"Predicting" Polymorphs of Pharmaceuticals Using Hydrogen Bond Propensities: Probenecid and Its Two Single-Crystal-to-Single-Crystal Phase Transitions.

abstract：:Thymoquinone (TQ) is the main bioactive component isolated from Nigella sativa essential oil and seeds and has been used for the treatment of inflammations, liver disorders, arthritis, and is of great importance as a promising therapeutic drug for different diseases including cancer. This paper reports the first exper...

journal_title：Journal of pharmaceutical sciences

authors： Lupidi G,Camaioni E,Khalifé H,Avenali L,Damiani E,Tanfani F,Scirè A

更新日期：2012-07-01 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 objective of this article was to monitor phase transformation in thiamine hydrochloride, from a nonstoichiometric hydrate (NSH) to a hemihydrate (HH), in stored tablets, prepared both by direct compression and wet granulation, and to relate the storage-induced phase transformation with changes in tablet microstruc...

journal_title：Journal of pharmaceutical sciences

authors： Chakravarty P,Suryanarayanan R,Govindarajan R

更新日期：2012-04-01 00:00:00

abstract：:Transcutaneous immunization is the administration of a vaccine on the skin to generate efficient systemic and mucosal immune responses against an antigen. In the present study, reconstituted hepatitis B surface antigen vesicles (HBsAg-REVs) integrated with monophosphoryl lipid A were prepared by the delipidation-recon...

journal_title：Journal of pharmaceutical sciences

authors： Kaurav M,Kumar R,Jain A,Pandey RS

更新日期：2019-11-01 00:00:00

abstract：:Some coated aspirin tablet formulations were evaluated by relating their properties to disintegrating force development patterns. The treatment of disintegrating force-time curves was effected using the Weibull distribution as proposed for dissolution. Such parameters as the maximum disintegrating force developed, the...

journal_title：Journal of pharmaceutical sciences

authors： Colombo P,Conte U,Caramella C,Geddo M,La Manna A

更新日期：1984-05-01 00:00:00

abstract：:A theory of charge, fluid-mass, and solute (including macromolecular) transport through porous media is applied to describe transport phenomena across the external layer of mammalian skin. Linear relationships are derived between transport fluxes and applied fields. These relationships introduce six effective transder...

journal_title：Journal of pharmaceutical sciences

authors： Edwards DA,Langer R

更新日期：1994-09-01 00:00:00

abstract：:Determining the aggregation propensity of protein-based biotherapeutics is an important step in the drug development process. Typically, a great deal of data collected over a large period of time is needed to estimate the aggregation propensity of biotherapeutics. Thus, candidates cannot be screened early on for aggre...

journal_title：Journal of pharmaceutical sciences

authors： Lauer TM,Agrawal NJ,Chennamsetty N,Egodage K,Helk B,Trout BL

更新日期：2012-01-01 00:00:00

abstract：:By using data from a sample of 1767 community pharmacies, a total cost function was estimated by a polynomial regression of total cost on output. The Cobb-Douglas production function was estimated by a multiple linear regression of natural logarithmic transformations of output on natural logarithmic transformation of ...

journal_title：Journal of pharmaceutical sciences

authors： Lohrisch D,Shull SC,Smith MC

更新日期：1976-02-01 00:00:00

abstract：:The development of an ocular dosage form containing xanthan gum and capable of interacting with mucin in the precorneal area is a challenge. The polymer concentration that can be applied is restricted because of the limited patient acceptability of highly viscous preparations. The precorneal mucin concentration is low...

journal_title：Journal of pharmaceutical sciences

authors： Ceulemans J,Vinckier I,Ludwig A

更新日期：2002-04-01 00:00:00

abstract：:Progesterone release from monolithic devices prepared from various copolymers of poly(hydroxyethyl methacrylate) and poly(methoxyethoxyethyl methacrylate) or poly(methoxyethyl methacrylate) was examined. In general, plots of the fraction of drug released versus (time)1/2 were linear during the early stages of drug rel...

journal_title：Journal of pharmaceutical sciences

authors： Song SZ,Cardinal JR,Kim SH,Kim SW

更新日期：1981-02-01 00:00:00

abstract：:Acrylic acid-esterified starch was produced by reacting starch with acrylic acid chloride. This reaction was rapid and easy to control. Introduction of acrylic groups into starch reduced the enzymatic degradability of starch (e.g., with 12 acrylic groups/100 glucose residues, approximately 75% of the degradation produ...

