Saccharin
Historical document, translated for reference. It reflects medical knowledge of the 1920s–30s and is not medical advice.
Summary
A 1930s overview of saccharin, detailing its chemical synthesis via the Heyden method, its use as a non-nutritive sugar substitute, and the contemporary medical debates regarding its safety and physiological effects.
Encyclopedia article (1928–1936)
SACCHARIN, the imide of orthosulfobenzoic acid, a white crystalline powder, melting
with partial decomposition at 224°, odorless, with a very sweet taste; it is used as a sugar substitute. Saccharin is sparingly soluble in cold water (1:350), significantly better in cold alcohol (1:40), and easily in hot water (1:28). The sodium salt of saccharin, well soluble in water, is known commercially as "easily soluble saccharin," "crystallose," "sucerin," "saccharinose," etc.; it appears as a white crystalline powder, possesses the same sweet taste as pure saccharin, and usually replaces it in the food industry. The ammonium salt of saccharin is called "sucramine" and in taste differs almost not at all from the sodium salt. The intensity of the sweet taste of saccharin can be judged by comparing it with cane sugar. To obtain an equally sweet taste, a dose of pure saccharin or its salts 350–550 times smaller than that of cane sugar is required. Factory production of saccharin at the present time is carried out by the Heyden method: a) toluene is treated with chlorosulfonic acid, resulting in the formation of a mixture of ortho- and paratoluenesulfonyl chlorides; b) the resulting mixture is cooled, paratoluenesulfonyl chloride precipitates in solid form and is centrifuged off; c) liquid orthotoluenesulfonyl chloride is washed with water and amidated with ammonia at a temperature of 30°, resulting in orthotoluenesulfonamide; d) after a rather complex subsequent purification from impurities of paratoluenesulfonamide (recrystallization from 80% alcohol, etc.), pure orthotoluenesulfonamide is oxidized in a strongly alkaline medium at 35° with potassium permanganate into orthosulfamidobenzoic acid and filtered; e) the filtrate is slightly acidified with hydrochloric or sulfuric acid, and residues of the unreacted amide precipitate; f) the liquid is filtered again and strongly acidified with the same acid; crystals of pure saccharin precipitate. If pure saccharin is treated with sodium alkali, the sodium salt of saccharin is easily formed. According to the requirements of the People's Commissariat of Health of the RSFSR (Circular No. 188 of July 8, 1922), the saccharin produced must be chemically pure and contain no more than 3% parasulfamidobenzoic acid. Saccharin purchased abroad must be submitted for analysis to the appropriate body of the People's Commissariat of Health before being released to the domestic market.
Saccharin does not possess the nutritional properties inherent in cane sugar and other types of sugar, as it is not assimilated by the body at all. There are different opinions regarding the admissibility of using saccharin as a sugar substitute. Some consider saccharin a completely harmless substance for the body and allow its unlimited use; others, on the contrary, point to some harm from it and do not recommend using it instead of sugar. The opinion of saccharin's defenders is based on the fact that saccharin, although easily absorbed in the intestine, is not assimilated by the body at all and is very quickly excreted unchanged in the urine. No serious pathological-anatomical changes as a result of using saccharin in food have been established. Some people have taken 5 g of saccharin per day without any ill effects. Opponents of allowing saccharin for widespread food consumption point out that saccharin increases diuresis; therefore, it cannot be considered a substance completely indifferent to the human body. Experimental work by Folbort and Rastorgueva showed that saccharin inhibits gastric secretion in dogs. V. Uglov found that saccharin weakens the action of digestive enzymes and exhibits bactericidal properties that exceed in strength the action of phenol and salicylic acid taken in the same doses. Jaksch points out that prolonged and frequent use of saccharin can cause loss of appetite, eructation, vomiting, and diarrhea. The Scientific Medical Council of the People's Commissariat of Health of the RSFSR allows the use of saccharin in the food industry with certain restrictions, namely, on the packaging and sealing of all kinds of products prepared with saccharin, there must be a label indicating that the product is made with saccharin and that it is not recommended for children, the sick, pregnant women, and the elderly. In medical practice, saccharin is used for sweetening the food of diabetics. The detection of saccharin in drinks and confectionery products comes down to extracting it from an acidified aqueous solution by means of ether, into which it easily passes. After evaporation of the ether extract, a dry residue remains, which is subjected to testing: a) by tasting (sweet taste); b) by conversion of saccharin by fusion with NaOH into salicylic acid and testing for it with a reaction with ferric chloride. If the product itself contains salicylic acid, it is preliminarily destroyed by heating with KMnO4; c) by oxidation of the sulfur contained in saccharin into sulfuric acid with subsequent qualitative and quantitative determination of it in the form of barium sulfate. 1 g of BaSO4 corresponds to 0.7857 g of saccharin.
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“Saccharin.” Soviet Medical Encyclopedia. English translation of Bolshaya Meditsinskaya Entsiklopediya, 1st ed. (Moscow, 1928–1936), ed. N. A. Semashko. https://sovietmedicalencyclopedia.com/article/saccharin/