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    Extending the duration of drug release within the stomach during the fed mode
    1.
    发明授权
    Extending the duration of drug release within the stomach during the fed mode 有权
    在喂食模式期间延长胃内药物释放的持续时间

    公开(公告)号：US06340475B2

    公开(公告)日：2002-01-22

    申请号：US09282233

    申请日：1999-03-29

    Applicant: John W. Shell ,  Jenny Louie-Helm ,  Micheline Markey

    Inventor： John W. Shell ,  Jenny Louie-Helm ,  Micheline Markey

    IPC: A61K926

    CPC classification number: A61K9/0065 ,  A61K9/2013 ,  A61K9/2031 ,  A61K9/205 ,  A61K9/2054

    Abstract: Drugs are formulated as unit oral dosage forms by incorporating them into polymeric matrices comprised of hydrophilic polymers that swell upon imbibition of water to a size that is large enough to promote retention of the dosage form in the stomach during the fed mode. The oral formulation is designed for gastric retention and controlled delivery of an incorporated drug into the gastric cavity, and thus administered, the drug is released from the matrix into the gastric fluid by solution diffusion. The swollen polymeric matrix, having achieved sufficient size, remains in the gastric cavity for several hours if administered while the patient is in the fed mode, and remains intact long enough for substantially all of the drug to be released before substantial dissolution of the matrix occurs. The swelling matrix lowers the accessibility of the gastric fluid to the drug and thereby reduces the drug release rate. This process, together with diffusion retardation by selection of specific polymers, polymer molecular weights, and other variables, results in a sustained and controlled delivery rate of the drug to the gastric cavity.

    Abstract translation: 将药物配制成单位口服剂型，通过将它们并入由亲水性聚合物组成的聚合物基质中，所述亲水性聚合物在吸水时膨胀至足够大以在给药模式期间促进剂型在胃中的保留。 口服制剂设计用于胃内保留和控制递送并入药物进入胃腔，并因此施用，通过溶液扩散将药物从基质释放到胃液中。 已经达到足够大小的溶胀的聚合物基质在患者处于喂养模式的同时在胃腔内保留数小时，并保持完整的时间足以使基本上所有的药物在基质溶解之前被释放出来 。 溶胀基质降低胃液对药物的可及性，从而降低药物释放速率。 该方法与通过选择特定聚合物，聚合物分子量和其他变量的扩散阻滞一起导致药物持续且受控制的胃腔输送速率。

    Alkyl-substituted cellulose-based sustained-release oral drug dosage forms
    2.
    发明授权
    Alkyl-substituted cellulose-based sustained-release oral drug dosage forms 失效
    烷基取代纤维素基持续释放口服药物剂型

    公开(公告)号：US5582837A

    公开(公告)日：1996-12-10

    申请号：US453144

    申请日：1995-05-30

    Applicant: John W. Shell

    Inventor： John W. Shell

    IPC: A61K9/16 ,  A61K9/20 ,  A61K9/26 ,  A61K9/52 ,  A61K9/22

    CPC classification number: A61K9/2077 ,  A61K9/1652 ,  Y10S514/925 ,  Y10S514/951

    Abstract: Sustained release oral drug dosage forms that comprise a tablet or capsule containing a plurality of particles of a solid-state drug dispersed in alkyl cellulose such as hydroxyethylcellulose or hydroxypropylcellulose. Once ingested the tablet or capsule disintegrates to disperse the particles into the stomach where they imbibe water to cause them to swell and also to become slippery, thus enhancing their retention in the stomach. Imbibed water from the gastric fluid dissolves the drug entrapped in the particles and the resulting solution diffuses from the dispersed particles, assuring that no solid drug, which with some drugs is more irritating, contacts the mucosal tissue. A number of embodiments of the dosage form utilizing different drugs are exemplified and the benefits are explained. Aspirin is one example.

    Abstract translation: 持续释放口服药物剂型，其包含含有分散在烷基纤维素如羟乙基纤维素或羟丙基纤维素中的多种固态药物颗粒的片剂或胶囊。 一旦摄取，片剂或胶囊就会崩解，将颗粒分散到胃中，在那里它们吸收水分，使它们膨胀并变得滑溜，从而增强其在胃中的保留性。 来自胃液的吸入水溶解包埋在颗粒中的药物，所得溶液从分散的颗粒中扩散，确保没有固体药物（其中一些药物更刺激）与粘膜组织接触。 使用不同药物的剂型的多个实施方案被举例说明，并且说明了益处。 阿司匹林是一个例子。

    Ocular system made of bioerodible esters having linear ether
    3.
    发明授权
    Ocular system made of bioerodible esters having linear ether 失效
    由具有线性醚的生物可降解酯制成的眼科系统

    公开(公告)号：US4115544A

    公开(公告)日：1978-09-19

    申请号：US850275

    申请日：1977-11-10

    Applicant: John W. Shell

    Inventor： John W. Shell

    IPC: A61K9/00 ,  A61K9/14 ,  A61K9/22 ,  A61K9/32

    CPC classification number: A61K9/0051

    Abstract: An ophthalmological bioerodible dosage form for ophthalmic drugs is disclosed. The dosage form comprises particles of 10 to 300 microns made of drug dispersed within a drug release rate controlling material which bioerodes in the environment of the eye.

