Preparation of levobupivacaine hydrochloride sustained-release in-situ gel injection and its pharmacokinetic and pharmacodynamic studies in animals
10.11665/j.issn.1000-5048.20150212
- VernacularTitle:盐酸左布比卡因原位凝胶注射剂的制备及其在动物体内的药代动力学和药效学
- Author:
Xinyong TONG
1
;
Limin LI
Author Information
1. 上海恒瑞医药有限公司
- Publication Type:Journal Article
- Keywords:
levobupivacaine hydrochloride;
in-situ gel;
sustained-release injection;
regional anesthesia
- From:
Journal of China Pharmaceutical University
2015;46(2):209-213
- CountryChina
- Language:Chinese
-
Abstract:
The purpose of this study was to develop a novel phospholipidas-based in-situ gel sustained-release formulation of levobupivacaine hydrochloride injection. Appropriate formulation was screened based on the factors such as phospholipid type, ratio of phospholipid to ethanol, ratio of water to phospholipid-ethanol mixture, which indicated typical in-situ gel profiles. Pharmacokinetic study using beagles showed that there were delayed tmax and prolonged t1/2 in levobupivacaine plasma-time profile after administration of the phospholipidas-based in-situ gel formulation if compared to commercially available conventional levobupivacaine hydrochloride injection. Pharmacodynamic studies conducted on guinea-pig demonstrated that it maintained 48-72 hr regional anesthesia, much longer than that of the anesthesia in the group receiving conventional injection. Hence, this novel in-situ gel intended for injection is worthy of development.
