High-Throughput Melanin-Binding Affinity and In Silico Methods to Aid in the Prediction of Drug Exposure in Ocular Tissue.

abstract：:Transformation of polymorph I of clopidogrel hydrogen sulfate (CHS) to polymorph II of CHS during the crystallization was monitored by using in situ measurement of ultrasonic velocity. Drowning-out crystallization using methanol as a solvent and isopropyl alcohol as nonsolvent was carried out. The polymorphs were iden...

journal_title：Journal of pharmaceutical sciences

authors： Kim HJ,Kim KJ

更新日期：2008-10-01 00:00:00

abstract：:Elucidation of the most stable form of an active pharmaceutical ingredient (API) is a critical step in the development process. Polymorph screening for an API with a complex polymorphic profile can present a significant challenge. The presented case illustrates an extensively polymorphic compound with an additional pr...

journal_title：Journal of pharmaceutical sciences

authors： Campeta AM,Chekal BP,Abramov YA,Meenan PA,Henson MJ,Shi B,Singer RA,Horspool KR

更新日期：2010-09-01 00:00:00

abstract：:The purpose of this study was to develop a nanocarrier system for codelivery of paclitaxel (PTX) and piperlongumine (PL) and investigate the therapeutic potential of improving efficacy and reducing toxicity. PTX and PL were formulated into poly lactic-co-glycolic acid and D-α-tocopheryl polyethylene glycol succinate v...

journal_title：Journal of pharmaceutical sciences

authors： Liu Q,Zhao D,Zhu X,Chen H,Yang Y,Xu J,Zhang Q,Fan A,Li N,Guo C,Kong Y,Lu Y,Chen X

更新日期：2017-10-01 00:00:00

abstract：:Complex dosing regimens simulated in the literature using a universal dosing regimen were calculated with a general dosing program developed using the program CONSAM. The program provides a rapid method of calculating nonuniform dosing regimens for up to n = 3 compartments for any linear model. Subject data can also b...

journal_title：Journal of pharmaceutical sciences

authors： Jackson AJ,Zech LA

更新日期：1991-04-01 00:00:00

abstract：:Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most frequently used drugs in the world, primarily for symptoms associated with osteoarthritis and other chronic musculoskeletal conditions. However, adverse effects caused by oral administration, such as local or systemic disturbance in the gastrointestinal ...

journal_title：Journal of pharmaceutical sciences

authors： Cheng Y,Man N,Xu T,Fu R,Wang X,Wang X,Wen L

更新日期：2007-03-01 00:00:00

abstract：:Biopharmaceuticals represent an important and growing class of medicines. Immunogenic responses to biopharmaceuticals in patients can sometimes result in reduced safety and efficacy. Although multiple factors are known to influence immunogenicity, our understanding of the complex underlying mechanisms remains imperfec...

journal_title：Journal of pharmaceutical sciences

authors： Bee JS,Goletz TJ,Ragheb JA

更新日期：2012-10-01 00:00:00

abstract：:Chlorthalidone was analyzed in the concentration range of 0.1-3.0 microgram/ml with a precision of +/- 0.05 microgram/ml. Chlorthalidone inhibition of the enzymatic hydrolysis rate of p-nitrophenyl acetate by bovine erythrocyte carbonic anhydrase was used as a basis for the determination. The amount of p-nitrophenol f...

journal_title：Journal of pharmaceutical sciences

authors： Johnston MM,Li H,Mufson D

更新日期：1977-12-01 00:00:00

abstract：:Nanospheres with D,L-lactide/glycolide copolymer (PLGA) were prepared as a biodegradable and biocompatible polymeric carrier for peptide drugs by a novel spontaneous emulsification solvent diffusion method. Nafarelin acetate (NA), a luteinizing hormone-releasing hormone analogue, was employed as a model peptide drug t...

journal_title：Journal of pharmaceutical sciences

authors： Niwa T,Takeuchi H,Hino T,Kunou N,Kawashima Y

更新日期：1994-05-01 00:00:00

abstract：:The antifungal drug, 5-fluorocytosine (FC), is marketed as a capsule (250 or 500 mg strength) instead of the preferred tablet dosage form. Through systematic characterization of solid-state properties, including mechanical properties, we identify tabletability and poor physical stability of FC as the problems that lik...

journal_title：Journal of pharmaceutical sciences

authors： Perumalla SR,Sun CC

更新日期：2014-04-01 00:00:00

abstract：:A roadmap for the selection of a pharmaceutical salt form for a development candidate is presented. The free base of the candidate did not have sufficient chemical stability for development. The initially selected salt form turned out to be undevelopable because it was unstable during scale-up synthesis and storage. T...

