Understanding disintegrant action by visualization.

abstract：:Poly(methyl [1-14C]methacrylate) nanoparticles were injected subcutaneously into rats. Almost all of the radioactivity stayed at the injection site. After an initial urinary and fecal excretion of approximately 1% of the administered dose per day, the rate of elimination dropped to a low level (approximately 0.005%/da...

journal_title：Journal of pharmaceutical sciences

authors： Kreuter J,Nefzger M,Liehl E,Czok R,Voges R

更新日期：1983-10-01 00:00:00

abstract：:This study was designed to assess the effects of cooling rate, storage temperature, and formulation composition on trehalose phase distribution and protein stability in frozen solutions. The data demonstrate that faster cooling rates (>100°C/min) result in trehalose crystallization and protein aggregation as determine...

journal_title：Journal of pharmaceutical sciences

authors： Connolly BD,Le L,Patapoff TW,Cromwell MEM,Moore JMR,Lam P

更新日期：2015-12-01 00:00:00

abstract：:Increasing costs of research and development in the pharmaceutical industry has necessitated a growing interest in the early prediction of human pharmacokinetics of drug candidates. Of growing interest is the need to understand oral absorption, the most common route of small molecule drug administration. The fraction ...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,Liu J,Fan P,Wong H

更新日期：2018-07-01 00:00:00

abstract：:Previously, we reported that repeated oral treatment with etoposide (ETP) increased ileal membrane localization of P-glycoprotein (P-gp) and that this was possibly mediated by increased expression of the ezrin/radixin/moesin (ERM)/phosphorylated ERM (p-ERM) via activation of RhoA/ROCK. These changes caused decreases i...

journal_title：Journal of pharmaceutical sciences

authors： Kobori T,Harada S,Nakamoto K,Tokuyama S

更新日期：2013-05-01 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：:Optical coherence tomography (OCT) is a recently developed optical technique that produces depth profiles of three-dimensional objects. It is a nondestructive interferometric method responding to refractive index variation in the sample under study and can reach a penetration depth of a few millimetres. OCT employs ne...

journal_title：Journal of pharmaceutical sciences

authors： Mauritz JM,Morrisby RS,Hutton RS,Legge CH,Kaminski CF

更新日期：2010-01-01 00:00:00

abstract：:Lipid-based dose forms, which encompass a wide variety of compositional and functional characteristics, can be advantageously utilized for the formulation of lipophilic drugs. There has been a traditional reluctance to develop lipid-based dose forms due to potential problems of chemical and physical instability, and a...

journal_title：Journal of pharmaceutical sciences

authors： Charman WN

更新日期：2000-08-01 00:00:00

abstract：:This study is to enhance the dissolution rate of a poorly water-soluble drug, quercetin, by fabricating nanocrystals using high-pressure homogenization. The particle size, crystallinity, dissolution, and antioxidant effects of fabricated quercetin nanocrystals have been investigated. Characterization of the original q...

journal_title：Journal of pharmaceutical sciences

authors： Sahoo NG,Kakran M,Shaal LA,Li L,Müller RH,Pal M,Tan LP

更新日期：2011-06-01 00:00:00

abstract：:The problem of optimizing ocular bioavailability of topically applied ophthalmic drugs is discussed. A formula for drug concentration in the tear film is derived using well-known pharmacokinetic relationships and a first-order drug decay model for the tear film. The time integral of the tear film concentration is then...

journal_title：Journal of pharmaceutical sciences

authors： Keister JC,Cooper ER,Missel PJ,Lang JC,Hager DF

更新日期：1991-01-01 00:00:00

abstract：:L-3-(3-Hydroxy-4-pivaloyloxyphenyl)alanine (1, NB-355) is a novel L-dopa prodrug. After oral administration with carbidopa in rats, 1 demonstrated 2.3 times longer duration (MRT) and 1.4 times larger bioavailability (AUC) on plasma L-dopa concentrations than those of L-dopa itself. Similar results were obtained in dog...

journal_title：Journal of pharmaceutical sciences

authors： Ihara M,Tsuchiya Y,Sawasaki Y,Hisaka A,Takehana H,Tomimoto K,Yano M

更新日期：1989-07-01 00:00:00

abstract：:Alpha-Hydroxyaryl ketones such as 2-hydroxypropiophenone and 1-(2,4-difluorophenyl)-2-hydroxy-1-propanone, the key intermediates in the preparation of antifungal agents, decompose into oxidized, rearranged, and condensed products. These products were isolated and characterized. The possible mechanisms for the formatio...

