US3449499A - Method for the reduction of glycemia - Google Patents
Method for the reduction of glycemia Download PDFInfo
- Publication number
- US3449499A US3449499A US427143A US3449499DA US3449499A US 3449499 A US3449499 A US 3449499A US 427143 A US427143 A US 427143A US 3449499D A US3449499D A US 3449499DA US 3449499 A US3449499 A US 3449499A
- Authority
- US
- United States
- Prior art keywords
- glycemia
- compositions
- patient
- reduction
- benzenesulphonylamino
- 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 - Lifetime
Links
- 238000000034 method Methods 0.000 title claims description 6
- 206010012601 diabetes mellitus Diseases 0.000 claims description 7
- NMWQEPCLNXHPDX-UHFFFAOYSA-N Glybuzole Chemical compound S1C(C(C)(C)C)=NN=C1NS(=O)(=O)C1=CC=CC=C1 NMWQEPCLNXHPDX-UHFFFAOYSA-N 0.000 claims description 2
- 239000000203 mixture Substances 0.000 description 8
- 150000001875 compounds Chemical class 0.000 description 4
- 239000003701 inert diluent Substances 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 241001465754 Metazoa Species 0.000 description 3
- 239000004480 active ingredient Substances 0.000 description 3
- 229920002472 Starch Polymers 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 239000008247 solid mixture Substances 0.000 description 2
- 108010010803 Gelatin Proteins 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 239000007891 compressed tablet Substances 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 239000000796 flavoring agent Substances 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
- 239000008187 granular material Substances 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000002304 perfume Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000008024 pharmaceutical diluent Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 229940100445 wheat starch Drugs 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
- C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
- C07D285/135—Nitrogen atoms
Definitions
- compositions useful for reducing glycemia for prolonged periods comprising, as active ingredients, the compound of formula:
- X is hydrogen in association with a pharmaceutical diluent.
- the active ingredient preferably constitutes 5 to 95% by weight of the said composition.
- Solid compositions for oral administration include compressed tablets, pills, powders, and granules.
- the active compound is admixed with at least one inert diluent such as starch, ucrose or lactose.
- the compositions may also comprise, as is normal practice, additional substances other than inert diluents, e.g. lubricating agents, such as magnesium stearate.
- Liquid compositions for oral administration include pharmaceutically-accepta-ble emulsions, solutions, suspensions, syrups and elixirs containing inert diluents commonly used in the art, such as water and liquid parafiin.
- compositions may also comprise adjuvants, such as wetting and suspending agents, and sweetening, flavoring, perfuming and preserving agents.
- adjuvants such as wetting and suspending agents, and sweetening, flavoring, perfuming and preserving agents.
- the compositions according to the invention, for oral administration also include capsules of absorbable material such as gelatin containing one or more of the active substances with or without the addition of diluents or excipients.
- compositions of the invention may be varied, it being necessary that it should constitute a proportion such that a suitable dosage shall be obtained.
- the dosage will depend upon the therapeutic effect sought, the route of administration, the length of treatment, and the size and species of animal.
- compositions should generally be 3,449,499 Patented June 10, 1969 administered so as to give, in the case of oral administration, between 500 mg. and 2 g. of active substance per day.
- a preferred form of tablet for use in accordance with the invention has the following composition.
- the invention also provides a method of reducing glycemia for prolonged periods which comprises administering to an animal organism a compound of the above formula in amount suflicient to reduce the glycemia. It is an advantage of the invention that a single daily dose only need be given, because of the prolonged action of the compounds characteristic of the new method. Ordinarily a dose of 5 to 40 mg. per kg. of animal organism will be administered, corresponding to a dose of about 0.5 to 2.0 g. for an average size adult. Such a dosage will maintain the glycemia of a diabetic patient at about the normal level for at least 24 hours.
