Abstract：
:A study was carried out in human volunteers to investigate whether ileal brake activators could alter the bioavailability of atenolol from the small intestine by slowing intestinal transit and thereby increasing the time available for absorption. Oleic acid and a monoglyceride were formulated into modified release capsules that were targeted to the small intestine. Atenolol was either dosed separately or incorporated into one of the capsules. Radiolabelled non-disintegrating tablets were dosed at the same time in order to determine the small intestinal transit time (SITT). Plasma concentrations of atenolol were determined by HPLC. The results showed that in some volunteers an increase in SITT did lead to an increase in the quantity of drug absorbed. However, drug absorption was related not only to the total time spent by the drug in the small intestine but other factors such as the proportion of such time spent at the ileocaecal junction. The study highlights the complexities of exploiting natural gastrointestinal processes to enhance the oral bioavailability of drugs.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Dobson CL,Davis SS,Chauhan S,Sparrow RA,Wilding IRdoi
10.1016/s0378-5173(02)00393-9keywords:
subject
Has Abstractpub_date
2002-11-06 00:00:00pages
61-70issue
1-2eissn
0378-5173issn
1873-3476pii
S0378517302003939journal_volume
248pub_type
杂志文章abstract：:Capping as well as lamination are two common problems, which affect the resulting product quality of the tablet. Usually, capping and lamination occur during or after tablet manufacturing, and may therefore influence follow-up processes such as the coating. In this context, there is an urgent need for approaches to ov...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119195
更新日期：2020-04-30 00:00:00
abstract：:Antimicrobial urological catheters were developed by the mixed, covalent and non-covalent binding of sparfloxacin (SPA) to heparin (HP) film which was first deposited on the latex surface of biomaterial. The SPA-HP modified surface was characterized by SEM analysis and ATR-Fourier transform infrared spectroscopy. For ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.10.014
更新日期：2010-12-15 00:00:00
abstract：:Previously, PTX/Pluronic F127 nanocrystals were prepared in our laboratory using the stabilization of nanocrystals (SNC) method. For PTX nanocrystals, dosages could be increased to yield improved antitumor activity over Taxol without incidence of acute toxicity. The objectives of this current study are to further unde...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.02.013
更新日期：2010-05-10 00:00:00
abstract：:In this study, the roll compaction of an intermediate drug load formulation was performed using horizontally and vertically force fed roll compactors. The horizontally fed roll compactor was equipped with an instrumented roll technology allowing the direct measurement of normal stress at the roll surface, while the ve...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.02.042
更新日期：2015-04-30 00:00:00
abstract：:Autophagy is a lysosomal degradation pathway that acts as a cytoprotective mechanism causing treatment resistance in various cancer cells. Recent studies showed that hydroxychloroquine can inhibit the latter step of autophagy and therefore enhance the anti-glioma efficiency of ZD6474, a tyrosine kinase inhibitor. Howe...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.09.007
更新日期：2018-01-30 00:00:00
abstract：:Extracellular vesicles (EVs) are nanosized vesicular structures released by cells to communicate with one another. The growing interest in the (patho)physiological function and potential pharmaceutical application of these vesicles is accompanied by a vast number of new research groups entering this research field and...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.10.022
更新日期：2018-09-15 00:00:00
abstract：:Titration calorimetry was used to investigate the interaction between a model antigen, bovine serum albumin (BSA), and a model particulate carrier, polystyrene (PS). The binding enthalpy was much higher than reported in the literature for a similar system and did not display a sigmoidal binding curve. These experiment...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.02.037
更新日期：2005-07-25 00:00:00
abstract：:Formulation intervention, through the application of processing technologies, is a requirement for enabling therapy for the vast majority of drugs. Without these enabling technologies, poorly soluble drugs may not achieve therapeutic concentrations in the blood or tissue of interest. Conversely, freely soluble and/or ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2013.04.042
更新日期：2013-06-25 00:00:00
abstract：:The inhalation of tobramycin is part of current cystic fibrosis (CF) therapy. Local therapy with inhaled antibiotics has demonstrated improvements in pulmonary function. Current inhalation therapy is limited by the available drug formulations in combination with the nebulization time. The aim of this study is to devel...
