TOPS-MODE approach for the prediction of blood-brain barrier permeation.

abstract：:Previous studies from this laboratory suggested that a solution model (Flory-Huggins equation) modified by a free volume model (Vrentas equation) could satisfactorily describe water absorption into an amorphous solid composed of a sugar or a polymer. This paper has extended the studies of single solutes to binary mixt...

journal_title：Journal of pharmaceutical sciences

authors： Zhang J,Zografi G

更新日期：2001-09-01 00:00:00

abstract：:Health interventions developed for wealthy nations are difficult to introduce in developing countries due to a lack of sufficient technological, financial, political, or infrastructural resources. Increasingly, however, product developers are creating new technologies that meet the needs of low-resource settings. Expe...

journal_title：Journal of pharmaceutical sciences

authors： Harner-Jay C,Sherris J

更新日期：2008-12-01 00:00:00

abstract：:An analysis of the disintegration-dissolution sequence of drug release from a tablet leads to a mathematical expression relating disintegration to the dissolution profile of the tablet and the dissolution rate of the primary drug particles in the tablet. The equation describing the disintegration of an acetaminophen t...

journal_title：Journal of pharmaceutical sciences

authors： Nelson KG,Wang LY

更新日期：1978-01-01 00:00:00

abstract：:The comparative pharmacokinetics of free MTP-PE (muramyl tripeptide phosphatidyl ethanolamine) and MTP-PE entrapped in negatively charged multilamellar liposomes (liposomal MPT-PE) was evaluated in rats at a bolus intravenous (i.v.) dose of 0.2 mg/kg and in dogs at a bolus i.v. dose of 0.1 mg/kg. Additional studies we...

journal_title：Journal of pharmaceutical sciences

authors： Gay B,Cardot JM,Schnell C,van Hoogevest P,Gygax D

更新日期：1993-10-01 00:00:00

abstract：:Model independent pharmacokinetic analysis of intravenous (iv) amphotericin B cochleates (CAMB), a new lipid-based drug delivery system, in mice (0.625 mg/kg) shows a two-phase disposition profile in blood [area under the curve of concentration versus time from time zero to infinity (AUC(0-infinity)) = 1.01 microg. h/...

journal_title：Journal of pharmaceutical sciences

authors： Segarra I,Movshin DA,Zarif L

更新日期：2002-08-01 00:00:00

abstract：:An HPLC method for determining total pyridoxal from plasma was developed for a relative bioavailability comparison of two oral vitamin B6 (pyridoxine HCl) preparations. After cleavage of the pyridoxal-5-phosphate with the acid phosphatase enzyme, the total pyridoxal was determined by HPLC. Pyridoxal was separated on a...

journal_title：Journal of pharmaceutical sciences

authors： Mascher H

更新日期：1993-09-01 00:00:00

abstract：:Low-frequency ultrasound (20 kHz) and surfactants have been individually shown to enhance transdermal drug transport. In this study, we investigated the synergistic effect of ultrasound and surfactants on transdermal drug delivery. Surfactants with different head group chemistries including anionic, cationic, and noni...

journal_title：Journal of pharmaceutical sciences

authors： Tezel A,Sens A,Tuchscherer J,Mitragotri S

更新日期：2002-01-01 00:00:00

abstract：:The use of intravascular tyrosine (TYR) to enhance catecholamine release in hemorrhagic shock and other cardiovascular diseases, or as a constituent of nutrient mixtures used for total parenteral nutrition, is limited by the unusually poor solubility of the amino acid in water. We have thus examined the ability of var...

journal_title：Journal of pharmaceutical sciences

authors： Maher TJ,Kiritsy PJ,Moya-Huff FA,Casacci F,De Marchi F,Wurtman RJ

更新日期：1990-08-01 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：: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 thiazide diuretic chlorothiazide is poorly metabolized, and is predominantly excreted via the kidneys. We have previously shown that chlorothiazide is transported by ATP-binding cassette transporter G2, suggesting a potential role for this transporter in apical efflux of chlorothiazide in the kidney. However, beca...

