蒋新国, 张奇志, 张奕, 奚念朱. 普萘洛尔鼻用制剂的纤毛毒性J. 药学学报, 1999, 34(6): 471-474.
引用本文: 蒋新国, 张奇志, 张奕, 奚念朱. 普萘洛尔鼻用制剂的纤毛毒性J. 药学学报, 1999, 34(6): 471-474.
Jiang Xinguo Zhang Qizhi, Zhang Yi , Xi Nianzhu, . CILIOTOXICITY OF PROPRANOLOL PREPARATIONS FOR INTRANASAL ADMINISTRATIONJ. Acta Pharmaceutica Sinica, 1999, 34(6): 471-474.
Citation: Jiang Xinguo Zhang Qizhi, Zhang Yi , Xi Nianzhu, . CILIOTOXICITY OF PROPRANOLOL PREPARATIONS FOR INTRANASAL ADMINISTRATIONJ. Acta Pharmaceutica Sinica, 1999, 34(6): 471-474.

普萘洛尔鼻用制剂的纤毛毒性

CILIOTOXICITY OF PROPRANOLOL PREPARATIONS FOR INTRANASAL ADMINISTRATION

  • 摘要: 目的:筛选一种合适的剂型以降低鼻用制剂的鼻纤毛毒性。方法:以盐酸普萘洛尔为模型药物,分别制备微球剂、复合乳剂和环糊精包合物。以在体蟾蜍上腭粘膜纤毛为动物模型,评价上述鼻用制剂对盐酸普萘洛尔纤毛毒性的改善作用。结果:微球剂能有效地降低盐酸普萘洛尔的纤毛毒性;复合乳剂因包裹率较低,而环糊精因与药物的结合常数较小,使这2种制剂对纤毛毒性均无明显的改善作用。结论:微球剂是降低药物鼻纤毛毒性的一种较为理想的剂型,机理主要是它的缓释作用。

     

    Abstract: AIM: To screen a suitable dosage form for reducing ciliotoxicity of intranasal preparations. METHODS: Propranolol hydrochloride (PRO) was selected as a model drug and microspheres, multiple-emulsions and cyclodextrin inclusions for intranasal administration were prepared. The effect of the above preparations on ciliary movement was evaluated with in situ toad palate model. RESULTS: The microspheres were shown to be able to reduce the ciliotoxicity of PRO, but multiple-emulsions and cyclodextrin inclusions in this research were found to be inefficient because the embedding rate of the multiple-emulsions was low and the binding constant between PRO and cyclodextrin was small. CONCLUSION: The microspheres are an ideal dosage form for reducing ciliotoxicity and the involved mechanism is the sustained release effect of the microspheres.

     

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