Icaritin tablet and preparation method therefor

Abstract

The invention belongs to the technical field of medicines, and particularly relates to an Icaritin tablet. The tablet is prepared by the following steps of adding Icaritin and part of low-melting-point auxiliary materials into a fluidized bed according to a prescription dosage, and performing melting and granulating in the fluidized bed; then adding microcrystalline cellulose, a disintegrating agent and the remaining low-melting-point auxiliary materials, continuing to perform granulating, and finishing the granules while granules are hot after granulation; and finally adding a lubricating agent, and performing tabletting to obtain the Icaritin tablet. The Icaritin tablet prepared through the method has good stability, also has the advantages of simple preparation process and strong operability, and can be suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an icarigenin tablet and a preparation method thereof. Background technique [0002] Icaritin (IT), also known as icariin, is a polyhydroxy flavonoid monomer compound extracted from the Berberidaceae plant Epimedium. Flavonoid glycosides, etc., icaritin has the strongest anti-osteoporosis effect, and the isopentenyl group in the molecule forms a ring to obtain cycloicaritin (Cycloicaritin, cIT, also known as cycloicaritin) , also has similar immunosuppressive and anti-osteoporosis pharmacological activities. The chemical structural formulas of icariin and cycloicariin are shown in formula I and formula II respectively. [0003] [0004] There are many hydroxyl substitutions and isopentenyl groups in icariin, and its thermal stability is poor. Studies have found that when icariin is heated to 70°C, its content drops to about 90.3%. Icariin is almost insoluble in...

AI Technical Summary

Problems solved by technology

The extremely low solubility of icariin will inevitably affect the absorption of drugs. Some researchers have improved the solubility of drugs by making them into microemulsions, liposomes, solid lipid nanoparticles and other preparations. Poor performance, the carrier material has limited drug loading capacity, the drug loading capacity is very low, and the use of too many excipients also brings drug safety problems

[0005] CN101485630B discloses a liposome of icariin, which improves the in vitro dissolution rate and low bioavailability of icariin, but the yield of liposome preparation is low, and the preparation process is in actual production Difficult to operate

[0006] CN101513388A discloses an icarigenin microemulsion and a preparation method thereof, inventing a microemulsion prepared by dissolving the active ingredient in oil, adding an emulsifier, a co-emulsifier and water with a particle size of 10-100nm. Emulsion, but a large amount of surfactant is used in the prescription, which has the risk of bringing a lot of toxic side effects to the human body

[0007] Jia Dongsheng et al published "Preparation of Icarigenin Phospholipid Complex and Research on Its Solid Dispersion" ([J]. Aurigenin phospholipid complexes or cyclic icarigenin phospholipid complexes greatly improve their solubility and solve their shortcomings of poor water solubility and fat solubility and low bioavailability; however, the preparation process is relatively complicated, and A large amount of organic solvents are used, which is not conducive to environmental protection

[0008] CN104546822A discloses a medical use of icariin. It is mentioned that the oral preparation of icariin can be developed into tablets, capsules or microemulsion preparations. The tablets are wet granulated, and the obtained tablets are not mentioned. The uniformity of the content of the agent, the preparation process is complicated, and it is necessary to repeatedly sieve, granulate and dry

[0009] CN105982869A discloses a cyclic icarigenin tablet, which combines solid dispersion technology with a solubilizer and an adsorbent to improve the in vitro dissolution and low bioavailability of cyclic icarigenin; The application of silicon oxide and silicon dioxide, because of its low density, is easy to float in the air, and there is an increased risk of worker inhalation dust injury

[0011] CN109718221A discloses a capsule of icarigenin, adding a thickener to protect the three-dimensional and electric charge, replacing the surfactant, and adding hydroxypropyl β-cyclodextrin at the same time, the dissolution rate of the obtained capsule is increased, but the preparation process is complicated , requires micronization treatment such as bead mill grinding, and the particle size of the obtained particles may be uneven, which affects the reproducibility of the dissolution effect

[0012] In summary, icariin is an insoluble drug with poor thermal stability. There is no icariin preparation in clinical practice. The preparation process in the prior art is complicated, the oral absorption rate is low, and harmful substances such as a large amount of organic solvents or diuretics are used. Silica, etc., have seriously limited its clinical application, so it is urgent to develop a new type of preparation for improving the absorption and bioavailability of icariin in the body and for industrial production, and it is also important for improving the research and development of traditional Chinese medicine preparations. The application has important practical significance

[0013] The inventor considers that making icariin into a solid dispersion can increase its solubility, and then increase the dissolution rate, but it is found through experiments that using polyethylene glycol and other high water-soluble and low-melting excipients, through the melting method The prepared solid dispersion can improve the solubility of icariin, but the dissolution improvement is small, and there are defects such as cumbersome operation, high hardness of the solid dispersion, and low yield after crushing and sieving; The method of granules, but the dissolution of the resulting tablet becomes worse, unexpectedly, the inventors thought of using microcrystalline cellulose with a porous structure, so that it can be loaded with icariin to solve the above problems

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