Preparation and evaluation of naloxone hydrochloride nasal spray
10.13220/j.cnki.jipr.2017.06.028
- VernacularTitle:盐酸纳洛酮鼻腔喷雾剂的制备及评价
- Author:
Peng YANG
;
Wanqing LI
;
Ying LI
;
Jianxu SUN
;
Hui ZHANG
;
Jing GAO
;
Xiaoxing YIN
;
Aiping ZHENG
- Keywords:
naloxone hydrochloride;
nasal spray;
penetration enhancers;
ciliotoxicity;
pharmacokinetics
- From:
Journal of International Pharmaceutical Research
2017;44(6):616-621
- CountryChina
- Language:Chinese
-
Abstract:
Objective To prepare naloxone hydrochloride nasal spray and evaluate the ciliotoxicity and pharmacokinetics of the formulation. Methods The stability of naloxone hydrochloride was studied in pH3.5-5.5. Penetration promoting effects of absorp-tion enhancers on the naloxone hydrochloride were evaluated. Nasal ciliotoxicity studies were carried out using isolated toad palate. Rats were treated with naloxone hydrochloride solution by intramuscular injection of nasal drops to evaluate the pharmacokinetics. Results Naloxone hydrochloride solution was stable in pH3.5-5.5. Disodium ethylenediaminetetraacetic acid(0.2%,W/V)had the best penetration promoting effect on naloxone hydrochloride. Naloxone hydrochloride nasal spray did not exhibit obvious nasal ciliotox-icity compared to the negative control. The nasal spray had a faster therapeutic effect and its bioavailability was similar to that of the in-tramuscular injection. Conclusion Naloxone hydrochloride nasal spray prepared in this research is stable with no obvious nasal cilio-toxicity,has faster therapeutic effect,and good bioavailability,so may have a broad application prospect.
