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栓剂药物主要在直肠两个部位吸收:其一,经直肠上静脉吸收,由门静脉入肝,这和口服给药一样在肝脏代谢,对容易受首过效应的药物不利.其二由直肠下静脉吸收,药物不经过肝脏,可直接进入体循环,能避免药物首过效应.为了使栓剂药物能在直肠下部有效地被吸收,特设计了由栓剂药物(直肠内吸收分泌液形成凝胶,以抑制药物从直肠下部扩散至上部)及栓剂后端(含有药物)所组成的双层栓剂.由于栓剂前端必须在后端熔融前形成凝胶塞,因而首先筛选出膨润性好的前端处方.其基质配比为聚二乙醇4000四份、聚乙二醇1000九十六份,并加入
Suppository drugs are mainly absorbed in two parts of the rectum: First, the absorption through the upper rectum, from the portal vein into the liver, which is the same as oral administration in the liver metabolism, susceptible to the first pass effect of the drug adversely affected by the second under the rectal vein Absorption, the drug does not go through the liver, can be directly into the systemic circulation, to avoid the first pass effect of the drug in order to make the suppository drugs can be effectively absorbed in the lower rectum, specially designed by the suppository drug (rectal absorption of secretions to form a gel to inhibit Drug spread from the lower rectum to the upper part) and the suppository’s rear (containing drug) suppository.Because the suppository front end must be formed in the rear end of the melt before the gel plug, so first screened the swelling of the front prescription The matrix ratio is 4000 parts of polyethylene glycol, polyethylene glycol 1000 96 parts, and added