当前位置： SCI文献检索 > INTERNATIONAL JOURNAL OF PHARMACEUTICS期刊下所有文献 > Prediction of oral absorption in humans by experimental immobilized artificial membrane chromatography indices and physicochemical descriptors.

Prediction of oral absorption in humans by experimental immobilized artificial membrane chromatography indices and physicochemical descriptors.

Abstract：

:The purpose of the present study was to examine the human oral absorption (HOA) predictability of the experimentally determined immobilized artificial membrane (IAM) chromatography capacity factor (log k'IAM) in conjunction with physicochemical descriptors. Transcellular permeation was modeled based on determination of log k'IAM considering pH partition hypothesis, and the independent variables were polar surface area (PSA) and molecular weight (MW). The correlation between log k'IAM determined at different pH and n-octanol/water partition coefficient (log P) and contribution of polarity (PSA) and size (MW) in the transcellular permeation model were the extension to the previous work. A data set of 37 compounds with partition coefficient values taken from the literature was employed to show importance of ionic interaction in oral absorption prediction. The highest log k'IAM value among screened pH 4.5, 5.5, 6.5 and 7.4 (log k'IAM4.5-7.4) in conjunction with PSA predicted HOA with coefficient of determination (CD) of 0.9001 compare to log k'IAM4.5-7.4 alone with CD of 0.8454 after excluding bretylium from the set of 28 structurally diverse drugs for known reason. PSA helped to avoid over estimation of HOA for amiloride, famotidine and furosemide. The model was tested for its applicability in drug development program and found to predict oral absorption using physically meaningful and structurally related properties making them relatively straightforward for a medicinal chemist to interpret.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Kotecha J,Shah S,Rathod I,Subbaiah G

doi

10.1016/j.ijpharm.2008.04.025

subject

Has Abstract

pub_date

2008-08-06 00:00:00

pages

96-106

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(08)00313-X

journal_volume

360

pub_type

杂志文章

相关文献

INTERNATIONAL JOURNAL OF PHARMACEUTICS文献大全
  • Formulation and in-vitro evaluation of directly compressed controlled release matrices of Losartan Potassium using Ethocel Grade 100 as rate retarding agent.

    abstract：:Current study was aimed to develop 200mg controlled release matrix tablets of Losartan Potassium using Ethocel 100 Premium and Ethocel 100 FP Premium as rate controlling polymer. In-vitro studies were performed according to USP Method-I in phosphate buffer (PH 6.8) using pharma test dissolution apparatus. The temperat...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2015.10.051

    authors： Khan KA,Khan GM,Zeeshan Danish M,Akhlaq,Khan H,Rehman F,Mehsud S

    更新日期：2015-12-30 00:00:00

  • Pharmacokinetics of acetaminophen in Hong Kong Chinese subjects.

    abstract：:The pharmacokinetics of acetaminophen have been well studied in different populations, especially in Caucasians. However, limited studies on acetaminophen pharmacokinetics have been conducted in the native Chinese and few such data have been reported in the English language literature. Previous published studies sugge...

    journal_title：International journal of pharmaceutics

    pub_type： 临床试验,杂志文章

    doi：10.1016/s0378-5173(01)00712-8

    authors： Yin OQ,Tomlinson B,Chow AH,Chow MS

    更新日期：2001-07-17 00:00:00

  • A systematic study of captopril-loaded polyester fiber mats prepared by electrospinning.

    abstract：:In this study, drug-loaded nanofibers were prepared by electrospinning captopril (CPL) with aliphatic biodegradable polyesters. Poly(L-lactic acid) (PLLA), poly(lactic-co-glycolic acid) (PLGA), and poly(lactic-co-ε-caprolactone) (PLCL) were used as filament-forming matrix polymers, and the concentration of CPL in each...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2012.09.055

    authors： Zhang H,Lou S,Williams GR,Branford-White C,Nie H,Quan J,Zhu LM

    更新日期：2012-12-15 00:00:00

  • Amorphization within the tablet: Using microwave irradiation to form a glass solution in situ.

