目的 制備潑尼松脈沖片并考察其在體外的釋放特性。方法 采用粉末直接壓片法制備速釋片芯, 以羥丙甲纖維素(HPMC)為溶脹層包衣材料, 以乙基纖維素(EC)為控釋層包衣材料, 采用多層包衣技術(shù)制備潑尼松脈沖片?？疾炝酥驴讋㏄EG 400、增塑劑PEG 6000比例與用量以及控釋層包衣增重對釋放的影響。以遲滯時(shí)間和累積釋放度為指標(biāo), 考察潑尼松脈沖片的體外釋放特性。結(jié)果 以片芯崩解劑用量為11%, 致孔劑用量為10%, 增塑劑用量為1%, 溶脹層和控釋層包衣分別增重為5%、10.5%制備的潑尼松脈沖片效果最佳。按照最優(yōu)處方工藝制備的潑尼松脈沖片體外釋放遲滯時(shí)間為4 h, 時(shí)滯后0.5~1.0 h累積釋放度達(dá)95%以上。結(jié)論 潑尼松脈沖片處方組成合理, 工藝簡便可行, 體外釋放特性符合脈沖釋放設(shè)計(jì)要求。

Objective To prepare Prednisone Pulse-release Tablets and investigate the release characteristics in vitro. Methods Powder direct compression method was adopted to prepare quick-release tablets core. Multilayer coating were used to prepared Prednisone Pulse-release Tablets, in which hypromellose (HPMC) and ethyl cellulose (EC) were used as coating materials of the swelling layer and controlled release layer respectively. Effects of dosages and ratio of porogenic agent and plasticizer, and different weight on release were studied. Lag time and the accumulated amounts of release were used to evaluate the release characteristics in vitro. Results The optimized formulation and preparation of Prednisone Pulse-release Tablets were as following: the dosage was 11%, 10%, and 1% of the disintegrate, porogenic agent, and plasticizer. As well as, the coating weight obtained 5% and 10.5% of swelling layer and controlled release layer. The optimized lag time was 4 h and the accumulated amounts of release were more than 95% when the pulse-release time was between 0.5 h and 1.0 h. Conclusion The formulation of Prednisone Pulse-release Tablets is reasonable, the industrial arts is convenient and feasible, and the release characteristics in vitro is fit to the design of pulse-release.

天津市科技計(jì)劃項(xiàng)目(13ZXCXSY13600)