Name | CHOLINE THIEOPHYLLINATE |
Synonyms | choledyl choledylsa400 cholinophylline theophyllinecholinate cholinetheophyllinesalt CHOLINE THIEOPHYLLINATE theophyllinesaltofcholine |
CAS | 4499-40-5 |
EINECS | 224-798-7 |
Molecular Formula | C12H21N5O3 |
Molar Mass | 283.33 |
Melting Point | 176-178 °C |
Physical and Chemical Properties | Chemical properties white crystalline powder. Melting point 187-192 ℃. Easily soluble in water, soluble in ethanol, slightly soluble in ether and chloroform. Slightly amine smelly, salty and bitter. |
Use | The use is the same as theophylline, used for cardiac or bronchial asthma, cardiac renal edema and other diseases. |
HS Code | 2939590000 |
Raw Materials | Choline hydroxide Theophylline Choline bicarbonate |
medicinal properties and applications
Choleophylline is a molecular compound of theophylline and choline, with high solubility, low irritation, rapid oral absorption and long maintenance time. The effect is similar to that of aminophylline, which has the effects of relaxing bronchial and vascular smooth muscle, strengthening the heart and diuresis. Bronchodilation is weaker than aminophylline and has less impact on the heart and nervous system. Oral absorption is rapid, less irritating to gastric mucosa, and the action time is longer. It is suitable for the treatment of bronchial asthma, and also for the treatment of cardiogenic asthma, angina pectoris, biliary colic and cardiac edema. Not applicable to authors of persistent asthma or acute bronchospasm.
Theophylline
theophylline (theophylline) has been used to treat asthma for more than 50 years. It is the most widely used anti-asthma drug in the world. Up to now, many countries and regions still use theophylline as the first-line antiasthmatic drug in clinical practice. However, the efficacy of this type of drug in the treatment of chronic asthma is still controversial, and some developed countries have used it as a third-line antiasthmatic drug. In recent years, low-dose theophylline has been found to have anti-inflammatory and immunomodulatory effects, which has once again aroused great interest in theophylline drugs. The pharmacological effects of theophylline drugs are extremely extensive. In addition to relaxing bronchial smooth muscle, it also has the effects of exciting the respiratory center, enhancing the contractility of the diaphragm, strengthening the heart and diuresis, reducing pulmonary vascular tension and reducing pulmonary vascular exudation. In addition, recent studies have shown that theophylline has airway anti-inflammatory effects, immunomodulatory effects and bronchial protection effects. It is manifested in that theophylline can inhibit inflammatory cells, including T lymphocytes, eosinophils, mast cells and macrophages. Activation of cells; inhibition of T lymphocytes (CD4 and CD8) from the peripheral blood circulation to the airway; interference with the activity of tumor necrosis factor (TNF-α), inhibition of airway hyperresponsiveness induced by TNF-α and induction of programmed apoptosis (apoptosis) of human peripheral blood B cells.
Theophylline currently used clinically can be divided into the following four categories.
1. The combination of theophylline and different salts or bases, such as aminophylline and cholophylline.
2. Theophylline N-7 derivatives substituted with different groups. The water solubility of these drugs increases, but the half-life shortening effect is not as strong as theophylline. It is generally used for theophylline or aminophylline cannot tolerate patients.
3. Enprotheophylline (enprophylline) is a newly developed xanthine derivative that replaces theophylline 3-methyl with 3-propyl.
4. Theophylline slow-release or controlled-release agent
The simple theophylline is absorbed rapidly, resulting in obvious fluctuations in blood concentration, short-term bronchodilation and more adverse reactions. Theophylline sustained-release or controlled-release agents can provide a more stable blood concentration.
biological activity
Choline theophyllinate (Oxtriphylline) is a choline salt of theophylline, which has anti-asthma effects.
Production method
It is obtained by condensation of theophylline and choline.