journal_title：Journal of pharmaceutical sciences

authors： Laakso T,Sjöholm I

更新日期：1987-12-01 00:00:00

abstract：:Caco-2 cell monolayers are widely used systems for predicting human intestinal absorption. This study was carried out to develop a quantitative structure-property relationship (QSPR) model of Caco-2 permeability using a novel genetic algorithm-based partial least squares (GA-PLS) method. The Caco-2 permeability data f...

journal_title：Journal of pharmaceutical sciences

authors： Yamashita F,Wanchana S,Hashida M

更新日期：2002-10-01 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：:A dermal penetration enhancer has been found which improves the dermal delivery of a wide variety of drugs and at the same time has a history of low toxicity for human dermal application. N,N-Diethyl-m-toluamide (I) has been shown to improve the delivery of many drugs through hairless mouse skin in an in vitro diffusi...

journal_title：Journal of pharmaceutical sciences

authors： Windheuser JJ,Haslam JL,Caldwell L,Shaffer RD

更新日期：1982-11-01 00:00:00

abstract：:Pyrimethamine, an antimalarial drug, was found to be able to inhibit both enzymes (DHFR-TS and PTR1) of the leishmanial folate pathway, although this effect in vivo appears only in relatively high concentrations. To reach the parasites inside macrophage cells, where they are sheltered, targeted drugs of pyrimethamine,...

journal_title：Journal of pharmaceutical sciences

authors： De Carvalho PB,Ramos DC,Cotrim PC,Ferreira EI

更新日期：2003-10-01 00:00:00

abstract：:A high-performance liquid chromatographic method was developed for the simultaneous determination of azobenzene, hydrazobenzene, and four other decomposition products in phenylbutazone injectable formulations. Separation was achieved on a C18 column, with 0.1 M Tris-citrate buffer (pH 5.25) and acetonitrile (52:48), a...

journal_title：Journal of pharmaceutical sciences

authors： Fabre H,Hussam-Eddine N,Mandrou B

更新日期：1984-12-01 00:00:00

abstract：:3-Fluoro-, 3-chloro-, and 3-bromocyclophosphamide were prepared from the reaction of trifluoromethylhypofluorite, sodium hypochlorite, and bromine with the anticancer drug cyclophosphamide. Treatment of cis- and trans-4-phenylcyclophosphamide and 5,6-benzocyclophosphamide with sodium hypochlorite afforded cis- and tra...

journal_title：Journal of pharmaceutical sciences

authors： Zon G,Ludeman SM,Ozkan G,Chandrasegaran S,Hammer CF,Dickerson R,Mizuta K,Egan W

更新日期：1983-06-01 00:00:00

abstract：:The objectives of this study were (i) to characterize the plasmid DNA encoding the chloramphenicol acetyltransferase reporter gene (pCAT) complexed with cationic liposomes (Lipofectin and LipofectACE) in terms of particle size and zeta potential, (ii) to compare pharmacokinetic characteristics, and (iii) to study the ...

journal_title：Journal of pharmaceutical sciences

authors： Mahato RI,Kawabata K,Nomura T,Takakura Y,Hashida M

更新日期：1995-11-01 00:00:00

abstract：:Ketoconazole and posaconazole are both Biopharmaceutics Classification System class 2 drugs (highly permeable, poorly soluble), are structurally similar, and are administered at the same doses. Nevertheless, the duodenal concentration profile and the magnitude of the positive food effect observed for these 2 drugs are...

journal_title：Journal of pharmaceutical sciences

authors： Cristofoletti R,Patel N,Dressman JB

更新日期：2016-09-01 00:00:00

abstract：:A rapid solubility-screening assay was developed with a focus on Biopharmaceutic Classification Scheme (BCS) class II drug solubility in animal and simulated human gastrointestinal (GI) fluids. The assay enables biologically promising drug leads to be evaluated for solubility limitations earlier in the drug developmen...

journal_title：Journal of pharmaceutical sciences

authors： Guo J,Elzinga PA,Hageman MJ,Herron JN

更新日期：2008-04-01 00:00:00

abstract：:Alkyl esters of ketorolac were synthesized as potential prodrugs for transdermal delivery and evaluated to determine the relationship between their skin permeation characteristics and their physicochemical properties. Solubility of the prodrugs in various vehicles was determined at room temperature while lipophilicity...

