Abstract：
:The insidious nature of Zika virus (ZIKV) infections can have a devastating consequence for fetal development. Recent reports have highlighted that chloroquine (CQ) is capable of inhibiting ZIKV endocytosis in brain cells. We applied pharmacokinetic modeling to develop a predictive model for CQ exposure to identify an optimal maternal/fetal dosing regimen to prevent ZIKV endocytosis in brain cells. Model validation used 13 nonpregnancy and 3 pregnancy clinical studies, and a therapeutic CQ plasma window of 0.3-2 μM was derived. Dosing regimens used in rheumatoid arthritis, systemic lupus erythematosus, and malaria were assessed for their ability to target this window. Dosing regimen identified that weekly doses used in malaria were not sufficient to reach the lower therapeutic window; however, daily doses of 150 mg achieved this therapeutic window. The impact of gestational age was further assessed and culminated in a final proposed regimen of 600 mg on day 1, 300 mg on day 2 and 3, and 150 mg thereafter until the end of trimester 2, which resulted in maintaining 65% and 94% of subjects with a trough plasma concentration above the lower therapeutic window on day 6 and at term, respectively.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Olafuyi O,Badhan RKSdoi
10.1016/j.xphs.2018.10.056subject
Has Abstractpub_date
2019-01-01 00:00:00pages
661-673issue
1eissn
0022-3549issn
1520-6017pii
S0022-3549(18)30689-0journal_volume
108pub_type
杂志文章abstract：:The adsorption of quinidine onto kaolin was studied as a function of pH in aqueous solutions in which the ionic strength was adjusted to 0.1. The interaction of quinidine with pectin also was investigated in water and in phosphate buffer; the buffer pH and ionic strength were adjusted to 6.5 and 0.1, respectively. The...
journal_title：Journal of pharmaceutical sciences
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600690329
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600750811
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journal_title：Journal of pharmaceutical sciences
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doi：10.1021/js950285r
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journal_title：Journal of pharmaceutical sciences
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更新日期：1992-09-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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更新日期：2005-01-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600740329
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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
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.1044
更新日期：2001-07-01 00:00:00
abstract：:A comprehensive model is developed to describe the swelling/dissolution behaviors and drug release from hydrophilic matrices. The major thrust of this model is to employ an important physical property of the polymer, the polymer disentanglement concentration, rho p,dis, the polymer concentration below which polymer ch...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600841214
更新日期：1995-12-01 00:00:00
abstract：:A high-performance liquid chromatographic method has been developed for the simultaneous determination of azobenzene and hydrazobenzene in phenylbutazone and sulfinpyrazone raw materials and formulations. The drug raw material or formulation is shaken with 1N NaOH and n-hexane and centrifuged. The n-hexane layer is in...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600721032
更新日期：1983-10-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600741018
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600831203
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600640909
更新日期：1975-09-01 00:00:00
abstract：:Conventionally, it is believed that the fraction of orally administered drugs absorbed from the intestine (Fa) and intestinal availability (Fg) are independently determined by the apical membrane permeation and intestinal metabolism, respectively. However, the validity of this belief has not been well discussed, and F...
journal_title：Journal of pharmaceutical sciences
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更新日期：2016-02-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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更新日期：2009-12-01 00:00:00
abstract：:One of the challenges with predictive modeling is how to quantify the reliability of the models' predictions on new objects. In this work we give an introduction to conformal prediction, a framework that sits on top of traditional machine learning algorithms and which outputs valid confidence estimates to predictions ...
journal_title：Journal of pharmaceutical sciences
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doi：10.1016/j.xphs.2020.09.055
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abstract：:Literature data relevant to the decision to waive in vivo bioequivalence testing for the approval of generic immediate release solid oral dosage forms of proguanil hydrochloride are reviewed. To elucidate the Biopharmaceutics Classification System (BCS) classification, experimental solubility and dissolution studies w...
journal_title：Journal of pharmaceutical sciences
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更新日期：2018-07-01 00:00:00
abstract：:Oxidation of 7,8-dimethoxy-1,2,3,4-tetrahydroisoquinoline with potassium permanganate in acetone afforded 7,8-dimethoxy-3,4-dihydroisoquinoline as the primary product. Hence, oxidation of the appropriate secondary nonphenolic 7,8-dioxygenated tetrahydroisoquinoline alkaloid is thus a facile method for the generation o...
journal_title：Journal of pharmaceutical sciences
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更新日期：1984-11-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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更新日期：2021-01-01 00:00:00
abstract：:The use of enzymes as therapeutics is very promising because of their catalytic activity and specificity. However, intracellular delivery of active enzymes is challenging due to their low stability and large size. The production of protein-enzyme nanoparticles was investigated with the goal of developing a protein car...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.23974
更新日期：2014-06-01 00:00:00
