A method of increasing viscosity of a pharmaceutical formulation for oral or topical administration comprises the steps of combining:
a) an effective amount of one or more hydrophobic active ingredients;
b) 5 to 50% of one or more compounds selected from polyglycerol esters of fatty acids of formula (1)
CH2OR-CHOR-CH2O-[CH2CHOR-CH2O-]NCH2-CHOR-CH2OR (1)
wherein n is an integer from 4 to 13 and R is H or CO.R' wherein R' is C8-22 saturated, unsaturated or hydroxylated alkyl and wherein at least one group R is not hydrogen;
c) 5 to 50% of one or more compounds selected from polyglycerol esters of fatty acids and/or unsaturated fatty acids of formula (2).
CH2OR-CHOR-CH2O-[CH2CHOR-CH2O]NCH2-CHOR-CH2OR (2)
wherein n is an integer from 0 - 10 and R = H or CO.R" wherein R" is C8-22 saturated, unsaturated or hydroxylated alkyl, and wherein while at least one group R is not hydrogen;
d) 5 to 50% of one or more compounds selected from triglyceride macrogol glycerol esters, partial glycerides or fatty acids or macrogol esters of fatty acids in which the average quantity of reacted ethylene oxide in the synthesis of these substances ranges between 50 to 150 mols and concurrently the ratio between components b) and d) is from 0.1 : 1 to 10 : 1;
wherein the above percentages are selected to total 100%;
and wherein upon dilution with water 1:1 by volume the viscosity of the formulation increases by at least 5 times in comparison to the undiluted composition.
一种增加口服或局部用药的药物制剂粘度的方法包括以下步骤: 将以下物质结合起来:
a) 有效量的一种或多种疏
水性活性成分;
b) 5-50%的一种或多种选自式(1)
脂肪酸聚
甘油酯的化合物
ch2or-chor-ch2o-[ch2chor-ch2o-]nch2-chor-ch2or (1)
其中 n 为 4 至 13 的整数,R 为 H 或 CO.R',其中 R' 为 C8-22 饱和、不饱和或羟基烷基,且至少一个基团 R 不是氢;
c) 5-50%的一种或多种选自
脂肪酸和/或式(2)不饱和
脂肪酸的聚
甘油酯的化合物。
ch2or-chor-ch2o-[ch2chor-ch2o]nch2-chor-ch2or (2)
其中 n 为 0-10 的整数,R = H 或 CO.R",其中 R" 为 C8-22 饱和、不饱和或羟基烷基,且至少有一个基团 R 不是氢;
d) 5%至 50%的一种或多种选自
甘油三酯大环
甘油酯、部分
甘油酯或
脂肪酸或
脂肪酸 大环
甘油酯的化合物,其中合成这些物质时反应的
环氧乙烷的平均量为 50 至 150 摩尔,同时成分 b) 和 d) 之间的比例为 0.1 :1 至 10 : 1;
上述百分比总计为 100%;
用 1:1 体积比的
水稀释后,制剂的粘度比未稀释组合物至少增加 5 倍。