Abstract：
:Owing to proliferation of antibiotic-resistant bacteria, the use of antibiotics for livestock growth promotion is banned in many countries and alternatives to in-feed antibiotics are needed. Cinnamon essential oil exhibits strong in vitro antibacterial activity; however, direct addition of essential oils to animal feed has limited practicality due to their high volatility, odor, fast decomposition, and poor availability in the lower intestines. To solve these problems, we formulated trans-cinnamaldehyde (CIN) with an adsorbent powder and fatty acid via a melt-solidification technique. Core granules of an optimized composition contained up to 48% wt/wt CIN. The granules were then coated with an enteric polymer to impart site-specific release of CIN. CIN was mostly retained in simulated gastric fluid and released rapidly (>80% under 2 h) in simulated intestinal fluids. Rapid CIN autoxidation into cinnamic acid was inhibited by adding 1% vol/vol eugenol, which maintained CIN stability for at least 1 y. The granule formulation increased the antimicrobial activity of CIN against Escherichia coli K88 slightly with a minimum bactericidal concentration of 450 μg/mL for CIN in lauric acid-based granules compared with 550-600 μg/mL for palmitic acid-based granules and free CIN, respectively. These results encourage the potential use of encapsulated CIN for control of animal enteric pathogens by oral in-feed administration.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Ma YH,Wang Q,Gong J,Wu XYdoi
10.1016/j.xphs.2015.10.001subject
Has Abstractpub_date
2016-03-01 00:00:00pages
1124-33issue
3eissn
0022-3549issn
1520-6017pii
S0022-3549(15)00002-7journal_volume
105pub_type
杂志文章abstract：:The binding of Cu2+ and Ni2+ to bovine, dog, and human serum albumin has been studied by the 35Cl NMR probe technique. The number of primary copper sites were estimated to be 1.3 for human serum albumin, 3.1 for bovine serum albumin, and 6.6 for dog serum albumin. A similar number of primary nickel sites was determine...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600740116
更新日期：1985-01-01 00:00:00
abstract：:A method is presented for determining the equilibrium solubility of a drug in a solid polymer at or near room temperature, which represents a typical storage temperature. The method is based on a thermodynamic model to calculate the Gibbs energy change ΔG(SS) associated with forming a binary drug-polymer solid solutio...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23319
更新日期：2012-12-01 00:00:00
abstract：:Hexamidine isethionate in various pharmaceutical formulations was analyzed quantitatively by high-performance liquid chromatography. The method is rapid, accurate, and precise. Excellent results were obtained from four commercial bases. ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600721229
更新日期：1983-12-01 00:00:00
abstract：:Polymeric nanoparticles (NPs) are interesting drug carriers for dermal application and drug targeting to certain skin structures. NP interactions with diseased skin and the associated benefits and risks have been hardly explored. Today, we study the behavior of polymeric NPs for selective drug delivery to inflamed ski...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23282
更新日期：2012-11-01 00:00:00
abstract：:In adult patients, nilotinib is indicated for chronic myeloid leukemia at an approved oral dose of 300 or 400 mg BID. Physiologically based pharmacokinetic (PBPK) model was developed to describe and supplement limited PK data in the pediatric population ranging from 2 to less than 6 years of age and ultimately inform ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2019.01.028
更新日期：2019-06-01 00:00:00
abstract：:The plasma concentrations and urinary excretions of bisoprolol enantiomers in four Japanese male healthy volunteers after a single oral administration of 20 mg of racemic bisoprolol were evaluated. The AUC(infinity) and elimination half-life of (S)-(-)-bisoprolol were slightly larger than those of (R)-(+)-bisoprolol i...
journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章
doi：10.1021/js970316d
更新日期：1998-03-01 00:00:00
abstract：:The pathogenic bacterium Staphylococcus aureus can penetrate host cells. However, intracellular S. aureus is not considered during antimicrobial agent selection in clinical chemotherapy because of the lack of information about drug transportability into cells in vivo. We focused on agents used to treat methicillin-res...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2020.09.045
更新日期：2021-02-01 00:00:00
abstract：:Metronidazole (MTZ) is a drug of choice for protozoal infections such as luminal amoebiasis. We designed and synthesized N-nicotinoyl-2-{2-(2-methyl-5-nitroimidazol-1-yl)ethyloxy}-D,L-glycine (NMG) as a colon-specific prodrug of MTZ. The synthetic yield of NMG was about 34%. The apparent partition coefficient of MTZ w...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21720
更新日期：2009-11-01 00:00:00
abstract：:Melanotan-II (1) is a cyclic heptapeptide analogue of alpha-melanocyte-stimulating hormone (alpha-MSH) which tans the skin and is currently being evaluated for the prevention of sunlight-induced skin cancers. The dissociation constants of 1 were determined using potentiometric titration and ultraviolet spectrophotomet...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600830805
更新日期：1994-08-01 00:00:00
abstract：:Acute experiments were performed on overnight fasted chloralose-urethan anesthetized dogs, cats, rabbits, and rats. Under these conditions, somatostatin practically abolished gastric contractions and decreased GI tonus in all species examined. The canine duodenum, jejunum, and ileum exhibited only a contractile respon...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600680913
更新日期：1979-09-01 00:00:00
abstract：:A round-robin study compared four methods of residual ethylene oxide analysis. Results from the six participating laboratories, along with a statistical treatment of the data, are presented. ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600640837
更新日期：1975-08-01 00:00:00
abstract：:First-order rate constants (k) were determined for the hydrolysis of ceftazidime in the pH range of 0.5 to 8.5 at 45, 55, and 65 degrees C by a stability-indicating HPLC assay. In the absence of buffer effects, the pH-rate expression was k = kH1f1(aH+) + kH2f2(aH+) + kH3f3(aH+) + kSf3 + kOHf3(aOH-), where KH and KOH a...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600840504
更新日期：1995-05-01 00:00:00
abstract：:A previous report detailed the derivation and validation of an equation for calculating the Gibbs free energy of liquid-solid adsorption via high-performance liquid chromatography (HPLC). This study utilizes an improved form of that equation in conjunction with an in vitro model of solute adsorption to give an ordered...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600770609
更新日期：1988-06-01 00:00:00
abstract：:The hydrolytic degradation of pirbuterol was investigated under saturated oxygen conditions over a wide range of pH values and at different temperatures. Two of the five observed breakdown products were positively identified. The first-order decomposition rate appeared to depend on the rate constants of the four disso...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600660620
更新日期：1977-06-01 00:00:00
abstract：:Certain disulfide analogues of cystamine were prepared and evaluated for the ability to inhibit gamma-glutamylcysteine synthetase (GCS), the rate-limiting enzyme in glutathione synthesis. The compound SAPH-3 disulfide (2a) was found to be the most effective inactivator of GCS reported to date. Studies of structural an...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600800404
更新日期：1991-04-01 00:00:00
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
pub_type： 杂志文章
doi：10.1021/js980393o
更新日期：1999-07-01 00:00:00
abstract：:Virtually all biological variables, including those affected by drugs, are subject to adaptive self regulation. In the description of the pharmacodynamics (PD) of drugs, it may be necessary to consider the endogenous control system (ECS) as an integral part of the PD. A PDECS model based on system analysis principles ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600820310
更新日期：1993-03-01 00:00:00
abstract：:Caco-2 cell monolayers are widely used systems for predicting human intestinal absorption. This study was carried out to develop a quantitative structure-property relationship (QSPR) model of Caco-2 permeability using a novel genetic algorithm-based partial least squares (GA-PLS) method. The Caco-2 permeability data f...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10214