journal_title：Journal of pharmaceutical sciences

authors： Doh HJ,Cho WJ,Yong CS,Choi HG,Kim JS,Lee CH,Kim DD

更新日期：2003-05-01 00:00:00

abstract：:A new indole based chalcone molecule MOMIPP induced methuosis mediated cell death in gliobastoma and other cancer cell lines. But the drug was insoluble in water and had a very short plasma half-life. The purpose of this work was to develop a formulation that can provide sustained levels of MOMIPP in vivo. Initial stu...

journal_title：Journal of pharmaceutical sciences

authors： Oppong F,Li Z,Fakhrabadi EA,Raorane T,Giri PM,Liberatore MW,Sarver JG,Trabbic CJ,Hosier CE,Erhardt PW,Maltese WA,Nesamony J

更新日期：2020-09-01 00:00:00

abstract：:The aims of this study were to evaluate the pharmacokinetics of doripenem (Finibax®, Doribax®, S-4661), a parenteral carbapenem antibiotic, in pediatric patients based on concentrations of doripenem in plasma after administration of 20 mg/kg 2 or 3 times daily and to evaluate the dosing regimens by using Monte-Carlo p...

journal_title：Journal of pharmaceutical sciences

authors： Matsuo Y,Ishibashi T,Matsumoto S,Katsube T,Wajima T

更新日期：2019-09-01 00:00:00

abstract：:Repeated acetaminophen (AP) administration modulates intestinal P-glycoprotein (P-gp) expression. Whether AP can modulate P-gp activity in a short-term fashion is unknown. We investigated the acute effect of AP on rat intestinal P-gp activity in vivo and in vitro. In everted intestinal sacs, AP inhibited serosal-mucos...

journal_title：Journal of pharmaceutical sciences

authors： Novak A,Carpini GD,Ruiz ML,Luquita MG,Rubio MC,Mottino AD,Ghanem CI

更新日期：2013-10-01 00:00:00

abstract：:Accelerated stability studies (37 degrees, 47 degrees, and 57 degrees) were conducted on buffered aqueous solutions (pH 7.4, 8.4, and 9.4) of hydrocortisone in the presence of various molar ratios of D-fructose. First-order degradation was observed. Significant improvement in hydrocortisone stability was seen in those...

journal_title：Journal of pharmaceutical sciences

authors： Bansal NP,Holleran EM,Jarowski CI

更新日期：1983-09-01 00:00:00

abstract：:The capacity factors of several penicillins and cephalosporins, as well as those of 7-aminocephalosporanic acid, 6-aminopenicillanic acid, and 7-aminodeacetoxycephalosporanic acid, were determined at pH 2.5-7.5 with different methanol concentrations in the mobile phase. The influence of ionic strength on activity fact...

journal_title：Journal of pharmaceutical sciences

authors： Salto F,Prieto JG,Alemany MT

更新日期：1980-05-01 00:00:00

abstract：:The poor membrane permeability and oral bioavailability of the iron chelating agent deferoxamine (DFO) mesylate result from the low octanol/water partition coefficient and high aqueous solubility. With the ultimate aim to improve biomembrane permeability while retaining the iron-binding ability of DFO, a series of mor...

journal_title：Journal of pharmaceutical sciences

authors： Ihnat PM,Vennerstrom JL,Robinson DH

更新日期：2000-12-01 00:00:00

abstract：:A novel process based on solvent extraction was developed to produce drug-loaded polyanhydride microspheres for controlled-release applications. The technique consists of adding a chloroform solution of polyanhydride and drug into a stirred silicone oil phase containing suspended droplets of surfactant. No chemical re...

journal_title：Journal of pharmaceutical sciences

authors： Bindschaedler C,Leong K,Mathiowitz E,Langer R

更新日期：1988-08-01 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：:Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing metronidazole are reviewed. Metronidazole can be assigned to Biopharmaceutics Classification System Class I. Most BE studies that were identifi...

journal_title：Journal of pharmaceutical sciences

authors： Rediguieri CF,Porta V,G Nunes DS,Nunes TM,Junginger HE,Kopp S,Midha KK,Shah VP,Stavchansky S,Dressman JB,Barends DM

更新日期：2011-05-01 00:00:00