Physicochemical properties and mechanism of drug release from ethyl cellulose matrix tablets prepared by direct compression and hot-melt extrusion

Crowley, Michael M.; Schroeder, Britta; Fredersdorf, Anke; Obara, Sakaé; Talarico, Mark; Kucera, Shawn A.; McGinity, James W.

doi:10.1016/j.ijpharm.2003.09.037

Cited by 212 publications

(99 citation statements)

References 48 publications

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“…Dissolution testing is the single most important tool for process control and quality assurance of solid oral dosage forms and is used to confirm that product performance is reproducible while meeting all regulatory requirements when product formulation changes are made (1). Apparatus 1 and 2, which are the most commonly used apparatus for dissolution testing of solid oral dosage forms, have also been applied to the evaluation of sustained-release dosage forms (2)(3)(4)(5)(6). However, some disadvantages exist when using Apparatus 1 and 2 to assess the dissolution rate of an active pharmaceutical ingredient (API) from modifiedrelease technologies.…”

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confidence: 99%

Development and Assessment of a USP Apparatus 3 Dissolution Test Method for Sustained-Release Nevirapine Matrix Tablets

Mwila¹,

Khamanga²,

Walker³

2016

Dissolution Technol.

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Dissolution testing is a quality control tool used to assess batch-to-batch performance of dosage forms, thereby providing continued assurance of product quality. Analytical methods for the assessment of pharmaceutical product quality must be validated according to regulatory guidelines to ensure that tests are reliable and valid. Agitation rate, mesh pore size, surfactant concentration, and dissolution medium molarity are experimental parameters that may affect nevirapine (NVP) release and were investigated and optimized to ensure that consistent, reliable, and valid results using Apparatus 3 were produced. Agitation rate was investigated to establish an equivalent response to that observed for NVP release using Apparatus 2 at 50 rpm. A reciprocation rate of 5-10 dpm produced dissolution profiles that were similar to those observed using Apparatus 2. An increase in the molarity of the dissolution medium slightly increased the release rate of NVP, and a 50 mM buffer maintained at pH values mimicking gastrointestinal tract (GIT) conditions was selected for all experiments. With the addition of 2% sodium lauryl sulfate (SLS) to the dissolution medium, >80% NVP was released from the tablets over the test period. The NVP release rate increased with an increase in the mesh pore size; however, the extent of release was not affected by this parameter. Dissolution test samples were analyzed using HPLC, and dissolution methods were validated for NVP stability in the dissolution medium, specificity, linearity and range, repeatability, intermediate precision, and accuracy as defined by ICH. The dissolution method used for testing NVP tablets can be regarded as an appropriate tool for the evaluation of sustained-release (SR) NVP formulations and the impact of formulation composition and product quality attributes on drug release.

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mentioning

confidence: 99%

Development and Assessment of a USP Apparatus 3 Dissolution Test Method for Sustained-Release Nevirapine Matrix Tablets

Mwila¹,

Khamanga²,

Walker³

2016

Dissolution Technol.

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“…In vitro Tablet Dissolution Study. Dissolution of the SR tablets was investigated using a modified version of the method described by Crowley et al in 2004. 13 Dissolution profiles were determined at 37°C in a dissolution tester using the paddle method at 50 rpm according to the Korea Pharmacopoeia (KP) dissolution procedure. The dissolution media were 0.01 N HCl buffer (pH 1.2), acetate buffer (pH 4.0), phosphate buffer (pH 6.8) and water.…”

Section: Methodsmentioning

confidence: 99%

Preparation of Lacosamide Sustained-release Tablets and Their Pharmacokinetics in Beagles and Mini-pigs

Ahn¹,

Kim²,

Nam³

et al. 2014

Bulletin of the Korean Chemical Society

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The aim of the present study was to improve dosing of lacosamide, a functionalized amino acid used as an antiepileptic agent, from twice daily to once daily for the convenience of patients. A sustained-release lacosamide tablet was developed and dissolution testing was employed to determine in vitro release behavior using water or buffer solutions at pH 1.2, 4.0, or 6.8. Lacosamide was released for 12 h from the sustainedrelease (SR) tablet, as compared to complete release within 1 h from an immediate-release Vimpat ® tablet. Each formulation (100 mg) was orally administered to six beagle dogs and six mini-pigs under fasted conditions, and pharmacokinetic parameters such as the area under the concentration time curve (AUC t ), the maximum plasma concentration (C max ), and the time at which this occurred (T max ) were calculated. These results showed similar values for AUC t , C max , and T max following oral administration of immediate-release (Vimpat ® ) and SR lacosamide tablets.

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“…Crowley et al investigated the physicochemical properties and drug release mechanism from ethyl cellulose (EC) matrix tablets prepared by direct compression or hot-melt extrusion of binary mixtures of a water soluble drug (Guaifenesin) and a polymer (Crowley et al, 2004b). Ethyl cellulose was separated into "fine" or "coarse" particle size fractions corresponding to 325-80 and 80-30 mesh particles, respectively.…”

Section: Tablets and Capsulesmentioning

confidence: 99%

“…Hot-melt extrusion (HME) is a manufacturing process widely used in plastics industry, and has significant potential as a continuous pharmaceutical process. During hot-melt extrusion of pharmaceutical dosage forms, a blend of active ingredient, thermoplastic polymeric carrier, and other processing aids, including plasticizers and antioxidants, is heated and softened inside the extruder and then pressurized through a die into granules, cylinders, or films (Crowley et al, 2004b;Crowley et al, 2002;Munjal et al, 2006a;Repka et al, 2005;Repka et al, 2003;Young Cr, 2005;Young, 2003;Zheng et al, 2004).…”

Section: Introductionmentioning

confidence: 99%

Pharmaceutical Applications of Hot-Melt Extrusion: Part II

Repka

Battu

Upadhye

et al. 2007

Drug Development and Industrial Pharmacy

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158

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The advent of high through-put screening in the drug discovery process has resulted in compounds with high lipophilicity and poor solubility. Increasing the solubility of such compounds poses a major challenge to formulation scientists. Various approaches have been adopted to address this including preparation of solid dispersions and solid solutions. Hot-melt extrusion is an efficient technology for producing solid molecular dispersions with considerable advantages over solvent-based processes such as spray drying and co-precipitation. Hot-melt extrusion has been demonstrated to provide sustained, modified, and targeted drug delivery. Improvements in bioavailability utilizing the hot-melt extrusion technique demonstrate the value of the technology as a potential drug delivery processing tool. The interest in hot-melt extrusion technology for pharmaceutical applications is evident from the increasing number of patents and publications in the scientific literature. Part II of this article reviews the myriad of hot-melt extrusion applications for pharmaceutical dosage forms including granules, pellets, tablets, implants, transmucosal, and transdermal systems.

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Physicochemical properties and mechanism of drug release from ethyl cellulose matrix tablets prepared by direct compression and hot-melt extrusion

Cited by 212 publications

References 48 publications

Development and Assessment of a USP Apparatus 3 Dissolution Test Method for Sustained-Release Nevirapine Matrix Tablets

Development and Assessment of a USP Apparatus 3 Dissolution Test Method for Sustained-Release Nevirapine Matrix Tablets

Preparation of Lacosamide Sustained-release Tablets and Their Pharmacokinetics in Beagles and Mini-pigs

Pharmaceutical Applications of Hot-Melt Extrusion: Part II

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