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Antifungal agent and preparation and use method

An antifungal and preparation technology, which is applied in the field of treating patients with fungal or bacterial infections and manufacturing the pharmaceutical preparation, can solve the problems of dissolution rate and bioavailability reduction, etc.

Inactive Publication Date: 2003-10-22
YUNG SHIN PHARMACEUTICALS INDUSTRIAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The seal-coated polymer layer is applied to the drug-coated core to prevent adhesion of the beads, which adversely affects both dissolution rate and bioavailability

Method used

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  • Antifungal agent and preparation and use method
  • Antifungal agent and preparation and use method

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0029] Home-prepared cores usually follow the following preparation procedure:

[0030] (a) Mix polyvinylpyrrolidone (PVP) with isopropanol and distilled water until

[0031] PVP is completely dissolved;

[0032] (b) Put the sucrose granules into a fluid bed granulator equipped with a spray insert (e.g.:

[0033] Glatt or Huttlin);

[0034] (c) mixing together starch and talc;

[0035] (d) Spray (a) onto sucrose granules while mixing (c) with the sprayed sucrose granules

[0036] to form a wet core; and

[0037] (e) drying the wet core to form the core of the composition. (B) Drug emulsification layer:

[0038] The drug emulsification layer contains azole antimicrobial drug, emulsifier, binder and absorption aid. Typically the azole antimicrobial is first dissolved in an organic solvent. Examples of organic solvents include, but are not limited to, dichloromethane, ethanol, and isopropanol. A preferred organic solvent is to use a combination of dichloromethan...

Embodiment 1

[0054] Embodiment 1 (A) prepares core material and method:

[0055] Element

quantity

Polyvinylpyrrolidone (PVP K-30)

40g

Isopropanol

300ml

purified water

200ml

sucrose

400g

starch

800g

Talc

900g

[0056] The core was prepared by a three-step method. The first step involved dissolving 40 g of PVP K-30 in 300 ml of isopropanol with stirring and subsequently mixing it with 200 ml of purified water to form an emulsion. The second step involves mixing together 800g of starch and 900g of talc. The final step involves placing the sucrose in a fluid bed granulator (e.g. Glatt or Huttlin) and spraying the PVP K-30 emulsion produced in the first step onto the sucrose while adding the starch-talc mixture to the sucrose to form the core of the description. The core is further dried in warm air. (B) Materials and methods for preparing the drug emulsification layer:

[0057]...

Embodiment 2

[0063] Element

[0064] In the pharmaceutical composition of Example 2, the weight ratio between the core and itraconazole is about 1:0.59. The weight percentages of the core, itraconazole, vitamin E polyethylene glycol succinate, DL-malic acid and HPMC are 40.4%, 23.7%, 0.01%, 0.01%, and 35.9%, respectively. It should be noted that two solvents, dichloromethane and ethanol, were used to help dissolve itraconazole. The volume ratio of dichloromethane and ethanol used to dissolve itraconazole was about 1:1.07. In addition, the protective layer contained 11.5% by weight of polyethylene glycol 20,000, also dissolved in methylene chloride and ethanol. The volume ratio of dichloromethane and ethanol is about 1:1.05.

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Abstract

The present invention provides new medicinal compositions of pyrrole antimicrobial medicines, such as itraconazole, cypconazole, ketoconazole and fluoroconazole. These medicinal compositions are made into the form of pill preparation, including core, medicine emulsion layer and randomly-selected protective layer, and the described medicine emulsion layer includes medicine, emulsifier, adhesive and absorption adjuvant, and the optimized emulsifier is vitamin E polyglycol succinic acid ester, and the optimized adhesive is hydroxypropyl methyl cellulose, the optimized absorption adjuvant is DL malic acid, said medicine is dissolved in organic solvent, and the optimized organic solvent is ethyl alcohol and dichloromethane, and the described protective layer contains polyglycol (PEG) 20000, and is coated on the medicine emulsion layer.

Description

technical field [0001] The present invention relates to a pharmaceutical composition comprising a core and a drug emulsifying layer and optionally a protective layer. Preferred cores are round, spherical cores comprising sucrose, lactose, starch, talc, or microcrystalline cellulose, or any combination thereof. Preferred drugs are azole antifungal or antibacterial drugs. Examples of azole antifungal or antibacterial agents include, but are not limited to, itraconazole, cyproconazole, ketoconazole, and fluconazole. The drug emulsifying layer includes drug, emulsifier, binder, and absorption aid. A preferred emulsifier is vitamin E polyethylene glycol succinate. A preferred binder is hydroxypropylmethylcellulose. A preferred absorption aid is DL malic acid. Preferably, the azole antifungal or antibacterial drug is dissolved in organic solvents such as ethanol and dichloromethane. The protective layer comprises polyethylene glycol (PEG) 20,000 and is coated on the emulsified...

Claims

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Application Information

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IPC IPC(8): A61K47/12A61K9/50A61K31/4196A61K31/496A61K47/04A61K47/20A61K47/22A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38A61P31/10
CPCA61K9/5078A61P31/10A61K9/00
Inventor 李芳裕陈善炯陈炳崑郭汉江
Owner YUNG SHIN PHARMACEUTICALS INDUSTRIAL CO LTD
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