FAQs - Minoxidil 12.5% Solution

Q. If propylene glycol is the component that makes Rogaine®/Regaine Extra Strength® and its generic versions feel greasy and take so long to dry, how is it your new 12.5% solution containing propylene glycol doesn't feel greasy and dries rapidly?  
A. The non-greasy feeling and the ability to dry rapidly are directly related to the proportions of propylene glycol and 200-proof ethyl alcohol in the base.  These are miscible liquids. The new 12.5% Minoxidil Solution has a fraction of the amount of propylene glycol and a larger component of ethyl alcohol than are present in Rogaine®/Regaine Extra Strength® solution and its generics.

Q. Why not compound the new 12.5% Minoxidil Solution without any propylene glycol?
A. Alcohol based minoxidil solutions with a concentration of 5% or more minoxidil require propylene glycol or glycerin or other such vehicles in the base to remain stable. Because it is so viscous, even a small amount of glycerin in a minoxidil solution will result in the solution having a bit of a "greasy feeling."

Q. Can you cite a scientific reference demonstrating that higher doses of topical minoxidil improve the results in the treatment of MPB?  
A. An excellent study relating dosage to results was reported in this article: Olsen, EA, DeLong ER, Weiner MS. Dose-response study of topical minoxidil in male pattern baldness. J Am Acad Dermatol. 1986;15:30-37.  

Q. Why is a 12.5% Minoxidil Solution more effective than other 12.5% minoxidil lotions, creams or gels?  
A. The absorption of minoxidil from a cream, gel or lotion is less efficient than with a solution because only the molecules directly adjacent to the skin can absorb into the scalp. In a true solution, such as the 12.5% Minoxidil Solution, the solute (minoxidil molecules), move freely within the solvent, whereas in a cream, lotion or gel, a substantial quantity of the minoxidil molecules remain suspended and unavailable within the viscous base.

Q. If more minoxidil absorbs into the scalp with the new 12.5% minoxidil solution than with a lotion, cream or gel, why do you still offer Xandrox 12.5% lotion®?  
A. Xandrox® formulations are notably different from minoxidil compounds. All Xandrox® products contain azelaic acid to decrease DHT in the scalp.   

Q. How safe is it to use a 12.5% Minoxidil Solution? 
A. Less than 0.1 % of patients experience side effects from 12.5% Minoxidil Solution. There is a reason for this high safety margin. It requires a serum concentration of 20 ng/mL of minoxidil to cause any hemodynamic or other systemic effect in the human body. Allowing for the average 1.4% absorption of minoxidil from topical application, a 5% minoxidil solution will result in 1.16 ng / mL of minoxidil in the serum and a 12.5% solution will result in a 2.9 ng / mL of minoxidil in the serum level. So, there is more than a 16-fold safety margin from the use of 5% topical minoxidil and a 7-fold safety margin from the use of 12.5% Minoxidil Solution.

Q. Can the 12.5% Minoxidil Solution be used twice / day?  
A. For almost all patients, yes. The safety margin with 1mL of the 12.5% Minoxidil Solution applied twice per day allows for the recommended routine use of topical minoxidil for the treatment of MPB.

Q. Is the 12.5% Minoxidil Solution an alcohol based solution?  
A. Fifty percent of the solvent base is 200 proof denatured ethyl alcohol. The ethyl alcohol allows optimal absorption into the scalp and dries quickly. . 

Q. Does the alcohol in the solution harm the skin or hair follicles?  
A. Not at all. When you apply the recommended 1mL of the 12.5% Minoxidil Solution to your scalp, the total amount of alcohol in the dosage is, at most, 0.5mL. That's a very small quantity of alcohol, which will neither be harmful to the hair follicles nor to the skin. When alcohol, e.g. rubbing alcohol, is applied to the skin, it is quickly absorbed and diluted by the body fluids and there is no harm to the body tissues.

