Abstract：
:Previously, 1 mL of purified water (hyposmotic) or saline (isosmotic) which dissolved 200 μM of FITC-dextran (FD-4), a nonabsorbable marker, was orally administered to rats, and luminal concentration-time profile of FD-4 was directly measured. In this study, at first, luminal FD-4 concentration was measured after oral administration of 0.5 mL of FD-4 purified water solution (200 μM). Then, kinetic analysis was conducted to calculate the fluid volume that passed through each segment of the gastrointestinal tract (Vfluid), based on the luminal FD-4 concentration-time profiles obtained from 3 different administration groups. In the group of 1 mL purified water administration, most of administered water was absorbed quickly from the duodenum and upper jejunum, whereas group of saline administration (1 mL) showed only a little amount of absorbed in the upper small intestine. In 0.5 mL purified water group, Vfluid in the stomach was approximately half compared to that in 1 mL purified water group. However, for small intestine, almost the same values of Vfluid were obtained regardless of the dose-volume. Our findings are valuable to improve the quality of in vitro predictive dissolution tools or in silico simulation for predicting oral drug absorption.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Tanaka Y,Higashino H,Kataoka M,Yamashita Sdoi
10.1016/j.xphs.2020.03.005subject
Has Abstractpub_date
2020-06-01 00:00:00pages
1863-1866issue
6eissn
0022-3549issn
1520-6017pii
S0022-3549(20)30129-5journal_volume
109pub_type
杂志文章abstract：:This study investigated the enhanced transdermal delivery of testosterone (Tes) and estradiol (E2) in swine in vivo with novel metered-dose topical aerosols containing the penetration enhancer padimate O (PadO) and predicted the dose deliverable in humans from the calculated drug flux across the skin. Weanling swine w...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js980026c
更新日期：1998-10-01 00:00:00
abstract：:In this study, we attempted to improve the oral absorption of ceftriaxone (CTX) by using an absorption carrier and the CTX complex together. After the CTX-Ca-carrageenan gel complex was prepared, several kinds of compounds (Capmul MCM C10, Gelucire 44/14, glycyrrhizin) were screened as potential oral enhancers for our...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10563
更新日期：2004-03-01 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：:Ambrisentan is a nonsulfonamide, ET(A)-selective endothelin receptor antagonist (ERA) approved for the treatment of pulmonary arterial hypertension (PAH), and tadalafil is a phosphodiesterase type 5 (PDE-5) inhibitor under investigation for treatment of PAH. Due to the potential combination use, the pharmacokinetic (P...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,随机对照试验
doi：10.1002/jps.21789
更新日期：2009-12-01 00:00:00
abstract：:Determination of the kinetics of water-soluble degradation products inside poly(lactide-co-glycolide) (PLGA) delivery systems during polymer degradation is important to evaluate the polymer microclimate conditions, particularly microclimate pH changes for optimization of encapsulated drug stability. A pre-derivatizati...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10524
更新日期：2004-02-01 00:00:00
abstract：:The interaction between four different microparticulate drug carriers and macrophages was investigated in vitro. The microparticles, consisting of crosslinked starch (1,4-alpha-D-glucan with 1,6-alpha-branches), dextran (1,6-alpha-D-glucan with 1,3-alpha-branches), lichenan (1,3-beta-D-glucan), or mannan (1,6-alpha-D-...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600760209
更新日期：1987-02-01 00:00:00
abstract：:By the use of NMR spectroscopy, the highly colored reaction products formed by ouabain or digitoxin in with 1,3,5-trinitrobenzene or 2,4,6-trinitroanisole in the presence of alkali (as used for the determination of these glycosides) are shown to be Meisenheimer complexes. The complexes are produced by attachment of a ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600660544
更新日期：1977-05-01 00:00:00
abstract：:An automated potentiometric procedure was used for studying in vitro dissolution kinetics of acidic drugs. Theoretical considerations indicated that the pH-stat method could be used to establish approximate sink conditions or, possibly, a perfect sink. Data obtained from dissolution studies using the pH-stat method we...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670837
更新日期：1978-08-01 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：:This article describes a procedure to facilitate scale-up for the primary drying phase of lyophilization using a combination of empirical testing and numerical modeling. Freeze dry microscopy is used to determine the temperature at which lyophile collapse occurs. A laboratory scale freeze-dryer equipped with manometri...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21430
更新日期：2009-01-01 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：:In this study, the cytotoxicity of doxorubicin (DOX) loaded stearic acid grafted chitosan oligosaccharide (CSO-SA) micelles and its core modified drug delivery systems were investigated in vitro. The in vitro drug release experiments using cellular culture medium, Roswell Park Memorial Institute 1640 (RPMI-1640) mediu...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21464
更新日期：2009-02-01 00:00:00
abstract：:The conditions of sorption of penicillins and cephalosporins on nonionic macroporous copolymers of styrenedivinylbenzene were evaluated. By increasing the methanol concentration in the eluent, the sorption decreased. Salts exerted little influence on sorption. However, pH exerted a remarkable effect on sorption, and t...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600700906
更新日期：1981-09-01 00:00:00
