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由于栓剂剂型的特点,药物的粒径在栓剂中有特殊的作用。药物粒径的作用取决于药物的水溶解度。前曾发现,粒径从250～300μm 减少至63～90μm 时,可使水易溶的药物的体外释放速率常数减少21～30%;但对难溶、微溶和几不溶性药物则无影响。本文选择不同溶解度的三种药物:易溶性药物苯巴比妥钠(1960mmol/l),难溶性药物茶碱(68.2mmol/l)和微溶性药物苯巴比妥(3.92mmol/l),分别为63～90,120～160和250～300μm 的粒径,以WitepsolH15作基质,用熔融法制成0.60±5%g 的栓剂,研究其粒径对生物利用度的影响。实验采用2.5～3.0kg 家兔。6只一组。剂量茶碱为200 mg/kg、苯巴比妥20 mg/kg、苯巴比妥钠22mg/kg。在给药后的0.25、1、2、3、
Because of the characteristics of suppository formulations, the particle size of the drug has a special effect in suppositories. The effect of drug particle size depends on the water solubility of the drug. It was previously found that reducing the particle size from 250 to 300 μm to 63 to 90 μm decreased the rate constant for in vitro release of water-soluble drugs by 21 to 30%, but had no effect on poorly soluble, sparingly soluble, and insoluble drugs. In this paper, we choose three drugs with different solubility: phenobarbital (1960mmol / l), poorly soluble theophylline (68.2mmol / l) and slightly soluble drug phenobarbital (3.92mmol / l) The particle sizes of 63 ~ 90, 120 ~ 160 and 250 ~ 300μm were studied. The effect of particle size on the bioavailability was studied by using the Witepsol H15 as matrix and the suppository of 0.60 ± 5% g by melt method. Experimental 2.5 ~ 3.0kg rabbits. 6 only one group. The dose of theophylline was 200 mg / kg, phenobarbital 20 mg / kg and phenobarbital 22 mg / kg. After administration of 0.25, 1, 2, 3,