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    • 1. 发明申请
    • BUSINESS METHOD TO TREAT AND/OR PREVENT A GASTRIC ACID DISORDER WITH A PROTON PUMP INHIBITOR (PPI) AND A CHOLINERGIC AGONIST TO INDUCE RAPID ONSET OF PPI ACTION WITH OR WITHOUT FOOD
    • 使用原料泵抑制剂(PPI)和胆碱激素治疗和/或预防胃酸疾病的业务方法,以诱导或不用食物的PPI行动的快速上升
    • WO2008016887A2
    • 2008-02-07
    • PCT/US2007074772
    • 2007-07-30
    • GRACEWAY PHARMACEUTICALS LLCWOLFE M MICHAELBROWN LARRY RMANSO PETER J
    • WOLFE M MICHAELBROWN LARRY RMANSO PETER J
    • G06Q10/00
    • G06Q10/00G06Q50/22
    • Pharmaceutical proton pump inhibitor (PPI) medications and methods are disclosed for preventing and/or treating gastrointestinal disorders characterized by abnormalities in gastric acid secretion at anytime of the day or night without the need for food effect or to be taken with food. The medications comprise a PPI and a cholinergic agonist for inducing rapid onset of PPI action, for increasing the duration of PPI efficacy and for optimizing clinical PPI effectiveness that may be administered at any time of the day or night without food or on an empty stomach, and possibly on an as-needed or on demand basis, In carrying out the methods, a PPI and cholinergic agonist may be administered together as a single unitary dose in the form of a liquid or solid, or administered together, but separately as either liquids or solids or a combination thereof. Preferably, an oral solid dosage form of the present invention allows for release of a proton pump inhibitor at a pH of about 5 or higher, e.g., pH about 5.5, 6, 6.5 or 7, followed by release of a cholinergic agonist within between about 10 minutes and about 60 minutes, preferably within about 15 minutes and about 30 minutes, after release of the proton pump inhibitor from the dosage form, so that it can be adminisisterd at any time of the day or night independent of food or food effect. It is believed that the methods and compositions of the present invention will increase the duration of PPI efficacy by between at least about 5 fold and about 10 fold or even about 20 fold, as compared to the duration of PPI efficacy derived from current PPI dosage forms adminsitered alone and without food or a food effect. Kits comprising a PPI, a cholinergic agonist and optionally an antacid are disclosed, such as kits containing each drug in conventional and commercially available dry or liquid dosage forms for simultaneous or concomitant administration or in dry dosage forms to provide for the easy preparation of a liquid composition from the dry dosage forms. These new medications and methods will simplify the traditional continous PPI regimen and improve patient compliance.
    • 公开了药物质子泵抑制剂(PPI)药物和方法,用于预防和/或治疗以白天或夜间的任何时间胃酸分泌异常为特征的胃肠道疾病,而不需要食物作用或与食物一起服用。 药物包括PPI和用于诱导PPI作用的快速发作的胆碱能激动剂,用于增加PPI功效的持续时间和优化可在白天或晚上的任何时间没有食物或空腹时施用的临床PPI有效性, 并且可能在需要或按需的基础上。在进行该方法时,PPI和胆碱能激动剂可一起施用为液体或固体形式的单次单一剂量,或一起施用,但分别作为液体 或固体或其组合。 优选地,本发明的口服固体剂型允许质子泵抑制剂在pH约为5或更高,例如pH约5.5,6,6.5或7的情况下释放,随后将胆碱能激动剂释放在约 在质子泵抑制剂从剂型中释放出来之后10分钟和约60分钟,优选在约15分钟和约30分钟之内,使得它可以在白天或晚上的任何时间被独立于食物或食物效应管理。 据信本发明的方法和组合物将PPI效力的持续时间提高至少约5倍至约10倍或甚至约20倍,与从当前PPI剂型形成的PPI功效的持续时间相比较 单独管理,没有食物或食物的影响。 公开了包含PPI,胆碱能激动剂和任选的抗酸剂的试剂盒,例如用于同时或伴随给药的常规和市售干燥或液体剂型中的每种药物的试剂盒,或用于干燥剂型,以提供易于制备液体 干剂型的组成。 这些新的药物和方法将简化传统的连续PPI方案并改善患者的依从性。
    • 3. 发明申请
    • METHODS AND PACKAGES TO ENHANCE SAFETY WHEN USING IMIQUIMOD TO TREAT CHILDREN DIAGNOSED WITH SKIN DISORDERS
    • 当使用IMIQUIMOD治疗患有皮肤病的儿童时,加强安全的方法和包装
    • WO2008118765A1
    • 2008-10-02
    • PCT/US2008/057761
    • 2008-03-20
    • GRACEWAY PHARMACEUTICALS, LLCSLADE, Herbert, B.LEE, James, H.
