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Startseite » Pellet » Evaluation of Drug Release From Coated Pellets Based on Isomalt, Sugar,and Microcrystalline Cellulose Inert Cores

Evaluation of Drug Release From Coated Pellets Based on Isomalt, Sugar,and Microcrystalline Cellulose Inert Cores

17. November 2015

The objective of the present study was to investigate the effect of the pellet core materials isomalt, sugar, and microcrystalline cellulose on the in vitro drug release kinetics of coated sustained-release pellets as well as to evaluate the influence of different ratios of polymethacrylate copolymers exhibiting different permeability characteristics on the drug release rate. For characterization of the drug release process of pellets, the effect of osmolality was studied using glucose as an osmotically active agent in the dissolution medium. The pellet cores were layered with diclofenac sodium as model drug and coated with different ratios of Eudragit® RS30D and Eudragit® RL30D (ERS and ERL; 0:1 and 0.5:0.5 and 1:0 ratio) in a fluid bed apparatus. Physical characteristics such as mechanical strength, shape, and size proved that the inert cores were adequate for further processing. The in vitro dissolution tests were performed using a USP Apparatus I (basket method). The results demonstrated that, besides the ratio of the coating polymers (ERS/ERL), the release mechanism was also influenced by the type of starter core used. Sugar- and isomalt-type pellet cores demonstrated similar drug release profiles. Continue reading on Evaluation of Drug Release From Coated Pellets Based on Isomalt, Sugar,and Microcrystalline Cellulose Inert Cores 

Citation: Evaluation of Drug Release From Coated Pellets Based on Isomalt, Sugar, and Microcrystalline Cellulose Inert Cores – Nikolett Kállai,1 Oliver Luhn,2 Judit Dredán,1 Kristóf Kovács,1 Miléna Lengyel,1 and István Antal1,3
Received 9 October 2009; accepted 16 February 2010; published online 17 March 2010
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Materials
Diclofenac sodium (Sigma-Aldrich Chemie GmbH, Germany) was used as model drug. Isomalt described in pharmacopeias [Eur. Ph., USP] is a pharmaceutically acceptable excipient, which was supplied by the manufacturer (BENEO-Palatinit GmbH, Germany) in the form of starter pellets (galenIQTM 980) in the size range of 700–1,000 μm. Sugar spheres (850–1,000 μm; pharm-a-spheres®, H.G.Werner GmbH, Germany) and MCC spheres (710–1,000 μm; Ethispheres® 850, NPPharm Ltd., France) were chosen as inert cores for compar- ison with isomalt spheres. The sugar spheres used were of pharmacopeial grade and as such contain little amount of starch. The other two pellet cores do not contain any additive material.
Hydroxypropyl methylcellulose (HPMC; Pharmacoat 606, Shin-Etsu Chemical Ltd., Japan) was used as binder for the drug- layering process. Polymethacrylate copolymers (Eudragit® RL30D and Eudragit® RS30D, Degussa, Germany)—ERL and ERS—were used as film-forming polymers. Triethyl citrate (TEC; Fluka Chemie AG, Switzerland) served as plasticizer and micronized talc (Sigma-Aldrich Chemie GmbH, Germany) was used as an antiadhesion agent. Glucose anhydrate (MOLAR, Hungary) served as an osmotically active ingredient.

 

Tags: excipientsformulation

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      • Sweeteners
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  • Sources
    • Handbook of Pharmaceutical Excipients – 9th Edition
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