Poly vinyl acetate and ammonio methacrylate copolymer as unconventional polymer blends increase the mechanical robustness of HPMC matrix tablets.
The objective was to investigate poly vinyl acetate (Kollicoat®SR 30 D) and ammonio methacrylate copolymer (Eudragit®RL 30 D) blends as coatings to increase the mechanical robustness of hydroxypropyl methylcellulose (HPMC) matrix tablets. Poly vinyl acetate (Kollicoat®SR 30 D - KSR) was selected for its flexibility and ammonio methacrylate copolymer (Eudragit®RL 30 D - ERL) because of its high permeability. Films based on KSR:ERL blends were prepared by casting or spraying aqueous dispersions of these polymers and were characterized by water uptake, dry mass loss and mechanical properties. KSR:ERL blends were investigated as coating materials to improve the robustness, mechanical strength and drug release from the HPMC matrix tablets containing propranolol HCl, caffeine and carbamazepine as model drugs. Both HPMC and the polymer coating affected the propranolol release. The release and the mechanical properties could be easily adjusted by varying the polymer blend ratio. The flexibility increased with increasing KSR content. At an 8% w/w coating level, a force of 3.2N was required to rupture the coating of the swollen tablet after 16h in the release medium; the coated tablets were thus robust to withstand gastrointestinal forces. The coating level (6%-10%, w/w) and dissolution agitation rate (50rpm to 150rpm) had no effect on the drug release. The water-insoluble carbamazepine was not released from the coated tablets as HPMC erosion, which is necessary for the release of a poorly water-soluble drug was hindered by the coating. The release of the water-soluble propranolol increased with increasing drug content and decreased with increasing HPMC content.


CONCLUSIONS
Poly vinyl acetate and ammonio methacrylate copolymer could be a proper polymer blend for coating HPMC matrix tablets to increase mechanical robustness, which characterized by its flexibility and permeability.
College of Pharmacy, Freie Universität Berlin, Kelchstr. 31, 12169 Berlin, Germany. Electronic address: rebaz.ali@univsul.edu.iq.
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Ali
College of Pharmacy, Freie Universität Berlin, Kelchstr. 31, 12169 Berlin, Germany. Electronic address: a.dashevskiy@fu-berlin.de.
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Dashevsky
College of Pharmacy, Freie Universität Berlin, Kelchstr. 31, 12169 Berlin, Germany. Electronic address: bodmeier@zedat.fu-berlin.de.
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Bodmeier
D002110:Caffeine / Q000008:administration & dosage / Q000737:chemistry; D002220:Carbamazepine / Q000008:administration & dosage / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004339:Drug Compounding; D065546:Drug Liberation; D005079:Excipients / Q000737:chemistry*; D065347:Hypromellose Derivatives / Q000737:chemistry*; D010539:Permeability; D011108:Polymers / Q000737:chemistry*; D011145:Polyvinyls / Q000737:chemistry*; D011433:Propranolol / Q000008:administration & dosage / Q000737:chemistry; D012995:Solubility; D013607:Tablets
D005079:Excipients; D011108:Polymers; D011145:Polyvinyls; D013607:Tablets; C013215:polyvinyl acetate; D002220:Carbamazepine; D002110:Caffeine; D065347:Hypromellose Derivatives; C058665:Eudragit RL; D011433:Propranolol
Ammonio methacrylate copolymer; HPMC; Matrix tablet; Mechanical properties; Oral controlled release; Poly vinyl acetate