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Bupropion Hcl price Bupropion Hydrochloride Powder
Detailed Description
Bupropion is a white powder, crystallized from isopropyl alcohol and absolute ethanol, with a melting point of 233--234°C. Solubility (mg/m1): water 312, ethanol 193, 0.1mol/L hydrochloric acid 333. Very easy to absorb moisture and decompose. Soluble in methanol, ethanol, acetone, ether or benzene. Bupropion belongs to the aminoketone class of antidepressants. It is suitable for patients with retarded depression and those who are ineffective or intolerant to other antidepressants.
Function：
1.Bupropion may also be used as a treatment to manage attention deficit hyperactivity disorder (ADHD).
2. Bupropion may also be used as a prescription treatment to help people quit smoking by decreasing cravings and nicotine withdrawal effects.
3. Bupropion may be used to prevent autumn-winter seasonal depression (seasonal affective disorder).
4. Bupropion may also be used with other medications as a treatment for bipolar disorder (depression phase).
5. Bupropion is used to as a prescription medical treatment for depression. It can improve mood and feelings of well-being. It may work by helping to restore the balance of certain natural chemicals (neurotransmitters) in the brain.
Production methods
Under stirring and cooling, add a solution of o-chlorophenylacetonitrile (688g, 5mol) dissolved in diethyl ether (2.5L) to the solution of ethylmagnesium bromide (2L, 3mol/L) within 40 minutes. Heat under gentle reflux for 5h. The reaction solution was hydrolyzed with cold dilute hydrochloric acid. After the ether was evaporated, the remaining aqueous solution was heated at 90°C for 1 hour. After cooling, add the seed crystal. Collect the solid by filtration, wash with cold water, and recrystallize with methanol to obtain 750g of o-chloropropiophenone, melting point 39-40°C.
Dissolve o-chloropropiophenone (698g, 4.15mmol) in dichloromethane (3L). The solution was stirred with activated carbon and magnesium sulfate for 2 hours and filtered. A solution of 662g (4.15mol) bromine dissolved in dichloromethane (1L) was added with stirring. When the bromine color completely disappears, concentrate in a vacuum to remove the solvent. The remaining oil is o-chloro-α-bromopropiophenone. It can be used directly in the next reaction without purification.
The oily residue obtained above was dissolved in acetonitrile (1300 ml), and a solution of tert-butylamine (733 g) in acetonitrile (1300 ml) was added below 32°C. Leave it overnight, add 4200ml water and 2700ml ether for distribution. The aqueous layer was extracted with 1300 ml of diethyl ether. After the ether layers were combined, 4200 ml of water was added, and hydrochloric acid was added until the Ph value of the water layer was 9. The separated aqueous layer was washed with 500 ml of diethyl ether. The ether layers were combined, 560g of ice and 324ml of concentrated hydrochloric acid were added and stirred together. Separate the ether layer and wash with 200ml water and 50ml concentrated hydrochloric acid. The last two acid layers were combined, concentrated in vacuo until crystallization appeared, and then cooled to 5°C. Filter, wash with acetone, and then recrystallize with a mixture of 3L isopropyl alcohol and 800ml absolute ethanol. Analytically pure and spectrally pure DL-bupropion hydrochloride was obtained, with a melting point of 233 to 234°C.
Pharmacological effects: Bupropion has a weak inhibitory effect on norepinephrine, 5-HT, and dopamine reuptake, but has no such effect on monoamine oxidase.
Drug interactions:
1. Drugs metabolized by cytochrome P450ⅡB6: In vitro experiments show that bupropion is mainly metabolized by cytochrome P450ⅡB6 isoenzyme, so there are potential interactions with other drugs that affect cytochrome P450ⅡB6 isoenzyme.
2. MAO inhibitors: Animal studies have shown that the monoamine oxidase inhibitor (MAOI) phenelzine can increase the acute toxicity of bupropion.
3. Levodopa: Clinical data show that the incidence of adverse reactions may increase after the simultaneous use of bupropion and levodopa. Patients taking levodopa should be cautious when taking this product at the same time. Start with the minimum dose and then gradually increase the dose.
4. Drugs that lower the seizure threshold: This product is combined with drugs that lower the seizure threshold (such as antipsychotics, antidepressants, theophylline, systemic steroids, etc.) or therapies (such as sudden interruption of benzodiazepines) ) should be used together with extreme caution.
5. Nicotine transdermal patch: Clinical studies suggest that the combined use of bupropion sustained-release tablets and nicotine transdermal patch has a higher incidence of emergency therapeutic hypertension. Therefore, blood pressure should be closely monitored for the combined use of the two.
Specification
