Abstract：
:The aim of this study was to investigate the role of porosity on the compression behavior and tablet tensile strength for granules produced by a dry granulation procedure. Microcrystalline cellulose was used as a typical pharmaceutical excipient and a comparison was made with the effect of granule porosity on the compression behavior and tablet tensile strength of wet-processed granules of the same composition. Both the wet and dry granulation process caused a loss in compactibility of the material that was controlled by the granule porosity up to a critical point of porosity and friability. Above this threshold value of porosity, the granules nearly collapsed completely into primary particles during compression. In these cases, the micro-structure and tensile strength of the formed tablets resembled that of tablets formed from the original ungranulated powder.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Nordström J,Alderborn Gdoi
10.1002/jps.24439subject
Has Abstractpub_date
2015-06-01 00:00:00pages
2029-2039issue
6eissn
0022-3549issn
1520-6017pii
S0022-3549(15)30090-3journal_volume
104pub_type
杂志文章abstract：:The present work describes the development of a novel formulation of amorphous agomelatine (AGM) that exhibits enhanced in vitro dissolution rate and bioavailability, as well as improved storage stability. AGM was loaded on a mixture of microcrystalline cellulose with a high specific surface area excipient, namely col...
journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1016/j.xphs.2017.09.017
更新日期：2018-01-01 00:00:00
abstract：:Although PEGylation of biologics is currently the gold standard for half-life extension, the technology has a number of limitations, most importantly the non-biodegradability of PEG and the extremely high viscosity at high concentrations. HESylation is a promising alternative based on coupling to the biodegradable pol...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24253
更新日期：2015-02-01 00:00:00
abstract：:A number of biopharmaceuticals are available as lyophilized formulations along with a prefilled syringe (PFS) containing water for injection (WFI). Submicron- and micron-size droplets of lubricating silicone oil (SO) applied to the inner surface of the PFS barrel might migrate into the WFI, to which protein pharmaceut...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2019.02.002
更新日期：2019-07-01 00:00:00
abstract：:Angiogenesis, the sprouting of capillaries from preexisting ones, is essential for the sustained growth of solid tumors. In this study, we used SU5416, a hydrophobic molecule with potent tyrosine kinase inhibitor of type 2 receptor for vascular endothelial growth factor (VEGF), as PEGylated emulsion (SU5416-PE), and e...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24071
更新日期：2014-08-01 00:00:00
abstract：:The penetration of benzyl alcohol (BA) through split-thickness cadaver skin was measured in nonoccluded Franz cells placed in a fume hood. BA, dissolved in a small volume of ethanol and spiked with (14)C radiolabel, was applied to skin at nine doses ranging from 0.9 to 10600 microg/cm(2). The percentage of radioactivi...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20513
更新日期：2006-02-01 00:00:00
abstract：:The recombinant fusion proteins hybrid 1 [H1 (Ag85B-ESAT-6)] and hybrid 56 [H56 (Ag85B-ESAT-6-Rv2660c)] derived from Mycobacterium tuberculosis are promising antigens for subunit vaccines against tuberculosis. Both antigens are early batches of antigens to be enrolled in human clinical trials and it is therefore impor...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23669
更新日期：2013-10-01 00:00:00
abstract：:DNA co-condensates were formed by reacting [125I]DNA with an admixture of a high-mannose glycopeptide (Man9-CWK(18)) and either of two poly(ethylene glycol) peptides (PEG-VS-CWK(18) or PEG-SS-CWK(18)) followed by cross-linking with 6-50 mol equiv of glutaraldehyde. [125I]DNA co-condensates were administered intravenou...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.1152
更新日期：2001-12-01 00:00:00
abstract：:The molecular connectivity indexes of various aliphatic alcohols, ketones, ethers, and esters were used to describe structural features influencing chromatographic retention indexes. Good correlations were obtained within chemical classes for a particular stationary phase. ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600680143
更新日期：1979-01-01 00:00:00
abstract：:The correlation between dynamic surface properties of drug molecules and drug absorption in two common in vitro models of the intestinal wall (Caco-2 monolayers and rat intestinal segments) has been investigated. A homologous series of beta-adrenoreceptor antagonists were used as model compounds. Dynamic molecular sur...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js950285r
更新日期：1996-01-01 00:00:00
abstract：:The aim of this study was to characterize the metabolic pathways of 2-methoxyestradiol (2ME2), an investigational anticancer drug. In vitro metabolism studies were performed by incubation of 2ME2 with human liver microsomes under various conditions and metabolite identification was performed using liquid chromatograph...
journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章
doi：10.1002/jps.20837
更新日期：2007-07-01 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
pub_type： 杂志文章
doi：10.1002/jps.21041
更新日期：2008-04-01 00:00:00
abstract：:The extent of formation of solasodiene from solasodine upon treatment with hydrochloric acid under various conditions was determined. The diene formed was assayed by using the characteristic extinction at 236 nm. Diene formation was effected by the acid concentration and the boiling point of the solvent used. Optimal ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670839
更新日期：1978-08-01 00:00:00
abstract：:The present studies were undertaken to describe the dynamic nature of the degradation and absorption of insulin in the subcutaneous injection site and to develop agents which would stabilize this dosage form. [125I]Insulin with 0.2-U/kg of unlabeled insulin in 10 microliters of aqueous solution was injected subcutaneo...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600720428
更新日期：1983-04-01 00:00:00
abstract：:One of the most important challenges for pharmaceutical and cosmetic industries is solubilization and preservation of their active ingredients. Therefore, most of these formulations contain irritant chemical additives to improve their shelf-life and the solubility of hydrophobic ingredients. An interesting alternative...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2019.02.010
更新日期：2019-07-01 00:00:00
abstract：:(6R,7R)-7-[2-(5-Amino-1,2,4-thiadiazol-3-yl)-(Z)-2-methoxy- iminoacetamid]-3- [(4-carbamoyl-1-quinuclidinio)methyl]-8-oxo-5-thia-1-azabicyclo [4,2,0]oct-2-ene-2-carboxylate (1; E1040) was isolated as alpha-(decahydrate), beta-(pentahydrate), and gamma-form (anhydrate) crystals and the X-ray amorphous form. The relatio...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600781103
更新日期：1989-11-01 00:00:00
abstract：:A series of gem-cichlorocyclopropyl and cyclopropyl analogs of stilbene congeners was synthesized and examined for estrogenic and antiestrogenic activity using the uterotropic assay in the immature mouse. The relative receptor affinity in vitro was determined by measuring [3H]estradiol displacement from the rat uterin...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600711012
更新日期：1982-10-01 00:00:00
abstract：:The physical state of a dosage form, crystalline versus amorphous, is critical in determining its solid-state physical and chemical properties. This minireview describes the physics associated with the preparation and storage of amorphous solids including a review of the common theories of the glass transition and rel...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
doi：10.1002/jps.10489
更新日期：2004-01-01 00:00:00
abstract：:We have recently reported the time course of acute myocardial drug uptake and simultaneous pharmacodynamic effects for metoprolol (4 mg; n = 12) and sotalol (20 mg; n = 10) in patients with ischemic heart disease. The acute pharmacodynamic effects of the two drugs included reductions in both spontaneous heart rate and...
journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章
doi：10.1021/js9702776
更新日期：1998-02-01 00:00:00
abstract：:A series of molecular complexes, both co-crystals and salts, of a triazole drug-alprazolam-with carboxylic acids, boric acid, boronic acids, and phenols have been analyzed with respect to heterosynthons present in the crystal structures. In all cases, the triazole ring behaves as an efficient hydrogen bond acceptor wi...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.22117
更新日期：2010-09-01 00:00:00
abstract：:The stability of aqueous solutions of luteinizing hormone-releasing hormone (LHRH) after extended storage at various temperatures was investigated using a newly developed HPLC assay and an in vitro dispersed pituitary cell culture bioassay. Good correlations were obtained between the potency obtained by HPLC and bioas...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600730628
更新日期：1984-06-01 00:00:00
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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doi：10.1002/jps.21557
更新日期：2008-12-01 00:00:00
abstract：:The present study pursued to profile the intestinal solubility of nine HIV protease inhibitors (PIs) in fasted- and fed-state human intestinal fluids (FaHIF, FeHIF) aspirated from four volunteers. In addition, the ability of fasted- and fed-state simulated intestinal fluids (FaSSIF, FeSSIF) to predict the intestinal s...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.23698
更新日期：2013-10-01 00:00:00
abstract：:Pretreatment with cyclosporine reportedly prolongs the effect of certain general anesthetics in humans and the sleeping time of mice after pentobarbital administration. This investigation was designed to determine the mechanism(s) of the cyclosporine-barbiturate interaction. Adult female Wistar rats received cyclospor...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600790106
更新日期：1990-01-01 00:00:00
abstract：:Role of water in chemical (in)stability is revisited, with focus on deamidation in freeze-dried amorphous proteins and peptides. Two distinct patterns for deamidation versus water have been reported, that is, a consistent increase in rate constant with water, and a "hockey stick"-type behavior. For the latter, deamida...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2017.09.003
更新日期：2018-01-01 00:00:00
abstract：:Acyclovir is an antiviral drug poorly absorbed in the gastrointestinal tract due to its hydrophilicity, with low oral bioavailability (~20%). Although acyclovir is prescribed in the management of herpes simplex encephalitis (HSE), the disease has a poor prognosis, particularly if the treatment is delayed, reaching mor...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
doi：10.1016/j.xphs.2021.01.003
更新日期：2021-01-13 00:00:00
abstract：:Different approaches for the colorimetric determination of acetaminophen, based on its coupling with diazotized o-nitroaniline, are described. Copper(II) chelation with the coupled compound makes the method highly selective. Sensitivity is increased when the acetaminophen assay is carried out indirectly through the de...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600680626
更新日期：1979-06-01 00:00:00
abstract：:5-Methyl-2-[(4-methyl-2-nitrophenyl)amino]-3-thiophenecarbonitrile is an example of conformational and color polymorphism. The compound crystallizes in red (R), dark red (DR), light red (LR), and orange (O) modifications. There are two specific goals for this study. One is to characterize the complex thermodynamic rel...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/1520-6017(200103)90:3<371::aid-jps12>3.0.c
更新日期：2001-03-01 00:00:00
abstract：:The dielectric constant of a solid substance in the dissolved state may be found by using a solvent with a dielectric constant that remains invariable when the solid substance is dissolved. The slope values obtained from dielectric constant versus concentration plots of the solid substance in two solvents with differe...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600680408
更新日期：1979-04-01 00:00:00
abstract：:Exposure of 4-methoxy-2-(3-phenyl-2-propynyl)phenol (CO/1828) to air and light (accelerated by temperature) yields 1-(2-hydroxy-5- methoxyphenyl)-3-phenylpropynone as the major degradation product. With extraction, this product rapidly degrades to 5-methoxyaurone and 6-methoxyflavone. In addition, a mixture of dimeric...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600810818
更新日期：1992-08-01 00:00:00
abstract：:The use of intravascular tyrosine (TYR) to enhance catecholamine release in hemorrhagic shock and other cardiovascular diseases, or as a constituent of nutrient mixtures used for total parenteral nutrition, is limited by the unusually poor solubility of the amino acid in water. We have thus examined the ability of var...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600790807
更新日期：1990-08-01 00:00:00
