JPH03291224A - Drug having improved absorptiveness - Google Patents
Drug having improved absorptivenessInfo
- Publication number
- JPH03291224A JPH03291224A JP9270190A JP9270190A JPH03291224A JP H03291224 A JPH03291224 A JP H03291224A JP 9270190 A JP9270190 A JP 9270190A JP 9270190 A JP9270190 A JP 9270190A JP H03291224 A JPH03291224 A JP H03291224A
- Authority
- JP
- Japan
- Prior art keywords
- active ingredient
- group
- water soluble
- polymer material
- methyl
- 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.)
- Pending
Links
- 239000003814 drug Substances 0.000 title abstract description 3
- 229940079593 drug Drugs 0.000 title abstract description 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 5
- 150000003839 salts Chemical class 0.000 claims abstract 5
- 239000007787 solid Substances 0.000 claims abstract 5
- 125000001624 naphthyl group Chemical group 0.000 claims abstract 4
- 229920003169 water-soluble polymer Polymers 0.000 claims abstract 4
- 239000002202 Polyethylene glycol Substances 0.000 claims abstract 2
- 125000002947 alkylene group Chemical group 0.000 claims abstract 2
- 239000007788 liquid Substances 0.000 claims abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract 2
- 229920001223 polyethylene glycol Polymers 0.000 claims abstract 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims abstract 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims abstract 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims abstract 2
- 125000001424 substituent group Chemical group 0.000 claims abstract 2
- -1 {5-[2 Chemical class 0.000 claims abstract 2
- 239000004480 active ingredient Substances 0.000 claims 7
- 239000000126 substance Substances 0.000 claims 5
- 238000009472 formulation Methods 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 2
- QHCPEVCCVPNQHM-UHFFFAOYSA-N 2-benzyl-1,3-benzoxazole Chemical compound N=1C2=CC=CC=C2OC=1CC1=CC=CC=C1 QHCPEVCCVPNQHM-UHFFFAOYSA-N 0.000 claims 1
- FQCUYGFIIAZMLU-UHFFFAOYSA-N 5-[[2-(naphthalen-2-ylmethyl)-1,3-benzoxazol-5-yl]methyl]-1,3-thiazolidine-2,4-dione Chemical group S1C(=O)NC(=O)C1CC1=CC=C(OC(CC=2C=C3C=CC=CC3=CC=2)=N2)C2=C1 FQCUYGFIIAZMLU-UHFFFAOYSA-N 0.000 claims 1
- PWVLZXAJWLEGAR-UHFFFAOYSA-N 5-[[2-[(4-chlorophenyl)methyl]-1,3-benzoxazol-5-yl]methyl]-1,3-thiazolidine-2,4-dione Chemical group C1=CC(Cl)=CC=C1CC1=NC2=CC(CC3C(NC(=O)S3)=O)=CC=C2O1 PWVLZXAJWLEGAR-UHFFFAOYSA-N 0.000 claims 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract description 5
- 239000002861 polymer material Substances 0.000 abstract 4
- BCMCBBGGLRIHSE-UHFFFAOYSA-N 1,3-benzoxazole Chemical class C1=CC=C2OC=NC2=C1 BCMCBBGGLRIHSE-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 108010010803 Gelatin Proteins 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 230000001079 digestive effect Effects 0.000 abstract 1
- 229920000159 gelatin Polymers 0.000 abstract 1
- 239000008273 gelatin Substances 0.000 abstract 1
- 235000019322 gelatine Nutrition 0.000 abstract 1
- 235000011852 gelatine desserts Nutrition 0.000 abstract 1
- 229920000609 methyl cellulose Polymers 0.000 abstract 1
- 239000001923 methylcellulose Substances 0.000 abstract 1
- 235000010981 methylcellulose Nutrition 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
- 238000010521 absorption reaction Methods 0.000 description 2
- 229940127003 anti-diabetic drug Drugs 0.000 description 2
- 239000003472 antidiabetic agent Substances 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 229940126585 therapeutic drug Drugs 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
PURPOSE:To obtain the subject remedy for diabetes mellitus having an improved absorptiveness in the digestive tube by solid dispersing a benzoxazole derivative or its salt in a water soluble polymer material showing a solid state at the ordinary temperatures or by dissolving the above mentioned compound in a water soluble liquid polymer material. CONSTITUTION:A compound, e.g. {5-[2,4-dioxothiazolidin-5-yl) methyl]-2-[4-(dimethylamino)benzyl]benzoxazole} of the formula (R is phenyl or naphthyl which may have substituent; Alk is lower alkylene) or a pharmacologically allowable salt thereof is solid dispersed or dissolved in a water soluble polymer material to produce the objective drug for remedy of diabetes mellitus having an excellent absorptiveness. As the water soluble polymer material, polyethylene glycol, polyvinyl pyrrolidone, methylcellulose, gelatin, etc., are used and the amount thereof used is preferably 3-20 pts.wt. and 30-50 pts.wt. based on 1 pts.wt. active component respectively in case of a solid state and a solution.