journal_title：Journal of pharmaceutical sciences

authors： Gala D,Puar MS,Das PR,Kugelman M,DiBenedetto DJ

更新日期：1992-12-01 00:00:00

abstract：:Chromatographic gel filtration matrixes used in various separation techniques are subject to microbial contamination. The need for a microbe-free column is critical when preparing materials that require a low or zero microbial count. This report proposes two alternative washing systems: 0.02 N HCl containing 0.81% NaC...

journal_title：Journal of pharmaceutical sciences

authors： Wen LF,Bohannon T,Crabb A,Mamaril F

更新日期：1980-02-01 00:00:00

abstract：:Hydrolytic degradation products of cefdinir were studied in acidic (pH 1), neutral (pH 6), and basic (pH 9) solutions. Seven major degradation products were isolated by preparative and/or high-performance liquid chromatography and characterized by UV, IR, 1H-NMR, and mass spectra. To clarify degradation pathways in ea...

journal_title：Journal of pharmaceutical sciences

authors： Okamoto Y,Kiriyama K,Namiki Y,Matsushita J,Fujioka M,Yasuda T

更新日期：1996-09-01 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：:To elucidate drug lipophilicity effects on the bioavailability (BA) of drugs from skin after administration by dissolving microneedles, nine compounds with different lipophilicity indexes (log p value) were formulated into two-layered dissolving microneedles and administered percutaneously to rat skin: desmopressin (D...

journal_title：Journal of pharmaceutical sciences

authors： Ito Y,Yoshimura M,Tanaka T,Takada K

更新日期：2012-03-01 00:00:00

abstract：:The purpose of the present study was to develop guidance toward rational choice of blenders and processing conditions to make robust and high performing adhesive mixtures for dry-powder inhalers and to develop quantitative experimental approaches for optimizing the process. Mixing behavior of carrier (LH100) and Astra...

journal_title：Journal of pharmaceutical sciences

authors： Sarkar S,Minatovicz B,Thalberg K,Chaudhuri B

更新日期：2017-01-01 00:00:00

abstract：:The Setschenow constant, K(salt), of a nonelectrolyte in a NaCl solution is shown to be related to the logarithm of its octanol-water partition coefficient, log K(ow), determined by K(salt) = A log K(ow) + B, where K(ow) is the octanol-water partition coefficient of the solute and the coefficients A and B are constant...

journal_title：Journal of pharmaceutical sciences

authors： Ni N,El-Sayed MM,Sanghvi T,Yalkowsky SH

更新日期：2000-12-01 00:00:00

abstract：:The effect of caffeine on the absorption of ergotamine from the rat small intestine was studied. The results of a series of experiments showed that caffeine significantly enhanced absorption of ergotamine from solutions of pH 5.0 when both substances were in solution and when an intact blood supply was either absent (...

journal_title：Journal of pharmaceutical sciences

authors： Anderson JR,Drehsen G,Pitman IH

更新日期：1981-06-01 00:00:00

abstract：:The advisability of a progressive curtailment of organic solvent film coating offers an incentive to develop latex systems. Here, the use of aqueous colloidal dispersions of cellulose acetate, plasticized with water-soluble additives, is proposed as an alternative way to obtain cellulose acetate membranes either by ca...

journal_title：Journal of pharmaceutical sciences

authors： Bindschaedler C,Gurny R,Doelker E

更新日期：1987-06-01 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 article was to monitor phase transformation in thiamine hydrochloride, from a nonstoichiometric hydrate (NSH) to a hemihydrate (HH), in stored tablets, prepared both by direct compression and wet granulation, and to relate the storage-induced phase transformation with changes in tablet microstruc...

journal_title：Journal of pharmaceutical sciences

authors： Chakravarty P,Suryanarayanan R,Govindarajan R

更新日期：2012-04-01 00:00:00

abstract：:A titration method was developed for the determination of diphenhydramine, quinine, neostigmine, sparteine, strychnine, homatropine, atropine, physostigmine, and procaine in aqueous solution. Tetraphenylborate was used as a titrant with tetrabromophenolphthalein ethyl ester as an indicator in the presence of organic s...