    Abstract translation: 公开了一种用于眼科药物的眼科生物可腐蚀剂型。 剂型包含10至300微米的由分散在药物释放速率控制材料中的药物制成的颗粒，其在眼睛的环境中生物化。

    Treatment of glaucoma using phosphodiesterase inhibitors
    6.
    发明授权
    Treatment of glaucoma using phosphodiesterase inhibitors 失效
    使用磷酸二酯酶抑制剂治疗青光眼

    公开(公告)号：US5011843A

    公开(公告)日：1991-04-30

    申请号：US531729

    申请日：1990-06-01

    Applicant: John W. Shell

    Inventor： John W. Shell

    IPC: A61K31/505 ,  A61K31/535

    CPC classification number: A61K31/535 ,  A61K31/505

    Abstract: Lowering of intraocular pressure, e.g. in the treatment of glaucoma is carried out by administering a phosphodiesterase inhibitor to a patient. Particular ophthalmic pharmaceutical compositions are disclosed for topical application to the eye.

    Abstract translation: 降低眼压，例如 在治疗青光眼中通过向患者施用磷酸二酯酶抑制剂进行。 公开了特定的眼用药物组合物用于局部施用于眼睛。

    Device for administering solid drug particles to an eye
    9.
    发明授权
    Device for administering solid drug particles to an eye 失效
    用于向眼睛施用固体药物颗粒的装置

    公开(公告)号：US4173226A

    公开(公告)日：1979-11-06

    申请号：US922742

    申请日：1978-07-07

    Applicant: John W. Shell

    Inventor： John W. Shell

    IPC: A61F9/00 ,  A61M1/00

    CPC classification number: A61F9/0017 ,  A61F9/0008

    Abstract: An ophthalmic bioerodible dosage form for ophthalmic drugs is disclosed. The dosage form comprises particles of 10 to 300 microns made of drug dispersed within a drug release rate controlling material which bioerodes in the environment of the eye.

    Abstract translation: 公开了一种用于眼科药物的眼用生物腐蚀剂型。 剂型包含10至300微米的由分散在药物释放速率控制材料中的药物制成的颗粒，其在眼睛的环境中生物化。

    Pharmacological inducement of the fed mode for enhanced drug administration to the stomach
    10.
    发明授权
    Pharmacological inducement of the fed mode for enhanced drug administration to the stomach 有权
    用于增强药物给予胃的喂养模式的药理学诱导

    公开(公告)号：US07405238B2

    公开(公告)日：2008-07-29

    申请号：US10235076

    申请日：2002-09-04

    Applicant: Micheline Markey ,  John W. Shell ,  Bret Berner

    Inventor： Micheline Markey ,  John W. Shell ,  Bret Berner

    IPC: A61K31/21 ,  A61K47/00

    CPC classification number: A61K9/0065 ,  A61K9/209 ,  A61K9/5084

    Abstract: Drugs intended for absorption in the stomach or upper intestinal tract are administered in oral drug delivery systems in conjunction with any of various substances that have been discovered to function as potent agents for inducing the fed mode. By inducing the onset of the fed mode, these agents cause the stomach to prolong its retention of the drug delivery system, which is either large enough to be retained in the stomach during the fed mode or swells or expands to such a size upon ingestion. The fed mode inducing agents include the following compounds and their salts: glycine and glycylglycine, xylitol and related sugar alcohols, sodium and other metal docusates, β-casomorphins, α-lipoic acid and similarly structured acids, 2,2-diaryl-4-(4′-aryl-4′-hydroxypipendino)butyramides, arginine, Trp-Trp, alkylpyridinium halides, dihydroxybenzoic acids, and potent sweeteners such as aspartame, aspartic acid, acesulfame, and stevioside.

    Abstract translation: 预期用于在胃或上肠道中吸收的药物在口服药物递送系统中与已被发现用作诱导喂养模式的有效药剂的任何各种物质一起施用。 通过诱导进食模式的发作，这些药物引起胃部延长其药物递送系统的保留，药物递送系统的大小足以在进食模式期间保留在胃中，或者在摄食时膨胀或膨胀至这样的大小。 饲喂模式诱导剂包括以下化合物及其盐：甘氨酸和甘氨酰甘氨酸，木糖醇和相关糖醇，钠和其他金属多库酯，β-半胱氨酸，α-硫辛酸和类似结构的酸，2,2-二芳基-4- （4'-芳基-4'-羟基磷脂）丁酰胺，精氨酸，Trp-Trp，烷基吡啶鎓卤化物，二羟基苯甲酸，以及强效甜味剂，如阿斯巴甜，天冬氨酸，乙酰磺胺酸和甜菊苷。

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