Itraconazole liposome and preparation process thereof

A technology of itraconazole lipid and itraconazole, applied in the field of liposome and its preparation, can solve the problems of limitation, drug accumulation, strong side effects, etc.

Inactive Publication Date: 2007-05-30
HARBIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] 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 liposome has not yet come out, and a kind of itraconazole liposome and its preparation method are disclosed

Method used

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  • Itraconazole liposome and preparation process thereof
  • Itraconazole liposome and preparation process thereof

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Effect test

specific Embodiment approach 1

[0008] Embodiment 1: The itraconazole liposome in this embodiment is composed of 18-22 mg itraconazole, 505-509 mg lecithin, 90-95 mg cholesterol, 73-77 mg sodium deoxycholate, 505-509 mg in the following proportions Mannitol, 505~509mg lactose and 18~22mL phosphate buffer with pH value of 5.5~6.5 are prepared.

[0009] In this embodiment, the drug prepared by itraconazole liposome can be used between meals or after meals, which can increase the absorption rate of the drug, but cannot be combined with terfenadine, astemizole or cisapride.

specific Embodiment approach 2

[0010] Embodiment 2: The difference between this embodiment and Embodiment 1 is: the itraconazole liposome is composed of 20 mg itraconazole, 507.7 mg lecithin, 92.3 mg cholesterol, 75 mg sodium deoxycholate in the following proportions , 507.7 mg of mannitol, 507.7 mg of lactose and 20 mL of phosphate buffer with a pH value of 5.5 to 6.5.

specific Embodiment approach 3

[0011] Embodiment 3: The difference between this embodiment and Embodiment 1 or 2 is that the pH value of the phosphate buffer is 6.0. Others are the same as the first or second embodiment.

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Abstract

The invention discloses an eosin liposome and making method, which comprises the following parts: 18-22mg eosin, 505-509mg lecithin, 90-95mg cholesterol, 73-77mg sodium deoxycholate, 505-509mg mannitol, 505-509mg lactose and 18-22mL phosphate buffer with pH value at 5.5-6.5. the making method comprises the following steps: (1) adding eosin, sodium deoxycholate, lecithin and cholesterol into chloroform; (2) decompressing; evaporating chloroform; (3) adding lactose and mannitol into phosphate buffer; (4) emulsifying phosphate buffer without fat film; (5) freezing; drying to obtain the product.

Description

technical field [0001] The present invention relates to a liposome and a preparation method thereof. Background technique [0002] There are three categories of human fungal infections: superficial, subcutaneous, and systemic fungal infection (SFI). The superficial and subcutaneous categories have been well controlled, but SFI is still intractable. With the large-scale application of broad-spectrum antifungal drugs, the development of bone marrow or organ transplantation, the widespread use of glucocorticoids and immunosuppressants, the widespread adoption of various catheter-based interventions, 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. [0003] Itraconazole (Itraconazole) is a second-generation triazole derivative, which exerts its antifungal effect by inhibiting the biosynthesis of ergosterol, an essential component of f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/28A61K31/496A61P31/10A61P17/00
Inventor 吴琳华董迪金锐纪宏宇刘红梅兰恭赞
Owner HARBIN MEDICAL UNIVERSITY
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