CYP1A1 and CYP1B1-mediated biotransformation of the antitrypanosomal methamidoxime prodrug DB844 forms novel metabolites through intramolecular rearrangement.

abstract：:Cyclosporin A (CyA) interacts with lipid membranes. Binding reaction and membrane location of CyA and analogs were examined with 2H-NMR, high-sensitivity isothermal titration calorimetry (ITC), and CD spectroscopy. Effects of CyA and charged analogs on the phosphocholine head group and on the membrane interior were in...

journal_title：Journal of pharmaceutical sciences

authors： Schote U,Ganz P,Fahr A,Seelig J

更新日期：2002-03-01 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：:Thymopentin (Tp5) was loaded in poly-butylcyanoacrylate (PBCA) nanoparticles (NP) in order to enhance the oral bioavailability of Tp5. PBCA-Tp5-NP was prepared by nanoprecipitation methods. Dialyzing membrane method was employed to examine the in vitro release of PBCA-Tp5-NP in PBS, and Tp5 samples in the release medi...

journal_title：Journal of pharmaceutical sciences

authors： He W,Jiang X,Zhang ZR

更新日期：2008-06-01 00:00:00

abstract：:Disintegration performance was measured by analysing both water ingress and tablet swelling of pure microcrystalline cellulose (MCC) and in mixture with croscarmellose sodium using terahertz pulsed imaging (TPI). Tablets made from pure MCC with porosities of 10% and 15% showed similar swelling and transport kinetics: ...

journal_title：Journal of pharmaceutical sciences

authors： Yassin S,Goodwin DJ,Anderson A,Sibik J,Ian Wilson D,Gladden LF,Axel Zeitler J

更新日期：2015-10-01 00:00:00

abstract：:The development of multiple drug modalities over the past 20 years has dramatically expanded the therapeutic space for intervention in disease processes. Rather than being alternative therapeutic approaches, these modalities tend to be complimentary both in the scope of target space and the biological mechanisms harne...

journal_title：Journal of pharmaceutical sciences

authors： Hochman JH

更新日期：2021-01-01 00:00:00

abstract：:Thiamine hydrochloride (Vitamin B(1), THCl) can exist as a nonstoichiometric hydrate (NSH) and as a hemihydrate (HH). NSH can contain up to approximately 1 molar equivalent of water and be dehydrated to an isomorphic desolvate (ID) with minimal change in lattice structure. Crystallographic and spectroscopic techniques...

journal_title：Journal of pharmaceutical sciences

authors： Chakravarty P,Berendt RT,Munson EJ,Young VG Jr,Govindarajan R,Suryanarayanan R

更新日期：2010-02-01 00:00:00

abstract：:The release characteristics of potassium chloride was studied when it was coated with a selection of polymers; from the results obtained, a suitable batch was microencapsulated using a gelatin-gum arabic coacervate system. The microencapsulated product offers better controlled release for this drug when compared to st...

journal_title：Journal of pharmaceutical sciences

authors： Harris MS

更新日期：1981-04-01 00:00:00

abstract：:Flumizole is a potent anti-inflammatory agent in animal models with an inhibitory activity severalfold that of indomethacin in rat foot edema and prostaglandin synthetase tests. The drug was well absorbed from the GI tract when administered in the solution used in pharmacological assays. However, markedly poorer absor...

journal_title：Journal of pharmaceutical sciences

authors： Wiseman EH,McIlhenny HM,Bettis JW

更新日期：1975-09-01 00:00:00

abstract：:The stereoselective pharmacokinetics of suprofen enantiomers has been studied in humans by means of stable isotope-labeled pseudoracemate-diastereomer methodology. After a single oral dose of a near equimolar mixture of unlabeled-(R)-(-)- and [2H3]-(S)-(+)-suprofen [or unlabeled-(S)- and [2H3]-(R)-suprofen] to three h...

journal_title：Journal of pharmaceutical sciences

authors： Shinohara Y,Magara H,Baba S

更新日期：1991-11-01 00:00:00

abstract：:Synthetic peptides corresponding to the variable tandem repeat domain of the cancer-associated antigen MUC1 mucin are candidates for cancer vaccines. In our investigation mice were immunized via subcutaneous injection with poly(d,l-lactic-co-glycolic acid) (PLGA) microspheres containing a MUC1 mucin peptide. It was hy...

