中国组织工程研究
中國組織工程研究
중국조직공정연구
Journal of Clinical Rehabilitative Tissue Engineering Research
2013年
29期
5337-5344
,共8页
谢明全%刘惠娟%李平%李玉民
謝明全%劉惠娟%李平%李玉民
사명전%류혜연%리평%리옥민
生物材料%生物材料与药物控释%卡马西平%壳聚糖%海藻酸钠%纳米粒%pH敏感性%磁敏感性%凝胶小球%性能%省级基金
生物材料%生物材料與藥物控釋%卡馬西平%殼聚糖%海藻痠鈉%納米粒%pH敏感性%磁敏感性%凝膠小毬%性能%省級基金
생물재료%생물재료여약물공석%잡마서평%각취당%해조산납%납미립%pH민감성%자민감성%응효소구%성능%성급기금
biomaterials%biomaterials and controlled drug release%carbamazepine%chitosan%alginate%nanoparticles%pH sensitivity%magnetic sensitivity%hydrogel beads%property%provincial grants-supported paper
背景：卡马西平药物剂型存在设计不足或缺陷，导致该药吸收不规则，个体间药代动力学差异大，治疗浓度范围窄，临床上需要进行治疗药物监测。目的：制备卡马西平pH/磁双重敏感性凝胶小球，评价其性能。方法：以壳聚糖、海藻酸钠和 Fe3O4纳米粒为主要载体材料，采用离子凝胶法成功将抗癫痫药卡马西平载入卡马西平pH/磁双重敏感性凝胶小球，并采用L9(34)正交试验设计优化凝胶小球处方组成及制备工艺，通过扫描电镜法、红外光谱法对凝胶小球的表面形态及内部结构进行表征，并检测其超顺磁性、溶胀度和体外释放性能。结果与结论：最佳制备工艺条件为：壳聚糖浓度0.5%，海藻酸钠浓度1.5%，氯化钙浓度2.0%，磁载比为1∶2。所得凝胶小球形状圆整，表面光滑，平均包封率为94.36%，载药量为25.05%，粒径为1.0-2.0 mm。卡马西平pH/磁双重敏感性凝胶小球具有超顺磁性，溶胀度与介质pH关联，在模拟胃液中2 h，累积释放率达22.77%，转移到模拟肠液中24 h后，累积释放率达91.63%。表明卡马西平pH/磁双重敏感性凝胶小球处方组成合理，制备工艺可行，具有明显的pH敏感性和磁敏感性，控释性能良好。
揹景：卡馬西平藥物劑型存在設計不足或缺陷，導緻該藥吸收不規則，箇體間藥代動力學差異大，治療濃度範圍窄，臨床上需要進行治療藥物鑑測。目的：製備卡馬西平pH/磁雙重敏感性凝膠小毬，評價其性能。方法：以殼聚糖、海藻痠鈉和 Fe3O4納米粒為主要載體材料，採用離子凝膠法成功將抗癲癇藥卡馬西平載入卡馬西平pH/磁雙重敏感性凝膠小毬，併採用L9(34)正交試驗設計優化凝膠小毬處方組成及製備工藝，通過掃描電鏡法、紅外光譜法對凝膠小毬的錶麵形態及內部結構進行錶徵，併檢測其超順磁性、溶脹度和體外釋放性能。結果與結論：最佳製備工藝條件為：殼聚糖濃度0.5%，海藻痠鈉濃度1.5%，氯化鈣濃度2.0%，磁載比為1∶2。所得凝膠小毬形狀圓整，錶麵光滑，平均包封率為94.36%，載藥量為25.05%，粒徑為1.0-2.0 mm。卡馬西平pH/磁雙重敏感性凝膠小毬具有超順磁性，溶脹度與介質pH關聯，在模擬胃液中2 h，纍積釋放率達22.77%，轉移到模擬腸液中24 h後，纍積釋放率達91.63%。錶明卡馬西平pH/磁雙重敏感性凝膠小毬處方組成閤理，製備工藝可行，具有明顯的pH敏感性和磁敏感性，控釋性能良好。
배경：잡마서평약물제형존재설계불족혹결함，도치해약흡수불규칙，개체간약대동역학차이대，치료농도범위착，림상상수요진행치료약물감측。목적：제비잡마서평pH/자쌍중민감성응효소구，평개기성능。방법：이각취당、해조산납화 Fe3O4납미립위주요재체재료，채용리자응효법성공장항전간약잡마서평재입잡마서평pH/자쌍중민감성응효소구，병채용L9(34)정교시험설계우화응효소구처방조성급제비공예，통과소묘전경법、홍외광보법대응효소구적표면형태급내부결구진행표정，병검측기초순자성、용창도화체외석방성능。결과여결론：최가제비공예조건위：각취당농도0.5%，해조산납농도1.5%，록화개농도2.0%，자재비위1∶2。소득응효소구형상원정，표면광활，평균포봉솔위94.36%，재약량위25.05%，립경위1.0-2.0 mm。잡마서평pH/자쌍중민감성응효소구구유초순자성，용창도여개질pH관련，재모의위액중2 h，루적석방솔체22.77%，전이도모의장액중24 h후，루적석방솔체91.63%。표명잡마서평pH/자쌍중민감성응효소구처방조성합리，제비공예가행，구유명현적pH민감성화자민감성，공석성능량호。
BACKGROUND:The faults or defects in pharmaceutical dosage form designed for carbamazepine may lead to irregular drug absorption, great individual differences between the pharmacokinetics, narrow therapeutic concentration range, and the therapeutic drug monitoring for this drug. OBJECTIVE:To prepare a magnetic/pH double sensitive hydrogel beads carrying carbamazepine and to evaluate its properties. METHODS:Using chitosan, alginate and Fe3O4 nanoparticle as carrier materials, the magnetic/pH double sensitive hydrogel beads carrying anti-epileptic carbamazepine were prepared, and the composition and preparation technology were optimized by orthogonal test of L9(34). The surface morphology and structure of the hydrogel beads were characterized by scanning electron microscopy and Fourier transform infrared spectroscopy respectively. Also, the superparamagnetism, swel ing and release in vitro of hydrogel beads were determined. RESULTS AND CONCLUSION:The optimized preparation technology were described as:0.5%(w/v) chitosan, 1.5%(w/v) alginate, 2.0%(w/v) calcium chloride, and 1:2 ratio for magnetic versus carrier materials. The hydrogel beads under the optimal preparation conditions showed a round shape and smooth surface, and average encapsulation efficiency, loading efficiency and hydrogel beads diameter were 94.36%, 25.05%and 1-2 mm respectively. The hydrogel beads appeared to have superparamagnetism, the swel ing degrees were associated with pH value of medium, and the sequential release amount of carbamazepine from the hydrogel beads in simulated gastric fluid was 22.77%for 2 hours. Then, the beads were moved to the simulated intestinal fluid, and this value approached 91.63%for 24 hours. Experimental findings indicate that, the composition and preparation technology of magnetic/pH double sensitive hydrogel beads carrying carbamazepine was rational and feasible, and hydrogel beads show obvious pH sensitivity and magnetic sensitivety. The control ed-release effect of hydrogel beads in vitro is also good.
