Phenytoin prodrugs VI: In vivo evaluation of a phosphate ester prodrug of phenytoin after parenteral administration to rats.

abstract：:The pharmacokinetics of atropine in three healthy male volunteers after intravenous administration of 1.35 and 2.15 mg of the drug was determined. Pharmacodynamic effects of atropine were measured simultaneously. All the data were fitted to a novel integrated kinetic-dynamic model. Plasma concentrations of atropine an...

journal_title：Journal of pharmaceutical sciences

authors： Hinderling PH,Gundert-Remy U,Schmidlin O

更新日期：1985-07-01 00:00:00

abstract：:Solvent-induced 3 frameworks (the monohydrate, methanol solvate, and dimethyl formamide [DMF] solvate) of an anticancer drug, 7-ethyl-10-hydroxycamptothecin (SN38), were constructed. The crystal structures of the 3 pseudopolymorphs were characterized by single-crystal X-ray diffraction technique for the first time. Cr...

journal_title：Journal of pharmaceutical sciences

authors： Fang L,Wang L,Yao C,Song S,Wu Z,Tao X

更新日期：2017-10-01 00:00:00

abstract：:Terbinafine is an allylamine antifungal agent that is highly lipophilic and keratophilic. The aim of this study was to investigate terbinafine distribution in peripheral and visceral tissues after intravenous administration to rats. Terbinafine, 6 mg/kg, was administered to 33 male Sprague-Dawley rats via a jugular ve...

journal_title：Journal of pharmaceutical sciences

authors： Hosseini-Yeganeh M,McLachlan AJ

更新日期：2001-11-01 00:00:00

abstract：:A combination of coformer screening and modeling, followed by characterization using calorimetry, structure elucidation, and solubility led to the identification of novel crystalline forms of the hepatitis C protease inhibitor, telaprevir. The lead crystalline form, a cocrystalline solid of telaprevir with 4-aminosaly...

journal_title：Journal of pharmaceutical sciences

authors： Stavropoulos K,Johnston SC,Zhang Y,Rao BG,Hurrey M,Hurter P,Topp EM,Kadiyala I

更新日期：2015-10-01 00:00:00

abstract：:The pharmacokinetics and safety of TY-11345 [(+/-)-2-[(4-methoxy-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9- yl)sulfinyl]-1H-benzimidazole sodium salt], a novel gastric proton pump inhibitor, were studied in healthy male volunteers after single (20, 40, and 80 mg) and repeated oral doses (60 mg, once daily for 7 day...

journal_title：Journal of pharmaceutical sciences

authors： Uematsu T,Nakano M,Kosuge K,Nagai A,Sato A,Nakashima M

更新日期：1994-10-01 00:00:00

abstract：:Dissolution profiles are classified in accordance with the shape of fractional dissolution rate function. This function is constant in time for the classical first-order model and, in this case, the dissolution is described by a monoexponential function. Therefore, any deviation of the fractional dissolution rate from...

journal_title：Journal of pharmaceutical sciences

authors： Lánský P,Weiss M

更新日期：2003-08-01 00:00:00

abstract：:The aim of this study is to evaluate the effect of peptide cyclization on the blood-brain barrier (BBB) modulatory activity and plasma stability of His-Ala-Val peptides, which are derived from the extracellular 1 domain of human E-cadherin. The activities to modulate the intercellular junctions by linear HAV4 (Ac-SHAV...

journal_title：Journal of pharmaceutical sciences

authors： Alaofi A,On N,Kiptoo P,Williams TD,Miller DW,Siahaan TJ

更新日期：2016-02-01 00:00:00

abstract：:The recently introduced four-parameter extended Hansen approach was used to study the solubility of p-hydroxybenzoic acid and methyl p-hydroxybenzoate in 32 and 35 individual solvents, respectively. The results are compared with those for benzoic acid in 40 solvents. Seventeen of the thirty-two or 53% of the calculate...

journal_title：Journal of pharmaceutical sciences

authors： Martin A,Wu PL,Beerbower A

更新日期：1984-02-01 00:00:00

abstract：:Oral Almotriptan maleate (ALM) is used in the treatment of migraine; however, due to its extreme aqueous solubility, shows poor penetration and lesser concentration in the brain thus requiring frequent oral dosing. Being flexible and lipophilic in nature, nanostructured lipid carriers (NLCs) represent a promising tool...