journal_title：Journal of pharmaceutical sciences

authors： Juhász V,Beéry E,Nagy Z,Bui A,Molnár E,Zolnerciks JK,Magnan R,Jani M,Krajcsi P

更新日期：2013-05-01 00:00:00

abstract：:Ensuring the health of street-involved children is a growing public health challenge. These children are vulnerable, neglected, and rarely a priority for basic service providers and governments. Sizable populations of street-involved children are present in major urban areas worldwide and current trends in urbanizatio...

journal_title：Journal of pharmaceutical sciences

authors： Osei-Twum JA,Wasan KM

更新日期：2012-10-01 00:00:00

abstract：:6-Amino-2-mercapto-5-methylpyrimidine-4-carboxylic acid proved to be a potent hypolipidemic agent in rodents at the low dose of 20 mg/kg/d. The agent effectively reduced the liver enzyme activities required for the synthesis of triglycerides and cholesterol. Lower lipid levels in tissue were observed in mice but not i...

journal_title：Journal of pharmaceutical sciences

authors： Hall IH,Cocolas GH,Murthy AR,Rhyne KA,Knowles M

更新日期：1985-07-01 00:00:00

abstract：:Several controlled ice nucleation techniques have been developed to increase the efficiency of the freeze-drying process as well as to improve the quality of pharmaceutical products. Owing to the reduction in ice surface area, these techniques have the potential to reduce the degradation of proteins labile during free...

journal_title：Journal of pharmaceutical sciences

authors： Fang R,Tanaka K,Mudhivarthi V,Bogner RH,Pikal MJ

更新日期：2018-03-01 00:00:00

abstract：:Metronidazole and four derivatives were studied in vitro to investigate the differences in the extent of their binding to plasma proteins. Modification at the terminal portion of the alkyl side chain resulted in wide differences in the extent of binding. Molecular orbital calculations were performed by the CNDO and MI...

journal_title：Journal of pharmaceutical sciences

authors： Sanvordeker DR,Chien YW,Lin TK,Lambert HJ

更新日期：1975-11-01 00:00:00

abstract：:The in vivo dissolution of many poorly soluble drugs is enhanced by the action of surfactants secreted into the upper gastrointestinal (GI) tract. These substances may act by solubilizing individual drug molecules into two separate liquid phases: the free aqueous phase and a micellar phase in which the drug is incorpo...

journal_title：Journal of pharmaceutical sciences

authors： Rao VM,Lin M,Larive CK,Southard MZ

更新日期：1997-10-01 00:00:00

abstract：:A difference spectrophotometric analytical method was developed for the selective determination of p-hydroxybenzoic acid in the presence of its alkyl esters without prior separation. Based on the spectral shift to a shorter wavelength accompanyint carboxyl dissociation, the procedure measures as little as 2% of this a...

journal_title：Journal of pharmaceutical sciences

authors： Fink DW,Fink HC,Tolan JW,Blodinger J

更新日期：1978-06-01 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：:Two new methods for the simultaneous determination of chloroquine and its two main metabolites (monodesethylchloroquine and bisdesethylchloroquine) in biological samples, radioimmunoassay (RIA) and enzyme-linked immunosorbent assay (ELISA), are described. Antiserum is produced in rabbits immunized with N-(2-carboxyeth...

journal_title：Journal of pharmaceutical sciences

authors： Escande C,Chevalier P,Verdier F,Bourdon R

更新日期：1990-01-01 00:00:00

abstract：:Toxin-conjugates, complexes designed from the fusion of tissue toxins and pathology-specific ligands, offer the potential for targeted cytotoxic therapy. Some have postulated that the recurrent failure of these conjugates to exhibit benefit in animal models of vascular injury arose because the timing and frequency of ...

