采用单因素法筛选了盐酸氟西汀肠溶片片芯、隔离层包衣液和肠溶衣包衣液的处方。结果表明，片芯中的关键辅料羟丙甲纤维素 E50、羧甲淀粉钠和微晶纤维素的用量分别为5％、15％和25％，黏合剂宜采用5％淀粉浆。以5％欧巴代Y-1-7000 水分散体对所得片芯包隔离衣层，增重为1％，再以5％聚丙烯酸树脂L30D-55( 含5％单硬脂酸甘油酯和1％甘露醇) 包肠溶衣层，增重为3％。所得制品在0.1 mol/L 盐酸中2 h 累积释放率≤ 5％，在pH 6.8 缓冲液中30 min 释放完全。3 批制品的体外释放曲线均与参比制剂(Prozac Weekly 胶囊) 相似，相似因子(f2) 均大于50。
Abstract
The formulations of tablet core, isolating layer and enteric layer coating solution for fluoxetine hydrochloride enteric tablets were optimized by single factor test. The results showed that the amount of three key excipients (hydroxypropyl methyl cellulose E50, sodium carboxymethyl starch and microcrystalline cellulose) in the tablet core were 5％, 15％ and 25％, respectively. The adhesive for tablet core was 5％ starch slurry. The isolating layer was coated by 5％ Opadry Y-1-7000 aqueous dispersion with the coating level of 1％. Then the enteric layer was coated by 5％ polyacrylic resin L30-55 (containing 5％ glycerin monostearate and 1％ mannitol) with the level of 3％. The cumulative release at 2 h of the product in 0.1 mol/L HCl was less than or equal to 5％, while the drug could completely release in the pH 6.8 buffer within 30 min. The in vitro release curves of three batches of the product were all similar to the reference preparation (Prozac Weekly capsules). The similarity factors (f2) between three batches of the product and reference capsules were all over 50.
关键词
盐酸氟西汀 /
抗抑郁药 /
肠溶片 /
制备 /
体外释放
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Key words
fluoxetine hydrochloride /
antidepressant drug /
enteric tablet /
preparation /
in vitro release
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参考文献
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