JPH0443887B2 - - Google Patents
Info
- Publication number
- JPH0443887B2 JPH0443887B2 JP29154286A JP29154286A JPH0443887B2 JP H0443887 B2 JPH0443887 B2 JP H0443887B2 JP 29154286 A JP29154286 A JP 29154286A JP 29154286 A JP29154286 A JP 29154286A JP H0443887 B2 JPH0443887 B2 JP H0443887B2
- Authority
- JP
- Japan
- Prior art keywords
- dihydroxyvitamin
- cataracts
- vitamin
- cataract
- crystalline lens
- 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.)
- Expired
Links
- 208000002177 Cataract Diseases 0.000 claims description 18
- 229930003316 Vitamin D Natural products 0.000 claims description 9
- 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 claims description 9
- 235000019166 vitamin D Nutrition 0.000 claims description 9
- 239000011710 vitamin D Substances 0.000 claims description 9
- 150000003710 vitamin D derivatives Chemical class 0.000 claims description 9
- 229940046008 vitamin d Drugs 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 5
- 229940124597 therapeutic agent Drugs 0.000 claims description 5
- 239000004480 active ingredient Substances 0.000 claims description 4
- OFHCOWSQAMBJIW-AVJTYSNKSA-N alfacalcidol 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)C[C@H](O)C1=C OFHCOWSQAMBJIW-AVJTYSNKSA-N 0.000 claims description 3
- FCKJYANJHNLEEP-OIMXRAFZSA-N 24,25-Dihydroxyvitamin D Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@@H](CCC(O)C(C)(C)O)C)=C\C=C1\C[C@H](O)CCC1=C FCKJYANJHNLEEP-OIMXRAFZSA-N 0.000 claims description 2
- 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 claims description 2
- 210000000695 crystalline len Anatomy 0.000 description 15
- 239000011575 calcium Substances 0.000 description 8
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 7
- 229910052791 calcium Inorganic materials 0.000 description 7
- 238000011282 treatment Methods 0.000 description 6
- 230000005856 abnormality Effects 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 241000700159 Rattus Species 0.000 description 2
- 230000003913 calcium metabolism Effects 0.000 description 2
- 230000007423 decrease Effects 0.000 description 2
- 230000037213 diet Effects 0.000 description 2
- 235000005911 diet Nutrition 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 238000002651 drug therapy Methods 0.000 description 2
- 239000003889 eye drop Substances 0.000 description 2
- 229940012356 eye drops Drugs 0.000 description 2
- RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 229930003231 vitamin Natural products 0.000 description 2
- 239000011782 vitamin Substances 0.000 description 2
- 235000013343 vitamin Nutrition 0.000 description 2
- 229940088594 vitamin Drugs 0.000 description 2
- 150000003722 vitamin derivatives Chemical class 0.000 description 2
- 208000006386 Bone Resorption Diseases 0.000 description 1
- 206010006956 Calcium deficiency Diseases 0.000 description 1
- 229920000818 Catalin Polymers 0.000 description 1
- 206010007747 Cataract congenital Diseases 0.000 description 1
- 206010007749 Cataract diabetic Diseases 0.000 description 1
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 description 1
- 108010024636 Glutathione Proteins 0.000 description 1
- OKPNYGAWTYOBFZ-UHFFFAOYSA-N Pirenoxine Chemical compound C12=NC3=CC=CC=C3OC2=CC(=O)C2=C1C(=O)C=C(C(=O)O)N2 OKPNYGAWTYOBFZ-UHFFFAOYSA-N 0.000 description 1
- 229930003268 Vitamin C Natural products 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 210000000988 bone and bone Anatomy 0.000 description 1
- 230000024279 bone resorption Effects 0.000 description 1
