Acetylcholine chloride

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. If tablets are used, pulverize the tablets to a fine powder, or use

bulk bethanechol chloride powder.

4. Slowly add the Ora-Plus and mix, forming a smooth paste and then a uniform suspension.

5. Slowly add the Ora-Sweet, Ora-Sweet SF, or cherry syrup to volume and mix well.

6. Package and label.

PACKAGING

Package in tight, light-resistant containers.

LABELING

Keep out of reach of children. Use only as directed. Protect from light. Shake well before taking (if tablets are used).

STABILITY

A beyond-use date of 60 days can be used for this preparation.1,2

USE

Bethanechol chloride oral liquid is used for its cholinergic effects.

QUALITY CONTROL

Quality-control assessment can include weight/volume, pH (pH 4.0 to 4.8 for the "Ora" family of vehicles and 2.6 to 3.4 if cherry syrup is used), specific gravity, active drug assay, color, clarity, rheological properties/pourability, physical observation, and physical stability (discoloration, foreign materials, gas formation, mold growth).1

DISCUSSION

Bethanechol has a myriad of actions in the body due to its cholinergic activities, including increased tone and peristaltic activity in the stomach/intestines, increased esophageal peristalsis, increased resting pressure of the lower esophageal sphincter, increased pancreatic and gastrointestinal secretions, contraction of the detrusor muscle of the urinary bladder, decreased bladder capacity, and increased frequency of ureteral peristaltic wave.4

Bethanechol chloride (C^sub 7^H^sub 17^ClN^sub 2^O^sub 2^, MW 196.68, Urecholine, Myotonachol) is a synthetic ester that is related both structurally and pharmacologically to acetylcholine. Since bethanechol is more stable to the hydrolytic action of cholinesterase than acetylcholine, it has a more prolonged duration of action than acetylcholine. It occurs as colorless or white crystals or as a white, crystalline powder usually having a slight, amine-like odor. It is hygroscopic and exhibits polymorphism; one crystalline form melts at 211°C and the other at about 219°C. It is freely soluble in water and in alcohol/ Bethanechol chloride is available as 5-, 10-, 25-, and 50-mgoral tablets and as a 5-mg/mL injection. The tablets (Urecholine) also include calcium phosphate, lactose, magnesium stearate, and cornstarch. The 10-mg tablets contain FD&C Red 3 and FD&C Red 40. The 25- and 50-mg tablets contain FD&C Yellow 10 and FD&C Yellow 6.5

Ora-Plus is an oral suspending vehicle with a pH of approximately 4.2 and an osmolality of about 230 mOsm/kg. It is thixotropic, with a viscosity of approximately 1,000 cps at 25°C. It contains purified water, microcrystalline cellulose, sodium carboxymethylcellulose, xanthan gum, carrageenan, sodium phosphate and citric acid as buffering agents; simethicone as an antifoaming agent; and potassium sorbate and methylparaben as preservatives.6

Ora-Sweet syrup is a flavoring vehicle with a citrus-berry flavor blend. It is buffered to a pH of approximately 4.2 and has an osmolality of about 3,240 mOsm/kg. It contains purified water, sucrose, glycerin, sorbitol (5%), flavoring, sodium phosphate and citric acid as buffering agents, and potassium sorbate and methylparaben as preservatives.7

Ora-Sweet SF is a sugar-free vehicle with a citrus-berry flavor blend. It is buffered to a pH of approximately 4.2 and may be used alone or in combination with other vehicles. It has an osmolality of 2,150 mOsm/kg. It contains water, sodium saccharin, xanthan gum, glycerin, and sorbitol; citric acid and sodium citrate as buffers; methylparaben, propylparaben, and potassium sorbate as preservatives; and flavoring agents.8

Cherry Syrup NF consists of cherry juice (475 mL), sucrose (800 g), alcohol (20 mL), and purified water (to make 1000 mL). It should be preserved in tight, light-resistant containers. Exposure to excessive heat should be prevented. It contains 1% to 2% alcohol.2

References

1. Allen LV Jr, Erickson MA III. Stability of bethanechol chloride, pyrazinamide, quinidine sulfate, rifampin, and tetracycline hydrochloride in extemporaneously compounded oral liquids. Am J Health Syst Pharm 1998; 55(17): 1804-1809.

2. US Pharmacopeial Convention, Inc. USP-Pharmacists' Pharmacopeia. Rockville, MD: US Pharmacopeial Convention, Inc.; 2005:362,408-431,672.

3. Allen LV Jr. Standard operating procedure for quality assessment of oral and topical liquids. IJPC 1999; 3(2): 146-147.

4. McEvoy GK, ed. AHFS Drug Information-2005. Bethesda, MD: American Society of Health-Systems Pharmacists; 2005:1209-1210.

5. [No author listed.] Physicians' Desk Reference. 58th ed. Montvale, NJ: Thomson PDR; 2004: 2095-2096.

6. Ora-Plus [product information]. Minneapolis, MN: Paddock Laboratories, Inc.

7. Ora-Sweet [product information]. Minneapolis, MN: Paddock Laboratories, Inc.

8. Ora-Sweet SF [product information]. Minneapolis, MN: Paddock Laboratories, Inc.

Copyright International Journal of Pharmaceutical Compounding Nov/Dec 2005
Provided by ProQuest Information and Learning Company. All rights Reserved