Medicine compound against acute myeloid leukemia

An acute myeloid and composition technology, applied in the direction of drug combination, antineoplastic drugs, active ingredients of hydroxyl compounds, etc., can solve problems such as no superiority found

Inactive Publication Date: 2012-04-11
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, its efficacy has not been found to be superior to existing drugs

Method used

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  • Medicine compound against acute myeloid leukemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 Preparation of all-trans retinoic acid / megestrol acetate / bezafibrate compound orally disintegrating tablet

[0027] Preparation prescription: 2g all-trans retinoic acid, 1g megestrol acetate, 100g bezafibrate, 80g microcrystalline cellulose, 60g mannitol, 30g low-substituted hydroxypropyl cellulose, 3g magnesium stearate, polyethylene Pyrrolidone 35g, made into 1000 tablets in total.

[0028] Preparation method: take the prescribed amount of all-trans retinoic acid, megestrol acetate, bezafibrate, microcrystalline cellulose, mannitol, and low-substituted hydroxypropyl cellulose, grind them separately, pass through a No. 4 sieve, and mix. Dissolve polyvinylpyrrolidone in an appropriate amount of 60% ethanol as a binder to make a soft material, wet granulate, dry at 60°C, sieve, add magnesium stearate, granulate, mix, and tablet. Instantly.

[0029] Disintegration time limit inspection: install a small cup on the dissolution tester, add 50ml of purified water ...

Embodiment 2

[0032] The preparation of embodiment 2 all-trans retinoic acid / megestrol acetate / bezafibrate compound liposome injection

[0033] (1) Dissolve 2 g of all-trans retinoic acid, 2 g of megestrol acetate, and 200 g of bezafibrate in 50 ml of phosphate buffer (pH 7.5), place it in a water bath at 65-70 ° C, keep warm, and set aside;

[0034] (2) 442g of stearoylphosphatidylcholine and 155g of cholesterol are dissolved in chloroform, and the chloroform in the solution is evaporated under reduced pressure with a rotary evaporator to form a lipid film;

[0035] (3) Take 50 ml of preheated all-trans retinoic acid / megestrol acetate / bezafibrate phosphate buffer solution to hydrate the lipid film. The hydration temperature is 65-70°C. After hydration, use a high-pressure homogenizer to pass through a polycarbonate film with a pore size of 50 nm. Dilute the water for injection to 5000ml, and pack it into 5ml / bottle after sterilization.

Embodiment 3

[0036] Example 3 Preparation of all-trans retinoic acid / megestrol acetate / bezafibrate compound folic acid targeting liposome

[0037] Preparation prescription:

[0038] All-trans retinoic acid 2g

[0039] Megestrol Acetate 2g

[0040] Bezafibrate 200g

[0041] Distearoylphosphatidylcholine 442g (0.56mol)

[0042] Cholesterol 155g (0.4mol)

[0043] PEG2000-phosphatidylethanolamine 104g (0.037mol)

[0044] Folic acid-cysteine-PEG3400-phosphatidylethanolamine 15g (0.003mol)

[0045] PEG2000-phosphatidylethanolamine (2805.497) was purchased from Lipoid GmbH, Germany; folic acid-cysteine-PEG3400-phosphatidylethanolamine was purchased from Endocyte, USA; phosphatidylcholine and cholesterol were purchased from Sigma, USA

[0046] Preparation:

[0047] (1) Dissolve 2 g of all-trans retinoic acid, 2 g of megestrol acetate, and 200 g of bezafibrate in 50 ml of phosphate buffer (pH 7.5) and place it in a water bath at 65-70 ° C, keep warm, and set aside;

[0048] (2) Dissolve st...

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Abstract

The invention discloses a medicine compound against acute myeloid leukemia; each unit dose of the medicine compound contains 2mg of all-trans-retinoic acid, 1 to 2mg of megestrol acetate, 100 to 200mg of bezafibrate and a carrier acceptable of medical science, and the mass ratio of megestrol acetate to bezafibrate is 1:100. The medicine compound can significantly improve the survival rate of patients with acute myeloid leukemia, and can open up a new way for clinical treatment.

Description

technical field [0001] The invention relates to an anti-acute myeloid leukemia pharmaceutical composition, in particular to an anti-acute myeloid leukemia pharmaceutical composition containing bezafibrate and megestrol. Background technique [0002] The incidence rate of leukemia in my country is 2.76 / 10 5 , among which the annual incidence rate of acute myeloid leukemia (AML) is the highest, reaching 1.62 / 10 5 . AML is a serious type of leukemia, which is mainly caused by the excessive proliferation of abnormal hematopoietic cells caused by the abnormal clone of myeloid hematopoietic stem cells, the inhibition of differentiation and the inhibition of apoptosis. Its incidence rate increases with age, and the median age is 65 to 70 years old. Clinically, the treatment of acute myeloid leukemia is more difficult, on the one hand because of its rapid onset, on the other hand because the vast majority of patients are elderly with weak physical functions and often cannot toler...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/57A61K31/192A61K31/203A61K47/34A61P35/02A61K47/28
Inventor 厉保秋
Owner SHANDONG UNIV
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