High Sensitivity Detection of a Solubility Limiting Surface Transformation of Drug Particles by DNP SENS.


:We investigate the presence of a surface species for the active pharmaceutical ingredient (API) AZD9496 with dynamic nuclear polarization surface enhanced nuclear spectroscopy (DNP SENS). We show that using DNP we can elucidate the presence of an amorphous form of the API at the surface of crystalline particles of the salt form. The amorphous form of the API has distinguishable 13C chemical shifts when compared to the salt form under various acidic conditions. The predominant form in frozen particles of AZD9496 is the salt, and we provide evidence to suggest that the amorphous layer at the surface is mainly made up of the dissociated free form.


J Pharm Sci


Viger-Gravel J,Pinon AC,Björgvinsdóttir S,Skantze U,Svensk Ankarberg A,Von Corswant C,Schantz S,Emsley L




Has Abstract


2021-01-05 00:00:00








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    journal_title:Journal of pharmaceutical sciences

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    authors: Kadir R,Stempler D,Liron Z,Cohen S

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  • Effect of dispersion on the coloring properties of aluminum dye lakes.

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    authors: Wou LL,Mulley BA

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    authors: Block JH,Levine HL,Ayres JW

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    abstract::Two high-performance liquid chromatographic (HPLC) assay procedures were developed for the determination of salicylamide and its metabolites in serum, urine, and saliva. One method involves reverse-phase ion-pair chromatography and UV detection, and is used to determine salicylamide, salicylamide glucuronide, and sali...

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    authors: Morris ME,Levy G

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    abstract::A general spectroscopic method is described that might be applied to validating amino acid sequences in peptides and protein fragments with a view to it becoming a routine procedure with which to characterize biotechnology drug products. The tripeptides are the L-enantiomers of GGA, GGH, GGI, GGL, GGF, GHG, LGG, and Y...

    journal_title:Journal of pharmaceutical sciences

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    authors: Purdie N,Province DW,Johnson EA

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    abstract::Dynamic imaging analysis instruments are used for sizing particles of different types that might appear in a biopharmaceutical. These instruments are calibrated using polystyrene latex microspheres in water, which is a significantly different system than the typical particles imaged in a formulation. We show how the i...

    journal_title:Journal of pharmaceutical sciences

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    authors: Cavicchi RE,Ripple DC,Bioprocess Measurements Group.

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    authors: Torchilin VP,Trubetskoy VS,Whiteman KR,Caliceti P,Ferruti P,Veronese FM

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    abstract::Aqueous wet massing of stable anhydrous theophylline (A) with polyvinylpyrrolidone (PVP) resulted in its complete transformation to theophylline monohydrate (M). Drying at 45 degrees C, resulted in the formation of metastable anhydrous theophylline (A*) which then transformed to A. PVP, a known crystallization inhibit...

    journal_title:Journal of pharmaceutical sciences

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    authors: Tantry JS,Tank J,Suryanarayanan R

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    journal_title:Journal of pharmaceutical sciences

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    authors: Wells-Knecht KJ,Dunn D

    更新日期:2019-09-01 00:00:00

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    journal_title:Journal of pharmaceutical sciences

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    authors: Tagami S,Maeda H

    更新日期:1983-09-01 00:00:00

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    abstract::The skin penetration of 10 nonsteroidal antiinflammatory drugs (NSAIDs) was investigated after application in the lipophilic vehicle light mineral oil. The skin permeabilities and maximum fluxes, which were calculated from the concentration decreases of the applied solutions in the steady state phases, were correlated...

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    authors: Wenkers BP,Lippold BC

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    journal_title:Journal of pharmaceutical sciences

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    authors: Konishi M,Hashimoto H

    更新日期:1990-05-01 00:00:00

  • Effect of micellization on rate of cupric-ion-promoted hydrolysis of dicarboxylic acid hemiesters.

    abstract::The effect of micellar sodium lauryl sulfate on the rate of cupric-ion-promoted hydrolysis of some dicarboxylic acid hemiesters was investigated at pH 5, ionic strength 0.1 M, and 40, 45, and 50 degrees. The rate of cupric-ion-promoted hydrolysis of sodium n-decyloxalate in the micellar phase is about 50 times as fast...

    journal_title:Journal of pharmaceutical sciences

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    authors: Ong JT,Kostenbauder HB

    更新日期:1976-12-01 00:00:00

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    abstract::The solvent-free melt electrospinning (MES) method was developed to prepare a drug delivery system with fast release of carvedilol (CAR), a drug with poor water solubility. To the authors knowledge, this is the first report for preparing drug-loaded melt electrospun fibers. Cationic methacrylate copolymer of Eudragit®...

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    authors: Nagy ZK,Balogh A,Drávavölgyi G,Ferguson J,Pataki H,Vajna B,Marosi G

    更新日期:2013-02-01 00:00:00

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    abstract::The delivery of active agents to the skin by liposome carriers is an interdisciplinary topic of great interest today. Data accumulated over the last decade strongly point to important advantages of these drug delivery systems. A symposium devoted to classic and new approaches in the use of liposomal systems was organi...

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    authors: Touitou E,Junginger HE,Weiner ND,Nagai T,Mezei M

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    abstract::Binding of (+)- and (-)-isomers and the racemate of sodium 2[6-(4-chlorophenoxy)-hexyl]-oxiran-2-carboxylate dihydrat (etomoxir) to the human serum albumin (HSA) was studied by the gel filtration method. The experimental results are presented graphically using the method of Scatchard. Measurements revealed the followi...

    journal_title:Journal of pharmaceutical sciences

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    authors: Vestemar V,Medic-Saric M,Rendic S

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    abstract::New dihydropyridine in equilibrium pyridinium salt-type redox carrier systems were developed in which the drug is linked via the ring nitrogen atom of nicotinamide. The rate of oxidation of the dihydropyridine forms, and thus the overall and brain-specific distribution of the corresponding 3-carbamoyl-1-carbamoylalkyl...

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    authors: Bodor N,AbdelAlim AM

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    abstract::Most of the global healthcare issues facing us--from expanding access to care, to providing medical and dental care in the aftermath of disasters--are far too complex for any single sector to successfully solve. Industry, the healthcare profession, government, academia and non-governmental organizations (NGOs) are all...

    journal_title:Journal of pharmaceutical sciences

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    authors: Bergman SM

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    authors: Knopp MM,Olesen NE,Holm P,Löbmann K,Holm R,Langguth P,Rades T

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    authors: Pedersen PV

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    authors: Okafor-Muo OL,Hassanin H,Kayyali R,ElShaer A

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    pub_type: 杂志文章


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

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    authors: Borchard RE,Welborn ME,Wiekhorst WB,Wilson DW,Hansen LG

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    abstract::The quassinoids bruceantin, brucein D, brucein E, bruceoside A, and brusatol significantly inhibited P-388 lymphocytic leukemic cell RNA and protein synthesis in tissue culture. However, DNA synthesis inhibition seemed to correlate more directly with the anti-neoplastic activity of these compounds in the in vivo P-338...

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


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