journal_title：Journal of pharmaceutical sciences

authors： Newman KD,Sosnowski DL,Kwon GS,Samuel J

更新日期：1998-11-01 00:00:00

abstract：:In this study, injectable microspheres were developed for the local treatment of joint degeneration in rheumatoid arthritis (RA). Microspheres loaded with triamcinolone (TA), a corticosteroid drug, and/or raloxifene (Ral), a cartilage regenerative drug, were prepared with a biodegradable and biocompatible polymer, pol...

journal_title：Journal of pharmaceutical sciences

authors： Ocal Y,Kurum B,Karahan S,Tezcaner A,Ozen S,Keskin D

更新日期：2014-08-01 00:00:00

abstract：:The aim of the present work was to prepare and characterize chitosan-stearic acid conjugate nanomicelles for encapsulation of amphotericin B (AmB) and to evaluate the in vitro nebulization of the formulations. Water soluble chitosan was grafted to stearic acid (SA) chains via 1-ethyl-3-(3-dimethylaminopropyl)carbodiim...

journal_title：Journal of pharmaceutical sciences

authors： Gilani K,Moazeni E,Ramezanli T,Amini M,Fazeli MR,Jamalifar H

更新日期：2011-01-01 00:00:00

abstract：:A sensitive, specific and reproducible high-performance liquid chromatographic procedure, using the normal phase and radial compression system, is described for the simultaneous determination of corticosterone, hydrocortisone, and dexamethasone in plasma, with prednisolone as the internal standard. Samples were extrac...

journal_title：Journal of pharmaceutical sciences

authors： Alvinerie M,Toutain PL

更新日期：1982-07-01 00:00:00

abstract：:The crystallization tendency of 2 crystalline polymorphs of indomethacin (Iα, Iγ) in the undercooled melt has been investigated using molecular dynamics simulations. The main thermodynamical and dynamical physical parameters involved in the nucleation and growth processes have been determined. A careful attention has ...

journal_title：Journal of pharmaceutical sciences

authors： Gerges J,Affouard F

更新日期：2020-02-01 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：:Simple assays for extraction and determination of the concentrations of the antibiotics oxytetracycline, oxolinic acid, and flumequine in a drug dosage form for farmed fish are described. HPLC with UV detection was used in the analyses. The recovery of all three drugs was approximately 100%, and the precision varied f...

journal_title：Journal of pharmaceutical sciences

authors： Rogstad A,Weng B

更新日期：1993-05-01 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：:Tissue-specific ultrasonic enhancement can be used for the detection and characterization of atherosclerosis. We have previously demonstrated the generation of inherently echogenic (acoustically reflective) liposomes solely by varying lipid composition and controlling the method of production. In this study, echogenic...

journal_title：Journal of pharmaceutical sciences

authors： Demos SM,Onyüksel H,Gilbert J,Roth SI,Kane B,Jungblut P,Pinto JV,McPherson DD,Klegerman ME

更新日期：1997-02-01 00:00:00

abstract：:A model for estimating in vivo skin permeability coefficients for finite doses is presented. The ratio of the maximum value of the excretion rate to the steady-state flux is a function of the thickness of the applied vehicle and the vehicle-skin partition coefficient. The decay rate of the excretion is a function of s...

journal_title：Journal of pharmaceutical sciences

authors： Cooper ER,Berner B

更新日期：1985-10-01 00:00:00

abstract：:Deiodination of diatrizoic acid, an anionic radiopaque, was found to be catalyzed by Cu(II). Through a detailed study of o-iodobenzoic acid, a model compound, the copper-catalyzed SN1 mechanism was established based on observations of common ion, salt, and pH effects. Meta- and para-iodobenzoic acids were unreactive. ...

journal_title：Journal of pharmaceutical sciences

authors： Wang YC

更新日期：1980-06-01 00:00:00

abstract：:A novel, general, theoretical equation that describes the release of polyionizable compounds from submicrometer emulsions was derived and evaluated. The model accounts for simultaneous partitioning, interfacial activity, and adsorption to surfactant for n independent drug species and j surfactant species in a single e...

