Making a Sildenafil (Viagra) Cream or Gel for Topical Use (e.g., for females)

[Expat98]

In another thread, the subject of topical application of sildenafil (Viagra) on the female clitoris came up. Here is an article about how to make a sildenafil cream or gel.

The steps below are pretty simple, but an even simpler method which SWIM has used in the past with female partners (with mixed results) is to just crush some sildenafil tablets with a mortar & pestle and mix the powder with Astroglide, then spread it around the clitoris area. (Note that sildenafil has a very bitter taste! )

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Sildenafil 1% Vaginal Cream or Gel
International Journal of Pharmaceutical Compounding, Mar/Apr 2005

METHOD OF PREPARATION

1. Calculate the required quantity of each ingredient for the total amount to be prepared.

2. Accurately weigh and/or measure each ingredient.

3. Thoroughly pulverize the required number of sildenafil tablets for the prescription. (A high-speed mill/coffee grinder works well.)

Cream

4a. Add the propylene glycol and purified water to the sildenafil citrate powder, and form a smooth paste.

5a. Incorporate into sufficient hydrophilic ointment (Dermabase, Vanicream) to final weight and mix well.

6a. Package and label.

Gel

4b. Mix the sildenafil and methylcellulose powders with the propylene glycol until uniform.

5b. Warm the purified water to about 70°C and add to the powder-propylene glycol mixture.

6b. Mix well and allow to congeal.

7b.Package and label.

PACKAGING

Package in tight, light-resistant containers.1

LABELING

Keep out of reach of children. Use only as directed.

STABILITY

A beyond-use date of 14 days can be used for this preparation when stored in a refrigerator.1

USE

Sildenafil cream and sildenafil gel have been used to improve uterine artery flow and endometrial development in patients undergoing in vitro fertilization.

QUALITY CONTROL

Quality-control assessment can include theoretical weight compared to actual weight, specific gravity, active-drug assay, color, clarity', texture-surface, texture-spatula spread, appearance, feel, rheological properties and physical observations.2

DISCUSSION

Sildenafil citrate (C^sub 22^H^sub 30^N^sub 6^O^sub 4^S.C^sub 6^H^sub 8^O^sub 7^, MW 666.70) occurs as a white to off-white crystalline powder that is soluble 3.5 mg/mL in water. It is formulated as blue, film-coated rounded-diamond-shaped tablets equivalent to 25 mg, 50 mg and 100 mg of sildenafil for oral administration. The tablets also contain microcrystalline cellulose, anhydrous dibasic calcium phosphate, croscarmellose sodium, magnesium stearate, hydroxypropyl methylcellulose, titanium dioxide, lactose, triacetin and FD&C Blue No. 2 aluminum lake. It is used as oral therapy for erectile dysfunction.3

Propylene glycol (C^sub 3^H^sub 8^O^sub 7^, MW 76.09) occurs as a clear, colorless, viscous, practically odorless liquid with a sweet taste. It is miscible with acetone, chloroform, 95% ethanol, glycerin and water. It is not miscible with fixed oils or light mineral oil; it will, however, dissolve some essential oils.4

Methylcellulose (Methocel) is a practically odorless and tasteless, white to yellowish-white colored granule or powder that is widely used in both oral and topical formulations. It is hygroscopic and practically insoluble in acetone, ethanol, saturated salt solutions and hot water, but is soluble in glacial acetic acid.5

Purified water is water that is obtained by distillation, ion exchange, reverse osmosis or some other suitable process.6

Hydrophilic ointment is a water-washable oil-in-water emulsion base containing methylparaben, propylparaben, sodium lauryl sulfate, propylene glycol, stearyl alcohol, white petrolatum and purified water. It is miscible with water and aqueous.7-8

Dermabase is an unscented, washable, oil-in-water emulsion cream base. It contains purified water (about 45%), mineral oil, petrolatum, cetostearyl alcohol, propylene glycol, sodium lauryl sulfate, isopropyl palniitate, imidazolidinyl urea, methylparaben and propylparaben. It is a smooth, white, water-washable cream with a slight, pleasant odor.9

Vanicream is an oil-in-water emulsion base containing white petrolatum, cetearyl alcohol, ceteareth-20, sorbitol, propylene glycol, simethicone, glyceryl monostearate, polyethylene glycol monostearate and sorbic acid. It is free of dyes, perfume, lanolin, parabens and formaldehyde and is a stable and widely compatible cream.10

REFERENCES

1. US Pharmacopeial Convention, Inc. United States Pharmacopeia 27-National Formulary 22. Rockville, MD: US Pharmacopeial Convention, Inc.; 2004: 2345-2349.

