US2252822A - Sulphanilamide solution - Google Patents

Description

, It has further been determined that oral adminisamount of sulphanilamide with a suitable excreted in th free tat As an example of the method followed in pro! Patented Au 1 9, 194i V l 2,252,822

UNITED STATES PATENT OFFICE 2,252,822 v SULPHANILAMIDE SOLUTION Clarence A. Vogenthaler, Ferguson, Mo., assignor to Donley-Evans & Company, St. Louis, Mo., a corporation of Missouri No Drawing. Application Aprllla, 1939',

Serial No. 267,619

4 Claims. (01. lav-es) Within recent years there has come to the much as sulphanilamide must be held in solution attention of the medical profession a chemical of not less than four percent by volume for praccomposition, or dye, known as para-aminobentical purposes and the solubility of sulphanilazenesulphonamide, that has been found to be of mide in cold water and cold alcohol is very much very considerable value in the internal treatment 5v less than this. of streptococcal, meningococcal,gonococcal, and Quite naturally the foregoing facts led to a other infections. For all ordinary purposes this Search or' ome manner or means for administerchemical agent has been termed sulphanilaming sulphanilamide orally that would enable the ide, and it has been observed by medical inhuman body to absorb it more quickly and more vestigators, and physicians who have prescribed completely. The problem so presented has been the composition in their practices, that in the solved by the discovery by me of an improved treatment of the above named and other infecth d n a rdan w th w h su p an lations, sulphanilamide is highly beneficial. mide may be presented in a stable solution of While much is yet to be learned of the actual approximately s ven p r t, by volume, which workings of this chemical agent, it has been deis of S fl c c strength to make 1188 D termined that its value is dependent primarily ticable, and which solution as composed includes on its absorption into the blood stream in sufother chemical agents that are nontoxic and do ficient quantity to reach a high concentration in not produce any chemical ch in h Sulpha short space of time and on maintaining that anilamide itself. a high concentration over the period of treatment. 0 y p v d met od o ves mixing a tration of sulphanilamide produces a higher solvent and subjecting the mixture so pr u d blood concentration than is obtained through its to the proper temperature for the proper period administration by sub-cutaneous or any' other of time. It has been discovered that a solvent method However, prior to this invention sulphthat lends itself admirably to the production of. anilamidc was considered relatively insoluble a sulphanilamide solution in accordanc with (0.8% at 37 C.) and therefore in the use ofthis the teachings of this invention, includes glucose agent heretofore large doses of the drug had to cut Wi h lyc rine. When such a solvent is embe administered frequently to produce the deployed a d mixtllrc 0 s p ilam de and the sired high blood concentration with the result solvent is subjected to the proper heat treatment that in many cases-55% to 60% of the drug was as disclosed herein a stable solution is produced.

Prior to this invention no substance was (11101118 the v d ulphanilamide solution a known which would act as a solvent for sulplimix ure is made up ofapproxima ely 48% anilamide and that could be safely taken into Gluc s pp oximately 1 3% glycerine; approxithe human system, the sulphanilamide marketed mat l sulp a amid and if required to prior to my discovery being in tablet form and give the desired consistency to the solution, an in the form of powder, the tablets containing 0.3 o t f d l d Wa e the percenta gm, and 0.5 gm. of the drug mixed with an ext on d bove\being by weight. The mixture so cipient. It was known heretofore that sulphproduced is slowly he p a y on a Water anilamide was soluble in hot water, hot alcobath. until it s b ought to .a te p tu e of hol and cold acetone, slightly soluble in cold f om C- t 90 C. and the mixture is held water and cold alcohol, practically insoluble in at Such emp e for at least thirty m nut s; hydrochloric acid, and insoluble in ether, benbeing stirred as required to facilitate solution zene, and chloroform. Obviously a hot solvent and to prev formation of u o 1 1 On the could not be used for a sulphanilamide solution surface of the mixture. After the heat is disto be marketed in bottles b cause the sulphntinued a sufll lent quanti f lucose is anilamide would crystallize out of the solution ed to e up for heat loss and the resultant as soon as the solution started to cool. Likewise a mixture is allowed to cool naturally. Obviously acetone, because of its nature, could not be emthe percentages of ingredients mentioned above ployed as a solvent for a composition intended I may, under different conditions, be varied withto taken taken into the human system. Furtherout departing from the spirit of the invention.- more because sulphanilamide is only slightly It has been discovered that the proper applicasoluble in cold water and cold alcohol these on h a 18 mattcr Of v a mportance in mediums could not be employed as solvents inas- 5 producing a sulphanilamide solution in accordance with this invention, it being absolutely essential that the mixture be subjected to the proper temperature for the proper period of time. In the absence of the proper application of heat a stable solution will not be produced even though the mixture is made up of the proper ingredients, such as those specified above, in the proper proportions.

This application is a continuation in part 01 an application for U, patent filed in my name on October 1, 1937, Serial No. 166,831.

I claim:

1. The method producing a therapeutic substance in stable solution form, which comprises producing a mixture which includes approximately 5% sulphanilamide, approximately 48% glucose, approximately 13% glycerine; said percentages being by weight, and subjecting the mixture so produced to a temperature of at least 75 C. for a period of time of at least thirty minutes to produce a non-toxic solution which is stable at all ordinary temperatures.

- 2. The method of producing a therapeutic substance in stable solution form, which comprises producing a mixture which includes :approxlmately 5% sulphanilamide, approximately 48% glucose, approximately 13% glycerine, said perform of a liquid which is stable at all centages being by weight. and water, and sub- Jecting the mixture so produced to a temperature of at least C. for a period 0! time 0! at least thirty minutes to produce a non-toxic solution which is stable at all ordinary temperatures.

3. A non-toxic therapeutic substance in the form of a liquid which is stable at all ordinary temperatures, comprising a mixture that includes approximately 5% sulphanilamide, approximately 48% glucose, and approximately 13% glycerine, said percentages being by weight, said therapeutic substance being produced by subjecting said mixture to a temperature or at least 75 C. for a period of time or at least thirty minutes.

substance in the ordinary temperatures, comprising a mixture that includes approximately 5% sulphanilamide, approximately 48% glucose, approximately 13% glycerine, said percentages being by weight, and water, said therapeutic substance being produced by subjecting said mixture to a temperatureof at least 75 C. for a period of time of at least thirty minutes.

4. A non-toxic therapeutic CLARENCE A. VOGENTHALER.