US 3137620 A
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United States Patent No Drawing. Filed Nov. 6, 1959, Ser. No. 851,271 3 Claims. (Cl. 167-55) This invention relates to an improved method in the treatment of acne particularly pustular acne, and more particularly to the treatment of acne by means of an orally ingested thiadiazole, more particularly 2-p-rnethoxyb enzenesulfonamide-S-isobutyl- 1 ,3 ,4-thiadi azole.
In severe cases of acute pustular acne, local therapy alone is of little value. The specific systemic measures usually employed in addition to local therapy depend upon the seriousness of the skin condition. Additional measures which have been used in the past include: hormone therapy, particularly diethylstilboestrol; dietary control; vitamin supplements, particularly vitamin A and vitamin C; ultraviolet and X-ray therapy; administration of toxoids and vaccines; and use of antibiotics, such as sulfonamides; pencillin, erythromycin, chloramphenicol, oleandomycin, tetracycline and novobiocin. Isoniazid has also been used. Most consistent results have been achieved with chloramphenicol and erythromycin. Nevertheless, treatment with antibiotics is unsatisfactory since, while a favourable response to usually obtained, this is followed by a new flare-up, and relapses are frequent after discontinuance of the antibiotics. The other forms of drug therapy are also not completely effective.
In pending application Serial Number 824,176 filed in the name of I. L. Cohen on July 1, 1959, now US. Patent No. 3,072,527, there is disclosed an improved method for the treatment of acne by the administration of tolbutamide. The utility of tolbutamide in the treatment of acne is unexpected, since tolbutamide has no bactericidal effect.
However, it is known that a 1.0 g. dosage of tolbutamide lowers blood sugar levels about in normal individuals. While this lowering of the blood sugar is not serious, there may be cases where acne is to be treated when such lowering of blood sugar levels may be critical.
It is an object of the present invention to provide an improved oral therapy for the relief of symptoms of acne.
This object is achieved in the method of treating acne which comprises: selecting a human having acne; and feeding said human a therapeutically effective dose of 2-pmethoxybenzenesulfonamide-S-isobutyl-1,3,4-thiadiazole.
Usually, the therapy consists in the ingestion, by the patient suffering from acne, of tablets containing the thiadiazole. Although doses of 2-3 grams per day of the thiadiazole may be safely used, effective doses will be in the range of 0.5-1.0 gram per day.
A convenient form of treatment is the use of tablets containing from about 250 mg. to about 1000 mg. of the 2 p methoxybenzene sulfonamide-S-isobutyl-l,3,4-thiadiazole, with an especially convenient amount being 500 mg. of the thiadiazole per tablet. Preparation of such tablets is given below.
EXAMPLE I.TABLETS The following proportions of ingredients were used:
Orange colored starch 6.5 Sodium bicarbonate 3.1 Magnesium stearate 0.8
The orange colors were dissolved in a granulating solution consisting of a 24% solution of gelatin and acacra in water. The thiadiazole was then granulated with 1.0 gm. of the colored starch, the amount of granulating solution originally used being suflicient to result in a dry granulation procedure. The balance of the starch, the sodium bicarbonate and the magnesium stearate were then intimately mixed therewith and the mixture was compressed into tablets.
The proportions used were sufiicient to result in the preparation of 100 tablets, each weighing 620 mg. and containing 500 mg. of the thiadiazole.
EXAMPLE ILL-CAPSULES In this case 50.0 gm. of 2-p-methoxybenzenesulfonamide-5-isobutyl-l,3,4-thiadiazole was intimately mixed with 1.0 gm. of a light mineral oil. 100 capsules each containing 500 mg. of the thiadiazole were then prepared by placing 510 mg. of that mixture into hard gelatin capsules.
A series of patients were treated with Z-p-methoxybeuzenesulfonamide-S-isobutyl-1,3,4-thiadiazole according to the method of the present invention. The results are tabulated in Table I below.
Table 1 Treatment with 2p-methoxybenzenesulfonamide-5-is0butyl- N 0 Diagnosis Prior 1,3,4-thiadiaz0le Treatment Side Effects Evaluation 1.. Cystic acne, Antivaccine None after 64 Good; patient recurring progesterdays. free of acne iurunculoone, antitype of insis. biotics X- faction, feels ray, cryobetter. therapy.
2 Furunculo- Antibiotics... None after 89 Good; furunsis, relapsdays. cles have mg. not relapsed.
3 Furunculo- Antibiotics 54 days Good; pussis. antivaccine treatments. tules dried serum up quickly. globulin.
4....-. Severe cystic Progesterone None after 101 Good; appears acne. serobacteridays. to prevent um 00; outbreak of slush. new cysts premenstrually.
5"--. Furunculo- Antibiotics, None after 90 Good.
sis. vaccine. days.
6 Cystic acne. None None after 42 Slow steady days. improvement.
It is seen from the above table that 2-p-methoxybenzenesnlfonamide-S-isobutyl-1,3,4-thiadiazole is efiective in the treatment of acne.
The eflect of 2-p-methoxybenzenesulfonamide-S-isobuty11,3,4-thiadiazole on the blood sugar of normal non- Table II 3000 mg. Z-p-methoxybenzene- Hours after sulfonamide-fi-isobutyl- 50 ggfi ingestion 1,3,4-th1admzole Number weight tolbutam 7 8 9 ide 100 100 100 100 s--. 56 100 97 95 68 t 72 93 100 I 70 72 c 56 93 100 79 It will be seen from Table II that While tolbutamide causes a rapid and substantial drop in blood sugar levels at dosage levels of 50 mg./kg. body weight, 2-p-methoxybenzenesulfonamide-S-isobutyl-1,3,4-thiadiazole, in the majority of cases, causes no significant decrease in blood sugar at approximately the same dosage (3 grams total). It is also to be emphasized that the dose of tolbutamide with which the results of the present invention are compared is 50 mg./kg.
1. The method of treating acne which comprises orally administering to a human affected with acne a daily dose of 0.5-3.0 grams, in individual doses of 250-1000 mg. of 2 p methoxybenzenesulfonamide 5 isobutyl-l,3,4-thiadiazole.
2. The method of claim 1 wherein the thiadiazole is fed in a dosage unit form containing about 0.5 gm. of said thiadiazole.
3. The method of claim 2 wherein the thiadiazole is fed in tablet form.
References Cited in the file of this patent Wortis: JAMA, 108112, March 20, 1937, p. 971.
Lessor: Drug and Cos. Ind, 63:4, October 1948, pp. 466-468, 544-547.
Meshard: Prods. Pharm., vol. 13, October 1958, pp.
Bulletin Johns Hopkins Hospital, 85(3), pp. 221-230,
20 September 1959.