Evaluation of high molecular weight poly(oxyethylene) (Polyox) polymer: studies of flow properties and release rates of furosemide and captopril from controlled-release hard gelatin capsules.
The powder characteristics and the effect of the molecular weight of polymers as diluents on the release rate of furosemide and captopril from hard gelatin capsules were evaluated. The high molecular weight polymers studied were poly(oxyethylene) homopolymers (Polyox), with molecular weight ranging from 4,000,000 to 7,000,000. Powder characteristics suggested good flowability for these materials and predicted capsule fill weight uniformity. Swelling experiments showed a very high degree of swelling for these materials in both gastric and buffer solution. These polymers can sustain the release rate of both water-soluble and insoluble drugs from drug delivery systems. The low molecular weight polymers have a less pronounced sustained-release effect compared to the high molecular weight polymer material (i.e., those with 7,000,000 molecular weight). An increase in the content of polymer results in a decrease in the release rate of the drug. The solubility of the drugs clearly influenced the release rate. Release kinetics were evaluated and appeared to be influenced by the molecular weight of the polymer, the solubility of drug, and the ratio of the drug to polymer in the capsule. Bimodal release kinetics were exhibited by a number of furosemide formulations (i.e., F5 and F8).
Efentakis
M
M
University of Athens, School of Pharmacy, Department of Pharmaceutical Technology, Greece. efentakis@pharm.uoa.gr
Vlachou
M
M
D002214:Capsules; D002216:Captopril / Q000008:administration & dosage* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D005665:Furosemide / Q000008:administration & dosage* / Q000737:chemistry; D005780:Gelatin; D008970:Molecular Weight; D011108:Polymers / Q000008:administration & dosage; D012995:Solubility
D002214:Capsules; D003692:Delayed-Action Preparations; D011108:Polymers; D005665:Furosemide; D005780:Gelatin; D002216:Captopril