Abstract: Provided are a long-acting ropivacaine pharmaceutical composition, a preparation method therefor and use thereof. The pharmaceutical composition comprises: ropivacaine; a pharmaceutical solvent; a pharmaceutical phospholipid; a pharmaceutical oil; and an efficacy enhancer, an optional antioxidant and an optional acid-base regulator. The pharmaceutical composition has a controllable release behavior and a sustained release effect, can significantly reduce the peak plasma concentration of the drug, maintain a stable plasma concentration in the body, prolong the effective treatment time, reduce the effective therapeutic dose, improve the utilization of the drug, and reduce the risk of neurotoxicity. The pharmaceutical composition has a long-acting analgesic effect and can be used for pain treatment.

Abstract: A non-aqueous sustained release drug delivery system, which contains, based on the total weight of the sustained release drug delivery system, about 0.1-20% of an active agent, about 0.5-50% of a drug solvent, about 1-98% of a drug sustained release agent, about 0.1-85% of a drug solubilizer, about 0.1-10% of an efficacy enhancer, about 0-1% of an antioxidant, and about 0-8% of an acid-base regulator. The non-aqueous sustained release drug delivery system can yield an improved sustained release effect, improve bioavailability, and enhance the therapeutic effect.