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    Useful pro-drug forms of theophylline
    31.
    发明授权
    Useful pro-drug forms of theophylline 失效
    茶碱的有用的前药形式

    公开(公告)号：US4002756A

    公开(公告)日：1977-01-11

    申请号：US617030

    申请日：1975-09-26

    Applicant: Takeru Higuchi ,  Nicolae S. Bodor ,  Yu-Neng Kuo

    Inventor： Takeru Higuchi ,  Nicolae S. Bodor ,  Yu-Neng Kuo

    IPC: A61K31/52

    CPC classification number: A61K31/52 ,  Y10S514/826

    Abstract: There is provided novel and useful pro-drug forms of theophylline having the formula: ##STR1## wherein R represents a member selected from the group consisting of a straight or branched C.sub.4 -C.sub.20 alkyl group, a straight or branched C.sub.14 -C.sub.20 alkenyl group, a substituted phenyl group or a substituted or unsubstituted naphthyl group whose substituents are selected from the group consisting of a hydroxy group, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.14 acyloxy group, and a halogen atom (Cl, Br, I), and a substituted or unsubstituted heteroaromatic group whose substituents are selected from the group consisting of a hydroxy group, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 acyloxy group, and a halogen atom (Cl, Br, I), and wherein A presents a member selected from the group consistng of a --CO-- group, a --CO--(CH.sub.2).sub.n --C-- group, wherein n represents an integer of from 1 to 16, a --CO--CH=CH--CO-- group (cis or trans), ##STR2## AND A ##STR3## group. The compounds of this invention are useful in the treatment of asthma in warm-blooded animals. Upon administration, the compounds of this invention slowly go into solution and subsequently cleave prior to and/or during the absorption process, releasing theophylline in a sustained manner at a non-toxic, therapeutic level; that is, without the large blood level variations normally observed when theophylline per se is administered.

    Abstract translation: 提供了具有下式的茶碱的新型有用的前药形式：其中R表示选自直链或支链C4-C20烷基的成员， 直链或支链C 14 -C 20烯基，取代苯基或取代或未取代的萘基，其取代基选自羟基，C1-C4烷基，C1-C4烷氧基，C1- C14酰氧基和卤素原子（C1，Br，I），以及取代或未取代的杂芳基，其取代基选自羟基，C1-C4烷基，C1-C4烷氧基， C 1 -C 4酰氧基和卤素原子（Cl，Br，I），其中A表示选自-CO-基团，-CO-（CH 2）n C - 基团的基团，其中n 表示1〜16的整数，-CO-CH = CH-CO-基（顺式或反式），和A 组。

    Ocular insert
    32.
    发明授权
    Ocular insert 失效
    眼插入

    公开(公告)号：US3995635A

    公开(公告)日：1976-12-07

    申请号：US520277

    申请日：1974-11-04

    Applicant: Takeru Higuchi ,  Anwar A. Hussain ,  John W. Shell

    Inventor： Takeru Higuchi ,  Anwar A. Hussain ,  John W. Shell

    IPC: A61F9/00 ,  A61K9/00 ,  A61K27/12 ,  A61M31/00

    CPC classification number: A61K9/0051 ,  A61F9/0017

    Abstract: A drug-dispensing ocular insert containing a drug and suited for application to the eyeball to dispense said drug to the eye over a prolonged period of time, includes, for permitting facile insertion into and comfortable retention within the eye, and more importantly for preventing the accidental expulsion of the insert therefrom, first detent means adapted for insertion into the cul-de-sac of the conjunctiva between the sclera of the eyeball and the upper eyelid, and second, conjoint detent means, cooperative with said first detent means, adapted for insertion into the cul-de-sac of the conjunctiva between the said sclera of the eyeball and the lower eyelid.

