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发明授权
CN101716134B 2-甲氧基雌二醇透皮搽剂和贴剂 失效 - 权利终止

2-甲氧基雌二醇透皮搽剂和贴剂
摘要：
本发明涉及2-甲氧基雌二醇透皮搽剂和贴剂，有效解决2-甲氧基雌二醇口服剂的水溶性差，疗效差，有肝脏首过效应，体内分布广泛的问题，其方法是，本发明由2-甲氧基雌二醇透皮搽剂和2-甲氧基雌二醇透皮贴剂两种剂型，2-甲氧基雌二醇透皮搽剂是由以质量百分比计的：基本载体74％-98％、2-甲氧基雌二醇0.5％-2％和促进剂1-25％，总量为100％制成，或以质量百分比计的：基本载体74％-98％、2-甲氧基雌二醇0.5％-2％、促进剂1-25％和羟丙甲基纤维素0.5％-2％，总量为100％制成2-甲氧基雌二醇透皮贴剂，本发明使用方便，通过局部透皮可使药物直达病灶，可使病灶长时间维持较高的治疗浓度，从而提高疗效，避免了肝脏的首过效应和全身分布，是医学上的创新。
摘要（英）：

The invention relates to a 2-methoxyestradiol transdermal liniment and a 2-methoxyestradiol transdermal patch, effectively solving the problems of poor water-solubility, poor curative effect, the existence of liver first-pass effect, wide distribution in vivo of a 2-methoxyestradiol oral agent. The invention comprises two agent types of the 2-methoxyestradiol transdermal liniment and the 2-methoxyestradiol transdermal patch, wherein the 2-methoxyestradiol transdermal liniment comprises the following components in percentage by weight relative to total does of 100 percent: 74-98 percent of basic carrier, 0.5-2 percent of 2-methoxyestradiol and 1-25 percent of accelerant; and the 2-methoxyestradiol transdermal patch comprises the following components in percentage by weight relative to the total dose of 100 percent: 74-98 percent of basic carrier, 0.5-2 percent of 2-methoxyestradiol, 1-25 percent of accelerant, and 0.5-2 percent of hydroxypropylmethyl cellulose. The invention is convenient to use, enables the medicines to reach nidus directly through local transdermal permeation and enable the nidus to maintain higher curative concentration for a long time, thereby enhancing curative effect and avoiding liver first-pass effect and whole body distribution. The invention is an innovation in medicine.

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