Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Desloratadine citrate disodium capsules as well as preparation method and application thereof

A technology of desloratadine and loratadine, which is applied in the field of pharmaceutical preparations, can solve the problems that the substance content of desloratadine cannot be solved well, so as to improve the dissolution rate and stability, improve the dissolution behavior, Effect of inhibiting the growth of related substances

Active Publication Date: 2020-07-17
HEFEI IND PHARMA INST CO LTD
View PDF10 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] But so far, the content of related substances in desloratadine has not been well resolved

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
  • Desloratadine citrate disodium capsules as well as preparation method and application thereof
  • Desloratadine citrate disodium capsules as well as preparation method and application thereof
  • Desloratadine citrate disodium capsules as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028]

[0029]

[0030] The preparation method is:

[0031] (1) Desloratadine citrate, ascorbic acid, calcium hydrogen phosphate, microcrystalline cellulose and pregelatinized starch are taken by weighing the prescription amount, sieved and premixed with 60 meshes;

[0032] (2) Weigh the PVP k30 of the prescribed amount, add the prescribed amount of purified water to prepare a binder solution, and add it to the mixture prepared in step (1), granulate with a 30-mesh sieve, and dry in a fluidized bed until the moisture content is ≤5.0%. After sizing through a 24-mesh sieve, add silicon dioxide for total mixing to obtain desloratadine citrate granules;

[0033] (3) Fill the desloratadine citrate granules into gelatin hollow capsules (No. 3) to prepare 1000 desloratadine citrate capsules.

Embodiment 2

[0035] Name of raw material Prescription amount desloratadine citrate 8.8g Calcium hydrogen phosphate 45g microcrystalline cellulose 65g silica 1.2g Povidone (PVPk30) 1.5g ascorbic acid 1g purified water 20g

[0036] The preparation method is:

[0037] (1) take desloratadine citrate, ascorbic acid, calcium hydrogen phosphate and microcrystalline cellulose of prescription quantity, 60 mesh sieve, premix;

[0038] (2) Weigh the PVP k30 of the prescribed amount, add the prescribed amount of purified water to prepare a binder solution, and add it to the mixture prepared in step (1), granulate with a 30-mesh sieve, and dry in a fluidized bed until the moisture content is ≤5.0%. After sizing through a 24-mesh sieve, add silicon dioxide for total mixing to obtain desloratadine citrate granules;

[0039] (3) Fill the desloratadine citrate granules into gelatin hollow capsules (No. 4) to prepare 1000 desloratadine citrate capsu...

Embodiment 3

[0041] Name of raw material Prescription amount desloratadine citrate 8.8g Calcium hydrogen phosphate 40g pregelatinized starch 70g silica 1.2g Povidone (PVPk30) 1.5g ascorbic acid 3g purified water 20g

[0042] The preparation method is:

[0043] (1) take by weighing desloratadine citrate, ascorbic acid, calcium hydrogen phosphate and pregelatinized starch of prescription quantity, 60 mesh sieve, premix;

[0044] (2) Weigh the PVP k30 of the prescribed amount, add the prescribed amount of purified water to prepare a binder solution, and add it to the mixture prepared in step (1), granulate with a 30-mesh sieve, and dry in a fluidized bed until the moisture content is ≤5.0%. After sizing through a 24-mesh sieve, add silicon dioxide for total mixing to obtain desloratadine citrate granules;

[0045] (3) Fill the desloratadine citrate granules into gelatin hollow capsules (No. 4) to prepare 1000 desloratadine citrate cap...

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

No PUM Login to View More

Abstract

The invention provides desloratadine citrate disodium capsules as well as a preparation method and application thereof. The capsules are composed of desloratadine citrate disodium particles and hollowcapsules, and the desloratadine citrate disodium particles contain desloratadine citrate disodium, ascorbic acid, a filler, a lubricant and an adhesive in a weight percentage ratio of (5-12):(1-3):(80-150):(0.5-2):(0.5-3). The invention also provides a preparation method of the desloratadine citrate disodium capsules and application of the capsules in preparation of medicines for treating rhinitis and urticaria. The desloratadine citrate disodium capsules disclosed by the invention are reasonable in formula and simple and convenient in production process; and by adding the ascorbic acid component, the dissolution rate and the stability of the desloratadine citrate disodium capsules are remarkably improved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to desloratadine citrate capsules and a preparation method and application thereof. Background technique [0002] Desloratadine (Desloratadine) is a non-sedative long-acting tricyclic antihistamine and an active metabolite of loratadine, which can relieve seasonal allergic rhinitis by selectively antagonizing peripheral H1 receptors or associated symptoms of chronic idiopathic urticaria. In addition, in vitro studies showed that desloratadine inhibited the release of histamine from human mast cells. Animal studies suggest that desloratadine does not readily cross the blood-brain barrier. However, due to the well-known instability and low water solubility of desloratadine, it encounters great difficulties in preparation, and many documents have reported different solutions. For example, US2002 / 123504, WO2006 / 020534, CN1246794, etc. [0003] Also for example, CN201410104...

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
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K31/4545A61K47/22A61P11/02A61P17/00A61P37/08
CPCA61K9/1617A61K31/4545A61P11/02A61P37/08A61P17/00
Inventor 何广卫李丰刘为中苏峰毕东辉
Owner HEFEI IND PHARMA INST CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products