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Effects of drug solubility, drug loading, and polymer molecular weight on drug release from Polyox tablets.
Drug Dev Ind Pharm. 1998 Jul; 24(7):645-51.DD

Abstract

This study investigated the effects of polymer molecular weight, drug solubility, addition of a water-soluble excipient, and drug loading on zero-order release kinetics and elucidated the release mechanism of a drug from directly compressed tablets. Directly compressed tablets consisting of polyethylene oxides (PEO) (MW = 0.9, 2.0 and 4.0 x 10(6)) and drugs (solubility ranging from 290 to 25,000 mg/l) were formulated with or without a water-soluble excipient (lactose). For PEO tablets (MW = 0.9 x 10(6)), drug release is primarily swelling/erosion controlled for drugs for which solubility is below 1%, resulting in zero-order release kinetics. For PEO tablets (MW = 4.0 x 10(6)), drug release is controlled at a zero-order rate by the dissolution rate of the drug at high loading (39%). At low loading (20%), drug diffusion through the swollen gel layer becomes the governing release mechanism. For a highly water-soluble drug (e.g., diclofenac Na), drug diffusion is the controlling mechanism regardless of the molecular weight of the PEOs. Zero-order release kinetics can be achieved with PEO tablets (MW = 0.9 x 10(6)) for drugs for which solubility is below 1%. PEO tablets (MW = 2.0 x 10(6)) provided zero-order release for poorly water-soluble drugs (below 0.2%) at 39% drug loading. It is possible to attain zero-order release kinetics with PEO tablets (MW = 4.0 x 10(6)) using a drug which has a solubility of less than 0.1%.

Authors+Show Affiliations

School of Pharmacy, Temple University, Philadelphia, Pennsylvania 19140, USA.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

9876509

Citation

Kim, C J.. "Effects of Drug Solubility, Drug Loading, and Polymer Molecular Weight On Drug Release From Polyox Tablets." Drug Development and Industrial Pharmacy, vol. 24, no. 7, 1998, pp. 645-51.
Kim CJ. Effects of drug solubility, drug loading, and polymer molecular weight on drug release from Polyox tablets. Drug Dev Ind Pharm. 1998;24(7):645-51.
Kim, C. J. (1998). Effects of drug solubility, drug loading, and polymer molecular weight on drug release from Polyox tablets. Drug Development and Industrial Pharmacy, 24(7), 645-51.
Kim CJ. Effects of Drug Solubility, Drug Loading, and Polymer Molecular Weight On Drug Release From Polyox Tablets. Drug Dev Ind Pharm. 1998;24(7):645-51. PubMed PMID: 9876509.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of drug solubility, drug loading, and polymer molecular weight on drug release from Polyox tablets. A1 - Kim,C J, PY - 1999/1/7/pubmed PY - 1999/1/7/medline PY - 1999/1/7/entrez SP - 645 EP - 51 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 24 IS - 7 N2 - This study investigated the effects of polymer molecular weight, drug solubility, addition of a water-soluble excipient, and drug loading on zero-order release kinetics and elucidated the release mechanism of a drug from directly compressed tablets. Directly compressed tablets consisting of polyethylene oxides (PEO) (MW = 0.9, 2.0 and 4.0 x 10(6)) and drugs (solubility ranging from 290 to 25,000 mg/l) were formulated with or without a water-soluble excipient (lactose). For PEO tablets (MW = 0.9 x 10(6)), drug release is primarily swelling/erosion controlled for drugs for which solubility is below 1%, resulting in zero-order release kinetics. For PEO tablets (MW = 4.0 x 10(6)), drug release is controlled at a zero-order rate by the dissolution rate of the drug at high loading (39%). At low loading (20%), drug diffusion through the swollen gel layer becomes the governing release mechanism. For a highly water-soluble drug (e.g., diclofenac Na), drug diffusion is the controlling mechanism regardless of the molecular weight of the PEOs. Zero-order release kinetics can be achieved with PEO tablets (MW = 0.9 x 10(6)) for drugs for which solubility is below 1%. PEO tablets (MW = 2.0 x 10(6)) provided zero-order release for poorly water-soluble drugs (below 0.2%) at 39% drug loading. It is possible to attain zero-order release kinetics with PEO tablets (MW = 4.0 x 10(6)) using a drug which has a solubility of less than 0.1%. SN - 0363-9045 UR - https://www.unboundmedicine.com/medline/citation/9876509/Effects_of_drug_solubility_drug_loading_and_polymer_molecular_weight_on_drug_release_from_Polyox_tablets_ L2 - https://www.tandfonline.com/doi/full/10.3109/03639049809082366 DB - PRIME DP - Unbound Medicine ER -