journal_title：Journal of pharmaceutical sciences

authors： He Y,Orton E,Yang D

更新日期：2018-01-01 00:00:00

abstract：:Treatment of systemic diseases by means of the inhalation route is hampered by uncertainties of the drug dose applied by inhalation. In this study, the hypothesis was tested that by standardization of the breathing maneuver used for inhalation, the interindividual variability of the dose deposited intrathoracically ca...

journal_title：Journal of pharmaceutical sciences

authors： Brand P,Friemel I,Meyer T,Schulz H,Heyder J,Häubetainger K

更新日期：2000-06-01 00:00:00

abstract：:A Bayesian approach was developed to determine an amikacin dosage regimen to achieve the desired plasma concentrations for each patient. Statistical characteristics of pharmacokinetic parameters were first evaluated in a group of patients (reference population), which when combined with three individual plasma concent...

journal_title：Journal of pharmaceutical sciences

authors： Garraffo R,Iliadis A,Cano JP,Dellamonica P,Lapalus P

更新日期：1989-09-01 00:00:00

abstract：:While the number of clinical trials has continued to grow by about 20% in the past six months, no corresponding growth in product approval by the food and drug administration is seen or anticipated in the near future. Late-stage clinical failures due to lack of efficacy or toxicity continues to be a challenge. The opt...

journal_title：Journal of pharmaceutical sciences

authors： Ho RJ,Chien JY

更新日期：2009-06-01 00:00:00

abstract：:A gas chromatographic-mass spectrometric method was developed for the stereoselective quantification of threo-methylphenidate (MPD) and its metabolite, ritalinic acid (RA), in plasma or urine. The plasma concentrations of (+)-MPD after oral administration of two 10-mg conventional tablets containing racemic MPD.HCl or...

journal_title：Journal of pharmaceutical sciences

authors： Aoyama T,Kotaki H,Honda Y,Nakagawa F

更新日期：1990-06-01 00:00:00

abstract：:A procedure is described for the analysis of urushiol content of pharmaceutical preparations containing extracts of poison ivy (Toxicodendron radicans) and poison oak (T. diversilobum) in vegetable oils. The procedure involves extraction of the urushiols from the oily solutions using 90% methanol in water followed by ...

journal_title：Journal of pharmaceutical sciences

authors： Elsohly MA,Turner CE

更新日期：1980-05-01 00:00:00

abstract：:The concept of cosolvent exclusion was developed by a group of Timasheff's laboratory in 1970-1990 and is currently used widely to explain the effects of a variety of cosolvents on the stability and solubility of macromolecules. Not surprisingly, these concepts have had substantial influence in the fields of formulati...

journal_title：Journal of pharmaceutical sciences

authors： Arakawa T,Gagnon P

更新日期：2018-09-01 00:00:00

abstract：:The new concept developed in this study is the design of poly(ethylene glycol) (PEG)-coated biodegradable nanoparticles coupled to folic acid to target the folate-binding protein; this molecule is the soluble form of the folate receptor that is overexpressed on the surface of many tumoral cells. For this purpose, a no...

journal_title：Journal of pharmaceutical sciences

authors： Stella B,Arpicco S,Peracchia MT,Desmaële D,Hoebeke J,Renoir M,D'Angelo J,Cattel L,Couvreur P

更新日期：2000-11-01 00:00:00

abstract：:For development and optimization of protein formulation sensitive analytical tools are required to follow both aggregation and changes in protein structure. The latter can be seen as the beginning of physical instability leading to aggregation. The focus of this work laid on the development of a novel analysis simulta...

journal_title：Journal of pharmaceutical sciences

authors： Printz M,Friess W

更新日期：2012-02-01 00:00:00

abstract：:The synthesis of the diethyl analog of neostigmine, its preliminary pharmacology, and its use as an internal standard for the GLC assay of neostigmine are described. Both the diethyl analog and neostigmine undergo thermal demethylation in the injection port. The column selected produced satisfactory resolution and sho...

journal_title：Journal of pharmaceutical sciences

authors： Ward HE Jr,Freeman JJ,Sowell JW,Kosh JW

更新日期：1981-04-01 00:00:00

abstract：:The wettability of the (001), (100), and (011) crystallographic facets of macroscopic aspirin crystals has been experimentally investigated using a sessile drop contact angle (theta) method. theta for a nonpolar liquid was very similar for all three facets, though significant theta differences were observed for three ...

