JPH03169818A - Inhibitor of blood platelet agglutination containing 1alpha-hydroxyvitamin d3 compounds - Google Patents
Inhibitor of blood platelet agglutination containing 1alpha-hydroxyvitamin d3 compoundsInfo
- Publication number
- JPH03169818A JPH03169818A JP24470790A JP24470790A JPH03169818A JP H03169818 A JPH03169818 A JP H03169818A JP 24470790 A JP24470790 A JP 24470790A JP 24470790 A JP24470790 A JP 24470790A JP H03169818 A JPH03169818 A JP H03169818A
- Authority
- JP
- Japan
- Prior art keywords
- hydroxyvitamin
- 1alpha
- inhibitor
- blood platelet
- compounds
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- OFHCOWSQAMBJIW-AVJTYSNKSA-N alfacalcidol Chemical class C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C\C=C1\C[C@@H](O)C[C@H](O)C1=C OFHCOWSQAMBJIW-AVJTYSNKSA-N 0.000 title claims abstract description 10
- 210000001772 blood platelet Anatomy 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 230000004520 agglutination Effects 0.000 title 1
- 230000000702 anti-platelet effect Effects 0.000 claims description 7
- 239000003146 anticoagulant agent Substances 0.000 claims description 7
- 238000004220 aggregation Methods 0.000 claims description 6
- 230000002776 aggregation Effects 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract description 13
- 235000019441 ethanol Nutrition 0.000 abstract description 5
- 239000000126 substance Substances 0.000 abstract description 5
- 239000000243 solution Substances 0.000 abstract description 4
- 239000004480 active ingredient Substances 0.000 abstract description 3
- 239000000203 mixture Substances 0.000 abstract description 3
- 239000007864 aqueous solution Substances 0.000 abstract description 2
- 239000007900 aqueous suspension Substances 0.000 abstract description 2
- 239000007891 compressed tablet Substances 0.000 abstract description 2
- 239000007902 hard capsule Substances 0.000 abstract description 2
- 239000007905 soft elastic gelatin capsule Substances 0.000 abstract description 2
- 239000002511 suppository base Substances 0.000 abstract description 2
- 239000003826 tablet Substances 0.000 abstract description 2
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 abstract description 2
- 244000299461 Theobroma cacao Species 0.000 abstract 1
- 235000005764 Theobroma cacao ssp. cacao Nutrition 0.000 abstract 1
- 235000005767 Theobroma cacao ssp. sphaerocarpum Nutrition 0.000 abstract 1
- 235000014121 butter Nutrition 0.000 abstract 1
- 235000001046 cacaotero Nutrition 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 210000000664 rectum Anatomy 0.000 abstract 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 4
- GMRQFYUYWCNGIN-NKMMMXOESA-N calcitriol Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@@H](CCCC(C)(C)O)C)=C\C=C1\C[C@@H](O)C[C@H](O)C1=C GMRQFYUYWCNGIN-NKMMMXOESA-N 0.000 description 3
- 239000002775 capsule Substances 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 239000007901 soft capsule Substances 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- 206010050661 Platelet aggregation inhibition Diseases 0.000 description 2
- QYSXJUFSXHHAJI-XFEUOLMDSA-N Vitamin D3 Natural products C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C/C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-XFEUOLMDSA-N 0.000 description 2
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 description 2
- 230000004071 biological effect Effects 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 239000003240 coconut oil Substances 0.000 description 2
- 235000019864 coconut oil Nutrition 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- 210000004623 platelet-rich plasma Anatomy 0.000 description 2
- 229930003231 vitamin Natural products 0.000 description 2
- 229940088594 vitamin Drugs 0.000 description 2
