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该实验研究了丹酚酸B在大鼠的鼻腔吸收特性,建立了HPLC测定灌流液中丹酚酸B的方法,考察了丹酚酸B的不同p H缓冲液对鼻腔的刺激性以及在鼻灌流液中的稳定性,并系统研究了丹酚酸B在体鼻黏膜吸收特性。采用改良的大鼠在体鼻循环模型,通过测定鼻灌流液中总蛋白和乳酸脱氢酶(LDH)的释放量,定量评价p H 4.0,5.0,6.0丹酚酸B磷酸缓冲液对大鼠鼻黏膜的刺激性及其在鼻灌流液中的稳定性,比较低、中、高质量浓度(200,400,800 mg·L-1)的p H 5.0丹酚酸B缓冲液中丹酚酸B大鼠鼻腔吸收特性。结果表明,鼻腔刺激性:p H 4.0>p H 5.0>p H 6.0,p H 6.0丹酚酸B缓冲液24 h内变化的RSD为3.1%,稳定性差。优选刺激性小,稳定性好的p H 5.0丹酚酸B缓冲液,其大鼠鼻灌流试验显示,丹酚酸B的鼻腔吸收符合一级吸收模型,为被动扩散。p H 5.0的丹酚酸B缓冲液对鼻腔刺激性小,稳定性良好,在大鼠鼻灌流试验中吸收良好,对丹酚酸B鼻用制剂的开发有一定的意义。
In this experiment, the nasal absorption characteristics of salvianolic acid B in rats were studied. A method for the determination of salvianolic acid B in the perfusate by HPLC was established. The irritation to the nasal cavity by different p H buffers of salvianolic acid B, Perfusate stability, and systematically studied the absorption of salvianolic acid B in the nasal mucosa. A modified rat nasal circulation model was used to assess the release of total protein and lactate dehydrogenase (LDH) in nasal perfusate. The effects of pH 4.0, 5.0, and 6.0 salvianolic acid B phosphate buffer on rats Nasal mucosa irritation and its stability in nasal perfusate, compared with low, medium and high concentration (200,400,800 mg · L-1) of pH 5.0 salvianolic acid B buffer salvianolic acid B rat nasal cavity Absorption characteristics. The results showed that nasal irritation: p H 4.0> p H 5.0> p H 6.0, p H 6.0 salvianolic acid B buffer within the change of RSD within 24 h was 3.1%, poor stability. Optimum irritation, pH 5.0 salvianolic acid B buffer with good stability and rat nasal perfusion test showed that nasal absorption of salvianolic acid B conforms to the first-order absorption model and is passive diffusion. The salvianolic acid B buffer of p H 5.0 is less irritating to the nasal cavity and has good stability. It is well absorbed in the rat nasal perfusion test and has certain significance for the development of the salvianolic acid B nasal preparation.