盐酸纳洛酮口腔速溶膜的制备及其体外释放研究

Preparation and in Vitro Release of Naloxone Hdrochloride Orodispersible Film

目的:制备盐酸纳洛酮口腔速溶膜(naloxone hydrochloride orodispersible film,NXH-ODF),并考察其体外溶出行为。方法:采用溶剂浇铸法制备NXH-ODF,以膜剂外观、厚度和崩解时间为评价指标,采用单因素试验法筛选成膜材料、增塑剂、表面活性剂及崩解剂的种类和用量,并对最优处方制备的NXH-ODF进行含量均匀度及体外释放度考察。结果:以最优处方NXH(1.8%)、羟丙甲基纤维素E30(63.9%)、丙二醇(24.8%)、羧甲基淀粉钠(3.6%)、吐温80(3.6%)、阿司帕坦(1.8%)和柠檬黄(0.5%)制备的NXH-ODF能在40 s内崩解,含量均匀度符合规定(A+2.2S<15.0),药物在10 min时的累积释放度达到(97.44±2.28)%。结论:制备的NXH-ODF外观平整光滑,崩解迅速,体外释放度良好。

OBJECTIVE:To prepare naloxone hydrochloride orodispersible film(NXH-ODF)and investigate dissolution behaviors in vitro.METHODS:Solvent casting method was applied to prepare the NXH-ODF,with film appearance,thickness and disintegration time as evaluation indexes.The type and dosage of NXH-ODF film-forming materials,plasticizers,surfactants and disintegrants were screened by single factor experiments.The content uniformity and in vitro release of NXH-ODF prepared with the best prescription were investigated.RESULTS:The NXH-ODF prepared by optimal formulation(NXH 1.8%,HPMC-E3063.9%,propylene glycol 24.8%,CMS-Na 3.6%,tween 803.6%,aspartame 1.8%,lemon yellow 0.5%)could disintegrate within 40 s,the conformity of drug content was up to the standard(A+2.2S<15.0),and the cumulative release in vitro at 10 min reached(97.44±2.28)%.CONCLUSIONS:The prepared NXH-ODF has smooth appearance,rapid disintegration and significant in vitro release.