2. Allen LV Jr. Standard operating procedure for performing physical quality assessment of ointments/creams/gels. IJPC1998; 2(4): 308-309.

3. [No author listed.] Physicians' Desk Reference. 58th ed. Oradel, NJ: Medical Economics Inc.; 2004: 2662-2665.

4. Weller PJ. Propylene glycol. In: Rowe RC, Sheskey PJ, Weller PJ, eds. Handbook of Pharmaceutical Excipients. 4th ed. Washington, DC: American Pharmaceutical Association; 2003: 521-523.

5. Allen LV Jr, Luner PE. Methylcellulose. In: Rowe RC, Sheskey PJ, Weller PJ, eds. Handbook of Pharmaceutical Excipients. 4th ed. Washington, DC: American Pharmaceutical Association; 2003: 386-389.

6. Ellison A, Nash RA, Wilkin MJ. Water. In: Rowe RC, Sheskey PJ, Weller PJ, eds. Handbook of Pharmaceutical Excipients. 4th ed. Washington, DC: American Pharmaceutical Association; 2003:672-676.

7. Reilly WJ Jr. Pharmaceutical necessities. In: Gennaro AR, ed. Remington: The Science and Practice of Pharmacy. 19th ed. Easton, PA: Mack Publishing Company; 1995:1402.

8. Block LH. Medicated applications. In: Gennaro AR, ed. Remington: The Science and Practice of Pharmacy. 19th ed. Easton, PA: Mack Publishing Company; 1995:1586.

9. Dermabase [product information], Minneapolis, MN: Paddock Laboratories, Inc.

10.Vanicream [product information]. Rochester, MN: Pharmaceutical Specialties, Inc.

Reputation Comments on this post:

thanks for posting this

[radiometer]

Do any of these references refer to the efficacy of such a cream, or only to technical information regarding how to formulate the compound? If the former, which ones?

[Expat98]

I have not looked at the references, but just judging by the titles and context in which they're cited, I'd be surprised if any of them address the efficacy of topical application for females. (There are probably references out there that do address this though.)

I can tell you SWIM's anecdotal experience. He has tried using both the aforementioned Astroglide mixture and a commercially available (at least in some places) sildenafil jelly that comes in a little one-dose sized packet designed for oral consumption. SWIM has consumed the jelly himself orally, and it tastes terrible, but it works. However, it did not give good results through topical application to a couple of females. It's also a little messy, so this way is not recommended.

The Astroglide mixture did work with a couple of other females, and worked *really* well for one of them. Also, SWIM has a friend who swears by the Astroglide mixture and says his girlfriend loves it. He's the one that gave SWIM the idea to try it.

I don't know why the Astroglide mixture would work better than the jelly...maybe the body absorbs it better with the Astroglide, or maybe they just liked the Astroglide more than anything else.

It seems like this should be a pretty simple thing to decide whether it works well or not, but there are a lot of variables...for example, in at least one of the cases where nothing was felt with the jelly, SWIM recalls that alcohol had been consumed. So it hasn't exactly been a controlled experiment...and the sample size has been small, so further experimentation is in order.

BTW, SWIM could not really ascertain a visible effect on the clitoris for any of the above-mentioned females, but their clitorises (had to look up the plural form of that ) were all very small and/or naturally hard/stimulated anyway, so it was hard to tell.

If anyone else has friends, pets, or lab animals who have tried topical sildenafil, I hope you will post your experience. It's been a couple of years since SWIM gave this a try. He says he will probably do it again some time, but is not in a hurry to do so because the results haven't really been spectacular enough to make it seem like it's worth the bother. SWIM is generally more interested in using drugs to enhance the mental aspects of the sexual experience than the physical ones. (The physical aspects are indirectly enhanced through the heightened mental aspects.)