    abstract：:In situ amorphization is a concept that allows to amorphize a given drug in its final dosage form right before administration. Hence, this approach can potentially be used to circumvent recrystallization issues that other amorphous formulation approaches are facing during storage. In this study, the feasibility of mic...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2017.01.035

    authors： Doreth M,Hussein MA,Priemel PA,Grohganz H,Holm R,Lopez de Diego H,Rades T,Löbmann K

    更新日期：2017-03-15 00:00:00

  • Evaluating tamsulosin hydrochloride-released microparticles prepared using single-step matrix coating.

    abstract：:The objective of the present study was to determine the optimum composition for sustained-release of tamsulosin hydrochloride from microparticles intended for orally disintegrating tablets. Microparticles were prepared from an aqueous ethylcellulose dispersion (Aquacoa®), and an aqueous copolymer based on ethyl acryla...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2011.01.053

    authors： Maeda A,Shinoda T,Ito N,Baba K,Oku N,Mizumoto T

    更新日期：2011-04-15 00:00:00

  • A novel image analysis methodology for online monitoring of nucleation and crystal growth during solid state phase transformations.

    abstract：:This study focuses on the development of an automated image analysis method to extract information on nucleation and crystal growth from polarized light micrographs. Using the developed image analysis method, four parameters related to nucleation and crystal growth could be extracted from the images. These parameters ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2012.04.074

    authors： Wu JX,Xia D,van den Berg F,Amigo JM,Rades T,Yang M,Rantanen J

    更新日期：2012-08-20 00:00:00

  • Fabrication and in vivo evaluation of ligand appended paclitaxel and artemether loaded lipid nanoparticulate systems for the treatment of NSCLC: A nanoparticle assisted combination oncotherapy.

    abstract：:The aim of present study was to develop folate appended PEGylated solid lipid nanoparticles(SLNs) of paclitaxel(FPS) and artemether(FAS). The SLNs were prepared by employing high pressure homogenization technique. The results of MTT assays revealed better cytotoxicity of FPS when given in combination with FAS on human...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2020.119386

    authors： Khatri H,Chokshi N,Rawal S,Patel BM,Badanthadka M,Patel MM

    更新日期：2020-06-15 00:00:00

  • Evaluation of the immunogenicity and in vivo toxicity of the antimicrobial peptide P34.

    abstract：:Immunogenicity and toxicity of antimicrobial peptide P34 were evaluated in vivo. BALB/c mice were inoculated intraperitoneally with peptide P34 alone and associated with Freund's adjuvant. For acute toxicity testing, different concentrations of the peptide P34 (82.5, 165.0, 247.5 and 330.0mg/kg) were orally administer...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2011.09.020

    authors： Vaucher Rde A,Velho Gewehr Cde C,Correa AP,Sant'Anna V,Ferreira J,Brandelli A

    更新日期：2011-12-12 00:00:00

  • Kinetics and mechanism of polymorphic transformation of sorbitol under mechanical milling.

    abstract：:In this paper, we present a kinetic investigation of the polymorphic transformation γ → α of sorbitol under milling in the objective to identify the microscopic mechanisms that govern this type of solid-state transformation. The milling was performed with a high energy planetary mill and the milled material was analys...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2020.119902

    authors： Dupont A,Guerain M,Danède F,Paccou L,Guinet Y,Hédoux A,Willart JF

    更新日期：2020-11-30 00:00:00

  • Physicochemical characterization techniques for lipid based delivery systems for siRNA.

    abstract：:siRNA based therapeutics is an emerging class of molecules with a high potential for fulfilling the promise of gene medicine. The high selectivity of siRNAs for their targets and subsequent gene ablation has been effectively demonstrated in a wide range of pre-clinical models. siRNA delivery in vivo has been most succ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章,评审

    doi：10.1016/j.ijpharm.2011.09.032

    authors： Kapoor M,Burgess DJ,Patil SD

    更新日期：2012-05-01 00:00:00

  • Ethanol effects on drug release from Verapamil Meltrex, an innovative melt extruded formulation.

