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Taste masked pharmaceutical composition comprising pH sensitive polymer

A composition and polymer technology, applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, block delivery, etc., can solve the problems of high dosage requirements and increased difficulty

Inactive Publication Date: 2006-12-13
COUNCIL OF SCI & IND RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The relatively high dose requirements of the second-generation cephalosporin antibiotics cefuroxime axetil and celecoxib from the cyclooxygenase 2 inhibitor class further complicate the administration of effective therapeutic dosing
However, such polymeric systems are rarely used in the taste-masking of drugs in solid as well as liquid compositions

Method used

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  • Taste masked pharmaceutical composition comprising pH sensitive polymer
  • Taste masked pharmaceutical composition comprising pH sensitive polymer
  • Taste masked pharmaceutical composition comprising pH sensitive polymer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0128] The pH sensitive polymers are synthesized by solution polymerization. 60% by weight of the hydrophobic monomer methyl methacrylate, 25% by weight of the hydrophilic monomer hydroxyethyl methacrylate, and 15% by weight of the basic monomer vinylpyridine are used for the synthesis of the polymer. These monomers are dissolved in the solvent dimethylformamide. The 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 synthesized polymer is recovered by precipitation in a non-solvent. Use diethyl ether as a non-solvent. The polymer was vacuum dried at 27°C. Characterize the viscosity, molecular weight and composition of the polymer. The polymer compositions, molecular weights and intrinsic viscosities of the polymers are summarized in Table 1.

[0129] Nu...

Embodiment 2

[0132] The pH sensitive polymers used to inhibit crystallization of polymorphic drugs at lower polymer loadings are polymers with higher molecular weight and higher viscosity. The higher molecular weight polymer is made with 60% by weight of the hydrophobic monomer methyl methacrylate, 25% by weight of the hydrophilic monomer hydroxyethyl methacrylate, and 15% by weight of the basic monomer vinylpyridine , and synthesized by changing the amount of initiator and solvent. Higher molecular weight polymers can also be synthesized by reducing the concentration of initiator relative to the monomer content. Alternatively, higher molecular weight polymers can be synthesized by reducing the amount of inert solvent to the monomer content.

[0133] The high molecular weight pH sensitive polymers of the present invention are synthesized by solvent polymerization. The hydrophobic monomer methyl methacrylate, the hydrophilic monomer hydroxyethyl methacrylate, and the basic monomer vinylpy...

Embodiment 3

[0138] Using a monomer composition of 60% weight / weight (w / w) methyl methacrylate, 25% weight / weight (w / w) hydroxyethyl methacrylate and 15% weight / weight (w / w) Vinylpyridine, 51% by weight (accounting for the monomer) of dimethylformamide as a solvent, and 0.0225% of azobisisobutyronitrile as an initiator to synthesize a high molecular weight polymer. The polymerization reaction is carried out by heating the reaction mixture to 60-70°C for 15-18 hours. The synthesized polymer was recovered by precipitation in the non-solvent diethyl ether. The polymer was dried under vacuum at 27°C. The polymer compositions are shown in Table 3.

[0139] Using a monomer composition of 60% weight / weight (w / w) methyl methacrylate, 25% weight / weight (w / w) hydroxyethyl methacrylate and 15% weight / weight (w / w) Vinylpyridine, with dimethylformamide of 34.72% by weight (accounting for monomer) as solvent, and azobisisobutyronitrile as initiator for 0.045% by weight (accounting for monomer), to sy...

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Abstract

The present invention discloses a substantially amorphous pharmaceutical composition comprising a drug that can exist in a variety of polymorphic forms and a pH sensitive polymer, which inhibits the crystallization of the drug during formulation and reconstitution. Polymers of higher molecular weight are more effective at lower loading, especially when the drug polymer matrix is prepared by the solvent evaporation or solvent extraction technique. The composition used as dry syrups maintain bioavailability of the drug and effectively mask the taste of the drug when the composition is reconstituted.

Description

field of invention [0001] The present invention relates to a taste-masking composition comprising a bitter drug and a pH-sensitive polymer, which substantially maintains the drug in an amorphous form and improves the bioavailability of the drug, and to a method of preparing the pharmaceutical composition. Background of the invention [0002] Although many delivery systems have been developed for different routes of administration, such as oral, parenteral, nasal, and transdermal, etc., the oral route remains the most attractive because the drug The drug modality is a simple, convenient, non-invasive and common method of drug delivery. Most prescription drugs are designed for oral use because patients can self-administer them without hospitalization. Oral dosage forms can be designed according to the nature of the drug, the nature of the administration and the need for any particular action desired in the delivery system. Conventional oral dosage forms include: liquid mixtu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/14
CPCA61K9/1635A61K9/0095A61K9/1694A61K47/32
Inventor 莫汉·戈帕里克希纳·库尔卡尼阿尼奥帕·拉梅什·曼乔治
Owner COUNCIL OF SCI & IND RES
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