Pulsatile controlled-release tablet containing fluticasone furoate and vilanterol and preparation method thereof

Abstract

The invention provides a pulsatile controlled-release tablet containing fluticasone furoate and vilanterol. The pulsatile controlled-release tablet can reach plasma concentration at midnight and early morning, so the purpose of chrono-chemotherapy is achieved. The pulsatile controlled-release tablet comprises a floating layer and a tablet core. The floating layer uses hydrophilic high molecules and fatty alcohol as adjuvant materials, so the floating layer can retain for a certain period of time in the stomach; when the tablet contacts with gastric juice, the surface of the floating layer hydrates to form gel, so the size of the tablet becomes larger; when the gel is smaller than the concentration of the gastric juice, the tablet is allowed to float above contents in the stomach; and the tablet core appears along with dissolution of the skeleton of the floating layer, so drugs are released from the tablet core.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a pulse-controlled release tablet containing fluticasone furoate and vilanterol and a preparation method thereof. Background technique [0002] Bronchial asthma is a chronic inflammatory disease of the airways that involves a variety of cells (such as eosinophils, mast cells, T lymphocytes, neutrophils, airway epithelial cells, etc.) and cell components. This chronic inflammation leads to the generation of airway hyperresponsiveness, usually with widespread and variable reversible airflow limitation, and causes recurrent symptoms such as wheezing, shortness of breath, chest tightness or coughing, often at night and / or in the early morning, Most patients can be relieved spontaneously or after treatment. [0003] Chronic obstructive pulmonary disease (COPD) is a chronic bronchitis and / or emphysema characterized by airflow obstruction, a common chronic disease that ca...

AI Technical Summary

Problems solved by technology

However, the dry powder inhaler still cannot solve the contradiction between increasing the lung deposition rate and reducing the patient's maximum inspiratory flow rate

This is quite disadvantageous for patients with COPD, there are cases of poor patient compliance

Moreover, the use of this dosage form will be affected by the age or physiological state of the patient, and it is difficult to use it for infants with weak respiratory muscles, the elderly and patients with severe asthma attacks, because some of these patients are difficult to reach The inhalation speed required by the inhaler makes it difficult for some to learn the correct use of dry powder inhalers

In addition, the existing dry powder inhaler products also have the disadvantages of high cost and complicated operation steps.

[0005] On the other hand, chronic obstructive pulmonary disease (COPD) and asthma attack usually in the early morning and early morning, relieve during the day, and existing common tablet can't guarantee blood drug concentration when 3-4 o'clock in the morning, although sustained-release tablet can Maintain the blood drug concentration for a long time, but the blood drug concentration has peaks and valleys, which may easily lead to the occurrence of toxic and side effects of the preparation and affect the safety of medication

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