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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。
OBJECTIVE: To screen a suitable dosage form to reduce nasal cilia toxicity in nasal preparations. Methods: Propranolol hydrochloride was used as model drug to prepare microsphere, composite emulsion and cyclodextrin inclusion compound respectively. In vivo toad palate mucosal cilia animal model, to evaluate the above nasal preparations of propranolol hydrochloride cork to improve the role of toxicity. Results: The microspheres could effectively reduce the ciliary toxicity of propranolol hydrochloride. The lower the encapsulation efficiency of the composite emulsion and the smaller the binding constant of the cyclodextrin to the drug, the two formulations had no obvious ciliary toxicity The improvement effect. Conclusion: Microsphere is an ideal dosage form to reduce the toxicity of nasal ciliates. Its mechanism is mainly its sustained release.