Transdermal delivery preparation in three-dimensional netty spatial configuration of agomelatine and preparation method thereof

Abstract

The invention discloses a transdermal delivery preparation in three-dimensional netty spatial configuration of agomelatine and a preparation method thereof. The transdermal delivery preparation consists of a backing layer, a medicine-loading system in a three-dimensional netty spatial configuration coated on the backing layer and an anti-sticking layer compounded on the system. The medicine-loading system in the three-dimensional netty spatial configuration comprises the following components in percentage by weight: 1-40% of agomelatine, 0-10% of nano-porous carbon dioxide, 40-90% of a pressure-sensitive adhesive, 1-30% of a transdermal penetration enhancer and 0-20% of a dispersant. The transdermal delivery preparation disclosed by the invention not only can continuously deliver the medicine in a transdermal manner for a longer time to maintain the constant blood concentration, but also is quick in transdermal absorption rate and high in transdermal absorptive amount, so that the preparation has the characteristics of stability and efficiency.

Description

Technical field [0001] The invention relates to a transdermal drug delivery preparation containing agomelatine and a preparation method. Background technique [0002] Depression is a subtype of mood disorder. Patients usually have typical manifestations such as low mood, loss of interest or pleasure, lack of energy or fatigue, and physical symptoms (such as sleep disorders). It can be caused by various reasons, with significant and lasting depression as the main clinical feature, and depression is not commensurate with the situation. In severe cases, suicidal thoughts and behaviors may occur. Most cases have a tendency to recurrent attacks, most of them can be relieved each time, and some may have residual symptoms or become chronic. [0003] At least 10% of patients with depression have episodes of manic symptoms, and bipolar disorder should be diagnosed at this time. In addition, what we often say of depression actually refers to clinical major depression, and 16% of the popula...

AI Technical Summary

Problems solved by technology

Both of the above two patents use the direct compression method to prepare orally disintegrating tablets. This orally disintegrating tablet may increase the bioavailability of agomelatine in the human body, but it may be directly disintegrated and released in the oral cavity. Lead to bad taste of the drug and reduce patient compliance

[0010] China CN101919800A and CN101836966A disclose orally disintegrating tablets and dispersible tablets of agomelatine. The above-mentioned patent documents are prepared according to the quality requirements of orally disintegrating tablets or dispersible tablets, but depression is not an emergency and does not need to be used Orally disintegrating or dispersible tablets, an expensive dosage form

Chinese patent CN101048791A discloses agomelatine pharmaceutical composition and its process. In this patent, agomelatine is passed through a 100-mesh sieve and mixed with pharmaceutical excipients to make oral preparations. The study determined the formulation prescription, but did not disclose the dissolution test method, and the dissolution results are open to question

[0013] The shortcomings of agomelatine preparations disclosed in the above patent documents in terms of drug stability, uniformity and bioavailability have not been substantially improved

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