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    Method of increasing oral absorption of glycosidic and related antibiotics
    41.
    发明授权
    Method of increasing oral absorption of glycosidic and related antibiotics 失效
    增加糖苷及相关抗生素口服吸收的方法

    公开(公告)号：US4459295A

    公开(公告)日：1984-07-10

    申请号：US387409

    申请日：1982-06-11

    Applicant: Takeru Higuchi ,  Toshiaki Nishihata

    Inventor： Takeru Higuchi ,  Toshiaki Nishihata

    IPC: A61K9/20 ,  A61K9/28 ,  A61K9/48 ,  A61K45/06 ,  A61K47/12 ,  A61K47/14 ,  A61K47/18 ,  A61K31/71

    CPC classification number: A61K31/70 ,  A61K45/06 ,  A61K47/12 ,  A61K47/14 ,  A61K47/18 ,  A61K9/2013 ,  A61K9/4858 ,  A61K9/2866 ,  A61K9/2886 ,  A61K9/4891

    Abstract: A method and drug form are provided for increasing the oral absorption of glycosidic and related antibiotics such as macrolide, aminoglycoside, lincomycin and anthracycline antibiotics and related chemical species by the oral administration of said glycosidic and related antibiotics in a suitable pharmaceutically accepted excipient to which has been added a hydroxyaryl or hydroxyaralkyl acid or salt thereof. The hydroxyaryl or hydroxyaralkyl acid or salt thereof is present in the drug form in quantities sufficient to be effective in enhancing the rate of oral absorption of glycosidic and related antibiotic.

    Abstract translation: 提供了一种方法和药物形式，用于通过在合适的药学上可接受的赋形剂中口服所述糖苷和相关抗生素来增加糖苷类和相关抗生素如大环内酯类，氨基糖苷类，林可霉素和蒽环类抗生素及相关化学物质的口服吸收， 加入羟基芳基或羟基烷基酸或其盐。 羟基芳基或羟基烷基酸或其盐以足以有效提高糖苷和相关抗生素的口服吸收速率的药物形式存在。

    Stable pro-drug forms of theophylline
    45.
    发明授权
    Stable pro-drug forms of theophylline 失效
    稳定的前药形式的茶碱

    公开(公告)号：US4085214A

    公开(公告)日：1978-04-18

    申请号：US732979

    申请日：1976-10-18

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

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

    IPC: C07D473/08 ,  A61K31/52

    CPC classification number: C07D473/08

    Abstract: There is provided exceptionally stable and useful pro-drug forms of theophylline having the formula: ##STR1## wherein R represents a straight or branched phenylalkenyl group having 2-8 carbon atoms in the alkenyl portion.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: 提供特别稳定和有用的具有下式的茶碱的前药形式：其中R表示烯基部分中具有2-8个碳原子的直链或支链苯基烯基。

    Novel pro-drug derivatives of pyridinium aldoxime type cholinesterase reactivators and method of using same
    48.
    发明授权
    Novel pro-drug derivatives of pyridinium aldoxime type cholinesterase reactivators and method of using same 失效
    吡啶鎓醛缩酶类胆碱酯酶激活剂的新型前药衍生物及其使用方法

    公开(公告)号：US3962447A

    公开(公告)日：1976-06-08

    申请号：US603612

    申请日：1975-08-11

    Applicant: Takeru Higuchi ,  Nicolae S. Bodor ,  Efraim Shek

    Inventor： Takeru Higuchi ,  Nicolae S. Bodor ,  Efraim Shek

    IPC: C07D211/82 ,  A61K31/44

    CPC classification number: C07D211/82

    Abstract: There is provided, novel pro-drug forms of pyridinium aldoxime type cholinesterase reactivators, namely, dihydropyridinium aldoximes, having the formula: ##SPC1##Wherein R represents a member selected from the group consisting of an alkyl (C.sub.1 -C.sub.4) group, a ##SPC2##Group, a ##SPC3##Group, ##SPC4##Group, and a ##SPC5##Wherein Z represents a member selected from the group consisting of a --CH.sub.2 --CH.sub.2 -- group, a --CH.sub.2 --O--CH.sub.2 -- group, a --CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 -- group, and a --CH.sub.2 O--CH.sub.2 --CH.sub.2 --O--CH.sub.2 -- group; wherein R.sub.1 represents a member selected from the group consisting of a hydrogen atom, a methyl group, an acyl group and a ##EQU1## group; and wherein X.sup.- represents an anion derived from a pharmaceutically acceptable acid addition salt.These compounds are useful in reactivating cholinesterase, inhibited following exposure to and/or ingestion of conventional anti-cholinesterase agents, especially in the brain.

    Abstract translation: 提供了吡啶鎓醛肟型胆碱酯酶再活化剂的新型前药形式，即二氢吡啶鎓醛肟，具有下式：

    Administration of alkali metal salicylamide salts
    50.
    发明授权
    Administration of alkali metal salicylamide salts 失效
    施用碱金属水杨酰胺盐

    公开(公告)号：US3950521A

    公开(公告)日：1976-04-13

    申请号：US580134

    申请日：1975-05-23

    Applicant: Takeru Higuchi ,  Anwar Hussain

    Inventor： Takeru Higuchi ,  Anwar Hussain

    IPC: A61K31/60 ,  A61K31/615

    CPC classification number: A61K31/621 ,  A61K31/60

    Abstract: Alkali and 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，水杨酰胺的碱金属盐和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。

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