Varenicline transdermal solution as well as preparation method and application thereof

Abstract

The present invention relates to a varenicline transdermal solution. The transdermal solution comprises varenicline or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier, wherein the pharmaceutically acceptable carrier is selected from any one or a combination of a penetration enhancer, a humectant, a preservative and a solvent, and the solvent is selected from any one or a combination of glycerol, propylene glycol, ethanol and water. The solution is absorbed through skin, has the advantages of being long-acting, high in bioavailability, good in patient compliance, convenient to carry and use, flexible in medication position, capable of achieving postaural targeted administration, free of skin irritation and the like, and the effectiveness and safety of the medicine and the medication compliance of the patient are remarkably improved.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a varenicline transdermal solution, a preparation method thereof and an application thereof. Background technique [0002] China is the largest tobacco producing and consuming country in the world. Up to 63% of adult males and 4% of adult females smoke, with a total of 350 million people, accounting for nearly 1 / 3 of the world's total smoking population. If 17% of Chinese smokers want to quit smoking, 60 million smokers need to accept smoking cessation. Calculated by the cost of 500 yuan per person to quit smoking, the scale of China’s smoking cessation market is nearly 300 billion, and the market potential is huge. The non-nicotine drug varenicline (see formula Ⅰ for structure) is the first-line drug for smoking cessation. [0003] [0004] Patients who quit smoking have bad emotions such as irritability, depression, insomnia, irritability, frustration, anger, anxiety, inability to c...

AI Technical Summary

Problems solved by technology

[0004] Patients who quit smoking have bad emotions such as irritability, depression, insomnia, irritability, frustration, anger, anxiety, inability to concentrate, and restlessness, which lead to problems such as poor compliance, low success rate, and high relapse rate

The currently marketed dosage form is only varenicline tablet, which has nausea, gastroesophageal reflux disease, vomiting, constipation, diarrhea, abdominal distension, abdominal pain, toothache, indigestion, flatulence, dry mouth and other gastrointestinal adverse effects reaction, and the tablets are bitter, which reduces the medication compliance of patients who quit smoking

When ex-smoking patients become addicted to smoking, they tend to tear off the nicotine patch and interrupt the smoking cessation treatment, which seriously affects the smoking cessation effect

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