Stability of the Hsp90 inhibitor 17AAG hydroquinone and prevention of metal-catalyzed oxidation.

abstract：:p-Bromospiperone was prepared from the reaction of spiperone with bromine. It was tested for dopamine receptor binding affinity in vitro and its ability to stimulate prolactin secretion in vivo. The results indicate no significant change of biological activities due to the bromination of spiperone. ...

journal_title：Journal of pharmaceutical sciences

authors： Huang CC,Friedman AM,So R,Simonovic M,Meltzer HY

更新日期：1980-08-01 00:00:00

abstract：:A α-helical GALA peptide (WEAALAEALAEALAEHLAEALAEALEALAA) has been found to possess dual functions: a pH-dependent inducer of endosomal escape, and a ligand that targets lung endothelium. In the present study, the flexibility of GALA was improved by modifying the edge with polyethylene glycol linker, to increase lung-...

journal_title：Journal of pharmaceutical sciences

authors： Santiwarangkool S,Akita H,Nakatani T,Kusumoto K,Kimura H,Suzuki M,Nishimura M,Sato Y,Harashima H

更新日期：2017-09-01 00:00:00

abstract：:A characterization and optimization of the in vitro transdermal iontophoretic transport of 5-hydroxy-2-(N,N,-di-n-propylamino)tetralin (5-OH-DPAT) is presented. The utility of acetaminophen as a marker of electroosmotic flow was studied as well. The following parameters of iontophoretic transport of 5-OH-DPAT were exa...

journal_title：Journal of pharmaceutical sciences

authors： Ackaert OW,Van Smeden J,De Graan J,Dijkstra D,Danhof M,Bouwstra JA

更新日期：2010-01-01 00:00:00

abstract：:Various complex mechanisms and their multifactorial pathways decisively provoke low-grade local and systemic inflammation in β-cells of pancreatic islets and peripheral tissues to induce β-cells' dysfunction and apoptosis, insulin resistance, and ultimately, overt type 2 diabetes mellitus (T2DM). Conventional antidiab...

journal_title：Journal of pharmaceutical sciences

authors： Akash MS,Shen Q,Rehman K,Chen S

更新日期：2012-05-01 00:00:00

abstract：:Several amides of cyclic amines were prepared and tested as penetration enhancers in the diffusion of various drugs through hairless mouse skin in vitro. Hexamethylenelauramide (hexahydro-1-lauroyl-1H-azepine) was selected as a broad spectrum penetration enhancer worthy of further study. Later, the duration of the eff...

journal_title：Journal of pharmaceutical sciences

authors： Mirejovsky D,Takruri H

更新日期：1986-11-01 00:00:00

abstract：:The aim of this study was to synthetize cocrystals of nateglinide, an antidiabetic agent of biopharmaceutics classification system Class IIa, as a strategy to improve both the solubility and the dissolution rate of the drug. Benzamide was selected by a screening procedure as a suitable coformer, and binary mixtures wi...

journal_title：Journal of pharmaceutical sciences

authors： Bruni G,Maggi L,Mustarelli P,Sakaj M,Friuli V,Ferrara C,Berbenni V,Girella A,Milanese C,Marini A

更新日期：2019-04-01 00:00:00

abstract：:Nasal administration as a means of delivering therapeutic agents preferentially to the brain has gained significant recent interest. While some substrates appear to be delivered directly to the brain via this route, the mechanisms governing overall brain uptake and exposure remain unclear. Some substrates utilize the ...

journal_title：Journal of pharmaceutical sciences

authors： Graff CL,Pollack GM

更新日期：2005-06-01 00:00:00

abstract：:The pharmacokinetics of drug delivery from transdermal controlled-release devices consisting of (a) a membrane plus a reservoir or (b) a monolithic slab are examined. For the period when the devices act as if the drug reservoir were infinite, simple relationships for the steady-state slope and time lag are derived and...

journal_title：Journal of pharmaceutical sciences

authors： Berner B

更新日期：1985-07-01 00:00:00

abstract：:The diffusion model for percutaneous absorption is developed for the specific case of delivery to the skin being limited by the application of a finite amount of solute. Two cases are considered; in the first, there is an application of a finite donor (vehicle) volume, and in the second, there are solvent-deposited so...

