Detection of a minor amorphous phase in crystalline etoricoxib by dynamic mechanical analysis: comparison with Raman spectroscopy and modulated differential scanning calorimetry.

abstract：:The total synthesis of d-pilocarpine specifically labeled as N-14CH3 is reported. dl-Homopilopic acid was prepared as a key intermediate and resolved into the d-enantiomer via the alpha-methylbenzylamine salt. The penultimate intermediate, 2-mercaptopilocarpine, was desulfurized by oxidation with dilute hydrogen perox...

journal_title：Journal of pharmaceutical sciences

authors： DeGraw JI,Engstrom JS,Willis E

更新日期：1975-10-01 00:00:00

abstract：:A novel technique is presented to allow measurement of the kinetics of protein inactivation during drying of an acoustically levitated single droplet. Droplets/particles are removed from the acoustic field after various times during drying, and the state of the protein within them is analyzed. The influence of drying ...

journal_title：Journal of pharmaceutical sciences

authors： Lorenzen E,Lee G

更新日期：2012-06-01 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 program is described that permits iterative least-squares nonlinear regression fitting of polyexponential curves using the Hewlett Packard HP 41 CV programmable calculator. The program enables the analysis of pharmacokinetic drug level profiles with a high degree of precision. Up to 15 data pairs can be used, and in...

journal_title：Journal of pharmaceutical sciences

authors： Thornhill DP,Schwerzel E

更新日期：1985-05-01 00:00:00

abstract：:Literature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate-release, solid oral dosage forms containing enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhi...

journal_title：Journal of pharmaceutical sciences

authors： Verbeeck RK,Kanfer I,Löbenberg R,Abrahamsson B,Cristofoletti R,Groot DW,Langguth P,Polli JE,Parr A,Shah VP,Mehta M,Dressman JB

更新日期：2017-08-01 00:00:00

abstract：:A rapid approach for estimating the pK(a) value of small organic molecules was developed using vacuum-assisted multiplexed capillary electrophoresis (VAMCE) with ultraviolet detection. The VAMCE method employed a 96-capillary array, arranged in a standard 8 x 12 microtiter plate configuration, with each row of capilla...

journal_title：Journal of pharmaceutical sciences

authors： Zhou C,Jin Y,Kenseth JR,Stella M,Wehmeyer KR,Heineman WR

更新日期：2005-03-01 00:00:00

abstract：:Many pharmaceuticals are formulated as powders to aid drug delivery. A major problem is how to produce powders having high purity, controlled morphology, and retained bioactivity. We demonstrate the use of supercritical carbon dioxide as an antisolvent for meeting this need for two model drug systems, quercetin, a spa...

journal_title：Journal of pharmaceutical sciences

authors： Jacobson GB,Shinde R,McCullough RL,Cheng NJ,Creasman A,Beyene A,Hickerson RP,Quan C,Turner C,Kaspar RL,Contag CH,Zare RN

更新日期：2010-06-01 00:00:00

abstract：:In phenobarbital measurement by GLC with the flash-methylation technique, using trimethylanilinium hydroxide as a methylating reagent, a small amount of water decomposed phenobarbital and interfered with the quantitative analysis. Thus, both the sample and the methylating reagent must be sufficiently dehydrated to att...

journal_title：Journal of pharmaceutical sciences

authors： Kurata K,Takeuchi M,Yoshida K

更新日期：1979-09-01 00:00:00

abstract：:Quercetin is a bioactive flavonoid widely used as a health supplement. Being sparingly soluble and chemically unstable in aqueous intestinal fluids, quercetin is poorly absorbed orally. This study aimed to investigate the effects of three beta-cyclodextrins, namely, unsubstituted beta-cyclodextrin (beta-CD), hydroxypr...

journal_title：Journal of pharmaceutical sciences

authors： Zheng Y,Haworth IS,Zuo Z,Chow MS,Chow AH

更新日期：2005-05-01 00:00:00

abstract：:Econazole is a feasible alternative treatment in the management of fungal keratitis. Nevertheless, its low water solubility is considered the main limitation to the incorporation into ophthalmic formulations. In this work, econazole nitrate is solubilized by using cyclodextrins to achieve an optimum therapeutic concen...

