Pharmaceutical composition containing sildenafil citrate, and preparation method and application thereof

Abstract

The invention provides a pharmaceutical composition containing sildenafil citrate, which adopts a wet granulation process and comprises the following components in percentage by weight: 3 to 45 percent of sildenafil citrate, 0.5 to 5 percent of adhesive, 2 to 20 percent of sweetening agent, 3 to 20 percent of disintegrating agent, 0.5 to 3 percent of flow aid, 0.5 to 5 percent of lubricating agent, and the balance of filler. The filler is selected from a mixture of microcrystalline cellulose and mannitol; the adhesive is selected from one or a mixture of more than one of povidone, hydroxypropyl methylcellulose and hydroxy propyl cellulose; the disintegrating agent is selected from one or a mixture of more than one of polyvinylpolypyrrolidone, croscarmellose sodium and low-substituted hydroxy propyl cellulose, and the pharmaceutical composition is a low-dose dispersible tablet of sildenafil citrate and has the advantages of low cost, easiness in preparation, high dissolution speed and short disintegration time.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing sildenafil citrate, a preparation method and application thereof Background technique [0002] Sildenafil citrate was the first drug developed by Pfizer in the United States, and it shines in the treatment of male erectile dysfunction (ED). It was launched in the United States in 1998 and entered China in 2002. At the same time, sildenafil citrate Nafil is also approved for use in children in the European Union and Japan, and is used for the treatment of pulmonary hypertension in children. [0003] Most of the sildenafil citrate preparations currently on the market are ordinary tablets, and the disintegration speed is not very fast. It is also difficult to treat the elderly, young and patients with swallowing dysfunction. Orally disintegrating tablets can help disintegrate quickly and dissolution, but there is a phenomenon that it is difficult to divide doses. For children and other grou...

AI Technical Summary

Problems solved by technology

[0006] Patent CN103040835 discloses a pharmaceutical composition of sildenafil citrate and PD-1 type pregelatinized starch and its preparation method, using auxiliary materials containing binder and flavoring agent, fluidized bed granulation Tablets are made into orally disintegrating tablets, which have better taste and disintegration; patent CN1254246 discloses a preparation method of orally disintegrating tablets of sildenafil and its salts. The active ingredients are taste-masked by powder coating technology, and then mixed directly Compressing tablets to prepare orally disintegrating tablets, the production control of the above two patents is difficult, and the finished products are easy to absorb moisture and have low hardness and cannot be packaged in plastic bottles, so the cost is also relatively high, and it is difficult to achieve sub-dose for low-dose patients The effect of taking it; patent CN104706606 discloses a tablet and its preparation method. It uses methyl cellulose to wrap the main drug for pretreatment, and then directly mixes it with auxiliary materials for tableting. The disintegration and dispersion performance is not good, so it is not suitable for Children or elderly patients who have difficulty swallowing

Patent CN108392639 discloses a pharmaceutical composition of sildenafil citrate, which adopts the method of sildenafil citrate-mesoporous molecular sieve compound for taste masking, the process is complex and difficult to industrialize

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