Formulation study and evaluation of matrix and three-layer tablet sustained drug delivery systems based on Carbopols with isosorbite mononitrate.

Abstract:

:The purpose of this research was to develop and evaluate different preparations of sustained delivery systems, using Carbopols as carriers, in the form of matrices and three-layer tablets with isosorbite mononitrate. Matrix tablets were prepared by direct compression whereas three-layer tablets were prepared by compressing polymer barrier layers on both sides of the core containing the drug. The findings of the study indicated that all systems demonstrated sustained release. The properties of the polymer used and the structure of each formulation appear to considerably affect drug release and its release rate. The three-layer formulations exhibit lower drug release compared to the matrices. This was due to the fact that the barrier-layers hindered the penetration of liquid into the core and modified drug dissolution and release. The geometrical characteristics/structure of the tablets as well as the weight/thickness of the barriers-layers considerably influence the rate of drug release and the release mechanisms. Kinetic analysis of the data indicated that drug release from matrices was mainly attributed to Fickian diffusion while three-layer tablets exhibited either anomalous diffusion or erosion/relaxation mechanisms. The advantage of Carbopol formulations is that a range of release profiles can easily be obtained through variations in tablet structure and thus Carbopols are appropriate carriers of oral sustained drug delivery systems for soluble drugs such as the isosorbite mononitrate.

journal_name

AAPS PharmSciTech

journal_title

AAPS PharmSciTech

authors

Efentakis M,Peponaki C

doi

10.1208/s12249-008-9084-2

subject

Has Abstract

pub_date

2008-01-01 00:00:00

pages

917-23

issue

3

issn

1530-9932

journal_volume

9

pub_type

杂志文章
  • Solubilization of cyclosporin A.

    abstract::This study investigated the solubilization of cyclosporin A (CsA), a neutral undecapeptide, by cosolvency, micellization, and complexation. Cosolvents (ethanol, propylene glycol, polyethylene glycol, tetrahydrofurfuryl alcohol polyethyleneglycol ether, and glycerin), surfactants (polyoxyethylene sorbitan monooleate [(...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt020102

    authors: Ran Y,Zhao L,Xu Q,Yalkowsky SH

    更新日期:2001-01-18 00:00:00

  • Effect of hydrophilic polymers on buccoadhesive Eudragit patches of propranolol hydrochloride using factorial design.

    abstract::The purpose of this study was to develop formulations and systematically evaluate in vitro performances of buccoadhesive patches of propranolol hydrochloride using the hydrophobic polymer Eudragit L-100 as the base matrix. The hydrophilic polymers Carbopol 934 and polyvinyl pyrrolidone (PVP) K30 were incorporated into...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt0802045

    authors: Patel VM,Prajapati BG,Patel MM

    更新日期:2007-06-22 00:00:00

  • Modeling of the Nanoparticles Absorption Under a Gastrointestinal Simulated Ambient Condition.

    abstract::Proanthocyanidins (PAs) have several bioactivities, but they are unstable in the digestive tract and possess low bioavailability. Nanoencapsulation stabilizes these compounds for oral administration. The intestinal absorption of grape seed and skin extracts, and the poly-lactic acid (PLA) nanoparticles loaded with suc...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0751-z

    authors: Fernández K,Roeckel M,Canales E,Dumont J

    更新日期:2017-10-01 00:00:00

  • Chitosan gels for the vaginal delivery of lactic acid: relevance of formulation parameters to mucoadhesion and release mechanisms.

    abstract::The aim of this work was to assess the effect of formulation parameters of a mucoadhesive vaginal gel based on chitosan and lactic acid, and to highlight its release mechanisms. Two molecular weight chitosans were used to prepare gels with 2 lactic acid concentrations. Both chitosan molecular weight and lactic acid co...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt0704104

    authors: Bonferoni MC,Giunchedi P,Scalia S,Rossi S,Sandri G,Caramella C

    更新日期:2006-01-01 00:00:00

  • Biodegradation and in vivo biocompatibility of rosin: a natural film-forming polymer.

    abstract::The specific aim of the present study was to investigate the biodegradation and biocompatibility characteristics of rosin, a natural film-forming polymer. Both in vitro as well as in vivo methods were used for assessment of the same. The in vitro degradation of rosin films was followed in pH 7.4 phosphate buffered sal...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt040455

    authors: Satturwar PM,Fulzele SV,Dorle AK

    更新日期:2003-10-22 00:00:00

  • An investigation into the influence of experimental conditions on in vitro drug release from immediate-release tablets of levothyroxine sodium and its relation to oral bioavailability.

    abstract::The aim of this study was to investigate the influence of experimental conditions on levothyroxine sodium release from two immediate-release tablet formulations which narrowly passed the standard requirements for bioequivalence studies. The in vivo study was conducted as randomised, single-dose, two-way cross-over pha...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-011-9660-8

    authors: Kocic I,Homsek I,Dacevic M,Parojcic J,Miljkovic B

    更新日期:2011-09-01 00:00:00

  • Preparation and Characterization of Minoxidil Loaded Nanostructured Lipid Carriers.

    abstract::Nanostructured lipid carriers (NLCs) are interesting delivery systems for enhancing the penetration of an active substance through the skin after topical administration. The present paper described the development of a novel NLCs for minoxidil (MXD) topical delivery. Stearic acid and oleic acid that showed the highest...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-016-0519-x

    authors: Wang W,Chen L,Huang X,Shao A

    更新日期:2017-02-01 00:00:00

  • Simultaneous Evaluation of Dissolution and Permeation of Oral Drug Solid Formulations for Predicting Absorption Rate-Limiting Factors and In Vitro-In Vivo Correlations: Case Study Using a Poorly Soluble Weakly Basic Drug.

    abstract::Combined dissolution and permeation systems are designed to simultaneously assess the dissolution of a pharmaceutical dosage form and the permeation of dissolved drugs therefrom. However, there were still some limitations on predicting the possible absorption rate-limiting steps and improving the in vitro-in vivo corr...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1544-3

    authors: Li Z,He X,Tian S,Feng G,Huang C,Xun M,Wu Z,Wang Y

    更新日期:2019-10-24 00:00:00

  • Direct compression behavior of low- and high-methoxylated pectins.

    abstract::The objective of this study was to evaluate possible usefulness of pectins for direct compression of tablets. The deformation behavior of pectin grades of different degree of methoxylation (DM), namely, 5%, 10%, 25%, 35%, 40%, 50%, and 60% were, examined in terms of yield pressures (YP) derived from Heckel profiles fo...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-009-9349-4

    authors: Salbu L,Bauer-Brandl A,Tho I

    更新日期:2010-03-01 00:00:00

  • Formulation and In Vitro Release Kinetics of Mucoadhesive Blend Gels Containing Matrine for Buccal Administration.

    abstract::Enterovirus 71 (EV71) is a pathogenic factor of severe hand, foot, and mouth disease (HFMD). No vaccine or specific treatment is currently available for EV71 infection. Hence, we developed a buccal mucoadhesive gel containing matrine to protect against HFMD. Mucoadhesive gels were prepared by Carbopol 974P and were co...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0853-7

    authors: Chen X,Yan J,Yu S,Wang P

    更新日期:2018-01-01 00:00:00

  • Isolation, Formulation, and Efficacy Enhancement of Morin Emulsified Carriers Against Lung Toxicity in Rats.

    abstract::The present study demonstrates a preparative medium-pressure liquid chromatography (MPLC) method for isolation of Morin besides evaluating its efficacy in comparison with its self-nanoemulsifying drug delivery (SNEDD) and nanoemulsion (NE) systems against in-vivo HgCl2-induced lung toxicity in rats. Morin was isolated...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1072-6

    authors: El-Haddad AE,Sheta NM,Boshra SA

    更新日期:2018-07-01 00:00:00

  • Use of Risk Assessment and Plackett-Burman Design for Developing Resveratrol Spray-Dried Emulsions: a Quality-by-Design Approach.

    abstract::In this study, the resveratrol spray-dried emulsions were developed using a quality-by-design approach. Further, the product and process factors that affected the quality of the spray-dried emulsions were analyzed and illustrated using an Ishikawa diagram. The product and process risks were prioritized using a risk-ra...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1220-z

    authors: Benjasirimongkol P,Piriyaprasarth S,Moribe K,Sriamornsak P

    更新日期:2018-12-18 00:00:00

  • Pharmacokinetic Study of Ferulic Acid Following Transdermal or Intragastric Administration in Rats.

    abstract::Ferulic acid is contained in some Chinese herbal medicines such as Ligusticum chuanxiong or Angelica sinensis. Studies have focused on the treatment of inflammatory diseases and pain using ferulic acid. However, little is known about its pharmacokinetics after transdermal administration. The present research investiga...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-01709-w

    authors: Yan N,Tang Z,Xu Y,Li X,Wang Q

    更新日期:2020-06-08 00:00:00

  • Development and Evaluation of Astaxanthin as Nanostructure Lipid Carriers in Topical Delivery.

    abstract::The study is designed to formulate, optimize, and evaluate astaxanthin (ASTA)-loaded nanostructured lipid carrier (NLC) with an aim to improve its stability, water solubility, skin permeability and retention and reduce drug-related side effects. ASTA was extracted from Haematococcus pluvialis. ASTA-NLC was formulated ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-01822-w

    authors: Geng Q,Zhao Y,Wang L,Xu L,Chen X,Han J

    更新日期:2020-11-11 00:00:00

  • Antiproliferative Activity and VEGF Expression Reduction in MCF7 and PC-3 Cancer Cells by Paclitaxel and Imatinib Co-encapsulation in Folate-Targeted Liposomes.

    abstract::Co-encapsulation of anticancer drugs paclitaxel and imatinib in nanocarriers is a promising strategy to optimize cancer treatment. Aiming to combine the cytotoxic and antiangiogenic properties of the drugs, a liposome formulation targeted to folate receptor co-encapsulating paclitaxel and imatinib was designed in this...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0830-1

    authors: Peres-Filho MJ,Dos Santos AP,Nascimento TL,de Ávila RI,Ferreira FS,Valadares MC,Lima EM

    更新日期:2018-01-01 00:00:00

  • Stability of a second-generation cephalosporin veterinary mastitis formulation after electron beam irradiation.

    abstract::This study focused on the chemical stability of the cephalosporin (6R, 7R)-7-(1-pentafluorophenoxyacetamido)-3-[2-(5-methyl-1,3,4-thiodiazolyl)thiomethyl]-Delta(3)-cephem-4-carboxylic acid, sodium salt (cephem 1) formulation after electron beam (e-beam) irradiation. The cephem 1 concentrations of samples irradiated at...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt020423

    authors: Johns PJ,Turberg M,Willard K,Matagne D,Cheesman D

    更新日期:2001-11-19 00:00:00

  • Prediction of Dissolution of Sustained Release Coated Ciprofloxacin Beads Using Near-infrared Spectroscopy and Process Parameters: a Data Fusion Approach.

    abstract::The aim of the work is to develop a data fusion model using near-infrared (NIR) and process parameters for the predictions of drug dissolution from controlled release multiparticulate beads. Using a design of experiments, ciprofloxacin-coated beads were manufactured and critical process parameters such as air volume, ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1401-4

    authors: Ibrahim A,Kothari BH,Fahmy R,Hoag SW

    更新日期:2019-06-18 00:00:00

  • Melt Extrusion for a High Melting Point Compound with Improved Solubility and Sustained Release.

    abstract::The objective of the current study was to develop an amorphous solid dispersion for a high melting point compound, griseofulvin (GRF), with an enhanced solubility and a controlled release pattern utilizing hot melt extrusion (HME) technology. Hypromellose acetate succinate (HPMCAS, Shin-Etsu AQOAT®, medium particle si...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0846-6

    authors: Lu J,Obara S,Liu F,Fu W,Zhang W,Kikuchi S

    更新日期:2018-01-01 00:00:00

  • Spray-Dried Succinylated Soy Protein Microparticles for Oral Ibuprofen Delivery.

    abstract::The potential value of succinylated soy protein (SPS) as a wall material for the encapsulation of ibuprofen (IBU), a model hydrophobic drug, by spray-drying was investigated. A succinylation rate of 93% was obtained for soy protein isolate, with a molar ratio of 1/1.5 (NH2/succinic anhydride). The solubility profile a...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1250-6

    authors: Anaya Castro MA,Alric I,Brouillet F,Peydecastaing J,Fullana SG,Durrieu V

    更新日期:2019-01-11 00:00:00

  • Transdermal Microneedles-A Materials Perspective.

    abstract::Transdermal drug delivery is an emerging field in the pharmaceutical remit compared with conventional methods (oral and parenteral). Microneedle (MN)-based devices have gained significant interest as a strategy to overcome the skin's formidable barrier: the stratum corneum. This approach provides a less invasive, more...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,评审

    doi:10.1208/s12249-019-1560-3

    authors: Ali R,Mehta P,Arshad MS,Kucuk I,Chang MW,Ahmad Z

    更新日期:2019-12-05 00:00:00

  • Characterization and In Vitro Evaluation of the Complexes of Posaconazole with β- and 2,6-di-O-methyl-β-cyclodextrin.

    abstract::Posaconazole is a triazole antifungal drug that with extremely poor aqueous solubility. Up to now, this drug can be administered via intravenous injection and oral suspension. However, its oral bioavailability is greatly limited by the dissolution rate of the drug. This study aimed to improve water solubility and diss...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-016-0497-z

    authors: Tang P,Wang L,Ma X,Xu K,Xiong X,Liao X,Li H

    更新日期:2017-01-01 00:00:00

  • Investigation of Effect of Isopropyl Palmitate on Drug Release from Transdermal Patch and Molecular Dynamics Study.