- 239000011782 vitamin Substances 0.000 description 2
- 235000013343 vitamin Nutrition 0.000 description 2
- QFMZQPDHXULLKC-UHFFFAOYSA-N 1,2-bis(diphenylphosphino)ethane Chemical compound C=1C=CC=CC=1P(C=1C=CC=CC=1)CCP(C=1C=CC=CC=1)C1=CC=CC=C1 QFMZQPDHXULLKC-UHFFFAOYSA-N 0.000 description 1
- 241000251468 Actinopterygii Species 0.000 description 1
- 206010061728 Bone lesion Diseases 0.000 description 1
- 206010006002 Bone pain Diseases 0.000 description 1
- 239000002126 C01EB10 - Adenosine Substances 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 208000013038 Hypocalcemia Diseases 0.000 description 1
- 208000000038 Hypoparathyroidism Diseases 0.000 description 1
- 235000019483 Peanut oil Nutrition 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- 208000003217 Tetany Diseases 0.000 description 1
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 1
- 229930003316 Vitamin D Natural products 0.000 description 1
- 201000006035 X-linked dominant hypophosphatemic rickets Diseases 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 229960005305 adenosine Drugs 0.000 description 1
- 229960005084 calcitriol Drugs 0.000 description 1
- 238000005119 centrifugation Methods 0.000 description 1
- 208000020832 chronic kidney disease Diseases 0.000 description 1
- 208000022831 chronic renal failure syndrome Diseases 0.000 description 1
- 229940110456 cocoa butter Drugs 0.000 description 1
- 235000019868 cocoa butter Nutrition 0.000 description 1
- 235000005687 corn oil Nutrition 0.000 description 1
- 239000002285 corn oil Substances 0.000 description 1
- 235000012343 cottonseed oil Nutrition 0.000 description 1
- 239000002385 cottonseed oil Substances 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 229960001617 ethyl hydroxybenzoate Drugs 0.000 description 1
- 235000010228 ethyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004403 ethyl p-hydroxybenzoate Substances 0.000 description 1
- NUVBSKCKDOMJSU-UHFFFAOYSA-N ethylparaben Chemical compound CCOC(=O)C1=CC=C(O)C=C1 NUVBSKCKDOMJSU-UHFFFAOYSA-N 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 235000019688 fish Nutrition 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 230000000705 hypocalcaemia Effects 0.000 description 1
- 208000011111 hypophosphatemic rickets Diseases 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 230000006371 metabolic abnormality Effects 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 235000019198 oils Nutrition 0.000 description 1
- 230000003287 optical effect Effects 0.000 description 1
- 208000005368 osteomalacia Diseases 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 229940068968 polysorbate 80 Drugs 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 235000010215 titanium dioxide Nutrition 0.000 description 1
- 238000000101 transmission high energy electron diffraction Methods 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- 208000032349 type 2B vitamin D-dependent rickets Diseases 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 235000019166 vitamin D Nutrition 0.000 description 1
- 239000011710 vitamin D Substances 0.000 description 1
- 150000003710 vitamin D derivatives Chemical class 0.000 description 1
- 235000005282 vitamin D3 Nutrition 0.000 description 1
- 239000011647 vitamin D3 Substances 0.000 description 1
- QYSXJUFSXHHAJI-YRZJJWOYSA-N vitamin D3 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C\C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-YRZJJWOYSA-N 0.000 description 1
- 229940046008 vitamin d Drugs 0.000 description 1
- 229940021056 vitamin d3 Drugs 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
本発明は、１α−ヒドロキシビタミンＤ３類を含有する
抗血小板凝集剤に関する。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an antiplatelet aggregation agent containing 1α-hydroxyvitamin D3.
