当前位置： SCI文献检索 > INTERNATIONAL JOURNAL OF PHARMACEUTICS期刊下所有文献 > Improved pH-dependent drug release and oral exposure of telmisartan, a poorly soluble drug through the formation of drug-aminoclay complex.

Improved pH-dependent drug release and oral exposure of telmisartan, a poorly soluble drug through the formation of drug-aminoclay complex.

Abstract：

:Telmisartan (TEL) belongs to BCS class II (low solubility/high permeability) and exhibits the pH-dependent drug release. Since 3-aminopropyl functionalized magnesium phyllosilicate (aminoclay) can intercalate or adsorb the negatively charged molecules via the electrostatic interaction, TEL-aminoclay complex was synthesized to improve the pH dependent drug release and the oral exposure of TEL. Co-precipitation method was adopted to incorporate TEL into aminoclay with the variation of drug/aminoclay ratios, and then dissolution profiles of TEL from TEL-aminoclay complex were evaluated at different pHs. Structural characterization was performed by XRD, ATR-FTIR, and TEM, indicating the electrostatic interaction between TEL and the surface of the aminoclay lamellae. Furthermore, drug crystallinity was changed to an amorphous form via the molecular interactions between TEL and aminoclay. TEL exhibited rapid and complete dissolution at pH 1.2 within 15 min from all the tested formulations. However, while the untreated powder indicated negligible dissolution at pH 4 and pH 6.8, the formation of drug-clay complex significantly improved the dissolution rate as well as the extent of drug release at the higher pHs. In addition, following an oral administration of TEL-aminoclay, Cmax and AUC of TEL increased by about 8 and 5 fold respectively, while Tmax was shorten. The results suggest that formation of aminoclay complex should be promising to enhance the bioavailability of a poorly soluble drug, TEL.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Yang L,Shao Y,Han HK

doi

10.1016/j.ijpharm.2014.05.009

subject

Has Abstract

pub_date

2014-08-25 00:00:00

pages

258-63

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(14)00326-3

journal_volume

471

pub_type

杂志文章

相关文献

INTERNATIONAL JOURNAL OF PHARMACEUTICS文献大全
  • Does ciprofloxacin interact with neutral bilayers? An aspect related to its antimicrobial activity.

    abstract：:Ciprofloxacin (CPX) physicochemical properties, mainly hydrophobicity and microspeciation, appear to be related with the ability of this drug to adsorb and diffuse through lipid environments. We have combined the information from fluorescence anisotropy, quenching and epifluorescence of phospholipid monolayers, to exp...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/s0378-5173(02)00633-6

    authors： Hernández-Borrell J,Montero MT

    更新日期：2003-02-18 00:00:00

  • Applications of NIR spectroscopy to monitoring and analyzing the solid state during industrial crystallization processes.

    abstract：:Fiber-optic near infrared (NIR) spectroscopy was used to investigate several key features of the polymorphic transitions observed during the crystallization and the filtration of SaC, an Active Pharmaceutical Ingredient (API) produced by Sanofi-Synthelabo. Using few samples, the spectroscopic data were calibrated to p...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2004.01.003

    authors： Févotte G,Calas J,Puel F,Hoff C

    更新日期：2004-04-01 00:00:00

  • Exosomes: From garbage bins to translational medicine.

    abstract：:Exosomes are lipid bilayer-enclosed vesicles of endosomal origin, which initially considered as garbage bins to dispose unwanted cellular components, but they are now emerged as an intercellular communication system involved in several physiological and pathological conditions. With the increasing understanding that t...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章,评审

    doi：10.1016/j.ijpharm.2020.119333

    authors： Liu Y,Wang Y,Lv Q,Li X

    更新日期：2020-06-15 00:00:00

  • In vitro experiment optimization for measuring tetrahydrocannabinol skin permeation.

    abstract：:The purpose of this study was to optimize in vitro experimental conditions for the measurement of Delta(9)-tetrahydrocannabinol (Delta(9)-THC) permeation across human skin using a flow-through diffusion cell system. The drug permeation rates through intact and stripped (stratum corneum (SC) removed) skin were also com...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/s0378-5173(02)00262-4

    authors： Challapalli PV,Stinchcomb AL

    更新日期：2002-07-25 00:00:00

  • Novel in situ gelling ophthalmic drug delivery system based on gellan gum and hydroxyethylcellulose: Innovative rheological characterization, in vitro and in vivo evidence of a sustained precorneal retention time.

