US3090724A - Method of treating dermatological conditions - Google Patents

Description

United States 3,090,724 METHGD F TREATING DERMATOLOGICAL CONDITIONS Edward H. Bowen, in, Evanston, 111., assignor to Baxter Laboratories, Inc. No Drawing. Filed Jan. 3, 1961, Ser. No. 80,025 5 Claims. (Cl. 16755) The present invention relates to treatment of dermatological conditions. More particularly, it relates to'the use of compositions not heretofore employed or recognized as effective in the treatment of acne vulgaris and related conditions.

Acne vulgaris and similar dermatological conditions, because of their common occurrence during puberty, and other periods when the thyroid gland is not assuming its full physiological function, have long been suspected by various clinicians as being related to faulty lipoid metabo lism. See Sutton, R. L., Jr., Acne Vulgaris, a pustular lipoidosis; South, M. 1., 34: 1071 (1941).

Until the present, it has been generally believed that the power of thyro-mimetic materials to favorably affect lipoid metabolism and improve conditions such as acne has been inseparable from their undesirable property of increasing the basal metabolic rate.

It has now been unexpectedly discovered that the administration of the d-isomer of a compound, the l-isomer of which is thyromimetic, produces beneficial efiects in the treatment of acne vulgaris and other dermatological conditions with negligible increase in the basal metabolic rate.

In accordance with this invention, dermatological conditions are treated by administering compositions comprising a d-isomer of thyroxine or of a compound the l-isomer of which is thyro-mimetic in pharmaceutical dosage form. The d-isomer may be associated with any pharmaceutical carrier suitable for the preparation of compositions in dosage form. For purposes of illustration, the invention is described with particular reference to d-thyroxine. It is understood, however, that the scope of the invention is not limited to d-thyroxine, but includes d-isomers of compounds, such as 3,5,3-triiodothyronine and 3,'5,3'-triiodo-5'-methyl thyronine. It is further understood that the compositions employed in the practice of this invention are substantially free of therapeutically significant calorigenic amounts of thyro-active compounds of the l-series. 'It is desirable that the compounds used in the methods of this invention be substantially devoid of thyro-active material, i.e., material which engenders in the individual an elfect on basal metabolic rate (BMR) analogous to that engendered by l-thyroxine. Such material normally comprises compounds of the l-series.

The compositions of this invention may take the form of tablets, powders, capsules or other dosage forms. The compositions employed in the methods of this invention may take the form of active material, namely, d-thyroxine, admixed with solid diluents and/or tableting adjuvants such as cornstarch, lactose, talc, stearic (acid, magnesium stearate, gums or the like. Any of the tableting materials used in pharmaceutical practice may be employed where there is no incompatability with the d-thyroxine. The m-aterial may be tableted with or without adjuvants. Alternatively, the d-thyroxine material with its adjuvant material may be placed in the usual capsule or resorbab-le material, such as the usual gelatin capsule, and administered in that form.

The d-thyroxine in particular has been found to have an insignificant eflect on the basal metabolic rate of the individual at doses :of 4-8 mgm./ day and yet possess the ability to aid in the treatment of acne vulgaris and the like. Surprising therapeutic results are generally obtained through daily doses of d-thyroxine and its pharmaco- 3,090,724 Patented May 21, 1963 logically acceptable salts in the range from 2 to about 8 milligrams. Higher doses may be administered in certain individuals with no undesirable BMR effects. Examples of these therapeutically active salts are the .alkali metal salts of d-thyroxine such as sodium d-thyroxine, potassium d-thy-roxine, d-thyroxine hydrochloride, and the like.

A more comprehensive understanding of this invention is obtained by reference to the following examples:

EXAMPLE I Tablets, each containing the following amounts of ingredients, were prepared:

Tests were conducted to determine the calorigenic effect of the tablets prepared in Example I on normal human volunteers. Volunteers receiving maximum daily doses of 3, 4 and 5 mg. of d-thyroxine for periods as long as days experienced only slight increases in basal metabolic rate.

