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Gemcitabine hydrochloride liposome injection

A technology for injections and plastids, applied in the field of medicine, can solve the problems of increased unqualified rate of freeze-dried drugs, negligible stabilizing effect, and low bioavailability, so as to improve bioavailability, good preparation stability, and improve preparation product quality Effect

Inactive Publication Date: 2012-10-10
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

However, this method increases the number of excipients while reducing the freeze-drying time, resulting in an increase in the failure rate of freeze-dried drugs and increasing the risk to the human body.
Patent literature CN1650883A discloses a gemcitabine hydrochloride solution injection and a preparation method thereof. The injection adds an alkaline substance or a weak acid salt as a stabilizer to improve the stability of the drug, but the stabilizing effect of this stabilizer is negligible, and the drug is not stable. Stability is still high, bioavailability is not high

Method used

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  • Gemcitabine hydrochloride liposome injection
  • Gemcitabine hydrochloride liposome injection
  • Gemcitabine hydrochloride liposome injection

Examples

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Effect test

Embodiment 1

[0056] The preparation of embodiment 1 gemcitabine hydrochloride liposome injection

[0057] The ingredients used and their weights are as follows:

[0058]

[0059] Adopt following process to prepare gemcitabine hydrochloride liposome injection:

[0060] (1) Dissolve 400g of cholesterol, 500g of egg yolk phosphatidylinositol, 100g of lecithin and 100g of Tween 80 in 2000ml of phosphate buffered saline solution with a pH of 7.2 to make blank liposomes;

[0061] (2) The blank liposomes prepared above were sterilized by circulating steam, and then sonicated twice, each time for 15 minutes;

[0062] (3) Under sterile conditions, add 200 g of gemcitabine hydrochloride to the liposome in solution state at 60°C, and add 100 g of trehalose, 200 g of mannitol and 40 g of PVP under constant stirring;

[0063] (4) Filtrate with a 0.45 μm microporous membrane, fill, and then freeze-dry. When freeze-drying, the pre-freezing temperature is -45°C, the pre-freezing time is 22 hours, t...

Embodiment 2

[0064] The preparation of embodiment 2 gemcitabine hydrochloride liposome injection

[0065] The ingredients used and their weights are as follows:

[0066]

[0067] Adopt following process to prepare gemcitabine hydrochloride liposome injection:

[0068] (1) Dissolve 800g of cholesterol, 1000g of egg yolk phosphatidylinositol, 200g of lecithin and 300g of Tween 80 in 3000ml of phosphate buffered saline solution with a pH of 7.2 to make blank liposomes;

[0069] (2) The blank liposomes prepared above were sterilized by circulating steam, and then sonicated twice, each time for 15 minutes;

[0070] (3) Under sterile conditions, add 200 g of gemcitabine hydrochloride to the liposome in solution state at 60°C, and add 300 g of trehalose, 600 g of mannitol and 60 g of PVP under constant stirring;

[0071] (4) Filtrate with a 0.45 μm microporous membrane, fill, and then freeze-dry. When freeze-drying, the pre-freezing temperature is -45°C, the pre-freezing time is 22 hours, ...

Embodiment 3

[0072] The preparation of embodiment 3 gemcitabine hydrochloride liposome injection

[0073] The ingredients used and their weights are as follows:

[0074]

[0075] Adopt following process to prepare gemcitabine hydrochloride liposome injection:

[0076] (1) Dissolve 2000g of cholesterol, 2500g of egg yolk phosphatidylinositol, 500g of lecithin and 500g of Tween 80 in 5000ml of phosphate buffered saline solution with a pH of 7.2 to make blank liposomes;

[0077] (2) The blank liposomes prepared above were sterilized by circulating steam, and then sonicated twice, each time for 15 minutes;

[0078] (3) Under sterile conditions, add 1000g of gemcitabine hydrochloride to the liposome in a solution state at 60°C, and add 1000g of trehalose, 2500g of mannitol and 50g of PVP under constant stirring;

[0079] (4) Filtrate with a 0.45 μm microporous membrane, fill, and then freeze-dry. When freeze-drying, the pre-freezing temperature is -45°C, the pre-freezing time is 22 hours...

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Abstract

The invention discloses a gemcitabine hydrochloride liposome injection and a preparation method thereof. The gemcitabine hydrochloride liposome injection is prepared from the following components in specific percentage by weight: gemcitabine hydrochloride, cholesterol, egg yolk phosphatidylinositol, phosphatidylcholine, tween 80, trehalose, mannitol and polyvinylpyrrolidone. The liposome injection is high in stability and cannot be cracked due to fusion, ice crystal and the like during freezing; and after long-term storage, liposome is still high in package rate. According to the gemcitabine hydrochloride liposome injection, the solubility of gemcitabine hydrochloride is improved; the quality of a product is improved; the toxic and side effects are reduced; the retention time of medicines during general circulation is prolonged; the biological utilization rate of the medicine is increased; the treating effect is obviously enhanced; the preparation method is simple; and the gemcitabine hydrochloride liposome injection is suitable for industrial large-scale production.

Description

technical field [0001] The invention relates to a liposome injection and a preparation method thereof, in particular to a gemcitabine hydrochloride liposome injection and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] The chemical name of gemcitabine hydrochloride is (+) 2'-deoxy-2',2'-difluorocytosine hydrochloride, molecular formula: C 9 h 11 f 2 N 3 o 4 HCl, molecular weight 299.70, structural formula as follows: [0003] [0004] Gemcitabine hydrochloride is a white crystalline powder; odorless. This product is soluble in water, slightly soluble in ethanol, almost insoluble in chloroform or acetone. [0005] Lung cancer is currently the most common malignant tumor that causes the death of cancer patients in the world. Its death toll is equivalent to the sum of the deaths from breast cancer, prostate cancer and colon cancer, among which non-small cell lung cancer (NSCLC) patients account for a considerabl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/127A61K31/7068A61K47/34A61P35/00
Inventor 陶灵刚
Owner 灵康药业集团股份有限公司
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