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1. 发明授权

US09220773B2 Pharmaceutical composition 有权
标题翻译：药物组成
公开(公告)号：US09220773B2
公开(公告)日：2015-12-29
申请号：US13988968
申请日：2011-11-28
申请人： Nthato Chirwa , Viness Pillay , Yahya Essop Choonara , Pradeep Kumar , Lisa Claire Du Toit
发明人： Nthato Chirwa , Viness Pillay , Yahya Essop Choonara , Pradeep Kumar , Lisa Claire Du Toit
IPC分类号： A61K39/395 , A61K9/00 , A61K9/107 , A61K31/337 , A61K39/44 , A61K31/282 , A61K31/4745 , A61K9/51 , A61K47/48 , C07K16/30 , A61K9/127
CPC分类号： A61K39/39558 , A61K9/0024 , A61K9/1075 , A61K9/1273 , A61K9/5146 , A61K9/5153 , A61K31/282 , A61K31/337 , A61K31/4745 , A61K39/44 , A61K47/6907 , C07K16/3092
摘要： A pharmaceutical composition for intraperitoneal delivery of an anti-neoplastic agent is provided for treating cancers associated with aberrant mucin expression, preferably ovarian cancer and pancreatic, prostate, metastatic breast, bladder and lung cancers. The composition comprises nanomicelles loaded with the anti-neoplastic agent, and antibodies such as anti-MUC16, anti-MUC1 or anti-MUC4 are conjugated to these nanomicelles. The antibody-bound nanomicelles are optionally embedded in a biodegradable pH- and thermo-responsive hydrogel capable of sol-gel transition at body temperature. The pharmaceutical composition is implantable in the peritoneum, where it transforms into a semi-solid gel at the body's core temperature. In response to pH, the hydrogel swells and releases the antibody-bound nanomicelles. The nanomicelles specifically target mucin antigens on cancer cells. The anti-mucin antibodies can be internalized by the tumor cells, enabling the drug-loaded nanomicelles to gain entry and deliver the chemotherapeutic drugs inside the tumor cell.
摘要翻译：提供用于腹膜内递送抗肿瘤剂的药物组合物用于治疗与异常粘蛋白表达相关的癌症，优选卵巢癌和胰腺，前列腺，转移性乳腺，膀胱和肺癌。组合物包含负载有抗肿瘤剂的纳米胶囊，抗体如抗MUC16，抗-MUC1或抗-MUC4与这些纳米胶束缀合。抗体结合的纳米胶囊任选地嵌入能够在体温下溶胶 - 凝胶转变的可生物降解的pH和热响应性水凝胶中。药物组合物可植入腹膜中，其在身体核心温度下转化为半固体凝胶。响应于pH，水凝胶溶胀并释放抗体结合的纳米胶束。纳米胶囊特异性靶向癌细胞上的粘蛋白抗原。抗粘蛋白抗体可以被肿瘤细胞内化，使载药纳米胶囊能够进入肿瘤细胞内并输送化学治疗药物。