journal_title：Journal of pharmaceutical sciences

authors： Díaz-Tomé V,Luaces-Rodríguez A,Silva-Rodríguez J,Blanco-Dorado S,García-Quintanilla L,Llovo-Taboada J,Blanco-Méndez J,García-Otero X,Varela-Fernández R,Herranz M,Gil-Martínez M,Lamas MJ,González-Barcia M,Otero-Espinar FJ,Fern

更新日期：2018-05-01 00:00:00

abstract：:A sensitive, specific, high-performance liquid chromatographic procedure was developed for the measurement of plasma tiflamizole levels. Acidic plasma samples were extracted with three volumes of ether. The ether extracts were combined and evaporated to dryness. The residue was dissolved in acetonitrile, washed with h...

journal_title：Journal of pharmaceutical sciences

authors： Rakestraw DC,Whitney CC Jr

更新日期：1984-12-01 00:00:00

abstract：:The isomerization reactions of ceftibuten and ceftibuten-related compounds in aqueous solution were investigated to estimate the substitution effect on the isomerization reaction and identify the three proximal dissociation constants of ceftibuten kinetically from the pH-rate profiles. The isomerization reaction of ce...

journal_title：Journal of pharmaceutical sciences

authors： Hashimoto N,Hirano K

更新日期：1998-09-01 00:00:00

abstract：:Spray freeze-drying is an evolving technology that combines the benefits of spray-drying and conventional lyophilization techniques to produce drug substance and drug product as free-flowing powders. The high surface-to-volume ratio associated to the submillimeter spray-frozen particles contributes to shorter drying a...

journal_title：Journal of pharmaceutical sciences

authors： Sebastião IB,Bhatnagar B,Tchessalov S,Ohtake S,Plitzko M,Luy B,Alexeenko A

更新日期：2019-06-01 00:00:00

abstract：:A series of even numbered fatty acid esters (C2-C18) of p-[N,N-bis(2-chloroethyl)amino]phenol were synthesized and evaluated as to acute toxicity as well as effectiveness against L-1210 mouse leukemia. The acetate through the decanoate derivatives demonstrated toxicity between 2 and 3 times that of phenol mustard in H...

journal_title：Journal of pharmaceutical sciences

authors： Wynn JE,Caldwell ML,Robinson JR,Beamer RL,Bauguess CT

更新日期：1982-07-01 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：:Despite being a major breakthrough in multiple myeloma therapy, carfilzomib (CFZ, a second-generation proteasome inhibitor drug) has been largely ineffective against solid cancer, possibly due to its pharmacokinetic drawbacks including metabolic instability. Recently, quinic acid (QA, a low-affinity ligand of selectin...

journal_title：Journal of pharmaceutical sciences

authors： Jun Y,Xu J,Kim H,Park JE,Jeong YS,Min JS,Yoon N,Choi JY,Yoo J,Bae SK,Chung SJ,Yeo Y,Lee W

更新日期：2020-04-01 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 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

authors： Perumalla SR,Sun CC

更新日期：2014-04-01 00:00:00

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 ...

journal_title：Journal of pharmaceutical sciences

authors： Petroski RJ,Bates RB,Linz GS,Rosazza JP

更新日期：1983-11-01 00:00:00

abstract：:Previous studies from this laboratory suggested that a solution model (Flory-Huggins equation) modified by a free volume model (Vrentas equation) could satisfactorily describe water absorption into an amorphous solid composed of a sugar or a polymer. This paper has extended the studies of single solutes to binary mixt...

journal_title：Journal of pharmaceutical sciences

authors： Zhang J,Zografi G

更新日期：2001-09-01 00:00:00

abstract：:Nonionic surfactants (caprylocaproyl macrogol-8 glycerides, octoxynol-12, polysorbate-20, and polyethylene glycol-40 hydrogenated castor oil) (47.03%, w/w), costabilizer (poloxamer 407) (12%-20%, w/w), oil (isopropyl myristate) (5.22%, w/w), water (q.s. ad 100%, w/w), and ibuprofen (5%, w/w) were used to develop oil-i...

