Preparation of levobupivacaine hydrochloride sustained-release <i>in-situ </i>gel injection and its pharmacokinetic and pharmacodynamic studies in animals

TONG Xinyong; LI Limin

doi:10.11665/j.issn.1000-5048.20150212

Journal of China Pharmaceutical University > 2015 > 46(2): 209-213. > DOI: 10.11665/j.issn.1000-5048.20150212

TONG Xinyong, LI Limin. Preparation of levobupivacaine hydrochloride sustained-release in-situ gel injection and its pharmacokinetic and pharmacodynamic studies in animals[J]. Journal of China Pharmaceutical University, 2015, 46(2): 209-213. DOI: 10.11665/j.issn.1000-5048.20150212

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Preparation of levobupivacaine hydrochloride sustained-release in-situ gel injection and its pharmacokinetic and pharmacodynamic studies in animals

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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 t_1/2 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.
- levobupivacaine hydrochloride,
- in-situ gel,
- sustained-release injection,
- regional anesthesia

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Preparation of levobupivacaine hydrochloride sustained-release in-situ gel injection and its pharmacokinetic and pharmacodynamic studies in animals

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