pH sensitive polymer and process for preparation thereof

A polymer and sensitive technology, applied in the field of preparation of the polymer, can solve the problems of no reports

Inactive Publication Date: 2009-05-27
COUNCIL OF SCI & IND RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The polymeric compositions disclosed in the present invention show specific pH-dependent dissolution properties and have not been reported in the past literature

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Synthesis of pH-sensitive polymers by bulk polymerization. 35% w / w methyl methacrylate, 30% w / w vinylpyridine and 35% w / w hydroxyethyl methacrylate monomers were mixed together and an azo initiator (1 Azobisisobutyronitrile in % w / w total amount of monomer). The reaction mixture was purged with nitrogen to provide an inert atmosphere. Polymerization was carried out by heating the reaction mixture to 65°C for 18 hours. The polymer thus synthesized was recovered by dissolving in a solvent including dichloromethane and methanol (1:1) and precipitating in a non-solvent. The non-solvent used was diethyl ether. The polymer was dried under vacuum at 27°C.

Embodiment 2

[0074] Synthesis of pH-sensitive polymers by bulk polymerization. 35% w / w methyl methacrylate, 30% w / w vinylpyridine and 35% w / w butyl acrylate monomers were mixed together and an azo initiator (1% w / w mono volume of azobisisobutyronitrile). The reaction mixture was purged with nitrogen to provide an inert atmosphere. Polymerization was carried out by heating the reaction mixture to 65°C for 18 hours. The polymer thus synthesized was recovered by dissolving in a solvent including dichloromethane and methanol (1:1) and precipitating in a non-solvent. The non-solvent used was diethyl ether. The polymer was dried under vacuum at 27°C.

[0075] Table 1

[0076] Polymer swelling / solubility properties in acidic buffer pH 1.2

[0077] S.NO polymer composition Measured properties 1

Methyl Methacrylate 35% w / w

Hydroxyethyl Methacrylate 35% w / w

Vinylpyridine 30% w / w The polymer film begins to dissolve immediately

Solution, the whole film is in ...

Embodiment 3

[0082] Synthesis of pH-sensitive polymers by solution polymerization. The hydrophobic monomer, basic monomer and optional hydrophilic monomer are dissolved in dimethylformamide solvent. An azo initiator (azobisisobutyronitrile) was added to the monomer solution in dimethylformamide. The reaction mixture was purged with nitrogen to provide an inert atmosphere. Polymerization was carried out by heating the reaction mixture to 65°C for 18 hours. The polymer thus synthesized was recovered by dissolving in a solvent comprising dichloromethane and methanol 1:1 and precipitating in a non-solvent diethyl ether. The polymer was dried under vacuum at 27°C. Polymers are characterized by molecular weight. The molecular weight of the synthesized polymer was determined by Waters Gel Permeation Chromatography with polystyrene standards (Polysciences, USA) as reference, using a polystyrene type cross-linked copolymer (Styragel) column. In Table 3 the monomer composition and molecular wei...

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Abstract

The present invention relates to novel pH sensitive polymers exhibiting pH dependent swelling / dissolution properties. The composition is used for taste masking of bitter drugs and gastric release of drugs. The polymer includes a hydrophobic monomer polymerized together with a basic monomer, or a hydrophobic monomer polymerized together with a basic monomer and a hydrophilic monomer.

Description

field of invention [0001] The present invention relates to a pH-sensitive polymer, which swells and / or dissolves under acidic conditions of pH ≤ 3 in the stomach, and maintains deswelling or Insoluble, the present invention also relates to the preparation method of the polymer. Background of the invention [0002] For more than two decades, the release of bioactive agents from polymeric materials has attracted considerable attention from researchers working in the field of drug delivery systems. New technological developments have brought many innovative drug delivery systems to the market, while others are approaching commercialization. Polymers play an important role in pharmaceutical formulations. Polymer-based excipients have been used in formulations for a variety of reasons, including taste masking, protection and stabilization of drugs, etc. Synthetic and naturally occurring polymers are being used in drug delivery systems in the form of matrices, hydrogels, microp...

Claims

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Application Information

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Patent Type & AuthorityPatents(China)
IPC IPC(8): C08F220/00
CPCC08F220/14C08F220/1804C08F226/06C08F220/20C08F220/34
Inventor莫汉·戈帕里克希纳·库尔卡尼阿尼奥帕·拉梅什·曼乔治
OwnerCOUNCIL OF SCI & IND RES