Design and development of adjuvant-active nonionic block copolymers.

abstract：:Accurate prediction of target occupancy facilitates central nervous system drug development. In this review, we discuss the predictability of serotonin transporter (SERT) occupancy in human brain estimated from in vitro Ki values for human SERT and plasma concentrations of unbound drug (Cu,plasma), as well as the impa...

journal_title：Journal of pharmaceutical sciences

authors： Yahata M,Chiba K,Watanabe T,Sugiyama Y

更新日期：2017-09-01 00:00:00

abstract：:A reported fluorometric method to determine tetracycline in biological material was modified to determine low levels of the antibiotics when using only small amounts of starting material. The method is applicable to tissue distribution studies in small experimental animals and also can be used for serial determination...

journal_title：Journal of pharmaceutical sciences

authors： van den Bogert C,Kroon AM

更新日期：1981-02-01 00:00:00

abstract：:The present work shows that the heated carbamazepine (CBZ) powder form III can be described as purely triclinic form I or a mixture of triclinic form I and monoclinic form III, depending on the resolution of the X-ray diffraction equipment used. Visual identification of the minor phase is possible when high-resolution...

journal_title：Journal of pharmaceutical sciences

authors： Antonio SG,Benini FR,Ferreira FF,Rosa PC,Paiva-santos Cde O

更新日期：2011-07-01 00:00:00

abstract：:Solvent influences on the crystallization of polymorph and hydrate forms of the nootropic drug piracetam (2-oxo-pyrrolidineacetamide) were investigated from water, methanol, 2-propanol, isobutanol, and nitromethane. Crystal growth profiles of piracetam polymorphs were constructed using time-resolved diffraction snapsh...

journal_title：Journal of pharmaceutical sciences

authors： DeMatos LL,Williams AC,Booth SW,Petts CR,Taylor DJ,Blagden N

更新日期：2007-05-01 00:00:00

abstract：:Eleven quinazolinylformamidines and quinazolinediylbisformamidines were synthesized and investigated for antihypertensive activity in spontaneous hypertensive rats. Several compounds showed moderate antihypertensive activity at 100 mg/kg po. The same compounds were not hypotensive in the normotensive dog. ...

journal_title：Journal of pharmaceutical sciences

authors： Warren JD,Lang SA Jr,Chan PS,Marsico JW

更新日期：1978-10-01 00:00:00

abstract：:This study is to prepare and evaluate Pluronics-modified mixed micelle (MM) to deliver polyphenolic myricetin (MYR) across the blood-brain barrier. MYR has been proven to be an effective anticancer agent against glioblastoma cells in our previous studies. However, the poor solubility of MYR limits its access to the br...

journal_title：Journal of pharmaceutical sciences

authors： Wang G,Wang JJ,Li F,To SS

更新日期：2016-04-01 00:00:00

abstract：:A physiological flow model was developed for the distribution of sulfathiazole residues in various tissues in swine. The approach was compartmental, in which the compartments and equilibrium constants had physiological meaning. Differential equations were developed, and appropriate parameter values and initial conditi...

journal_title：Journal of pharmaceutical sciences

authors： Duddy J,Hayden TL,Bourne DW,Fiske WD,Benedek IH,Stanley D,Gonzalez A,Heierman W

更新日期：1984-11-01 00:00:00

abstract：:A reinvestigation of the constituents of the Osage orange (maclura pomifera) yielded, in addition to the previously reported triterpenses (lupeol, butyrospermol, and lupan-3beta,20-diol), the pigments osajin and pomiferin, and a previously unreported constituent. The structure of this new compound was investigated. On...

journal_title：Journal of pharmaceutical sciences

authors： Gearien JE,Klein M

更新日期：1975-01-01 00:00:00

abstract：:A rotating-basket apparatus for dissolution testing of veterinary bolus tablets was designed and constructed. Sulfamethazine boluses containing different disintegrating agents were evaluated in vitro and by blood level data following administration to cattle. The dissolution t50 and various pharmacokinetic parameters ...

journal_title：Journal of pharmaceutical sciences

authors： Frazier WF,Nuessle NO

更新日期：1976-12-01 00:00:00

abstract：:The acidic, neutral, and alkaline degradations of six therapeutically useful cephalosporins (cephalothin, cephaloridine, cephaloglycin, cephalexin, cephradine, and cefazolin), 7-amino-cephalosporanic acid, 7-aminodeacetoxycephalosporanic acid, and some 7-substituted derivatives were followed by high-pressure liquid ch...

