Modeling the controlled release of drug embedded in a plate-like polymer matrix

The controlled release of over-loaded drug in a plate-like polymer matrix, the Higuchi's problem, is investigated theoretically. Taking the advantage of Landau transformation, we restore the concentration profile of drug in a polymer matrix, the rate of release of drug from the polymer matrix, and the temporal variation of location of the moving boundary taking the external mass transfer resistance into account. The applicability of the series of moving boundaries, a numerical approach often adopted, is examined. We found that it may become ineffective when the over-loading of drug in a polymer matrix is too small. In contrast, our method has no such limitation. We conclude that assuming the transfer of drug to occur at a pseudo-steady-state condition is inadequate if the degree of over-loading for drug is low or the external mass transfer resistance is significant.     

核桃壳活性炭的制备及其对烟酸缓释性能的研究

以二氧化碳(CO2)物理活化法制备了核桃壳活性炭,考察了活化温度、活化时间对核桃壳活性炭得率及烟酸吸附量的影响。以所制备的核桃壳活性炭为烟酸载体,在不同的释放介质(蒸馏水、人工胃液或人工肠液)中进行烟酸释放性能研究。结果表明,人工胃液和人工肠液能促进活性炭对烟酸的释放,其累计释放率分别达到43.96%和47.69%。核桃壳活性炭在3种不同介质中的不同释放阶段的释放过程均符合Higuchi模型。     

Curcumin nanoemulsion for transdermal application: formulation and evaluation

The aim of this work is to develop a curcumin nanoemulsion for transdermal delivery. The incorporation of curcumin inside a nanoglobul should improve curcumin stability and permeability. A nanoemulsion was prepared by the self-nanoemulsification method, using an oil phase of glyceryl monooleate, Cremophor RH40 and polyethylene glycol 400. Evaluation of the nanoemulsion included analysis of particle size, polydispersity index, zeta potential, physical stability, Raman spectrum and morphology. In addition, the physical performance of the nanoemulsion in Viscolam AT 100P gel was studied. A modified vertical diffusion cell and shed snake skin of Python reticulatus were used to study the in vitro permeation of curcumin. A spontaneously formed stable nanoemulsion has a loading capacity of 350?mg curcumin/10?g of oil phase. The mean droplet diameter, polydispersity index and zeta potential of optimized nanoemulsion were 85.0?±?1.5?nm, 0.18?±?0.0 and ?5.9?±?0.3?mV, respectively. Curcumin in a nanoemulsion was more stable than unencapsulated curcumin. Furthermore, nanoemulsification significantly improved the permeation flux of curcumin from the hydrophilic matrix gel; the release kinetic of curcumin changed from zero order to a Higuchi release profile. Overall, the developed nanoemulsion system not only improved curcumin permeability but also protected the curcumin from chemical degradation.     

中药白芷中欧前胡素、异欧前胡素体外经皮渗透特性的串联质谱研究

欧前胡素和异欧前胡素属于6,7-呋喃香豆素类化合物,是中药白芷的主要药效成分。为了考察二者的经皮渗透特性,采用改进型的Franz扩散池,以大鼠离体皮肤作为渗透屏障,以高效液相色谱-串联质谱（HPLC-MS/MS）法测定白芷提取液的经皮渗透液中欧前胡素和异欧前胡素的含量,据此来考察白芷提取液中欧前胡素和异欧前胡素的经皮渗透特性。实验结果表明,欧前胡素和异欧前胡素在48 h内,单位面积的累积渗透量分别为116.11 μg/cm²和140.84 μg/cm²,累积渗透百分率分别为37.75%和71.86%。欧前胡素的稳态渗透速率为26.5 μg/h•cm²,其体外经皮渗透符合Higuchi方程。本研究阐明了欧前胡素的体外经皮渗透机制,可为白芷作为外用经皮给药制剂的发展提供实验依据和理论基础。     

APPLICATION OF GELATIN FOR ENCAPSULATING ASPIRIN INTO ETHYL CELLULOSE MICROCAPSULE IN AN O/W EMULSION

The application of gelatin protective colloid for microencapsulating aspirin in ethylcellulose was demonstrated using an oil-in-water emulsification/solvent evaporation technique. The gelatin concentration, alcohol co-solvent amount, and ethylcellulose viscosity were investigated by analyzing the recovered weight, particle size distribution, drug loading efficiency, aspirin release rate, surface characteristics, and release kinetics. Results showed that recovery increased with greater concentrations of gelatin (up to 1%). Adding co-solvent (ethanol) also changed the microcapsule particle size distribution. Higher recovery and release rates were obtained when the ethanol content in polymer solvent was at 25% and the viscosity of ethylcellulose was low (45cps). The release rate followed Higuchi matrix release kinetics, suggesting a monolithic system with aspirin uniformly distributed over the microcapsule.     