journal_title：Journal of pharmaceutical sciences

authors： Anissimov YG,Roberts MS

更新日期：2001-04-01 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：: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：:The purpose of the study is to understand the effect of altitude on the performance of selected pressurized metered dose inhalers (pMDIs) and dry powder inhalers (DPIs). A testing apparatus that created consistent breath profiles through the Alberta Idealized Throat was designed to test five pMDIs and two DPIs at alti...

journal_title：Journal of pharmaceutical sciences

authors： Titosky JTF,Morin CMD,Suderman JD,Olfert JS,Finlay WH,Vehring R

更新日期：2014-07-01 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：:The present studies were undertaken to describe the dynamic nature of the degradation and absorption of insulin in the subcutaneous injection site and to develop agents which would stabilize this dosage form. [125I]Insulin with 0.2-U/kg of unlabeled insulin in 10 microliters of aqueous solution was injected subcutaneo...

journal_title：Journal of pharmaceutical sciences

authors： Hori R,Komada F,Okumura K

更新日期：1983-04-01 00:00:00

abstract：:A procedure was developed for the separation and selective quantitative determination of the (S)(+)- and (R)(-)-enantiomers of the racemic anti-inflammatory drug carprofen as their diastereomeric l-(-)-alpha-methylbenzylamides. These derivatives are obtained in equivalent yields by reacint purified 14C-carprofen from ...

journal_title：Journal of pharmaceutical sciences

authors： Kemmerer JM,Rubio FA,McClain RM,Koechlin BA

更新日期：1979-10-01 00:00:00

abstract：:Flightless I (Flii) is an actin remodeling protein important for cytoskeletal regulation and cellular processes including migration, proliferation, and adhesion. Previous studies have clearly identified Flii as a novel therapeutical target for improved wound repair and have demonstrated Flii regulation using Flii neut...

journal_title：Journal of pharmaceutical sciences

authors： Haidari H,Zhang Q,Melville E,Kopecki Z,Song Y,Cowin AJ,Garg S

更新日期：2017-07-01 00:00:00

abstract：:Quality-by-design (QbD) is a systematic approach to drug development, which begins with predefined objectives, and uses science and risk management approaches to gain product and process understanding and ultimately process control. The concept of QbD can be extended to analytical methods. QbD mandates the definition ...

journal_title：Journal of pharmaceutical sciences

authors： Vogt FG,Kord AS

更新日期：2011-03-01 00:00:00

abstract：:Human alpha(1)-acid glycoprotein (AGP), a major carrier of many basic drugs in circulation, consists of at least two genetic variants, namely A and F1*S variant. Interestingly, the variants of AGP have different drug-binding properties. The purpose of this study was to identify the amino acid residues that are respons...

journal_title：Journal of pharmaceutical sciences

authors： Nishi K,Ueno M,Murakami Y,Fukunaga N,Akuta T,Kadowaki D,Watanabe H,Suenaga A,Maruyama T,Otagiri M

更新日期：2009-11-01 00:00:00

abstract：:In this study a 3D printed capsule designed to break from the physiological pressures in the antropyloric region was evaluated for its ability to deliver the synthetic octapeptide octreotide in beagle dogs when co-formulated with the permeation enhancer sodium caprate. The pressure sensitive capsules were compared to ...

journal_title：Journal of pharmaceutical sciences

authors： Berg S,Krause J,Björkbom A,Walter K,Harun S,Granfeldt A,Janzén D,Nunes SF,Antonsson M,Van Zuydam N,Skrtic S,Hugerth A,Weitschies W,Davies N,Abrahamsson B,Bergström CAS

更新日期：2021-01-01 00:00:00

abstract：:Some fused pyridazino[4,5-b]indoles (7) were synthesized. These new compounds present a planar topography and some resemblance to carbazeram, imadozan, and other pyridazino agents with cardiotonic activity. These compounds also possess a complementary effect as inhibitors of platelet aggregation. 6-(3,5-Dimethylpyrazo...

journal_title：Journal of pharmaceutical sciences

authors： Monge A,Aldana I,Losa MJ,Font M,Castiella E,Frechilla D,Cenarruzabeitia E,Martinez de Irujo JJ,Lopez-Unzu J,Alberdi E

更新日期：1993-05-01 00:00:00

abstract：:Most anticancer drugs are intended to function in the nuclei of cancer cells. If an anticancer drug could be delivered to mitochondria, the source of cellular energy, this organelle would be destroyed, resulting in the arrest of the energy supply and the killing of the cancer cells. To achieve such an innovative strat...

