Synthesis,characterization, and in vitro drug‐release properties of 2‐hydroxyethyl methacrylate copolymers

2‐Hydroxyethyl methacrylate was copolymerized with acrylamide, N‐vinyl‐2‐pyrrolidone, and n‐butyl methacrylate by free‐radical solution polymerization with α,α′‐azobisisobutyronitrile as an initiator at 70 ± 1°C. The average molecular weights and molar compositions of the resultant copolymers were determined with gel permeation chromatography and ¹H‐NMR spectroscopy data, respectively. Diclofenac or 2‐[(2,6‐dichlorophenyl)amino]benzene acetic acid, a nonsteroidal anti‐inflammatory drug, was chemically attached to the copolymers by transesterification reaction in the presence of N,N′‐dicyclohexylcarbodiimide to give macromolecular prodrugs. All the synthesized polymers were characterized with Fourier transform infrared, ¹H‐, and ¹³C‐NMR spectroscopy techniques. The polymer–drug conjugates were hydrolyzed in cellophane member dialysis bags containing aqueous buffered solutions (pH 8) at 37°C, and the hydrolysis solutions were detected by UV spectrophotometer at selected intervals. The results showed that the drug could be released by selective hydrolysis of the ester bond from the side chain of the drug moiety. The release profiles of the drug indicated that the hydrolytic behavior of polymeric prodrugs strongly depends on the hydrophilicity of the polymer. The results suggest that the synthesized copolymers could be useful carriers for the release of diclofenac in controlled‐release systems. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci 104: 2403–2409, 2007     

硅丙乳液的合成及其吸水性的研究

以丙烯酸丁酯、甲基丙烯酸甲酯、丙烯酸、乙烯基三乙氧基硅烷(VTES)为原料,分别采用半连续法、种子预乳化法和后添加VTES法制得了硅丙乳液。研究了聚合工艺对硅丙乳液的吸水率、冻融稳定性、钙离子稳定性等的影响。结果表明,采用半连续法和种子预乳化法制得的硅丙乳液,冻融稳定性比较好,经过冻融循环后可以复原;采用半连续法制得的乳胶膜的吸水率随着乙烯基三乙氧基硅烷的用量的增加而降低;采用后添加VTES法制得的硅丙乳液,其吸水率则随VTES用量的增加而升高,冻融循环后发生破乳。     

甲基丙烯酸缩水甘油酯熔融接枝聚丙烯研究

利用双螺杆挤出机研究甲基丙烯酸缩水甘油酯(GMA)接枝改性聚丙烯,探讨了停留时间、单体组成、引发剂用量等因素对接枝反应的影响。结果表明,通过工艺条件的控制在双螺杆挤出上可制备出接枝率高、流动性、色泽度良好的接枝产物。     

复合氨基酸月桂醇酯的合成及性能

以菜籽粕水解制得的复合氨基酸浓缩液为原料,与月桂醇酯化制得复合氨基酸月桂醇酯.探讨了物料配比、反应时间、带水剂及催化剂对合成的影响,并对产品的表面活性进行了测定.结果表明:合成反应的最佳条件是月桂醇与复合氨基酸的摩尔比为1∶2.甲苯作带水剂(反应温度110～122℃),反应时间为4h,催化剂浓H2SO4的用量为复合氨基酸的8%,少量的聚乙二醇(PEG600)作相转移催化剂.制得的产品具有良好的泡沫稳定性.     

甲基丙烯酸全氟辛基乙酯-甲基丙烯酸丁酯乳液共聚动力学

采用十二烷基硫酸钠和OP-10混合乳化剂，将甲基丙烯酸全氟辛基乙酯-甲基丙烯酸丁酯进行乳液共聚，研究了反应温度、引发剂浓度、乳化剂浓度、全氟单体浓度等因素对聚合速率(RP)的影响。结果表明，聚合速率随着引发剂浓度、乳化剂浓度的增加而增加；随着全氟单体浓度的增加而降低，该体系的表现活化自由能为106．27kJ／mol，RP∝[I]^.68，RP∝[S]^0.88，RP∝[FMA8]^0.33     

