中文摘要：本发明公开了一种可用于活性亲脂化合物口腔粘膜给药的药物组合物，该组合物由一种亲脂活性化合物、一种由2种或2种以上水溶性聚合物和一种快速溶解介质组成的聚合物基体组成；其中，至少一种水溶性聚合物是两性分子聚合物，一种水溶性聚合物是包含疏水-亲水平衡基的亲水性或两性分析聚合物，后一种聚合物与前一种完全不同。此外，这种聚合物基体不是交联的，同时聚合物之间以及聚合物与脂溶性活性物质之间不发生共价相互作用，而这种交互作用发生在脂溶性活性物质与上述聚合物基体之间。这种药物组合物可用于治疗偏头痛、糖尿病、化疗引起的恶心、突发性疼痛、急性精神病和神经系统紊乱。
外文摘要：A pharmaceutical composition is provided for transmucosal administration of an active lipophilic compound through the oral mucosa comprising a lipophilic active compound, a polymeric matrix formed by two or more water-soluble polymers and a rapid dissolution agent. At least one of the water-soluble polymers is an amphiphilic polymer and at least one is either a hydrophilic polymer or an amphiphilic polymer with a hydrophobic-hydrophilic balance different from the first amphiphilic polymer. In addition, the polymeric matrix is not crosslinked and no covalent interaction occurs between the two or more polymers and between the polymers and the lipophilic active compound, which is interwoven with the aforesaid polymeric matrix.
NOVELTY - Pharmaceutical composition comprises (a) a lipophilic active compound, (b) a polymeric matrix formed by two or more water-soluble polymers, where at least one of the two or more water-soluble polymers is an amphiphilic polymer and at least one other of the two or more water-soluble polymers is either a hydrophilic polymer or an amphiphilic polymer, and (c) a rapid dissolution agent.
USE - The pharmaceutical composition is useful for treating migraines, diabetes, chemotherapy-induced nausea, breakthrough pain, and acute psychotic and neurological disorders.
ADVANTAGE - The pharmaceutical composition has controlled adhesiveness to mucosal surface, improved solubility and high dissolution rate of a pharmaceutical compound in saliva, release of drug with a sufficient residual time for mucosal absorption, delivery of the drug in a non-ionizing lipophilic form in order to permeate series of barriers to re! ach the circulatory system via the most efficient trans-cellular route, improvement of the permeability properties, that together with the high dissolution rate and sufficient residual time, translates into earlier and higher drug exposure and faster absorption with a lower delivered dose than the oral tablet, hence the fast onset of action is observed, similarity of the earlier exposure to that of the nasal spray, yet the sublingual transmucosal form presents a higher initial peak and prolonged exposure compared with the intranasal formulation, ability to deliver the relatively high dose of drug, in order to provide both important features: fast onset of action and therapeutic effect prolongation, the former is a result of transmucosal absorption, and the latter is a result of the gastrointestinal absorption of the swallowed drug, improved bioavailability of the drug (75 mg sublingual tablet showed the pharmacokinetics similar to 100 mg existing oral tablet).
主权项：DETAILED DESCRIPTION - Pharmaceutical composition comprises (a) a lipophil ic active compound, (b) a polymeric matrix formed by two or more water-soluble polymers, where (i) at least one of the two or more water-soluble polymers is an amphiphilic polymer and at least one other of the two or more water-soluble polymers is either a hydrophilic polymer or an amphiphilic polymer with a hydrophobic-hydrophilic balance different from the first amphiphilic polymer, and (ii) the polymeric matrix is not crosslinked and no covalent interaction occurs between the two or more polymers and between the polymers and the lipophilic active compound, which is interwoven with the polymeric matrix, and (c) a rapid dissolution agent. An INDEPENDENT CLAIM is included for method for the preparation of the composition, which involves (i) preparing a clear and homogeneous solution of the two or more polymers, the rapid dissolution agent and the lipophilic active compound in water or in a mixture of water and one or more organic solvents, and (ii) drying the obtained clear and homogeneous solution, preferably by spray drying, to form a dry powder.
申请号：US201615337251
公开/公告号：US2017119660A1
申请日：2016-10-28
公开/公告日：2017-05-04
申请/专利权人：SOLUBEST LTD (SOLU-N)
发明/设计人：TEMTSIN-KRAYZ, G; GLOZMAN, S; KAZHDAN, P
分类号：A61K31/05; A61K31/352; A61K31/4045; A61K31/5377; A61K31/573; A61K38/28; A61K9/006; A61K9/1611; A61K9/1623; A61K9/1635; A61K9/1641; A61K9/1652; A61K9/2009; A61K9/2018; A61K9/2031; A61K9/2054; A61K9/2059
主分类号：A61K31/05; A61K31/352; A61K31/4045; A61K31/573; A61K38/28; A61K9/00; A61K9/16; A61K9/20
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