    abstract：:The potential effect of ethanol to accelerate drug release from sustained release (SR) oral formulations is a general concern. Marketed Verapamil is a calcium channel blocker, mainly used as antihypertensive and anti-anginal drug and available in various dose and dosage forms. One is Verapamil Meltrex, combining an in...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2008.09.052

    authors： Roth W,Setnik B,Zietsch M,Burst A,Breitenbach J,Sellers E,Brennan D

    更新日期：2009-02-23 00:00:00

  • Combining ibuprofen sodium with cellulosic polymers: a deep dive into mechanisms of prolonged supersaturation.

    abstract：:The combination of a highly soluble salt form of a drug with a polymeric precipitation inhibitor has the potential to prolong drug supersaturation even following salt disproportionation. In this study, dissolution profiles of ibuprofen sodium in the presence of various cellulosic polymers, including hydroxypropyl meth...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2014.09.015

    authors： Terebetski JL,Michniak-Kohn B

    更新日期：2014-11-20 00:00:00

  • Dry powder inhalation of colistin sulphomethate in healthy volunteers: A pilot study.

    abstract：BACKGROUND:Pulmonary administration of the antimicrobial drugs colistin sulphomethate and tobramycin has been shown to be effective in slowing down pulmonary deterioration in cystic fibrosis (CF) patients. Both drugs are administered by liquid nebulisation, a technique known to have disadvantages. Dry powder inhalation...

    journal_title：International journal of pharmaceutics

    pub_type： 临床试验,杂志文章

    doi：10.1016/j.ijpharm.2006.11.021

    authors： Westerman EM,de Boer AH,Le Brun PPH,Touw DJ,Frijlink HW,Heijerman HGM

    更新日期：2007-04-20 00:00:00

  • Combinatorial design of passive drug delivery platforms.

    abstract：:We introduce a novel computational approach to designing passive drug delivery systems based on porous materials such as hydrogels. Our approach uses three tools: a method to establish the exact release pattern from all possible loading sites inside a given hydrogel; a method to generate a large number of hydrogel str...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2007.02.029

    authors： Casault S,Kenward M,Slater GW

    更新日期：2007-07-18 00:00:00

  • Comparison of in vitro cell models in predicting in vivo brain entry of drugs.

    abstract：:Although several in vitro models have been reported to predict the ability of drug candidates to cross the blood-brain barrier, their real in vivo relevance has rarely been evaluated. The present study demonstrates the in vivo relevance of simple unidirectional permeability coefficient (P(app)) determined in three in ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2010.09.016

    authors： Hakkarainen JJ,Jalkanen AJ,Kääriäinen TM,Keski-Rahkonen P,Venäläinen T,Hokkanen J,Mönkkönen J,Suhonen M,Forsberg MM

    更新日期：2010-12-15 00:00:00

  • Practical approach to prepare solid dispersion drug product using spherical silicate.

    abstract：:The purpose of this study is to establish a novel approach for preparing a solid dispersion drug product using spherical silicate by a Wurster-type fluidized bed granulator. The spherical silicate used in this study has porous structure and ideal particle size for loading by a Wurster-type fluidized bed granulator. As...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2014.08.016

    authors： Nagane K,Kimura S,Ukai K,Ogawa N,Yamamoto H

    更新日期：2014-11-20 00:00:00

  • A novel aqueous parenteral formulation of docetaxel using prodrugs.

    abstract：:The aim of this study is to develop an aqueous parenteral solution of docetaxel using prodrugs. Docetaxel (DTX) is a highly lipophilic drug and practically insoluble in water. To overcome insolubility of docetaxel, three kinds of docetaxel prodrugs were synthesized using succinyl linker such as DTX-G, DTX-L or DTX-S a...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2013.12.027

    authors： Park MH,Keum CG,Song JY,Kim D,Cho CW

    更新日期：2014-02-28 00:00:00

  • Mucoadhesive zein/beta-cyclodextrin nanoparticles for the buccal delivery of curcumin.

