Abstract：
:To evaluate the intestinal permeability of poorly water-soluble compounds, it is of importance to completely dissolve them in a medium and to avoid precipitation during experiments. This study was undertaken to find an agent possessing a high-solubilizing capacity and exhibiting minimal modulating impact on membrane integrity and absorption systems such as passive diffusion and carrier-mediated permeation. Phenytoin dissolution was compared in the presence of seven solubilizing agents at concentrations of 1, 2, or 5% using a centrifugation method. The capacity to dissolve phenytoin was great in beta-cyclodextrin (beta-CD) and hydroxypropyl beta-cyclodextrin, followed by Tween 80. Those of methanol, dimethyl sulfoxide, dimethyl acetoamide, and polyethylene glycol 400 were much lower than expected. One percent beta-CD did not alter the absorption of fluorescein isothiocyanate-dextran 4,000 or the release of protein and lactate dehydrogenase into in situ loop contents, suggesting that 1% beta-CD had no significant impact on the integrity of the intestinal membrane. One percent beta-CD also did not alter the absorption of caffeine, ceftibuten, or rhodamine 123 from in situ jejunal loops, indicating no interference with passive diffusion and active transports mediated by a peptide transporter and P-glycoprotein. In conclusion, 1% beta-CD is a suitable solubilizing agent for evaluating in situ intestinal absorption of poorly water-soluble compounds.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Oda M,Saitoh H,Kobayashi M,Aungst BJdoi
10.1016/j.ijpharm.2004.05.003keywords:
subject
Has Abstractpub_date
2004-08-06 00:00:00pages
95-102issue
1-2eissn
0378-5173issn
1873-3476pii
S0378517304002868journal_volume
280pub_type
杂志文章abstract：:Ethylene-vinyl acetate (EVA) is widely used as a membrane or matrix for transdermal drug delivery systems. In an attempt to determine the state of a drug in the EVA matrix, X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR) and thermal analysis of the quinupramine-EVA matrix were carried out and ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.06.016
更新日期：2006-08-31 00:00:00
abstract：:The objective of this study was to evaluate the combination of pH-dependent and time-dependent polymers as a single coating for design of colon delivery system of indomethacin pellets. Eudragit S100 and Eudragit L100 were used as pH-dependent polymers and Eudragit RS was used as a time-dependent polymer. A statistical...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.05.011
更新日期：2006-08-31 00:00:00
abstract：:Achieving drug delivery at the ocular level encounters many challenges and obstacles. In situ gelling delivery systems are now widely used for topical ocular administration and recognized as a promising strategy to improve the treatment of a wide range of ocular diseases. The present work describes the formulation and...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.118734
更新日期：2020-01-25 00:00:00
abstract：:Amorphous lactose will crystallise rapidly if its glass transition temperature is reduced below its storage temperature. This is readily achieved by storing samples at ambient temperature and a relative humidity (RH) of greater than 50%. If the sample is monitored in an isothermal microcalorimeter as it crystallises, ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.07.016
更新日期：2004-10-13 00:00:00
abstract：:The electrochemical reduction of ornidazole was studied at a glassy carbon electrode activated by applying a new pretreatment. The dependence of intensities of currents and potentials on pH, concentration, scan rate, nature of the solvent (aqueous media, mixed aqueous-organic systems) and surfactant was investigated. ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(97)00208-1
更新日期：1997-11-28 00:00:00
abstract：:This work aimed to clarify the relationship between polymer function and insulin absorption, and to evaluate the optimized preparative formulation predicted from this relationship. Insulin-loaded polymer (ILP) carrier systems were prepared following a two-factor composite second-order spherical experimental design. To...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.10.050
更新日期：2008-04-16 00:00:00
abstract：:Following vascular bypass interventions, autologous saphenous vein grafts are prone to fail due to intimal hyperplasia development. An atorvastatin (ATV)-eluting tubular mesh coated with poly(d,l-lactide-co-glycolisde) acid (PLGA) was designed for perivascular application, in order to prevent the development of this p...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.12.026
更新日期：2018-02-15 00:00:00