journal_title：Journal of pharmaceutical sciences

authors： Yamana T,Tsuji A

更新日期：1976-11-01 00:00:00

abstract：:Several Several 10-(1-acetyl-4-arylthiosemicarbazido) phenothiazines and their corresponding cyclized 10-(2-arylimino-3-acetylamino-4-thiazolidonyl)phenothiazines were synthetized and characterized by their sharp melting points and elemental analyses. All compounds inhibited nicotinamide adenine dinucleotide (NAD)-dep...

journal_title：Journal of pharmaceutical sciences

authors： Singh SP,Ali B,Auyong TK,Parmar SS,De Boer B

更新日期：1976-03-01 00:00:00

abstract：:A high-performance liquid chromatographic method with spectrofluorometric detection has been developed for the analysis of a new substituted benzamide and its metabolite in body fluids. The detection was performed at 270 nm for excitation, and 370 nm for emission. The proposed technique is selective, reliable, and sen...

journal_title：Journal of pharmaceutical sciences

authors： Bressolle F,Bres J,Moulin A

更新日期：1990-06-01 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 effects of various factors on the adsorption of nicotinic acid onto and desorption from activated charcoal were investigated in vitro. The affinity of nicotinic acid for charcoal was poor both in acidic and neutral media. Adsorption increased with increasing charcoal:drug ratios and decreasing incubation volume:ch...

journal_title：Journal of pharmaceutical sciences

authors： Roivas L,Neuvonen PJ

更新日期：1992-09-01 00:00:00

abstract：:The effect of dimethyl sulfoxide, dimethyl formamide, and dimethyl acetamide on the basal stratum corneum of excised nude mouse skin was investigated. All of these dipolar aprotic solvents caused a swelling of the basal stratum corneum cells and a disruption of the normal keratin pattern. This behavior suggests that d...

journal_title：Journal of pharmaceutical sciences

authors： Sharata HH,Burnette RR

更新日期：1988-01-01 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：:An immune response for a nasal ovalbumin (OVA) powder formulation with an applied nasal delivery platform technology, consisting of a powdery nasal carrier and a device, was evaluated in monkeys with similar upper respiratory tracts and immune systems to those of humans, in order to assess the applicability to a vacci...

journal_title：Journal of pharmaceutical sciences

authors： Torikai Y,Sasaki Y,Sasaki K,Kyuno A,Haruta S,Tanimoto A

更新日期：2020-12-03 00:00:00

abstract：:The oral dose metabolism of dilazep dihydrochloride [tetrahydro-1H-1,4-diazepine-1,4(5H)-dipropanol 3,4,5-trimethoxybenzoate] was examined in six hypertensive patients receiving a single oral dose of 600 mg of dilazep (3-3.8 mg/kg BW). Blood was collected at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, and 24 h after administratio...

journal_title：Journal of pharmaceutical sciences

authors： Sambhi MP,Kannan R,Thananopavarn C,Ookhtens M,Gudenzi M

更新日期：1989-04-01 00:00:00

abstract：:Papers and patents that deal with polymorphism (crystal systems for which a substance can exist in structures characterized by different unit cells, but where each of the forms has exactly the same elemental composition) and solvatomorphism (systems where the crystal structures of the substance are defined by differen...

journal_title：Journal of pharmaceutical sciences

authors： Brittain HG

更新日期：2009-05-01 00:00:00

abstract：:Anhydrotetracycline (AHTC), one of the major toxic decomposition products of the antibiotic tetracycline, contains several potential binding sites to metal ions. The acidity constants of the ligand were calculated in aqueous medium (I = 0.1 M) at 25 and 37 degrees C. We found pKa1 = 3.23 +/- 0.08, pKa2 = 5.94 +/- 0.09...

journal_title：Journal of pharmaceutical sciences

authors： de Siqueira JM,Carvalho S,Paniago EB,Tosi L,Beraldo H

更新日期：1994-03-01 00:00:00

abstract：:The hydrolysis of acetylcholine and acetylcholine mustard by acetylcholinesterase was compared over a substrate concentration range of 1-10 mM. Reactions were allowed to proceed for 2 min at 25 degrees. Results of these experiments reveal that the substrates have similar affinities for the enzyme, whereas the maximum ...

