鲑降钙素经鼻干粉吸入剂的制备及评价

Preparation and Evaluation of Salcatonin Nasal Dry Powder Inhalation

采用冷冻干燥法制备鲑降钙素生物黏附附聚物,研究表面活性剂泊洛沙姆用量对容器吸附降钙素的作用;用改进的Twin-impinger进行体外模拟试验,并测定家兔静脉和经鼻腔给药后的血钙降低情况。结果表明,当泊洛沙姆188浓度为0.25%时,具良好的抗容器吸附主药能力,与溶液型喷雾剂和胶囊干粉吹入剂相比,主动吸入的泡囊型干粉吸入剂较溶液型喷雾剂更易在具治疗意义的部位沉积;家兔试验表明,鼻腔给药后,其降血钙作用相当于静注给药的72%,达峰时间为3.5h(静注为1.5h),作用时间可持续约10h(静注约为7h)。

Freezing dried method was used to prepare salcatonin bio-adhesive aggregate. The effect of amount of surfactant Poloxamer F68 in formulation to inhibit the adsorption of salcatonin on container was investigated. The improved Twin-impinger was used to imitate the nasal inhalation of salcatonin dry powder in vitro. The effects of reducing of blood calcium between intranasal and intravenous routes in rabbit were compared. The results showed that the concentration of F68 at 0.25 % demonstrated a stronger inhibition effect on adsorption of calcitonin to container, and the deposition of the powder inhalation in effective area was more than those of the powder insufflation and liquid spray. The reduction of blood calcium by nasal inhalation was equivalent to 72 % by iv, Cmax was 3.5h （iv： 1.5h）, and the effect lasted about 1Oh （iv： 7h）.