- a method of treating diabete which comprises administering orally to a human diabetic patient Z-benzenesulphonylamino-S-t-butyl-1-thia-3,4-diazole in a single daily dose of 5 to 40 milligrams per kilogram of said patient.
- a method of treating diabetes which comprises administering orally to a human diabetic patient 2-benzenesulphonylamino-5-t-butyl-1-thia-3,4-diazole in a daily dose of 5 to 40 milligrams per kilogram of said patient.
Description
United States Patent Int. Cl. Alslk 27/00 US. Cl. 424-270 2 Claims This invention relates to the reduction of glycemia.
The present invention accordingly provides pharmaceutical compositions useful for reducing glycemia for prolonged periods comprising, as active ingredients, the compound of formula:
where X is hydrogen in association with a pharmaceutical diluent. The active ingredient preferably constitutes 5 to 95% by weight of the said composition.
Solid compositions for oral administration include compressed tablets, pills, powders, and granules. In such solid compositions the active compound is admixed with at least one inert diluent such as starch, ucrose or lactose. The compositions may also comprise, as is normal practice, additional substances other than inert diluents, e.g. lubricating agents, such as magnesium stearate. Liquid compositions for oral administration include pharmaceutically-accepta-ble emulsions, solutions, suspensions, syrups and elixirs containing inert diluents commonly used in the art, such as water and liquid parafiin. Besides inert diluents such compositions may also comprise adjuvants, such as wetting and suspending agents, and sweetening, flavoring, perfuming and preserving agents. The compositions according to the invention, for oral administration, also include capsules of absorbable material such as gelatin containing one or more of the active substances with or without the addition of diluents or excipients.
The percentage of active ingredient in the compositions of the invention may be varied, it being necessary that it should constitute a proportion such that a suitable dosage shall be obtained. The dosage will depend upon the therapeutic effect sought, the route of administration, the length of treatment, and the size and species of animal. In human therapy the compositions should generally be 3,449,499 Patented June 10, 1969 administered so as to give, in the case of oral administration, between 500 mg. and 2 g. of active substance per day.
A preferred form of tablet for use in accordance with the invention has the following composition.
2-benzenesulphonylamino-S-t-butyl-lthia-3,4-diazole 250 Potato starch 6 Talc 3 Magnesium stearate 0.5 Wheat starch to 330 The invention also provides a method of reducing glycemia for prolonged periods which comprises administering to an animal organism a compound of the above formula in amount suflicient to reduce the glycemia. It is an advantage of the invention that a single daily dose only need be given, because of the prolonged action of the compounds characteristic of the new method. Ordinarily a dose of 5 to 40 mg. per kg. of animal organism will be administered, corresponding to a dose of about 0.5 to 2.0 g. for an average size adult. Such a dosage will maintain the glycemia of a diabetic patient at about the normal level for at least 24 hours.
I claim:
1. A method of treating diabete which comprises administering orally to a human diabetic patient Z-benzenesulphonylamino-S-t-butyl-1-thia-3,4-diazole in a single daily dose of 5 to 40 milligrams per kilogram of said patient.
2. A method of treating diabetes which comprises administering orally to a human diabetic patient 2-benzenesulphonylamino-5-t-butyl-1-thia-3,4-diazole in a daily dose of 5 to 40 milligrams per kilogram of said patient.
References Cited UNITED STATES PATENTS 3,121,089 2/1964 Jansson.
FOREIGN PATENTS 822,947 11/1959 Great Britain. 824,978 12/1959 Great Britain.
ALBERT T. MEYERS, Primary Examiner.