journal_title：International journal of pharmaceutics
pub_type： 评论,杂志文章
doi：10.1016/s0378-5173(99)00252-5
更新日期：1999-11-05 00:00:00
abstract：:The effects of carriers, the drug:carrier ratio and a 1 month storage period of a formulation in permeable polystyrene tube at 40 degrees C/75% RH on the in vitro pulmonary deposition of model drugs from dry powder inhaler (DPI) were evaluated. Budesonide (hydrophobic) and salbutamol sulphate (hydrophilic) were used a...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(03)00357-0
更新日期：2003-09-16 00:00:00
abstract：:Sustained-release nitrendipine microspheres were prepared in liquid system by quasi-emulsion solvent diffusion method, in which the Aerosil was employed as an inert dispersing carrier to improve the dissolution rate of nitrendipine, and Eudragit RS as a retarding agent to control the release rate. The resultant micros...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(03)00209-6
更新日期：2003-06-18 00:00:00
abstract：:Hexamidine diisethionate (HEX D) has been used in the personal care industry and in a number of over-the-counter (OTC) drug products as an antimicrobial agent since the 1950's. Recently, the compound has also been investigated for its beneficial effects on skin health. Surprisingly, there is only limited information d...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.07.071
更新日期：2015-09-30 00:00:00
abstract：:The purpose of the study is to screen the interactions of fourth generation fluoroquinolone-gatifloxacin with efflux pumps, i.e., P-gp, MRP2 and BCRP. Mechanism of gatifloxacin interaction with efflux transporters may explain its acquired resistance. Such clarification may lead to the development of strategies to over...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.05.027
更新日期：2010-08-16 00:00:00
abstract：:Superparamagnetic iron oxide nanoparticles (SPIO-NPs) have traditionally been used as MRI contrast agent for disease imaging via passive targeting. However, there has been an increasing interest in the development of SPIO-NPs to cellular-specific targeting for imaging and drug delivery currently. The objective of our ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.10.038
更新日期：2011-02-14 00:00:00
abstract：:The buccal administration of ergotamine tartrate (ET) combined with polyvinyl alcohol (PVA) gel brought about higher plasma concentration of ET compared with that of oral administration of capsules in guinea-pigs. T(max) of ET in plasma of buccal administration was significantly smaller than that of oral administratio...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00070-4
更新日期：2002-05-15 00:00:00
abstract：:Curcumin (CUR) has been formulated into a host of nano-sized formulations in a bid to improve its in vivo solubility, stability and bioavailability. The aim of this study was to investigate whether the encapsulation of CUR in nanocarriers would impede its biological interactivity, specifically its potential anti-cance...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.08.066
更新日期：2015-11-10 00:00:00
abstract：:Antibiotics are well-known disruptive elements of the intestinal microbiota and antibiotic-associated diarrhea appeared as the most common complication related with post-antibiotic dysbiosis. Lactobacillus rhamnosus GG (LGG) strain is very effective in preventing antibiotic-associated diarrhea in children and adults. ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119414
更新日期：2020-06-30 00:00:00
abstract：:Lipoproteins are naturally occurring nano sized transport vehicles in the human body. Therefore, lipoproteins could be applied as a drug carrier system. Additionally, several reports of apolipoprotein mediated blood-brain barrier (BBB) crossing suggest lipoprotein mimicking nanoparticles (NPs) as possible drug deliver...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119821
更新日期：2020-08-28 00:00:00
abstract：:Multilayered coated liposomes were prepared using the layer-by-layer (LbL) technique in an effort to improve their stability in biological media. The formulation strategy was based on the alternate deposition of two biocompatible and biodegradable polyelectrolytes - poly(L-lysine) (PLL) and poly(L-glutamic acid) (PGA)...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119568
更新日期：2020-08-30 00:00:00
