Oxaliplatin vesicular phospholipid gel injection

A gel injection and oxaliplatin technology, applied in the field of pharmaceutical preparations, can solve problems such as long-term stability to be improved, and achieve the effects of improving bioavailability, improving curative effect, and improving long-term stability

Inactive Publication Date: 2012-10-03
灵康药业集团股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Patent document CN101204376A discloses a freeze-dried preparation of oxaliplatin and its preparation method. Glucose is used as the carrier, and the stability of the preparation is much improved compared with the injection, but its bioavailability and long-term stability still need to be improved.

Method used

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  • Oxaliplatin vesicular phospholipid gel injection
  • Oxaliplatin vesicular phospholipid gel injection
  • Oxaliplatin vesicular phospholipid gel injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1 Preparation of Oxaliplatin Vesicular Phospholipid Gel Injection

[0052] Prescription: (100 bottles)

[0053]

[0054] making process:

[0055] (1) Dissolve 10g of oxaliplatin, 170g of soybean lecithin, 50g of cholesterol and 30g of PEG400 in 300ml of methanol solution, stir and sonicate for 30 minutes, and then do gradient homogenization at 200bar to 1000bar for 6 to 7 times to obtain PEG Saliplatin vesicular phospholipid gel solution;

[0056] (2) Add 80g of glucose to the oxaliplatin vesicular phospholipid gel solution prepared above to dissolve, add methanol solution to 500ml and mix well;

[0057] (3) Filtrate with a 0.45 μm microporous membrane, pack in 5 ml / bottle, and quickly freeze and vacuum-dry at -40°C to obtain oxaliplatin vesicular phospholipid gel freeze-dried powder injection.

Embodiment 2

[0058] Example 2 Preparation of Oxaliplatin Vesicular Phospholipid Gel Injection

[0059] Prescription: (100 bottles)

[0060]

[0061] making process:

[0062] (1) Dissolve 5g of oxaliplatin, 100g of soybean lecithin, 30g of cholesterol and 20g of PEG600 in 200ml of methanol solution, stir and sonicate for 30 minutes, and then do gradient homogenization at 200bar to 1000bar for 6 to 7 times to obtain PEG Saliplatin vesicular phospholipid gel solution;

[0063] (2) Add 50g of glucose to the oxaliplatin vesicular phospholipid gel solution prepared above to dissolve, add methanol solution to 400ml and mix well;

[0064] (3) Filtrate with a 0.45 μm microporous membrane, pack in 5 ml / bottle, and quickly freeze and vacuum-dry at -40°C to obtain oxaliplatin vesicular phospholipid gel freeze-dried powder injection.

Embodiment 3

[0065] Example 3 Preparation of Oxaliplatin Vesicular Phospholipid Gel Injection

[0066] Prescription: (100 bottles)

[0067]

[0068] making process:

[0069] (1) Dissolve 10g of oxaliplatin, 140g of soybean lecithin, 40g of cholesterol and 20g of PEG800 in 300ml of methanol solution, stir and sonicate for 30 minutes, and then do gradient homogenization at 200bar to 1000bar for 6 to 7 times to obtain PEG Saliplatin vesicular phospholipid gel solution;

[0070] (2) Add 50g of glucose to the oxaliplatin vesicular phospholipid gel solution prepared above to dissolve, add methanol solution to 500ml and mix evenly;

[0071] (3) Filtrate with a 0.45 μm microporous membrane, and quickly freeze and vacuum dry at -40°C to obtain oxaliplatin vesicular phospholipid gel freeze-dried powder, then add water for injection to 10 L to disperse evenly, and 0.22 μm microporous filter Membrane fine filtration, 100ml / bottle sub-package to obtain oxaliplatin vesicular phospholipid gel inj...

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PUM

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Abstract

The invention discloses an oxaliplatin vesicular phospholipid gel injection and a preparation method thereof. The injection is prepared from oxaliplatin, soybean lecithin, cholesterol, PEG (polyethylene glycol) and glucose according to specific weight proportion. The vesicular phospholipid gel injection is good in preparation stability, and the vesicular phospholipid gel retains well encapsulation rate as well after long-term storage of the injection. According to the invention, quality of preparation product is improved, drug bio-availability is improved, toxic and side effects are reduced, and the preparation method is simple and is suitable for industrialized production.

Description

technical field [0001] The invention relates to a novel oxaliplatin injection and a preparation method thereof, in particular to an oxaliplatin vesicular phospholipid gel injection and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Oxaliplatin (Oxaliplatin) chemical name: (1R-trans)-(1,2-cyclohexanediamine-N, N’) [oxalic acid (2-)-O, O’] platinum. This product is white or off-white crystalline powder; odorless. This product is slightly soluble in N,N'-dimethylformamide, slightly soluble in water or methanol, almost insoluble in chloroform or ether, relative molecular mass: 397.29, molecular formula: C 8 h 14 N 2 o 4 Pt; the structural formula is as follows: [0003] [0004] Oxaliplatin, which was first developed by Debiopharm, belongs to platinum group metal complexes and is a new generation of platinum-based antitumor drugs after cisplatin and carboplatin. It does not have the nephrotoxi...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K9/10A61K31/282A61K47/34A61P35/00
Inventor 陶灵刚
Owner 灵康药业集团股份有限公司
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