2. 发明申请

US20140004185A1 PHARMACEUTICAL COMPOSITION 有权
标题翻译：药物组合物
公开(公告)号：US20140004185A1
公开(公告)日：2014-01-02
申请号：US13988968
申请日：2011-11-28
申请人： Nthato Chirwa , Viness Pillay , Yahya Essop Choonara , Pradeep Kumar , Lisa Claire Du Toit
发明人： Nthato Chirwa , Viness Pillay , Yahya Essop Choonara , Pradeep Kumar , Lisa Claire Du Toit
IPC分类号： A61K39/395 , A61K39/44 , A61K31/282 , A61K31/337 , A61K31/4745
CPC分类号： A61K39/39558 , A61K9/0024 , A61K9/1075 , A61K9/1273 , A61K9/5146 , A61K9/5153 , A61K31/282 , A61K31/337 , A61K31/4745 , A61K39/44 , A61K47/6907 , C07K16/3092
摘要： A pharmaceutical composition for intraperitoneal delivery of an anti-neoplastic agent is provided for treating cancers associated with aberrant mucin expression, preferably ovarian cancer and pancreatic, prostate, metastatic breast, bladder and lung cancers. The composition comprises nanomicelles loaded with the anti-neoplastic agent, and antibodies such as anti-MUC16, anti-MUC1 or anti-MUC4 are conjugated to these nanomicelles. The antibody-bound nanomicelles are optionally embedded in a biodegradable pH- and thermo-responsive hydrogel capable of sol-gel transition at body temperature. The pharmaceutical composition is implantable in the peritoneum, where it transforms into a semi-solid gel at the body's core temperature. In response to pH, the hydrogel swells and releases the antibody-bound nanomicelles. The nanomicelles specifically target mucin antigens on cancer cells. The anti-mucin antibodies can be internalized by the tumour cells, enabling the drug-loaded nanomicelles to gain entry and deliver the chemotherapeutic drugs inside the tumour cell.
摘要翻译：提供用于腹膜内递送抗肿瘤剂的药物组合物用于治疗与异常粘蛋白表达相关的癌症，优选卵巢癌和胰腺，前列腺，转移性乳腺，膀胱和肺癌。组合物包含负载有抗肿瘤剂的纳米胶囊，抗体如抗MUC16，抗-MUC1或抗-MUC4与这些纳米胶束缀合。抗体结合的纳米胶囊任选地嵌入能够在体温下溶胶 - 凝胶转变的可生物降解的pH和热响应性水凝胶中。药物组合物可植入腹膜中，其在身体核心温度下转化为半固体凝胶。响应于pH，水凝胶溶胀并释放抗体结合的纳米胶束。纳米胶囊特异性靶向癌细胞上的粘蛋白抗原。抗粘蛋白抗体可以被肿瘤细胞内化，使载药纳米胶囊能够进入肿瘤细胞内并输送化学治疗药物。

3. 发明申请

US20130337022A1 PHARMACEUTICAL DOSAGE FORM 有权
标题翻译：药物剂型
公开(公告)号：US20130337022A1
公开(公告)日：2013-12-19
申请号：US13988959
申请日：2011-11-28
申请人： Viness Pillay , Rubina Perveen Shaikh , Yahya Essop Choonara , Lisa Claire Du Toit
发明人： Viness Pillay , Rubina Perveen Shaikh , Yahya Essop Choonara , Lisa Claire Du Toit
IPC分类号： A61K9/00
CPC分类号： A61K9/00 , A61K9/006 , A61K9/0065
摘要： A pH responsive and mucoadhesive pharmaceutical dosage form for the release of a pharmaceutically active agent is described. The dosage form includes a mucoadhesive layer for site-specific mucoadhesion, a water-insoluble outer layer, and an intermediate layer including one or more pharmaceutically active agents for site-specific delivery. The different membranous layers perform different functions in order to create a drug delivery system which is able to deliver a drug to a specific site, for a particular period of time and with a specific drug release pattern. The dosage form can have two or more intermediate layers, each layer comprising an active agent. The mucoadhesive layer can also include an active agents. The dosage form is preferably an oral or buccal delivery form for release of the active agent into the gastro intestinal tract. The intermediate layer can be an electrospun fibrous membrane layer containing the active agent.
摘要翻译：描述了用于释放药物活性剂的pH响应和粘膜粘附药物剂型。剂型包括用于位点特异性粘膜粘附的粘膜粘附层，水不溶性外层和包含用于位点特异性递送的一种或多种药物活性剂的中间层。不同的膜层执行不同的功能，以便产生药物递送系统，其能够将药物递送到特定部位一段特定的时间段并且具有特定的药物释放模式。剂型可以具有两个或更多个中间层，每个层包含活性剂。粘膜粘附层也可以包括活性剂。剂型优选是用于将活性剂释放到胃肠道中的口服或口腔递送形式。中间层可以是含有活性剂的电纺纤维膜层。

