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Itraconazole butyl ester and preparation method thereof

The technology of itraconazole butyl ester and itraconazole is applied in the field of itraconazole butyl ester and its preparation, and can solve the problems of strong toxicity, drug accumulation, strong side effects and the like of itraconazole capsules and injections, To achieve the effect of improving pharmacokinetic properties, reducing accumulation, reducing toxicity and side effects

Inactive Publication Date: 2014-07-30
成都摩尔生物医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The purpose of the present invention is to solve the limitations of current itraconazole capsules in the treatment of systemic fungal infections, the long-term use of itraconazole injections in large quantities causes drug accumulation in the body, and both itraconazole capsules and injections have strong Toxicity and strong side effects and the problem that itraconazole butyl has not yet come out, but a kind of itraconazol butyl and its preparation method are disclosed

Method used

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specific Embodiment approach 1

[0021] Specific embodiment 1: In this embodiment, itraconazole butyl ester is composed of 18-22 mg itraconazole, 505-509 mg lecithin, 90-95 mg cholesterol, 73-77 mg sodium deoxycholate, and 505-509 mg manna Alcohol, 505~509mg lactose and 18~22mL phosphate buffer solution with a pH value of 5.5~6.5. In this embodiment, the drug made of itraconazole butylate can be used between meals or after meals to increase the absorption rate of the drug, but it cannot be used in combination with terphenadine, astemizole or cisapride.

specific Embodiment approach 2

[0022] Specific embodiment two: the difference between this embodiment and specific embodiment one is: itraconazole butylate is composed of 20 mg itraconazole, 507.7 mg lecithin, 92.3 mg cholesterol, 75 mg sodium deoxycholate, 507.7mg of mannitol, 507.7mg of lactose and 20mL of phosphate buffer with a pH value of 5.5-6.5.

specific Embodiment approach 3

[0023] Embodiment 3: The difference between this embodiment and Embodiment 1 or 2 is that the pH value of the phosphate buffer solution is 6.0; the others are the same as Embodiment 1 or 2.

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PUM

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Abstract

The invention discloses itraconazole butyl ester and a preparation method thereof. The itraconazole butyl ester is prepared from the following components in proportion: 18 to 22mg of itraconazole, 505 to 509mg of lecithin, 90 to 95mg of cholesterol, 73 to 77mg of deoxysodium cholate, 505 to 509mg of mannitol, 505 to 509mg of lactose, and 18 to 22ml of phosphate buffer solution with pH of 5.5 to 6.5. The itraconazole butyl ester and the preparation method of the itraconazole butyl ester are disclosed for the first time. The prepared itraconazole butyl ester contains lipidosome pharmic content more than 98%, and has the encapsulation efficiency of 74.3 to 75.5% and the leakage rate of 3.120 / -3.37%; the itraconazole butyl ester is also high in stability, and the Ke value reaches 0.946 to 1.12%.

Description

technical field [0001] The invention relates to an itraconazole butylate and a preparation method thereof. Background technique [0002] There are three types of human fungal infections: superficial, subcutaneous and systemic fungal infections (SFI). The superficial and subcutaneous types have been better controlled, but SFJ is still difficult. With the extensive application of broad-spectrum antifungal drugs, the development of bone marrow or organ transplantation, the widespread use of glucocorticoids and immunosuppressants, the widespread use of various catheter interventional treatments, and the emergence of AIDS, the number of systemic fungal infections is increasing day by day , and has the characteristics of difficult diagnosis, rapid disease progression and high mortality. Itraconazole (Itrac0naz0le) is a second-generation triazole derivative that exerts its antifungal effect by inhibiting the biosynthesis of ergosterol, an essential component of fungal cell membra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/19A61K9/00A61K31/496A61P31/10
Inventor 李智勇
Owner 成都摩尔生物医药有限公司
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