Dear colleagues, during the winter season when the weather gets cold, we will examine together this formula in syrup form, which is used for persistent, dry coughs and is subject to a red prescription (controlled drug prescription) because it contains codeine.
Rp
Codeine phosphate 500 mg
Purified water 10 ml
Glycerol 20 ml
Methyl hydroxybenzoate solution 1 ml
Syrup to 100 ml
Substances in the formula
Codeine phosphate-Codeine dihydrogen phosphate-Anhydrous codeine phosphate:
Codeine occurs as colorless crystals or a crystalline powder. Its melting point is between 155-159°C. It slowly effloresces into a powder in dry air. It is affected by light. It is sparingly soluble in water (1:20); soluble in boiling water; soluble 1:2 in alcohol, 1:0.5 in chloroform, and 1:50 in ether. The pH of its 0.5% aqueous solution is higher than 9. Codeine is an opioid agonist. It exists in the form of phosphate or sulfate salts. Both of these salts can be administered orally, subcutaneously, or intramuscularly. Codeine is the drug with the highest bioavailability among orally administered opioids. The potency of parenteral preparations is greater than that of oral preparations. Oral preparations can show approximately two-thirds of the potency of parenteral preparations. It is used alone or in combination with acetaminophen and similar drugs for mild to moderate pain. It is also used as a cough suppressant and an antidiarrheal agent. Codeine administration is controlled under regulations specific to addictive drugs and is prescribed on a red prescription. Opioid agonists also exhibit other clinical effects such as cough suppression, hypotension, and nausea/vomiting. The antitussive effects of opioid agonists are due to their direct action on receptors located in the cough center in the medulla. Cough suppression occurs at lower doses than those required for analgesic effects. The hypotension they cause is likely related to increased histamine release and/or depression of the vasomotor center in the medulla. Their emetic effects likely stem from direct stimulant activity on the “chemoreceptor trigger zone (CTZ)”. Codeine is administered orally and parenterally. Its pharmacokinetics do not vary depending on its salts. Phosphate and sulfate salts share the same pharmacokinetics. Codeine is well absorbed when administered orally and parenterally. Its effect is observed 10-30 minutes after parenteral administration and 30-60 minutes after oral administration. The maximum analgesic effect it provides is seen 30-60 minutes after intramuscular administration and 60-90 minutes after oral administration. Its analgesic effect lasts about 4-6 hours. It binds to plasma proteins at a rate of approximately 7%. It is primarily metabolized in the liver; metabolism takes place via demethylation and conjugation with glucuronic acid. The elimination half-life of codeine is 3-4 hours, while that of its active metabolite morphine is approximately 2 hours. However, the actual amount of codeine metabolized into free morphine is low (likely less than 10%). Elimination occurs via the renal route as unchanged drug, norcodeine, and free and conjugated morphine. Fecal excretion is negligible.
Purified water- Aqua destillata- Eau distillée- Distilled water
Glycerol-Glycerine-Glycerol; – 85%
Glycerin is a clear, colorless or very pale-colored, hygroscopic, syrupy liquid that is odorless or has a very faint odor and a sweet taste. It is miscible with water and alcohol; slightly soluble in acetone; practically insoluble in chloroform, ether, fixed oils, and essential oils. Its aqueous solutions are neutral to litmus. According to the United States Pharmacopeia (USP), the pH of Glycerin Oral Solution, USP is between 5.5-7.5. Strong oxidizing agents form explosive mixtures with glycerin.
Methyl hydroxybenzoate solution-methylparaben– 4-hydroxybenzoic acid methyl ester – E218
Methylparaben is widely used as an antimicrobial preservative in pharmaceutical formulations, cosmetic products, and food products. It is used alone or in combination with other parabens or other antimicrobial agents. It is the most commonly used preservative, especially in cosmetics. In the presence of nonionic surfactants, its antimicrobial activity is significantly reduced. The estimated acceptable daily intake (ADI) for methyl, ethyl, and propylparaben is reported as 10 mg per kg of body weight. Methylparaben occurs as odorless or faintly odorous colorless crystals or a white crystalline powder. It is freely soluble in ethanol, methanol, ether, and propylene glycol; sparingly soluble in water; practically insoluble in liquid paraffin.
Syrup
SIMPLE SYRUP–SIROP SIMPLE
SYRUPUS SIMPLEX T.K.(1954) TF (1974)
Sugar ………… 64 g
Water……………….36 g
Preparation of the formula
After codeine, whose solubility increases in hot water, is dissolved, it is mixed with the addition of glycerol into the previously prepared simple syrup, and the formula is completed with methylparaben added as a preservative.
Codeine syrup, used as an antitussive for sedative cough relief, should be stored protected from light in tightly closed containers at a temperature of 25°C unless otherwise specified. Once prepared, the formula must be consumed within 28 days. It should be administered at a dose of 5 ml. It must be used with caution in individuals operating motor vehicles and heavy machinery, as it will create a sedative effect. It should not be forgotten that its effect will increase with alcohol.
Wishing you a great week…
SOURCE: 8-Australian Pharmaceutical Formulary
Specialist Pharmacist Ahmet Nezihi Pekcan
Pekcan Pharmacy – Konya
[email protected]
Tel: (332) 3520657
Fax: (332) 3512816
http://www.majistralformul.com/