journal_title：Journal of pharmaceutical sciences

authors： Salem LH,El-Feky GS,Fahmy RH,El Gazayerly ON,Abdelbary A

更新日期：2020-07-01 00:00:00

abstract：:In a continuing search for new biologically active agents derived from indolizine, 3-(2-aminoethyl)-2-methylindolizine, 3-(2-aminoethyl)-2-methyl-5,6,7,8-tetrahydroindolizine, and some mono- and di-N-substituted derivatives were prepared. Initial pharmacological screening showed that these compounds possess anti-5-hyd...

journal_title：Journal of pharmaceutical sciences

authors： Antonini I,Claudi F,Gulini U,Micossi L,Venturi F

更新日期：1979-03-01 00:00:00

abstract：:Remifentanil (Ultiva) is a novel, ultra-short-acting opioid which has recently been approved for use as an analgesic during induction and maintenance of general anesthesia. Esmolol is a short-acting beta-blocker used during surgical procedures to reduce heart rate and blood pressure. Both drugs are metabolized by nons...

journal_title：Journal of pharmaceutical sciences

authors： Haidar SH,Moreton JE,Liang Z,Hoke JF,Muir KT,Eddington ND

更新日期：1997-11-01 00:00:00

abstract：:Crystallization of drugs in metastable, supersaturated adhesive polymeric matrices in transdermal drug delivery devices can be avoided by determination of the solubility of the drug in the adhesive polymer. A novel method is described to determine the solubility of the drug in polymeric matrices. Unlike existing metho...

journal_title：Journal of pharmaceutical sciences

authors： Jasti BR,Berner B,Zhou SL,Li X

更新日期：2004-08-01 00:00:00

abstract：:First-order rate constants (k) were determined for the hydrolysis of ceftazidime in the pH range of 0.5 to 8.5 at 45, 55, and 65 degrees C by a stability-indicating HPLC assay. In the absence of buffer effects, the pH-rate expression was k = kH1f1(aH+) + kH2f2(aH+) + kH3f3(aH+) + kSf3 + kOHf3(aOH-), where KH and KOH a...

journal_title：Journal of pharmaceutical sciences

authors： Zhou M,Notari RE

更新日期：1995-05-01 00:00:00

abstract：:Cytochrome P450 1B1 (CYP1B1) has been reported to have a major role in metabolizing arachidonic acid (AA) into cardiotoxic metabolites, mid-chain hydroxyeicosatetraenoic acids (HETEs). Recently, we have shown that fluconazole decreases the level of mid-chain HETEs in human liver microsomes. Therefore, the objectives o...

journal_title：Journal of pharmaceutical sciences

authors： Alammari AH,Shoieb SM,Maayah ZH,El-Kadi AOS

更新日期：2020-07-01 00:00:00

abstract：:The combined clearance of endogenous 6β-hydroxycortisol and 6β-hydroxycortisone is suggested biomarker for in vivo cytochrome P450 3A (CYP3A) activity. We aimed to determine whether the combined clearance of these two markers together with information of biopharmaceutics classification system (BCS) of drugs could be u...

journal_title：Journal of pharmaceutical sciences

authors： Luo X,Zheng L,Cai N,Liu Q,Yang S,He X,Cheng Z

更新日期：2015-10-01 00:00:00

abstract：:Chitosan microspheres were evaluated for sustained-release of recombinant human interleukin-2 (rIL-2) in this study. In addition, the effects of different formulation factors, such as chitosan and protein concentrations, the volume of sodium sulfate solution, addition technique of rIL-2, and presence of glutaraldehyde...

journal_title：Journal of pharmaceutical sciences

authors： Ozbaş-Turan S,Akbuğa J,Aral C

更新日期：2002-05-01 00:00:00

abstract：:Gelrite, a heteropolysaccharide that forms a gel in the presence of cations, was tested in humans for its efficacy as an ophthalmic vehicle by a nonivasive fluorometric technique. Fluorescein was used as the tracer, and its concentration in the anterior chamber was used as the principal measure of bioavailability. The...

journal_title：Journal of pharmaceutical sciences

authors： Maurice DM,Srinivas SP

更新日期：1992-07-01 00:00:00

abstract：:The fungal microorganism Cunninghamella echinulata was utilized to para-hydroxylate the synthetic substrate (+/-)-1-isopropylamino-3-phenoxy-propan-2-ol (1). The resulting product, (+/-)-1-(4-hydroxyphenoxy)-3-isopropylamino-propan-2-ol, or (+/-)-prenalterol, (2) was formed in greater than 85% yield. Extracts from inc...