    • SLADE, Herbert, B.LEE, James, H.
    • A01N43/42A61K31/44
    • A61K31/44
    • Pharmaceutical packages and methods for enhancing the safety of imiquimod when used to treat children affected by skin disorders are disclosed. More particularly, the safety profile of imiquimod use is enhanced by providing information to the children, guardians of the children, including parents and health care professionals, that systemic absorption of imiquimod and other effects may be observed when imiquimod therapy is used to treat children of between about 2 and about 12 years of age. Examples of systemic absorption include a serum imiquimod concentrations of less than about 2 ng/mL, a decrease in median white blood cell count by about 1.4*10 9 /L or a decrease in median absolute neutrophil count by about 1.42*10 9 /L. Topical and/or transdermal delivery of imiquimod, including creams, ointments, gels, lotions, salves and pressure- sensitive adhesive compositions to treat dermatological disorders in children, namely, molluscum contagiosum, viral infections, such as Type I or Type Il Herpes simplex infections and condyloma acuminata, genital warts and perianal warts, actinic keratosis and superficial basal cell carcinoma, and to induce interferon biosynthesis, are disclosed.
    • 公开了当用于治疗受皮肤病症影响的儿童时用于增强咪喹莫特安全性的药物包装和方法。 更特别地,通过向儿童,儿童的监护人,包括父母和保健专业人员提供信息来增强咪喹莫特使用的安全性,当咪喹莫特治疗用于治疗儿童时,可观察到咪喹莫特的全身吸收和其他作用 约2至约12岁。 全身吸收的实例包括小于约2ng / mL的血清咪喹莫特浓度,白细胞计数中位数降低约1.4×10 9 / L或中位绝对嗜中性粒细胞计数降低 约1.42×10 9 / L。 咪喹莫特的局部和/或透皮递送,包括霜剂,软膏,凝胶,洗剂,药膏和压敏粘合剂组合物,用于治疗儿童皮肤病,即传染性软疣,病毒感染如I型或II型单纯疱疹感染 和尖锐湿疣,生殖器疣和肛周疣,光化性角化病和浅表性基底细胞癌,并诱导干扰素生物合成。
    • 4. 发明申请
    • METHODS AND PACKAGES TO ENHANCE SAFETY WHEN USING IMIQUIMOD TO TREAT CHILDREN DIAGNOSED WITH SKIN DISORDERS
    • 使用IMIQUIMOD治疗患有皮肤疾病的儿童治疗儿童时的安全性的方法和包装
    • WO2008118762A9
    • 2011-01-06
    • PCT/US2008057758
    • 2008-03-20
    • GRACEWAY PHARMACEUTICALS LLCSLADE HERBERT BLEE JAMES H
    • SLADE HERBERT BLEE JAMES H
    • A01N43/42A61K31/44
    • A61K31/44
    • Pharmaceutical packages and methods for enhancing the safety of imiquimod when used to treat chiidren affected by skin disorders are disclosed. More particularly, the safety profile of imiquimod use is enhanced by providing information to the children, guardians of the children, including parents and health care professionals, that systemic absorption of imiquimod and other effects may be observed when imiquimod therapy is used to treat children of between about 2 and about 12 years of age. Examples of systemic absorption include a serum imiquimod concentrations of less than about 2 ng/mL, a decrease in median white blood cell count by about 1.4*109/L or a decrease in median absolute neutrophil count by about 1.42*109/L. Topical and/or transdermal delivery of imiquimod, including creams, ointments, gels, lotions, salves and pressure- sensitive adhesive compositions to treat dermatologica! disorders in children, namely, molluscum contagiosum, viral infections, such as Type I or Type Il Herpes simplex infections and condyloma acuminata, genital warts and perianal warts, actinic keratosis and superficial basal cell carcinoma, and to induce interferon biosynthesis, are disclosed.
