用于鼻腔给药的聚乙烯醇微粒。I. 通过喷雾干燥和喷雾去溶剂化制备

Microparticles of polyvinyl alcohol for nasal delivery. I. Generation by spray-drying and spray-desolvation.

作者信息

Ting T Y, Gonda I, Gipps E M

机构信息

Glaxo Australia Pty Ltd, Boronia, Victoria.

出版信息

Pharm Res. 1992 Oct;9(10):1330-5. doi: 10.1023/a:1015869704171.

DOI:10.1023/a:1015869704171

PMID:1448434

Abstract

Spray-drying and spray-desolvation are described for the generation of polyvinyl alcohol microparticles intended for nasal administration. The spray-dried microparticles of polyvinyl alcohol were of an appropriate size distribution but consisted of hollow spheres, which made them unsuitable for nasal delivery, as rapid clearance and a varied deposition pattern would be expected. Microparticles were also produced by spraying polyvinyl alcohol (average molecular weight of 14,000) solution (12.5%, w/v) at 0.332 ml/min onto the surface of acetone (spray-desolvation). These microparticles were solid collapsed spheres with the desired size for nasal deposition (10-200 microns). This method can be applied to encapsulation of drugs that are heat labile such as peptides and proteins.

摘要

描述了喷雾干燥和喷雾去溶剂化法用于制备用于鼻腔给药的聚乙烯醇微粒。喷雾干燥的聚乙烯醇微粒具有合适的粒径分布，但由空心球体组成，这使得它们不适合鼻腔给药，因为预期会有快速清除和不同的沉积模式。还通过以0.332 ml/min的速度将聚乙烯醇（平均分子量为14,000）溶液（12.5%，w/v）喷到丙酮表面（喷雾去溶剂化）来制备微粒。这些微粒是具有鼻腔沉积所需尺寸（10 - 200微米）的实心塌陷球体。该方法可应用于封装对热不稳定的药物，如肽和蛋白质。