The Control of Drug Release from Conventional Melt Granulation Matrices

Flanders, P.; Dyer, G. A.; Jordan, D W

doi:10.3109/03639048709068366

Cited by 30 publications

(11 citation statements)

References 1 publication

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“…However, at low pH values (ISS-acetate buffer, pH 5), the Prot-S-S-Prot (8) matrixes are fairly soluble; thus, the drug diffusion rates are slower and almost independent of the degree of cross-linking of the matrix. Nevertheless, at pH 7.4, increasing the crosslinking degree of the polymer matrix is a possible route to adjust the system to the individual needs of the drug.…”

Section: Influence Of Formulation 321 Cross-linkingmentioning

confidence: 99%

“…However, the release kinetics was found to be greatly dependent on the compaction properties of the polymer-drug granules. [6][7][8][9] Other alternatives include the design of matrix drug delivery systems in which the drug particles are dispersed in a melted polymeric phase. A common example is the compression of drug-filled polymeric compounds above the melting point of the polymer to form a solid part containing the drug.…”

Section: Introductionmentioning

confidence: 99%

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Soy Matrix Drug Delivery Systems Obtained by Melt-Processing Techniques

et al. 2003

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The aim of this study was to develop new soy protein drug delivery matrix systems by melt-processing techniques, namely, extrusion and injection moulding. The soy matrix systems with an encapsulated drug (theophylline, TH) were previously compounded by extrusion performed at two different pH values, (i) pH 4 (SIpDtp) and (ii) pH 7 (SIDtp), and further injection-moulded into a desired shape. During the extrusion process the matrixes SIDtp were also cross-linked with glyoxal (0.6X-SIDtp) and reinforced with a bioactive filler, hydroxylapatite (SI-HADtp). The obtained mouldings were used to study the drug-release mechanisms from the plastic soy-TH matrixes. In an isotonic saline solution (ISS) buffered at pH 5.0 (200 mM acetate buffer), the resulting release kinetics could be described using the Fick's second law of diffusion. Because the diffusion coefficients were found to be constant and the boundary conditions to be stationary, these systems are drug-diffusion controlled. Conversely, the dominant phenomena in an isotonic saline solution buffered at pH 7.4 (200 mM Tris/HCl buffer) are more complex. In fact, because of the higher polymer solubility, the resulting matrix is time-variant. So, the drug release is affected by swelling, drug diffusion, and polymer dissolution, being faster when compared to ISS-200 mM acetate buffer, pH 5.0. The changes in the formulation composition affecting the correspondent release rates were also investigated. At pH 7.4, increasing the cross-linking degree of the polymer matrix (via reaction with glyoxal or heat treatment) or decreasing the net charge (extruding at pH near its isoelectric point) led to lower release rates. The incorporation of ceramic filler caused the opposite effect. Because of the low solubility of the matrix at pH 5.0, no significant variations were detected with variations in the selected formulations. These systems, based on a nonstandard protein-based material, seem to be very promising to be used as carriers for drug delivery.

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Section: Influence Of Formulation 321 Cross-linkingmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Soy Matrix Drug Delivery Systems Obtained by Melt-Processing Techniques

et al. 2003

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“…The materials were mixed for 5 min at the setting 1 with no heat and the Granulations were prepared by raising the jacket temperature to approximately 85 • C. The applied heat and the heat of friction generated during mixing caused the softening or melting of the binder to form agglomerates with the drug substance. Since the binder was added in powder form to the starting materials at ambient temperature followed by heating above the melting point of the binder, the temperature of the mixture was increased by the heating jacket (Kinget and Kemel, 1985) along with the heat of friction (McTaggart et al, 1984;Flanders et al, 1987). Therefore, the impeller and chopper speeds were set on low.…”

Section: Melt Granulationmentioning

confidence: 99%

“…Immediately after the granulation endpoint was reached, the mixer was stopped and cold water was allowed to circulate through the jacket. Since the fast cooling of melt granules was reported to have a negative effect on drug release (Flanders et al, 1987), the contents of the mixing bowl were discharged and the warm granules were cooled at room temperature by spreading them out on trays before milling. Granules were milled through a No.…”

Section: Melt Granulationmentioning

confidence: 99%

Application of melt granulation technology to enhance stability of a moisture sensitive immediate-release drug product

Kowalski

Kalb

Joshi

et al. 2009

International Journal of Pharmaceutics

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“…Traditional compression methods often involve solvent granulation of the drug with the matrix material (Onay-Basaran & Olsen 1985; Parab et al 1987). Manufacture using melt-dispersion technology offers the same advantages of simplicity and cost-efficiency, but eliminates the safety concerns associated with the use of organic solvents (Flanders et al 1987).…”

mentioning

confidence: 99%

Release of Chlorpheniramine Maleate from Fatty Acid Ester Matrix Disks Prepared by Melt-extrusion

Prapaitrakul

Sprockel

Shivanand

1991

Journal of Pharmacy and Pharmacology

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Chlorpheniramine maleate was incorporated into disks consisting of glyceryl fatty acid esters, polyethylene glycol fatty acid esters or a combination of the two. A melt-extrusion process was used to prepare the matrix disks containing the drug. The release of the drug into distilled water, pH 1.2 buffer, and pH 7.5 buffer showed the expected square root of time dependence. An increase in the fatty acid ester hydrophilic-lipophilic balance (HLB) from 1 to 14 resulted in a 10-fold increase in the drug release rate from 0.25 +/- 0.01 to 25.84 +/- 1.29 mg cm-2 h-1/2. The maximum release rate was seen from the fatty acid ester with a melting point of 44 degrees C. The pH of the dissolution medium had a small impact on the rate of drug release, but the rate of agitation had no significant influence on the rate of drug release. By blending a fatty acid ester of a high melting point (64 degrees C) and a low HLB value of 2 with esters of lower melting points (33 to 50 degrees C) or higher HLB values (10 to 14), it was possible to modify the release from 10.0 +/- 0.70 to 21.5 +/- 0.57 mg cm-2 h-1/2.

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The Control of Drug Release from Conventional Melt Granulation Matrices

Cited by 30 publications

References 1 publication

Soy Matrix Drug Delivery Systems Obtained by Melt-Processing Techniques

Soy Matrix Drug Delivery Systems Obtained by Melt-Processing Techniques

Application of melt granulation technology to enhance stability of a moisture sensitive immediate-release drug product

Release of Chlorpheniramine Maleate from Fatty Acid Ester Matrix Disks Prepared by Melt-extrusion

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