Simethicone

Production Methods

The method is mixed with Simethicone by silicon-dioxide, stirs, and is heated to 150 DEG C ± 5 DEG C, stirring reaction 4 ~ 5 hours and get final product. This method utilizes heat expansion principle, and silicon-dioxide is fully dissolved in Simethicone. Silicon dioxide is initially rendered hydrophobic in one of a variety of proprietary processes specific to a particular manufacturer. It is then slowly mixed with the silicone fluids in a formulation. After mixing, the simethicone is milled to ensure uniformity.

Manufacturing Process

In a 5 liter three-necked flask, fitted with a reflux condenser, agitator and thermometer, were placed 1,393 g (9.41 mold) of redistilled (CH3)2Si(OEt)2 and 1,110 g (9.41 mols) of (CH3)3SiOEt. To this solution was added 254 g (14.11 mols) of water containing 7.5 g of NaOH (approximately 1 NaOH per 100 silicon atoms). This insured the formation of only straight chain polymers. The mixture was heated to 40°C and the temperature continued to rise for nearly an hour. After adding 50 cc (20% excess) more water, the mixture was refluxed for two hours and then allowed to stand overnight.Alcohol was then distilled off, until the temperature reached 100°C. 1,706.6 g of distillate was collected. (Theory 1,430 g.) This alcohol was poured into four times its volume of water and an insoluble oil separated (457 g). The insoluble fraction was added back to the copolymer residue from the distillation and 555 cc of 20% hydrochloric acid was added. The acid mixture was refluxed for two hours, and the silicon oils were carefully washed with distilled water until neutral. The yield was 1,420 g. (Theory 1,409 g.)

Therapeutic Function

Antiflatulent

Pharmaceutical Applications

Simethicone is used to treat the symptoms of too much stomach acid such as stomach upset, heartburn, and acid indigestion. It is also used to relieve symptoms of extra gas such as belching, bloating, and feelings of pressure/discomfort in the stomach/gut. Simethicone helps break up gas bubbles in the gut. The main use of simethicone as an excipient is as an antifoaming agent in pharmaceutical manufacturing processes, for which 1–50 ppm is used. Therapeutically, simethicone is included in a number of oral pharmaceutical formulations as an antiflatulent, although its therapeutic benefit is questionable. It is also included in antacid products such as tablets or capsules. In some types of surgical or gastroscopic procedures where gas is used to inflate the body cavity, a defoaming preparation containing simethicone may be used in the area to control foaming of the fluids. When simethicone is used in aqueous formulations, it should be emulsified to ensure compatibility with the aqueous system and components. In the USA, up to 10 ppm of simethicone may be used in food products.

Safety

Simethicone is used in cosmetics, foods, and oral and topical pharmaceutical formulations, and is generally regarded as a relatively nontoxic and nonirritant material when used as an excipient. Direct contact with the eye may cause irritation. Therapeutically, oral doses of 125–250mg of simethicone, three or four times daily, have been given as an antiflatulent. Doses of 20–40 mg of simethicone have been given with feeds to relieve colic in infants. LD50 (dog, IV): 0.9 g/kg

Brand name

Gas-X (Novartis); Mylanta Gas Relief (Johnson & Johnson-Merck Consumer); Mylicon Infant’s Drops (Johnson & Johnson-Merck Consumer); Sentry Simethicone (Witco); Sentry Simethicone Emulsion (Witco).

Who Evaluation

Evaluation year: 2011