery rate of NTX across human skin by using lipophilic alkyl ester prodrugs. Straight-cha...

journal_title：Journal of pharmaceutical sciences

authors： Stinchcomb AL,Swaan PW,Ekabo O,Harris KK,Browe J,Hammell DC,Cooperman TA,Pearsall M

更新日期：2002-12-01 00:00:00

abstract：:The release through silicone rubber membranes of benzocaine suspended in carbomer hydrogels containing different concentrations of low molecular weight polysols (ethylene glycol, propylene glycol, glycerol, and sorbitol) was studied to establish general principles and procedures for control of the effects on percutane...

journal_title：Journal of pharmaceutical sciences

authors： Di Colo G,Carelli V,Giannaccini B,Serafini MF,Bottari F

更新日期：1980-04-01 00:00:00

abstract：:A Modified Crisp Equation, describing the differential Gibbs free energy of the adsorption process, is being proposed, which considers multiple sites available on the surface for adsorption and their relative fractions. The differential Gibbs free energy can be calculated by the van't Hoff Equation, which depends on t...

journal_title：Journal of pharmaceutical sciences

authors： Yu P,Wurster DE

更新日期：2018-04-01 00:00:00

abstract：:Co-amorphous drug-amino acid systems have gained growing interest as an alternative to common amorphous formulations which contain polymers as stabilizers. Several preparation methods have recently been investigated, including vibrational ball milling on a laboratory scale or spray drying in a larger scale. In this st...

journal_title：Journal of pharmaceutical sciences

authors： Lenz E,Löbmann K,Rades T,Knop K,Kleinebudde P

更新日期：2017-01-01 00:00:00

abstract：:Anthralin and its decomposition products were separated by both column chromatographic and TLC techniques. Two decomposition products were characterized by TLC, melting-point data, and UV and IR spectroscopy. Pure anthralin and its decomposition products also were determined quantitatively. ...

journal_title：Journal of pharmaceutical sciences

authors： Elsabbagh HM,Whitworth CW,Schramm LC

更新日期：1979-03-01 00:00:00

abstract：:The transport rate constant of a drug partitioned in a two-phase system from an aqueous to an organic phase (k1obs) and vice versa (k2obs) is a function of the partition coefficient P and of a solvent system-dependent parameter beta. Drug transport is shown to be independent of molecular structure for a number of arbi...

journal_title：Journal of pharmaceutical sciences

authors： van de Waterbeemd H,van Bakel P,Jansen A

更新日期：1981-09-01 00:00:00

abstract：:Repeated acetaminophen (AP) administration modulates intestinal P-glycoprotein (P-gp) expression. Whether AP can modulate P-gp activity in a short-term fashion is unknown. We investigated the acute effect of AP on rat intestinal P-gp activity in vivo and in vitro. In everted intestinal sacs, AP inhibited serosal-mucos...

journal_title：Journal of pharmaceutical sciences

authors： Novak A,Carpini GD,Ruiz ML,Luquita MG,Rubio MC,Mottino AD,Ghanem CI

更新日期：2013-10-01 00:00:00

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 high-pressure liquid chromatographic procedure for quantitative dexamethasone and dexamethasone sodium phosphate determinations in all types of commercially available pharmaceutical dosage forms was developed. The method also separates dexamethasone from its phosphate salt and separates dexamethasone or its salt fro...

journal_title：Journal of pharmaceutical sciences

authors： Gupta VD

更新日期：1979-07-01 00:00:00

abstract：:Two polymorphs of celastrol were discovered and fully characterized by X-ray powder diffraction, thermogravimetry analysis, and differential scanning calorimetry. The single-crystal structures of form I and the isostructural solvate of form II were disclosed by single-crystal X-ray diffraction. The apparent solubility...

journal_title：Journal of pharmaceutical sciences

authors： Zha J,Zhang Q,Li M,Wang JR,Mei X

更新日期：2018-11-01 00:00:00

abstract：:Microparticles are of considerable interest for drug delivery, vaccination and diagnostic imaging. In order to obtain microparticles with long circulation times, or to provide the prerequisite for tissue specific targeting through decoration with suitable ligands, their surfaces need to be modified such that they beco...

journal_title：Journal of pharmaceutical sciences

authors： Wattendorf U,Merkle HP

更新日期：2008-11-01 00:00:00

abstract：:The thiazide diuretic chlorothiazide is poorly metabolized, and is predominantly excreted via the kidneys. We have previously shown that chlorothiazide is transported by ATP-binding cassette transporter G2, suggesting a potential role for this transporter in apical efflux of chlorothiazide in the kidney. However, beca...

