External preparation of neurokinin 1 receptor inhibitor and preparation method of external preparation

Abstract

The invention discloses an external preparation of a series of neurokinin-1 receptors (NK1 receptors) inhibitors and a preparation method of the external preparation. The NK1 receptor inhibitors comprise, but are not limited to, aprepitant, fosaprepitant, rolapitant, netupitant or pharmaceutically acceptable salts thereof. The external preparation comprises, but is not limited to, ointment, cream, gel, tincture, lotion, aerosol, spray, liniment, a foaming agent, patch, emplastrum and the like. The external preparation of the NK1 receptor inhibitors can slowly deliver the medicine at a constant speed, and reduce the blood concentration fluctuation caused by dissolution and absorption of the oral medicine; the pertinence to local lesions can be improved, and the side effects of the whole body are reduced; and meanwhile, a choice with high compliance is provided for patients inconvenient to take orally, and the external preparation has important significance in relieving the pain of cancer patients clinically.

Description

technical field

[0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a series of external preparations of NK1 receptor inhibitors and a preparation method thereof. Background technique

[0002] At present, the main treatment methods for cancer include surgery, chemotherapy and radiotherapy, but many adverse reactions are often caused during the treatment process, such as wound pain after surgery, and chemotherapy with cisplatin and other drugs can cause nausea, vomiting, dermatitis, hair loss, etc., which greatly increase the risk of cancer. Physical and psychological pain of the patient.

[0003] Chemotherapy-induced nausea and vomiting (CINV) is the most common adverse reaction during cancer treatment, and about 70% to 80% of patients will experience this symptom. Severe nausea and vomiting not only lead to nutritional deficiencies, Dehydration and electrolyte imbalance can also force patients to discontinue effe...

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