abstract：:The kinetics of irreversible aggregation of bovine Granulocyte-Colony Stimulating Factor (bG-CSF) in solution were investigated as a function of temperature (T), concentration, and pH, and analyzed in terms of an Extended Lumry-Eyring model of protein aggregation proceeding via a non-native conformational state. In th...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10377
更新日期：2003-05-01 00:00:00
abstract：:The elementary osmotic pump is a new delivery system for drugs or other active agents; it delivers the agent by an osmotic process at a controlled rate. Control resides in the: (a) water permeation characteristics of a semipermeable membrane surrounding the formulated agent, and (b) osmotic properties of the formulati...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600641218
更新日期：1975-12-01 00:00:00
abstract：:The solvent-free melt electrospinning (MES) method was developed to prepare a drug delivery system with fast release of carvedilol (CAR), a drug with poor water solubility. To the authors knowledge, this is the first report for preparing drug-loaded melt electrospun fibers. Cationic methacrylate copolymer of Eudragit®...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23374
更新日期：2013-02-01 00:00:00
abstract：:Substance P (SP) was degraded by synaptic membranes of rat spinal cord. Cleavage products were separated by reversed phase high performance liquid chromatography and identified by amino acid composition analyses. Major products of SP were phenylalanine, SP(1-4), SP(1-6), SP(1-7), SP(10-11), and SP(8-9). Both the degra...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js990149c
更新日期：1999-11-01 00:00:00
abstract：:Vitamin E tocopherol polyethylene glycol succinate (TPGS) is a non-ionic surface active agent, known to enhance the bioavailability of lipophilic compounds via wettability, solubility, and in some cases permeability enhancement. MK-0536 is an anti-retroviral drug with poor wettability and solubility and a high dose. B...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24585
更新日期：2015-11-01 00:00:00
abstract：:Biodegradable, dextran-based ion-exchange microspheres (IE-MS) have been used for localized delivery of anticancer drugs and chemosensitizers. Because of their hydrophilic nature, the IE-MS release their payload quickly. The purpose of this work was to develop an IE-MS system that could provide a broad range of releas...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/(SICI)1520-6017(200006)89:6<807::AID-JPS13
更新日期：2000-06-01 00:00:00
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：:The liquid sponge phase, a bicontinuous lipid-water system, formed in solvent-monoolein-water systems was investigated with respect to drug compatibility. The solvents propylene glycol and poly(ethylene glycol) swell the bicontinuous cubic phase of the monoolein-water system and form the sponge phase at constant water...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js980209z
更新日期：1998-12-01 00:00:00
abstract：:Studies directed at the synthesis of tetracycline ring A analogs are described. 4-Carbethoxycyclohexane-1,3-dione was converted to the ethyl urethan dispiro[1,3-dioxolane-2,2'-cyclohexane-4',2"(1,3)-dioxolane]-1'-carbamic acid ethyl ester via the dispiro[1,3-dioxolane-2,2'-cyclohexane-4'-2"(1,3)-dioxolane]-1'-carboxyl...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600700508
更新日期：1981-05-01 00:00:00
abstract：:The purpose of this study was to develop quantitative structure-activity/pharmacokinetic relationships (QSAR/QSPKR) for 11 selected corticosteroids in man. Multiple linear regression analysis with an automatic forward step-wise inclusion algorithm was used to construct QSAR/QSPKR models from molecular and submolecular...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10231
更新日期：2002-11-01 00:00:00
abstract：:The aim of this work was to optimize the absorption of parathyroid hormone 1-34 (PTH) from the lungs by determining factors favoring its transport from the air spaces into the bloodstream. We simultaneously conducted pharmacokinetic and regional lung deposition studies in vivo in the rat following intratracheal admini...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20053
更新日期：2004-05-01 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
pub_type： 杂志文章,评审
doi：10.1016/j.xphs.2018.05.006
更新日期：2018-09-01 00:00:00
abstract：:The effect of excipient, drug, and osmotic agent loaded in the inner core tablet on the time-controlled disintegration of compression-coated tablet prepared by direct compression with micronized ethylcellulose was investigated. The excipients [spray-dried lactose, hydroxypropyl methyl cellulose, sodium starch glycolat...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10197
更新日期：2002-09-01 00:00:00
abstract：:The effects of physical aging and antiplasticization on the water transport properties of glassy cellulose acetate film-coated tablets were investigated. The gradual approach toward thermodynamic equilibrium during physical aging decrease the free volume of the polymers. This decrease in free volume is accompanied by ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600830337
更新日期：1994-03-01 00:00:00
abstract：:17-Chloroacetylajmaline and 17-acetylajmaline are reported to have in vivo antiarrhythmic activity and are metabolized by hydrolysis. Since the hydrolysis product, ajmaline, may be the actual antiarrhythmic agent, the hydrolysis of these derivatives by various tissues of the guinea pig, rat, and mouse was determined i...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600640933
更新日期：1975-09-01 00:00:00
abstract：:The release of potassium chloride from hydroxypropyl methylcellulose matrices was investigated for tablets prepared with several different compression forces. It was determined that the release kinetics for these systems deviates significantly from the classical t1/2 dependence. This behavior was attributed to air ent...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600721021
更新日期：1983-10-01 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
