公开(公告)号：US06201009B1

公开(公告)日：2001-03-13

申请号：US09430250

申请日：1999-10-29

申请人： Masahiro Ozaki ,  Miwako Hagiuda ,  Daiichi Watanabe

发明人： Masahiro Ozaki ,  Miwako Hagiuda ,  Daiichi Watanabe

IPC分类号： A61K31335

CPC分类号： A61K31/351 ,  A61K9/4858 ,  A61K47/14 ,  A61K47/22 ,  A61K47/26 ,  A61K47/44

摘要： A composition showing an improved bioavailability rate of pantothenic acid derivatives represented by the following general formula and improved storage stability and being applicable as drugs over an enlarged range: wherein R1 and R2 are the same or different and each represents a hydrogen atom or a hydroxyl-protective group; R3 represents a saturated or unsaturated, linear, branched or cyclic C5-25 monovalent aliphatic hydrocarbon group optionally substituted by an aromatic group, or an amino group represented by the formula —N(R4)R5 (wherein R4 represents a saturated or unsaturated, linear, branched or cyclic C5-25 monovalent aliphatic hydrocarbon group; and R5 represents a hydrogen atom or a saturated or unsaturated, linear, branched or cyclic monovalent aliphatic hydrocarbon group optionally substituted by an aromatic group); A represents a saturated or unsaturated, linear, branched or cyclic C2-16 divalent aliphatic hydrocarbon group, divalent aromatic hydrocarbon group or divalent heteroaryl group optionally substituted by an aromatic group; one of X and Y represents an amino group represented by the formula —N(R6)— while the other represents —O—, —S— or an amino group represented by the formula —N(R7)— (wherein R6 and R7 represent each a hydrogen atom or a lower alkyl group); and n is an integer of from 1 to 4. The pantothenic acid derivative represented by the above general formula (I) is dissolved in a neutral or alcoholic ester and a nonionic surfactant is added thereto to give the absorption-enhancing composition.

摘要翻译： 一种组合物，其显示由以下通式表示的泛酸衍生物的改善的生物利用度和改进的储存稳定性，并且可用作扩大范围的药物：其中R1和R2相同或不同，并且各自表示氢原子或羟基保护 基团; R3表示任选被芳基取代的饱和或不饱和的直链，支链或环状的C5-25一价脂族烃基，或由式-N（R4）R5表示的氨基（其中R4表示饱和或不饱和的 直链，支链或环状的C5-25一价脂族烃基; R5表示氢原子或任选被芳基取代的饱和或不饱和的直链，支链或环状的一价脂族烃基; A表示饱和或不饱和的， 直链，支链或环状C2-16二价脂族烃基，二价芳族烃基或二价h 任选被芳基取代的芳基; X和Y之一表示由式-N（R6）表示的氨基，而另一个表示-O-，-S-或由式-N（ R7） - （其中R6和R7各自表示氢原子或低级烷基）; 和n为1〜4的整数。将由上述通式（I）表示的泛酸衍生物溶于中性或醇类的酯中，加入非离子表面活性剂，得到吸收促进组合物。

公开(公告)号：US5663322A

公开(公告)日：1997-09-02

申请号：US582735

申请日：1996-01-04

申请人： Tatsuo Katayama ,  Yoshihiro Nishikawa ,  Mayumi Hayashi ,  Hiroshi Nakajima ,  Masahiro Ozaki ,  Daiichi Watanabe

发明人： Tatsuo Katayama ,  Yoshihiro Nishikawa ,  Mayumi Hayashi ,  Hiroshi Nakajima ,  Masahiro Ozaki ,  Daiichi Watanabe

IPC分类号： C12P19/36 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7076 ,  A61K31/7084 ,  A61P3/00 ,  A61P7/02 ,  A61P43/00 ,  C07H19/20 ,  C07H19/207 ,  C07H21/02

CPC分类号： C07H21/02

摘要： The present invention is directed to diadenosine tetraphosphate (AP4A) tetrasodium salt dodecahydrate crystals represented by the following structure: ##STR1## Compared with the conventional amorphous anhydride of AP4A tetrasodium salt, the AP4A tetrasodium salt dodecahydrate crystals of the present invention have a low hygroscopicity and very stable physical properties. During storage, they are scarcely affected by environmental humidity. Thus, the present crystals can be easily handled as a medicine or a starting material for preparing a medicine, which broadens their application range.

摘要翻译： 本发明涉及由以下结构表示的二钠腺苷四磷酸四钠盐十二水合物晶体：AP4A四钠盐，本发明的AP4A四钠盐十二水合物晶体具有低吸湿性和非常稳定的物理性能。 储存期间几乎不受环境湿度的影响。 因此，本发明的晶体可以容易地作为药物或用于制备药物的起始材料处理，这扩大了其应用范围。