To demonstrate the efiicacy of the d-thyroxine in treating dermatological conditions the following representative clinical case histories are submitted:

Case N 0. 1

A white unmarried female, age 26, suitering from acne vulgaris received 2 mg. of d-thyroxine twice daily for approximately 4 months. Medication was then reduced to 2 mg. daily. The acne vulgaris was kept under control during this time but flared when medication was discontinued.

Case No. 2

A while male, age 64, suffering from follicular pustules received 2 mg. of d-thyroxine twice daily for approximately 2 /2 months during which period his dermatological condition improved.

Case No. 3

A white female, age 70, suffering from xanthel asma received 2 mg. of d-thyroxine twice daily for 2 months during which period her condition improved.

Case No. 4

A white male, age 37, suffering firom psoriasis and xanthelasma received 2 mg. of d-thyroxine twice daily for 5 weeks and then twice daily for 5 weeks during which period the patents dermatological condition improved.

Case N0. 5

A white male, age 34, suffering from xanthelasma received 2 mg. of d-thyroxine thrice daily for 9 months during which period his condition was generally much improved and very few lesions recurred.

Case No. 6

A white unmarried female, age 57, suffering from xanthelasma received 2 mg. of d-thyroxine twice daily for 3 weeks. Patient reported feeling less bloated since taking medication and was pleased with progress.

Case No. 7

A white male, age 15, suffering atopic dermatitis and contact dematitis received 2 mg. of d-thyroxine twice daily for 9 weeks during which period the dermatological conditions, in general, improved.

Case No. 8

A white female, age 42, suffering from lichen planus and stasis dermatitis received 2 mg. of d-thyroxine twice daily -for 5 weeks then 2 mg. once daily during which period the patients dermatological condition generally improved.

Case No. 9

A white female, age 53, suffering from a condition diagnosed as intertrigo onychomycosis received 2 mg. of d-thyroxine twice daily for 4 months during which period the patients dermatological condition generally improved. More specifically, a clearing of the afflicted hand areas was noted.

7 Case No. 10

A white female, age 41, suffering from seborrheic dermatitis and blepharitis marginalis received 2 mg. of dthyroxine twice daily for 2 weeks at the end of which period her dermatological condition was much improved.

Case N0. 11

A white male, age 27, sufiering from necrobiosis lipoidica diabeticorum received 2 mg. of d-thyroxine twice daily for 18 Weeks at the end of which time he was doing well and his general appearance was improved.

Case Nos. 12-22 4 similar results are obtainable with d-tri-iodothyronine and the like.

It is apparent from the foregoing case histories that the d-isomers of compounds the l-isomer of which is thyro-mimetic e.g. d-thyroxine, d-tri-iodothyronine and the like, are valuable additions to the. dermatologists arsenal for the treatment of acne vulgaris, psoriasis, Xanthelasma, xanthomatosis and a Wide variety of related dermatological conditions in which aberrant lipoid metabolism may play a role.

The embodiments of the invention in which an exclusive property or privilege is claimed are:

1. In the treatment of patients afilicted with acne vulgaris the improvement which comprises administering to said patients d-thyroxine in an amount from about 2 to about 8 mg. daily.

2. The improvement in the treatment of dermatological conditions which comprises administering to a patient suifering from a dermatological condition of d-isomer of a compound selected from the class consisting of thyroxine, 3,5,3 tn iodothyronine, and 3,5,3 triiodo 5' methyl thyronine.

3. The method of claim 2 in which the d-isomer is d-thyroxine.

4. The improvement in the treatment of humans having dermatological conditions which comprises administering to said humans a daily dosage in tolerated levels of a d-isomer of a compound selected from the class consisting of thyroxine, 3,5,3'-tri-iodothyronine, and 3,5 ,3'-triiodo-5 -methyl thyronine.

5. The method of claim 4 in which the d-isomer is d-thyroxine.

References Cited in the file of this patent Freinkel: J. of Investigative Dermatology, vol. 34, April 1960, pp. 277-279.