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Investigation of Insoluble Drug Release Behaviors from Hydroxypropyl Wethycellulose (HPMC) Matrices Tablets

Author: MaXiaoWei
Tutor: LiangWenQuan
School: Zhejiang University
Course: Pharmacy
Keywords: hydroxypropyl methycellulose(HPMC) Carbamazepine drug release drug release mechanism
CLC: R94
Type: Master's thesis
Year: 2002
Downloads: 418
Quote: 1
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Abstract


In previous research it have been Investigated to soluble drug release from hydroxypropyl methycellulose (HPMC) matrices tablets. The present research it have been investigated insoluble drug release from hydroxypropyl methycellulose matrices tablets. Carbamazepine (CBZ) was used as model insoluble drug. Drug release profile from hydrated matrices and HPMC erosion rate has been investigated. Several internal and external factors to effect drug release have been Investigated. The formulation factors involve drug load,The amount of HPMC and its viscosity,filling. The external factors were such as experimental setting the stirring rate. CBZ release rates were determined in dissolution setting and the HPMC matrices erosion rate were determined.Results show that fractional CBZ released decreases with increasing HPMC viscosity,while CBZ release rate is respectively 12.06,8.2,6. 45(%-h-1) for K4M,K15M,K100M. In addition,with an increase loading in HPMCK15M there was a corresponding decrease in release rate,while CBZ release rate is respectively 9.05,7.11,4.48,4.08,3.44(%-h"1) in HPMCK15M loading 10%,15%,20%,25%,30%. There was also same affect to the fractional CBZ released with its load dose. CBZ release rate for 50,100 and ISOrpm speed is 5.07,8.20,10.95(%-h"1) respectively,further indicate that with an increase in stirring rate there was a corresponding increase in release rate. Finally,Results indicate that the insoluble drug release rate from filling lactose was higher 32% compared to dextrin.An zero-order and Higuchi diffusion mechanism is frequently applied to the CBZ release data. In addition,The insoluble drug release has been also expressed as F(t) = a t1/2+3 t,while CBZ each release parameter was fitted by multiple linear regression analysis. The better fitting results suggested that insoluble drug (CBZ) release behavior was approximately zero-order kinetics. Results fitted by an Pappas exponential model suggested that the insoluble drug release from hydroxypropyl methycellulose matrices can be regarded as following matrix erosion mechanism.The mathematics model by matrix erosion rate and drug release from HPMCK15M are established for the fractional HPMC and drug released as MP(t)/MP((00) = - [0.80951n(t) + 1.2775]Meqc -ot-0.305,&nd Md(t)/Md(= - [0.1891t -0.1294]Meq -a9326. Finally,in comparison with the data of HPMCK4M matrix erosion and drug release from HPMCK4M matrices,theory value agree well with experimental data. The agreement indicates that the two mathematics models can be applied to desire insoluble drug release whose is governed by matrix erosion. Model pre’dictions for polymer and drug release agree well with observations,within 15% error. The two mathematics model imply that,if the release profiles are known for one HPMC type,release profile for other HPMC type can be predicted.

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