Structural and thermal characterization of zolpidem hemitartrate hemihydrate (Form E) and its decomposition products by laboratory X-ray powder diffraction.

abstract：:A diffusion model for the percutaneous absorption of a solute through the skin is developed for the specific case of a constant donor concentration with a finite removal rate from the receptor due to either perfusion rate or sampling. The model has been developed to include a viable epidermal resistance and a donor-st...

journal_title：Journal of pharmaceutical sciences

authors： Anissimov YG,Roberts MS

更新日期：1999-11-01 00:00:00

abstract：:Variability in the time to crystallization is a major technical and economic hurdle in using amorphous solids in dosage forms. It is hypothesized that amorphous solids "age", and that the older they are, the more relaxed they are and the higher the probability of crystallization. At present, there is no method that al...

journal_title：Journal of pharmaceutical sciences

authors： Hilden LR,Morris KR

更新日期：2003-07-01 00:00:00

abstract：:While the number of clinical trials has continued to grow by about 20% in the past six months, no corresponding growth in product approval by the food and drug administration is seen or anticipated in the near future. Late-stage clinical failures due to lack of efficacy or toxicity continues to be a challenge. The opt...

journal_title：Journal of pharmaceutical sciences

authors： Ho RJ,Chien JY

更新日期：2009-06-01 00:00:00

abstract：:Spray-dried dispersions (SDDs) are an important technology for enhancing the oral bioavailability of poorly water-soluble drugs. To design an effective oral SDD formulation, the key rate-determining step(s) for oral drug absorption must be understood. This work combined in vivo and in vitro tests with in silico modeli...

journal_title：Journal of pharmaceutical sciences

authors： Stewart A,Yates I,Mudie D,Pivette P,Goodwin A,Sarmiento A,Winter M,Morgen M,Vodak D

更新日期：2019-01-01 00:00:00

abstract：:Mechanisms of inhibitory action of sodium salicylate on L-glutamine-D-fructose-6-phosphate aminotransferase, prepared from rat gastric mucosa, were studied. Sodium salicylate at lower concentrations (10-20 mM) inhibited reversibly aminotransferase activity by competing with fructose-6-phosphate. At higher concentratio...

journal_title：Journal of pharmaceutical sciences

authors： Chan J,Lee KH

更新日期：1975-07-01 00:00:00

abstract：:Employing the roots of Iris missouriensis, two known triterpenes, iso-iridogermanal and zeorin, were isolated and identified. As presently reported, they were found to demonstrate cytotoxic activity toward cultured P-388 cells (ED50 = 0.1 and 1.1 microgram/mL, respectively). Additionally, a new triterpene that demonst...

journal_title：Journal of pharmaceutical sciences

authors： Wong SM,Oshima Y,Pezzuto JM,Fong HH,Farnsworth NR

更新日期：1986-03-01 00:00:00

abstract：:The absorption of propicillin from the rat stomach and small intestine in situ was examined as a function of recirculating solution pH. The in vitro interphase transport from an aqueous buffer of various pH values to the octanol phase was also studied for several penicillins by the use of a two-phase rolling cell. The...

journal_title：Journal of pharmaceutical sciences

authors： Tsuji A,Miyamoto E,Hashimoto N,Yamana T

更新日期：1978-12-01 00:00:00

abstract：:Acyclovir is an antiviral drug poorly absorbed in the gastrointestinal tract due to its hydrophilicity, with low oral bioavailability (~20%). Although acyclovir is prescribed in the management of herpes simplex encephalitis (HSE), the disease has a poor prognosis, particularly if the treatment is delayed, reaching mor...

journal_title：Journal of pharmaceutical sciences

authors： Gurgel Assis MS,Fernandes Pedrosa TC,de Moraes FS,Caldeira TG,Pereira GR,de Souza J,Ruela ALM

更新日期：2021-01-13 00:00:00

abstract：:The synthesis, hydrolysis rate, and bioavailability of 1-(p-acetaminophenoxy)-1-ethoxyethane, an acetaminophen prodrug, are described. The prodrug is less soluble than acetaminophen and stable at neutral pH. However, in an acidic environment, the compound cleaves rapidly, generating acetaminophen. When both the prodru...