    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

    authors： Destruel PL,Zeng N,Seguin J,Douat S,Rosa F,Brignole-Baudouin F,Dufaÿ S,Dufaÿ-Wojcicki A,Maury M,Mignet N,Boudy V

    更新日期：2020-01-25 00:00:00

  • A mechanism on the drug release into a perfect sink from a coated planar matrix with a super-saturation loading in the core.

    abstract：:A comprehensive model is proposed to accurately describe drug release kinetics from a coated plane sheet when drug loading in the core is above its saturation level. The general solutions are acquired in a dimensionless form by the Laplace transform and the solution for the special case-a perfect sink condition, is de...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/s0378-5173(99)00373-7

    authors： Tongwen X,Binglin H

    更新日期：2000-03-20 00:00:00

  • The influence of formulation variables on in vitro transfection efficiency and physicochemical properties of chitosan-based polyplexes.

    abstract：:The aim of this study was to investigate how a selection of formulation variables affects the in vitro transfection efficiency and physicochemical properties (particle size, zetapotential and chitosan-plasmid association) of chitosan-based polyplexes. Experimental designs in combination with multivariate data analysis...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/s0378-5173(03)00301-6

    authors： Romøren K,Pedersen S,Smistad G,Evensen Ø,Thu BJ

    更新日期：2003-08-11 00:00:00

  • Effects of carriers and storage of formulation on the lung deposition of a hydrophobic and hydrophilic drug from a DPI.

    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

    authors： Harjunen P,Lankinen T,Salonen H,Lehto VP,Järvinen K

    更新日期：2003-09-16 00:00:00

  • Physicochemical properties of tamoxifen hemicitrate sesquihydrate.

    abstract：:A novel modification of tamoxifen [(Z)-2-[4-(1,2-diphenyl-1-butenyl) phenoxy]-N,N-dimethylethylamine] citrate, tamoxifen hemicitrate hydrate was prepared. The crystalline form was identified and characterized by powder and single crystal X-ray diffractometries, differential scanning calorimetry (DSC), thermal gravimet...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2007.10.021

    authors： Kojima T,Katoh F,Matsuda Y,Teraoka R,Kitagawa S

    更新日期：2008-03-20 00:00:00

  • MALDI mass spectrometry imaging as a complementary analytical method for improved skin distribution analysis of drug molecule and excipients.

    abstract：:In cutaneous drug delivery, it is widely accepted that the choice of excipients affects the delivery of a drug molecule to the skin. MALDI mass spectrometry imaging (MALDI-MSI) is an imaging technique which enables the simultaneous detection of multiple compounds. MALDI-MSI was applied to study the penetration of tofa...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2020.119949

    authors： Handler AM,Fallah M,Just Pedersen A,Pommergaard Pedersen G,Troensegaard Nielsen K,Janfelt C

    更新日期：2020-11-30 00:00:00

  • Polymer sutures for simultaneous wound healing and drug delivery - A review.

    abstract：:Drug delivery using suitable polymeric devices has gathered momentum in the recent years due to their remarkable properties. The versatility of polymeric materials makes them reliable candidates for site targeted drug release. Among them biodegradable sutures has received considerable attention because they offer grea...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章,评审

    doi：10.1016/j.ijpharm.2017.03.041

    authors： Joseph B,George A,Gopi S,Kalarikkal N,Thomas S

    更新日期：2017-05-30 00:00:00

  • Distinct transduction modes of arginine-rich cell-penetrating peptides for cargo delivery into tumor cells.

    abstract：:The application of cell-penetrating peptides (CPPs) for delivering various cargo molecules with biological functions into cells has gained much attention in recent years. However, the internalization mechanisms and delivery properties of CPP-cargo remains controversial. In this study, low- and high-molecular-weight ca...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2011.08.001

    authors： Ma DX,Shi NQ,Qi XR

    更新日期：2011-10-31 00:00:00

  • Poly(epsilon-caprolactone) and Eudragit microparticles containing fludrocortisone acetate.

    abstract：:Substitutive hormonal therapies have to be administered for long periods. Thus, the development of sustained-release forms, as microparticle suspensions, is interesting in order to improve patient compliance by reducing dosing frequencies and side effects. The aim of this work was to compare different formulations of ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2003.09.040

    authors： Gibaud S,Jabir Al Awwadi N,Ducki C,Astier A

    更新日期：2004-01-28 00:00:00

  • Danshen extract does not alter pharmacokinetics of docetaxel and clopidogrel, reflecting its negligible potential in P-glycoprotein- and cytochrome P4503A-mediated herb-drug interactions.

