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Decitabine sustained release microsphere and preparation method thereof

A technology of decitabine and sustained-release microspheres, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. It can avoid direct contact, improve effective concentration, and achieve the effect of small loss

Active Publication Date: 2011-02-09
苏州科耐尔医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] At present, decitabine has only ordinary freeze-dried injections on the market at home and abroad, and the specified storage temperature is 25°C, which shows that the stability of this product is not good; The rapid inactivation of enzymes has a half-life of 15-25 minutes, and the half-life is relatively short, causing an increase in the clinical dosage (about 20,000 yuan / 50mg / bottle), which brings a serious burden to the patient's medical expenses; the adverse reactions of this product include leukopenia and thrombocytopenia , mild to moderate nausea, vomiting, etc., the main toxicity is bone marrow suppression

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] A kind of decitabine sustained-release microspheres, the process of its preparation is as follows:

[0064] ①Dissolve chitosan with 1%~5% acetic acid to prepare a 3.0%~10.0% (V / W) solution, add 0.15%~3% (V / W) drug decitabine, stir to disperse Evenly, use 0.1mol / L NaOH solution to adjust the pH value to 5-7 as the water phase;

[0065] ②Preparation containing 1.5%~3% (W / W) Span-20, 0.1%~0.2% (W / W) Pluronic F 68 The liquid paraffin solution is used as the oil phase;

[0066] ③According to the water phase: oil phase volume ratio 1:8~1:10, add the water phase to the oil phase dropwise, stir for 10~30 minutes at 15~25℃, 1200~1500r / min, and make W / O type Emulsion;

[0067] ④ adding a suitable crosslinking agent to the W / O emulsion for crosslinking and curing for 1 to 3 hours;

[0068] ⑤ Wash with an organic solvent for 2 to 3 times to remove the oil phase, and wash with a cross-linking agent washing reagent to remove the residual cross-linking agent;

[0069] ⑦ Wash with...

Embodiment 2

[0075] A kind of decitabine sustained-release microspheres, the process of its preparation is as follows:

[0076] ① Dissolve sodium alginate with water for injection to make a 1.0%-6.0% (W / V) sodium alginate solution, add 0.15%-3% (V / W) drug decitabine, stir to disperse evenly , using a suitable alkaline solution to adjust the pH value to 5-7 as the water phase;

[0077] ② Take calcium chloride and add water for injection to make a 2.0% to 4.0% (W / V) calcium chloride solution as a solidification solution;

[0078] ③Slowly add the solidified solution dropwise into the water phase under stirring, and stir for 10-30 minutes at 15-25°C and 1200-1500r / min;

[0079] ④ Suction filtration, suitable for washing with organic solvent or water for injection 3 to 4 times;

[0080] ⑤ The obtained product is aseptically freeze-dried to obtain decitabine sustained-release microspheres.

Embodiment 3

[0082] A kind of decitabine sustained-release microspheres, the process of its preparation is as follows:

[0083] ① Dissolve sodium alginate with water for injection to make a 1.0%-6.0% (W / V) sodium alginate solution, add 0.15%-3% (V / W) drug decitabine, stir to disperse evenly , using a suitable alkaline solution to adjust the pH value to 5-7 as the water phase;

[0084] ② Take calcium chloride and chitosan, add water for injection to make solutions containing calcium chloride 2.0% to 4.0% (W / V) and chitosan 0.1% to 0.3% (W / V);

[0085] ③ Slowly add the mixed solution of calcium chloride and chitosan into the water phase under stirring, and stir for 10-30 minutes at 15-25°C and 1200-1500r / min;

[0086] ④ Suction filtration, suitable for washing with organic solvent or water for injection 3 to 4 times;

[0087] ⑤ The obtained product is aseptically freeze-dried to obtain decitabine sustained-release microspheres.

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Abstract

The invention discloses a Decitabine sustained release microsphere, which comprises Decitabine and a carrier material, wherein the weight percentage of the Decitabine and the carrier material is 1-8%, the partical size of the Decitabine sustained release microsphere is below 10 mu m, and the entrapment rate of the Decitabine sustained release microsphere is more than 75%. The Decitabine sustainedrelease microsphere provided by the invention has higher loading rate, no in-vivo burst effect, stable blood concentration, and no drug release delivery deadtime, thus greatly reducing clinical interval of drug administration, reducing dosage, improving compliance of patients, and reducing hazard rating of adverse reaction.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an antitumor drug decitabine sustained-release microsphere and a preparation method thereof. Background technique [0002] Myelodysplastic syndrome (MDS) is an acquired stem cell disorder that causes ineffective hematopoiesis and peripheral blood cytopenias, with a tendency to develop into acute myeloid leukemia (AML). Its etiology is unknown, both men and women can be affected, men are more than women, more common in the elderly over 60 years old, it is estimated that 7000-12000 cases of MDS patients are newly diagnosed in the United States every year. In recent years, the incidence rate is on the rise. The clinical manifestations are abnormal changes in quality and quantity of hematopoietic cells, such as anemia, often accompanied by infection and (or) hemorrhage, and some (30%) can develop into acute leukemia. [0003] The treatment of MDS inc...

Claims

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Application Information

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IPC IPC(8): A61P35/02A61K47/36A61K31/706A61K9/16
Inventor 初虹王浩龚金红
Owner 苏州科耐尔医药科技有限公司
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