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Oral formulation containing itraconazole and methods for manufacturing and using the same

A technology for itraconazole and pharmaceutical preparations, applied in the field of preparation and application of the oral pharmaceutical preparations, can solve the problems of low solubility and bioavailability, low pKa value, low solubility and the like of itraconazole and saconazole

Inactive Publication Date: 2007-07-25
YUNG SHIN PHARMACEUTICALS INDUSTRIAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Due to the fact that these compounds have low solubility in water and low pKa values, the solubility and bioavailability of itraconazole and saconazole are very low

Method used

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  • Oral formulation containing itraconazole and methods for manufacturing and using the same
  • Oral formulation containing itraconazole and methods for manufacturing and using the same
  • Oral formulation containing itraconazole and methods for manufacturing and using the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] (A) Materials and methods for preparing the core:

[0066] The cores were prepared using the following ingredients:

[0067] Element

Dosage

Polyvinylpyrrolidone (PVP K-30)

40g

[0068] Isopropanol

300ml

purified water

200ml

sucrose

400g

starch

800g

Talc

900g

[0069] The cores were produced by a 3-step process. The first step involved dissolving 40 g of PVP K-30 in 300 ml of isopropanol with stirring and then mixing with 200 ml of distilled water, which produced a binder solution. The second step involves mixing together 800g of starch and 900g of talc. The final step consists of adding sucrose to a fluid bed granulator (such as Glatt or Huttlin) and spraying the PVP K-30 binder solution produced in the first step onto the sucrose while the starch-talc mixture Add to sucrose to form a nucleus. The cores are further dried in warm air.

[0070] T...

Embodiment 2

[0078] The core and drug coating of the drug formulation in Example 2 were prepared according to the procedure described in Example 1, except that the amount of core used in Example 2 was different from that in Example 1. The pharmaceutical preparation of embodiment 2 contains following composition:

[0079] Element

Embodiment 3

[0081] The core and drug coating of the drug formulation of Example 3 were the same as those described in Examples 1-2, except that the drug formulation of Example 3 contained a protective layer serving as a seal coat of the drug coating. The pharmaceutical preparation of embodiment 3 contains following composition:

[0082] Element

Dosage

1. Core: 1155g

2. Drug coating:

Itraconazole

600g

Hydroxypropyl Methyl Cellulose (HPMC)

945g

Dichloromethane

6900ml

ethanol

12600ml

3. Protective layer:

Polyethylene glycol (PEG) 20000

27g

distilled water

270ml

[0083] A protective layer was prepared by adding distilled water to PEG 20,000 followed by stirring until PEG 20,000 was completely dissolved.

[0084] After the drug-coated particles are made in the Glatt and dried, while the Glatt is still centrifuging, the protective layer is sprayed onto the drug-c...

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Abstract

The present invention provides oral pharmaceutical formulation for azole antimicrobial drugs such as itraconazole, saperconazole, ketoconazole, and fluconazole. The oral pharmaceutical formulation contains a core and a drug coating layer. The drug coating layer contains the azole antimicrobial drug and a binder, but not containing an emulsion (such as polyoxypropylene-polyoxyethylene block copolymers, polyoxyethylene-sorbitan-fatty acid esters, sodium lauryl sulfate, or vitamin E polyethylene glycol succinate) and / or an absorbent aid (such as DL-malic acid, citric acid, ascorbic acid, and alginic acid). The oral pharmaceutical formulation can optionally contain a protective layer, such as polyethylene glycol 20,000. The present invention also provides a method for preparing and using the formulation.

Description

technical field [0001] The present invention relates to an oral pharmaceutical formulation comprising a core and a drug coating. The core is preferably a round, spherical core comprising sucrose, lactose, starch, talc or microcrystalline cellulose or any combination thereof. The preferred drugs are azole antifungal drugs, which include, but are not limited to, itraconazole, saconazole, ketoconazole, and fluconazole. The drug coating includes drugs and binders, but does not include emulsions (such as polyoxypropylene-polyoxyethylene block copolymers, polyoxyethylene-sorbitan fatty acid esters, sodium lauryl sulfate, or vitamin E polyethylene succinate) and an absorption aid which is an organic acid (such as DL-malic acid, citric acid, ascorbic acid, and alginic acid). The invention also relates to methods of making and using said oral pharmaceutical formulations. Background technique [0002] US Patent No. 4,267,179 discloses a number of 1H-imidazole and 1H-1,2,4-triazole ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/496A61K31/4196A61K47/32A61K47/34A61K47/38A61P31/10
CPCA61K9/2054A61K31/496A61K9/209A61P31/10
Inventor 李芳裕陈善炯陈炳崑郭汉江
Owner YUNG SHIN PHARMACEUTICALS INDUSTRIAL CO LTD
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