近年、デルカ（Ｄｅ Ｌｕｃａ ）等及びコディック（
Ｋｏｄｉｅｋ）等の一連の研究の結果、ビタミンＤ３の
生体内活性物質が１α，２５−ジヒドロキシビタミンＤ
３ （以下１α．２５− （ＯＨ） ２−Ｄ３と略称す
る）であり、また工α位の水酸基の存在がその生物活性
の発現には必須であることが明らかにされた。以後この
活性型の１α， ２５−（Ｏ Ｈ ）２−Ｄ ３の類似
体、例えば１α−ヒドロキシビタミンＤ３（以下１α−
（ＯＨ）−Ｄ３と略称する）、１α．２４−ジヒドロキ
シビタミンＤ３ （以下ｌα，２４一（ Ｏ Ｈ） ２
Ｄ ３と略称する）など多くの１α一ヒドロキシビ
タミンＤ３類が合成され、工α，２５（ Ｏ Ｈ ）
２ Ｄ ａとともにそのビタミンＤ様生物活性が注目
されており、１α−（ＯＨ）−Ｄ３は慢性腎不全、副甲
状腺機能低下症．ビタミンＤ抵抗性クル病・骨軟化症に
おけるビタミンＤ代謝異常を伴う諸症状（低カルシウム
血症，テタニ骨痛，骨病変等）の改善に適応されている
。In recent years, De Luca et al. and Kodic (
As a result of a series of studies by Kodiek et al., the in vivo active substance of vitamin D3 was found to be 1α,25-dihydroxyvitamin D.
3 (hereinafter abbreviated as 1α.25-(OH)2-D3), and the presence of a hydroxyl group at the α-position is essential for the expression of its biological activity. Hereinafter, analogs of this active form of 1α,25-(OH)2-D3, such as 1α-hydroxyvitamin D3 (hereinafter referred to as 1α-
(OH)-D3), 1α. 24-dihydroxyvitamin D3 (hereinafter referred to as lα, 24-(OH) 2
Many 1α-hydroxyvitamin D3s have been synthesized, such as α,25 (OH)
Along with 2D a, its vitamin D-like biological activity has attracted attention, and 1α-(OH)-D3 is associated with chronic renal failure, hypoparathyroidism. It is indicated for improving symptoms associated with vitamin D metabolic abnormalities (hypocalcemia, tetani bone pain, bone lesions, etc.) in vitamin D-resistant rickets and osteomalacia.
本発明者等は、その後鋭意研究を続けた結果、１α−ヒ
ドロキシビタミンＤ３類に後述の抗血小板凝集作用のあ
ることを見出し、本発明を完或した。As a result of continued intensive research, the present inventors discovered that 1α-hydroxyvitamin D3 has an antiplatelet aggregation effect as described below, and completed the present invention.
即ち本発明は、１α−ヒドロキシビタミンＤ３類の抗血
小板凝集剤に関する。That is, the present invention relates to antiplatelet aggregation agents of the 1α-hydroxyvitamin D3 class.
本発明において用いられる１α−ヒドロキシビタミンＤ
３類とは
１α−（ＯＨ）−Ｄ３，
１α，２５− （Ｏ｝Ｉ），，−Ｄ３，工α，２４Ｓ−
（ＯＲ） ２−Ｄ３，１α，２４Ｒ− （ＯＨ） ２
−Ｄ３，工α． ２４８． ２５− （ＯＨ） ３−Ｄ
３，ｌα，２４Ｒ．２５− （ＯＨ） ３−Ｄ３，ｌα
．２５３．２６− （ＯＨ） ３−Ｄ３，１α・２５Ｒ
・２６− （ＯＨ） ３−Ｄ３・ｌα，２５− （ＯＨ
） ２−２３−ＯＸＯ−Ｄ３．１ α，２５ （ Ｏ
Ｈ ） ２ ２４ ０ Ｘ Ｏ − Ｄ ３ ，
１α， ２５Ｓ． ２６ − （Ｏ｝Ｉ）３−２３
−ＯＸＯ−Ｄ３１ ａ， ２ＳＲ， ２６ − （
ＯＨ）３−２３−ＯＸＯ−Ｄ３ ，１ ａ， ２５Ｓ
− （Ｏ Ｈ）２−０３−２６．２３Ｓ − ｌｓ
ｃｊｏｎｅ ．１ ａ． ２５Ｒ − （Ｏｆ｛）
２ Ｄ３−２６．２３Ｓ−１ｘｃｌｏｎｅ ，１ ａ
一 （Ｏ Ｈ）−２４．２５．２６．２７ −ｔｅ
ｊｔｉａｃ’ｒ−２３−Ｃｏｏ｝Ｉ−Ｃ３
などが含まれる。1α-hydroxyvitamin D used in the present invention
Type 3 is 1α-(OH)-D3, 1α,25- (O}I),,-D3, engineering α, 24S-
(OR) 2-D3,1α,24R- (OH) 2
-D3, engineering α. 248. 25- (OH) 3-D
3, lα, 24R. 25- (OH) 3-D3,lα
．． 253.26- (OH) 3-D3,1α・25R
・26- (OH) 3-D3・lα,25- (OH
) 2-23-OXO-D3.1 α,25 (O
H) 2 24 0 X O - D 3,
1α, 25S. 26-(O}I)3-23
-OXO-D31 a, 2SR, 26 - (
OH)3-23-OXO-D3,1a,25S
-(OH)2-03-26.23S-ls
cjone. 1 a. 25R - (Of{)
2 D3-26.23S-1xclone, 1 a
1 (OH)-24.25.26.27 -te
jtiac'r-23-Coo}I-C3 and the like.