abstract：:In this note we describe the substitution of the phospholipid component in classical ISCOMs (immune-stimulating complexes) with the cationic lipid dioleoyl-trimethyl-ammonium-propane (DOTAP). The self-assembled colloidal structures formed by DOTAP, Quil-A and cholesterol were characterised using transmission electron ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.09.029
更新日期：2007-03-06 00:00:00
abstract：:This paper describes a rational method of characterizing the biopharmaceutical stability of two oral suspensions of ursodeoxycholic acid (UDCA) used in pediatrics. Because there is no commercial presentation of UDCA that can administer appropriate doses for infants and children, an active pharmaceutical ingredient (AP...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.10.011
更新日期：2014-12-30 00:00:00
abstract：:Development of novel anticancer formulations is a priority challenge in biomedicine. However, in vitro models based on monolayer cultures (2D) which are currently used for cytotoxicity tests leave much to be desired. More and more attention is focusing on 3D in vitro systems which can better mimic solid tumors. The ai...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.04.005
更新日期：2016-06-15 00:00:00
abstract：:The aim of the present work was the synthesis and study the kinetics and profiles of camptothecin (CPT) release form block co- and ter-polymer conjugates comprising polylactide (PLA) segments and CPT moieties, structurally diverse by degrees of branching, content of d-PLA units and poly(ethylene glycol) methyl ether m...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.01.022
更新日期：2018-03-01 00:00:00
abstract：:The interaction between packaging materials and drug products is an important issue for the pharmaceutical industry, since during manufacturing, processing and storage a drug product is continuously exposed to various packaging materials. The experimental investigation of a great variety of different packaging materia...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.03.049
更新日期：2012-07-15 00:00:00
abstract：:Enhancing transdermal delivery of insulin using chemical penetration enhancers (CPEs) has several advantages over other non-traditional methods; however, lack of suitable predictive models, make experimentation the only alternative for discovering new CPEs. To address this limitation, a quantitative structure-property...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.12.028
更新日期：2010-03-30 00:00:00
abstract：PURPOSE:This study aimed to investigate the penetration of topical and oral ofloxacin into aqueous humor and vitreous humor in post-traumatic endophthalmitis model in rabbits. METHODS:A standardized intraocular infection after penetrating injury was made in the right eyes of 16 rabbits. Intraocular infection was induc...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00482-8
更新日期：2000-08-25 00:00:00
abstract：:Here we explore the opportunity to design and then produce tailored release of therapeutic drugs from microcapsules. By use of "building blocks," formed from well characterized microcapsule populations, an inverse design algorithm has been developed that provides an optimal (in a least squares sense) combination of bu...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.09.010
更新日期：2010-01-04 00:00:00
abstract：:Our capacitance and conductance measurements on reconstituted planar lipid bilayers (BLM) suggest an insertion of the flavonoid quercetin (QCT) in the membranes, which is concentration- and pH-dependent. Interaction of the flavonoid with the membrane has no impact on either structure or integrity of the lipid bilayer....
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00503-2
更新日期：2000-09-15 00:00:00
abstract：:In spite of the high incidence of breast cancer worldwide, there are few strategies for its chemoprevention, and they have limited adherence mainly due to their serious adverse effects. As a new approach for local breast cancer chemoprevention, we developed and optimized microemulsions for topical delivery of celecoxi...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.02.011
更新日期：2019-04-05 00:00:00
abstract：:Three novel amino acid based anionic amphiphilic copolymers poly(sodium N-acryloyl-l-valinate-co-alkylacrylamide) (where, alkyl=octyl and dodecyl) with either 9 or 16 mol% hydrophobic substitution were synthesized. These hydrophobically modified polyelectrolytes (HMPs), above a critical concentration, self-assemble in...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.01.041
更新日期：2011-04-04 00:00:00
