得到性能良好的SA/PU共混微球以用于药物缓控释;方法:利用预聚-扩链-中和-分散法合成阴离子型PU水溶液;将SA水溶液与PU水溶液按质量比为1∶1,1∶2,1∶3,1∶4,1∶5混合,用滴制法制备共混微球;测定了微球的凝胶化、圆整性及溶胀性能。结果表明:用TDI与PEG-6000和PEG-4000反应才能制备出PU水溶液,而只有水溶液才能和海藻酸钠水溶液混合完全得到理想的共混溶液;SA/PU共混微球28h后凝胶化完全,SA微球48h后可凝胶化完全。PEG-6000合成的PU与海藻酸钠共混得到的微球圆整性要好于PEG-4000合成的PU与海藻酸钠共混得到的微球。且随着复合微球中PU的含量增大,微球的圆整性变好;SA/PU复合微球在蒸馏水(pH7)和盐酸(pH1)中均不溶胀,在磷酸缓冲溶液(pH6.86)中快速溶胀,在4~5h后开始崩解。结论:SA/PU复合微球在胃液中保持原状,在肠液中溶胀,可作为药物的缓释载体。
Objective: The study was aimed at obtaining favourable SA/PU complex hydrogel microspheres for drug controlled delivery System. Methods: First PU anionic solution was synthesized by prepolymer-chain-neutralization-dispersion. Subsequently SA solution and PU solution was completely mixed with different quality rate (1 ~ 1,1 : 2,1 : 3,1 : 4, 1 : 5), which was trickled to shape complex microspheres. Finally, the nature including gelatinize, round and swelling of microspheres was determined. Results: PU solution, which could only be synthesized by TDI responded with PEG-6000 or PEG-4000, could be mingled with SA solution to form ideal solution. SA/PU microspheres were gelatinized completely in 28 hours and SA microspheres was 48 hours. The entire round of microspheres formed by composite solution of PU which was synthesis by PEG-6000 and SA was better than that of PEG-4000, and with content of PU in the complex micro spheres increased, roundness was improved. SA/PU microspheres didn't swell in distilled water (pH 7) and HC1 (pH 1), but them swelled rapidly in phosphate buffer solution (pH 6.86) and disaggregated after 4-5 hours in phosphate. Conclusion: SA/PU composite microspheres in gastric juice doesn't changed, but swell in intestinal fluid, so them can be used as drug delivery carrier.