乌苯美司胶囊的处方配比与制备工艺的研究
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摘要
目的:研究适合乌苯美司胶囊的处方配比和制备工艺。方法:拟定4种处方(处方-1,处方-2,处方-3和处方-4)成分,并对各处方的装量、流动性、累积溶出百分比与原研药(Bestatin)进行实验,比较其差异,筛选与优化。结果:拟定的处方-4每粒含乌苯美司10 mg,淀粉191 mg,蔗糖硬脂酸酯4.4 mg(外加),十二烷基硫酸钠(SDS)2.2 mg(内加),淀粉浆10%,硬脂酸镁1.76 mg;其水中在15 min累积溶出百分比大于85%。结论:与对照品各指标的比较,处方-4各成分用量的拟合较为合理。
Objective: To study the optimization on formulation and process of ubenimex capsules. Methods: Designing 4 kinds of formulation for ubenimex capsules(formulation-1, formulation-2, formulation-3 and formulation-4),then selecting this formulation by comparing the costume quantity, flowability and dissolution of one formulation with the original drug(Bestatin). Results: Finally, the more reasonable one is the formulation- 4(1 granule), for example Ubenimex is 10 mg, starch is 191 mg, sucrose stearate is 4.4 mg(add out), SDS is 2.2 mg(add in), starch paste is 10%and magneslum stearat is 1.76 mg. The cumulative dissolution percentage in the water in 15 min is greater than 85%.Conclusion: The No 4 formulation is more reasonable by comparing with reference.
Objective: To study the optimization on formulation and process of ubenimex capsules. Methods: Designing 4 kinds of formulation for ubenimex capsules(formulation-1, formulation-2, formulation-3 and formulation-4),then selecting this formulation by comparing the costume quantity, flowability and dissolution of one formulation with the original drug(Bestatin). Results: Finally, the more reasonable one is the formulation- 4(1 granule), for example Ubenimex is 10 mg, starch is 191 mg, sucrose stearate is 4.4 mg(add out), SDS is 2.2 mg(add in), starch paste is 10%and magneslum stearat is 1.76 mg. The cumulative dissolution percentage in the water in 15 min is greater than 85%.Conclusion: The No 4 formulation is more reasonable by comparing with reference.
引文
[1]Umezawa H,Aoyagi T,Suda H,et al.Bestatin,an inhibitor of aminopeptidase B,produced by actinomycetes[J].J Antibiotics,1976,29(1):97-99.
[2]Ino K,Goto S,Okamoto T,et al.Expression of amiopeptidase N on human choriocarcinoma cells and cell growth suppression by the inhibition of aminopeptidase N activity[J].Cancer Science,1994,85(9):927-933.
[3]Sakurada K,Imamura M,Kobayashi M,et al.Inhibitory effect of Bestatin on the growth of human leukemic cells[J].Acta Oncol,1990,29(6):799-802.
[4]Schorlemmer HU,Bosslet K,Sedlacek HH.Ability of the immunomodulating dipeptide Bestatin to activate cytoxicmono nuclear phagocytes[J].Cancer Res,1983,43(9):4148-4153.
[5]Ezawa K,Minato K,Dobashi K.Induction of apoptosis by ubenimex(Bestatin)in human non-small-cell lung cancer cell lines[J].Biomed Phamacother,1996,50(67):283-289.
[6]Sehine K,Fujii H,Abe F.Induction of apoptosis by Bestatin(ubenimex)in human an leukemic cell lines[J].Leukemia,1999,13(5):729-734.
[7]周善学,艾琳.乌苯美司应用研究进展[J].国外医药:抗生素分册,1997,18(004):304-307.
[8]夏锦辉,刘昌孝.固体药物制剂的体外溶出度的统计学评价分析[J].中国药学杂志,2000,35(2):130-131.
[9]邓亚利,黄泓,唐继红,等.琥乙红霉素胶囊处方工艺研究及溶出度测定[J].西北药学杂志,2004,19(3):115-116.
[2]Ino K,Goto S,Okamoto T,et al.Expression of amiopeptidase N on human choriocarcinoma cells and cell growth suppression by the inhibition of aminopeptidase N activity[J].Cancer Science,1994,85(9):927-933.
[3]Sakurada K,Imamura M,Kobayashi M,et al.Inhibitory effect of Bestatin on the growth of human leukemic cells[J].Acta Oncol,1990,29(6):799-802.
[4]Schorlemmer HU,Bosslet K,Sedlacek HH.Ability of the immunomodulating dipeptide Bestatin to activate cytoxicmono nuclear phagocytes[J].Cancer Res,1983,43(9):4148-4153.
[5]Ezawa K,Minato K,Dobashi K.Induction of apoptosis by ubenimex(Bestatin)in human non-small-cell lung cancer cell lines[J].Biomed Phamacother,1996,50(67):283-289.
[6]Sehine K,Fujii H,Abe F.Induction of apoptosis by Bestatin(ubenimex)in human an leukemic cell lines[J].Leukemia,1999,13(5):729-734.
[7]周善学,艾琳.乌苯美司应用研究进展[J].国外医药:抗生素分册,1997,18(004):304-307.
[8]夏锦辉,刘昌孝.固体药物制剂的体外溶出度的统计学评价分析[J].中国药学杂志,2000,35(2):130-131.
[9]邓亚利,黄泓,唐继红,等.琥乙红霉素胶囊处方工艺研究及溶出度测定[J].西北药学杂志,2004,19(3):115-116.