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Netilmicin sulphate nano micelle preparation for intravenous injection and preparation method thereof

A technology of netilmicin sulfate and nano micelles, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, which can solve the problems of poor stability, obvious oxidative decomposition, and preparation quality. Difficult to guarantee and other issues, to achieve good stability, simple preparation process, and improve the effect of bioavailability

Inactive Publication Date: 2009-06-24
HAINAN YONGTIAN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The sulfate of netilmicin, netilmicin sulfate has increased the wide application of its preparations, but the stability of this product in aqueous solution is still very poor, especially under heating conditions, the oxidative decomposition is obvious, and the quality of the preparation is difficult to guarantee

Method used

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  • Netilmicin sulphate nano micelle preparation for intravenous injection and preparation method thereof
  • Netilmicin sulphate nano micelle preparation for intravenous injection and preparation method thereof
  • Netilmicin sulphate nano micelle preparation for intravenous injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Netilmicin Sulfate 50g

[0037] Macrogol 2000 Distearoyl Phosphatidylethanolamine 250g

[0038] Sodium bisulfite 2g

[0039] Mannitol 100g

[0040] Phosphate buffer solution to adjust the pH value to 4.5-7.0

[0041] Preparation Process

[0042] (1) Take netilmicin sulfate 50g and polyethylene glycol 2000 distearoylphosphatidylethanolamine 250g and dissolve in 500ml n-hexane, mix and disperse evenly, remove n-hexane under reduced pressure to obtain the polymerization of netilmicin sulfate lipid film;

[0043] (2) 100g of mannitol and 2g of sodium bisulfite were dissolved in water, added to the obtained polymer lipid film, then added to a phosphate buffer solution to adjust the pH value to 5.8, heated in a water bath to 70°C for hydration for 1 hour, and obtained sodium sulfate Polyethylene glycol 2000 distearoylphosphatidylethanolamine-loaded nanomicelles of tilmicin;

[0044] (3) Freeze-drying the obtained micellar solution to obtain a freeze-dried preparation of...

Embodiment 2

[0046] Netilmicin Sulfate 300g

[0047] Macrogol 2000 Dipalmitoyl Phosphatidylethanolamine 3000g

[0048] Sodium metabisulfite 10g

[0049] Glucose 1000g

[0050] Citrate buffer to adjust the pH to 4.5-7.0

[0051] Preparation Process

[0052] (1) Take netilmicin sulfate 300g and macrogol 2000 dipalmitoylphosphatidylethanolamine 3000g and dissolve in 6000ml dehydrated alcohol, mix and disperse evenly, remove dehydrated alcohol under reduced pressure, get netilmicin sulfate polymer lipid film;

[0053](2) Dissolve 1000g of glucose and 10g of sodium metabisulfite in water, add it to the obtained polymer lipid film, then add citrate buffer solution to adjust the pH value to 5.6, heat it in a water bath to 50°C for hydration for 3 hours, and obtain sodium sulfate The macrogol 2000 dipalmitoylphosphatidylethanolamine of tilmicin encapsulates nanomicelles;

[0054] (3) Freeze-drying the obtained micellar solution to obtain a freeze-dried preparation of netilmicin sulfate.

Embodiment 3

[0056] Netilmicin Sulfate 100g

[0057] PEG 2000 Dioleoyl Phosphatidylethanolamine 800g

[0058] Sodium Thiosulfate 5g

[0059] Lactose 500g

[0060] Citrate buffer to adjust the pH to 4.5-7.0

[0061] The preparation method is the same as in Example 1, and a freeze-dried preparation of netilmicin sulfate nanomicelles is obtained.

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Abstract

The invention provides a netilmicin sulfate nano-micelle preparation capable of being intravenously injected and a preparation method thereof. The netilmicin sulfate nano-micelle preparation is prepared from netilmicin sulfate, polyethylene glycol-phospholipid and an additive by the method comprising the following steps: the netilmicin sulfate and the polyethylene glycol-phospholipid are prepared into a polymer lipid membrane, and water or a buffer solution which is dissolved with the additive is added into the polymer lipid membrane for hydration to be prepared into the netilmicin sulfate nano-micelle preparation capable of being intravenously injected. The netilmicin sulfate nano-micelle preparation achieves the aim of long-acting circulation in blood, greatly improves the bioavailability, and also greatly increases the stability.

Description

technical field [0001] The invention relates to an intravenously injectable netilmicin sulfate nano-micelle preparation and a preparation method thereof. It belongs to the field of pharmaceutical preparations. Background technique [0002] Netilmicin is a semi-synthetic broad-spectrum aminoglycoside antibiotic. Its mechanism of action is by inhibiting the normal protein synthesis of susceptible microorganisms. Netilmicin has a wide range of antimicrobial effects, mainly against Gram-negative bacilli and a few Gram-positive bacteria, including Citrobacter, Enterobacter, Escherichia coli, Klebsiella, and Proteus morganii , Pseudomonas aeruginosa, Salmonella, Shigella and Staphylococcus (penicillin and methicillin resistant). This product is also active against certain isolated Acinetobacter, Neisseria, indole-positive Proteus, Pseudomonas, and Serratia in vitro. It is suitable for the treatment of complicated urinary tract infection, sepsis, skin and soft tissue infection,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7036A61P31/04A61K47/24
Inventor 邱民
Owner HAINAN YONGTIAN PHARMA INST
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