    abstract：:Herein, we have developed sprayable dispersions of mucoadhesive nanoparticles (NPs) made of zein, a hydrophobic plant-based protein, for the buccal delivery of curcumin (CUR), a poorly water-soluble polyphenol. NPs were prepared by the liquid-liquid dispersion method using an antisolvent water solution without or with...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2020.119587

    authors： Esposito D,Conte C,d'Angelo I,Miro A,Ungaro F,Quaglia F

    更新日期：2020-08-30 00:00:00

  • Blending of agglomerates into powders 1: Quantification of abrasion rate.

    abstract：:A very common situation in the pharmaceutical arena is that a small amount of cohesive drug substance needs to be distributed in a large bulk of free-flowing filler such as lactose. The key topic of attention is that aggregates of a cohesive drug substance need to be sufficiently broken up in an acceptable time-frame....

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2009.12.006

    authors： Willemsz TA,Oostra W,Hooijmaijers R,de Vegt O,Morad N,Vromans H,Frijlink HW,Van der Voort Maarschalk K

    更新日期：2010-03-15 00:00:00

  • Nanoparticles for direct nose-to-brain delivery of drugs.

    abstract：:This review aims to evaluate the evidence for the existence of a direct nose-to-brain delivery route for nanoparticles administered to the nasal cavity and transported via the olfactory epithelium and/or via the trigeminal nerves directly to the CNS. This is relevant in the field of drug delivery as well as for new de...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章,评审

    doi：10.1016/j.ijpharm.2009.06.019

    authors： Mistry A,Stolnik S,Illum L

    更新日期：2009-09-08 00:00:00

  • Induction of immunogenic cell death of cancer cells through nanoparticle-mediated dual chemotherapy and photothermal therapy.

    abstract：:The use of nanomedicines to induce immunogenic cell death is a new strategy that aims to increase tumor immunogenicity and thereby prime tumors for further immunotherapies. In this study, we developed a nanoparticle formulation for combinatory chemotherapy and photothermal therapy based only on materials previously us...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2020.119787

    authors： Heshmati Aghda N,Abdulsahib SM,Severson C,Lara EJ,Torres Hurtado S,Yildiz T,Castillo JA,Tunnell JW,Betancourt T

    更新日期：2020-09-06 00:00:00

  • Advances of nanosystems containing cyclodextrins and their applications in pharmaceuticals.

    abstract：:For many years, researchers have worked with supramolecular structures involving inclusion complexes with cyclodextrins. These studies have resulted in new commercially available drugs which have been of great benefit. More recently, studies using nanoparticles, including nanosystems containing cyclodextrins, have bec...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章,评审

    doi：10.1016/j.ijpharm.2019.01.041

    authors： Menezes PDP,Andrade TA,Frank LA,de Souza EPBSS,Trindade GDGG,Trindade IAS,Serafini MR,Guterres SS,Araújo AAS

    更新日期：2019-03-25 00:00:00

  • Critical factors in manufacturing multi-layer tablets--assessing material attributes, in-process controls, manufacturing process and product performance.

    abstract：:Advancement in the fields of material science, analytical methodologies, instrumentation, automation, continuous monitoring, feed forward/feed back control and comprehensive data collection have led to continual improvement of pharmaceutical tablet manufacturing technology, notably the multi-layer tablets. This review...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章,评审

    doi：10.1016/j.ijpharm.2010.07.025

    authors： Vaithiyalingam SR,Sayeed VA

    更新日期：2010-10-15 00:00:00

  • Facile synthesis of pH sensitive polymer-coated mesoporous silica nanoparticles and their application in drug delivery.