- 208000022458 calcium metabolism disease Diseases 0.000 description 1
- XFQYJNINHLZMIU-UHFFFAOYSA-N cataline Natural products CN1CC(O)C2=CC(OC)=C(OC)C3=C2C1CC1=C3C=C(OC)C(OC)=C1 XFQYJNINHLZMIU-UHFFFAOYSA-N 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 201000007025 diabetic cataract Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 208000030533 eye disease Diseases 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 210000004907 gland Anatomy 0.000 description 1
- 229960003180 glutathione Drugs 0.000 description 1
- 239000007902 hard capsule Substances 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- SQEHCNOBYLQFTG-UHFFFAOYSA-M lithium;thiophene-2-carboxylate Chemical compound [Li+].[O-]C(=O)C1=CC=CS1 SQEHCNOBYLQFTG-UHFFFAOYSA-M 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 208000030212 nutrition disease Diseases 0.000 description 1
- 230000011164 ossification Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 230000000079 pharmacotherapeutic effect Effects 0.000 description 1
- NLKNQRATVPKPDG-UHFFFAOYSA-M potassium iodide Chemical compound [K+].[I-] NLKNQRATVPKPDG-UHFFFAOYSA-M 0.000 description 1
- 210000001747 pupil Anatomy 0.000 description 1
- 201000008525 senile cataract Diseases 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000004304 visual acuity Effects 0.000 description 1
- 230000000007 visual effect Effects 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
本発明は、白内障の治療剤に関するものであ
る。白内障は一般に「しろそこひ」といわれる眼
疾患で瞳孔からのぞける水晶体が白く混濁してみ
えることから、その名前がついている。水晶体が
混濁しその透明度が低下するので眼底にまで達す
ることのできる光量が低下し、その結果、必然的
に視力が低下するという症状になつて現われる。
白内障の種類としては先天性白内障、老人性白
内障、併発白内障、糖尿病性白内症等があり、そ
の成因は複雑であるが、生化学的には混濁した水
晶体では、そのカルシウム含量が異常であるとい
う現象がある。
そしてかかる白内障の治療法としては現在のと
ころ、手術的療法が主体であり、補助的に薬物療
法が行われている。薬物療法としはカタリン、グ
ルタチオンの点眼、睡液腺ホルモンの注射、ヨー
ドカリやビタミンＣ等の投与が行われており、白
内障の進行を遅らせるのにある程度有効であると
いわれている。しかし混濁化した水晶体を透明化
する、即ち、白内障を根本的に治療することは、
従来の薬物療法では不可能である。
ところで前述のごとく、白内障においては水晶
体におけるカルシウム異常が多く見られるが、ま
た栄養障害特にカルシウムの欠乏が視覚異常を引
き起こすことも知られている。従つて白内障に
は、カルシウムの代謝異常ひいてはそれと関連の
深いビタミンＤの存在が何らかの影響を有するの
ではないかと推定される。
一方、1α−ヒドロキシビタミンＤ、1α、24−
ジヒドロキシビタミンＤ、1α、25−ジヒドロキ
シビタミンＤ等の活性型ビタミンＤ類は小腸でカ
ルシウムの吸収運搬を促進し、骨で骨吸収、骨形
成を調節するなどの作用を有し、種々のカルシウ
ム代謝異常に基づく疾患の治療薬として、ビタミ
ンＤ以上に有用であること、もとビタミンＤ代謝
異常に基づく疾患の治療において欠くべからざる
治療であることがよく知られている。
そこで本発明者等は、この活性型ビタミンＤが
白内障にどの様な影響を与えるかを検討してみた
ところ、驚くべきことに、非常に少量で活性型ビ
タミンＤは水晶体中のカルシウム含量のレベルを
正常化する作用、水晶体の混濁を改善する作用が
あることを知見し本発明に到達した。
即ち、本発明は活性型ビタミンＤを有効成分と
する白内障治療剤である。
本発明における活性化ビタミンＤとしては、例
えば1α−ヒドロキシビタミンＤ、1α、24−ジヒ
ドロキシビタミンＤ、1α、25−ジヒドロキシビ
タミンＤ、24、25−ジヒドロキシビタミンＤ、
1α、24、25−トリヒドロキシビタミンＤ、24、
24−F2−1α、25−ジヒドロキシビタミンＤ及び
26、26、26、27、27、27−F6−1α、25−ジヒド
ロキシビタミンＤがある。
これらの有効成分は公知の方法で適当な賦型剤
等を用いて軟カプセル剤、硬カプセル剤、錠剤、
シロツプ等の経口剤、注射剤、点眼剤等にして使
用できる。有効成分の投与量は通常0.01〜10μ
ｇ／日／人程度であり、投与回数は通常１〜３
回／日であり、この様な条件を満足するように製
剤を調製するのが好ましい。
本発明の方法は既存の薬物療法治療剤と併用す
ることも可能である。
以下、実施例を用いて本発明の方法を記述す
る。
実施例 １
４週令のSLC−WISTAR雄ラツト８匹を、カ
ルシウム含量0.09wt％のビタミン欠乏食
（TEKLAD社製）で78日間飼育し、白内障ラツ
トを作製した。SLITLAMPで水晶体を観察の
後、４匹（白内障群とする）を屠殺後、水晶体を
取り出して文献（木下他、日本眼科紀要28、1429
〜1433（1973））記載の方法で水晶体中のカルシウ
ム含量を測定した。残り４匹については同じ飼料
で更に99日間飼育しつつ、その間1α−（OH）
D30.050μｇ／体重Kg・日を経口投与した。（1α−
（OH）D3治療群とする）。水晶体をSLIT LAMP
で観察するとともに、屠殺後、水晶体をとり出し
カルシウム含量を測定した。各群の平均値を第１
表に示す。なお非白内障のコントロール群ではそ
の値は20〜27（μｇ）／水晶体湿重量（ｇ）であ
ることが別の実験で確かめられた。