    abstract：:Danshen (Salvia miltiorrhiza) contains tanshinones, which inhibit P-glycoprotein (P-gp) and the cytochrome P450 (CYP) system. In the present study, we evaluated the possible pharmacokinetic interactions of Danshen extract with docetaxel and clopidogrel in rats. Docetaxel (5 mg/kg intravenously and 40 mg/kg orally) or ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2011.03.031

    authors： Lee JH,Shin YJ,Kim HJ,Oh JH,Jang YP,Lee YJ

    更新日期：2011-05-30 00:00:00

  • Gastroretentive drug delivery system of DA-6034, a new flavonoid derivative, for the treatment of gastritis.

    abstract：:A gastroretentive drug delivery system of DA-6034, a new synthetic flavonoid derivative, for the treatment of gastritis was developed by using effervescent floating matrix system (EFMS). The therapeutic limitations of DA-6034 caused by its low solubility in acidic conditions were overcome by using the EFMS, which was ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2007.12.042

    authors： Jang SW,Lee JW,Park SH,Kim JH,Yoo M,Na DH,Lee KC

    更新日期：2008-05-22 00:00:00

  • A thermo-responsive and self-healing liposome-in-hydrogel system as an antitubercular drug carrier for localized bone tuberculosis therapy.

    abstract：:Isoniazid (INH) is a first-line therapy for bone tuberculosis (TB), but its clinic benefits are limited by severe side-effects after long-time administration. While nano-drug delivery systems present as promising strategies for INH delivery, the therapeutic efficacies are usually suboptimal due to ineffective drug acc...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2018.12.083

    authors： Liu P,Guo B,Wang S,Ding J,Zhou W

    更新日期：2019-03-10 00:00:00

  • Small-scale preparation of perfluorocarbon-nanoemulsions utilizing dual centrifugation.

    abstract：BACKGROUND:Perfluorocarbon-nanoemulsions (PFC-NE) made of PFC and phospholipids (PL) by homogenization are optimal for in vivo-19F labelling of monocytes and subsequently of inflamed tissues in magnetic resonance imaging (MRI). Necessary requirements for in vivo use of PFC-NE are sterility, suitable droplet sizes and t...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2019.118753

    authors： Krämer W,Schubert R,Massing U

    更新日期：2019-12-15 00:00:00

  • Air classifier technology (ACT) in dry powder inhalation. Part 2. The effect of lactose carrier surface properties on the drug-to-carrier interaction in adhesive mixtures for inhalation.

    abstract：:The effect of carrier surface properties on drug particle detachment from carrier crystals during inhalation with a special test inhaler with basic air classifier has been studied for mixtures containing 0.4% budesonide. Carrier crystals were retained in the classifier during inhalation and subsequently examined for t...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/s0378-5173(03)00264-3

    authors： de Boer AH,Hagedoorn P,Gjaltema D,Goede J,Kussendrager KD,Frijlink HW

    更新日期：2003-07-24 00:00:00

  • Gelatin-based membrane containing usnic acid-loaded liposome improves dermal burn healing in a porcine model.

    abstract：:There are a range of products available which claim to accelerate the healing of burns; these include topical agents, interactive dressings and biomembranes. The aim of this study was to assess the effect of a gelatin-based membrane containing usnic acid/liposomes on the healing of burns in comparison to silver sulfad...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2016.09.040

    authors： Nunes PS,Rabelo AS,Souza JC,Santana BV,da Silva TM,Serafini MR,Dos Passos Menezes P,Dos Santos Lima B,Cardoso JC,Alves JC,Frank LA,Guterres SS,Pohlmann AR,Pinheiro MS,de Albuquerque RL Júnior,Araújo AA

    更新日期：2016-11-20 00:00:00

  • The novel immunogenic chimeric peptide vaccine to elicit potent cellular and mucosal immune responses against HTLV-1.

    abstract：:This study reports on the immunogenicity assessment of a novel chimeric peptide vaccine including Tax, gp21, gp46, and gag immunodominant epitopes of human T-cell lymphotropic virus type 1 (HTLV-1) to induce immunity against HTLV-1 after subcutaneous (SC) or intranasal administration in a mice model. Additionally, to ...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2018.07.069

    authors： Kabiri M,Sankian M,Hosseinpour M,Tafaghodi M

    更新日期：2018-10-05 00:00:00

  • Impact of blend properties on die filling during tableting.

    abstract：:Based on characterization of a wide range of fillers and APIs, thirty divergent blends were composed and subsequently compressed on a rotary tablet press, varying paddle speed and turret speed. The tablet weight variability was determined of 20 grab samples consisting of each 20 tablets. Additionally, the bulk residen...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2018.08.015

    authors： Van Snick B,Grymonpré W,Dhondt J,Pandelaere K,Di Pretoro G,Remon JP,De Beer T,Vervaet C,Vanhoorne V

    更新日期：2018-10-05 00:00:00

  • Maintaining a frozen shipping environment for Phase I clinical trial distribution.