更新日期：2002-10-01 00:00:00
abstract：:The spherically agglomerated crystals of aminophylline (theophylline-ethylenediamine complex) can be compounded directly into pharmaceutical formulations without further processing, e.g., granulation. Such crystals were prepared by mixing theophylline and ethylenediamine in a partially miscible solvent system, i.e., o...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600731021
更新日期：1984-10-01 00:00:00
abstract：:Therapeutic use of anti-inflammatory steroids is limited due to their potential suppressive effects on pituitary-adrenal function and the immune system. Based on the antedrug concept, a new class of potent locally active compounds with reduced risk of side effects has been synthesized from prednisolone by introducing ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600790716
更新日期：1990-07-01 00:00:00
abstract：:The inclusion complexation of homologous derivatives of steroid hormones with cyclodextrins and 2-hydroxypropyl-beta-cyclodextrin (2-HP-beta-CD) was investigated with regard to underlying structure-interaction relationship. The interaction was studied by phase solubility analysis and stabilization effects of complex f...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600810808
更新日期：1992-08-01 00:00:00
abstract：:Intravenously administered (i.v.) drug-cyclodextrin (CD) inclusion complexes are generally expected to dissociate rapidly and completely, such that the i.v. pharmacokinetic profile of a drug is unchanged in the presence of CD. The altered pharmacokinetics of a synthetic ozonide in rats has been attributed to an unusua...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24331
更新日期：2015-04-01 00:00:00
abstract：:Water vapor absorption isotherms for amorphous solids with the same chemical composition but differing in molecular weight (i.e., PVP-90, PVP-30, and PVP-12), and for glucose, trehalose, and two molecular weight grades of dextran were obtained at 30 degrees C and analyzed using the Brunauer-Emmett-Teller (BET) equatio...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/1520-6017(200008)89:8<1063::aid-jps11>3.0.
更新日期：2000-08-01 00:00:00
abstract：:Nephropathic cystinosis is a rare autosomal recessive disease characterised by raised lysosomal levels of cystine in the cells of all the organs. It is treated by the 6-h oral administration of the aminothiol, cysteamine, which has an offensive taste and smell. In an attempt to reduce this frequency and improve the tr...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23246
更新日期：2012-10-01 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
pub_type： 杂志文章
doi：10.1002/jps.20745
更新日期：2007-03-01 00:00:00
abstract：:Disintegration performance was measured by analysing both water ingress and tablet swelling of pure microcrystalline cellulose (MCC) and in mixture with croscarmellose sodium using terahertz pulsed imaging (TPI). Tablets made from pure MCC with porosities of 10% and 15% showed similar swelling and transport kinetics: ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24544
更新日期：2015-10-01 00:00:00
abstract：:A GLC method for determining theophylline, hydroxyethyltheophylline, and diphenylpyraline hydrochloride is presented. The method permits the separation and quantitative determination of the therapeutically active ingredients with a single injection in an overall time of approximately 2.5 hr. ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600680438
更新日期：1979-04-01 00:00:00
abstract：:Phenylpropanolamine was determined by measuring its fluorescent fluorescamine derivative. The method is rapid, sensitive, and easily automated. Statistics are presented for an effervescent cold product, and recovery data are presented for other commercially available products. ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600671137
更新日期：1978-11-01 00:00:00
abstract：:In many manufacturing and research areas, the ability to accurately monitor and characterize nanoparticles is becoming increasingly important. Nanoparticle tracking analysis is rapidly becoming a standard method for this characterization, yet several key factors in data acquisition and analysis may affect results. Nan...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2016.02.005
更新日期：2016-04-01 00:00:00
abstract：:Citric acid anhydrate (CAA) and paracetamol (PARA), prepared as crystalline physical mixtures and as amorphous blends, were studied using (13)C solid-state cross polarization magic angle spinning (CPMAS) NMR. Amorphous blends showed significant line broadening from the conformational distribution as compared to the cr...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21559
更新日期：2009-05-01 00:00:00
