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    • 3. 发明申请
    • Blockade of sodium channels by phenol derivatives
    • 苯酚衍生物阻断钠通道
    • US20040044084A1
    • 2004-03-04
    • US10416632
    • 2003-09-08
    • Gertrud HaeselerMartin Leuwer
    • A61K031/075A61K031/045
    • A61K8/498A61K8/347A61K8/4973A61K31/05A61K31/055A61K31/35A61K31/352A61K2800/28A61Q19/00
    • The invention relates to a pharmaceutical composition comprising at least one phenol derivative represented by formula (I) 1 wherein R1 represents a hydrogen atom, a halogen atom or a hydrocarbon group containing up to 12 carbon atoms; R2 represents a hydrogen atom or a C1-C7 alkyl group; wherein R1 and R2 may optionally form a carbocyclic 5- or 6-membered ring; R3 represents a hydrogen atom, a halogen atom or a C1-C7 alkyl group; R4 represents a hydrogen atom, a C1-C7 alkyl group or a halogen atom; R5 represents hydrogen atom, a halogen atom or a C1-C7 alkyl group; and R6 represents a hydrogen atom, a C1-C7 alkyl group or a C2 or C3 alkenyl group, under the proviso that R2 and R4 can only both represent a hydrogen atom if both R1 and R5 represent a C1-C7 alkyl group and R3 represents a halogen atom. The composition is particularly useful for the blockade of sodium channels and/or influencing the kinetics of sodium channels and thus can be used as local anesthetic, antidysrhythmic, anticonvulsant/antiepilepticand spasmolytic.
    • 本发明涉及包含至少一种由式(I)表示的苯酚衍生物的药物组合物,其中R 1表示氢原子,卤素原子或含有至多12个碳原子的烃基; R 2表示氢原子或C 1 -C 7烷基; 其中R 1和R 2可任选地形成碳环5或6元环; R 3表示氢原子,卤原子或C 1 -C 7烷基; R 4表示氢原子,C 1 -C 7烷基或卤素原子; R 5表示氢原子,卤素原子或C 1 -C 7烷基; 并且R 6表示氢原子,C 1 -C 7烷基或C 2或C 3烯基,条件是R 2和R 4只有两个R 2均表示氢原子, R 5表示C 1 -C 7烷基,R 3表示卤素原子。 该组合物特别可用于阻断钠通道和/或影响钠通道的动力学,因此可用作局部麻醉剂,抗心律失常药,抗惊厥药/抗癫痫药和解痉药。
    • 6. 发明申请
    • Sustained release of guaifenesin combination drugs
    • 愈创甘油联合药物的持续释放
    • US20030215508A1
    • 2003-11-20
    • US10413530
    • 2003-04-15
    • Robert D. DavisRalph W. BlumeDonald Jeffrey Keyser
    • A61K009/22A61K031/075
    • A61K9/2027A61K9/2054A61K9/209A61K9/5084A61K31/09A61K31/137A61K31/485A61K31/495A61K2300/00
    • The invention relates to a novel pharmaceutical modified release formulation of guaifenesin and dextromethorphan. The formulation may comprise a hydrophilic polymer, preferably a hydroxypropyl methylcellulose, and a water-insoluble polymer, preferably an acrylic resin, in a ratio range of about one-to-one (1:1) to about nine-to-one (9:1), more preferably a range of about three-to-two (3:2) to about six-to-one (6:1), and most preferably in a range of about two-to-one (2:1) to about four-to-one (4:1) by weight. This formulation capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject. The invention also relates to a modified release product which has two portions: a first portion having an immediate release formulation of guaifenesin and a second portion having a sustained release formulation of guaifenesin, wherein one or both portions further comprises dextromethorphan. The modified release product has a maximum guaifenesin serum concentration equivalent to that of an immediate release guaifenesin tablet, and is capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject.
    • 本发明涉及愈创甘油醚和右美沙芬的新型药物改良释放制剂。 制剂可包含亲水性聚合物,优选羟丙基甲基纤维素和水不溶性聚合物,优选丙烯酸树脂,其比例范围为约一对一(1:1)至约九对一(9 :1),更优选约三至二(3:2)至约六对一(6:1)的范围,最优选在约二至一(2:1)的范围内 )至约四对一(4:1)重量比。 该制剂能够在给予人受试者后至少十二个小时提供愈创甘油的治疗有效的生物利用度。 本发明还涉及一种具有两部分的改性释放产物:第一部分具有愈创甘油醚的立即释放制剂,第二部分具有愈创甘油醚的持续释放制剂,其中一个或两个部分还包含右美沙芬。 改性释放产物具有与立即释放愈创甘油醚片剂相当的最大愈创甘油醚血清浓度,并且能够在给予人受试者后至少十二个小时提供愈创甘油的治疗有效的生物利用度。