これらの本物質は例えばＵ．Ｓ．Ｐａｌｅｎｌ ３６９
７５５９ ．特開昭５１−７６２５２．特開昭５１−７
６２５４， Ｕ．Ｓ．Ｐｓｌｅｎｌ３７４１９９６
，特開昭５５−２２６５５．特開昭５５−２２６５６，
特開昭５ｆｉ−６Ｈ５１， Ａｒｃｈ．Ｂｉｏｃｂｅ
ｍ，Ｂｉｏｐｈ７ｔ．， ２０４３８７ （１９８１
）， Ｈ． Ｆ． Ｄｅ ｌ，ａｃｔ， ビタミ：
／Ｄ − ［その新しい流れ］，講談社，サイエンティ
フィク（１９Ｂ２）などに開示されている。These substances include, for example, U. S. Palenl 369
7559. Japanese Patent Publication No. 51-76252. Japanese Patent Publication No. 51-7
6254, U. S. Pslenl3741996
, Japanese Patent Publication No. 55-22655. Japanese Patent Publication No. 55-22656,
JP-A-5FI-6H51, Arch. Biocbe
m, Bioph7t. , 204387 (1981
), H. F. De l, act, vitamins:
/D - Disclosed in [The New Flow], Kodansha, Scientific (19B2), etc.
本発明においては光学異性体のいずれを用いてもよく、
又、二種以上を混合して用いてもよい。In the present invention, any of the optical isomers may be used,
Also, two or more types may be used in combination.
本発明の抗血小板凝集剤は活性成分として上記本物質を
含有して、下記に示す種々の製剤形態にて用いられる。The antiplatelet aggregation agent of the present invention contains the above-mentioned present substance as an active ingredient and is used in various formulations shown below.
本発明の抗血小板凝集剤は、経口的、非経口的に投与さ
れる。The antiplatelet aggregation agent of the present invention is administered orally or parenterally.
投与形態としては例えば、圧縮錠剤、被覆錠剤，硬又は
軟弾性ゼラチンカプセル，エチルアルコール溶液，油性
または水性溶液または懸濁液などが用いられる。Examples of dosage forms that can be used include compressed tablets, coated tablets, hard or soft elastic gelatin capsules, ethyl alcohol solutions, oily or aqueous solutions or suspensions.
油性溶液の溶媒としては、植物油例えばヤシ油，トウモ
ロコシ油，綿実油．ココナッツ油，落花生油，魚肝油．
油状エステル例えばポリソルベート８０などを使用する
ことができる。Vegetable oils such as coconut oil, corn oil, cottonseed oil are suitable as solvents for oily solutions. Coconut oil, peanut oil, fish liver oil.
Oily esters such as polysorbate 80 can be used.
直腸内投与の場合には坐剤ベース例えばカカオ脂または
そのトリグリセライドなどを含む薬用組成物とすること
ができる。For rectal administration, the pharmaceutical composition may include a suppository base, such as cocoa butter or its triglycerides.
