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Stable supersaturated gemcitabine hydrochloride solution and its prepn process

A gemcitabine hydrochloride solution technology, which is applied in the field of supersaturated drug solution and its preparation, can solve the problems of difficult preparation of high-concentration injections and increase of degradation products, etc.

Active Publication Date: 2007-12-19
QILU PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] When preparing injections according to CN1650883A, the solubility of gemcitabine hydrochloride is only 15g / L at 23°C and pH 4-7, making it difficult to prepare high-concentration injections, and the prepared solution is placed at 60°C for 10 days, and the degradation products increase significantly

Method used

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  • Stable supersaturated gemcitabine hydrochloride solution and its prepn process

Examples

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Embodiment 1

[0034] Example 1: Get 227.7 mg of gemcitabine hydrochloride (containing 200 mg of gemcitabine), dissolve it with 6 ml of water for injection, add 0.09 g of sodium chloride, and then add 0.5 N sodium hydroxide to adjust the pH to 4.5. The above solution is heated to 30-40 ° C, Dissolve the precipitated crystals completely, and dilute to 10ml with water for injection. Then sterilize and filter while it is hot, pack in 10ml ampoules, each 10ml, and seal.

Embodiment 2

[0035] Embodiment 2: get gemcitabine hydrochloride 341.6mg (containing gemcitabine 300mg), dissolve with 6ml water for injection, add 0.09g sodium chloride, then add 0.5N sodium hydroxide, adjust pH to be 6.0, above-mentioned solution is heated to 50~60 ℃, Dissolve the precipitated crystals completely, and dilute to 10ml with water for injection. Then sterilize and filter while hot, pack in ampoules, fill with nitrogen, and seal.

Embodiment 3

[0036]Embodiment 3: get gemcitabine hydrochloride 455mg (containing gemcitabine 400mg), dissolve with 6ml water for injection, add 0.09g sodium chloride, then add 0.5N sodium hydroxide, adjust pH to be 5.5, above-mentioned solution is heated to 60~80 ℃, makes The precipitated crystals were completely dissolved and diluted to 10ml with water for injection. Then sterilize and filter while hot, pack in 5ml ampoules, each 5ml, fill with nitrogen, and seal.

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Abstract

The present invention discloses stable supersaturated gemcitabine hydrochloride solution and its preparation process. Gemcitabine hydrochloride in certain amount is heated in pH 4-8 condition for being dissolved completely to obtain supersaturated gemcitabine hydrochloride solution of 45 g / l concentration, higher than the saturation concentration at 23 deg.c, and the supersaturated gemcitabine hydrochloride solution is packed in single dosage container while the solution is still hot. The supersaturated gemcitabine hydrochloride solution may be maintained at room temperature without separating out, and filling nitrogen and / or adding antioxidant can further raise the chemical stability. It may be used in preparing gemcitabine hydrochloride preparation for intravenous injection.

Description

technical field [0001] The invention relates to a supersaturated solution of medicine and a preparation method thereof, in particular to a supersaturated solution containing gemcitabine hydrochloride and a preparation method thereof. Background technique [0002] Gemcitabine, English name Gemcitabine, its chemical name is 2'-deoxy-2', 2'-difluoroadenosine (β-isomer), and its molecular formula is C 9 h 11 f 2 N 3 o 4 , the molecular weight is 299.66. [0003] Gemcitabine is an anti-tumor drug produced by Lilly Pharmaceutical Company of the United States. In 1996, the US FDA approved it as a first-line drug for the treatment of pancreatic cancer and in 1998 as a drug for the treatment of non-small cell lung cancer. my country approved the import in 1999, and domestic imitation products were approved for clinical trials on June 15, 2000. [0004] At present, the gemcitabine produced both at home and abroad is gemcitabine hydrochloride freeze-dried powder injection. The r...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/7068A61K47/02A61K47/06A61P35/00
CPCA61K9/0019A61K31/7068A61P35/00
Inventor 杨清敏刘宝明张桂婷韩作宏张明会王晶翼
Owner QILU PHARMA HAINAN
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