Pharmaceutical composition for sustained or continuous releasing therapeutic active components

An active ingredient, sustained release technology, applied in the direction of drug combinations, organic active ingredients, medical formulations containing active ingredients, etc., can solve the problem of drug release at a meaningful and beneficial rate, and rarely reported drug release with limited water solubility and other problems, to achieve the effects of easy mass production, improved drug release, and easy dissolution

Inactive Publication Date: 2005-06-01
科学和工业研究委员会
View PDF22 Cites 13 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] It is readily understood by those skilled in the art that although the release of water-soluble drugs using pharmaceutical compositions has been reported, the release of drugs with limited water solubility has rarely been reported.
In those cases where the composition is used to deliver a drug of limited water solubility, the number of manufacturing steps including separate coating or dispersing the solubility modifier in the matrix limits the use of such compositions
Furthermore, the control of solubility and the resulting release of the drug from the composition relies primarily on the release of the solubility modifier from the coating or matrix, which itself can be very variable and is subject to many factors such that the drug may not be released at a meaningful and beneficial rate

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
  • Pharmaceutical composition for sustained or continuous releasing therapeutic active components
  • Pharmaceutical composition for sustained or continuous releasing therapeutic active components
  • Pharmaceutical composition for sustained or continuous releasing therapeutic active components

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0073] Another embodiment of the present invention relates to the preparation of coating liquid, and this coating liquid wraps tablet core with the mixture of water-insoluble semipermeable membrane film-forming polymer and water-soluble polymer, and can change semipermeable membrane film-forming polymer and Permeability of the membrane is controlled by the proportion of the membrane-forming polymer.

[0074] In general, increasing the concentration of water-insoluble semipermeable membrane-forming polymers decreases membrane permeability and drug release. On the other hand, increasing the concentration of water-soluble polymers increases membrane permeability and drug release. During operation, the core compartment absorbs aqueous liquid from the surrounding environment via the controlled release membrane. The dissolution of the alkalinizing agent / buffer in direct contact with the therapeutically active ingredient results in an increase in the pH of the microenvironment withi...

Embodiment 1

[0097] Prepare the pharmaceutical composition of delayed-release weakly acidic drug-glipizide as follows:

[0098] Tablet cores containing glipizide are prepared as follows:

[0099] No. Ingredient Weight % g mg / tablet

[0100] 1 Glipizide 2.78 6.95 10.00

[0101] 2 TRIS buffer 48.61 121.53 175.00

[0102] 3 Mannitol 29.89 74.73 107.60

[0103] 4 Sodium chloride 9.72 24.30 35.00

[0104] 5 polyvinylpyrrolidone 5.00 12.50 18.00

[0105] 6 Magnesium stearate 1.50 3.75 5.40

[0106] 7 Talc 2.00 5.00 7.20

[0107] 8 Silica airgel 0.50 1.25 1.80

[0108] TRIS buffer (Loba Chemie, India) was mixed with directly compressible mannitol (Pearlitol SD 200, Roquette, France) and sodium chloride (Loba Chemie, India), and passed through a 30-mesh sieve (British Standard Sieve, BSS). Glipizide was mixed with a part of the material obtained above, and passed through a 30-mesh sieve (BSS) after mixing. Mix for 10 minutes and add polyvinylpyrrolidone (Plasdone K 29 / 32, ISP, USA) to the...

Embodiment 2

[0123] The method for preparing as embodiment 1 has the tablet core of the glipizide of following composition:

[0124] No. Ingredient Weight % g mg / tablet

[0125] 1 Glipizide 2.78 2.78 10.00

[0126] 2 TRIS buffer 48.61 48.61 175.00

[0127] 3 Mannitol 30.39 30.39 109.40

[0128] 4 Sodium chloride 9.72 9.72 35.00

[0129] 5 polyvinylpyrrolidone 5.00 5.00 18.00

[0130] 6 Magnesium stearate 1.00 1.00 3.60

[0131] 7 Talc 2.00 2.00 7.20

[0132] 8 Silica airgel 0.50 0.50 1.80

[0133] 100 of the tablets were mixed with 350 grams of filled tablets (filled tablets were prepared with a 7.00 mm round concave punch and contained microcrystalline cellulose, starch, calcium hydrogen phosphate, magnesium stearate, and silica gas Gel) are placed together in the laboratory grade 10 porous applicator, and are coated with a coating solution with the following components:

[0134] No. Ingredient Weight % Grams

[0135] 1 Cellulose acetate 2.58 65.00

[0136] 2 Triacetin 0.26 6.50...

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
thicknessaaaaaaaaaa
thicknessaaaaaaaaaa
Login to view more

Abstract

A pharmaceutical composition useful for sustained / extended release of a therapeutically active ingredient to an environment of use, said composition comprises a tablet core composition consists of a therapeutically active ingredient that is weakly acidic in nature and has a limited solubility in the aqueous environment, said the therapeutically active ingredient is in immediate contact with the agents that are capable of improving the solubility of the agent within the core, for e.g., by changing the micro environmental pH of the core and the tablet core is surrounded by a release rate controlling membrane consisting of a semi-permeable membrane forming polymer, permeable membrane forming polymer, and at least one plasticizer capable of modulating the film formation properties of the polymers.

Description

technical field [0001] The present invention relates to pharmaceutical compositions for sustained / delayed release of therapeutically active ingredients. [0002] The present invention relates to novel, useful pharmaceutical compositions for the sustained release of therapeutically active ingredients into the environment of use. More particularly, the present invention relates to oral pharmaceutical compositions that function according to the principle of osmotic pressure, the principle of diffusion, or a combination of both. The pharmaceutical composition of the present invention comprises a tablet core containing a therapeutically active ingredient, a solubility modifier, an osmagent and other conventional excipients. The tablet core is coated with a controlled-release membrane wall made of a semipermeable membrane-forming polymer and a permeable membrane-forming polymer. The therapeutically active ingredients of the present invention are slightly acidic and have limited so...

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): A61K9/00A61K9/20A61K9/22A61K9/28
CPCA61K9/0004A61K9/2009A61K9/2031A61K9/2853A61K9/2866A61P1/04A61P29/00A61P31/04A61P3/06A61P7/10A61P9/12A61P3/10A61K9/20A61K9/209
Inventor 桑贾伊·加尔拉詹·库马尔·维尔马查曼·拉尔·考尔
Owner 科学和工业研究委员会
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