journal_title：Journal of pharmaceutical sciences

authors： Heng JY,Bismarck A,Lee AF,Wilson K,Williams DR

更新日期：2007-08-01 00:00:00

abstract：:The estimation of aqueous solubilities of organic nonelectrolytes by the General Solubility Equation (GSE) as proposed by Valvani and Yalkowsky (1980) is used in this study. The data and assumptions on which the GSE are based are reevaluated, and the equation is revised. The revised GSE is validated on a set of 580 ph...

journal_title：Journal of pharmaceutical sciences

authors： Jain N,Yalkowsky SH

更新日期：2001-02-01 00:00:00

abstract：:The antimalarial endoperoxides, such as artemisinin, are postulated to exert their potent parasiticidal activity via the formation of reactive intermediates in the iron-rich infected erythrocyte. The in vitro chemical reaction profile of putative endoperoxide antimalarials and ferrous iron is often qualitatively used ...

journal_title：Journal of pharmaceutical sciences

authors： Creek DJ,Chiu FC,Prankerd RJ,Charman SA,Charman WN

更新日期：2005-08-01 00:00:00

abstract：:The intrinsic absorption of salbutamol in different intestinal segments of the rat was measured and related with the corresponding intestinal P-glycoprotein (P-gp) expression levels. The apparent absorption rate constants (k(a), h(-1)) observed in each fraction by means of the "in situ" rat gut absorption method after...

journal_title：Journal of pharmaceutical sciences

authors： Valenzuela B,Nácher A,Ruiz-Carretero P,Martín-Villodre A,López-Carballo G,Barettino D

更新日期：2004-06-01 00:00:00

abstract：:In this work, a novel risk-based methodology for lot release is proposed. Its objective is to assess the risk that a lot declared to have passed truly meets product specifications. The methodology consists of 3 parts: adaptive sample size determination, estimation of the probability that the product was within specifi...

journal_title：Journal of pharmaceutical sciences

authors： Mockus L,Reklaitis G,Morris K,LeBlond D

更新日期：2020-02-01 00:00:00

abstract：:A novel method is described for the preparation of sterile and pyrogen-free submicron liposomes of narrow size distribution. The method is based on the formation of a homogeneous dispersion of lipids in water-soluble carrier materials. To obtain the lipid-containing solid dispersion, liposome-forming lipids and water-...

journal_title：Journal of pharmaceutical sciences

authors： Li C,Deng Y

更新日期：2004-06-01 00:00:00

abstract：:High protein concentration formulations are required for low-volume administration of therapeutic antibodies targeted for subcutaneous, self-administration by patients. Ultra-high concentrations (≥150 mg/mL) can lead to dramatically increased solution viscosities, which in turn can lead to stability, manufacturing, an...

journal_title：Journal of pharmaceutical sciences

authors： Whitaker N,Xiong J,Pace SE,Kumar V,Middaugh CR,Joshi SB,Volkin DB

更新日期：2017-11-01 00:00:00

abstract：:Povidone-iodine USP was tested for mutagenicity in mice by the dominant lethal assay or micronucleus test and in Chinese hamsters by the bone marrow test. None of the three tests revealed any evidence of mutagenic effect. ...

journal_title：Journal of pharmaceutical sciences

authors： Merkle J,Zeller H

更新日期：1979-01-01 00:00:00

abstract：:(+-)-Carbovir [(+-)-9-[4 alpha-(hydroxymethyl)-cyclopent-2-ene-1 alpha-yl]guanine; NSC 614846] is a novel carbocyclic nucleoside analogue which has been shown to be a potent and selective inhibitor of HIV in vitro. As part of an effort to develop a parenteral formulation for subsequent clinical and toxicological evalu...

journal_title：Journal of pharmaceutical sciences

authors： Anderson BD,Chiang CY

更新日期：1990-09-01 00:00:00

abstract：:Tryptophan (Trp) oxidation in proteins leads to a number of events, including changes in color, higher order structure (HOS), and biological activity. We describe here a number of new findings through a comprehensive characterization of 6 monoclonal antibodies (mAbs) following selective oxidation of Trp residues by 2,...

journal_title：Journal of pharmaceutical sciences

authors： Barnett GV,Balakrishnan G,Chennamsetty N,Hoffman L,Bongers J,Tao L,Huang Y,Slaney T,Das TK,Leone A,Kar SR

更新日期：2019-06-01 00:00:00

abstract：:The in vitro binding of warfarin by human serum albumin was studied at various temperatures and at pH 7.4 by a frontal gel filtration technique. The results can be best described in terms of a two class-of-binding site model, in which the numbers of primary and secondary sites are constrained to the average values for...

journal_title：Journal of pharmaceutical sciences

authors： Oester YT,Keresztes-Nagy S,Mais RF,Becktel J,Zaroslinski JF

更新日期：1976-11-01 00:00:00