Development and evaluation of a miniaturized procedure for determining the bonding index: a novel prototype for solid dosage formulation development.

Abstract:

:The purpose of this study was a comparative evaluation of miniaturized vs. University of Minnesota's (i.e., U of Minn. = Hiestand's) procedures for determining the tensile strength, indentation hardness, and bonding index (BI), one out of three Indices of Tableting Performance (ITP). Tableting properties of six direct compression placebo formulations were determined by using a compaction simulator and a Texture Analyser TA-XT2I, or by following the U of Minn. method, which included a specially designed triaxial compression device, a computer-controlled mechanical stress-strain analyzer, and a dynamic pendulum impact apparatus. Miniaturization of the procedures to determine the ITP, as well as the ability to differentiate between materials while operating compaction cycles more comparable to standard tablet production conditions, enabled proper evaluation of each material's inherent tableting properties. Indentation diameter calculated via an empirical equation appeared to correlate well with, and provided acceptable precision of accuracy to, the determination of indentation diameter via standard optical microscopy methods. The miniaturized and U of Minn. procedure exhibited a significant degree of correlation when comparing the BI. However, the tensile strength and indentation hardness values were somewhat different due to the use of triaxial decompression for the U of Minn. procedure vs. standard compaction profiling for the miniaturized procedure. The present direct compression placebo formulation data gathered from the miniaturized procedures and compared with the U of Minn. method for determining the ITP suggest that both techniques yield similar conclusions. However, discrimination of out-of-die compaction properties determined via the miniaturized procedures, such as tensile strength and indentation hardness, appeared to associate more precisely with changes in strain rate, thus allowing better discrimination of particle-particle interactions and ductile-to-brittle characteristics as a function of compaction speed and pressure.

journal_name

Pharm Dev Technol

authors

Lamey K,Schwartz J,Muller F

doi

10.1081/pdt-120022153

subject

Has Abstract

pub_date

2003-08-01 00:00:00

pages

239-52

issue

3

eissn

1083-7450

issn

1097-9867

journal_volume

8

pub_type

杂志文章
  • Starch-quercetin conjugate by radical grafting: synthesis and biological characterization.

    abstract::A novel flavonoid-polysaccharide conjugate was synthesized by free radical grafting of quercetin on starch. The covalent insertion of quercetin in the polymeric chain was confirmed by FT-IR, DSC and fluorescence analyses, while an estimation of the amount of quercetin bound per g of polymer was obtained by the Folin-C...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2010.546413

    authors: Cirillo G,Puoci F,Iemma F,Curcio M,Parisi OI,Spizzirri UG,Altimari I,Picci N

    更新日期:2012-07-01 00:00:00

  • Iontophoretic enhancement of leuprolide acetate by fatty acids, limonene, and depilatory lotions through porcine epidermis.

    abstract::The effect of chemical enhancers (e.g., fatty acids, limonene, depilatory lotions) and iontophoresis was investigated on the in vitro permeability of leuprolide acetate through porcine epidermis. Franz diffusion cells and Scepter iontophoretic power source were used for the percutaneous absorption studies. Anodal iont...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-200032986

    authors: Rastogi SK,Singh J

    更新日期:2004-11-01 00:00:00

  • Prolonged injectable formulation of Nafarelin using in situ gel combination delivery system.

    abstract::The principal purpose of the present study was to prepare and characterize a complex drug delivery system consisting of Nafarelin-poly (3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) nanoparticles (NPs) in combination with sodium alginate/poloxamer 407 in situ gel. Nafarelin-loaded PHBV NPs were prepared via double em...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2017.1321662

    authors: Alizadeh B,Bahari Javan N,Akbari Javar H,Khoshayand MR,Dorkoosh F

    更新日期:2018-02-01 00:00:00

  • Influence of molecular properties on oral bioavailability of lipophilic drugs - mapping of bulkiness and different measures of polarity.

    abstract::The biopharmaceutical assessment of new drug candidates based on their chemical structure is important in drug discovery and development. The scope of this study is to focus on lipophilic drugs and to clarify the role of their chemical predictors on oral bioavailability in humans. First their chemical properties were ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450802626296

    authors: Kuentz MT,Arnold Y

    更新日期:2009-01-01 00:00:00

  • The effect of composition on the tableting indices of binary powder mixtures.

    abstract::The purpose of this study was to investigate the effect of the composition of a binary powder mixture on the bonding index, the brittle fracture index, and the strain index, as defined by Hiestand. The studies involved tensile strength and dynamic indentation hardness determinations of square compacts, the solid fract...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459709022630

    authors: Majuru S,Wurster DE

    更新日期:1997-11-01 00:00:00

  • Stability of dry coated solid dosage forms.

    abstract::The dry coating process was evaluated in terms of storage stability investigating drug release and agglomeration tendency of the different coated oral dosage forms; hydroxypropyl methylcellulose acetate succinate (HPMCAS) was used with triethylcitrate (TEC) as plasticizer and acetylated monoglyceride (Myvacet) as wett...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450902882336

    authors: Kablitz CD,Urbanetz NA

    更新日期:2009-01-01 00:00:00

  • Controlled-release drug delivery system based on fluocinolone acetonide-cyclodextrin inclusion complex incorporated in multivesicular liposomes.

    abstract::Multivesicular liposomes (MVLs) have been widely studied for encapsulation of hydrophilic drugs due to their structural properties and large aqueous inner cavities. In this study, to investigate MVLs and their potential application for incorporation of hydrophobic drugs, new drug delivery system for fluocinolone aceto...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2014.920358

    authors: Vafaei SY,Dinarvand R,Esmaeili M,Mahjub R,Toliyat T

    更新日期:2015-11-01 00:00:00

  • Development of controlled-release SK&F 82526-J buffer bead formulations with tartaric acid as the buffer.

    abstract::The purpose of this research was to design and develop a novel controlled-release bead formulation for oral administration with buffer crystals as a carrier for loading of fenoldopam mesylate, an intravenous antihypertensive agent, which provides an in vitro release rate of 30-50 mg/hr for 6-8 hr. Buffer crystals were...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459809028629

    authors: Venkatesh GM

    更新日期:1998-11-01 00:00:00

  • Mucoadhesive films based on gellan gum/pectin blends as potential platform for buccal drug delivery.

    abstract::Films of gellan gum:pectin blends were prepared by solvent casting method. Gellan gum:pectin mass ratios were varied (4:1; 1:1; 1:4) at different concentrations (3% or 4%) and glycerol was used as plasticizer (1 or 2%). The films were thin (18-30 µm), translucent, flexible, and homogeneous. The surface pH was suitable...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2019.1682608

    authors: Prezotti FG,Siedle I,Boni FI,Chorilli M,Müller I,Cury BSF

    更新日期:2020-02-01 00:00:00

  • Improvement of the material motion in a rotary processor.

    abstract::The purpose of this paper is to reject or to confirm the hypothesis that the influence of the water addition rate on the size and size distribution of pellets is caused by insufficient spreading of the added water at higher water addition rates. To overcome insufficient spreading of the added water, the agitation in t...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459609031431

    authors: Vertommen J,Jaucot B,Rombaut P,Kinget R

    更新日期:1996-12-01 00:00:00

  • Dissolution rate enhancement by adsorption of poorly soluble drugs on hydrophilic silica aerogels.

    abstract::The aim of this work is to evaluate the feasibility of hydrophilic silica aerogels as drug carriers and to investigate the influence of the aerogels properties on the release rate of poorly water-soluble drugs. Hydrophilic silica aerogels of different densities were loaded with two model drugs, ketoprofen and griseofu...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-200035804

    authors: Smirnova I,Suttiruengwong S,Seiler M,Arlt W

    更新日期:2004-11-01 00:00:00

  • Formulation factors affecting the isomerization rate of betamethasone-17-valerate in a developmental hydrophilic cream - a HPLC and microscopy based stability study.

    abstract::The formulation of betamethasone-17-valerate (BV) into topical medicines presents a significant challenge for the formulation chemist. The substance is susceptible to acid and base catalyzed isomerization in aqueous environments, which results in valerate transesterification from carbon 17 to carbon 21 of the steroid ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2016.1143003

    authors: Byrne J,Wyraz A,Velasco-Torrijos T,Reinhardt R

    更新日期:2017-06-01 00:00:00

  • Design and evaluation of thermoreversible in situ gelling system of forskolin for the treatment of glaucoma.

