E-Mail:
REGROWTH@minoxidil.comAn Important
Announcement from Richard Lee, M.D.
12.5% Minoxidil Solution
Please scroll to bottom of this page for facts regarding availability of the new solution
It was a frustrating and humbling ordeal to postpone the availability of the 12.5% Minoxidil Solution, but after many months of exhaustive experimentation, it has finally been possible to compound a safe, effective, stable and cosmetically acceptable high concentration minoxidil solution. Thank you for your patience.
Please scroll to bottom of this page for facts regarding how to order the new solution
Good news. After years of intensive research, exhaustive experimentation, assistance from a consulting pharmaceutical biochemist and extensive clinical testing, Regrowth is able to offer 12.5% Minoxidil in a solution form, which is a stable, close to colorless, non-greasy liquid that dries rapidly after it has been applied.
To date, topical minoxidil is the only FDA approved, safe and effective medication that is a non-specific promoter of hair growth. When topical minoxidil is used in conjunction with a medication or medications, which decrease the amounts of DHT in the scalp, the treatment of MPB is effective for most patients.
There are many benefits to using the 12.5% Minoxidil Solution: (1) Success with topical minoxidil in promoting hair growth is dose dependent. (2) In solution form, more minoxidil absorbs into the scalp than in lotion, cream or gel compounds of minoxidil. (3) The 12.5% Minoxidil Solution has a smooth, pleasant quality. (4) The 12.5% Minoxidil Solution can be applied twice per day without compromising the aesthetic appearance of the hair. (5) For patients beginning treatment of MPB, the high concentration of minoxidil is more likely than the standard 5% minoxidil solutions to recruit more miniaturized hair follicles to mature again. (6) And for those patients who have been using 5% minoxidil for more than two or three years, better maintenance or new recruitment of hair follicles to mature again is more likely with the 12.5% Minoxidil Solution.
FAQ's
Q. If propylene glycol is the component that
makes Rogaine 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 as greasy and dries rapidly?
A. The 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 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 "greasy feeling."
It is for this reason that propylene glycol was used, as it has a less "greasy
feeling" to it, than does glycerin. The new 12.5% minoxidil solution has
about the same "feel" to it, as does Rogaine Extra Strength®
solution.
Q. How does minoxidil work to promote hair growth?
A. Despite decades of widespread use, exactly how minoxidil works to promote hair growth is not understood. One of the most comprehensive articles, entitled 'Hair growth effect of minoxidil' was published in 2002 (Nippon Yakurigaku Zasshi. 2002 Mar; 119(3): 167-74). "The mode of action of hair growth effect of minoxidil is not completely elucidated, but the most plausible explanation proposed here is that minoxidil works as a sulfonylurea receptor (SUR) activator and prolongs the anagen phase of hair follicles."
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 a 12.5% minoxidil lotion, cream or gel?
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. 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 going to be at most 0.5mL. That's a very, 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 very quickly absorbed and diluted by the body fluids and there is no harm to the body tissues.
Q. What is phosphoric acid? And why is it 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.
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 becomes counter productive in promoting hair growth.
Q. If I shouldn't use Xandrox15 twice / day, why can I use 12.5% twice a day?
A. The reason Xandrox15 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 be applied at night. If a patient is not hypersensitive to minoxidil, there is no safety issue with the application of either Xandrox15 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. It is rich amber in color. As you may know, amber comes in different shades, from light green, to yellow, to wine red.
Q. What is the explanation for why minoxidil products can
vary in color?
A. There are two reasons for the variations in color of
minoxidil solutions. (1) Pure minoxidil crystals are white with a slightly
yellowish hue. When the minoxidil crystals are milled, i.e. micronized, trace
elements can be introduced which result in a change in hue for minoxidil
solutions. The color change in no way affects either the efficacy or the safety
of the minoxidil compounds. As an analogy, consider the diamond. Not all
diamonds are colorless. Diamonds can be blue or yellow or pink, etc. Again, the
color is due to the presence of trace elements, but there is no significant
change in the chemical or physical composition of the gem. (2) With
passing time, all minoxidil solutions become darker, approaching a deep amber
color. Even though minoxidil is essentially insoluble in water, the addition of
water in the formulation of a minoxidil solution helps to stabilize the solution
and to preclude precipitation of the minoxidil. With the passage of time,
the hydration of the minoxidil molecule in solution form changes the refractory
characteristics, resulting in a yellowish cast that can intensify rapidly,
especially with increases in the ambient temperature. The color change in no way
affects either the efficacy or the safety of the minoxidil compounds. There is
an analogous example in the color of water when it freezes. The change in the
physical characteristics makes a difference in the way the water refracts light.
As rain, it is clear. As snow, it is white. But there is no change in the
chemical characteristics. It is still H2O.
Q. What are the physical characteristics of the 12.5% Minoxidil Solution?
A. The 12.5% Minoxidil Solution is odorless and non-viscous. It does not have the greasiness of Rogaine Extra Strength® 5% minoxidil solution or the generic versions of it.
Q. Can the 12.5% Minoxidil Solution be used by both males and females?
A. Absolutely, 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.
Q. What should male patients use to decrease the dihydrotestosterone (DHT) in the scalp?
A. There are many medications, which have been shown to decrease DHT in the scalp. These include topical azelaic acid, topical spironolactone, ketoconazole shampoo, oral finasteride, etc. Recent observations suggest shampoos with 1% pyrithione zinc (Denorex, Head & Shoulders, DHS, etc.) may also be helpful in decreasing DHT in the scalp.
Q. Is Proscar (5 mg finasteride) available in a generic form?
A. If you access the Teva Pharmaceutical website (http://www.tevapharm.com/pr/2004/pr_485.asp), you will read "Jerusalem, Israel, October 27, 2004 - Teva Pharmaceutical Industries Ltd. (Nasdaq: TEVA) announced today that the U.S. Food and Drug Administration has granted tentative approval for the Company's ANDA (Abbreviated New Drug Application) for Finasteride Tablets USP, 5 mg. Final approval is subject to the expiration of patent protection on June 19, 2006 and any exclusivity period."
Q. How much does the new 12.5% Solution cost?
A. A large, 125 mL bottle of the new 12.5% Solution will costs $67.00.
Q. I just received my order for Product Y. Can I exchange product Y for the new 12.5% Solution?
A. When prescription drugs are returned, even if they haven't been opened, they must be destroyed. The law clearly states we cannot exchange one prescription drug for another.
Q. I live outside the U.S.A. Can I order the new 12.5% solution?
A. Check in the Secure Order Form for your specific
country. If the new 12.5% Solution doesn't appear in your country's list
of products, it will in the not distant future.
15 December 2006
The new 12.5% Minoxidil Solution is now available to my patients, and appears as product number 700 in the Secure Order Form on this web site.
Thank you,
Richard Lee, M.D.
Consulting Physician
Regrowth
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