本物質は単位投与形態中、２Ｘ １Ｇ’乃至ＩＸ １Ｇ
％、好ましくは ２Ｘ１０’乃至１％を含有する。The substance may be present in unit dosage form from 2X 1G' to IX 1G'
%, preferably 2X10' to 1%.
又、投与量はｆｌ．Ｉ乃至１０’ ＩＩＩ／日／人、好
ましくは ０．５乃至１０３ＩＩＩｌ日／人とすること
ができる。Also, the dosage is fl. It can be from 1 to 10' day/person, preferably from 0.5 to 103 day/person.
そして、上記量的関係が保持されるように、１日ｌ〜３
回の投与回数となるように調製される。Then, so that the above quantitative relationship is maintained, 1 to 3
It is prepared so that the number of administrations is 1.
以下、実施例により本発明を詳述する。Hereinafter, the present invention will be explained in detail with reference to Examples.
実施例１
抗血小板凝集作用
２０週齢正常ウィスタ一系雄ラットよりチトラート採血
（チトラートは全血液の １７ｌＯ量）を行ない、これ
を１． ５００ｔｐｍで６分間遠心分離し、その上澄か
ら多血小板血漿（Ｐｌａｌｅｌｅｊ Ｒｉｃｈ Ｐｌｔ
ｓｍａ ；以下、ＰＲＰと略す）を得た。これを用いて
ｉｎｙｉｔｒｏでＡｄｅｎｏｓｉｎｅ Ｄｉｐｈｏｓ
ｐｈＮｅ （以下ＳＡＤＰと略す）惹起血小板凝集に対
するｌα−ヒドロキシビタミンＤ３類の効果を検討した
。Example 1 Anti-platelet aggregation effect Chitrate blood was collected from 20-week-old normal Wista strain male rats (titrate amount was 17 lO of whole blood). Centrifugation was performed at 500 tpm for 6 minutes, and platelet-rich plasma (Platelet rich plasma) was extracted from the supernatant.
sma; hereinafter abbreviated as PRP) was obtained. Adenosine Diphos in vitro using this
The effect of lα-hydroxyvitamin D3 on phNe (hereinafter abbreviated as SADP)-induced platelet aggregation was investigated.
ｌα−ヒドロキシビタミンＤ３類のエタノール溶液を
ｔ．ｓＪｌ１とり、ＰＲＰ２ＳＯｍｌ中に添加し、２分
間３７℃にてインキュベート後、ＡＤＰを３０μＭ入れ
、血小板凝集測定に供した。このときのｌα一ヒドロキ
シビタミンＤ３類の最終濃度は０． １２／Ｉｇ／ｍｌ
（［１．６％エタノールＰＲＰ）となる。対照には、１
．５ｄのエタノールを用いた。尚、血小板凝集測定には
、ＰｇＹｔｏｎ Ｌｕｍ：Ｈｇｔｅｇｇｌｉｏｎ Ｍｏ
ｄｕｌｅＭｏｄｅｌ １００Ｇを用いた。An ethanol solution of lα-hydroxyvitamin D3
t. sJl1 was taken, added to PRP2SOml, and incubated at 37°C for 2 minutes, then 30 μM of ADP was added and subjected to platelet aggregation measurement. The final concentration of lα-hydroxyvitamin D3 at this time was 0. 12/Ig/ml
([1.6% ethanol PRP). For control, 1
．． 5d ethanol was used. In addition, for platelet aggregation measurement, PgYton Lum: Hgtegglion Mo
duleModel 100G was used.
対照に対する血小板凝集阻害率を下記式より求めた。The platelet aggregation inhibition rate relative to the control was determined from the following formula.
血小板凝集阻害率は、
１α−（ＯＨ）−Ｄ３・・・・・・・・・１３％，１α
，２５− （ＯＨ） ２−Ｄ３・・・・・・１５％，１
α，２４Ｒ− （ＯＨ） ２−Ｄ３・・・・・・１３％
であった。Platelet aggregation inhibition rate is 1α-(OH)-D3...13%, 1α
,25-(OH)2-D3...15%,1
α,24R- (OH) 2-D3...13%
Met.
