羟吗啡酮的鼻内吸收

Intranasal absorption of oxymorphone.

作者信息

Hussain M A, Aungst B J

机构信息

The DuPont Merck Pharmaceutical Company, Pharmaceutical R&D, Wilmington, DE 19880-0400, USA.

出版信息

J Pharm Sci. 1997 Aug;86(8):975-6. doi: 10.1021/js960513x.

DOI:10.1021/js960513x

PMID:9269879

Abstract

The nasal bioavailability of oxymorphone HCI was determined. Rats were surgically prepared to isolate the nasal cavity, into which a solution of oxymorphone was administered. A reference group of rats was administered oxymorphone HCl intravenously. Plasma oxymorphone concentrations were determined by HPLC. Nasal absorption was rapid, nasal bioavailability was 43%, and the iv and nasal elimination profiles were similar. Oxymorphone HCI appears to have the solubility, potency, and absorption properties required for efficient nasal delivery, which is an alternative to injections.

摘要

测定了盐酸羟吗啡酮的鼻腔生物利用度。对大鼠进行手术以分离鼻腔，并向其中给药盐酸羟吗啡酮溶液。另一组作为参照的大鼠通过静脉注射给予盐酸羟吗啡酮。通过高效液相色谱法测定血浆中盐酸羟吗啡酮的浓度。鼻腔吸收迅速，鼻腔生物利用度为43%，静脉注射和鼻腔给药后的消除曲线相似。盐酸羟吗啡酮似乎具有高效鼻腔给药所需的溶解性、效力和吸收特性，这是注射给药的一种替代方式。