journal_title：Journal of pharmaceutical sciences

authors： Tsubouchi M,Mitsushio H,Yamasaki N,Matsuoka K

更新日期：1981-11-01 00:00:00

abstract：:A crude chloroform-soluble fraction of the ethanol extract of the leaves of Bursera klugii showed activity against two test systems, the P-388 lymphocytic leukemia (3PS) and the human epidermoid carcinoma of the nasopharynx (9KB). The PS activity was due to two constituents, sapelins A and B. ...

journal_title：Journal of pharmaceutical sciences

authors： Jolad SD,Wiedhopf RM,Cole JR

更新日期：1977-06-01 00:00:00

abstract：:The association efficiency of oxytetracycline (OTC) to pharmaceutical available, ionic oil-in-water nanoemulsions is studied. Theoretical mathematical developments allowed us to differentiate by diafiltration (DF) between thermodynamically and kinetically controlled binding of the drug to the nanoemulsions, and relate...

journal_title：Journal of pharmaceutical sciences

authors： Orellana SL,Torres-Gallegos C,Araya-Hermosilla R,Oyarzun-Ampuero F,Moreno-Villoslada I

更新日期：2015-03-01 00:00:00

abstract：:Diazepam (1), a hypnotic and anxiolytic drug in worldwide use, formed an intermediate product in a mixture of ethanol and sodium hydroxide ([NaOH] > or = 1 M). The intermediate product slowly decomposed to form 2-(methylamino)-5-chlorobenzophenone imine (2) and 2-(methylamino)-5-chlorobenzophenone (3). The amount of 2...

journal_title：Journal of pharmaceutical sciences

authors： Yang SK,Tang R,Yang TJ,Pu QL,Bao Z

更新日期：1996-07-01 00:00:00

abstract：:The aminoxyl (nitroxyl) labeled (2-chloroethyl)nitrosocarbamoyl (CNC) derivatives of amino acids, i.e., N-[[N'-(2-chloroethyl)-N'-nitrosoamino]carbonyl]-A-(1-oxy-2,2,6,6- tetramethylpiperidin-4-yl)amides, A = glycyl (10a), A = L-alanyl (10b), A = L-valyl (10c), A = L-phenylalanyl (10d), were synthesized and evaluated ...

journal_title：Journal of pharmaceutical sciences

authors： Sosnovsky G,Baysal M,Erciyas E

更新日期：1994-07-01 00:00:00

abstract：:The pharmacokinetics of tamsulosin (TAM) was investigated using male Sprague-Dawley rats in which plasma alpha(1)-acid glycoprotein (alpha(1)-AGP) levels were elevated by the subcutaneous injection of 0.2 mL/kg of turpentine oil. alpha(1)-AGP levels increased about eight times after turpentine oil treatment, causing a...

journal_title：Journal of pharmaceutical sciences

authors： Matsushima H,Watanabe T,Higuchi S

更新日期：2000-04-01 00:00:00

abstract：:The use of second generation cationic liposomes to deliver cytotoxic drugs to solid tumors is a rational and promising therapeutic approach, given the natural affinity of cationic carrier molecules for the tumor microvasculature. Cationic liposomal therapeutics are effective in the treatment of cancers that are resist...

journal_title：Journal of pharmaceutical sciences

authors： Campbell RB,Ying B,Kuesters GM,Hemphill R

更新日期：2009-02-01 00:00:00

abstract：:Quantification of protein binding of new chemical entities is an important early screening step during drug discovery and is of fundamental interest for the estimation of safety margins during drug development. In this publication, we describe the development of a new high-throughput assay for the determination of the...

journal_title：Journal of pharmaceutical sciences

authors： Schuhmacher J,Kohlsdorfer C,Bühner K,Brandenburger T,Kruk R

更新日期：2004-04-01 00:00:00

abstract：:DNA co-condensates were formed by reacting [125I]DNA with an admixture of a high-mannose glycopeptide (Man9-CWK(18)) and either of two poly(ethylene glycol) peptides (PEG-VS-CWK(18) or PEG-SS-CWK(18)) followed by cross-linking with 6-50 mol equiv of glutaraldehyde. [125I]DNA co-condensates were administered intravenou...

journal_title：Journal of pharmaceutical sciences

authors： Yang Y,Park Y,Man S,Liu Y,Rice KG

更新日期：2001-12-01 00:00:00