実施例２
工α一（ＯＨ） 一Ｄ３をパナセート ８００（日本浦
脂製．中級脂肪酸のトリグリセライド）にｌＯ屠／ｍｌ
の濃度に溶解し、エカプセル中に工α（ＯＨ）−０３を
１埒含有するように下記剤皮或分を加温溶解し、軟カプ
セル製造機を用いて常法により軟カプセル剤を作或した
。Example 2 Technique α-1 (OH)-D3 was added to Panacet 800 (manufactured by Nihon Urashi. Triglyceride of intermediate fatty acids) to 10/ml.
A portion of the following agent was heated and dissolved so that each capsule contained 1 gram of α(OH)-03, and soft capsules were made using a soft capsule making machine in a conventional manner. did.
剤皮処方例
ゼラチン ｌＯ重量部グリセリン
２重量部防腐剤（エチルバラベン）
０、０５重量部チタンホワイト ０
．２重量部水 ０．２重量部
（最終形態に於ける重量部）
実施例３
実施例２の工α−（ＯＨ）−Ｄ３に代えて、ｌα．２５
− （ＯＨ） ２−Ｄ３を用い、以下同様にしてｌα，
２５− （ＯＨ） ２−Ｄ３を１カプセル当り１埒を含
有する軟カプセル剤を得た。Shell formulation example Gelatin 10 parts by weight Glycerin
2 parts by weight preservative (ethylparaben)
0.05 parts by weight titanium white 0
．． 2 parts by weight Water 0.2 parts by weight (parts by weight in final form) Example 3 In place of α-(OH)-D3 in Example 2, lα. 25
- Using (OH) 2-D3, lα,
Soft capsules containing 1 g of 25-(OH)2-D3 per capsule were obtained.
実施例４
実施例２のｌα−（ＯＨ）−Ｄ３に代えて、１α，２４
Ｒ− （ＯＨ） ２−Ｄ３を用い、以下同様にして１α
，２４Ｒ− （ＯＨ） ２−Ｄ３をｌカブセル当り１屠
を含有する軟カプセル剤を得た。Example 4 In place of lα-(OH)-D3 in Example 2, 1α,24
Using R- (OH) 2-D3, 1α in the same manner
, 24R- (OH) 2-D3 was obtained per capsule.
Claims (1)
とを特徴とする抗血小板凝集剤。(1) An antiplatelet aggregation agent characterized by containing 1α-hydroxyvitamin D_3.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP24470790A JPH03169818A (en) | 1983-08-02 | 1990-09-14 | Inhibitor of blood platelet agglutination containing 1alpha-hydroxyvitamin d3 compounds |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP14132383A JPS6045516A (en) | 1983-08-02 | 1983-08-02 | Physiologically active agent containing 1alpha- hydroxyvitamin d3 |
| JP24470790A JPH03169818A (en) | 1983-08-02 | 1990-09-14 | Inhibitor of blood platelet agglutination containing 1alpha-hydroxyvitamin d3 compounds |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP14132383A Division JPS6045516A (en) | 1983-08-02 | 1983-08-02 | Physiologically active agent containing 1alpha- hydroxyvitamin d3 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH03169818A true JPH03169818A (en) | 1991-07-23 |
| JPH054367B2 JPH054367B2 (en) | 1993-01-19 |
Family
ID=26473578
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP24470790A Granted JPH03169818A (en) | 1983-08-02 | 1990-09-14 | Inhibitor of blood platelet agglutination containing 1alpha-hydroxyvitamin d3 compounds |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH03169818A (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6045516A (en) * | 1983-08-02 | 1985-03-12 | Kureha Chem Ind Co Ltd | Physiologically active agent containing 1alpha- hydroxyvitamin d3 |
-
1990
- 1990-09-14 JP JP24470790A patent/JPH03169818A/en active Granted
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6045516A (en) * | 1983-08-02 | 1985-03-12 | Kureha Chem Ind Co Ltd | Physiologically active agent containing 1alpha- hydroxyvitamin d3 |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH054367B2 (en) | 1993-01-19 |
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