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Pharmaceutical composition for improving palatability of drugs and process for preparation thereof

A composition and drug technology, applied in drug delivery, pharmaceutical formulations, antibacterial drugs, etc., can solve the problems of delayed drug release and inability to provide taste-masking effect, etc.

Inactive Publication Date: 2007-04-25
COUNCIL OF SCI & IND RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Co-application of water-swellable or water-soluble polymers with lipids provides the desired immediate drug release but does not provide the desired taste-masking effect, especially in the case of liquid oral compositions or granules for reconstitution
The use of pH-independent polymers such as ethylcellulose in combination with lipids in taste-masking provides compositions that prevent drug leaching in aqueous media like oral fluid environments, but with delayed ingestion. release of the drug

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] Examples 1 and 2 disclose methods for preparing acid soluble / swellable polymers. As illustrated in Examples 3-9, time-dependent drug release was determined for the taste-masked pharmaceutical compositions given below. The samples were wetted in the dissolution medium taken from 900ml of medium and placed again in the dissolution vessel. The glass beaker used to wet the sample was excessively rinsed with the removed dissolution medium prior to dissolution, and the dissolution medium was again placed in the dissolution vessel.

[0086] The release of cefuroxime axetil from taste-masked granules was tested in 900 ml of 0.07N hydrochloric acid at 37±0.5°C using a USP type II apparatus rotating at 100 rpm. Samples were taken at 30, 60, 120, 180 and 240 minutes. Each withdrawn volume was replaced with fresh media to maintain sink conditions.

[0087] The release of ciprofloxacin hydrochloride from the taste-masked granules was tested in 900 ml of 0.01N hydrochloric acid bu...

Embodiment 2

[0092] Acid-soluble or swellable polymers are synthesized by solution polymerization. The hydrophobic monomer, basic monomer and optional hydrophilic monomer are dissolved in dimethylformamide solvent. The polymer had the following monomer composition: 73% by weight methyl methacrylate, 18% by weight hydroxyethyl methacrylate and 9% by weight vinylpyridine. The azo initiator, azobisisobutyronitrile, was added to the monomer in dimethylformamide solution. The reaction mixture was purged with nitrogen to provide an inert atmosphere. Polymerization was accomplished by heating the reaction mixture to 65°C for 18 hours. The synthesized polymer was recovered by precipitation in a non-solvent (here water) and dried under vacuum at 45°C. The molecular weight of the synthesized polymer was determined by Waters Gel Permeation Chromatography, using a polystyrene type cross-linked copolymer (Styragel) column, with a polystyrene standard (Polysciences, USA) as a reference. The polymer ...

Embodiment 3

[0094] A taste-masked composition is obtained by dissolving a drug in an organic solvent solution of a lipid and a polymer, and obtaining microparticles containing the drug by microencapsulation in water and evaporation of the organic solvent.

[0095] Lipid-polymer solutions: Table 1 shows the compositions containing various lipid-polymer mixtures. The acid soluble polymer prepared in Example 1 was used as one of the pH dependent polymers in all compositions. The amount of solvent used was 7 ml of chlorinated hydrocarbons such as chloroform and dichloromethane. The amounts of lipids and polymers are shown in Table 1.

[0096] Taste-masked microparticles were obtained by emulsification solvent evaporation technique. Cefuroxime axetil was dissolved in the lipid-polymer solution prepared with the necessary amount of solvent. The lipid-polymer solution containing the drug was added dropwise into a distilled water bath under mechanical stirring. 0.1% by weight of polyvinyl alc...

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Abstract

The present invention discloses compositions, comprising a lipid-polymer matrix to mask the bitter or unpleasant taste of the medicament. The lipid or a blend of lipids, are used in combination with the pH dependent polymer where the said polymer is acid soluble or swellable. The process for the preparation of taste masked pharmaceutical compositions of the bitter drugs comprising the said lipid-polymer compositions are disclosed. The concomitant use of the acid soluble polymer, which remains collapsed at the pH of saliva, inhibits the release of drug at that pH and hence they further help in bitterness inhibition. The said compositions deliver substantial amount of the bitter drug immediately at the gastric pH with improved palatability.

Description

field of invention [0001] The present invention provides pharmaceutical compositions that improve the palatability of drugs. More specifically, the present invention relates to suppressing the bitter taste of drugs by dispersing the drugs within lipid-polymer matrices. The compositions of the present invention release a substantial amount of drug immediately at the pH of the stomach. The invention also relates to processes for the preparation of these compositions. Background of the invention [0002] Although many delivery systems are being developed for different routes of administration, such as oral, parenteral, nasal, and transdermal, among others, the oral route remains the most attractive for drug delivery, Because this mode of administration is simple, convenient, non-invasive and common drug delivery method. Conventional oral dosage forms include: liquid mixtures such as solutions and suspensions, solid dosage forms such as tablets and capsules, liquid-filled cap...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/20
CPCA61K9/1635A61K9/1617A61K9/1694A61K9/0095A61K9/0056A61P31/04
Inventor 阿尼奥帕·拉梅什·曼乔治莫汉·戈帕克里希纳·库尔卡尼
Owner COUNCIL OF SCI & IND RES
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