Ergoloid Mesylates

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. Dissolve the ergoloid mesylates in the alcohol.

4. Add the glycerin, propylene glycol and flavor.

5. Add sufficient purified water to about 95 mL and add the saccharin sodium.

6. Add sufficient purified water to volume and mix well.

7. Package and label.

PACKAGING

Package in a tight, light-resistant dropper bottle.1

LABELING

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

STABILITY

A beyond-use date of up to 6 months can be used for this preparation.1

USE

Ergoloid mesylates are indicated in patients with signs and symptoms of an idiopathic decline in mental capacity, including cognitive and interpersonal skills, mood, self-care and apparent motivation.2

QUALITY CONTROL

Quality-control assessment can include weight/volume, pH, specific gravity, active-drug assay, color, clarity, physical observation and physical stability (discoloration, foreign materials, gas formation, mold growth).3

DISCUSSION

Ergoloid mesylates liquid, formerly available as Hydergine by Sandoz Pharmaceuticals Corporation and more recently by Novartis Corporation, is now not commercially available.

Ergoloid mesylates, as described in the United States Pharmacopeia, consists of a mixture of the methanesulfonate salts of the three hydrogenated alkaloids, dihydroergocristine (C^sub 36^H^sub 41^N^sub 5^O^sub 5^.CH^sub 4^O^sub 3^S, MW 707.84), dihydroergocornine (C^sub 31^H^sub 41^N^sub 5^O^sub 5^.CH^sub 4^O^sub 3^S, MW 659.79) and dihydroergocryptine (C^sub 32^H^sub 43^N^sub 5^O^sub 5^.CH^sub 4^O^sub 3^S, MW 673.82) in an approximate weight ratio of 1:1:1. They should be preserved in tight, light-resistant containers. Ergoloid mesylates are described as a white to off-white, microcrystalline or amorphous, practically odorless powder that is slightly soluble in water and is soluble in alcohol.1

Alcohol (C^sub 2^H^sub 5^OH, MW 46.07, ethyl alcohol, ethanol, grain alcohol) is a clear, colorless mobile and volatile liquid with a slight, characteristic odor and a burning taste. It is miscible with chloroform, glycerin, and water.4

Glycerin (C^sub 3^H^sub 8^O^sub 3^, MW 92.10, glycerol, 1,2,3-propane triol) occurs as a clear, colorless, odorless, viscous, hygroscopic liquid with a sweet taste about two thirds as sweet as that of sucrose. It is used as a sweetening agent in alcoholic elixirs (up to 20% concentration). It has a specific gravity of about 1.25. It is miscible with water and 95% ethanol. It is hygroscopic and should be stored in airtight containers in a cool place.5

Propylene glycol (C^sub 3^H^sub 8^O^sub 2^, MW 76.09) occurs as a clear, colorless, viscous, practically odorless liquid somewhat resembling glycerin. It has a sweet taste. It has a specific gravity of 1.038 g/mL and is miscible with acetone, chloroform, 95% ethanol, glycerin and water.6

Saccharin sodium (soluble saccharin, Sucaryl, Sweeta-with Sorbitol) is an intense sweetening agent with a molecular weight of 205 for the anhydrous form. It is a white, odorless or faintly aromatic, efflorescent, crystalline powder with an intensely sweet taste and a metallic aftertaste. A 10% solution has a pH of about 6.6 and a tapped density of about 0.9 to 1.2 g/mL. It decomposes upon heating to a high temperature (125°C) at a low pH (about pH 2). One gram is soluble in about 1.2 mL water, 50 mL of 95% ethanol and 3.5 mL propylene glycol.7

Purified water is water that is obtained by distillation, ion exchange, reverse osmosis or some other suitable process. Water has a specific gravity of 0.9971 at room temperature, a melting point at 0°C and a boiling point at 100°C. It is miscible with most polar solvents and is chemically stable in all physical states (ice, liquid and steam).8

REFERENCES

1. US Pharmacopeial Convention, Inc. United States Pharmacopeia 26-National Formulary 21. Rockville, MD:US Pharmacopeial Convention, Inc.; 2003:718-720, 2197-2201, 2560.

2. [No author listed.] Physicians' Desk Reference. 51st ed. Oradell, NJ:Medical Economics, Inc.; 1997:2392-2393.

3. Allen LV Jr. Standard operating procedure for performing physical quality assessment of oral and topical liquids. IJPC 1999;3:146-147.

4. Weller PJ. Alcohol. In: Kibbe AH, ed. Handbook of Pharmaceutical Excipients. 3rd ed. Washington, DC:American Pharmaceutical Association; 2000:7-9.

5. Price JC. Glycerin. In: Kibbe AH, ed. Handbook of Pharmaceutical Excipients. 3rd ed. Washington, DC:American Pharmaceutical Association; 2000:220-222.

6. Dandiker Y. Propylene glycol. In: Kibbe AH, ed. Handbook of Pharmaceutical Excipients. 3rd ed. Washington, DC:American Pharmaceutical Association; 2000:442-444.

7. Russell G, Thurgood DM. Saccharin sodium. In: Kibbe AH, ed. Handbook of Pharmaceutical Excipients. 3rd ed. Washington, DC:American Pharmaceutical Association; 2000:457-459.

8. Ellison A, Nash RA, Wilkin MJ. Water. In: Kibbe AH, ed. Handbook of Pharmaceutical Excipients. 3rd ed. Washington, DC:American Pharmaceutical Association; 2000:580-584.

Copyright International Journal of Pharmaceutical Compounding Nov/Dec 2003
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