Immediate release cinacalcet hydrochloride preparation and preparation method thereof

A technology of cinacalcet hydrochloride instant and cinacalcet hydrochloride, which is applied in the field of cinacalcet hydrochloride immediate-release preparations and its preparation, can solve the limitation of the applicable population and the poor dissolution rate of cinacalcet hydrochloride instant preparations and other issues to achieve the effect of expanding the population of drug users

Active Publication Date: 2017-05-24
CHANGZHOU SUNLIGHT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The dissolution rate of the cinacalcet hydrochloride instant preparation disclosed in this document is not good, and its dissolution rate in 0.05mol / L hydrochloric acid was measured on a USP2 device at about 37°C and 75rpm, and it took 30 minutes to reach more than 85%.
In addition, the rotation speed of 75rpm is equivalent to the peristaltic strength of the gastrointestinal tract of young and middle-aged adults. If it is measured at a rotational speed of 50rpm, which is more suitable for the peristaltic strength of the gastrointestinal tract of children and middle-aged and elderly people, it will take 45 minutes to achieve a dissolution rate of more than 85%. Therefore, this document The disclosed cinacalcet hydrochloride instant preparation is not suitable for children or middle-aged and elderly people, and the scope of applicable population is relatively limited

Method used

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  • Immediate release cinacalcet hydrochloride preparation and preparation method thereof

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Experimental program
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Effect test

Embodiment 1）

[0023] The immediate-release formulation of cinacalcet hydrochloride in this embodiment is a 25 mg cinacalcet tablet.

[0024] The tablet core of this 25mg cinacalcet tablet is made of the following components by weight percentage: 27.55% cinacalcet hydrochloride; 37.47% pregelatinized starch; 24.98% microcrystalline cellulose; 4% Polyvinylpyrrolidone; 4% cross-linked polyvinylpyrrolidone; 1% colloidal silicon dioxide; 1% magnesium stearate; see Table 1 for details.

[0025] The preparation method of this 25mg cinacalcet tablet has the following steps:

[0026] ① 27.55mg of cinacalcet hydrochloride (D 90 50 90 50 90 <250μm, intragranular), 4.00mg polyvinylpyrrolidone and 2.00mg cross-linked polyvinylpyrrolidone (intragranular) were mixed evenly.

[0027] ②Add an appropriate amount of purified water as a wetting agent, pass through a 30-mesh sieve to granulate, and put the prepared granules into an oven at 60°C to dry, and control the moisture content of the granules to ≤5%. ...

Embodiment 2）

[0032] The immediate-release formulation of cinacalcet hydrochloride in this embodiment is a 25 mg cinacalcet tablet.

[0033] The preparation method of this 25mg cinacalcet tablet is the same as that of Example 1, except that the tablet core is made of the following components by weight percentage: 27.55% cinacalcet hydrochloride; 31.20% pregelatinized starch; 26.00% microcrystalline cellulose; 4.25% polyvinylpyrrolidone; 8% cross-linked polyvinylpyrrolidone; 1.50% colloidal silicon dioxide; 1.50% magnesium stearate; see Table 1 for details.

Embodiment 3）

[0035] The immediate-release formulation of cinacalcet hydrochloride in this embodiment is a 75 mg cinacalcet tablet.

[0036] The preparation method of this 75mg cinacalcet tablet is the same as Example 1, and the difference is that the tablet core is made of the following components by weight percentage: 41.325% cinacalcet hydrochloride; 28.005% pregelatinized starch; 18.67 % microcrystalline cellulose; 4% polyvinylpyrrolidone; 6% cross-linked polyvinylpyrrolidone; 1% colloidal silicon dioxide; 1% magnesium stearate; see Table 1 for details.

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Abstract

The invention discloses an immediate release cinacalcet hydrochloride preparation and a preparation method thereof. The immediate release cinacalcet hydrochloride preparation comprises a tablet core and a coating material, wherein the tablet core is prepared from the following ingredients in percentage by weight: 10%-50% of cinacalcet hydrochloride, 27%-54% of pregelatinized starch, 13%-26% of microcrystalline celluloses, 1%-5% of polyvinylpyrrolidone, 1%-10% of crosslinked polyvinylpyrrolidone, 0.05%-2% of colloidal silicon dioxide and 0.05%-2% of magnesium stearate. The immediate release cinacalcet hydrochloride preparation disclosed by the invention is very good in dissolving-out speed, the dissolution rate of the preparation in 0.05mol/L hydrochloric acid is measured at the temperature of 37 DEG C by adopting a USP2 (united states pharmacopoeia) device, and over 85% of the dissolution rate can be achieved at rotation speeds of 75rpm and 50rpm only within 15min, therefore, the preparation can be suitable for patients with weak gastric motility such as children, middle and aged men and the like, and the population taking the preparation of the product is enlarged.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a cinacalcet hydrochloride immediate-release preparation and a preparation method thereof. Background technique [0002] Cinacalcet hydrochloride, the first drug in a new class of compounds known as calcimimetics, activates calcium receptors in the parathyroid glands, thereby reducing parathyroid hormone (PTH) secretion and is used in the treatment of Secondary hyperparathyroidism in patients with chronic kidney disease (CKD) on dialysis and hypercalcemia in patients with parathyroid carcinoma; cinacalcet hydrochloride belongs to BCS class Ⅱ drugs, and its solubility is significantly affected by pH, limited Solubility can lead to lower bioavailability. [0003] Chinese patent document CN1946382A discloses a quick-dissolving preparation of a calcium receptor active compound, which comprises about 10% to about 40% by weight of cinacalcet hydrochlori...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K31/137A61K47/38A61K47/36A61P5/16A61P3/14
CPCA61K9/0002A61K9/2054A61K9/2059A61K9/2806A61K31/137
Inventor 胡国宜胡锦平张孟陈玮琦奚小金
Owner CHANGZHOU SUNLIGHT PHARMA
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