Dissolution and Solubility Behavior of Fenofibrate in Sodium Lauryl Sulfate Solutions

The solubility of fenofibrate in pH 6.8 McIlvaine buffers containing varying concentrations of sodium lauryl sulfate was determined. The dissolution behavior of fenofibrate was also examined in the same solutions with rotating disk experiments. It was observed that the enhancement in intrinsic dissolution rate was approximately 500-fold and the enhancement in solubility was approximately 2000-fold in a pH 6.8 buffer containing 2% (w/v) sodium lauryl sulfate compared to that in buffer alone. The micellar solubilization equilibrium coefficient (k*) was estimated from the solubility data and found to be 30884 ± 213 L/mol. The diffusivity for the free solute, 7.15 × 10^{? 6} cm²/s, was calculated using Schroeder's additive molal volume estimates and Hayduk-Laurie correlation. The diffusivity of the drug-loaded micelle, estimated from the experimental solubility and dissolution data and the calculated value for free solute diffusivity, was 0.86 × 10^{? 6} cm²/s. Thus, the much lower enhancement in dissolution of fenofibrate compared to its enhancement in solubility in surfactant solutions appears to be consistent with the contribution to the total transport due to enhanced micellar solubilization as well as a large decrease ( ～ 8-fold) in the diffusivity of the drug-loaded micelle.     

Synthesis of Hydroxypropyl Methacrylate/Polysaccharide Graft Copolymers as Matrices for Controlled Release Tablets

ABSTRACT

Hydrophilic matrices are an interesting option when developing drug delivery systems. With this aim, hydroxypropyl methacrylate was grafted onto hydroxypropyl starch and hydroxypropyl cellulose substrates by following the Ce(IV) redox initiation method. Different amounts of ethyleneglycol dimethacrylate, 7 and 34 mol%, as the crosslinking monomer, were also added. The drying of grafted products was carried out by lyophilization, obtaining white powders. Reaction yields (percent grafting, grafting efficiency, etc.) and some physical characteristics of the powders (particle size, moisture uptake, density, morphology, etc.) were determined. These parameters indicate how useful these products may be as potential matrices for direct compressed tablets. In this light, the powder flowability and the binding properties of each copolymer were determined. The graft copolymers can be considered of great interest as direct compression excipients. Due to their different chemical structure and composition, they showed differences in viscoelastic properties that revealed an interesting range of possibilities for use in drug delivery formulations. Tablets formulated with conventional excipients were also tested. Dissolution tests of various tablets were carried out. In 12 hr, 60–80% of the model drugs was released.     

Irradiation Grafted Polymeric Films. II. Gas Transport Properties of Hydrated Potassium Acrylate-Grafted Polyethylene Films

Abstract

The permeability constants of oxygen and carbon dioxide through hydrated potassium acrylate-grafted polyethylene films increase rapidly as the degree of hydration of the films increases above about 28 wt %. Below about 28 wt %, the carbon dioxide permeability constant increases with the degree of hydration. In the case of oxygen, the opposite is true.

The separation factor (CO₂/O₂) increases rapidly with film hydration up to about 28 wt %. Above this degree of hydration, the separation factor gradually approaches the value for pure water. An explanation for the results obtained is presented.     

Physical and Morphological Properties of Combined Treated Wood Polymer Composites by Maleic Anhydride and Methyl Methacrylate

Wood polymer composites were prepared by consecutive impregnation with maleic anhydride (MAN) and methyl methacrylate (MMA). Samples impregnated with MAN alone, were heated at 120°C and 150°C for 4 and 8 h. Based on the Fourier transform infrared (FT-IR) analysis and soaking-drying test results, treatment with MAN at 150°C for 4 h resulted in formation of stable crosslinks. In the second stage, MMA was used for in situ polymerization within MAN-treated wood. Field emission scanning electron microscopy observation and FT-IR analysis indicated that MMA copolymerized with MAN, and the resultant polymer filled up the lumen and is also grafted on to the cell wall. Improvement of water repellency and dimensional stability were observed in the treated samples, particularly in combined treated samples. The MAN/MMA treatment improved interaction between polymer and wood.