The present invention relates to a therapeutic agent for cataract. Cataract is an eye disease commonly referred to as ``shirozokohi,'' which gets its name from the fact that the lens that looks through the pupil appears cloudy. As the crystalline lens becomes cloudy and its transparency decreases, the amount of light that can reach the fundus of the eye decreases, which inevitably results in a symptom of decreased visual acuity. Types of cataracts include congenital cataracts, senile cataracts, combined cataracts, and diabetic cataracts.The causes are complex, but from a biochemical perspective, the calcium content of a cloudy lens is abnormal. There is a phenomenon called. At present, the main treatment for cataracts is surgical therapy, with drug therapy being used as an adjunct. Medicinal treatments include eye drops of catalin and glutathione, injections of fluid gland hormones, and administration of iodopotassium and vitamin C, which are said to be somewhat effective in delaying the progression of cataracts. However, it is impossible to make the cloudy crystalline lens transparent, that is, to fundamentally treat cataracts.
This is not possible with conventional drug therapy. As mentioned above, calcium abnormalities in the crystalline lens are often seen in cataracts, and it is also known that nutritional disorders, particularly calcium deficiency, cause visual abnormalities. Therefore, it is presumed that abnormalities in calcium metabolism and the presence of vitamin D, which is closely related to this, have some influence on cataracts. On the other hand, 1α-hydroxyvitamin D, 1α, 24-
Active vitamin Ds such as dihydroxyvitamin D, 1α, and 25-dihydroxyvitamin D promote the absorption and transportation of calcium in the small intestine, regulate bone resorption and bone formation in the bones, and play a role in various calcium metabolism. It is well known that it is more useful than vitamin D as a therapeutic agent for diseases caused by abnormalities, and that it is an indispensable treatment for diseases originally caused by abnormalities of vitamin D metabolism. Therefore, the present inventors investigated how this active form of vitamin D affects cataracts, and surprisingly found that even in very small amounts, active form of vitamin D affects the level of calcium content in the crystalline lens. The present invention was achieved based on the discovery that the present invention has the effect of normalizing the lens and improving the opacity of the crystalline lens. That is, the present invention is a cataract therapeutic agent containing active vitamin D as an active ingredient. Examples of activated vitamin D in the present invention include 1α-hydroxyvitamin D, 1α,24-dihydroxyvitamin D, 1α,25-dihydroxyvitamin D, 24,25-dihydroxyvitamin D,
1α, 24, 25-trihydroxyvitamin D, 24,
24-F 2 -1α, 25-dihydroxyvitamin D and
There is 26, 26, 26, 27, 27, 27-F 6 -1α, 25-dihydroxyvitamin D. These active ingredients can be prepared into soft capsules, hard capsules, tablets, etc. using appropriate excipients by known methods.
It can be used as oral preparations such as syrup, injections, eye drops, etc. The dosage of active ingredient is usually 0.01-10μ
g/day/person, and the number of administrations is usually 1 to 3.
times/day, and it is preferable to prepare a preparation to satisfy such conditions. The methods of the invention can also be used in combination with existing pharmacotherapeutic treatments. The method of the present invention will be described below using examples. Example 1 Eight 4-week-old SLC-WISTAR male rats were fed a vitamin-deficient diet (manufactured by TEKLAD) with a calcium content of 0.09 wt% for 78 days to produce cataract rats. After observing the crystalline lens with SLITLAMP, we sacrificed 4 animals (assumed to be cataract group), and removed the crystalline lens.