journal_title：Journal of pharmaceutical sciences

authors： Juhász V,Beéry E,Nagy Z,Bui A,Molnár E,Zolnerciks JK,Magnan R,Jani M,Krajcsi P

更新日期：2013-05-01 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：:Aqueous wet massing of stable anhydrous theophylline (A) with polyvinylpyrrolidone (PVP) resulted in its complete transformation to theophylline monohydrate (M). Drying at 45 degrees C, resulted in the formation of metastable anhydrous theophylline (A*) which then transformed to A. PVP, a known crystallization inhibit...

journal_title：Journal of pharmaceutical sciences

authors： Tantry JS,Tank J,Suryanarayanan R

更新日期：2007-05-01 00:00:00

abstract：:This in vitro study evaluated the extent of the absorption and metabolism of propranolol in human skin from four sources. Between 10.4 +/- 3.1 and 36.6 +/- 2.6% of the applied dose was absorbed; however, only a small portion (between 4.1 +/- 0.9 and 16.1 +/- 1.3%) of the dose permeated through the skin. Naphthoxyaceti...

journal_title：Journal of pharmaceutical sciences

authors： Ademola JI,Chow CA,Wester RC,Maibach HI

更新日期：1993-08-01 00:00:00

abstract：:A series of 1-(substituted benzyl)-3,4,5,6-tetrahydro-2(1H)-pyrimidones was synthesized primarily by catalytic hydrogenation of the corresponding 1-(substituted benzyl)-2(1H)-pyrimidone. The pharmacological evaluation of these compounds in mice revealed a unique profile that included evidence of CNS stimulation and de...

journal_title：Journal of pharmaceutical sciences

authors： Ellis KO,Schwan TJ,Wessels FL,Miles NJ

更新日期：1980-10-01 00:00:00

abstract：:Azo compounds are commonly used to study radical-mediated degradation of pharmaceutical compounds. The favorable chemical and physical properties of 2,2'-azobis(2-methylpropanenitrile) (AIBN) have made it one of the most widely used compound for these type of studies. This article describes the characterization of a s...

journal_title：Journal of pharmaceutical sciences

authors： Wells-Knecht KJ,Dunn D

更新日期：2019-09-01 00:00:00

abstract：:We characterized a glucose-sensitive, controlled-release insulin delivery system. Insulin release rates increased when glucose was perfused in the release media surrounding the matrix. The system was composed of solid, particulate insulin, incorporated into an ethylene-vinyl acetate copolymer (EVAc) matrix. Feedback c...

journal_title：Journal of pharmaceutical sciences

authors： Brown LR,Edelman ER,Fischel-Ghodsian F,Langer R

更新日期：1996-12-01 00:00:00

abstract：:In the present work, authors produced tablets of anhydrous sodium naproxen by wet granulation using a high-shear mixer-granulator. Drug hydrated to the tetrahydrated form, as observed by X-ray powder diffractometry. After wet granulation, authors then performed two different drying procedures, obtaining granules of di...

journal_title：Journal of pharmaceutical sciences

authors： Di Martino P,Malaj L,Censi R,Martelli S

更新日期：2008-12-01 00:00:00

abstract：:The aim of this study is to explore hot melt extrusion (HME) as a solvent-free drug loading technique for preparation of stable amorphous solid dispersions using mesoporous silica (PSi). Ibuprofen and carvedilol were used as poorly soluble active pharmaceutical ingredients (APIs). Due to the high friction of an API:PS...

journal_title：Journal of pharmaceutical sciences

authors： Genina N,Hadi B,Löbmann K

更新日期：2018-01-01 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 kinetics of decomposition of the following conformationally restricted N-chloro-alpha-amino acids were studied: 1-amino-1-cyclopentanecarboxylic acid (2), 1-amino-1-cyclohexanecarboxylic acid (4), 2-amino-2-norbornanecarboxylic acid (6), and 2-amino-2-benzonorbornanecarboxylic acid (8). The first-order rate consta...

journal_title：Journal of pharmaceutical sciences

authors： Awad R,Hussain A,Crooks PA

更新日期：1990-12-01 00:00:00

abstract：:The effect of micellar sodium lauryl sulfate on the rate of cupric-ion-promoted hydrolysis of some dicarboxylic acid hemiesters was investigated at pH 5, ionic strength 0.1 M, and 40, 45, and 50 degrees. The rate of cupric-ion-promoted hydrolysis of sodium n-decyloxalate in the micellar phase is about 50 times as fast...

journal_title：Journal of pharmaceutical sciences

authors： Ong JT,Kostenbauder HB

更新日期：1976-12-01 00:00:00