journal_title：Journal of pharmaceutical sciences

authors： Hussain A,Kulkarni P,Perrier D

更新日期：1978-04-01 00:00:00

abstract：:A pharmacokinetic model that permits prediction of aqueous humor pilocarpine levels following topical application to rabbit eyes was developed. The model is able to account for changes in both instilled solution volume and drug concentration. The model, although simplified, relies mainly on experimentally verifiable a...

journal_title：Journal of pharmaceutical sciences

authors： Himmelstein KJ,Guvenir I,Patton TF

更新日期：1978-05-01 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：: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：:Two natural products isolated from the plant Daphne genkwa have been shown to possess antileukemic activity in mice. Genkwadaphnin and yuanhuacine were observed to inhibit DNA and protein synthesis in P-388 leukemic cells. A detailed study of the effects of these two diterpene esters on protein synthesis of leukemic c...

journal_title：Journal of pharmaceutical sciences

authors： Liou YF,Hall IH,Lee KH

更新日期：1982-12-01 00:00:00

abstract：:A number of isomeric benzoylpyrroleacetic acids (1-6) were prepared and tested in vitro for rat lenses aldose reductase activity. These pyrrole derivatives are structurally related to the acidic nonsteroidal anti-inflammatory drugs. Therefore, their anti-inflammatory properties were also evaluated in the carrageenan-i...

journal_title：Journal of pharmaceutical sciences

authors： Demopoulos VJ,Rekka E

更新日期：1995-01-01 00:00:00

abstract：:Dendrimers have emerged as a promising drug delivery system due to their well defined size, tailorability, and multifunctional nature. However, their application in brain delivery is relatively a new area of research. The present study was aimed at evaluating the uptake and permeation of polyether-copolyester (PEPE) d...

journal_title：Journal of pharmaceutical sciences

authors： Dhanikula RS,Hammady T,Hildgen P

更新日期：2009-10-01 00:00:00

abstract：:A method for the measurement, in human plasma, of all tertiary and secondary tricyclic antidepressants prescribed in the United States is described. The method uses electron beam ionization GLC-mass spectrometry, employing a computer-controlled multiple-ion detector. This method, mass fragmentography, is used with int...

journal_title：Journal of pharmaceutical sciences

authors： Biggs JT,Holland WH,Chang S,Hipps PP,Sherman WR

更新日期：1976-02-01 00:00:00

abstract：:In vivo studies were conducted in rats to determine the role of hyperglycemia and hypoinsulinemia in the previously reported reduction in the hepatic accumulation and increase in the serum concentrations of 70-kDa fluorescein-dextran (FD-70) in diabetic (D) rats. The serum, urine, and hepatic concentrations of FD-70 w...

journal_title：Journal of pharmaceutical sciences

authors： Mehvar R,Reynolds J

更新日期：1994-07-01 00:00:00

abstract：:The transition temperature, T(t), of polymorphs is estimated from both their heats of solution and solubilities (or intrinsic dissolution rates) determined at any one temperature (e.g., ambient). At a given temperature, T, the enthalpy difference, DeltaH, between polymorphs, I and II, is equal to the difference betwee...

journal_title：Journal of pharmaceutical sciences

authors： Gu CH,Grant DJ

更新日期：2001-09-01 00:00:00

abstract：:The expression of carboxylesterase (CES) and the transdermal movement of an ester prodrug were studied in rat skin. Ethyl-fexofenadine (ethyl-FXD) was used as a model lipophilic prodrug that is slowly hydrolyzed to its parent drug, FXD (MW 502). Among the CES1 and CES2 isozymes, Hydrolase A is predominant in rat skin ...

journal_title：Journal of pharmaceutical sciences

authors： Imai T,Ariyoshi S,Ohura K,Sawada T,Nakada Y

更新日期：2016-02-01 00:00:00

abstract：:A stability-indicating assay procedure for the determination of norethindrone on the surface of Red Delicious apple slices was developed. The apple slice is homogenized in pH 10 borate buffer solution and norethindrone is then partitioned into chloroform using a diffusion chamber that has a membrane that is permeable ...

journal_title：Journal of pharmaceutical sciences

authors： Mayberry DO,Kowblansky M,Lane PA,Wray PE

更新日期：1990-08-01 00:00:00

abstract：:Spectrophotometric assay for cycloserine based on the interaction of the drug with 9-methoxyacridine as a chromogenic agent is described. The highly colored substituted acridine product was identified as 9-(d-4-imino-3-isoxazolidinone)acridine. Color development was affected by time and temperature of heating and by t...

