Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Local anesthetic effect and safety of ropivacaine oily solution

Wudang M Lu¹, Tong Yao¹, Minquan Hui², Jingliang Gu³, Manli Wu¹, Liqiang Zhou³, Yi Yang², Lei Cao¹, Yongxiao Cao¹

¹School of Basic Medical Sciences, Xi’an Jiaotong University Health Science Center, Xi’an, Shannxi 710061, China; ²Xi’an Libang Pharmaceutical Co. Ltd, Xi’an, Shaanxi 710077, China; ³JOINN Laboratories Co. Ltd, Suzhou, Jiangsu 215400, China.

For correspondence:- Yongxiao Cao Email: yxy@xjtu.edu.cn Tel:+862982655140

Accepted: 28 November 2023 Published: 31 December 2023

Citation: Lu WM, Yao T, Hui M, Gu J, Wu M, Zhou L, et al. Local anesthetic effect and safety of ropivacaine oily solution. Trop J Pharm Res 2023; 22(12):2449-2457 doi: 10.4314/tjpr.v22i12.5

© 2023 The authors.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..

Abstract

Purpose: To investigate the effectiveness and safety of ropivacaine oily solution (ROPOS).

Methods: After effecting nerve block in postoperative rats by injection of ROPOS near the sciatic nerve, the expression levels of sodium-potassium-chloride co-transporter 1 (NKCC1) and potassium-chloride co-transporter 2 (KCC 2) in the spinal dorsal horn, were assayed. The safety of ROPOS in beagle dogs was evaluated through subcutaneous injection.

Results: The duration of anesthetic effect of ROPOS was 5 times longer than that of ropivacaine hydrochloride injection. The analgesic effect occurred via downregulation of the expression of NKCC1. Dogs administered ROPOS had acute inflammatory reactions at the injection sites within 3 days, but they recovered after 14 days. No other toxic reactions were observed. The T_max values for dogs subcutaneously injected with ROPOS at doses of 15, 30 and 60 mg/kg were 2.15 ± 3.09, 6.25 ± 9.62 and 14.85 ± 11.82 h; with the C_max values of 0.78 ± 0.51, 1.35 ± 0.38 and 2.09 ± 0.53 µg/mL, while the AUC_(0-48h) values were 15.88 ± 5.41, 31.46 ± 11.45 and 66.10 ± 17.81 h·µg/mL, respectively. The values of T_max, C_max and AUC_(0-48h) were positively correlated with ROPOS dose.

Conclusion: Ropivacaine oily solution has a longer duration of local anesthetic effect than ropivacaine hydrochloride injection and it also possesses a good safety profile. The acute inflammatory reactions are noteworthy and will be further investigated in subsequent studies.

Keywords: Ropivacaine oily solution, Local anesthesia, Rats, Safety evaluation, Beagle dogs