4. 发明申请

US20130344125A1 DRUG DELIVERY DEVICE 审中-公开
标题翻译：药物递送装置
公开(公告)号：US20130344125A1
公开(公告)日：2013-12-26
申请号：US13989402
申请日：2011-11-28
申请人： Thiresen Govender , Viness Pillay , Yahya Essop Choonara , Lisa Claire Du Toit , Girish Modi , Dinesh Naidoo , Maluta Steven Mufamadi
发明人： Thiresen Govender , Viness Pillay , Yahya Essop Choonara , Lisa Claire Du Toit , Girish Modi , Dinesh Naidoo , Maluta Steven Mufamadi
IPC分类号： A61K9/00 , A61K31/5415
CPC分类号： A61K9/0085 , A61K9/0024 , A61K9/127 , A61K9/5153 , A61K31/5415 , A61K47/34 , A61K47/6911 , B82Y5/00
摘要： The invention provides an implantable intracranial device for the site-specific delivery of a pharmaceutically active agent to a human or animal for treating a mental or neurological disorder, such as Alzheimer's disease, schizophrenia or other psychoses. The biodegradable device includes a pharmaceutically active agent for treating the disorder, polymeric nano-lipoparticles into or onto which the pharmaceutically active agent is embedded; and a polymeric matrix or scaffold incorporating the nano-lipoparticles. The nano-lipoparticles can be in the form of nano-liposhells or nano-lipobubbles. The nano-liposhells or nano-lipobubbles can include an essential fatty acid or can be conjugated to a peptide ligand which targets the device to a specific cell into which the therapeutic agent can be delivered. The device can be implanted in the sub-arachnoid space in the region of the frontal lobe of the brain.
摘要翻译：本发明提供了用于将药物活性剂向人或动物的位点特异性递送用于治疗精神或神经障碍（例如阿尔茨海默病，精神分裂症或其它精神病）的可植入颅内装置。可生物降解的装置包括用于治疗病症的药物活性剂，将药学活性剂嵌入其中或其上的聚合纳米脂质体; 和包含纳米脂质体的聚合物基质或支架。纳米脂质颗粒可以是纳米脂壳或纳米脂泡的形式。纳米脂壳或纳米脂泡可以包括必需脂肪酸，或者可以将靶向该装置的肽配体缀合到可以递送治疗剂的特定细胞。该装置可以植入在大脑额叶区域的蛛网膜下腔中。

5. 发明申请

US20100179170A1 HETEROGENEOUSLY CONFIGURED MULTIPARTICULATE GASTROINTESTINAL DRUG DELIVERY SYSTEM 审中-公开
标题翻译：异构配体多功能胃肠道给药系统
公开(公告)号：US20100179170A1
公开(公告)日：2010-07-15
申请号：US12312843
申请日：2007-12-03
申请人： Lisa Claire Du Toit , Michael Paul Danckwerts , Viness Pillay , Shivaan Cooppan , Yahya Essop Choonara
发明人： Lisa Claire Du Toit , Michael Paul Danckwerts , Viness Pillay , Shivaan Cooppan , Yahya Essop Choonara
IPC分类号： A61K31/496 , A61K31/44 , A61P31/04
CPC分类号： A61K31/495 , A61K9/5084
摘要： This invention relates to a heterogeneously configured multiparticulate drug delivery system for gastrointestinal delivery of at least one or a combination of active pharmaceutical compositions. The system comprises a multiplicity of enterosoluble or gastrosoluble multiparticulates loaded with the active pharmaceutical composition or compositions for the site-specific delivery of said active pharmaceutical composition or compositions to a specific region in the gastrointestinal tract of a human or animal body. The system can be supplied as reconstitutable granules which are reconstituted immediately before oral administration.
摘要翻译：本发明涉及用于胃肠递送活性药物组合物的至少一种或组合的非均匀配置的多颗粒药物递送系统。该系统包含负载有活性药物组合物或组合物的多种肠溶性或胃溶性多颗粒，用于将所述活性药物组合物或组合物的位点特异性递送至人或动物体的胃肠道中的特定区域。该系统可以作为在口服给药之前立即重建的可重构颗粒提供。