journal_title：Journal of pharmaceutical sciences

authors： Silvestri S,Wu LL,Bowser B

更新日期：1992-05-01 00:00:00

abstract：:In vitro iontophoretic administration of drugs through a microporous polyolefin membrane with hydrophilic urethane polymerfilled pores was done for the ionized drugs dexamethasone sodium phosphate, hydrocortisone sodium phosphate, and prednisolone sodium succinate, and for a nonionizable drug cortisone acetate. Curren...

journal_title：Journal of pharmaceutical sciences

authors： Tu YH,Allen LV Jr

更新日期：1989-03-01 00:00:00

abstract：:The blood-brain barrier (BBB) limits the distribution of systemically administered therapeutics to the central nervous system (CNS). Intranasal delivery is a noninvasive method that targets drugs to the brain and spinal cord along olfactory and trigeminal neural pathways, bypassing the BBB and minimizing systemic expo...

journal_title：Journal of pharmaceutical sciences

authors： Dhuria SV,Hanson LR,Frey WH 2nd

更新日期：2009-07-01 00:00:00

abstract：:Hemoglobin microcapsules were prepared through cross-linking of hemoglobin itself with various acyldichlorides. Variations in the reticulation conditions were preformed in order to ameliorate the oxygen dissociation curve, the mean diameter, and the possibility for the microcapsules to be lyophilized. With terephthalo...

journal_title：Journal of pharmaceutical sciences

authors： Lévy MC,Rambourg P,Lévy J,Potron G

更新日期：1982-07-01 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：:Amphiphilic cyclodextrins (CDs) are biocompatible derivatives of natural CDs and are able to form nanoparticles or polyplexes spontaneously. In this study, nanoparticles prepared from nonionic (6OCaproβCD) or cationic amphiphilic CD (PC βCDC6) were used comparatively to develop nanoparticles intended for breast cancer...

journal_title：Journal of pharmaceutical sciences

authors： Varan G,Öncül S,Ercan A,Benito JM,Ortiz Mellet C,Bilensoy E

更新日期：2016-10-01 00:00:00

abstract：:Apomorphine, a dopamine receptor agonist for treating Parkinson's disease, has very poor oral bioavailability (<2%) due to the first-pass effect. The aim of this work was to investigate whether the oral bioavailability and brain regional distribution of apomorphine could be improved by utilizing solid lipid nanopartic...

journal_title：Journal of pharmaceutical sciences

authors： Tsai MJ,Huang YB,Wu PC,Fu YS,Kao YR,Fang JY,Tsai YH

更新日期：2011-02-01 00:00:00

abstract：:The quassinoids bruceantin, brucein D, brucein E, bruceoside A, and brusatol significantly inhibited P-388 lymphocytic leukemic cell RNA and protein synthesis in tissue culture. However, DNA synthesis inhibition seemed to correlate more directly with the anti-neoplastic activity of these compounds in the in vivo P-338...

journal_title：Journal of pharmaceutical sciences

authors： Hall IH,Lee KH,Eigebaly SA,Imakura Y,Sumida Y,Wu RY

更新日期：1979-07-01 00:00:00

abstract：:Coralyne analogues, isomers, and related alkaloids were examined as inhibitors of reverse transcriptase of RNA tumor viruses in the presence of polyriboadenylic acid-oligodeoxythymidylic acid (Poly rA.oligo dT), polydeoxyadenylic acid-oligodeoxythymidylic acid (Poly dA.oligo dT), polyribocytidylic acid-oligodeoxyguany...

journal_title：Journal of pharmaceutical sciences

authors： Sethi ML

更新日期：1985-08-01 00:00:00

abstract：:The direct photoisomerization of (E)-4-(1-imidazoylmethyl)-cinnamic acid (IMC), a thromboxane synthetase inhibitor, to its (Z)-isomer at pH 2.0 was decelerated by beta-cyclodextrin (beta-CyD) and heptakis(2,6-di-O-methyl)-beta-cyclodextrin (DM-beta-CyD). The photostationary composition [(Z)-isomer:IMC ratio] was shift...

journal_title：Journal of pharmaceutical sciences

authors： Hirayama F,Utsuki T,Uekama K,Yamasaki M,Harata K

更新日期：1992-08-01 00:00:00