    abstract::Chemical penetration enhancers are widely used in transdermal drug delivery system. However, few studies have focused on changes of concentration in chemical penetration enhancers. In this study, the effect of concentrations of enhancers on drug release and its mechanism were investigated. Zolmitriptan (ZOL) was used ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1370-7

    authors: Ruan J,Wan X,Quan P,Liu C,Fang L

    更新日期:2019-04-25 00:00:00

  • Highly Soluble Glimepiride and Irbesartan Co-amorphous Formulation with Potential Application in Combination Therapy.

    abstract::One-third of the population of the USA suffers from metabolic syndrome (MetS). Treatment of patients with MetS regularly includes drugs prescribed simultaneously to treat diabetes and cardiovascular diseases. Therefore, the development of novel multidrug formulations is recommended. However, the main problem with thes...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1359-2

    authors: Cruz-Angeles J,Videa M,Martínez LM

    更新日期:2019-03-18 00:00:00

  • Pulmonary and Regional Deposition of Nebulized and Dry Powder Aerosols in Ferrets.

    abstract::The utilization of ferrets as a non-clinical model for disease is rapidly increasing within drug development. Many of these models include respiratory diseases that involve targeted drug delivery via nose-only inhalation. While the deposition patterns within other non-clinical models (mice, rats, canines, and non-huma...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1382-3

    authors: Kuehl PJ,Chand R,McDonald JD,Hava DL,DeHaan WH

    更新日期:2019-07-01 00:00:00

  • Preparation of gelatin microbeads with a narrow size distribution using microchannel emulsification.

    abstract::The purpose of this study was to prepare monodisperse gelatin microcapsules containing an active agent using microchannel (MC) emulsification, a novel technique for preparing water-in-oil (W/O) and oil-in-water (O/W) emulsions. As the first step in applying MC emulsification to the preparation of monodisperse gelatin ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt030325

    authors: Iwamoto S,Nakagawa K,Sugiura S,Nakajima M

    更新日期:2002-01-01 00:00:00

  • Stage 2 Process Performance Qualification (PPQ): a Scientific Approach to Determine the Number of PPQ Batches.

    abstract::The approach documented in this article reviews data from earlier process validation lifecycle stages with a described statistical model to provide the "best estimate" on the number of process performance qualification (PPQ) batches that should generate sufficient information to make a scientific and risk-based decisi...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,评审

    doi:10.1208/s12249-015-0409-7

    authors: Pazhayattil A,Alsmeyer D,Chen S,Hye M,Ingram M,Sanghvi P

    更新日期:2016-08-01 00:00:00

  • The Sensitivity of In Vitro Permeation Tests to Chemical Penetration Enhancer Concentration Changes in Fentanyl Transdermal Delivery Systems.

    abstract::Chemical penetration enhancers (CPEs) are frequently incorporated into transdermal delivery systems (TDSs) to improve drug delivery and to reduce the required drug load in formulations. However, the minimum detectable effect of formulation changes to CPE-containing TDSs using in vitro permeation tests (IVPT), a widely...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1130-0

    authors: Shin SH,Srivilai J,Ibrahim SA,Strasinger C,Hammell DC,Hassan HE,Stinchcomb AL

    更新日期:2018-10-01 00:00:00

  • Influence of Polyvinyl Alcohol (PVA) on PVA-Poly-N-hydroxyethyl-aspartamide (PVA-PHEA) Microcrystalline Solid Dispersion Films.

    abstract::This study was conducted to formulate buccal films consisting of polyvinyl alcohol (PVA) and poly-N-hydroxyethyl-aspartamide (PHEA), to improve the dissolution of the drug through the oral mucosa. Ibuprofen sodium salt was used as a model drug, and the buccal film was expected to enhance its dissolution rate. Two diff...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-01811-z

    authors: Al-Sahaf Z,Raimi-Abraham B,Licciardi M,de Mohac LM

    更新日期:2020-10-02 00:00:00

  • Emerging freeze-drying process development and scale-up issues.

    abstract::Although several guidelines do exist for freeze-drying process development and scale-up, there are still a number of issues that require additional attention. The objective of this review article is to discuss some emerging process development and scale-up issue with emphasis on effect of load condition and freeze-dry...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,评审

    doi:10.1208/s12249-011-9599-9

    authors: Patel SM,Pikal MJ

    更新日期:2011-03-01 00:00:00

  • Pulmonary Administration of Microparticulate Antisense Oligonucleotide (ASO) for the Treatment of Lung Inflammation.

    abstract::Targeted delivery to the lung for controlling lung inflammation is an area that we have explored in this study. The purpose was to use microparticles containing an antisense oligonucleotide (ASO) to NF-κB to inhibit the production of proinflammatory cytokines. Microparticles were prepared using the B-290 Buchi Spray D...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1002-7

    authors: Ubale RV,Shastri PN,Oettinger C,D'Souza MJ

    更新日期:2018-05-01 00:00:00