盐酸罗哌卡因明胶微球的药效学研究
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The preparation and characteristic pharmacodynamics s of Ropivacaine Gelatin Microspheres
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    摘要:目的 采用乳化-交联的方法制备盐酸罗哌卡因明胶微球并探讨其药效学特性。方法 采用乳化-交联法制备盐酸罗哌卡因明胶微球,高倍显微镜观察微球粒径大小及形态,紫外分光光度法检测微球中盐酸罗哌卡因的含量,外科植入手术法给药将其植入大鼠坐骨神经,观测其镇痛持续时间及其对运动的影响。结果 盐酸罗哌卡因和明胶制成的盐酸罗哌卡因明胶微球为深黄色粉末,光镜下呈散在圆形,平均粒径约28.9士9.8um,计算出盐酸罗哌卡因微球的载药量为21.4%,药物包封产率为74.8%,制备工艺优选中盐酸罗哌卡因与明胶最佳投料比1:2.5。体内药效学显示微球可较明显地延长盐酸罗哌卡因镇痛持续时间至4小时以上。结论: 盐酸罗哌卡因明胶微球是一种较新剂型,原材料易得,制备工艺简便,自制的微球具有一定的缓释性,能适当延长罗哌卡因作用时间。

    Abstract:

    Objective: to study the preparation and pharmacodynamics of Ropivacaine Gelatin Microspheres . Method: Ropivacaine Gelatin Microspheres were prepared by emulsion-crosslinking method, and were observed by super-microscope and the diameter of microsphere was measured, the content of ropivacaine is measured by method of ultraviolet spectrophotometer. The microspheres were also implanted into rats’s sciatic nerve to study the maintainess time of analgesia. Results: the Ropivacaine Gelatin Microspheres were deep yellow powders and they were globular when observed in the super-microscope. The average diameter of the RPGMs were 28.9士9.8um The content of ropivacaine in the microspheres is 21.4%,and the ratio of drug envelopment is 74.8%. The best ratios of RP and carriers was 1:2.5. The results of phamacodynamics in rats showed Ropivacaine Gelatin Microspheres could prolonged the time of analgesia to about 4 hours. Conclusion: The Ropivacaine Gelatin Microspheres is an new altered dosage form and preparing method easy,hading good erties of drug sustain releasing. They can prolong the analgesia time of ropivacaine

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陆璐. 盐酸罗哌卡因明胶微球的药效学研究[J]. 科学技术与工程, 2010, (35): .
LULU. The preparation and characteristic pharmacodynamics s of Ropivacaine Gelatin Microspheres[J]. Science Technology and Engineering,2010,(35).

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  • 收稿日期:2010-03-23
  • 最后修改日期:2010-06-09
  • 录用日期:2010-06-11
  • 在线发布日期: 2010-11-19
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