Dissolution Mechanism of Diclofenac Sodium from Wax Matrix Granules

Satō, Hiroshi; Miyagawa, Yasuhiko; Okabe, Toshio; Miyajima, Masaharu; Sunada, Hisakazu

doi:10.1021/js960221w

Cited by 70 publications

(53 citation statements)

References 13 publications

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“…The incorporation of a low melting compound into a low melting point wax may form a eutectic mixture or reduce the melting point of the mixture preventing the formation of a solid dosage form. The production of granules using carnauba wax has been reported (Miyagawa et al, 1996(Miyagawa et al, , 1999Sato et al, 1997). The granules contained diclofenac sodium and could be produced at temperatures less than the reported melting point of the wax material.…”

Section: Carriersmentioning

confidence: 99%

“…It has been reported that Explotab ® could be used as a "super-absorbent" in hydroxypropylcellulose hot-melt extruded transdermal films to facilitate moisture uptake in wound care applications (Repka et al, 2000b). A similar approach of drug release modification was applied to wax-containing systems (Miyagawa et al, 1996(Miyagawa et al, , 1999Sato et al, 1997). Hydroxypropylcellulose, Eudragit® L, and sodium chloride were incorporated into diclofenac sodium/carnauba wax matrices.…”

Section: Carriersmentioning

confidence: 99%

“…Triacetin, citrate esters, and low molecular weight polyethylene glycols have been investigated as plasticizers in hot-melt extruded systems. Recently, surfactants have also been shown to be promising (Follonier, N. et al, 1994;Kidokoro et al, 2001;Zhu et al, 2002) Poly(dimethylaminoethylmethacrylate-co- - (Repka et al, 1999a;Repka et al, 2000a;Repka et al, 2000b;Repka et al, 2001a;Repka et al, 2001b;Repka et al, 2002d;Sato et al, 1997) Ethyl cellulose Ethocel ® 133 - (Crowley et al, 2004b;De Brabander et al, 2002;Follonier, N. et al, 1994;Follonier et al, 1995) Cellulose acetate butyrate CAB 381-0.5 125 157 (Follonier, N. et al, 1994;Follonier et al, 1995;Sprockel et al, 1997) Cellulose Acetate Phthalate -165 192 (Follonier et al, 1995;Rippie et al, 1969) Poly(ethylene oxide)…”

Section: Plasticizersmentioning

confidence: 99%

See 2 more Smart Citations

Pharmaceutical Applications of Hot-Melt Extrusion: Part I

Crowley¹,

Zhang²,

Repka

et al. 2007

Drug Development and Industrial Pharmacy

643

365

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Interest in hot-melt extrusion techniques for pharmaceutical applications is growing rapidly with well over 100 papers published in the pharmaceutical scientific literature in the last 12 years. Hot-melt extrusion (HME) has been a widely applied technique in the plastics industry and has been demonstrated recently to be a viable method to prepare several types of dosage forms and drug delivery systems. Hot-melt extruded dosage forms are complex mixtures of active medicaments, functional excipients, and processing aids. HME also offers several advantages over traditional pharmaceutical processing techniques including the absence of solvents, few processing steps, continuous operation, and the possibility of the formation of solid dispersions and improved bioavailability. This article, Part I, reviews the pharmaceutical applications of hot-melt extrusion, including equipment, principles of operation, and process technology. The raw materials processed using this technique are also detailed and the physicochemical properties of the resultant dosage forms are described. Part II of this review will focus on various applications of HME in drug delivery such as granules, pellets, immediate and modified release tablets, transmucosal and transdermal systems, and implants.

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Section: Carriersmentioning

confidence: 99%

Section: Carriersmentioning

confidence: 99%

Section: Plasticizersmentioning

confidence: 99%

See 1 more Smart Citation

Pharmaceutical Applications of Hot-Melt Extrusion: Part I

Crowley¹,

Zhang²,

Repka

et al. 2007

Drug Development and Industrial Pharmacy

643

365

View full text Add to dashboard Cite

show abstract

“…Prepared tablets were stored at room temperature in airtight photo film container. The technique for tablet production was followed as mentioned previously [7][8][9]. …”

Section: Preparation Of Sustained Release Tabletmentioning

confidence: 99%

Development and Characterization of Atorvastatin Calcium Sustained Release Tablet Using Carbomer-974 and Hypromellose-15000 cps

Akbar¹,

Bhatta²,

Rahman³

et al. 2017

J. Sci. Res.

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A new sustained release formulation of Atorvastatin Calcium tablet, exhibiting improved swelling property and compatibility to prolong the drug release was prepared. Sustained release tablets were formulated using varying concentration of Carbomer-974 and Hypromellose-15000 cps, by direct compression method. Physical characteristics, compactibility, swelling index and drug content uniformity of the prepared formulations were determined. The drug release studies was carried out in USP dissolution test apparatus II (paddle) using phosphate buffer of pH 6.8 as dissolution medium for 8 hours and documented the effects of polymers on the drug release profile. The release mechanism was explored and explained with Zero order & Higuchi kinetic models. Formulation F1 and F5 were best fitted in the Higuchi model, representing diffusion mechanism of drug release, while Formulations F2, F3 and F4 showed Zero order model of drug release profile. The drug release pattern, compactibility and swelling index property of the formulated preparations were concentration dependent of the polymers used. Further study is necessary to evaluate the in vitro-in vivo relationship, but this study will be helpful for future to exploit the potential of this drug delivery system for the benefit of the mankind.

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“…In 1996 and 1997, Miyagawa, Sato et al prepared controlled release matrices containing diclofenac as a model drug by hot-melt extrusion (Miyagawa et al, 1996;Miyagawa et al, 1999;Sato et al, 1997). The authors used a twin-screw compounding extruder to prepare wax matrix granules composed of carnauba wax, the model drug, and other rate controlling agents.…”

Section: Granules Pellets and Spheresmentioning

confidence: 99%

Pharmaceutical Applications of Hot-Melt Extrusion: Part II

Repka

Battu

Upadhye

et al. 2007

Drug Development and Industrial Pharmacy

317

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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Dissolution Mechanism of Diclofenac Sodium from Wax Matrix Granules

Cited by 70 publications

References 13 publications

Pharmaceutical Applications of Hot-Melt Extrusion: Part I

Pharmaceutical Applications of Hot-Melt Extrusion: Part I

Development and Characterization of Atorvastatin Calcium Sustained Release Tablet Using Carbomer-974 and Hypromellose-15000 cps

Pharmaceutical Applications of Hot-Melt Extrusion: Part II

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