    Abstract translation: 包含药物并且适用于眼球以将药物长时间分配给眼睛的药物分配眼部插入物包括用于允许容易地插入眼睛内并舒适地保持在眼睛内，并且更重要的是防止 插入物的意外排出，适于插入眼球巩膜与上眼睑之间的结膜死腔的第一止动装置，以及与所述第一制动装置配合的第二联合制动装置，适于 插入眼球的巩膜和下眼睑之间的结膜的死腔。

    Bioerodible ocular device
    33.
    发明授权
    Bioerodible ocular device 失效
    生物蚀刻眼睛装置

    公开(公告)号：US3981303A

    公开(公告)日：1976-09-21

    申请号：US600793

    申请日：1975-07-31

    Applicant: Takeru Higuchi ,  Anwar A. Hussain ,  John W. Shell

    Inventor： Takeru Higuchi ,  Anwar A. Hussain ,  John W. Shell

    IPC: A61F9/00 ,  A61K9/00 ,  A61M31/00

    CPC classification number: A61K9/0051 ,  A61F9/0017

    Abstract: An ocular insert for the continuous controlled administration of a predetermined therapeutically effective dosage of drug to the eye over a prolonged period of time. The device meters the flow of drug by means of a drug release rate controlling material. The insert bioerodes in the environment of the eye concurrently with the dispensing or at a point in time after the dispensing of the therapeutically desired amount of drug.

    Abstract translation: 用于在长时间内连续控制施用预定的治疗有效剂量的眼药物的眼部插入物。 该装置通过药物释放速率控制材料来衡量药物的流动。 在眼睛的环境中插入生物元件与分配或在分配治疗期望量的药物之后的时间点同时进行。

    Administration of alkaline earth metal salts of salicylamide
    34.
    发明授权
    Administration of alkaline earth metal salts of salicylamide 失效
    施用水杨酰胺的碱土金属盐

    公开(公告)号：US3956490A

    公开(公告)日：1976-05-11

    申请号：US557367

    申请日：1975-03-11

    Applicant: Takeru Higuchi ,  Anwar A. Hussain

    Inventor： Takeru Higuchi ,  Anwar A. Hussain

    IPC: A61K31/60 ,  A61K31/615

    CPC classification number: A61K31/621 ,  A61K31/60

    Abstract: Alkaline earth metal salts of salicylamide are administered in solid oral dosage forms with substantially improved analgesic, anti-inflammatory, antipyretic and sedative results as compared with salicylamide. Highest blood levels are obtained by administering enteric-coated salicylamide salt dosage forms.

    Abstract translation: 与水杨酰胺相比，水杨酰胺的碱土金属盐以固体口服剂型施用，具有显着改善的镇痛，抗炎，解热和镇静作用。 通过施用肠溶衣水杨酰胺盐剂型获得最高血液水平。

    Methods and apparatus for determining the rate of movement of a study substance through a membrane
    38.
    发明授权
    Methods and apparatus for determining the rate of movement of a study substance through a membrane 失效
    用于确定研究物质通过膜的移动速率的方法和装置

    公开(公告)号：US4740309A

    公开(公告)日：1988-04-26

    申请号：US901659

    申请日：1986-08-29

    Applicant: Takeru Higuchi

    Inventor： Takeru Higuchi

    IPC: B01D61/28 ,  G01N13/00 ,  G01N33/15 ,  G01N35/00 ,  B01D13/00

    CPC classification number: B01D61/28 ,  G01N13/00 ,  G01N2013/006 ,  G01N2035/00198 ,  G01N33/15

    Abstract: A diffusion cell for use in determining the absorption rate of a study substance through a permeable membrane. The cell includes a receptor chamber which contains receptor fluid to receive study substance absorbed through the membrane. The receptor chamber includes a fluid inlet and a fluid outlet. A rotary stirrer is situated adjacent the fluid outlet. The stirrer is rotated so as to rotate the receptor fluid in the receptor chamber in such manner that the fluid pressure is greater at the outlet than at the inlet, so that the stirrer defines a pump which pumps receptor fluid outwardly through the outlet, then through a detector, and then back into the receptor chamber through the inlet. The detector determines the concentration of study substance within the receptor fluid.

    Abstract translation: 用于通过可渗透膜测定研究物质的吸收速率的扩散池。 细胞包括受体腔室，其包含受体液体以接收通过膜吸收的研究物质。 受体室包括流体入口和流体出口。 旋转搅拌器位于流体出口附近。 旋转搅拌器以使接收器腔中的受体流体以这样的方式旋转，使得出口处的流体压力大于在入口处的流体压力，使得搅拌器限定泵，其将受体流体向外通过出口泵送，然后通过 检测器，然后通过入口回到受体室。 检测器确定研究物质在受体液体内的浓度。

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