摘要
采用一步制丸和薄膜包衣工艺研制了盐酸普萘洛尔控释微丸（Ｐｒｏｐｒａｎｏｌｏｌｃｏｎｔｒｏｌｌｅｄ－ｒｅｌｅａｓｅｐｅｌｌｅｔｓ，ＰＣＰ），体外释药符合双相零级动力学过程，释药速率常数分别为Ｋ＿（ｐ１）＝１１．１３％／ｂ（０≤ｔ≤７）和Ｋ＿（ｐ２）＝３．７３％／ｈ（７＜ｔ≤１２），在ｐＨ２．２～５．６之间释药行为不变。与国外同类产品ＩｎｄｅｒａｌＬＡ的体内外数据均无显著性差异（Ｐ＞０．０５），ＰＣＰ在模似胃肠体液中的体外累积释药百分率与其体内吸收百分率之间有显著相关性，相关方程Ｆ（ｔ）＝２．００５Ａ（ｔ）－９．３９（ｒ＝０．９９５６）。
Propranolol controlled-release pellets (PCP) were developed by means of the one-step spheronization and pan-coating technique. The dissolution behavior of PCP was examined using the rotary basket method. The accumulative dissolution amount/time profile could be described by′two-phase Zero-order kinetics and dissolution rate constants were found to be 11.13%/h (0≤t≤7) and 3. 73%/h (7<t≤12) in two phases respectively. There were no significant difference in vitro and in vivo tests (P>0. 05) between PCP and one commercial extended-release propranolol capsule which named Inderal LA in trade mark. The effective therapeutic plasma level was prolonged to a large extent for PCP. The absorption rate constant of PCP in vivo was 18. 49%/h which would be related gression equation (F(t)=2.005A (t)-9.39,r=0.9956).
出处
《中国药科大学学报》
CAS
CSCD
北大核心
1994年第2期83-87,共5页
Journal of China Pharmaceutical University
关键词
盐酸普萘洛尔
控释制剂
微丸
Propranolol hydrochloride
Controlled-release system
Pellets
