Oral solid rapid release preparation of cinacalcet hydrochloride

Abstract

The invention discloses an oral solid rapid release preparation of cinacalcet hydrochloride. The oral solid rapid release preparation comprises cinacalcet hydrochloride and medicinal auxiliary materials, wherein the average particle diameter of cinacalcet hydrochloride is 5-15 mum; the cinacalcet hydrochloride is needlelike crystalized fine particles; the medicinal auxiliary materials include a filling agent, a bonding agent, a disintegrating agent and a lubricating agent; and the preparation is in the form of a tablet. The oral solid rapid release preparation has the beneficial effects that: the average particle diameter of cinacalcet hydrochloride is defined, so that the dissolution rate and dissolution amount of cinacalcet are increased, a preparation process is simple and safe, the quality is controllable, and cost is low; and the oral solid rapid release preparation is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an oral solid immediate-release preparation of cinacalcet hydrochloride. Background technique [0002] The chemical name of Cinacalcet Hydrochloride is (R)-N-[1-(1-naphthyl)]-3-[3-(trifluoromethyl)phenylpropane-1-amine hydrochloride , whose structural formula is: [0003] [0004] Cinacalcet hydrochloride is a calcimimetic agent, which is a white or off-white non-hygroscopic solid powder. There is a stable crystal form at room temperature. It is slightly soluble in water and can be quickly dissolved in methanol and 95% ethanol. Among them, the solubility is pH-dependent, and in alkaline pH, the solubility is less than 0.001 mg / mL, but it has high permeability. [0005] At present, the drug was approved by the US Food and Drug Administration (FDA) on March 8, 2004, and is listed under the trade name Sensipar. Hyperthyroidism and for the treatment of symptoms of elevated calcium level...

AI Technical Summary

Problems solved by technology

[0007] Chinese patent publication CN1946382A discloses a cinacalcet hydrochloride composition with a specific dissolution behavior. In this composition, silicon dioxide is selected as a glidant. This product is easy to disperse in the air, which is not good for the health of workers, and this The patent claims the D of cinacalcet hydrochloride microparticles 50 Less than or equal to 50 μm, the particle size range is wide, and the dissolution rate and dissolution amount of cinacalcet hydrochloride cannot be well controlled within this range

[0009] Chinese Patent Publication CN102198108A discloses tablets or capsules, specifies the types of specific excipients PEG-6000, mannitol, MCC, crospovidone, pregelatinized starch, and magnesium stearate, etc., specifies the dosage range, and dry granulates , the dissolution characteristics of the preparation, 5-10min dissolution 40-80%, 15-20min dissolution 80-90%, 30-45min dissolution 90-100%, and the commercially available preparation Sensipar has similar drug release behavior, this patent mainly protects A composition is disclosed, which is characterized in that it mainly contains cinacalcet hydrochloride, and additionally contains polyethylene glycol 6000, mannitol, microcrystalline cellulose, crospovidone, partially precrossified starch and hardened starch. Magnesium fatty acid, in which polyethylene glycol 6000, mannitol and API are separately dry granulated to improve the dissolution rate of cinacalcet, and the operation is also relatively complicated

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