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    • 44. 发明申请
    • ANTI-MISUSE MICROPARTICULATE ORAL DRUG FORM
    • 抗微生物口服药物形式
    • US20100266701A1
    • 2010-10-21
    • US12560044
    • 2009-09-15
    • Florence GuimberteauRemi MeyrueixGerard Soula
    • Florence GuimberteauRemi MeyrueixGerard Soula
    • A61K9/14A61K31/52A61K31/155
    • A61K9/5047A61K9/5078A61K31/196A61K31/522
    • The invention relates to solid microparticulate oral dosage forms having a composition that prevents the misuse of the active pharmaceutical ingredient (API) contained therein. The aim of the invention is to prevent the improper use of solid oral drugs for any use other than the therapeutic use(s) officially approved by the appropriate public health authorities. Another aim of the invention is to provide novel analgesic drugs which can be used to: prevent the misuse of, and addiction to certain analgesics and/or to control plasma concentration variability and/or to facilitate oral; administration; and/or to combine analgesics with one another and/or with one or more active ingredients in the same oral form. More specifically, the invention relates to a solid oral drug form comprising anti-misuse means and at least one active ingredient, which is characterized in that: at least part of the active ingredient is contained in microparticles; and the anti-misuse means comprise anti-crushing means (a) which enable the microparticles of the active ingredient to resist crushing, such as to prevent the misuse thereof. According to the invention, the drug form can also comprise means (b) for preventing the misuse of the active ingredient following a possible liquid extraction process.
    • 本发明涉及具有防止滥用其中所含的活性药物成分(API)的组合物的固体微粒口服剂型。 本发明的目的是防止不适当地使用固体口服药物以用于由适当的公共卫生当局正式批准的治疗用途以外的任何用途。 本发明的另一个目的是提供新的止痛药,其可用于:防止某些止痛剂的滥用和成瘾和/或控制血浆浓度变异性和/或促进口服; 行政; 和/或将镇痛药彼此和/或以相同口服形式的一种或多种活性成分组合。 更具体地,本发明涉及包含抗滥用手段和至少一种活性成分的固体口服药物形式,其特征在于:至少部分活性成分包含在微粒中; 并且防误用手段包括能够使活性成分的微粒抵抗破碎的抗破碎装置(a),以防止其误用。 根据本发明,药物形式还可以包括用于防止在可能的液体提取过程后滥用活性成分的装置(b)。
    • 49. 发明申请
    • Galenic microparticulate oral formulation for delayed and controlled release of pharmaceutical active principles
    • 用于延迟和控制释放药物活性成分的Galenic微粒口服制剂
    • US20050037077A1
    • 2005-02-17
    • US10492129
    • 2002-10-09
    • Valerie LegrandCatherine CastanRemi MeyrueixGerard Soula
    • Valerie LegrandCatherine CastanRemi MeyrueixGerard Soula
    • A61K9/14A61K9/22A61K9/26A61K9/48A61K9/50A61K9/52A61K31/155A61K31/522A61K47/14A61K47/26A61K47/32A61K47/36A61K47/38A61P3/10A61P7/02A61P15/18A61P25/00A61P29/00A61P31/04A61P31/10A61P31/12
    • A61K9/5078
    • The invention relates to a microparticulate system for the delayed and controlled release of active principles (AP) whose absorption window in vivo is essentially limited to the upper parts of the gastrointestinal tract, this system being intended for oral administration. The object of the invention is to provide a system ensuring that the AP is released with certainty by means of a dual mechanism of “time-dependent” and “pH-dependent” release. To achieve this object, the invention proposes a multimicrocapsular oral galenical form which is designed so as to guarantee therapeutic efficacy, and in which the release of the AP is governed by a dual release triggering mechanism that is “time-triggering” and “pH-triggering”. This system consists of microcapsules (200 to 600 μm) comprising a core of AP coated with a film (maximum 40% by weight) comprising a hydrophilic polymer A (Eudragit® L) and a hydrophobic compound B (vegetable wax, melting point=40-90° C.), B/A being between 0.2 and 1.5. These microcapsules have a dissolution behavior in vitro such that, at a constant pH of 1.4, a latency phase of between 1 and 5 hours is observed, followed by a release of the AP, and such that the change from pH 1.4 to pH 6.8 results in a release of the AP without a latency period in vitro.
    • 本发明涉及一种用于延迟和控制释放活性成分(AP)的微粒体系,其活性成分在体内的吸收窗口基本上限于胃肠道的上部,该系统用于口服给药。 本发明的目的是提供一种确保通过“时间依赖”和“依赖于pH”释放的双重机制确定地释放AP的系统。 为了实现该目的,本发明提出了一种多微囊口服盖仑型,其设计以保证治疗功效,并且其中AP的释放由双时间触发机制(“触发时间”和“pH- 触发“。 该系统由包含涂覆有包含亲水性聚合物A(EudragitL)和疏水性化合物B(植物蜡,熔点)的膜(最大40重量%))的AP芯组成的微胶囊(200至600μm) = 40-90℃),B / A在0.2和1.5之间。 这些微胶囊在体外具有溶解行为,使得在1.4的恒定pH下,观察到1至5小时的潜伏期,随后释放AP,并且使得从pH1.4变为pH6.8的结果 在AP的释放中没有潜伏期在体外。