Prolongation of nerve block by complexation of local anesthetic with cyclodextrin

通过局麻药与环糊精的络合延长神经阻滞

基本信息

  • 批准号:
    12470323
  • 负责人:
  • 金额:
    $ 4.61万
  • 依托单位:
  • 依托单位国家:
    日本
  • 项目类别:
    Grant-in-Aid for Scientific Research (B)
  • 财政年份:
    2000
  • 资助国家:
    日本
  • 起止时间:
    2000 至 2001
  • 项目状态:
    已结题

项目摘要

Background : Neural blockade is widely used for acute and chronic pain management, however existing local anesthetics have a short duration of action. The cyclodextrin-based drug delivery system, consisting of levobupivacaine complexed with maltosyl-β-cyclodextrin, was used in spinal and sciatic nerve blocks in rats, anticipating the prolonged local anesthetic effect.Methods : Muscle tone and tail flick latency were studied over time following intrathecal administration of the complex of levobupivacaine with maltosyl-β-cyclodextrin in rats. In addition, the time course of changes in proprioception, motor function, and nociception following circumferential subcutaneous administration of the complex to the sciatic nerve were also examined.Results : With the intrathecal block, all rats stopped tail movement immediately after injection of the local anesthetics. Intrathecal injection of the complexed levobupivacaine significantly prolonged motor blockade, but not sensory blockade. In sciatic nerve block, all rats were temporarily immobilized after injection of levobupivacaine, its complexed form significantly prolonging the anesthetic effects, as evaluated by proprioception, motor function, and nociception. Furthermore, neither histological nor neurological signs were observed following the nerve blocks with the levobupivacaine preparations tested.Conclusions : The complexation of levobupivacaine with maltosyl-β-cyclodextrin safely prolonged the anesthetic effect of levobupivacaine in both intrathecal and sciatic nerve blocks in rats. The complexation of levobupivacaine with maltosyl-β-cyclodextrin is particularly useful for designing safer and long-acting formulations for levobupivacaine in both intrathecal and sciatic nerve blocks.
背景:神经阻滞广泛用于急慢性疼痛的治疗,但现有的局麻药作用时间较短。将左旋布比卡因与麦芽糖基-β-环糊精复合构成的环糊精给药系统应用于大鼠脊髓和坐骨神经阻滞,以期获得较长的局麻药效应。方法:鞘内注射左旋布比卡因-麦芽糖基-β-环糊精复合体,观察肌张力和甩尾潜伏期的变化。结果:鞘内阻滞后,所有大鼠在注射局麻药后立即停止尾部运动。鞘内注射复合左旋布比卡因可显著延长运动阻滞时间,但不能延长感觉阻滞时间。在坐骨神经阻滞中,所有大鼠在注射左旋布比卡因后都被暂时固定,其复合体明显延长了麻醉效果,通过本体感觉、运动功能和伤害性感觉来评价。结论:左旋布比卡因与麦芽糖基-β-环糊精的络合作用安全地延长了左旋布比卡因在鞘内和坐骨神经阻滞中的麻醉效果。左旋布比卡因与麦芽糖基-β-环糊精的络合对于设计鞘内和坐骨神经阻滞中左旋布比卡因更安全和长效的制剂特别有用。

项目成果

期刊论文数量(6)
专著数量(0)
科研奖励数量(0)
会议论文数量(0)
专利数量(0)
Karashima Ken, Nakamura Tadashi and Takasaki Mayumi: "Prolongation of nerve block by complexation of levobupivacaine with cyclodextrin"Journal of Anesthesia. 15 Suppl. Pd1K01 (2001)
Karashima Ken、Nakamura Tadashi 和 Takasaki Mayumi:“左布比卡因与环糊精络合延长神经阻滞”麻醉杂志。
  • DOI:
  • 发表时间:
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  • 影响因子:
    0
  • 作者:
  • 通讯作者:
辛島 謙: "シクロデキストリンによるレボブピバカインの効果延長について"Journal of Anesthesia. 15 Suppl. Pd1KOl (2001)
Ken Karashima:“环糊精延长左布比卡因的作用”麻醉杂志 15 Suppl。
  • DOI:
  • 发表时间:
  • 期刊:
  • 影响因子:
    0
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  • 通讯作者:
辛島謙: "シクロデキストリンによるレボブピバカインの効果延長について"Journal of Anesthesia. 15Suppl. Pd1KO1 (2001)
Ken Karashima:“环糊精延长左布比卡因的作用”麻醉杂志 15Suppl。
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    0
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TAKASAKI Mayumi其他文献

TAKASAKI Mayumi的其他文献

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{{ truncateString('TAKASAKI Mayumi', 18)}}的其他基金

Studies of local anesthetics on use-dependent block
局麻药对使用依赖性阻滞的研究
  • 批准号:
    18591711
  • 财政年份:
    2006
  • 资助金额:
    $ 4.61万
  • 项目类别:
    Grant-in-Aid for Scientific Research (C)
Prolongation of anesthetic effects of levobupivacaine with maltosyl-β -cyclodextrin
麦芽糖基-β-环糊精延长左布比卡因的麻醉效果
  • 批准号:
    13557131
  • 财政年份:
    2001
  • 资助金额:
    $ 4.61万
  • 项目类别:
    Grant-in-Aid for Scientific Research (B)
Study for levobupivacaine
左布比卡因的研究
  • 批准号:
    10671427
  • 财政年份:
    1998
  • 资助金额:
    $ 4.61万
  • 项目类别:
    Grant-in-Aid for Scientific Research (C)
Pharmacological studies of the enantiomer of bupivacaine
布比卡因对映体的药理学研究
  • 批准号:
    08671755
  • 财政年份:
    1996
  • 资助金额:
    $ 4.61万
  • 项目类别:
    Grant-in-Aid for Scientific Research (C)
Clinical and laboratory investigations about preemptive analgesia
超前镇痛的临床和实验室研究
  • 批准号:
    06671541
  • 财政年份:
    1994
  • 资助金额:
    $ 4.61万
  • 项目类别:
    Grant-in-Aid for General Scientific Research (C)
Effect of epidural anesthesia on sympathetic nerve activities.
硬膜外麻醉对交感神经活动的影响。
  • 批准号:
    04670933
  • 财政年份:
    1992
  • 资助金额:
    $ 4.61万
  • 项目类别:
    Grant-in-Aid for General Scientific Research (C)
Does epidural anesthesia have protective effect on hemorrhagic shock?
硬膜外麻醉对失血性休克有保护作用吗?
  • 批准号:
    02807146
  • 财政年份:
    1990
  • 资助金额:
    $ 4.61万
  • 项目类别:
    Grant-in-Aid for General Scientific Research (C)

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