?-(Trimethylsilyl)-?-methylpolyoxy(dimethylsilylene), mixture with silicon dioxide.
>> Simethicone is a mixture od fully methylated linear siloxane containing repeating units of the formula -(CH3)3 SiO- and silico dioxide. It contains not less than 90.5 percent and not more than 99.0 percent of polydimethylsiloxne (-(CH3)2SiO-n) and not less than 4.0 percent and not more than 7.0 percent of silicon dioxide.
Packaging and storage – Preserve in tight containers.
Foaming solution- Dissolve 1 g of octoxynol 9 in 100 mL of water
Test preparation- Transfer 200 mg of Simethicone to a 60-mL bottle, add 50 mL of tertiary butyl alcohol, cap the bottle, shake vigorously.
Procedure- Dropwise add 500 mL of the test preparation to a lean cylindrical 250-mL glass jar, fitted with a cap containing 100 mL of the Foaming solution. Cap jar and clamp in an upright position on a wrist-action shaker. Shake for 10 seconds at a frequency of 300 strokes, recording the time it takes for the foam to collapse back.
Chewable Tablets (It can be better absorbed, increasing bioavailability and rapid disintegration) — sealed in blister packets
Active Ingredient: Simethicone———125mg (in each tablet)
Fillers: Calcium phosphate tribasic- 45mg, colloidal silicon dioxide (coating of tablets)
Dye/Color: D&C No. 30 Aluminum Lake
Flavor/ Binding Agent: Dextrose (simple sugar made from corn), can also increase person’s sugar level.
Lubricant: Propylene glycol
The drug that I chose was a chewable tablet because it is used for the purpose to relieve gas and give comfort quickly, so a rapid absorption would give in faster results. It has an active ingredient simethicone, whose molecular weight is 222.462 g/mol. Some characteristics of simethicone is that has polar and non-polar groups (oxygen and methyl), it is an anti-foaming agent with the “intent of therapeutic use for anti-gas/anti-bloating agent” and it has a topological polar surface area of 43.4 A2. Some inactive ingredients were calcium phosphate tribasic, colloidal silicon dioxide, D aluminum lake, maltodextrin, propylene glycol and soy protein isolate.
Calcium phosphate tribasic is used as a filler along with the active ingredient to make the bulk powder, it is an insoluble filler with no therapeutic effect. In general calcium phosphate reacts with the acid in the stomach to raise pH, in this case it is used as diluent as it is a polar compound that can interact with simethicone to form as a mixture. Colloidal silicon dioxide can be used as a filler but also as a coating for the tablets. D Red 30 aluminum lake is used as a dye for drugs generally to give the color of the tablet. Dextrose a form of sugar is used as a binding agent to make all the ingredients compatible and bring it together during the dry granulation. Maltodextrin are composed of water soluble glucose polymers which are obtained from the reaction of starch with acid. The amount of simethicone and maltodextrin plays a role in keeping the tablet preserved. According to European Patent, “A 30% by weight of simethicone to 70% by weight of maltodextrin ratio represents the prefect product performance for tableting”. Propylene glycol is used as a lubricant to enhance the flow of powder as it passes through the GIT. According to European medicines agency (2014), “Propylene glycol has a wide range of applications in food and drug, it is used as an excipient in a variety of drugs (p. 4)”.
Steps in preparation of the tablet according to European patent as well an example of a formula
“The simethicone and calcium phosphate admixture composition are conveniently prepared by a dry blend procedure. The calcium phosphate tribasic is first granulated either by dry compaction. Next, the simethicone compound is added to a moving bed of tribasic calcium phosphate so that the simethicone is uniformly distributed. The bed is kept in motion by low shear mixers. After the tribasic calcium phosphate bed has absorbed the simethicone and a finely divided granular composition is maintained, the silicon dioxide powder may be added. The granulation may then be screened through a No. 20 US Standard screen (about 840 microns). The solid oral dosage forms of the present invention may be prepared in the form of tablets, gel caps, capsules, chewable tablets, and other known and effective delivery modes. The free-flowing simethicone/tribasic calcium phosphate composition may be admixed with a variety of pharmaceutically acceptable excipients including fillers, binders, sweeteners, artificial sweeteners, lubricants, glidants, disintegrants, colors, and flavoring agents. The choice of excipient will depend on the solid oral dosage form (i.e. tablets, caplets, or capsules) and whether the dosage form is chewable or a swallow able formulation. Swallow able oral tablets prepared by direct compression are preferred” (pp.18).