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Amikacin sulfate multivesicular liposome for local injection and preparation method of amikacin sulfate multivesicular liposome

A technology of amikacin sulfate and multivesicular liposome, which is applied in the field of amikacin sulfate multivesicular liposome for local injection and its preparation, can solve the problem of difficult to kill living bacteria, poor antibiotic treatment effect, and chronic infection Recurrent infection and other problems, to achieve the effect of improving bioavailability, good antibacterial treatment effect, and reducing the toxicity of preparations

Inactive Publication Date: 2021-07-27
CHENGDU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Looking at the annual reports of CHINET (China Bacterial Resistance Monitoring Network) in recent years, Amikacin, a representative of aminoglycoside antibiotics, has a very low resistance rate to Enterobacteriaceae and Pseudomonas aeruginosa. There are many problems in antibiotic therapy: antibiotics are rapidly metabolized and excreted from the body after administration, only a small part of the drug reaches the infection site, and the bioavailability is low, which makes it often necessary to administer large doses and long-term treatment in clinical practice, which will lead to significant Toxic and side effects; in addition, antibiotics have poor therapeutic effects on bacteria in biofilms, and it is difficult to enrich and kill intracellular surviving bacteria, resulting in frequent chronic infections and recurrent infections
In addition, foreign reviews mentioned that there are companies currently developing amikacin multivesicular liposome suspension (DepoAmikacin TM ) and entered the phase I clinical research stage in 2005, but after further searching, no relevant content on the preparation process research was obtained, and no product was listed

Method used

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  • Amikacin sulfate multivesicular liposome for local injection and preparation method of amikacin sulfate multivesicular liposome
  • Amikacin sulfate multivesicular liposome for local injection and preparation method of amikacin sulfate multivesicular liposome
  • Amikacin sulfate multivesicular liposome for local injection and preparation method of amikacin sulfate multivesicular liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Amikacin sulfate multivesicular liposomes, including the raw material formula in the following table 1: in combination with literature information and drug dosage, the fixed main drug concentration is 50mg / mL, and the SPC:CH:TO:ODA quality in the lipid material The ratio is 4:3:2:1, and the changes in the appearance, particle size and encapsulation efficiency of this product are investigated when the drug-to-lipid ratio is 3:1, 2:1, and 1:1.

[0046] Table 1

[0047]

[0048]

[0049] The preparation process is as follows:

[0050] Each group of samples was dissolved in 3ml chloroform of SPC, CH, TO, ODA respectively, as the oil phase for later use; Amikacin sulfate was dissolved in 3ml 7% sucrose solution, as the inner water phase for later use; 625mg glucose Dissolve in 12.5ml of 0.5% PVA (polyvinyl alcohol) solution, and use it as the outer water phase for later use; disperse the inner water phase into the oil phase, stir at 10000r / min for 5min, and then ultra...

Embodiment 2

[0053] Combining with literature reports and pre-experimental results, this example elaborates in detail stearylamine as a membrane stabilizer, whether it is added to the formula and the effect of its dosage on the appearance, particle size and encapsulation efficiency of this product.

[0054] Amikacin sulfate multivesicular liposomes, including the raw material formula of following table 2:

[0055] Table 2

[0056]

[0057] The preparation process is as follows:

[0058] For each group of samples, dissolve SPC, CH, TO, and ODA in 3ml chloroform respectively, and use it as an oil phase; dissolve amikacin sulfate in 3ml 7% sucrose solution, and use it as an internal water phase; Glucose was dissolved in 20ml of 0.5% PVA solution and used as the external water phase for later use; the internal water phase was dispersed into the oil phase, stirred at 10,000r / min for 5min, and ultrasonically disrupted for 4min in an ice bath (power 300W) to form a stable W / O-type colostrum...

Embodiment 3

[0061] Amikacin sulfate multivesicular liposomes, including the raw material formula of following table 3:

[0062] table 3

[0063]

[0064] The preparation process is as follows:

[0065] Two groups of samples were respectively dissolved in 3ml of chloroform-ether mixture (v / v, 1:1) in the SPC, CH, TO, ODA of formula quantity, as the oil phase standby; Amikacin sulfate was dissolved in 3ml of 7% The sucrose solution is used as the inner water phase for later use; 1 g of glucose is dissolved in 20 ml of 0.5% PVA solution, and it is used as the outer water phase for later use. For sample 8, disperse the inner water phase into the oil phase, stir at 10000r / min for 9min, draw colostrum into 12.5ml of outer water phase at a certain speed with a syringe, vortex mix for 10s to form a double emulsion, and transfer the double emulsion to an open glass Place the bottle in a water bath at 37±0.2°C, stir at a certain speed and blow with nitrogen for 10-15 minutes, remove the organi...

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Abstract

The invention provides amikacin sulfate multivesicular liposome for local injection and a preparation method of the amikacin sulfate multivesicular liposome. The amikacin sulfate multivesicular liposome is prepared from the following raw materials in parts by weight: 35 to 180 parts of amikacin sulfate; 35 to 300 parts of a lipid material; 195-410 parts of an osmotic pressure regulator; and 0.50 to 35.50 parts of an auxiliary emulsifier material; and the lipid material is composed of phospholipid, cholesterol, triglyceride and a membrane stabilizer according to the mass ratio of (5-7.5): (3-5.5): (3-6): (1.0-3.0), and the membrane stabilizer comprises at least one of negatively charged phosphatidyl glycerol, fatty acid or stearylamine. The amikacin sulfate multivesicular liposome provided by the invention has the characteristics of high encapsulation efficiency, large drug loading capacity and uniform particle size, can be prepared into a powder injection for injection, can have a better slow release effect, and is beneficial to improving the bioavailability of drugs, so that the curative effect is remarkably improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a local injection of amikacin sulfate multivesicular liposomes and a preparation method and application thereof. Background technique [0002] With the widespread use and abuse of antibiotics, the problem of antibiotic resistance has become a global public health security problem, especially the problem of drug resistance of Gram-negative bacteria. limited. Looking at the annual reports of CHINET (China Bacterial Resistance Monitoring Network) in recent years, Amikacin, a representative of aminoglycoside antibiotics, has a very low resistance rate to Enterobacteriaceae and Pseudomonas aeruginosa. There are many problems in antibiotic therapy: antibiotics are rapidly metabolized and excreted from the body after administration, only a small part of the drug reaches the infection site, and the bioavailability is low, which makes it often necessary to...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/19A61K31/7036A61K47/24A61K47/18A61K47/32A61P31/04
CPCA61K31/7036A61K9/0019A61K9/1271A61K9/1277A61K47/24A61K47/18A61K47/32A61K9/19A61P31/04
Inventor 陶静张淼李楠邓盛齐张晓郑林陈仰张亦斌李黎
Owner CHENGDU UNIV
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