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The effect of the ratio of two acrylic polymers on the in vitro release kinetics of ketoprofen from pellets prepared by extrusion and spheronisation technique.

Golam Kibria, Reza Ul-Jalil

Open publisher page 6 citations

Abstract

The aim of this study was to investigate the effect of physico-chemical properties of the polymers on the release profile of ketoprofen from the pellets dosage form. Ammonio Methacrylate Copolymer Type A (Eudragit RL 30 D) & Ammonio Methacrylate Copolymer Type B (Eudragit RS 30 D) were used as release rate retarding polymers. The drug containing core pellets were prepared by extrusion spheronisation technique and subsequently coated with 15% (w/w) polymer load of the combination of Eudragit RL 30 D & Eudragit RS 30 D having ratio 1:0, 4:1, 3:2, 1:1, 2:3, 1:4, 0:1 respectively. Significant differences were found among the drug release profile from different formulations. It was revealed that Eudragit RL 30 D has the effect to increase the initial drug release more significantly where as Eudragit RS 30 D has the effect to minimize the initial drug release but increase the terminal drug release more significantly. In acid media about 50% drug was released from pellets coated only with Eudragit RL 30 D where as only 5% drug was released in case of Eudragit RS 30 D but maximum 10% drug was released from pellets when coated with the combination of Eudragit RL 30 D & Eudragit RS 30 D. In buffer media, evidence of burst release was observed for the pellets coated with Eudragit RL 30 D & Eudragit RS 30 D having ratio of 1:0, 4:1, 3:2 respectively. It was also observed that drug release increases sharply as well as the release best fit to the zero order release kinetics when pellets coated with 1:1 ratio of Eudragit RL 30 D & Eudragit RS and follows Higuchi's release kinetics when ratio was 1:0 & 3:2. The results generated in this study showed that proper selection of polymeric materials based on their physico-chemical properties is important in designing sustained release pellets dosage form with suitable dissolution profile.

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What this paper is about

The aim of this study was to investigate the effect of physico-chemical properties of the polymers on the release profile of ketoprofen from the pellets dosage form. Ammonio Methacrylate Copolymer Type A (Eudragit RL 30 D) & Ammonio Methacrylate Copolymer Type B (Eudragit RS 30 D) were used as release rate retarding polymers. The drug containing core pellets were prepared by extrusion spheronisation technique and subsequently coated with 15% (w/w) polymer load of the combination of Eudragit RL 30 D & Eudragit RS 30 D having ratio 1:0, 4:1, 3:2, 1:1, 2:3, 1:4, 0:1 respectively. Significant differences were found among the drug release profile from different formulations. It was revealed that Eudragit RL 30 D has the effect to increase the initial drug release more significantly where as Eudragit RS 30 D has the effect to minimize the initial drug release but increase the terminal drug release more significantly. In acid media about 50% drug was released from pellets coated only with Eudragit RL 30 D where as only 5% drug was released in case of Eudragit RS 30 D but maximum 10% drug was released from pellets when coated with the combination of Eudragit RL 30 D & Eudragit RS 30 D. In buffer media, evidence of burst release was observed for the pellets coated with Eudragit RL 30 D & Eudragit RS 30 D having ratio of 1:0, 4:1, 3:2 respectively. It was also observed that drug release increases sharply as well as the release best fit to the zero order release kinetics when pellets coated with 1:1 ratio of Eudragit RL 30 D & Eudragit RS and follows Higuchi's release kinetics when ratio was 1:0 & 3:2. The results generated in this study showed that proper selection of polymeric materials based on their physico-chemical properties is important in designing sustained release pellets dosage form with suitable dissolution profile.

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Available abstract

The aim of this study was to investigate the effect of physico-chemical properties of the polymers on the release profile of ketoprofen from the pellets dosage form. Ammonio Methacrylate Copolymer Type A (Eudragit RL 30 D) & Ammonio Methacrylate Copolymer Type B (Eudragit RS 30 D) were used as release rate retarding polymers. The drug containing core pellets were prepared by extrusion spheronisation technique and subsequently coated with 15% (w/w) polymer load of the combination of Eudragit RL 30 D & Eudragit RS 30 D having ratio 1:0, 4:1, 3:2, 1:1, 2:3, 1:4, 0:1 respectively. Significant differences were found among the drug release profile from different formulations. It was revealed that Eudragit RL 30 D has the effect to increase the initial drug release more significantly where as Eudragit RS 30 D has the effect to minimize the initial drug release but increase the terminal drug release more significantly. In acid media about 50% drug was released from pellets coated only with Eudragit RL 30 D where as only 5% drug was released in case of Eudragit RS 30 D but maximum 10% drug was released from pellets when coated with the combination of Eudragit RL 30 D & Eudragit RS 30 D. In buffer media, evidence of burst release was observed for the pellets coated with Eudragit RL 30 D & Eudragit RS 30 D having ratio of 1:0, 4:1, 3:2 respectively. It was also observed that drug release increases sharply as well as the release best fit to the zero order release kinetics when pellets coated with 1:1 ratio of Eudragit RL 30 D & Eudragit RS and follows Higuchi's release kinetics when ratio was 1:0 & 3:2. The results generated in this study showed that proper selection of polymeric materials based on their physico-chemical properties is important in designing sustained release pellets dosage form with suitable dissolution profile.

Key concepts: Ketoprofen, Pellets, Polymer, Chemistry, Copolymer, Nuclear chemistry, Dosage form, Extrusion

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The effect of the ratio of two acrylic polymers on the in vitro release kinetics of ketoprofen from pellets prepared by extrusion and spheronisation technique. — Research Paper | ScholarLens