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Voriconazole suppository and preparation method and application thereof

A voriconazole suppository, voriconazole technology, applied in suppository delivery, antifungal agents, pharmaceutical formulations, etc., can solve the problems of small side effects, multiple side effects and adverse reactions, and good curative effect

Active Publication Date: 2012-07-04
LIVZON GROUP LIVZON PHARMA FACTORY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Therefore, the purpose of the present invention is to overcome the shortcomings of the existing voriconazole dosage forms, which are mainly oral administration and intravenous administration, have liver first-pass metabolic effects, and have more side effects and adverse reactions, and provide a safe and effective voriconazole administration The pharmaceutical form and its preparation method and application avoid the first-pass effect of the liver, so that the side effects are small and the curative effect is good

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] This embodiment is used to illustrate the voriconazole suppository provided by the present invention and its preparation method.

[0035] A suppository with a specification of 2 g / capsule is prepared, 1000 suppositories are prepared and 100 g of voriconazole is added, and the total weight of the matrix is ​​1900 g, which contains 2-10% by weight of purified water. According to the test, to meet the requirements of preparation melting time limit, hardness and delamination resistance, the matrix composition is formulated as follows: the total weight of the matrix is ​​the weight of 1000 suppositories-medicine powder weight-pure water weight, that is: 1900 (in g).

[0036] Mixture of various fatty acid glycerides 1623.68 4.4%

[0037] Polyoxyethylene 6 fatty acid ester 57 3%

[0038] Macrogol 400 Dilaurate 38 2%

[0039] Glyceryl Behenate 19 1%

[0040] Dimethyldihydroxyethylhydantoin 9.5 0.5%

[0041] Propylene Glycol 38 2%

[0042] Ethanol 38 2%

[0043] Azone 1.9 ...

Embodiment 2

[0049] This embodiment is used to illustrate the voriconazole suppository provided by the present invention and its preparation method.

[0050] Prepare a suppository with a specification of 2 g / capsule, add 100 g of voriconazole to the prepared 1000 capsules, and add 500 mg of antifungal immunosuppressant tacrolimus to the matrix.

[0051] The total weight of the matrix was 1900 g. According to the test, to meet the requirements of preparation melting time limit, hardness and delamination resistance, the matrix composition is formulated as follows: the total weight of the matrix is ​​the weight of 1000 suppositories-medicine powder weight-pure water weight, that is: 1900 (in g).

[0052] A mixture of fatty acid glycerides 1500 78.99%

[0053] Polyoxyethylene 6 fatty acid ester 57 3%

[0054] Macrogol 400 Dilaurate 38 2%

[0055]Dimethyldihydroxyethylhydantoin 1.9 0.1%

[0056] Propylene Glycol 19 1%

[0057] Ethanol 19 1%

[0058] Macrogol hydroxy 15 stearate 38 2%

[...

Embodiment 3

[0067] This embodiment is used to illustrate the voriconazole suppository provided by the present invention and its preparation method.

[0068] The immunomodulator cordycepin is added to the matrix.

[0069] Prepare suppositories with a specification of 1.5g / capsule, prepare 1000 capsules, add 100g of voriconazole, 50g of cordycepin or cordyceps extract, and the total weight of the matrix is ​​about 1350g. According to the test, to meet the requirements of preparation melting time limit, hardness, and delamination resistance, the matrix composition is formulated as follows: the total weight of the matrix is ​​the weight of 1000 suppositories-medicine powder weight-pure water weight, that is: 1350 (in g)

[0070] Mixture of various fatty acid glycerides 1158.3 77.89%

[0071] Polyethylene glycol hydroxy 15 stearate 40.5 3%

[0072] Macrogol 400 Distearate 40.5 3%

[0073] Ethyl Benzoate 1.35 0.1%

[0074] Ethanol 67.5 5%

[0075] Polyoxyethylene hydrogenated castor oil 27...

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PUM

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Abstract

The invention provides a voriconazole suppository and a preparation method and application thereof. The suppository comprises an effective dose of voriconazole, a dispersion carrier and a matrix, wherein the matrix comprises a forming agent, an emulsifying agent and a suspension aid agent. The preparation method comprises the following steps of: dissolving or dispersing voriconazole in the dispersion carrier, and uniformly mixing with the molten matrix to obtain the suppository; or adding the dispersion carrier into the molten matrix, and adding the voriconazole powder and the suspension aid agent, and uniformly mixing to obtain the suppository. The voriconazole suppository is applied to rectal or gynecological cavity administration and to the therapy for local or whole-body deep fungus infection. The invention provides a safe and effective cavity or rectal administration drug form which avoids the first-pass effect of liver, directly reaches the focus, reduces the medicine dosage, isparticularly suitable for the therapy for local deep fungus infection in gynecological cavity, pelvic cavity, accessory and the like, and ensures little side effect and good curative effect.

Description

technical field [0001] The invention relates to a voriconazole suppository, a preparation method and application thereof. Background technique [0002] Due to the widespread use of antibiotics, the symbiotic relationship between bacteria and fungi has been destroyed. Various immunosuppressants, corticosteroids, and radiation therapy have reduced the body's resistance to fungi. Major surgery, organ transplantation, and AIDS that seriously damage the body's immune function The spread of infection will damage the body's immune system, significantly increasing the rate of deep fungal infection and its mortality. Therefore, effective control and treatment of fungal infections has important clinical significance. About 80 kinds of antifungal drugs have been used clinically so far. Among them, azole antifungal drugs are developing the most rapidly. Because of their good curative effect, low toxicity, oral administration and good tolerance, they are the main force of antifungal tr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/02A61K31/506A61K31/7076A61P31/02A61P31/10A61K31/436
Inventor 郭国领曹晖周俊陈晓勤何诗文桑梓福
Owner LIVZON GROUP LIVZON PHARMA FACTORY
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