Pharmaceutical composition, itraconazole pellet, preparation method and itraconazole capsule

A technology of itraconazole pellets and itraconazole is applied in the field of itraconazole capsules and pharmaceutical compositions to achieve the effects of reducing the incidence or severity, reducing the amount of use and promoting absorption

Pending Publication Date: 2022-07-22
SUZHOU CHUNGHWA CHEM & PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Therefore, the technical problem to be solved by the present invention is to reduce the incidence of adverse reactions or alleviate the degree of adverse reactions caused by itraconazole while ensuring the bioavailability of itraconazole, thereby providing a pharmaceutical composition, itraconazole Azole pellets and preparation method thereof and itraconazole capsules

Method used

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  • Pharmaceutical composition, itraconazole pellet, preparation method and itraconazole capsule
  • Pharmaceutical composition, itraconazole pellet, preparation method and itraconazole capsule
  • Pharmaceutical composition, itraconazole pellet, preparation method and itraconazole capsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] The present embodiment provides a preparation method of itraconazole pellets, comprising the following operations:

[0055] (1) Drug-containing layer coating:

[0056] A. Take 20g of sodium lauryl sulfate (lubricant), dissolve in 1000g of 95% ethanol, add 200g of hydroxypropyl methylcellulose 5cps (second binder), and disperse evenly;

[0057] B, get itraconazole 75g, rhubarb aconite extract (penetration enhancer) 6g and be dispersed in the solution obtained in item A, then add 1500g methylene chloride, stir and disperse evenly, wherein the raw rhubarb and The dosage ratio of Cannon Fuzi is 1:1;

[0058] C, get talcum powder (lubricant) 15g and be dispersed in the 95% ethanol of 200g;

[0059] D, the solution obtained in item C is added to the solution obtained in item B after passing through a 325 mesh screen, and stirred to obtain a drug-containing suspension;

[0060] E, get starch sucrose ball core (blank ball core) 100g and put it in the coating pot, heat, after...

Embodiment 2

[0069] The present embodiment provides a preparation method of itraconazole pellets, comprising the following operations:

[0070] (1) Preparation of pill-containing core:

[0071] Dissolve 6 g of rhubarb aconite extract (penetration enhancer) and 54 g of sucrose (first binder) in water, add 50 g of starch (filler), and then granulate through a fluidized bed to obtain a 20-25 mesh containing The pill core, wherein the dosage ratio of raw rhubarb and aconite in the preparation of rhubarb aconite extract is 1:1.

[0072] (2) Drug-containing layer coating:

[0073] A. Take 20g of sodium lauryl sulfate (lubricant), dissolve in 1000g of 95% ethanol, add 200g of hydroxypropyl methylcellulose 5cps (second binder), and disperse evenly;

[0074] B, get itraconazole 75g and be dispersed in the obtained solution of item A, then add 1500g methylene chloride, stir and disperse uniformly;

[0075] C, get talcum powder (lubricant) 15g and be dispersed in the 95% ethanol of 200g;

[0076]...

Embodiment 3

[0086] The present embodiment provides a preparation method of itraconazole pellets, comprising the following operations:

[0087] (1) Drug-containing layer coating:

[0088] A. Take 20g of sodium lauryl sulfate (lubricant), dissolve in 1000g of 95% ethanol, add 200g of hydroxypropyl methylcellulose 5cps (second binder), and disperse evenly;

[0089] B, get itraconazole 75g, rhubarb Aconite Asarum extract (penetration enhancer) 6g and disperse in the solution obtained in item A, then add 1500g of dichloromethane, stir and disperse evenly, use when preparing Rhubarb Aconite Asarum extract The dosage ratio of raw rhubarb, aconite and asarum is 1:1:0.6;

[0090] C, get talcum powder (lubricant) 15g and be dispersed in the 95% ethanol of 200g;

[0091] D, the solution obtained in item C is added to the solution obtained in item B after passing through a 325 mesh screen, and stirred to obtain a drug-containing suspension;

[0092] E, get starch sucrose ball core (blank ball core...

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Abstract

The invention relates to the technical field of pharmaceutical preparations, in particular to a pharmaceutical composition, itraconazole pellets, a preparation method of the itraconazole pellets and itraconazole capsules. The pharmaceutical composition comprises itraconazole and a penetration enhancer, wherein the penetration enhancer contains a rheum officinale extract and a radix aconiti carmichaeli extract. Due to the penetration promoting effect of the penetration promoting agent, the pharmaceutical composition can ensure the bioavailability of itraconazole, and meanwhile, the dosage of itraconazole is remarkably reduced, so that the occurrence rate or severity of untoward effects of itraconazole is reduced.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a pharmaceutical composition, itraconazole pellets, a preparation method and itraconazole capsules. Background technique [0002] Itraconazole i.e. (±)-cis-4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-tris oxazol-1-methyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazine]phenyl]-2,4-dihydro-2-(1- Methylpropyl)-3H-1,2,4-triazol-3-one is a triazole class of high-efficiency broad-spectrum antifungal drugs, which can bind to fungal cytochrome P450 isoenzymes and inhibit the synthesis of ergosterol. Itraconazole against Dermatophytes, Candida, Cryptococcus neoformans, Pityrosporum, Aspergillus, Histoplasma, Paracoccidioides brasiliensis, Sporothrix schenckii, Chromophytes, Cladosporium It is effective in infections such as mold, blastomycosis dermatitis, and is mainly used to treat systemic infections caused by deep fungi, such as blastomycosis, histoplasmosis, ...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K36/714A61K9/50A61K9/58A61K47/46A61P31/10A61P17/00
CPCA61K31/496A61K36/708A61K36/714A61K36/268A61K9/5073A61K9/5031A61K47/46A61P31/10A61P17/00A61K9/5084A61K2236/331A61K2300/00
Inventor 陆妤茜
Owner SUZHOU CHUNGHWA CHEM & PHARMA IND
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