磺胺类药物在丝素膜中的释放及释放机理

通过实验测定了磺胺类药物在丝素膜中的释放情况,得出了此类药物的释放规律,并研究了其释放机理.     

Evaluation of AISI 4140 Steel Repair Without Post-Weld Heat Treatment

The present work evaluates the two-layer technique on the heat affected zone (HAZ) of AISI 4140 steel welded with different heat input levels between the first and second layer. The weld heat input levels selected by the Higuchi test were 5/5, 5/10, and 15/5 kJ/cm. The evaluation of the refining and/or tempering of the coarsened grain HAZ of the first layer was carried out using metallographic tests, microhardness measurements, and the Charpy-V impact test. The tempering of the first layer was only reached when the weld heat input ratio was 5/5 kJ/cm. The results of the Charpy-V impact test showed that the two-layer technique was efficient, from the point of view of toughness, since the toughness values reached were greater than the base metal for all weld heat input ratios applied. The results obtained indicate that the best performance of the two-layer deposition technique was for the weld heat input ratio 5/5 kJ/cm employing low heat input.     

APPLICATION OF GELATIN FOR ENCAPSULATING ASPIRIN INTO ETHYL CELLULOSE MICROCAPSULE IN AN O/W EMULSION

The application of gelatin protective colloid for microencapsulating aspirin in ethylcellulose was demonstrated using an oil-in-water emulsification/solvent evaporation technique. The gelatin concentration, alcohol co-solvent amount, and ethylcellulose viscosity were investigated by analyzing the recovered weight, particle size distribution, drug loading efficiency, aspirin release rate, surface characteristics, and release kinetics. Results showed that recovery increased with greater concentrations of gelatin (up to 1%). Adding co-solvent (ethanol) also changed the microcapsule particle size distribution. Higher recovery and release rates were obtained when the ethanol content in polymer solvent was at 25% and the viscosity of ethylcellulose was low (45cps). The release rate followed Higuchi matrix release kinetics, suggesting a monolithic system with aspirin uniformly distributed over the microcapsule.     

盐酸二甲双胍缓释片的制备工艺及体外释放度研究

制备盐酸二甲双胍缓释片,并建立测定其释放度的方法。采用羟丙甲纤维素（HPMC）为缓释材料制备盐酸二甲双胍缓释片,用紫外分光光度法测定其释放度。考察了填充剂的种类、粘合剂的种类对本品释放度的影响,井采用正交试验进行处方优化。依据最优处方制备了三批缓释片。与盐酸二甲双胍普通片比较,本品有显著的缓释效果,其体外释放度曲线12g内符合Higuchi方程。     

Properties of Hot-Melt Extruded Theophylline Tablets Containing Poly(Vinyl Acetate)

The objectives of this study were to investigate the properties of poly(vinyl acetate) (PVAc) as a retardant polymer and to study the drug release mechanism of theophylline from matrix tablets prepared by hot-melt extrusion. A physical mixture of drug, polymer, and drug release modifiers was fed into the equipment and heated inside the barrel of the extruder. The cylindrical extrudates were either cut into tablets or ground into granules and compressed with other excipients into tablets. Due to the low glass transition temperature of the PVAc, the melt extrusion process was conducted at approximately 70°C. Theophylline was used as the model drug in this study. Theophylline was present in the extrudate in its crystalline form and was released from the tablets by diffusion. The Higuchi diffusion model and percolation theories were applied to the dissolution data to explain the drug release properties of the matrix systems. The release rate was shown to be dependent on the granule size, drug particle size, and drug loading in the tablets. Water-soluble polymers were demonstrated to be efficient release rate modifiers for this system.