What Is Codeine Phosphate?

Codeine phosphate, a 17-methyl-3-methoxy-4,5-epoxy-7,8-didehydromorphin-6-alcohol phosphate sesquihydrate. Can be used to treat frequent and severe dry cough medicine.

Codeine phosphate

Codeine phosphate, a 17-methyl-3-methoxy-4,5-epoxy-7,8-didehydrogen

Common name: Codeine phosphate.

Alias: codeine, phosphoric acid

The chemical name is 17-methyl-3-methoxy-4,5-epoxy-7,8-didehydromorphinan-6-alcohol phosphate sesquihydrate. Molecular formula: C18H21NO3 · H3PO4 · 1 & frac12; H20. Molecular weight: 424.39

Method name: Codeine Platycodon Tablets-Codeine Phosphate-High Performance Liquid Chromatography

Scope of application: This method uses high performance liquid chromatography to determine the content of codeine phosphate in codeine Platycodon tablets.

This method is applicable to codeine bellflower tablets.

Principle of the method: The test sample was disintegrated by adding water to ultrasound, dissolved by adding ultrasound to methanol, and then diluted with mobile phase. Then it was subjected to high performance liquid chromatography for chromatographic separation. The ultraviolet absorption detector was used to detect codeine phosphate at a wavelength of 220nm. Peak area and calculate its content.

Reagent:

Methanol

Potassium dihydrogen phosphate

3. Phosphoric acid

Equipment: 1. Instrument

1.1 HPLC

1.2 Column

Octadecylsilane-bonded silica gel is used as a filler, and the number of theoretical plates should not be less than 1000 based on the codeine phosphate peak.

1.3 UV absorption detector

Chromatographic conditions

2.1 Mobile phase: 0.05mol / L potassium dihydrogen phosphate (pH adjusted to 3.0 with phosphoric acid) Acetonitrile = 3.5 1

2.2 Detection wavelength: 220nm

2.3 Column temperature: room temperature

Sample preparation:

Preparation of reference solution

Accurately weigh an appropriate amount of codeine phosphate reference substance, dissolve and quantitatively dilute it with mobile phase to make a solution containing approximately 48 g of codeine phosphate per 1 mL, which is the reference solution.

2. Preparation of test solution

Take 20 tablets for testing, accurately weigh, grind, and accurately weigh an appropriate amount (approximately 12 mg of codeine containing phosphate), put it in a 50 mL volumetric flask, add 2.5 mL of water, disintegrate with ultrasound, add an appropriate amount of methanol, and ultrasound Treat for 10 minutes to dissolve codeine phosphate, let cool, dilute to the mark with methanol, shake well, filter through the membrane, accurately measure 2 mL of the filtrate, place it in a 10 mL volumetric flask, add mobile phase to dilute to the mark, shake well That is the test solution.

Note: "Precision weighing" means that the weighed weight should be accurate to one thousandth of the weighed weight. "Precision measurement" means that the accuracy of measuring the volume should meet the accuracy requirements of the volume pipette in national standards.

Operation steps: Precisely pipet 10 mL of each of the reference solution and the test solution, and inject them into a high-performance liquid chromatograph. Use an ultraviolet absorption detector to measure at a wavelength of 220 nm. Use external standard method with codeine phosphate (C16H21NO3 · H3PO4 · 3). / 2H2O) peak area calculated content.

References: Pharmacopoeia of the People's Republic of China, compiled by the National Pharmacopoeia Committee, Chemical Industry Press, 2005 edition, one, p.74.

This product has a direct inhibitory effect on the cough center of Yannao. Its antitussive effect is strong and rapid, similar to morphine. In addition to its antitussive effect, it also has analgesic and sedative effects.

It selectively suppresses the cough center of the medulla oblongata, and has strong and rapid antitussive effect. It also has analgesic effect, its analgesic effect is about 1/12 to 1/7 of morphine, but stronger than general antipyretic analgesics. Can inhibit the secretion of bronchial glands, can make sputum thick and difficult to cough, so it should not be used for patients with thick sputum.

Codeine and its salts are quickly and completely absorbed from the gastrointestinal tract after oral administration. Its bioavailability is 40% to 70%. It takes effect about 20 minutes after oral administration and Tmax is about 1 hour. It is metabolized by the liver in the body and mainly excreted in the urine. About 10% of the morphine can be replaced by demethylation in the body, and T1 / 2 is 3 to 4 hours.

Tablets: It is easily absorbed by the stomach and intestines after oral administration, and is mainly distributed in the lungs, liver, kidneys and pancreas. This product easily penetrates the blood-brain barrier and can penetrate the placenta.

Occasionally nausea, vomiting, constipation, and dizziness; can also make patients irritable. See below for details:

1. The more common adverse reactions are:

psychological abnormality or fantasy;

Breathing is weak, slow or irregular;

Drinking alcohol while taking it can seriously impair the patient's ability to drive safely. Synergistic with antipyretic and analgesics. Combined with methaqualone, they have a synergistic effect.

This product and

Oral or subcutaneous injection: 15mg-30mg / time, 2-3 times / day. Oral Extreme: 100mg / time. Children, 250 g / kg each time, 4 times a day.

Commonly used in children: analgesic, 0.5-1 mg / kg orally once a day, 3 times a day. The amount of antitussive is 1 / 2-1 / 3. Use with caution in newborns and infants.

Pregnancy class C. Convulsions can occur in pediatric overdose, counteracted by naloxone. Continuous application can be addictive. Use with caution in patients with thick sputum.

2010 Chinese Pharmacopoeia revised and updated content

Codeine phosphate

Linsuan Kedaiyin

Codeine Phosphate

Page number: 2005 Part Two of Chinese Pharmacopoeia -870

[Updated]

[Inspection] Take this product, dissolve and dilute it with mobile phase to make a solution containing 10mg per 1ml as the test solution; take an appropriate amount of morphine reference substance, accurately weigh, dissolve and dilute it with mobile phase to make each A solution containing 1 mg in 1 ml was used as a reference solution. Accurately take 0.2ml of the test solution and 1ml of the reference solution into the same 100ml volumetric flask, use mobile phase to make up to the mark, shake well, and use it as the control solution. According to

Boy drinking codeine phosphate cough water atrophy 10 cm:

"Cough water" mainly refers to a compound oral solution containing codeine phosphate. It is a prescription medicine for cough. Codeine contained in cough water is one of the narcotic drugs listed in the United Nations Single Convention on Narcotic Drugs of 1961. In Guangdong, the 20-year-old Qiangzi obviously lost her spine during the abuse of "cough water" and her ability to bear weight decreased significantly. Due to severe calcium loss, height has shrunk from 1.72 meters at the highest height to 1.60 meters. In addition, Qiang Zi also suffered from gastric ulcers, intestinal dysfunction, liver damage and kidney stones.

According to the doctor, Qiangzai abused cough medicine from the age of 12, ranging from seven or eight bottles per day to as many as 20 bottles of 120ml per bottle. Based on an average of 1,000ml per day, Qiangzai drank at least three tons of cough water every year. many. Qiang Zi has a history of drug abuse for up to eight years. ^[1]