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    Alprazolam inclusion complexes and pharmaceutical compositions thereof
    2.
    发明授权
    Alprazolam inclusion complexes and pharmaceutical compositions thereof 失效
    阿普唑仑包合物及其药物组合物

    公开(公告)号：US07202233B2

    公开(公告)日：2007-04-10

    申请号：US11144965

    申请日：2005-06-03

    Applicant: Lawrence John Penkler

    Inventor： Lawrence John Penkler

    IPC: A61K31/724 ,  A61K31/517

    CPC classification number: B82Y5/00 ,  A61K47/6951

    Abstract: A pharmaceutical composition an inclusion complex and methods for treating patients and preparing said complex disclosed for transmucosal delivery comprising an inclusion complex of (a) alprazolam and (b) a water soluble 2-hydroxypropyl-beta-cyclodextrin, and a pharmaceutically acceptable carrier therefor, wherein all the alprazolam is present in ring-closed form.

    Abstract translation: 一种药物组合物，包含复合物和用于治疗患者并制备所述经粘膜递送的所述复合物的方法，其包含（a）阿普唑仑和（b）水溶性2-羟丙基-β-环糊精的包合物及其药学上可接受的载体， 其中所有的阿普唑仑以环封形式存在。

    Pharmaceutical cyclosporin formulation with improved biopharmaceutical properties, improved physical quality and greater stability, and method for producing said formulation
    3.
    发明授权
    Pharmaceutical cyclosporin formulation with improved biopharmaceutical properties, improved physical quality and greater stability, and method for producing said formulation 失效
    具有改善的生物药物性质，改善的物理质量和更大的稳定性的药物环孢菌素制剂以及用于生产所述制剂的方法

    公开(公告)号：US06551619B1

    公开(公告)日：2003-04-22

    申请号：US09674417

    申请日：2001-01-22

    Applicant: Lawrence John Penkler ,  Rainer Helmut Müller ,  Stephan Anton Runge ,  Vittorino Ravelli

    Inventor： Lawrence John Penkler ,  Rainer Helmut Müller ,  Stephan Anton Runge ,  Vittorino Ravelli

    IPC: A61K914

    CPC classification number: A61K9/5123 ,  A61K9/1075 ,  A61K9/1617 ,  A61K38/13 ,  Y10S514/951 ,  Y10S514/969 ,  Y10S514/975 ,  Y10S977/906

    Abstract: The invention relates to solid, particulate lipid-based excipients which are loaded with cyclosporine. Said excipients have improved biopharmaceutical properties for cyclosporines in vivo, are of a better quality (in terms of fineness, homogeneity of the particles, inclusion of the medicament) and are more physically stable in the particulate formulation (no aggregation or gel formation). The invention also relates to a therapeutic treatment with cyclosporine formulations which produce an average blood level concentration in the steady state range of 300 ng/ml to over 1000 ng/ml, preferably over 800 ng/ml, especially up to 900 ng/ml, preferably 400 ng/ml to 800 ng/ml in the absence of high initial blood level concentrations essentially over 1500 ng/ml, especially over 1200 ng/ml. This blood level concentration is preferably maintained for an extended period of at least 5 hours, preferably at least 7 hours.

    Abstract translation: 本发明涉及负载有环孢菌素的固体颗粒状基于脂质的赋形剂。 所述赋形剂在体内具有改善的环孢菌素的生物药物性质，具有更好的质量（在细度，颗粒的均匀性，药物的包合性方面），并且在颗粒制剂中更具物理稳定性（无聚集或凝胶形成）。 本发明还涉及使用环孢菌素制剂的治疗性治疗，其在300ng / ml至超过1000ng / ml，优选超过800ng / ml，特别是至多900ng / ml的稳态范围内产生平均血液浓度， 优选400ng / ml至800ng / ml，在不存在高的初始血液浓度基本上超过1500ng / ml，特别是超过1200ng / ml的情况下。 该血液浓度优选保持至少5小时，优选至少7小时的延长时间。

    STABLE INJECTABLE COMPOSITIONS
    6.
    发明申请
    STABLE INJECTABLE COMPOSITIONS 审中-公开
    稳定的注射组合物

    公开(公告)号：US20120142779A1

    公开(公告)日：2012-06-07

    申请号：US13153283

    申请日：2011-06-03

    Applicant: Lawrence John PENKLER ,  Barry Paul Daisley

    Inventor： Lawrence John PENKLER ,  Barry Paul Daisley

    IPC: A61K31/196 ,  A61P29/00

    CPC classification number: A61K47/183 ,  A61K9/0019 ,  A61K31/195 ,  A61K31/724 ,  A61K47/20 ,  A61K47/40

    Abstract: This invention relates to a stable parenteral aqueous solutions comprising either (a) diclofenac or a pharmaceutically acceptable diclofenac salt and a cyclodextrin, or (b) an inclusion complex of diclofenac or a pharmaceutically acceptable diclofenac salt and a cyclodextrin, or a mixture of (a) and (b), which are suitable for intramuscular and intravenous administration. The solutions contain diclofenac or diclofenac salt, cyclodextrin, and an antioxidant selected from monothioglycerol, or a combination of ethylene diamine tetra-acetic acid and N-acetyl-cysteine.

    Abstract translation: 本发明涉及一种稳定的肠胃外水溶液，其包含（a）双氯芬酸或药学上可接受的双氯芬酸盐和环糊精，或（b）双氯芬酸或其药学上可接受的双氯芬酸盐和环糊精的包合络合物或（a ）和（b），适用于肌内和静脉内给药。 溶液含有双氯芬酸或双氯芬酸盐，环糊精和选自一硫代甘油的抗氧化剂，或乙二胺四乙酸和N-乙酰半胱氨酸的组合。

    Amphiphilic macrocyclic derivatives and their analogues
    7.
    发明授权
    Amphiphilic macrocyclic derivatives and their analogues 有权
    两亲大环衍生物及其类似物

    公开(公告)号：US07786095B2

    公开(公告)日：2010-08-31

    申请号：US11295724

    申请日：2005-12-07

    Applicant: Raphael Darcy ,  Lawrence John Penkler ,  Bart Jan Ravoo

    Inventor： Raphael Darcy ,  Lawrence John Penkler ,  Bart Jan Ravoo

    IPC: A61K31/724

    CPC classification number: C08B37/0012 ,  A61K47/6951 ,  B82Y5/00

    Abstract: Soluble amphiphilic macrocycle analogues having lipophilic groups attached to one side of the units making up the macrocycle and hydrophilic groups attached to the other side. These amphiphilic macrocyclic derivatives have the ability to self-assemble in aqueous solvent forming micelles or vesicles and can be used as hosts for the solubilization and/or stabilization of various compounds. Embodiments of the present invention utilize macrocyclic oligosaccharides and preferably cyclodextrin as the macrocyclic derivatives to be modified.

    Abstract translation: 可溶性两亲大环化合物类似物具有连接在构成大环的单元的一侧的亲油基团和连接到另一侧的亲水基团。 这些两亲性大环衍生物具有在含水溶剂形成胶束或囊泡中自组装的能力，并且可以用作各种化合物的溶解和/或稳定化的宿主。 本发明的实施方案使用大环寡糖，优选环糊精作为待修饰的大环衍生物。

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