journal_title：Journal of pharmaceutical sciences

authors： Hudgins PM,Stubbins JF

更新日期：1975-08-01 00:00:00

abstract：:Oxycodone is an opioid analgesic that is administered orally or parenterally. The time-course of opioid action is a function of the systemic kinetics of the opioid, and the rate and extent of its entry into the brain and central nervous system. The latter is incompletely understood for oxycodone. Therefore, the cerebr...

journal_title：Journal of pharmaceutical sciences

authors： Villesen HH,Foster DJ,Upton RN,Somogyi AA,Martinez A,Grant C

更新日期：2006-08-01 00:00:00

abstract：:Pepsin adsorbed on gibbsite or boehmite, non-acid-reactive forms of aluminum hydroxide, had a significantly lower activity than pepsin in solution. IR and desorbed pepsin activity studies showed that the reduced activity of adsorbed pepsin was not due to denaturation of pepsin on adsorption. Steric occlusion of the ac...

journal_title：Journal of pharmaceutical sciences

authors： Sepelyak RJ,Feldkamp JR,Regnier FE,White JL,Hem SL

更新日期：1984-11-01 00:00:00

abstract：:Arginine-glycine-aspartate (RGD) has been shown to be essential for the recognition of integrins overexpressed in tumor cells, especially during tumor invasion, angiogenesis, and metasis. In this study, a novel tetrapeptide, RGD-valine (RGDV), was designed and attached to the N position of 1-β-D-arabinofuranosylcytosi...

journal_title：Journal of pharmaceutical sciences

authors： Wang F,Cui C,Ren Z,Wang L,Liu H,Cui G

更新日期：2012-12-01 00:00:00

abstract：:Thirty-four vasodilators were screened in several in vitro biochemical assays related to smooth muscle excitation-contraction coupling, binding to beta 1-,beta 2-, and alpha-adrenergic receptors, inhibition of phosphodiesterase activity, and antagonism of calcium accumulation. Isoproterenol and perhexiline only exhibi...

journal_title：Journal of pharmaceutical sciences

authors： Greenslade FC,Scott CK,Newquist KL,Krider KM,Chasin M

更新日期：1982-01-01 00:00:00

abstract：:Cosalane is a potent inhibitor of HIV replication with multiple sites of action. The purposes of this study were to (a) determine the extent and nature of cosalane binding to mucin, alpha(1)-acid glycoprotein (AAG), plasma, and human (HSA) and bovine serum (BSA) albumin, and (b) determine the primary site(s) of cosala...

journal_title：Journal of pharmaceutical sciences

authors： Kuchimanchi KR,Ahmed MS,Johnston TP,Mitra AK

更新日期：2001-05-01 00:00:00

abstract：:Experimental sulfadiazine tablets prepared by direct compression, using a commercially available direct compression tablet mass, were compared with experimental sulfadiazine tablets prepared by fluidized-bed granulation and commercially available sulfadiazine tablets USP. The values for friability and the time require...

journal_title：Journal of pharmaceutical sciences

authors： Ritschel WA,Erni W

更新日期：1977-10-01 00:00:00

abstract：:There is a need to identify suitable blends of solvents to dissolve drugs. Empirical approaches, such as trial-and-error and response surface, require several solubility measurements. In this study the UNIFAC method was used to predict solubility in highly nonideal multicomponent systems in which only the solute entha...

journal_title：Journal of pharmaceutical sciences

authors： Ochsner AB,Sokoloski TD

更新日期：1985-06-01 00:00:00

abstract：:Successful development of stable solid protein formulations usually requires the addition of one or several excipients to achieve optimal stability. In these products, there is a potential risk of an inhomogeneous distribution of the various ingredients, specifically the ratio of protein and stabilizer may vary. Such ...

journal_title：Journal of pharmaceutical sciences

authors： Nguyen KTT,Frijlink HW,Hinrichs WLJ

更新日期：2020-01-01 00:00:00

abstract：:Recently, our laboratory reported that intravenous immunoglobulin (IVIG) treatment increased antiplatelet antibody (7E3) clearance in a rat model of immune thrombocytopenic purpura (ITP). However, due to the multifaceted nature of IVIG therapy, the contribution of this increase in antiplatelet antibody clearance to th...

journal_title：Journal of pharmaceutical sciences

authors： Hansen RJ,Balthasar JP

更新日期：2003-06-01 00:00:00