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In-situ gel injection of poloxamer-based metamizole provides long-acting antipyretic effects

Wang Yueli,Li Dongbo,Li Xiaojuan,Ren Dandan,Zhang Wei,Shu Gang,Lin Juchun,Li Haohuan,Xu Funeng,Peng Guangneng,Fu Hualin

Metamizole easily decomposes in the body and has a short action time and low bioavailability. Hence, frequent injection administrations are needed to maintain its plasma concentration. This study aimed to design and develop an in-situ gel based on poloxamer 407 and 188 to assess its long-acting antipyretic effects. The in-situ gel-forming systep00m with optimum sol–gel transition temperature of 35.9 °C to 36.3 °C could be formed using a combination of P407 at a ratio of 21–23% (w/v) and P188 at a ratio of 2–4% (w/v). In vitro erosion test showed that the in-situ gel’s erosion curve and the metamizole release rate both reached about 90% at 6 h, revealing a good linear relationship between the in-situ gel erosion and the drug release. In vitro release test with dialysis tube showed that the release of metamizole from the in-situ gel was remarkably slower than that from the metamizole solution. Approximately 85% of metamizole was released in the dialysis tube within 7 h, implying a good sustained release effect. Pharmacodynamic study showed that the in-situ gel injection extended the action time of metamizole relative to that when using the metamizole solution. Pharmacokinetic study revealed that the in-situ gel significantly increased the blood serum half-life and area under the curve), contributing to a sustained release and improved bioavailability. This study demonstrated that in-situ gel injection could prolong the action of metamizole in the body to reduce the number of administration times and has good clinical application. Graphical Abstract