6. 发明申请

US20140037574A1 PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：药物组合物
公开(公告)号：US20140037574A1
公开(公告)日：2014-02-06
申请号：US13989153
申请日：2011-11-28
申请人： Pius Sedowhe Fasinu , Viness Pillay , Yahya Essop Choonara , Lisa Claire Du Toit
发明人： Pius Sedowhe Fasinu , Viness Pillay , Yahya Essop Choonara , Lisa Claire Du Toit
IPC分类号： A61K31/785 , A61K31/765 , A61K31/78 , A61K31/44
CPC分类号： A61K31/785 , A61K31/44 , A61K31/4422 , A61K31/765 , A61K31/78 , A61K45/06 , A61K2300/00
摘要： The invention provides a pharmaceutical composition for oral administration of a pharmaceutically active agent to a subject, including the pharmaceutically active agent and an inhibitor of CYP3A4. Administration of the inhibitor and the pharmaceutically active agent reduces pre-systemic degradation of the pharmaceutically active agent by CYP3A4. The inhibitor can be poly(ethylene glycol), methoxy poly(ethylene glycol), aminated poly(ethylene glycol), O-(2-aminoethyl)-O-methoxy poly(ethylene glycol), polyoxyethylene glycol, branched poly(ethylene glycol), 3-arm poly(ethylene glycol), 4-arm poly(ethylene glycol), 8-arm-poly(ethylene glycol)polyamine, poly(L-lysine), poly(L-arginine), poly(L-alanine), poly(L-valine), poly(L-serine), poly(L-histidine), poly(L-isoleucine), poly(L-leucine), poly(L-glutamic acid), poly(L-glutamine), poly(L-guanidine), poly(methyl methacrylate), polyvinyl acetate, polyacrylate, poly(lactic-co-glycolic acid) and derivatives thereof. A method of treatment is also described.
摘要翻译：本发明提供了一种用于向受试者口服给药药物活性剂的药物组合物，包括药物活性剂和CYP3A4抑制剂。抑制剂和药物活性剂的给药减少CYP3A4对药物活性剂的系统前降解。抑制剂可以是聚（乙二醇），甲氧基聚（乙二醇），胺化聚（乙二醇），O-（2-氨基乙基）-O-甲氧基聚（乙二醇），聚氧乙二醇，支链聚（乙二醇），3-臂聚（乙二醇），4-臂聚（乙二醇），8-臂聚（乙二醇）多胺，聚（L-赖氨酸），聚（L-精氨酸），聚（L-丙氨酸），聚（L-缬氨酸），聚（L-丝氨酸），聚（L-组氨酸），聚（L-异亮氨酸），聚（L-亮氨酸），聚（L-谷氨酸），聚（L-胍），聚（甲基丙烯酸甲酯），聚乙酸乙烯酯，聚丙烯酸酯，聚（乳酸 - 共 - 乙醇酸）及其衍生物。还描述了一种治疗方法。