journal_title：Journal of pharmaceutical sciences

authors： Yamada Y,Munechika R,Kawamura E,Sakurai Y,Sato Y,Harashima H

更新日期：2017-09-01 00:00:00

abstract：:The effects of chlorpromazine, prochlorperazine, and trifluoperazine on the pressor actions of serotonin, angiotensin, and bradykinin in the perfused vessels of full-term human placentas were investigated. A significant inhibition of the effect of serotonin was observed with trifluoperazine and chlorpromazine but not ...

journal_title：Journal of pharmaceutical sciences

authors： Wolstenholme WW,Gautieri RF

更新日期：1976-10-01 00:00:00

abstract：:In the present study, a previously described sulfenamide prodrug of a basic antidiabetic drug, metformin, was evaluated further. This sulfenamide prodrug was designed to improve the permeability and consequently the oral absorption and bioavailability (F) of the highly water-soluble metformin. Bioactivation of the pro...

journal_title：Journal of pharmaceutical sciences

authors： Huttunen KM,Leppänen J,Vepsäläinen J,Sirviö J,Laine K,Rautio J

更新日期：2012-08-01 00:00:00

abstract：:This study was designed to examine the effect of benzalkonium chloride/ethylenediaminetetraacetic acid (BAK/EDTA) on the ocular bioavailability (Focular) of ketorolac tromethamine after ocular instillation to normal and de-epithelialized corneas of rabbits both in vitro and in vivo. The in vitro Focular of the formula...

journal_title：Journal of pharmaceutical sciences

authors： Madhu C,Rix PJ,Shackleton MJ,Nguyen TG,Tang-Liu DD

更新日期：1996-04-01 00:00:00

abstract：:For development and optimization of protein formulation sensitive analytical tools are required to follow both aggregation and changes in protein structure. The latter can be seen as the beginning of physical instability leading to aggregation. The focus of this work laid on the development of a novel analysis simulta...

journal_title：Journal of pharmaceutical sciences

authors： Printz M,Friess W

更新日期：2012-02-01 00:00:00

abstract：:A novel method is described for the preparation of sterile and pyrogen-free submicron liposomes of narrow size distribution. The method is based on the formation of a homogeneous dispersion of lipids in water-soluble carrier materials. To obtain the lipid-containing solid dispersion, liposome-forming lipids and water-...

journal_title：Journal of pharmaceutical sciences

authors： Li C,Deng Y

更新日期：2004-06-01 00:00:00

abstract：:The aim of this work was to evaluate the low molecular weight chitosans (LMWCs) as enhancers of transdermal administration of baicalin, an useful drug for the treatment of atopic dermatitis, viral hepatitis, and HIV infection. Permeation experiments were performed in vitro through mouse skin by using Franz cells. Impr...

journal_title：Journal of pharmaceutical sciences

authors： Zhou X,Liu D,Liu H,Yang Q,Yao K,Wang X,Wang L,Yang X

更新日期：2010-07-01 00:00:00

abstract：:The plasma protein binding of zomepirac, a new nonnarcotic analgesic, was studied using equilibrium dialysis. Experiments were performed using human plasma and plasma from mice, rats, and rhesus monkeys, all species of pharmacological or toxicological interest. At concentrations approximating those achieved in vivo, t...

journal_title：Journal of pharmaceutical sciences

authors： O'Neill PJ

更新日期：1981-07-01 00:00:00

abstract：:The purpose of this study was to develop a nanocarrier system for codelivery of paclitaxel (PTX) and piperlongumine (PL) and investigate the therapeutic potential of improving efficacy and reducing toxicity. PTX and PL were formulated into poly lactic-co-glycolic acid and D-α-tocopheryl polyethylene glycol succinate v...

journal_title：Journal of pharmaceutical sciences

authors： Liu Q,Zhao D,Zhu X,Chen H,Yang Y,Xu J,Zhang Q,Fan A,Li N,Guo C,Kong Y,Lu Y,Chen X

更新日期：2017-10-01 00:00:00

abstract：:Avoiding unwanted immunogenicity is of key importance in the development of therapeutic drug proteins. Animal models are of less predictive value because most of the drug proteins are recognized as foreign proteins. However, different methods have been developed to obtain immunotolerant animal models. So far, the immu...

journal_title：Journal of pharmaceutical sciences

authors： Brenden N,Madeyski-Bengtson K,Martinsson K,Svärd R,Albery-Larsdotter S,Granath B,Lundgren H,Lövgren A

更新日期：2013-03-01 00:00:00