The objectives of this study were to investigate the effect of storage temperature on drug release from matrices containing 10, 40 and 70% w/w ibuprofen in Kollidon® SR (KSR). The matrix tablets were produced by direct compression and then kept at 30 and 45 °C for 3 months. Drug release from the matrix tablets was examined after storage for 0, 1, 4 and 12 weeks. Scanning electron microscope was used to reveal physical appearance of the tablet surface at the respective time intervals. In addition, differential scanning calorimeter was used to investigate glass transition temperature (Tg) of ibuprofen in KSR at 0-100% w/w based on the principle of Gordon-Taylor equation. At 45 °C, the dissolution of ibuprofen in KSR as well as the coalescence of polymer particles were observed to be higher than those of storage at 30 °C. The physical state of ibuprofen dispersed in the polymeric matrix and degree of polymer coalescence led to the variation of drug release. The coalescence of polymer particles was a result of the polymer transition from glassy to rubbery state according to water absorption of KSR and plasticizing effect of ibuprofen. The reduction of the Tg of ibuprofen blended with KSR could be better described by the Kwei equation, a modified version of Gordon-Taylor equation.
The objective of this study was to investigate thermal and mechanical properties as well as in vitro drug release of Eudragit® RL (ERL) film using chlorpheniramine maleate (CPM) as either active pharmaceutical ingredient or non-traditional plasticizer. Differential scanning calorimeter was used to measure the glass transition temperature (Tg) of 0-100% w/w CPM in ERL physical mixture. Instron testing machine was used to investigate Young's modulus, tensile stress and tensile strain (%) of ERL film containing 20-60% w/w CPM. Finally, a Franz diffusion cell was used to study drug release from ERL films obtained from four formulations, i.e. CRHP0/0, CRHP0/5, CRHP2/0 and CRHP2/5. The Tg of ERL was decreased when the weight percentage of CPM increased. The reduction of the Tg could be described by Kwei equation, indicating the interaction between CPM and ERL. Modulus and tensile stress decreased whereas tensile strain (%) increased when weight percentage of CPM increased. The change of mechanical properties was associated with the reduction of the Tg when weight percentage of CPM increased. ERL films obtained from four formulations could release the drug in no less than 10 h. Cumulative amount of drug release per unit area of ERL film containing only CPM (CRHP0/0) was lower than those obtained from the formulations containing traditional plasticizer (CRHP0/5), surfactant (CRHP2/0) or both of them (CRHP2/5). The increase of drug release was a result of the increase of drug permeability through ERL film and drug solubility based on traditional plasticizer and surfactant, respectively.
Andrographolide (AGP), a major component of Andrographis paniculata (Burm.f.) Nees (AP), has several biological activities. Nevertheless, poorly water solubility and low bioavailability of AGP lead to decrease clinical benefits. Therefore, this study aims to develop of AP extract-chitosan solid dispersion using central composite design (CCD) to enhance AGP release. AP crude extract was obtained by Soxhlet extractor using 85%v/v ethanol as a solvent extraction. Then, AP extract, chitosan, and poloxamer 188 in the concentrations provided by CCD was spray dried. The in-vitro release of AP extract-chitosan spray dried powder was studied by dissolution equipped with enhancer cell in 200 ml of 50%v/v methanol at 37°C and 50 rpm of paddle speed. Samples were withdrawn at 0.25-96 hours and then determined AGP by UV spectrophotometer at 224 nm. The results of CCD indicated that %ethanol and %AGP from concentrated AP extract had significant (P < 0.05) effect on the concentration of AGP released at 5 hours. The optimum formulation composed of %ethanol of 18.25, %AGP in extract of 0.38, and %poloxamer 188 of 0.17 resulted in more AGP concentration at 5 hours than 50 μg/mL. Release kinetic study revealed that %release of the optimal formulation was best fitted to first order kinetic. In powder X-ray diffraction, intensity of AGP characteristic peaks in the optimal formulation decreased by 7.17-25.69 times compared with AGP standard. It was concluded that the optimal formulation of AP extract-chitosan solid dispersion could improve AGP release due to changing crystalline AGP to amorphous state.
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