7. 发明申请

US20140005269A1 POLYMERIC MATRIX OF POLYMER-LIPID NANOPARTICLES AS A PHARMACEUTICAL DOSAGE FORM 审中-公开
标题翻译：聚合物脂质纳米粒子作为药物剂型的聚合物
公开(公告)号：US20140005269A1
公开(公告)日：2014-01-02
申请号：US13989462
申请日：2011-11-28
申请人： Ndidi Ngwuluka , Viness Pillay , Yahya Essop Choonara , Lisa Claire Du Toit
发明人： Ndidi Ngwuluka , Viness Pillay , Yahya Essop Choonara , Lisa Claire Du Toit
IPC分类号： A61K47/32 , A61K31/198
CPC分类号： A61K47/32 , A61K9/2077 , A61K9/513 , A61K31/198
摘要： A pharmaceutical dosage form for the release of at least one pharmaceutically active ingredient is claimed. The pharmaceutical dosage form includes a polymer matrix, polymer-lipid nanoparticles incorporated within the matrix and the pharmaceutically active ingredient(s). The polymer matrix is formed from at least two crosslinked cationic and anionic polymers, such as Eudragit® E100 and sodium carboxymethlycellulose. It can also include a neutral polymer, such as one derived from locust bean. The polymer-lipid nanoparticles are formed from at least one polymer, such as Eudragit® E100 and/or chitosan, and at least one phospholipid, such as lecithin. The polymer(s) and phospholipid are crosslinking with a chelating agent, such as sodium tripolyphosphate. The active ingredient or ingredients can be any pharmaceutically active compound(s), and in particular poorly absorbed compounds such as levodopa for the treatment of Parkinson's disease.
摘要翻译：要求保护用于释放至少一种药物活性成分的药物剂型。药物剂型包括聚合物基质，掺入基质内的聚合物 - 脂质纳米颗粒和药物活性成分。聚合物基质由至少两种交联的阳离子和阴离子聚合物如Eudragit E100和羧甲基纤维素钠形成。它还可以包括一种中性聚合物，如从刺槐豆衍生的聚合物。聚合物 - 脂质纳米颗粒由至少一种聚合物如Eudragit E100和/或壳聚糖和至少一种磷脂如卵磷脂形成。聚合物和磷脂与螯合剂如三聚磷酸钠交联。活性成分或成分可以是任何药物活性化合物，特别是不良吸收的化合物，例如用于治疗帕金森病的左旋多巴。

8. 发明授权

US09808418B2 Pharmaceutical dosage form 有权
公开(公告)号：US09808418B2
公开(公告)日：2017-11-07
申请号：US13988959
申请日：2011-11-28
申请人： Viness Pillay , Rubina Perveen Shaikh , Yahya Essop Choonara , Lisa Claire Du Toit
发明人： Viness Pillay , Rubina Perveen Shaikh , Yahya Essop Choonara , Lisa Claire Du Toit
IPC分类号： A61K9/00 , A61K9/52
CPC分类号： A61K9/00 , A61K9/006 , A61K9/0065
摘要： A pH responsive and mucoadhesive pharmaceutical dosage form for the release of a pharmaceutically active agent is described. The dosage form includes a mucoadhesive layer for site-specific mucoadhesion, a water-insoluble outer layer, and an intermediate layer including one or more pharmaceutically active agents for site-specific delivery. The different membranous layers perform different functions in order to create a drug delivery system which is able to deliver a drug to a specific site, for a particular period of time and with a specific drug release pattern. The dosage form can have two or more intermediate layers, each layer comprising an active agent. The mucoadhesive layer can also include an active agents. The dosage form is preferably an oral or buccal delivery form for release of the active agent into the gastro intestinal tract. The intermediate layer can be an electrospun fibrous membrane layer containing the active agent.

