SARMs taste masking
Selective Androgen Receptor Modulators (SARM) are a novel class of androgen receptor ligands, possessing a non-steroid anabolic effect. Despite the fact that SARMs are illegal, they have been used by athletes of gymnastics lovers for bodybuilding and fitness. SARMs are insoluble in water and hence, organic solvents or solubilization approaches are used instead. Typical values for solubility of SARM in those solvents are presented below. SARM’s solubility might change for the same chemical because of solvent of crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature, and dissolved oxygen.
Users commonly follow a cycle-therapy according to a daily dosage. This dosage is usually calculated empirically (by evaluating the outcome of the tested dosage). The dosage is approximately 20 mg per day. People prefer making liquid formulations (e.g., 20 mg/mL dissolution medium) than measuring every day at this accuracy the amount needed. In order to make liquid formulations from SARM powder, one needs an organic solvent, such as DMSO, DMF, ethanol, to dissolve the powder.
Suppliers give detailed product information regarding the solubility of the SARM in different solvents. Because of the forbidden usage of SARMs, there are not specific formulas with instructions on how to effectively make liquid SARMS. On the other hand, commercial aqueous solutions of SARMs do not always guarantee user's daily dosage. For this reason, people involved with SARMs make their own liquid formulations which suffer from failed measurements, insufficient mixing, contamination effects and undesired binding and aggregation. Furthermore, the presence of organic solvent and drug has a "bad" taste and results in "bad" odor as well. The addition of sweeteners does only eliminate about 20-25 % of the bitterness. Over the past decades, great interest has been expressed in taste and/or odor masking of bitter taste products both in food and pharmaceutical industry. In general, such taste masking in the pharmaceutical industry is based on one of the following approaches:
1. Taste masking: addition of flavors and or sweetening agents, liquid syrups (e.g., fructose corn syrup).
2. Solubility modification: renders the drug insoluble in the liquid base, not accessible to taste receptors in the mouth, sugar alcohols could be used for this purpose.
3. Adsorption/ loading of the drug onto the surface of a carrier (e.g., clays or inorganic phosphates).
4. Complexation: maintains the drug in a sequestered state while in the mouth, yet still allowing for dissolution and absorption in the stomach and gastrointestinal tract.
5. Barrier systems: physically remove the drug from exposure to the taste buds.
We were asked to come up with a solution for the known problem of the removal of SARMs’ taste and odor for a commercial product. We worked on solubilization enhancement by two parallel pathways, without using any sweeteners in the process. We succeeded into producing a fully soluble aqueous formulation of SARM, with a solubility comparable to the most suitable organic solvents, with a simultaneous disappearance of the taste and odor effect. Our work resulted to a very successful formulation with potential variations. SARMs’ solubilities have been confirmed by a series of testing in the manufacturer’s facilities.