    abstract：:The need for stringent temperature control provides significant challenges to pharmaceutical distributors operating in all sectors of the industry. Products with a frozen storage label requirement can be significantly problematic. This study aimed to provide evidence of robust and reproducible frozen shipment arrangem...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2007.06.008

    authors： Elliott MA,Halbert GW

    更新日期：2008-01-04 00:00:00

  • Modified local diatomite as potential functional drug carrier--A model study for diclofenac sodium.

    abstract：:Diatomite makes a promising candidate for a drug carrier because of its high porosity, large surface area, modifiable surface chemistry and biocompatibility. Herein, refined diatomite from Kolubara coal basin, which complied with the pharmacopoeial requirements for heavy metals content and microbiological quality, was...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2015.10.047

    authors： Janićijević J,Krajišnik D,Čalija B,Vasiljević BN,Dobričić V,Daković A,Antonijević MD,Milić J

    更新日期：2015-12-30 00:00:00

  • The influence of excipients on the diffusion of ibuprofen and paracetamol in gastric mucus.

    abstract：:The aim of this study was to examine the diffusion of commonly administered analgesics, ibuprofen and paracetamol, through gastric mucus. As ibuprofen and paracetamol are often formulated with alkalising excipients, or are commonly co-administered with antacids that have been demonstrated to alter their absorption, di...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2004.11.028

    authors： Shaw LR,Irwin WJ,Grattan TJ,Conway BR

    更新日期：2005-02-16 00:00:00

  • The influence of plate design on the properties of pellets produced by extrusion and spheronization.

    abstract：:The aim of this work was to produce pellets using a standard formulation by means of extrusion and spheronization. Three different spheroniser friction plate patterns (i.e. cross-hatch, radial, striated edge pattern) have been used in order to investigate whether the plate pattern affects physical properties of the pe...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2012.05.050

    authors： Michie H,Podczeck F,Newton JM

    更新日期：2012-09-15 00:00:00

  • One-week in vivo sustained release of a peptide formulated into in situ forming implants.

    abstract：:The LR12 peptide has been reported to reduce the size of infarct and improve both cardiac function and survival in myocardial infarction in murine models, after daily repeated intraperitoneal injections. In order to protect peptide from degrading and to prolong its release, in situ implants based on biocompatible biod...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2017.02.046

    authors： Parent M,Clarot I,Gibot S,Derive M,Maincent P,Leroy P,Boudier A

    更新日期：2017-04-15 00:00:00

  • Preparation of cyclosporine A nanoparticles by evaporative precipitation into aqueous solution.

    abstract：:Amorphous nanoparticle suspensions of a poorly water-soluble drug, cyclosporine A, are produced by a new process, evaporative precipitation into aqueous solution (EPAS). The rapid evaporation of a heated organic solution of the drug, which is atomized into an aqueous solution, results in fast nucleation leading to nan...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/s0378-5173(02)00147-3

    authors： Chen X,Young TJ,Sarkari M,Williams RO 3rd,Johnston KP

    更新日期：2002-08-21 00:00:00

  • Effect of process parameters on compressibility of granulation manufactured in a high-shear mixer.

    abstract：:Various processing variables that can influence granulation characteristics of a lactose-based formulation were evaluated using a Plackett-Burman experimental design. These parameters were impeller speed, granulating solution addition rate, total amount of water added in the granulation step, wet massing time, moistur...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/s0378-5173(99)00445-7

    authors： Badawy SI,Menning MM,Gorko MA,Gilbert DL

    更新日期：2000-03-30 00:00:00

  • Stability study of amorphous valdecoxib.

    abstract：:Formulation of poorly water-soluble drugs in the most stable dosage form for oral delivery perhaps presents the greatest challenge to pharmaceutical industry. Physical transformation of drug substance into its more soluble but metastable amorphous form is one of the approaches for improving dissolution rate of such dr...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章

    doi：10.1016/j.ijpharm.2004.06.009

    authors： Ambike AA,Mahadik KR,Paradkar A

    更新日期：2004-09-10 00:00:00

  • Recent advances in local drug delivery to the inner ear.

    abstract：:Inner ear diseases are not adequately treated by systemic drug administration mainly because of the blood-perilymph barrier that reduces exchanges between plasma and inner ear fluids. Local drug delivery methods including intratympanic and intracochlear administrations are currently developed to treat inner ear disord...

    journal_title：International journal of pharmaceutics

    pub_type： 杂志文章,评审

    doi：10.1016/j.ijpharm.2015.08.015

    authors： El Kechai N,Agnely F,Mamelle E,Nguyen Y,Ferrary E,Bochot A

    更新日期：2015-10-15 00:00:00