journal_title：Journal of pharmaceutical sciences

authors： Stewart JT,Yoo GS

更新日期：1988-05-01 00:00:00

abstract：:beta-Cyclodextrin was ethylated at the 2- and 6-hydroxyl positions. Diethyl sulfate was employed as an alkylating reagent. NMR spectra data indicate that heptakis(2,6-di-O-ethyl)-beta-cyclodextrin (DCD) is the principal component of the product obtained. In addition, the FAB mass spectra obtained in nitrobenzyl alcoho...

journal_title：Journal of pharmaceutical sciences

authors： Vakily M,Pasutto FM,Daneshtalab M,Jamali F

更新日期：1995-08-01 00:00:00

abstract：:Isoperibol calorimetry was used to evaluate protein/carbohydrate interactions after freeze drying. rh-DNase, rh-GH, rh-MetGH, and rh-IGF-I were freeze dried with either mannitol, sucrose, trehalose, or dextran at concentrations ranging from 0% to 100% (w/w). Enthalpies of solution for both freeze-dried and physical mi...

journal_title：Journal of pharmaceutical sciences

authors： Souillac PO,Costantino HR,Middaugh CR,Rytting JH

更新日期：2002-01-01 00:00:00

abstract：:High protein concentration formulations are required for low-volume administration of therapeutic antibodies targeted for subcutaneous, self-administration by patients. Ultra-high concentrations (≥150 mg/mL) can lead to dramatically increased solution viscosities, which in turn can lead to stability, manufacturing, an...

journal_title：Journal of pharmaceutical sciences

authors： Whitaker N,Xiong J,Pace SE,Kumar V,Middaugh CR,Joshi SB,Volkin DB

更新日期：2017-11-01 00:00:00

abstract：:Herein, curcumin amorphous solid dispersions (Cur ASDs) were prepared using binary polymers (Eudragit EPO with polyvinylpyrrolidone K30 [EuD-PVP], Eudragit EPO with hydroxypropyl methylcellulose E50 [EuD-HPMC]) as excipient, and surface tracking of Cur ASDs was mainly addressed. Infrared spectroscopy, in situ Raman im...

journal_title：Journal of pharmaceutical sciences

authors： Fan N,Lu T,Li J

更新日期：2020-02-01 00:00:00

abstract：:Isomazole matrix tablet formulations, with various concentrations of hydroxypropyl methylcellulose (HPMC) hydrogel, were prepared and tested for sustained-release activity. Sustained-release activity was determined by administering isomazole test formulations orally to conscious dogs, instrumented with an indwelling l...

journal_title：Journal of pharmaceutical sciences

authors： Wilson HC,Cuff GW

更新日期：1989-07-01 00:00:00

abstract：:Gepirone hydrochloride, an investigational anxiolytic drug, was found to have at least three polymorphic forms which melted at 180 degrees C (I), 212 degrees C (II), and 200 degrees C (III). Thermal analytical studies showed that forms I and II were an enantiotropic pair, as were forms I and III. Form III was monotrop...

journal_title：Journal of pharmaceutical sciences

authors： Behme RJ,Brooke D,Farney RF,Kensler TT

更新日期：1985-10-01 00:00:00

abstract：:The present work employs recent advances in high-resolution real-time magnetic resonance imaging (MRI) to investigate the disintegration process of tablets containing disintegrants. A temporal resolution of 75 ms and a spatial resolution of 80 × 80 µm with a section thickness of only 600 µm were achieved. The histogra...

journal_title：Journal of pharmaceutical sciences

authors： Quodbach J,Moussavi A,Tammer R,Frahm J,Kleinebudde P

更新日期：2014-01-01 00:00:00

abstract：:The absorption and pharmacokinetics of sulofenur [N-(indan-5-sulfonyl)-N'-(4-chlorophenyl)urea, LY186641] and its major metabolites were examined in mice, rats, monkeys, and dogs. The compound is a diarylsulfonylurea currently being evaluated as an oncolytic agent in phase I and II trials. In all species, sulofenur wa...

journal_title：Journal of pharmaceutical sciences

authors： Ehlhardt WJ,Sullivan HR,Wood PG,Woodland JM,Hamilton M,Hamilton C,Cornpropst D,Grindey GB,Worzalla JF,Bewley JR

更新日期：1993-07-01 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