    abstract::The contact time of a vehicle on the cornea is of utmost importance for ophthalmic drug delivery. The poor bioavailability and therefore poor therapeutic response exhibited by the conventional ophthalmic solutions due to pre-corneal elimination of a drug may be overcome by the use of the in situ gel forming systems, w...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450903262033

    authors: Gupta S,Samanta MK

    更新日期:2010-07-01 00:00:00

  • Development and evaluation of mathematical model to predict disintegration time of fast disintegrating tablets using powder characteristics.

    abstract::The objective of the study was to develop a mathematical model for predicting the disintegration time of fast disintegrating tablets (FDTs) by estimating the powder characteristics of powder blend prior to compression. A combination of chitosan-alginate complex and glycine in the ratio of 50:50 was used for preparing ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450903479996

    authors: Goel H,Arora A,Tiwary AK,Rana V

    更新日期:2011-02-01 00:00:00

  • Conjugates of TAT and folate with DOX-loaded chitosan micelles offer effective intracellular delivery ability.

    abstract::The key for better antitumor efficacy is to improve the specificity of antitumor drugs for tumor cells and diminish their cytotoxicity to normal tissues. Targeted nanoparticles as antitumor drug delivery system can resolve this problem. In this study, we prepared folate and TAT (arginine-rich cell-penetrating peptide)...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1469147

    authors: Zhang S,Liu Y,Gan Y,Qiu N,Gu Y,Zhu H

    更新日期:2019-02-01 00:00:00

  • Multivariate analysis in the pharmaceutical industry: enabling process understanding and improvement in the PAT and QbD era.

    abstract::In the pharmaceutical industry, chemometrics is rapidly establishing itself as a tool that can be used at every step of product development and beyond: from early development to commercialization. This set of multivariate analysis methods allows the extraction of information contained in large, complex data sets thus ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章,评审

    doi:10.3109/10837450.2014.898656

    authors: Ferreira AP,Tobyn M

    更新日期:2015-01-01 00:00:00

  • A quality by design approach using artificial intelligence techniques to control the critical quality attributes of ramipril tablets manufactured by wet granulation.

    abstract::Quality by design (QbD) is an essential part of the modern approach to pharmaceutical quality. This study was conducted in the framework of a QbD project involving ramipril tablets. Preliminary work included identification of the critical quality attributes (CQAs) and critical process parameters (CPPs) based on the qu...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2012.705294

    authors: Aksu B,Paradkar A,de Matas M,Özer Ö,Güneri T,York P

    更新日期:2013-02-01 00:00:00

  • Recent progress in transdermal sonophoresis.

    abstract::Transdermal drug administration has a number of advantages that cannot be leveraged for therapeutic benefits because of the robust barrier provided by the stratum corneum. One of the promising techniques for circumventing the stratum corneum is sonophoresis - the use of ultrasound for facilitating transdermal drug del...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章,评审

    doi:10.3109/10837450.2015.1116566

    authors: Ita K

    更新日期:2017-06-01 00:00:00

  • Correlation of the thermal stability of phospholipid-based emulsions and the microviscosity measurements using fluorescence polarization.

    abstract::The fluorescence polarization technique was used to measure the microviscosity of a series of phospholipid-based emulsions. Fourteen different oil-in-water emulsions containing 20% medium chain length triglycerides, various concentrations and types of phospholipids, and 2.2% glycerin were prepared by microfluidization...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-120030251

    authors: Zhang X,Kirsch LE

    更新日期:2004-01-01 00:00:00

  • Nano drug delivery systems and gamma radiation sterilization.

    abstract::In recent years, drug delivery systems such as liposomes and microparticles have been used in clinic for the treatment of different diseases and from a regulatory point of view, a parenterally applied drug and drug delivery systems must be sterile and pyrogen free. Radiation sterilization is a method recognized by pha...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2016.1163393

    authors: Sakar F,Özer AY,Erdogan S,Ekizoglu M,Kart D,Özalp M,Colak S,Zencir Y

    更新日期:2017-09-01 00:00:00

  • Photoinduced particulate matter in a parenteral formulation for bisnafide, an experimental antitumor agent.

    abstract::This paper assesses the cause of particulate formation in vials of the experimental antitumor agent bisnafide and investigates pharmaceutical techniques to reduce the number of particulates in the product. Solution preparation and particulate isolation were performed under Class 100 laminar air flow. Reversed-phase HP...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100101380

    authors: Rubino JT,Chan LL,Walker JT,Segretario J,Everlof JG,Hussain MA

    更新日期:1999-08-01 00:00:00

  • Preparation and characterization of a powder containing an oily liquid drug with Eudragit EPO or L100 copolymer.

