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Azacitidine freeze-dried preparation for injection and preparation method thereof

A technology of azacitidine and freeze-dried preparations is applied in the field of stable freeze-dried preparations of azacitidine for injection and its preparation, which can solve the problem of affecting the bioequivalence of reconstituted suspension and affecting the crystal grains in the pre-freezing stage. It can solve problems such as path and path, and achieve the effect of solving the peak-to-valley fluctuation of blood drug concentration, solving frequent dosing and high encapsulation efficiency.

Active Publication Date: 2020-10-16
SHANGHAI HANSOH BIOMEDICAL +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The study found that the ethanol, isopropanol, methanol and other hydroxy alcohol organic solvents used in this patent will interact with the hydroxyl groups in mannitol and azacitidine, which will significantly affect the particle size of the crystals in the pre-freezing stage, which will affect the complex process. Bioequivalence of Suspensions

Method used

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  • Azacitidine freeze-dried preparation for injection and preparation method thereof
  • Azacitidine freeze-dried preparation for injection and preparation method thereof
  • Azacitidine freeze-dried preparation for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The azacitidine of 2 weight parts, the gelatin of 1 weight part are dissolved in the water of 6 volume parts, dissolve and mix as internal water (W 1 ) phase; 5 parts by weight of polylactic acid-glycolic acid (the molar ratio of lactic acid and glycolic acid in polylactic acid-glycolic acid is 75 / 25, molecular weight 6000) is dissolved in 60 parts by volume of dichloromethane as oil (O) Phase; 5 parts by weight of polyvinyl alcohol was dissolved in 600 parts of water for injection at 75°C as (W 2 ) phase; the W 1 Slowly drop the phase into the O phase, emulsify at a high speed of 18000r / min for about 3~5min, and add W 2 In the phase, 18000r / min high-speed oscillation emulsification for 3~5min, 500r / min for 3h to evaporate dichloromethane, 12000r / min high-speed centrifugation, wash 5 times with water for injection, sub-package, freeze-dry to obtain.

[0037] The freeze-drying method is:

[0038] The lyophilizer is cooled to -40°C in advance, and the filled samples ar...

Embodiment 2

[0040] The azacitidine of 2 weight parts, the gelatin of 1 weight part are dissolved in the water of 6 volume parts, dissolve and mix as internal water (W 1 ) phase; 3 parts by weight of polylactic acid-glycolic acid (the molar ratio of lactic acid and glycolic acid in polylactic acid-glycolic acid is 75 / 25, molecular weight 6000) is dissolved in 60 parts by volume of dichloromethane as oil (O) Phase; 5 parts by weight of polyvinyl alcohol was dissolved in 600 parts of water for injection at 75°C as (W 2 ) phase; the W 1 Slowly drop the phase into the O phase, emulsify at a high speed of 18000r / min for about 3~5min, and add W 2In the phase, 18000r / min high-speed oscillation emulsification for 3~5min, 500r / min for 3h to evaporate dichloromethane, 12000r / min high-speed centrifugation, wash 5 times with water for injection, sub-package, freeze-dry to obtain. The freeze-drying method is the same as in Example 1.

Embodiment 3

[0042] The azacitidine of 2 weight parts, the gelatin of 1 weight part are dissolved in the water of 6 volume parts, dissolve and mix as inner water (W 1 ) phase; 6 parts by weight of polylactic acid-glycolic acid (the molar ratio of lactic acid and glycolic acid in polylactic acid-glycolic acid is 75 / 25, molecular weight 6000) is dissolved in 60 parts by volume of dichloromethane as oil (O) Phase; 10 parts by weight of polyvinyl alcohol was dissolved in 1000 parts of water for injection at 75°C as (W 2 ) phase; the W 1 Slowly drop the phase into the O phase, emulsify at a high speed of 18000r / min for about 3~5min, and add W 2 In the phase, 18000r / min high-speed oscillation emulsification for 3~5min, 500r / min for 3h to evaporate dichloromethane, 12000r / min high-speed centrifugation, wash 5 times with water for injection, sub-package, freeze-dry to obtain. The freeze-drying method is the same as in Example 1.

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly provides a stable azacitidine freeze-dried preparation for injection and a preparation method thereof. Theazacitidine freeze-dried preparation for injection is prepared from azacitidine, gelatin and polylactic acid-glycolic acid. The azacitidine freeze-dried preparation for injection is high in stability, high in encapsulation efficiency and proper in drug loading capacity, the effective blood concentration of drugs can be maintained for a long time, the peak-valley fluctuation of the blood concentration is reduced, the administration frequency is reduced, the compliance of a patient is improved, and the problems of the peak-valley fluctuation of the blood concentration and frequent administration caused by conventional preparations are solved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a stable freeze-dried preparation of azacitidine for injection and a preparation method thereof. Background technique [0002] Myelodysplastic syndromes (myelodysplastic syndromes, MDS) are a group of heterogeneous myeloid clonal diseases originating from hematopoietic stem cells, characterized by abnormal differentiation and development of myeloid cells, manifested as ineffective hematopoiesis, refractory hematopoiesis, hematopoietic Functional failure, high risk of transformation 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-transformed (REAB) -T) and chronic myelomonocytic leukemia (CMML). [0003] Azacitidine (Azacitidine) is a DNA methyltransferase inhibitor that can cause D...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K9/52A61K31/706A61K47/34A61K47/42A61P7/00A61P7/06A61P35/02
CPCA61K9/0019A61K9/19A61K9/5031A61K9/5057A61K9/5089A61K31/706A61K47/34A61K47/42A61P7/00A61P7/06A61P35/02
Inventor 张春林申升秦梦郭彦亮张小兵陈晶
Owner SHANGHAI HANSOH BIOMEDICAL
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