    abstract：:pH-responsive polymer shell chitosan/poly (methacrylic acid) (CS-PMAA) was coated on mesoporous silica nanoparticles (MSN) through the facile in situ polymerization method. The resultant composite microspheres showed a flexible control over shell thickness, surface charges and hydrodynamic size by adjusting the feedin...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2011.10.013

    authors： Tang H,Guo J,Sun Y,Chang B,Ren Q,Yang W

    更新日期：2011-12-15 00:00:00

  • Monitoring of the freezing stage in a freeze-drying process using IR thermography.

    abstract：:This paper presents a new Process Analytical Technology based on the use of an infrared camera and a mathematical model to estimate the ice crystal size distribution obtained at the end of the freezing stage of a vial freeze-drying process. Both empirical laws and first-principle based equations, already presented in ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2019.06.005

    authors： Colucci D,Maniaci R,Fissore D

    更新日期：2019-07-20 00:00:00

  • Preparation and quality assessment of itraconazole transfersomes.

    abstract：:Drug-loading transfersomes were prepared with itraconazole, a lipophilic drug, as a model drug to investigate the key factor affecting transfersomes quality and to evaluate their qualities. Drug-loading transfersomes were prepared using film dispersion method. The quality of transfersomes was evaluated by HPLC, transm...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2012.07.003

    authors： Zheng WS,Fang XQ,Wang LL,Zhang YJ

    更新日期：2012-10-15 00:00:00

  • Transdermal delivery of flurbiprofen from surfactant-based vesicles: particle characterization and the effect of water on in vitro transport.

    abstract：:Flurbiprofen loaded rigid and elastic vesicles comprising the bilayer-forming surfactant sucrose-ester laurate were prepared by the film rehydration and extrusion method. The charge-inducing agent sodium dodecyl sulfate, and the micelle-forming surfactants, sorbitan monolaurate, polyethylene glycol monolaurate, and po...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2013.12.051

    authors： Uchino T,Matsumoto Y,Murata A,Oka T,Miyazaki Y,Kagawa Y

    更新日期：2014-04-10 00:00:00

  • Polymeric micelles for the solubilization and delivery of STAT3 inhibitor cucurbitacins in solid tumors.

    abstract：:Poly(ethylene oxide)-block-poly(epsilon-caprolactone) (PEO-b-PCL) and newly developed poly(ethylene oxide)-block-poly(alpha-benzyl carboxylate epsilon-caprolactone) (PEO-b-PBCL) micelles were evaluated for the solubilization and delivery of cucurbitacin I and B, poorly water soluble inhibitors of signal transducer and...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2007.06.032

    authors： Molavi O,Ma Z,Mahmud A,Alshamsan A,Samuel J,Lai R,Kwon GS,Lavasanifar A

    更新日期：2008-01-22 00:00:00

  • Preparation and characterization of two-phase melt systems of lidocaine.

    abstract：:The melting point of lidocaine was significantly lowered when mixed with thymol and/or aqueous ethanol. Mixtures of lidocaine and thymol at ratios within the range of 30:70-70:30 (w:w) became homogeneous oils at 25 degrees C. In a pH 9.2 carbonate buffer containing 25% ethanol, lidocaine (5%, w:w) also liquefied at 25...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/s0378-5173(01)00689-5

    authors： Kang L,Jun HW,Mani N

    更新日期：2001-07-03 00:00:00

  • Carrier mediated uptake of L-tyrosine and its competitive inhibition by model tyrosine linked compounds in a rabbit corneal cell line (SIRC)--strategy for the design of transporter/receptor targeted prodrugs.

    abstract：:The objective of this study was to investigate the presence of amino acid transporters on the corneal epithelium and to enhance corneal drug absorption through prodrug modification targeted to the amino acid transporters. SIRC was used as a model cell line representing the corneal epithelium. Uptake studies were carri...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/s0378-5173(02)00405-2

    authors： Balakrishnan A,Jain-Vakkalagadda B,Yang C,Pal D,Mitra AK

    更新日期：2002-10-24 00:00:00