Description
【発明の詳細な説明】
［産業上の利用分野］
本発明は、吸収性、特に経口投与時の吸収性が改善され
た糖尿病治療薬に関する。DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to a therapeutic drug for diabetes that has improved absorption, particularly absorption upon oral administration.
［従来技術と発明が解決すべき課題］
糖尿病治療薬の開発は、糖尿病患者の増加に伴い、ます
ます重要となり、様々な医薬が提供されている。とりわ
け糖尿病患者の負担を軽減し、治療を容易にする上で経
口投与に適した、消化管での吸収性の高い新規な糖尿病
治療薬の開発が強く求められている。[Prior Art and Problems to be Solved by the Invention] The development of antidiabetic drugs is becoming increasingly important as the number of diabetic patients increases, and a variety of drugs are being provided. In particular, in order to reduce the burden on diabetic patients and facilitate treatment, there is a strong need for the development of novel antidiabetic drugs that are highly absorbable in the gastrointestinal tract and are suitable for oral administration.
Claims (1)
はナフチル基、Ａｌｋは低級アルキレン基を表す。） で示されるベンゾオキサゾール誘導体またはその薬理的
に許容し得る塩が固体分散もしくは溶解してなる製剤。 ２、常温で固体状の水溶性高分子物質中に有効成分が固
体分散してなるか、あるいは液状の水溶性高分子物質中
に有効成分を溶解してなる請求項１記載の製剤。 ３、水溶性高分子物質がポリエチレングリコール、ポリ
ビニルピロリドン、ヒドロキシプロピルセルロースであ
る請求項２記載の製剤。 ４、一般式（ I ）において、Ｒがハロゲン原子および
ジ（低級アルキル）アミノ基から選ばれる１〜３個の基
で置換されていてもよいフェニル基またはナフチル基で
ある請求項１、２または３記載の製剤。 ５、一般式（ I ）において、Ｒがハロゲン置換フェニ
ル基、ジ（低級アルキル）アミノ基置換フェニル基また
はナフチル基である請求項４記載の製剤。 ６、有効成分が５−［（２，４−ジオキソチアゾリジン
−５−イル）メチル］−２−［４−（ジメチルアミノ）
ベンジル］ベンゾオキサゾールまたはその薬理的に許容
し得る塩である請求項５記載の製剤。 ７、有効成分が５−［（２，４−ジオキソチアゾリジン
−５−イル）メチル］−２−［（２−ナフチル）メチル
］ベンゾオキサゾールまたはその薬理的に許容し得る塩
である請求項５記載の製剤。 ８、有効成分が５−［（２，４−ジオキソチアゾリジン
−５−イル）メチル］−２−（４−クロロベンジル）ベ
ンゾオキサゾールまたはその薬理的に許容し得る塩であ
る請求項５記載の製剤。[Claims] 1. The water-soluble polymer substance has a general formula ▲mathematical formula, chemical formula, table, etc. as an active ingredient▼(I) (However, R is a phenyl group or naphthyl that may have a substituent. group, Alk represents a lower alkylene group. 2. The preparation according to claim 1, wherein the active ingredient is solidly dispersed in a water-soluble polymeric substance that is solid at room temperature, or the active ingredient is dissolved in a liquid water-soluble polymeric substance. 3. The preparation according to claim 2, wherein the water-soluble polymeric substance is polyethylene glycol, polyvinylpyrrolidone, or hydroxypropylcellulose. 4. In general formula (I), R is a phenyl group or a naphthyl group optionally substituted with 1 to 3 groups selected from a halogen atom and a di(lower alkyl)amino group. 3. The formulation described in 3. 5. The preparation according to claim 4, wherein in the general formula (I), R is a halogen-substituted phenyl group, a di(lower alkyl)amino group-substituted phenyl group, or a naphthyl group. 6. The active ingredient is 5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-[4-(dimethylamino)
6. The preparation according to claim 5, which is benzylbenzoxazole or a pharmacologically acceptable salt thereof. 7. Claim 5, wherein the active ingredient is 5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-[(2-naphthyl)methyl]benzoxazole or a pharmacologically acceptable salt thereof. The formulation described. 8. The active ingredient according to claim 5, wherein the active ingredient is 5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-(4-chlorobenzyl)benzoxazole or a pharmacologically acceptable salt thereof. formulation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP9270190A JPH03291224A (en) | 1990-04-06 | 1990-04-06 | Drug having improved absorptiveness |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP9270190A JPH03291224A (en) | 1990-04-06 | 1990-04-06 | Drug having improved absorptiveness |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH03291224A true JPH03291224A (en) | 1991-12-20 |
Family
ID=14061794
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP9270190A Pending JPH03291224A (en) | 1990-04-06 | 1990-04-06 | Drug having improved absorptiveness |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH03291224A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4806885B2 (en) * | 2000-06-14 | 2011-11-02 | 日本新薬株式会社 | Solid dispersions and drugs |
-
1990
- 1990-04-06 JP JP9270190A patent/JPH03291224A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4806885B2 (en) * | 2000-06-14 | 2011-11-02 | 日本新薬株式会社 | Solid dispersions and drugs |
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