Drug Development and Industrial Pharmacy 2011-12-01

Preparation and evaluation of zolmitriptan submicron emulsion for rapid and effective nasal absorption in beagle dogs.

Chaoqun Yu, Pengfei Gu, Wenjun Zhang, Na Qi, Cuifang Cai, Haibing He, Xing Tang

文献索引：Drug Dev. Ind. Pharm. 37(12) , 1509-16, (2011)

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摘要

Submicron emulsion was prepared for rapid and effective nasal absorption of zolmitriptan (ZT). The different charge inducers and pH values of the formulations were evaluated to optimize the formulations. Submicron emulsion prepared by using stearylamine as positive charge inducer with pH of 5.0 was stable and most of ZT was freely dispersed in the aqueous phase of the preparation. In vitro release study demonstrated that ZT from the submicron emulsion preparation could be released as fast as that from the solution preparation. The pharmacokinetics was studied after intranasal administration of the submicron emulsion and solution preparation of ZT to beagle dogs. ZT from the submicron emulsion was absorbed much more rapidly and the absolute availability of the submicron emulsion preparation was significantly higher compared with the solution preparation. The nasal ciliotoxicity of the preparations was evaluated by using in situ toad palate model, which indicated that the submicron emulsion of ZT did not exhibit any obvious nasal ciliotoxicity. These results demonstrated that the submicron emulsion preparation of ZT was a relatively safe dosage form for rapid and effective intranasal delivery of ZT.