Long-acting 5-HT1A receptor stimulant and preparation method thereof

Abstract

The invention discloses a sustained release preparation of tandospirone citrate with the 5-HT1A receptor stimulating effect, and a preparation method of the sustained release preparation. The preparation contains tandospirone citrate, a hydrophilic gel material and a wax material at a certain ratio, and an appropriate amount of filler and an appropriate amount of lubricant are added. The sustained release preparation has the effect of maintaining 24h sustained release, meanwhile, during the release period of medicines, no burst release risk exists, the medicine release uniformity is good, a preparation process is simple, the controllability of the process is strong, after medication, the too large blood concentration fluctuation is avoided, and the medication safety, effectiveness and compliance are improved.

Description

technical field [0001] The invention relates to a long-acting 5-HT1A receptor agonist and a preparation method thereof, more specifically, to a sustained-release tandospirone citrate preparation and a preparation method thereof. Background technique [0002] With the continuous acceleration and complexity of social life, the life pressure brought to Chinese residents has also increased sharply, and the number of people who cause anxiety or have anxiety symptoms is estimated to be tens of millions. There is a lack of drugs with good curative effect and strong specificity. Tandospirone citrate is a 5-HT1A receptor agonist, it can selectively act on 5-HT1A receptors in the brain, exert anxiolytic effect, long-term use can also exert antidepressant effect, which is different from traditional sedative Compared with hypnotics, it has the advantages of specific anti-anxiety effect, less side effects, weak sedative-hypnotic effect, no muscle relaxation effect, no laziness and withd...

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Problems solved by technology

[0003] Patent CN200610021419 protects a sustained-release pharmaceutical composition of tandospirone citrate, specifically a sustained-release tablet, which can reduce the number of administrations from three times a day to twice a day. However, with the pace of life Acceleration, increase of work pressure, for most patients, the doctor's order is poor, and the compliance of taking medicine is poor, which affects the therapeutic effect. Therefore, it is imperative for clinical and patients to take medicine once a day. In addition, the patent US5185158 and its relatives Patents WO9416699, US5330762, US5858407, AU9453545, CA2152673, AU674898, AU1994053545 and EP0681473 protect a tandospirone citrate sustained-release tablet with an osmotic pump structure. In order to maintain the internal osmotic pressure and sufficient drug dose for 24-hour release, the dosage form of this structure will use many times more main ingredients than conventional preparations. It also needs to be coated with semi-permeable membrane materials and prepared through a precise drilling process. , but this will bring the risk of sudden release of the drug due to the rupture of the coating and the disadvantages of complex preparation process and poor controllability

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