Skeleton type roxithromycin sustained release pellet capsule

A technology of roxithromycin and sustained-release pellets, which is applied in the direction of medical preparations of non-active ingredients, organic active ingredients, oil/fat/wax non-effective ingredients, etc., and can solve the problem that the slow-release pellets cannot float and release Poor stability, long production process, etc., to achieve the effect of improving bioavailability, delaying release, and prolonging residence time

Active Publication Date: 2011-09-21
西安远大德天药业股份有限公司
View PDF0 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, roxithromycin sustained-release pellet preparations have film-controlled sustained-release pellets, which cannot produce floating effects. The production process is long, requires an aging process, and consumes a lot of energy. During storage, the release rate is stable. poor sex

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
  • Skeleton type roxithromycin sustained release pellet capsule
  • Skeleton type roxithromycin sustained release pellet capsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Taking the production of 1000 skeleton-type roxithromycin sustained-release pellet capsule products of the present invention as an example, the used bulk drug and auxiliary materials and their weight ratios are:

[0037] Roxithromycin 150g

[0038] Octadecanol 4.29g

[0039] Microcrystalline Cellulose 38.57g

[0040] Anhydrous sodium carbonate 4.29g

[0041] Carbomer 974P 4.29g

[0042] Mannitol 12.86g

[0043] In the present embodiment, the weight percent distribution ratio of each raw material is:

[0044] Roxithromycin 70%

[0045] Stearyl Alcohol 2%

[0046] Microcrystalline Cellulose 18%

[0047] Anhydrous Sodium Carbonate 2%

[0048] Carbomer 974P 2%

[0049] Mannitol 6%

[0050] Its preparation method is as follows:

[0051] Roxithromycin was crushed through a 120-mesh sieve, stearyl alcohol was crushed through a 80-mesh sieve, each component was weighed according to the above ratio, mixed evenly, and about 80 g of purified water was added to prepare a...

Embodiment 2

[0055] Taking the production of 1000 skeleton type roxithromycin sustained-release pellet capsule products of the present invention as an example, used bulk drug and adjuvant and weight ratio thereof are:

[0056] Roxithromycin 150g

[0057] Octadecanol 5g

[0058] Microcrystalline Cellulose 62.5g

[0059] Carbomer 974P 5g

[0060] Anhydrous sodium carbonate 2.5g

[0061] Mannitol 25g

[0062] In the present embodiment, the weight percent distribution ratio of each raw material is:

[0063] Roxithromycin 60%

[0064] Stearyl Alcohol 2%

[0065] Microcrystalline Cellulose 25%

[0066] Carbomer 974P 2%

[0067] Anhydrous Sodium Carbonate 1%

[0068] Mannitol 10%

[0069] Its preparation method is identical with embodiment 1. The prepared skeleton-type roxithromycin sustained-release pellet capsules each contain 150 mg of roxithromycin.

[0070] Determination of the release rate, the assay method was the same as in Example 1, and the measurement results: the release r...

Embodiment 3

[0072] Taking the production of 1000 skeleton-type roxithromycin sustained-release pellet capsule products of the present invention as an example, the used bulk drug and auxiliary materials and their weight ratios are:

[0073] Roxithromycin 150g

[0074] Octadecanol 10g

[0075] Microcrystalline Cellulose 20g

[0076] Carbomer 974P 10g

[0077] Anhydrous sodium carbonate 2g

[0078] Mannitol 8g

[0079] In the present embodiment, the weight percent distribution ratio of each raw material is:

[0080] Roxithromycin 75%

[0081] Stearyl Alcohol 5%

[0082] Microcrystalline Cellulose 10%

[0083] Carbomer 974P 5%

[0084] Anhydrous Sodium Carbonate 1%

[0085] Mannitol 4%

[0086] Its preparation method is identical with embodiment 1. The prepared skeleton-type roxithromycin sustained-release pellet capsules each contain 150 mg of roxithromycin.

[0087] Determination of the release rate, the assay method was the same as in Example 1, and the measurement results: the...

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
diameteraaaaaaaaaa
release amountaaaaaaaaaa
Login to view more

Abstract

The invention provides a matrix-typed roxithromycin sustained release micropill capsule which is prepared by 60-75wt percent of roxithromycin, 2-5wt percent of waxy matrix material, 10-25wt percent of microcrystalline cellulose, lactose, cane sugar or xylose, 2-5wt percent of hydrophilic matrix material, 1-4wt percent of anhydrous sodium carbonate and 4-10wt percent of mannite according to the normal preparation method. The waxy matrix material is octodecyl alcohol, cetyl alcohol, octadecanoic acid, glycerin monostearate or hydrogenated castor oil. The hydrophilic matrix material is xanthan gum, alginic acid or carbomer 974P. The matrix material adopted in the invention delays the release of the drug, reduces the density of sustained release micropill, prolongs the staying time of the sustained release micropill in the stomach and intestinal tract and improves the bioavailability of the medicine. A comparison test between the medicine of the invention and the roxithromycin sustained release pill is carried out in eighteen testers and the test shows that the matrix-typed roxithromycin slow-release micropill capsule of the invention and the roxithromycin slow-release pill have bioequiavailability.

Description

technical field [0001] The invention belongs to the technical field of antibiotic drugs, and in particular relates to skeleton-type roxithromycin sustained-release pellet capsules. Background technique [0002] Roxithromycin (RXM) is a semi-synthetic erythromycin derivative with a chemical name of 9-[0-[(2-methoxyethoxy)-methyl]oxime erythromycin. Roxithromycin is a new generation of 14-membered macrolide antibiotics. It was first used in France in 1988 and has been used in more than 90 countries in the world so far. Roxithromycin has good acid stability, is easy to absorb when taken orally, and has good pharmacokinetic characteristics. The antibacterial spectrum and antibacterial activity of roxithromycin in vitro are similar to erythromycin, and its effect on Gram-positive bacteria is slightly worse than that of erythromycin, and its effect on Legionella pneumophila is stronger than that of erythromycin. Very sensitive or moderately sensitive, it has moderate antibacteri...

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 Patents(China)
IPC IPC(8): A61K31/7048A61K9/22A61K47/44A61K47/36A61K47/34A61K47/10A61K47/12A61K47/38A61P31/04
Inventor 唐星于叶淼任延成宋莹王亚轩
Owner 西安远大德天药业股份有限公司
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