abstract：:Biodegradable poly(l-lactide-co-ε-caprolactone) (PLCL) are used to prepare inflatable balloon implants in treating rotator-cuff injuries and tissue separation. These balloon implants act as a temporary spacer for tissues, while reducing pain and allowing rehabilitation after surgery. It is essential to ensure that eac...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.118870
更新日期：2020-01-25 00:00:00
abstract：:Herein, a series of new amino acid-functionalized hollow mesoporous silica nanospheres (HMSNs) by post-grafting methods were prepared. These new materials were characterized by different techniques and were studied as matrices for the antineoplastic drug (cisplatin) transport and delivery. The results demonstrate that...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.118709
更新日期：2019-12-15 00:00:00
abstract：:Experiments were conducted to illustrate some of the challenges associated with measuring dynamic MDI aerosols. Experimental HFA-134a solution MDIs containing 8 or 20% ethanol were measured using the Andersen cascade impactor using three different inlets. It was demonstrated that the size distribution of MDI aerosols ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.11.047
更新日期：2008-05-01 00:00:00
abstract：:Dissolution research started to develop about 100 years ago as a field of physical chemistry and since then important progress has been made. However, explicit interest in drug related dissolution has grown only since the realisation that dissolution is an important factor of drug bioavailability in the 1950s. This re...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.07.011
更新日期：2006-09-14 00:00:00
abstract：:Nanoparticles (NPs) have shown a certain potential to overcome the drawbacks of oral peptide delivery in the gastrointestinal tract such as low peptide stability and permeability. The preparation of insulin loaded NPs was carried out with Eudragit RL or RS dissolved in different non-toxic polyethylene glycol (PEG) der...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.01.017
更新日期：2013-02-25 00:00:00
abstract：:The objective of this study was to determine, using a Caco-2 cell monolayer model, the extent to which the paracellular and transcellular routes are altered by citicholine (CDP-Ch) and DMSO in the presence of human serum albumin (HSA). The apparent permeability (Papp) of mannitol in the presence of 4% (w/v) HSA was in...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00588-4
更新日期：2003-01-30 00:00:00
abstract：:Tumor growth and metastasis are multistep processes regulated by multiple signaling pathways. The successful treatment of cancer largely depends on the ability to inhibit metastatic process. Multiphase inhibition of metastasis is a promising approach. Here, we described a targeting delivery system which was constructe...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119085
更新日期：2020-03-15 00:00:00
abstract：:The stability of solid dispersions (SD) during storage is of concern. We prepared the pH-modulated SD (pSD) and compressed tablets consisting of polyethylene glycol (PEG) 6000 as a carrier, drug and MgO (alkalizer). Telmisartan (TEL), an ionizable poorly water-soluble drug, was chosen as a model drug. The changes in p...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.04.065
更新日期：2011-07-29 00:00:00
abstract：:This investigation has examined possible causes of the poor bioavailability of the beta(3)-adrenoceptor agonist BTA-243. The aqueous solubility of BTA-243 is pH dependent with a solubility minimum at pH 1.5. However, the dissolution rate of the disodium salt of BTA-243 is similar at both pH 2.0 and 7.4 indicating that...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00657-8
更新日期：2001-02-01 00:00:00
abstract：:Squamous cell carcinoma treatment has limited therapeutic options and the incidence rate is increasing recently. In the present investigation, we developed poly(lactic-co-glycolic acid) (PLGA) nanopatterned films (NPFs) through poly dimethyl siloxane (PDMS) cast molding technique and explored its therapeutic efficacy ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119100
更新日期：2020-03-30 00:00:00
abstract：:Block-polymer nanoparticles are now well-known candidates for the delivery of various non-soluble drugs to cells. The release of drugs from these nanoparticles is a major concern related to their efficiency as nanovectors and is still not completely deciphered. Various processes have been identified, depending of both...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.09.032
更新日期：2015-11-30 00:00:00
abstract：:Our research on topical application of lidocaine-loaded non-ionic surfactant vesicles (NSVs) was prompted by the great interest on new delivery systems for local anaesthetics. This study is focused on a novel formulation of NSVs entrapping lidocaine in the form of a free base (LID) and a hydrochloride (LIDHCl). NSVs w...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(01)00828-6
更新日期：2002-01-01 00:00:00
abstract：:The objective of this study was to synthesize and evaluate novel enzymatically stable dipeptide prodrugs for improved absorption of acyclovir. l-Valine-l-valine-acyclovir (LLACV), l-valine-d-valine-acyclovir (LDACV), d-valine-l-valine-acyclovir (DLACV) and d-valine-d-valine-acyclovir (DDACV) were successfully synthesi...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.05.024
更新日期：2008-09-01 00:00:00
abstract：:Niosomes are novel carriers that show superior transdermal permeation enhancement but require the addition of charged stabilizers. In this study, niosomes were prepared using Span 40, cholesterol, and sodium dodecyl sulfate (SDS) as stabilizers for transdermal delivery of salidroside. At concentrations of 0.05-0.40% (...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119183
更新日期：2020-04-30 00:00:00
abstract：:The permeation of cyproterone acetate (CPA) from Derma Membrane Structure (DMS) creams and liposomal formulations was investigated. Standard diffusion experiments with dermatomed porcine skin were performed. The cumulative CPA amount permeated of the DMS creams was between 2.9 and 6.8 microg/cm(2) within 48 h. By addi...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(03)00180-7
更新日期：2003-06-04 00:00:00
abstract：:Personalized medicine is a challenging research area in paediatric drug design since no suitable pharmaceutical forms are currently available. Furosemide is an anthranilic acid derivative used in paediatric practice to treat cardiac and pulmonary disorders in premature infants and neonates. However, it is not commerci...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.08.059
更新日期：2014-11-20 00:00:00
abstract：:The present investigation aims at formulating lipid based drug delivery system of β-Artemether and Lumefantrine and comparative pharmacological evaluation with innovator formulation. Commercial modified oil and indigenous natural fatty acids comprised the oily phase in developing lipidic formulation of β-Artemether an...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.07.033
更新日期：2013-10-15 00:00:00
abstract：:A new class of surfactants with glycerate headgroups, that form viscous lyotropic liquid crystalline phases in excess water, have been investigated for their potential to provide sustained release matrices for depot drug delivery. Oleyl glycerate and phytanyl glycerate were used as representative surfactants of this n...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.11.033
更新日期：2006-02-17 00:00:00
abstract：:The aim of this study was to elucidate the importance of potential limited solubility effects for the control of drug release from hydrophilic matrix tablets loaded with a freely water-soluble drug. It is often assumed that the considerable amounts of water penetrating into this type of advanced drug delivery systems ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.05.001
更新日期：2017-06-30 00:00:00
abstract：:To develop a low-dose therapeutic system for amphotericin B (AmB), the efficacy and toxicity of lipid nano-sphere (LNS) incorporating AmB (LNS-AmB) were evaluated and compared with those of Fungizone, the conventional dosage form of AmB with sodium deoxycholate. LNS-AmB and Fungizone showed nearly equal activity again...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(03)00342-9
更新日期：2003-09-16 00:00:00
abstract：:Progesterone-loaded poly(lactic) acid fibrous polymeric patches were produced using electrospinning and pressurized gyration for intra-vaginal application to prevent preterm birth. The patches were intravaginally inserted into rats in the final week of their pregnancy, equivalent to the third trimester of human pregna...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119782
更新日期：2020-10-15 00:00:00
abstract：:Rheumatoid arthritis (RA) is an autoimmune disease featured with chronic joint inflammation. Suppression of inflammation is critical to RA treatment and joint protection. In this study, DNA nanodrugs are prepared via the conjugation of NF-κB decoy oligodeoxynucleotides (dODNs) and VCAM-1 targeted peptides (P) onto sel...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119047
更新日期：2020-03-15 00:00:00
abstract：:Raman spectroscopy may be implemented through a microscope to provide fine scale axial and lateral chemical maps. The molecular structure of many drugs makes Raman spectroscopy particularly well suited to the investigation of pharmaceutical systems. Chemometric methods currently used to assess bulk Raman spectroscopic...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2010.12.030
更新日期：2011-09-30 00:00:00
