Cinacalcet hydrochloride solid dispersion and preparation method thereof and cinacalcet hydrochloride oral solid dosage form

A technology of cinacalcet hydrochloride and solid dispersion, which is applied in the direction of medical preparations containing non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., and can solve the problem of high price, difficulty in obtaining, and unavailability of polacrilin potassium. It is suitable for industrialized large-scale production and other problems, and achieves the effect of low price, convenient operation and good dissolution rate

Active Publication Date: 2018-06-22
CHANGZHOU SUNLIGHT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the price of polacrilin potassium is high and difficult to obtain, therefore, the method of document 3 is not suitable for industrialized large-scale production

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1）

[0030] This embodiment is cinacalcet hydrochloride solid dispersion and its preparation method.

[0031] The cinacalcet hydrochloride solid dispersion is made of cinacalcet hydrochloride and hydroxypropyl cellulose in a weight ratio of 1:3, and the hydroxypropyl cellulose used in this example is Nisso HPC- SL.

[0032] The preparation method of this cinacalcet hydrochloride solid dispersion is as follows: the cinacalcet hydrochloride that 0.25kg crosses 40 mesh sieves and the hydroxypropyl cellulose that 0.75kg crosses 40 mesh sieves mix homogeneously, then the mixed material is added to hot water Hot-melt extrusion in a melt extruder, and finally the extruded material is cooled at room temperature, pulverized, and passed through an 80-mesh sieve.

[0033] Wherein, the hot-melt extrusion temperature is 200° C., the screw speed of the extruder is 30 r / min, and the torque is 20 N·cm.

Embodiment 2～ Embodiment 3）

[0035] Each example is basically the same as Example 1, except for the weight ratio of cinacalcet hydrochloride to hydroxypropyl cellulose and the source of hydroxypropyl cellulose used, see Table 1 for details.

[0036] Table 1

[0037]

Embodiment 4）

[0043] This embodiment is an oral solid preparation of cinacalcet hydrochloride and its preparation method.

[0044] The oral solid preparation is a 200 mg capsule [containing 27.55 mg of cinacalcet hydrochloride, that is, a 25 mg cinacalcet capsule], and its formula is shown in Table 3.

[0045] table 3

[0046]

Cinacalcet hydrochloride

filler

Adhesive

disintegrant

lubricant

implement

Example 4

55.1% Example 1

solid dispersion of

19.9% ​​Microcrystalline Cellulose+

15.0% lactose

2.5% povidone

6.0% cross-linked polydimensional

ketone

0.5% colloidal silicon dioxide + 1.0% hard

Magnesium fatty acid

implement

Example 5

20.7% Example 2

solid dispersion of

18.0% corn starch + 52.3%

lactose

4.0% Hydroxypropyl

Cellulose

4.0% cross-linked carboxymethyl

sodium cellulose

0.5% colloidal silicon dioxide + 0.5% hard

Magnesium fatty acid

implement

Example ...

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PUM

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Abstract

The invention discloses a cinacalcet hydrochloride solid dispersion and a preparation method thereof and a cinacalcet hydrochloride oral solid dosage form. The cinacalcet hydrochloride solid dispersion is prepared from cinacalcet hydrochloride and hydroxy propyl cellulose according to a hot-melt extrusion technology, wherein the weight ratio of cinacalcet hydrochloride to hydroxy propyl celluloseranges from 1:0.5 to 1:3. The preparation method comprises the following steps: uniformly mixing cinacalcet hydrochloride and hydroxy propyl cellulose based on the weight ratio; adding the mixture into a hot-melt extrusion machine for thermally melting and extruding; cooling and crushing the extruded materials to obtain the product. According to the preparation method, hydroxy propyl cellulose isused as a carrier; cinacalcet hydrochloride and hydroxy propyl cellulose are processed according to the hot-melt extrusion technology based on a certain weight ratio to prepare the solid dispersion; the solid dispersion is further processed into the solid form which is high in dissolution ratio in a neutral medium. The method is simple in process, convenient to operate, wide in raw material source, low in raw material price, and suitable for industrial mass production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a solid dispersion of cinacalcet hydrochloride, a preparation method thereof and an oral solid preparation of cinacalcet hydrochloride. Background technique [0002] Cinacalcet hydrochloride is a calcimimetics developed by NPS Pharmaceuticals in the United States. It activates the calcium receptors in the parathyroid glands, thereby reducing the secretion of parathyroid hormone (PTH), regulates the behavior of the calcium receptors in the parathyroid glands, and reduces the thyroid gland by enhancing the sensitivity of the receptors to calcium levels in the blood stream. Levels of parathyroid hormone, calcium, phosphorus, and calcium-phosphorus complex. It is mainly used for the treatment of secondary hyperparathyroidism in patients with chronic kidney disease (CKD) on dialysis and hypercalcemia in patients with parathyroid carcinoma. [0003] Th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/38A61K31/137A61P5/20A61P3/14A61P35/00A61P13/12
CPCA61K9/146A61K31/137
Inventor 胡国宜胡锦平黄健丁盛李喜龙奚小金
Owner CHANGZHOU SUNLIGHT PHARMA
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