Abstract：
:Nanocrystals have emerged as a potential formulation strategy to eliminate the bioavailability-related problems by enhancing the initial dissolution rate and moderately super-saturating the thermodynamic solubility. This review contains an in-depth knowledge of, the processing method for formulation, an accurate quantitative assessment of the solubility and dissolution rates and their correlation to observe pharmacokinetic data. Poor aqueous solubility is considered the major hurdle in the development of pharmaceutical compounds. Because of a lack of understanding with regard to the change in the thermodynamic and kinetic properties (i.e., solubility and dissolution rate) upon nanosizing, we critically reviewed the literatures for solubility determination to understand the significance and accuracy of the implemented analytical method. In the latter part, we reviewed reports that have quantitatively studied the effect of the particle size and the surface area change on the initial dissolution rate enhancement using alternative approaches besides the sink condition dissolution. The lack of an apparent relationship between the dissolution rate enhancement and the observed bioavailability are discussed by reviewing the reported in vivo data on animal models along with the particle size and food effect. The review will provide comprehensive information to the pharmaceutical scientist in the area of nanoparticulate drug delivery.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Shah DA,Murdande SB,Dave RHdoi
10.1002/jps.24694subject
Has Abstractpub_date
2016-01-01 00:00:00pages
10-24issue
1eissn
0022-3549issn
1520-6017pii
S0022-3549(15)00159-8journal_volume
105pub_type
杂志文章,评审abstract：:A rapid approach for estimating the pK(a) value of small organic molecules was developed using vacuum-assisted multiplexed capillary electrophoresis (VAMCE) with ultraviolet detection. The VAMCE method employed a 96-capillary array, arranged in a standard 8 x 12 microtiter plate configuration, with each row of capilla...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.20275
更新日期：2005-03-01 00:00:00
abstract：:Jet-milling as the common way for micronization of drugs shows several disadvantages. Drug powder properties are decisive for pulmonary use because, besides a small particle size, a good deagglomeration behavior is required. In this study, several anti-inflammatory drugs [beclomethasone-17,21-dipropionate (BDP), betam...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10274
更新日期：2003-01-01 00:00:00
abstract：:Reactive high gravity controlled precipitation (HGCP) was carried out to produce salbutamol sulphate (SS) particles suitable for inhalation. Aqueous solutions of free salbutamol base and sulphuric acid were mixed intensely inside a HGCP reactor to form the particles. Spray drying was employed to obtain dry powders. Ph...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.21026
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doi：10.1016/j.xphs.2017.02.009
更新日期：2017-06-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600671046
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doi：10.1002/jps.2600680834
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pub_type： 杂志文章
doi：10.1016/j.xphs.2020.09.052
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.20239
更新日期：2005-01-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.23834
更新日期：2014-02-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js990053i
更新日期：1999-11-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600770408
更新日期：1988-04-01 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
pub_type： 杂志文章
doi：10.1002/jps.20400
更新日期：2005-08-01 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
pub_type： 杂志文章
doi：10.1002/jps.2600790602
更新日期：1990-06-01 00:00:00
abstract：:Fluconazole concentrations in biological fluids were determined by high-performance gas chromatography. A simple extraction procedure with chloroform, under basic conditions and after the addition of UK-47,265 as the internal standard and with no evaporation stage, was carried out prior to analysis. A solid injector a...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600770615
更新日期：1988-06-01 00:00:00
abstract：:There is a recognized need for new approaches to understand unit operations with pharmaceutical relevance. A method for analyzing complex interactions in experimental data is introduced. Higher-order interactions do exist between process parameters, which complicate the interpretation of experimental results. In this ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21565
更新日期：2009-05-01 00:00:00
abstract：:Lysosomes are acidic intracellular organelles that can extensively sequester basic lipophilic drugs due to pH and membrane partitioning, and therefore may significantly influence subcellular drug concentrations. Current in vitro methods for lysosomal drug sequestration evaluation typically lack the ability to accurate...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2020.05.026
更新日期：2020-09-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2018.10.056
更新日期：2019-01-01 00:00:00
abstract：:Emodin, a natural anthraquinone polyphenol, has been reported to possess promising in vitro antioxidation, anticancer and anti-inflammatory activities. Whether the in vitro bioactivities can predict in vivo effects remained an unanswered question without understanding emodin pharmacokinetics in animals. To fill this b...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21978
更新日期：2010-04-01 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
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更新日期：2011-05-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600830419
更新日期：1994-04-01 00:00:00
abstract：:The objective of this study was to establish the optimal blood concentrations of the potent P-glycoprotein (P-gp) inhibitor GF120918 (Elacridar) required to achieve maximal knockout of this efflux transporter in the blood-brain barrier (BBB) of mice, rats, and guinea pigs. Genetic mdr1a/b(-/-) knockout mice and "chemi...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.20658
更新日期：2006-09-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js980048z
更新日期：1998-09-01 00:00:00
abstract：:Modifications of antibacterial activity have been demonstrated using combinations of two antibacterials from trimethoprim, sulfonamides (sulfadiazine, sulfamerazine, and silver sulfadiazine), silver nitrate, and dibromopropamidine isethionate, either formulated in a cream base or dissolved in peptone water. The creams...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600800912
更新日期：1991-09-01 00:00:00
abstract：:The physical stability of an immunoglobulin G4 monoclonal antibody (mAb) upon dilution into intravenous (i.v.) bags containing 0.9% saline was examined. Soluble aggregates and subvisible particles were observed by size-exclusion high-performance liquid chromatography (SE-HPLC) and light obscuration when formulated wit...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23224
更新日期：2012-10-01 00:00:00
abstract：:The objective of the current study was to evaluate the performance of Raman and near-infrared (NIR) techniques combined with chemometrics in characterizing the critical quality attributes of brompheniramine (BP)-tannate complexes. Seven complexes were prepared and evaluated for chemical interactions, solubilities, dis...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.23030
更新日期：2012-04-01 00:00:00
abstract：:Alzheimer's disease (AD) is historically difficult to treat, in part because of the inaccessible nature of brain pathology. Amyloid beta and tau proteins drive pathology by forming toxic oligomers that eventually deposit as insoluble amyloid plaques and neurofibrillary tangles. Recent clinical studies suggest that eff...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2019.10.024
更新日期：2020-01-01 00:00:00
abstract：:Vehicle effects may be caused by thermodynamic effects and by specific (penetration enhancing) effects. To investigate the effects of various lipophilic vehicles on drug penetration, an in vivo permeability study was conducted with methyl nicotinate as the model drug. The drug was dissolved in the respective vehicles ...
journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章
doi：10.1002/jps.2600840214
更新日期：1995-02-01 00:00:00
abstract：:Because the ionized species is more polar than its un-ionized counterpart, it is often assumed that the ionized species of the drug does not make a meaningful contribution to solubilization by either cosolvents or surfactants. This report extends previous studies on solubilization of the ionic species by a combination...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js980433o
更新日期：1999-05-01 00:00:00
abstract：:The impact of intestinal conjugative metabolism on oral bioavailability was assessed by sequential and simultaneous analyses of the reported data in humans. The data were retrieved from reports on drugs that are metabolized by sulfate conjugation, and the organ availabilities affecting oral bioavailability were differ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20269
更新日期：2005-03-01 00:00:00
abstract：:In vitro studies on the photodecomposition of uric acid in the presence of the monosodium salt of riboflavin 5'-phosphate in buffers at various pH values, in methanol, and in human plasma are reported. The decomposition rate increased with increasing pH and was independent of solvent or buffer species. The mechanism a...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600661115
更新日期：1977-11-01 00:00:00