The calcium content in the crystalline lens was measured by the method described in 1433 (1973). The remaining four animals were kept on the same diet for an additional 99 days, during which they were fed 1α-(OH).
D 3 was orally administered at 0.050 μg/kg body weight/day. (1α−
(OH)D 3 treatment group). SLIT LAMP
After sacrifice, the lens was removed and the calcium content was measured. The average value of each group is
Shown in the table. It was confirmed in another experiment that in the non-cataract control group, the value was 20 to 27 (μg)/wet weight of crystalline lens (g).
【表】
実施例 ２
実施例１において飼料の組成をカルシウム含量
0.18％とした以外は同じ条件で実験を行なつたと
ころ、実施例１と同様な1α−（OH）D3の治療効
果が判明した。
すなわち、治療後、水晶体のCa含量は26.3μ
ｇ／水晶体湿重量、白内障の程度は中等度より軽
度に改善された。[Table] Example 2 The composition of the feed in Example 1 was calculated based on the calcium content.
An experiment was conducted under the same conditions except that the concentration was 0.18%, and the same therapeutic effect of 1α-(OH)D 3 as in Example 1 was found. That is, after treatment, the Ca content of the crystalline lens is 26.3μ
g/wet weight of lens and the degree of cataract were improved to mild from moderate.
Claims (1)
療剤。 ２ 活性型ビタミンＤが1α−ヒドロキシビタミ
ンＤ、1α、24−ジヒドロキシビタミンＤ、1α、
25−ジヒドロキシビタミンＤ、24、25−ジヒドロ
キシビタミンＤ、1α、24、25−トリヒドロキシ
ビタミンＤ、24、24−F2−1α、25−ジヒドロキ
シビタミンＤ及び26、26、26、27、27、27−F6
−1α、25−ジヒドロキシビタミンＤからなる群
から選ばれたものである特許請求の範囲第１項記
載の白内障治療剤。[Claims] 1. A cataract therapeutic agent containing active vitamin D as an active ingredient. 2 Active vitamin D is 1α-hydroxyvitamin D, 1α, 24-dihydroxyvitamin D, 1α,
25-dihydroxyvitamin D, 24,25-dihydroxyvitamin D, 1α, 24, 25-trihydroxyvitamin D, 24, 24- F2-1α , 25-dihydroxyvitamin D and 26, 26, 26, 27, 27, 27−F 6
The therapeutic agent for cataract according to claim 1, which is selected from the group consisting of -1α,25-dihydroxyvitamin D.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP29154286A JPS63145233A (en) | 1986-12-09 | 1986-12-09 | Remedy for cataract |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP29154286A JPS63145233A (en) | 1986-12-09 | 1986-12-09 | Remedy for cataract |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS63145233A JPS63145233A (en) | 1988-06-17 |
| JPH0443887B2 true JPH0443887B2 (en) | 1992-07-20 |
Family
ID=17770254
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP29154286A Granted JPS63145233A (en) | 1986-12-09 | 1986-12-09 | Remedy for cataract |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS63145233A (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW422696B (en) * | 1995-03-20 | 2001-02-21 | Katsuhiko Mukai | Ophthalmic composition containing active vitamin D |
| US6162801A (en) * | 1995-11-20 | 2000-12-19 | Kita; Kiyoshi | External ophthalmic preparation containing vitamin D |
| AU2792997A (en) * | 1997-05-26 | 1998-12-30 | New Vision Co., Ltd. | Medicinal compositions for topical administration containing vitamin d and vitamin k |
| US6187331B1 (en) | 1997-06-10 | 2001-02-13 | New Vision Co., Ltd. | Composition for prophylaxis and/or treatment of dry syndrome comprising vitamin D |
-
1986
- 1986-12-09 JP JP29154286A patent/JPS63145233A/en active Granted
Also Published As
| Publication number | Publication date |
|---|---|
| JPS63145233A (en) | 1988-06-17 |
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