盐酸普萘洛尔脉冲释放片的制备及其体外释药研究

Development of Propranolol Hydrochloride Pulsatile Release Tablets and in Vitro Release Characterization

关键词:  盐酸普萘洛尔  脉冲释放  羟丙甲纤维素  丙烯酸树脂

Key words:  propranolol hydrochloride  pulsatile release  HPMC  eudragit

摘要:

目的 制备盐酸普萘洛尔双层包衣脉冲释放片，并研究其体外释药行为。方法 采用粉末直接压片法制备盐酸普萘洛尔片芯，滚转包衣锅法分别包羟丙甲纤维素溶胀层和丙烯酸树脂控释层。采用体外溶出试验考察处方及溶出条件对本品释药行为的影响。结果 本品经过一定时滞后以脉冲形式释药，渗透活性物质氯化钠、溶胀层及控释层厚度、丙烯酸树脂RS/RL的配比均影响本品时滞。溶出方法及不同pH溶出介质对本产品的时滞无影响。结论 盐酸普萘洛尔脉冲释放片具有脉冲释放特性，体外时滞约为4 h。

Abstract:

OBJECTIVE To prepare propranolol hydrochloride bi-layered pulsatile release tablets, and study the drug release properties of the tablets. METHODS Propranolol hydrochloride core tablets were prepared by direct compression and spray-coated with HPMC E5 swelling layer and eudragit polymeric layer subsequently. The effects of formulation and dissolution methods on the in vitro release profiles of the tablets were studied using in vitro dissolution test. RESULTS Propranolol hydrochloride released from the tablet in pulsatile behavior after a certain lag time. The osmotically active substance sodium chloride, the thickness of the swelling layer and the polymeric layer, and the ratio of Eudragit RS/RL all had effects on the lag time. Dissolution method and the pH of dissolution medium had no influence on the lag time. CONCLUSION The propranolol hydrochloride pulsatile release tablets have pulsatile release characteristics with lag time of about 4 h.