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Tigecycline liposome preparation

A technology of liposome preparation and tigecycline, applied in the directions of liposome delivery, tetracycline active ingredients, inorganic non-active ingredients, etc., can solve the problems of low local concentration, oxidative degradation, poor stability, etc.

Active Publication Date: 2019-12-17
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the Tygacil preparation has the following two problems: one is that the lyophilized powder of tigecycline has poor stability after dissolution, and it is prone to oxidative degradation and epimerization; the other is that tigecycline has a relatively wide range of tissues in the body Distribution, after intravenous injection, it can be distributed in bone, spleen, liver, kidney and other organs, resulting in low local concentration, which is easy to cause adverse reactions and drug resistance except the affected area

Method used

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  • Tigecycline liposome preparation
  • Tigecycline liposome preparation
  • Tigecycline liposome preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] The detection method of embodiment 1 tigecycline

[0061] Establish tigecycline standard curve in the present embodiment, concrete process is as follows:

[0062] Using ultraviolet (ultraviolet, UV) detection and analysis method: the detection instrument is TECAN 200 PRO; the detection wavelength is 350nm; the detection temperature is 23°C; the detection orifice plate is 96 well plates, UV-transparent; assay volume 200 μL.

[0063] 1.1 UV standard curve of tigecycline in normal saline

[0064] Accurately weigh 2.51mg of tigecycline, dissolve it in a 25mL volumetric flask with normal saline, and obtain a tigecycline aqueous solution with a concentration of 0.10mg / mL; use normal saline to carry out gradient dilution of tigecycline solution to obtain Tigecycline standard solutions with concentrations of 15 μg / mL, 20 μg / mL, 30 μg / mL, 35 μg / mL, 40 μg / mL, 45 μg / mL and 50 μg / mL. The standard solution of tigecycline with the above concentration was detected by UV method, ...

Embodiment 2

[0073] Example 2 Preparation and Characterization of Tigecycline Liposomes Using Calcium Acetate Solution with pH 4.0~7.0 as Internal Water Phase

[0074] All the phospholipids used in this example were purchased from Lipoid Company of Germany. Specifically hydrogenated soy lecithin (HSPC, molecular weight 783.8); PEGylated phospholipid is specifically distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000); cholesterol (CHOL, molecular weight 386.7); Cyclocycline was purchased from TCI Company; the calcium acetate used was purchased from Shanghai Bailingwei Chemical Technology (J&K SCIENTIFIC) Co., Ltd.; the acetic acid used was purchased from Sinopharm Chemical Reagent Co., Ltd.

[0075] It should be noted that the phospholipids used in the following examples are all hydrogenated soy lecithins of Lipoid Company; the pegylated phospholipids used are all distearoylphosphatidylethanolamine-polyethylene glycol of Lipoid Company; The cholesterol used was Lipoi...

Embodiment 3

[0095] Example 3 Preparation and Characterization of Tigecycline Liposomes Using Calcium Acetate Solution with pH 7.0~8.0 as Internal Water Phase

[0096] Sodium hydroxide used in this example was purchased from Shanghai Lingfeng Chemical Reagent Co., Ltd.

[0097] Accurately weigh 1.5860g CaAc 2 ·H 2 O, add an appropriate amount of deionized water, adjust the pH to 7.5 / 8.0 with 1M acetic acid solution or 1M sodium hydroxide solution, add deionized water to set the volume to 30mL, and obtain a 300mM calcium acetate buffer solution with a pH of 7.5 / 8.0.

[0098] To prepare tigecycline liposomes, refer to Example 2 for the specific preparation process. The difference is that in step (3), 10ml of 300mM calcium acetate buffer solution with a pH of 7.5 / 8.0 should be added to the ethanol mixed solution obtained in step (1), instead of acetic acid with a pH of 4.0 / 5.5 / 7.0 calcium buffer.

[0099] The characterization method of tigecycline liposome is with reference to embodiment ...

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Abstract

The invention discloses a tigecycline liposome preparation and a preparation method thereof. The preparation contains tigecycline liposome particles. The liposome particles comprise a carrier. The carrier is a liposome membrane with a bimolecular structure. The tigecycline is positioned in the liposome membrane or in the middle of the liposome membrane. On the premise of ensuring the stability andslow release of the tigecycline, the preparation provided by the invention improves the in-vivo distribution of the tigecycline, increases the local concentration of inflammatory sites, reduces toxicand side effects, and has good clinical application prospects.

Description

technical field [0001] The invention belongs to the technical field of nano drug delivery, and in particular relates to a tigecycline liposome preparation and a preparation method thereof. Background technique [0002] Tigecycline (Tigecycline) is a new type of glycylcycline antibiotics and the third-generation structural analogue of tetracycline, which has extended-spectrum antibacterial activity. Its mechanism of action is to block bacterial protein synthesis by inhibiting peptide chain elongation through a strong combination with the 30S ribosomal subunit of bacteria. Compared with other tetracyclines, the steric hindrance generated by the unique 9-tert-butylglycylamide group of tigecycline allows it to evade bacterial resistance mechanisms to tetracyclines, including ribosome protection and Active efflux system, etc. In addition, tigecycline is not affected by resistance mechanisms such as β-lactamase, target modification, and enzyme target change. Therefore, tigecycl...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/02A61K31/65A61P31/04
CPCA61K9/1271A61K9/1277A61K47/02A61K31/65A61P31/04
Inventor 魏晓慧鲁珊珊
Owner SHANGHAI JIAO TONG UNIV
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