    • 公开了用于增强咪喹莫特用于治疗受皮肤疾病影响的儿童的安全性的药物包装和方法。 更特别地,通过向儿童,儿童的监护人,包括父母和保健专业人员提供信息来增强咪喹莫特使用的安全性,当咪喹莫特治疗用于治疗儿童时,可观察到咪喹莫特的全身吸收和其他作用 约2至约12岁。 全身吸收的实例包括小于约2ng / mL的血清咪喹莫特浓度,白细胞计数中位数降低约1.4 * 109 / L或中位绝对嗜中性粒细胞计数降低约1.42 * 109 / L。 咪喹莫特的局部和/或透皮给药,包括霜剂,软膏,凝胶,洗剂,药膏和压敏胶粘剂组合物以治疗皮肤病! 公开了儿童疾病,即传染性软体动物,病毒感染,例如I型或II型单纯疱疹感染和尖锐湿疣,生殖器疣和肛周疣,光化性角化病和浅表性基底细胞癌,以及诱导干扰素生物合成。
    • 10. 发明申请
    • METHODS AND PACKAGES TO ENHANCE SAFETY WHEN USING IMIQUIMOD TO TREAT CHILDREN DIAGNOSED WITH SKIN DISORDERS
    • 当使用IMIQUIMOD治疗患有皮肤病的儿童时,加强安全的方法和包装
    • WO2008118762A1
    • 2008-10-02
    • PCT/US2008/057758
    • 2008-03-20
    • GRACEWAY PHARMACEUTICALS, LLCSLADE, Herbert, B.LEE, James, H.
    • SLADE, Herbert, B.LEE, James, H.
    • A01N43/42A61K31/44
    • A61K31/44
    • Pharmaceutical packages and methods for enhancing the safety of imiquimod when used to treat chiidren affected by skin disorders are disclosed. More particularly, the safety profile of imiquimod use is enhanced by providing information to the children, guardians of the children, including parents and health care professionals, that systemic absorption of imiquimod and other effects may be observed when imiquimod therapy is used to treat children of between about 2 and about 12 years of age. Examples of systemic absorption include a serum imiquimod concentrations of less than about 2 ng/mL, a decrease in median white blood cell count by about 1.4*10 9 /L or a decrease in median absolute neutrophil count by about 1.42*10 9 /L. Topical and/or transdermal delivery of imiquimod, including creams, ointments, gels, lotions, salves and pressure- sensitive adhesive compositions to treat dermatologica! disorders in children, namely, molluscum contagiosum, viral infections, such as Type I or Type Il Herpes simplex infections and condyloma acuminata, genital warts and perianal warts, actinic keratosis and superficial basal cell carcinoma, and to induce interferon biosynthesis, are disclosed.
    • 公开了用于增强咪喹莫特用于治疗受皮肤疾病影响的儿童的安全性的药物包装和方法。 更特别地,通过向儿童,儿童的监护人,包括父母和保健专业人员提供信息来增强咪喹莫特使用的安全性,当咪喹莫特治疗用于治疗儿童时,可观察到咪喹莫特的全身吸收和其他作用 约2至约12岁。 全身吸收的实例包括小于约2ng / mL的血清咪喹莫特浓度,白细胞计数中位数降低约1.4×10 9 / L或中位绝对嗜中性粒细胞计数降低 约1.42×10 9 / L。 局部和/或透皮给药咪喹莫特,包括霜剂,软膏,凝胶,洗剂,药膏和压敏胶粘剂组合物以治疗皮肤病! 公开了儿童疾病,即传染性软体动物,病毒感染,例如I型或II型单纯疱疹感染和尖锐湿疣,生殖器疣和肛周疣,光化性角化病和浅表性基底细胞癌,以及诱导干扰素生物合成。