PH对盐酸氯胺酮离体家兔鼻粘膜渗透性的影响
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文章编号：(2003)01-0001-05,PH对盐酸氯胺酮离体家兔鼻粘膜渗透性的影响
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王惠姝1，张 锦2 ，徐 晖1 ，陈大为1，丁平田1
(1.沈阳药科大学药学院，辽宁沈阳 110016; 2. 中国医科大学第二临床学院麻醉科，辽宁沈阳110014)
摘要：目的 研究pH值对盐酸氯胺酮经离体家兔鼻粘膜渗透性的影响，为经鼻腔给药的处方设计和优化提供依据。方法 用体外扩散实验考察各种pH值条件下离体兔鼻粘膜对氯胺酮的透过性。结果 pH值小于7.40时,氯胺酮的渗透系数无明显的变化,而当pH值由7.40升高至8.23时，渗透系数大幅度增加。结论 pH对氯胺酮经离体兔鼻粘膜的渗透性有较大的影响。对于弱酸弱碱性药物，pH值是一个必须考虑的处方因素。
关键词：药剂学；鼻腔给药；鼻粘膜渗透性；盐酸氯胺酮； pH
中图分类号：R94 文献标识码：A
Effects of pH on the permeability of ketamine hydrochloride through excised rabbit nasal mucosa
WANG Hui-shu1, ZHANG Jin2, XU Hui1, CHEN Da-wei1, DING Ping-tian1
(1. School of Pharmacy, Shenyang Pharmaceutical University， Shenyang 110016, China; 2. Department of Anesthesiology，China Medical University Attached Second Hospital，Shenyang 110014，China)
Abstract: Objective To study the effects of pH on the nasal permeability of ketamine hydrochloride (KET·HCl). Methods The permeability of KET across excised rabbit nasal mucosa was measured using in vitro diffusion cell method at various pH. Results The partition coefficient does not vary obviously when the pH in donor is below 7.40, while it increases markedly when pH changed from 7.40 to 8.23. Conclusion The pH value is an important factor that affected the penetrability of ketamine hydrochloride through the excised rabbit nasal mucosa, which must be considered when designing a nasal used formulation, especially for a weak base or acid drug.
Key words: pharmaceutics; nasal drug administration；nasal permeability；ketamine hydrochloride；pH value
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