journal_title：Journal of pharmaceutical sciences

authors： Yu C,Cunningham M,Rogers C,Dinbergs ID,Edelman ER

更新日期：1998-11-01 00:00:00

abstract：:Quercetin is a bioactive flavonoid widely used as a health supplement. Being sparingly soluble and chemically unstable in aqueous intestinal fluids, quercetin is poorly absorbed orally. This study aimed to investigate the effects of three beta-cyclodextrins, namely, unsubstituted beta-cyclodextrin (beta-CD), hydroxypr...

journal_title：Journal of pharmaceutical sciences

authors： Zheng Y,Haworth IS,Zuo Z,Chow MS,Chow AH

更新日期：2005-05-01 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：:Two novel series of benzimidazole derivatives bearing structural modifications of certain drugs were prepared for evaluation for potential anticancer activity. The first series was a group of alkylating agents, and the second series was a variety of 4-substituted-1-thioacetyl-3-thiosemicarbazides. The tests of some re...

journal_title：Journal of pharmaceutical sciences

authors： Ibrahim ES,Omar AM,Khalil MA

更新日期：1980-11-01 00:00:00

abstract：:Protein and peptide antigens frequently are only slightly immunogenic when utilized alone in vaccines. Formulation of these antigens in a carrier vehicle, particularly when an adjuvant is included, often results in markedly enhanced immune responses. Encapsulation of peptide and protein antigens in liposomes generally...

journal_title：Journal of pharmaceutical sciences

authors： Richards RL,Alving CR,Wassef NM

更新日期：1996-12-01 00:00:00

abstract：:The O-trifluoroacetyl and N,O-trifluoroacetyl derivatives of a series of aporphine and noraporphine alkaloids were prepared, and their GLC and mass spectrometric characteristics were determined. The positional isomers apocodeine and isoapocodeine were resolved chromatographically as their trifluoroacetyl derivatives, ...

journal_title：Journal of pharmaceutical sciences

authors： Green JF,Jham GN,Neumeyer JL,Vouros P

更新日期：1980-08-01 00:00:00

abstract：:The release of potassium chloride from hydroxypropyl methylcellulose matrices was investigated for tablets prepared with several different compression forces. It was determined that the release kinetics for these systems deviates significantly from the classical t1/2 dependence. This behavior was attributed to air ent...

journal_title：Journal of pharmaceutical sciences

authors： Korsmeyer RW,Gurny R,Doelker E,Buri P,Peppas NA

更新日期：1983-10-01 00:00:00

abstract：:N-Acetyl-DL-penicillamine (IIIb), a structural analog of N-acetyl-L-cysteine (IIIa), did not protect mice from lethal doses of acetaminophen (I), whereas IIIa offered protection. This lack of efficacy of IIIb probably is due to the decreased nucleophilicity of its sulfhydryl group compared to that of IIIa, the probabl...

journal_title：Journal of pharmaceutical sciences

authors： Zera RT,Nagasawa HT

更新日期：1980-09-01 00:00:00

abstract：:Sucrose is a common cryoprotectant and lyoprotectant to stabilize labile biopharmaceuticals during freeze-drying and storage. Sucrose-based formulations require low primary drying temperatures to avoid collapse and monoclonal antibody (mAb) containing products need to be stored refrigerated. The objective of this stud...

journal_title：Journal of pharmaceutical sciences

authors： Haeuser C,Goldbach P,Huwyler J,Friess W,Allmendinger A

更新日期：2020-01-01 00:00:00

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：:Contraceptive natural steroids, such as progesterone and estradiol, are ineffective when administered orally because of extensive metabolism in the gastrointestinal (GI) tract during absorption and first-pass metabolism. Consequently, highly potent and potentially harmful synthetic steroids are now being used in oral...

journal_title：Journal of pharmaceutical sciences

authors： Hussain AA,Hirai S,Bawarshi R

更新日期：1981-04-01 00:00:00