journal_title：Journal of pharmaceutical sciences

authors： Djekic L,Martinovic M,Stepanović-Petrović R,Tomić M,Micov A,Primorac M

更新日期：2015-08-01 00:00:00

abstract：:(+-)-Carbovir [(+-)-9-[4 alpha-(hydroxymethyl)-cyclopent-2-ene-1 alpha-yl]guanine; NSC 614846] is a novel carbocyclic nucleoside analogue which has been shown to be a potent and selective inhibitor of HIV in vitro. As part of an effort to develop a parenteral formulation for subsequent clinical and toxicological evalu...

journal_title：Journal of pharmaceutical sciences

authors： Anderson BD,Chiang CY

更新日期：1990-09-01 00:00:00

abstract：:Optical crystallographic data were determined on a variety of newer USP drugs for which data had not been previously obtained. The ingredients in an unknown sample can be identified by polarized light microscopy by mounting small amounts of the material in successive specific refractive index liquids and determining r...

journal_title：Journal of pharmaceutical sciences

authors： Jordan DD

更新日期：1993-12-01 00:00:00

abstract：:Solubilities in isoctane and water were determined for several C1-phenolic esters of prostaglandin F2 alpha and prostaglandin E2 and acetates having the same phenol moiety. Linear free energy relationships for solubility among the series were observed with slopes of approximately 1. These results suggest that the cont...

journal_title：Journal of pharmaceutical sciences

authors： Anderson BD,Conradi RA

更新日期：1980-04-01 00:00:00

abstract：:The objective of this study was to investigate the permeation-enhancing effect of thiolated polycarbophil (PCP) on peptide drugs. Mediated by a carbodiimide, increasing amounts of cysteine (Cys) were covalently bound to sodium neutralized PCP (NaPCP). The extent of covalently attached Cys was determined by quantifying...

journal_title：Journal of pharmaceutical sciences

authors： Clausen AE,Bernkop-Schnürch A

更新日期：2000-10-01 00:00:00

abstract：:Inducing immune responses protecting from HIV infection or at least controlling replication poses a huge challenge to modern vaccinology. An increasingly discussed strategy to elicit a potent and broad neutralizing antibody response is the immobilization of HIV's trimeric envelope (Env) surface receptor on a nanoparti...

journal_title：Journal of pharmaceutical sciences

authors： Thalhauser S,Peterhoff D,Wagner R,Breunig M

更新日期：2020-01-01 00:00:00

abstract：:Thymoquinone (TQ) is the main bioactive component isolated from Nigella sativa essential oil and seeds and has been used for the treatment of inflammations, liver disorders, arthritis, and is of great importance as a promising therapeutic drug for different diseases including cancer. This paper reports the first exper...

journal_title：Journal of pharmaceutical sciences

authors： Lupidi G,Camaioni E,Khalifé H,Avenali L,Damiani E,Tanfani F,Scirè A

更新日期：2012-07-01 00:00:00

abstract：:Systematic structural modifications were performed on the natural sesquiterpene lactone tenulin to define those groupings essential to, or significant in, its in vivo antitumor activity. Accordingly, the following tenulin analogs were prepared: dihydrotenulin, 2,3-epoxytenulin, isotenulin, dihydroisotenulin, 2,3-epoxy...

journal_title：Journal of pharmaceutical sciences

authors： Waddell TG,Austin AM,Cochran JW,Gerhart KG,Hall IH,Lee KH

更新日期：1979-06-01 00:00:00

abstract：:We have developed a hydrogel patch, which could promote antigen penetration through stratum corneum (SC), and have demonstrated its safety and efficacy in animals and humans. For the availability improvement of our system, it is important to develop a device, which enhances antigen penetration through SC more efficien...

journal_title：Journal of pharmaceutical sciences

authors： Matsuo K,Ishii Y,Kawai Y,Saiba Y,Quan YS,Kamiyama F,Hirobe S,Okada N,Nakagawa S

更新日期：2013-06-01 00:00:00

abstract：:Methods were developed for the determination of octanoic acid and N-acetyl-DL-tryptophan, which are used as stabilizers in the human blood-derived therapeutic products normal serum albumin and plasma protein fraction. The method for octanoic acid uses GC; quantitation is achieved using heptanoic acid as the internal s...

journal_title：Journal of pharmaceutical sciences

authors： Yu MW,Finlayson JS

更新日期：1984-01-01 00:00:00