journal_title：Journal of pharmaceutical sciences

authors： Pasutto FM,Singh NN,Jamali F,Coutts RT,Abuzar S

更新日期：1987-02-01 00:00:00

abstract：:The solubility of a drug is ultimately governed by its chemical potential as it is present in the undissolved solute. For a pharmaceutical amorphous solid dispersion (ASD), its solubility depends on the state and composition of the undissolved solute when the ASD is equilibrated with water. Concerning the undissolved ...

journal_title：Journal of pharmaceutical sciences

authors： Huang S,Mao C,Williams RO 3rd,Yang CY

更新日期：2016-12-01 00:00:00

abstract：:In this study, we explored the bioavailability in dogs and chemical potency of generic ritonavir and lopinavir/ritonavir tablet products manufactured by various pharmaceutical companies. Chemical potency of the products was examined by HPLC quantitation of ritonavir and lopinavir. Using a dog model, we determined poin...

journal_title：Journal of pharmaceutical sciences

authors： Garren KW,Rahim S,Marsh K,Morris JB

更新日期：2010-02-01 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：:A new extraction-spectrophotometric method for the determination of hydralazine, based on its reaction with 2-hydroxy-1-naphthaldehyde at 25 degrees C, is described. The calibration curve was linear between 0.4 and 6 mg/mL of hydralazine. The molar absorbtivity of the product at 408 nm is 40,900 L.mol-1.cm-1. The meth...

journal_title：Journal of pharmaceutical sciences

authors： Mari-Buigues J,Mañes-Vinuesa J,Garcia-Domenech R,Pous-Miralles G

更新日期：1991-07-01 00:00:00

abstract：:The oral absorption of drugs has been represented by various concepts such as the absorption potential, the maximum absorbable dose, the biopharmaceutics classification system, and in vitro-in vivo correlation. The aim of this article is to provide an overview of the theoretical relationships between these concepts. I...

journal_title：Journal of pharmaceutical sciences

authors： Sugano K,Terada K

更新日期：2015-09-01 00:00:00

abstract：:The pharmacokinetics of valproic acid after oral administration of sustained-release formulations were studied in 12 healthy volunteers. The objective of the present study was to find an appropriate mathematical model to describe the complex drug intake process. The concentration of valproic acid in plasma was measure...

journal_title：Journal of pharmaceutical sciences

authors： Bressolle F,Gomeni R,Alric R,Royer-Morrot MJ,Necciari J

更新日期：1994-10-01 00:00:00

abstract：:Continuing work on the interaction of inorganic additives with nonionic surfactants in aqueous solution dealt with their effect on the CMC and surface tension. The surfactants were octoxynol and polyoxyethylated oleyl alcohol, containing an average of 9.5 and 10 ethylene oxide units, respectively. Their CMC values wer...

journal_title：Journal of pharmaceutical sciences

authors： Schott H,Han SK

更新日期：1976-07-01 00:00:00

abstract：:The aim of this study is to explore hot melt extrusion (HME) as a solvent-free drug loading technique for preparation of stable amorphous solid dispersions using mesoporous silica (PSi). Ibuprofen and carvedilol were used as poorly soluble active pharmaceutical ingredients (APIs). Due to the high friction of an API:PS...

journal_title：Journal of pharmaceutical sciences

authors： Genina N,Hadi B,Löbmann K

更新日期：2018-01-01 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：:Surfactants stabilize proteins through two major mechanisms: (1) their preferential location at nearby interfaces, in this way precluding protein adsorption; and/or (2) their association with protein into "complexes" that prevent proteins from interacting with surfaces as well as each other. However, selection of surf...

journal_title：Journal of pharmaceutical sciences

authors： Kim HL,McAuley A,McGuire J

更新日期：2014-05-01 00:00:00

abstract：:Although insulin receptor is expressed at the human blood-brain barrier (BBB), the physiological and pathologic roles of insulin signaling in biologic responses at the BBB remain unclear. Here, we investigate insulin signaling at the human BBB using human cerebral microvascular endothelial cell line (hCMEC/D3) as a we...

journal_title：Journal of pharmaceutical sciences

authors： Ito S,Yanai M,Yamaguchi S,Couraud PO,Ohtsuki S

更新日期：2017-09-01 00:00:00

abstract：:It was reported that wax matrix (WM) particles composed of low-melting-point microcrystalline wax showed unique release behaviors; the particles released only a small amount of the entrapped drug (non-diffusion-controlled release) at 37°C, whereas it showed comparatively fast drug release in a diffusion-controlled man...

journal_title：Journal of pharmaceutical sciences

authors： Matsumoto K,Kimura SI,Noguchi S,Itai S,Kondo H,Iwao Y

更新日期：2019-06-01 00:00:00