Q. Why is phosphoric acid an ingredient of the 12.5% Minoxidil Solution?  
A. Phosphoric acid is an inorganic acid commonly used in cosmetic products to enhance their water retention. As an ingredient in the 12.5% Minoxidil Solution, the phosphoric acid serves several important functions. (1) It helps to stabilize the minoxidil, which is more soluble in an acidic base. (2) Retaining water in the 12.5% Minoxidil Solution has an effect similar to hydrating the scalp and enhances the absorption of minoxidil. And (3), Stabilizing the acidity of the 12.5% Minoxidil Solution balances the pH to approximate the pH of the skin, which is optimal at a pH of ~5.5. This degree of acidity helps the skin to ward off the advances of harmful bacteria and fungi.

Q. Are there any patients who should not use the 12.5% Minoxidil Solution?  
A. Patients who have untoward reactions to minoxidil or to any of the ingredients in the base should not use 12.5% Minoxidil Solution. Also patients who are hypersensitive to the action of minoxidil should not use the 12.5% Minoxidil Solution.

Side Effects: Patients with any history of heart disease should not use Xandrox® formulas or minoxidil.  Also patients who have a known adverse reaction to minoxidil should avoid using Xandrox® formulas or minoxidil. Although rare, patients who are sensitive to minoxidil can experience a rapid heart rate, a drop in blood pressure and water retention. As a result, they may experience headaches, dizziness, chest pain and/or edema of the ankles. If that happens, these patients should discontinue use of any formulas containing minoxidil. In our experience, these side effects have occurred in less than 0.1% of patients.

Q. If minoxidil is soluble in alcohol only to ~5%, how can you make a true 12.5% solution?  
A. According to Remington’s Pharmaceutical Science (20th Edition), minoxidil is soluble to the extent of "1gm in 25ml alcohol” (4% solution). When the solution is acidified, for example by azelaic acid, the solubility is increased to approximately 5%. With the addition of propylene glycol or glycerin, a true 5% minoxidil solution can be stabilized.

Making a 12.5% minoxidil solution is much more complicated and the compounding technique is going to have to remain a closely guarded trade secret.  After years of personal research and experimentation, an international patent (PCT/US2003/041196) is pending for our technique of compounding higher (much greater than 5%) alcohol-based solutions of minoxidil.

Q. If it's possible to make a 12.5% Minoxidil Solution, why not increase the concentration even more? Wouldn't a higher concentration make the medication even more effective in treating MPB?  
A. Not necessarily. As previously noted, the increased efficacy of minoxidil in promoting hair growth is not directly proportional to the increases in the concentrations of minoxidil. There are diminishing returns. In fact, in a study reported in Skin Pharmacology [Skin Pharmacol 1997;10(4):206-20] it was shown that 'minoxidil had biphasic effects on the proliferation and differentiation of normal human keratinocytes (NHK): Minoxidil stimulated NHK proliferation at micromolar doses, while antiproliferative, pro-differentiative and partially cytotoxic effects were observed with millimolar concentrations.'  In other words, too much minoxidil can become counter productive in promoting hair growth.  

Q. If I shouldn't use Xandrox 15% Solution® twice / day, why can I use 12.5% Minoxidil Solution twice a day?  
A. The reason Xandrox 15% Solution® is not recommended for twice/day use is that the addition of azelaic acid results in a solution that has a sticky residual and may cause the hair to look unkempt. For that reason alone, it is suggested that Xandrox15 Solution® be applied at night. If a patient is not hypersensitive to minoxidil, there is no safety issue with the application of either Xandrox 15 Solution® or 12.5% Minoxidil Solution twice /day.   

Q. How stable is the 12.5% Minoxidil Solution?  
A. Extremely stable. Before making the 12.5% Minoxidil Solution available on the market, batches of the solution were subjected to temperatures up to 149o Fahrenheit (65o Celsius) and were also stored for months in sub-freezing temperatures with no change in the chemical or physical characteristics of the solution.

Q. Under what conditions should the 12.5% Minoxidil Solution be stored?  
A. The 12.5% Minoxidil Solution should be stored with the container's cap tightly attached, at room temperature and out of direct sunlight.      

Q. Can the 12.5% Minoxidil Solution be used by both males and females?  
A. Yes. For optimal results, it is recommended that male patients use the 12.5% Minoxidil Solution in combination with an agent or agents that decrease the DHT in the scalp. The 12.5% Minoxidil Solution can be used as the sole medication in the treatment of female pattern baldness (FPB), but should not be used by nursing mothers.