Acitidine for injection and preparation method thereof

A technology for azacitidine and injection, applied in the field of pharmaceutical preparations, can solve the problems of poor compliance, long reconstitution time, uneven dispersion, etc., and achieves convenient clinical use, high patient acceptance, and short reconstitution time. Effect

Inactive Publication Date: 2017-09-08
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Patent CN103251564A and patent CN105769775A disclose azacitidine for injection and its preparation method. By controlling the dispensing temperature and adjusting the pH value of the solution, each tube is filled with 25ml and 23ml respectively. The freeze-drying process is not good, and finally the The particle size of the freeze-dried powder is not good, and the particle size and sedimentation volume ratio of the suspension are not good when used as intramuscular injection
[0007] Patent CN104739778A discloses azacitidine for injection and its preparation method. The pH value is adjusted by adding phosphate buffered saline, and each tube is filled with 10ml. Although the freeze-drying cycle is shortened to save costs, it does not take into account when it is administered as an intravenous injection. Effects of reconstitution time and particle size of suspension during intramuscular injection on drug absorption and patient compliance
[0008] The azacitidine freeze-dried powder prepared by the above-mentioned patented method takes a long time for reconstitution during intravenous administration, which affects product quality. The absorption of the drug, the uneven dispersion of the drug in the solvent, can easily lead to local swelling and pain in the patient's muscles, and poor compliance

Method used

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  • Acitidine for injection and preparation method thereof
  • Acitidine for injection and preparation method thereof
  • Acitidine for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] 1) Prescription

[0025] Azacitidine 50g

[0026] Mannitol 50g

[0027] Water for injection to 5L

[0028] 2) Preparation of azacitidine freeze-dried powder for injection:

[0029] Accurately weigh 90% of the prescribed amount of water for injection; weigh the prescribed amount of azacitidine and mannitol, slowly add to the water for injection, and stir to dissolve. Sampling and testing the content of intermediate products; according to the test results of intermediates, fill the liquid medicine in 10ml / bottles into vials, and half-stopper; the freeze dryer is cooled to -40°C in advance, and the filled samples are sent to the freeze-drying box. Keep it for 2.5 hours; evacuate the freeze dryer and keep it at 0.15±0.02mbar, raise the temperature of the shelf to -10℃ at 10℃ / h, and keep it for 5 hours; then raise the temperature of the shelf to -5℃ at 10℃ / h, Keep warm for 8 hours; the shelf temperature is raised to 20°C at 20°C / h, and held for 8 hours; the shelf tempera...

Embodiment 2

[0031] 1) Prescription

[0032] Azacitidine 50g

[0033] Mannitol 50g

[0034] Water for injection up to 7.5L

[0035] 2) Preparation of azacitidine freeze-dried powder for injection:

[0036] Accurately weigh 90% of the prescribed amount of water for injection; weigh the prescribed amount of azacitidine and mannitol, slowly add to the water for injection, and stir to dissolve. Sampling to detect the content of the intermediate product; according to the test result of the intermediate, fill the liquid medicine into a vial with a volume of 15ml / bottle, and half stopper; the freeze dryer is cooled to -40°C in advance, and the filled sample is sent to the freeze-drying box. Keep it for 2.5 hours; evacuate the freeze dryer and keep it at 0.15±0.02mbar, raise the temperature of the shelf to -10℃ at 10℃ / h, and keep it for 5 hours; then raise the temperature of the shelf to -5℃ at 10℃ / h, Keep warm for 8 hours; the shelf temperature is raised to 20°C at 20°C / h, and held for 8 hour...

Embodiment 3

[0038] 1) Prescription

[0039] Azacitidine 50g

[0040] Mannitol 50g

[0041] Water for injection up to 10L

[0042] 2) Preparation of azacitidine freeze-dried powder for injection:

[0043] Accurately weigh 90% of the prescribed amount of water for injection; weigh the prescribed amount of azacitidine and mannitol, slowly add to the water for injection, and stir to dissolve. Sampling to detect the content of the intermediate product; according to the test result of the intermediate, fill the liquid medicine in a 20ml / bottle into a vial, and half stopper it; the freeze dryer is cooled to -40°C in advance, and the filled sample is sent to the freeze-drying box. Keep it for 2.5 hours; evacuate the freeze dryer and keep it at 0.15±0.02mbar, raise the temperature of the shelf to -10℃ at 10℃ / h, and keep it for 5 hours; then raise the temperature of the shelf to -5℃ at 10℃ / h, Keep warm for 8 hours; the shelf temperature is raised to 20°C at 20°C / h, and held for 8 hours; the she...

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PUM

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Abstract

The invention belongs to the technical field of Western medicinal preparations, and particularly provides freeze-dried azacitidine powder for injection and a preparation method thereof. Mainly through control over the unit filling volume and optimization on a freeze-drying process, the freeze-dried powder with smaller particle size is prepared; when the freeze-dried powder is applied to intramuscular injection, a suspension prepared from the freeze-dried powder has the smallest particle size and the maximum settling speed rate and is good in stability, easy to absorb and good in patient compliance; when the freeze-dried powder is applied to intravenous injection, the redissolution time is shortest, visible foreign matters meet requirements, few impurities are contained, and the stability is higher.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to azacitidine for injection and a preparation method thereof. Background technique [0002] Myelodysplastic syndrome (MDS) is a group of diseases characterized by clonal abnormalities of hematopoietic stem cells, which can lead to hematopoietic failure and a high risk of progression to acute myeloid leukemia (AML). The disease is divided into 5 types, namely refractory anemia (RA), ring sideroblastic anemia, refractory anemia with increased blasts (REAB), refractory anemia with increased blasts-transition (RAEB) -T) and chronic myelomonocytic leukemia (CMML). [0003] Azacitidine (Azacitidine) is a DNA methyltransferase inhibitor, which can cause DNA hypomethylation and has direct cytotoxicity. It was developed by Pharmion Pharmaceutical Company of the United States. In May 2004, the FDA approved the drug Vidaza for the treatment of all subtypes of...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/706A61P7/06A61P7/00
Inventor 张贵民贾俊伟秦士慧
Owner LUNAN PHARMA GROUP CORPORATION
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