9. 发明申请

US20140023692A1 DRUG DELIVERY DEVICE 审中-公开
标题翻译：药物递送装置
公开(公告)号：US20140023692A1
公开(公告)日：2014-01-23
申请号：US13989401
申请日：2011-11-28
申请人： Lisa Claire Du Toit , Viness Pillay , Yahya Essop Choonara , Thirumala Govender , Trevor Robin Carmichael
发明人： Lisa Claire Du Toit , Viness Pillay , Yahya Essop Choonara , Thirumala Govender , Trevor Robin Carmichael
IPC分类号： A61K9/00 , A61K31/496 , A61K45/06 , A61K31/405
CPC分类号： A61K9/0051 , A61K9/0024 , A61K31/405 , A61K31/496 , A61K45/06 , A61K47/32 , A61K47/36
摘要： The invention provides an inflammation-responsive implantable device for the in situ delivery of one or more pharmaceutically active agents to a human or animal. The device comprises two differential release bioresponsive polymeric matrices (BPMs): an outer polymetric matrix and an inner polymeric matrix, both of which contain at least one pharmaceutically active agent or drug, typically an antibiotic and an anti-inflammatory agent, respectively. The therapeutically effective agent may be embedded in nanoparticles or nanobubbles. In response to inflammation, the pharmaceutically active agents are released, but at different rates: the rate of drug release from the inner polymeric matrix is lower than the rate of drug release from the outer polymeric matrix. Suitable polymers for forming the outer and inner polymeric matrices are hyaluronic acid and chitosan, respectively. A method of making the device and a method of treatment are also described.
摘要翻译：本发明提供了用于将一种或多种药物活性剂原位递送至人或动物的炎症反应性可植入装置。该装置包括两个差异释放的生物反应性聚合物基质（BPM）：外部多聚基质和内部聚合物基质，两者均分别含有至少一种药物活性剂或药物，通常为抗生素和抗炎剂。治疗有效的药剂可以嵌入纳米颗粒或纳米气泡中。响应于炎症，药物活性剂被释放，但是以不同的速率释放：从内部聚合物基质释放的药物的速率低于从外部聚合物基质释放药物的速率。用于形成外部和内部聚合物基质的合适的聚合物分别是透明质酸和壳聚糖。还描述了制造该装置的方法和一种治疗方法。

10. 发明申请

US20140005199A1 IMPLANT FOR THE CONTROLLED RELEASE OF PHARMACEUTICALLY ACTIVE AGENTS 审中-公开
标题翻译：用于控制释放药物活性剂的植物
公开(公告)号：US20140005199A1
公开(公告)日：2014-01-02
申请号：US13989346
申请日：2011-11-28
申请人： Ameena Wadee , Viness Pillay , Yahya Essop Choonara , Lisa Claire Du Toit
发明人： Ameena Wadee , Viness Pillay , Yahya Essop Choonara , Lisa Claire Du Toit
IPC分类号： A61K9/00 , A61K45/06 , A61K47/32 , A61K31/519
CPC分类号： A61K9/0024 , A61K9/5026 , A61K31/519 , A61K45/06 , A61K47/32
摘要： A pharmaceutical composition or dosage form is described for the delivery of at least one pharmaceutically active agent or drug in a sustained and controlled manner. The pharmaceutical composition is an injectable formulation which is capable of responding to local stimuli at the site of injection, such as pH and temperature, and comprises a thermoresponsive polymer composition with a suspension of pH responsive micro- or nano-particles which contain the at least one pharmaceutically active agent or drug. The thermoresponsive polymer composition is formed from poly(methyl vinyl ether) (PMVE), and an inorganic salt, and the micro- or nano-particles are formed from chitosan and eudragit. The composition can be used to treat any disease or condition which results in a decrease in pH, such as for treating a solid tumour, gout, acidosis, ketosis and the like.
摘要翻译：描述了用于以持续和受控的方式递送至少一种药物活性剂或药物的药物组合物或剂型。药物组合物是能够对注射部位的局部刺激如pH和温度进行响应的可注射制剂，并且包含具有pH响应性微纳米颗粒悬浮液的热反应性聚合物组合物，其含有至少一种药物活性剂或药物。热聚合物组合物由聚（甲基乙烯基醚）（PMVE）和无机盐形成，微米或纳米颗粒由壳聚糖和eudragit形成。该组合物可用于治疗导致pH降低的任何疾病或病症，例如用于治疗实体瘤，痛风，酸中毒，酮症等。

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