A pharma-robust design method to investigate the effect of PEG and PEO on matrix tablets.
Even though polyethyleneoxide (PEO)-polyethyleneglycol (PEG) blends have been used widely for sustained release matrix tablets, evaluations of the effects of PEG or PEO on the matrix properties have been limited. In order to evaluate gelling behavior and drug release profiles of PEG, various contents of the polymers were investigated through a robust experimental design method. When exposed to an aqueous environment, the PEO-PEG matrix hydrated slowly and swelled, causing a thick gel layer to form on the surface, the thickness of which increased significantly depending on the PEG contents. Since polyacrylate plates were used for the study, the matrix was not completely hydrated and gelled even after 5h. However, the results could be applied to the time-oriented responses RD (robust design) models to obtain optimal settings and responses for the observed times. The optimal settings of PEO and PEG were 94.26 and 140.04 mg, respectively (PEG rate of 148.57%). Moreover, as the amount of PEG increased, the release rate also increased. When the formulation contained more than 150% of PEG, most of the drug loaded in the tablet was released in about 12 h. When the amount of PEG was less than 100%, the drug release rate was sustained significantly. Based on the RD optimization model for drug release, the optimal settings were PEG and PEO of 124.3 and 110 mg, respectively (PEG rate of 88.50%). Therefore, PEG rate of about 90-150% is suggested for matrix tablet formulations, and the exact ratio could be formulated according to the resulting tablet's properties.
Park
Jun Sang
JS
GL PharmTech Corp., Seongnam, Gyeonggi, 462-807, South Korea.
Shim
Ji Yeon
JY
Nguyen
Khoa Viet Truong
KV
Park
Jung Soo
JS
Shin
Sangmun
S
Choi
Young Wook
YW
Lee
Jaehwi
J
Yoon
Jeong-Hyun
JH
Jeong
Seong Hoon
SH
D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004058:Diffusion; D004339:Drug Compounding; D005782:Gels; D007700:Kinetics; D008956:Models, Chemical; D015233:Models, Statistical; D011092:Polyethylene Glycols / Q000737:chemistry*; D011224:Prazosin / Q000031:analogs & derivatives* / Q000737:chemistry; D012995:Solubility; D013607:Tablets; D013678:Technology, Pharmaceutical / Q000379:methods*; D014867:Water / Q000737:chemistry
D003692:Delayed-Action Preparations; D005782:Gels; D013607:Tablets; D014867:Water; D011092:Polyethylene Glycols; C041226:Terazosin; D011224:Prazosin