J. D. GOLDBERG, Assistant Examiner.
Claims (1)
1. A METHOD OF TREATING DIABETES WHICH COMPRISES ADMINISTERING ORALLY TO A HUMAN DIABETIC PATIENT 2-BENZENESULPHONYLAMINO-5-T-BUTYL-1-THIA-3,4-DIAZOLE IN A SINGLE DAILY DOSE OF 5 TO 40 MILLIGRAMS PER KILOGRAM OF SAID PATIENT.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR961646A FR3389M (en) | 1964-01-27 | 1964-01-27 | New drugs derived from thiadiazole. |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| US3449499A true US3449499A (en) | 1969-06-10 |
Family
ID=8821781
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| US427143A Expired - Lifetime US3449499A (en) | 1964-01-27 | 1965-01-21 | Method for the reduction of glycemia |
Country Status (3)
| Country | Link |
|---|---|
| US (1) | US3449499A (en) |
| BE (1) | BE658828A (en) |
| FR (1) | FR3389M (en) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB822947A (en) * | 1957-01-25 | 1959-11-04 | Smith & Nephew | Improvements in and relating to sulphonamides |
| GB824978A (en) * | 1957-02-05 | 1959-12-09 | Smith & Nephew | Improvements in sulphonamides |
| US3121089A (en) * | 1964-02-11 | Z-arylsulfonamido-s-alkyl-l |
-
1964
- 1964-01-27 FR FR961646A patent/FR3389M/en not_active Expired
-
1965
- 1965-01-21 US US427143A patent/US3449499A/en not_active Expired - Lifetime
- 1965-01-26 BE BE658828A patent/BE658828A/xx unknown
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3121089A (en) * | 1964-02-11 | Z-arylsulfonamido-s-alkyl-l | ||
| GB822947A (en) * | 1957-01-25 | 1959-11-04 | Smith & Nephew | Improvements in and relating to sulphonamides |
| GB824978A (en) * | 1957-02-05 | 1959-12-09 | Smith & Nephew | Improvements in sulphonamides |
Also Published As
| Publication number | Publication date |
|---|---|
| FR3389M (en) | 1965-06-21 |
| BE658828A (en) | 1965-07-26 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US3174901A (en) | Process for the oral treatment of diabetes | |
| ES2239799T3 (en) | USE OF TETRAHIDROLIPSTATIN IN THE TREATMENT OF TYPE II DIABETES. | |
| AU596296B2 (en) | Treatment of diabetes | |
| US4387093A (en) | Arthritis treatment | |
| US3867539A (en) | Method of producing anorexia as a treatment for obesity | |
| US3196078A (en) | Process for combating retinits pigmentosa | |
| US2789938A (en) | Method of producing a diuretic effect with p-carboxybenzenesulfonamide | |
| US3230142A (en) | Oral contraceptive compositions and methods | |
| US3449499A (en) | Method for the reduction of glycemia | |
| US2878263A (en) | 4-methyl-4-phenyl-5-pyrazolone | |
| US2403473A (en) | Therapeutic compositions | |
| US3137625A (en) | Diuretic combinations containing a thiazide and a mercurial | |
| US3044932A (en) | Appetite suppressant drugs | |
| US3940481A (en) | Treatment of hepatic coma with isomaltitol | |
| US4042698A (en) | Treatment of myasthenia gravis and oral medication therefor | |
| US3222253A (en) | Antimitotic colchicines | |
| US3565560A (en) | Pharmaceutical preparation containing hydrofuramide and method of using it | |
| US3057777A (en) | Method of reducing cholesterol level of the blood | |
| US3332846A (en) | Method of inducing hypoglycemia with a substituted indole | |
| US2793157A (en) | Anticonvulsant 3-ethyl-5-phenyl hydantoin unit dosages and method of using same | |
| US3772433A (en) | Treatment of hepatopathias with saccharides | |
| US3150043A (en) | Anorectic composition | |
| CA1172566A (en) | Method for producing pharmaceutical preparation | |
| US3296074A (en) | Methods and compositions for treating psychoses and neuroses | |
| US2991225A (en) | Omicron-methylbenzhydryl-beta-dimethylaminoethyl ether process and composition for symptomatic relief of the syndrome of parkinsonism and of spastic skeletal muscle disorders |