Oral solid rapid release preparation of cinacalcet hydrochloride

A technology for cinacalcet hydrochloride and immediate-release preparations, applied in the field of medicine, can solve the problems of complicated operation, inability to control the dissolution rate and amount of cinacalcet hydrochloride well, unfavorable health and the like, and achieves simple preparation process, Improve the dissolution rate and dissolution amount, and the effect of controllable quality

Inactive Publication Date: 2013-01-23
CHINA RESOURCES SAIKE PHARMA
View PDF8 Cites 14 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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., sp

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Oral solid rapid release preparation of cinacalcet hydrochloride
  • Oral solid rapid release preparation of cinacalcet hydrochloride
  • Oral solid rapid release preparation of cinacalcet hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0027] The preparation method of the cinacalcet hydrochloride tablet of the present invention adopts a wet granulation process, that is, through micronization, sieving, mixing, granulation, drying, granulation, tabletting and other technical processes.

[0028] Particle size distribution determination method:

[0029] a) method parameters

[0030]

[0031] b) Determination process

[0032] The sample to be analyzed was prepared by weighing 60 mg of cinacalcet hydrochloride into 20 mL of sample dispersant, which was previously prepared by diluting 1.5 g of soybean lecithin to 200 mL with Isopar G. The suspension was added dropwise to a background-corrected measuring cell previously filled with a dispersant (Isopar G) until the refractive index reached approximately 15%. After the measurement is completed, the sample cell is emptied and rinsed, the suspension medium is refilled, and the sampling procedure is repeated here. For characterization, specifically list D 10 、D ...

Embodiment 1

[0048] Example 1 Preparation of oral solid immediate-release formulation of cinacalcet hydrochloride

[0049] Preparation of raw material composition containing 90 mg (calculated as cinacalcet hydrochloride free base) active ingredient of specified particle size distribution

[0050]

[0051] The preparation of the oral solid immediate-release preparation of cinacalcet hydrochloride comprises the following steps:

[0052] (1) Micronize cinacalcet hydrochloride, weigh it, and sieve it to obtain particles with an average particle size of 5-15 μm, prepare a certain concentration of adhesive solution, and then mix cinacalcet hydrochloride with filler and disintegrate The agent is mixed evenly;

[0053] (2) Add the binder into the uniformly mixed powder of the main ingredient and excipients, granulate, granulate, and dry at a certain temperature until the moisture meets the requirements, that is, dry granules are obtained;

[0054] (3) Then add a disintegrating agent and a lub...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
The average particle sizeaaaaaaaaaa
Wavelengthaaaaaaaaaa
Login to view more

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...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K9/20A61K31/137A61P5/20A61P5/22
Inventor 何凤娟张松涛蒋玲敏关津杨琰王文峰
Owner CHINA RESOURCES SAIKE PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap