A predictive model for the release of slightly water-soluble drugs from HPMC matrices.
A model to predict the fraction of slightly water-soluble drug released as a function of release time (t, h), HPMC concentration (C(H), w/w), drug solubility in distilled water at 37 degrees C (C(s), g/100 mL), and volume of drug molecule (V, nm3) was derived when theophyline, tinidazole, and propylthiouracil were selected as model drugs. The model is log (M(t)/M(infinity)) = 0.8683 logt-0.1930C(s) logt + 0.5406V logt-1.227C(H) + 0.1594C(s) + 0.4423C(H)C(s) - 0.8655 (n = 130, r = 0.9969), where Mt is the amount of drug released at time t, Minfinity is the amount of drug released over a very long time, which corresponds in principle to the initial loading, n is the number of samples, and r is the correlation coefficient. The model was validated using sulfamethoxazole and satisfactory results were obtained. The model can be used to predict the release fraction of variousslightly water-soluble drugs from HPMC matrices having different polymer levels.
Fu
X C
XC
Department of Pharmacy, Zhejiang University City College, Hangzhou, P.R. China. Fuxc@zucc.edu.cn
Wang
G P
GP
Wang
Y H
YH
Liang
W Q
WQ
D003692:Delayed-Action Preparations; D004058:Diffusion; D005079:Excipients; D007700:Kinetics; D007785:Lactose / Q000031:analogs & derivatives* / Q000737:chemistry*; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry*; D008956:Models, Chemical; D008970:Molecular Weight; D010078:Oxazines; D011237:Predictive Value of Tests; D012995:Solubility; D013607:Tablets; D014867:Water
D003692:Delayed-Action Preparations; D005079:Excipients; D010078:Oxazines; D013607:Tablets; D014867:Water; D008747:Methylcellulose; C071191:MK 458; D007785:Lactose