    abstract::Oily liquid drugs are not convenient for oral administration. We developed a powder containing clofibrate (CF), a model of an oily drug, using aminoalkyl methacrylate copolymer (EPO) or methacrylic acid copolymer (L100). CF or a mixture of CF and soybean oil was emulsified with EPO or L100 aqueous solution. Using a hi...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1086370

    authors: Fujii M,Kawakami A,Saito A,Tuchiya H,Koizumi N,Watanabe Y

    更新日期:2016-12-01 00:00:00

  • Transdermal delivery of diclofenac using water-in-oil microemulsion: formulation and mechanistic approach of drug skin permeation.

    abstract::The objective of the present investigation was to enhance skin permeation of diclofenac using water-in-oil microemulsion and to elucidate its skin permeation mechanism. The w/o microemulsion formulations were selected based on constructed pseudoternary phase diagrams depending on water solubilization capacity and ther...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2013.788658

    authors: Thakkar PJ,Madan P,Lin S

    更新日期:2014-05-01 00:00:00

  • Effect of degree of methoxylation and particle size on compression properties and compactibility of pectin powders.

    abstract::This study examines the effect of the degree of methoxylation (DM) and particle size on compression properties and compactibility of pectin powders. A powder classification system based on sequential handling of compression parameters was applied. A single size fraction (90-125 μm) of pectin powders with DM values ran...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2010.535831

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

    更新日期:2012-05-01 00:00:00

  • Identification and characterization of potential impurities of quetiapine fumarate.

    abstract::Seven potential impurities, including by-products, starting materials and intermediates were identified in pharmaceutical substance quetiapine fumarate and characterized by spectroscopic methods (MS, IR, NMR). Based on these methods the structures of the impurities were assigned or confirmed as: impurity I: 2-(phenylt...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450802409388

    authors: Stolarczyk EU,Kaczmarek L,Eksanow K,Kubiszewski M,Glice M,Kutner A

    更新日期:2009-01-01 00:00:00

  • A new method for evaluating the dissolution of orodispersible films.

    abstract::The aim of this research was to develop and assess a new dissolution apparatus for orodispersible films (ODFs). The new apparatus was based on a flow-through cell design which requires only a limited amount of dissolution medium and can automatically collect samples in short-time intervals. Compared with the dissoluti...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2014.882936

    authors: Xia Y,Chen F,Zhang H,Luo C

    更新日期:2015-05-01 00:00:00

  • Utilizing quantitative certificate of analysis data to assess the amount of excipient lot-to-lot variability sampled during drug product development.

    abstract::Understanding variability in excipient physico-chemical properties is becoming an important aspect of Quality-by-Design drug product development. However, present experimental methods have only been able to study a few physico-chemical properties for a few excipient lots due to time, cost, and sample gathering conside...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2011.604784

    authors: Kushner J 4th

    更新日期:2013-03-01 00:00:00

  • The apparent solubilizing capacity of simulated intestinal fluids for poorly water-soluble drugs.

    abstract::Drug solubility testing in biorelevant media has become an indispensable tool in pharmaceutical development. Despite this importance, there is still an incomplete understanding of how poorly soluble compounds interact with these media. The aim of this study was to apply the concept of the apparent solubilization capac...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837451003664099

    authors: Schwebel HJ,van Hoogevest P,Leigh ML,Kuentz M

    更新日期:2011-06-01 00:00:00

  • Developing an injectable formula containing an oxygen-sensitive drug: a case study of danofloxacin injectable.

    abstract::The purpose of this study was to assess the impact of impurities in formulation components, antioxidants, formulation pH, and processing/packaging on the extent of color change associated with oxidation of danofloxacin injectable. The methods used in this study include reversed-phase HPLC, UV-VIS spectrophotometry, at...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100101384

    authors: Kasraian K,Kuzniar AA,Wilson GG,Wood JA

    更新日期:1999-01-01 00:00:00

  • Relating formulation variables to in vitro dissolution using an artificial neural network.

    abstract::The purpose of this paper was to investigate the effect of several experimental variables on the ability of a neural network to predict in vitro dissolution rate as a function of product formulation changes. Neural network software was trained with sets of hypothetical and experimental data consisting of 4-15 formulat...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459709031442

    authors: Ebube NK,McCall T,Chen Y,Meyer MC

    更新日期:1997-08-01 00:00:00