Teniposide nanosuspension and preparation method thereof

A niposide nano- and nano-suspension technology, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, emulsion delivery, etc., can solve the problems of large toxic and side effects, poor patient compliance, and small drug loading. Achieve the effects of low toxic and side effects, small toxic and side effects, and large drug loading

Inactive Publication Date: 2015-01-21
HENAN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a teniposide nanosuspension, which solves the problems of small drug loading, large toxic and side effects and poor patient compliance in the existing teniposide preparations

Method used

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  • Teniposide nanosuspension and preparation method thereof
  • Teniposide nanosuspension and preparation method thereof
  • Teniposide nanosuspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] The teniposide nanosuspension of this embodiment contains 5 mg of teniposide and 5 mg of polyvinylpyrrolidone (PVP K30) per 1 ml of the nanosuspension, and the balance is water for injection.

[0049] The preparation method of the teniposide nanosuspension of the present embodiment comprises the following steps:

[0050] 1) Take 500mg of polyvinylpyrrolidone and dissolve it in water for injection to form an aqueous phase; take acetone as organic phase A for subsequent use;

[0051] 2) Dissolve 500 mg of teniposide in organic phase A to form organic phase B;

[0052] 3) Under the condition of stirring at room temperature and rotating speed of 10000rpm, after fully mixing the organic phase B obtained in step 2) with the aqueous phase obtained in step 1), a transparent teniposide emulsion with blue opalescence is formed, and then the acetone is removed by rotary evaporation , and dried in a vacuum drying oven at 40°C for 12 hours to further remove the organic solvent, dil...

Embodiment 2

[0058] The teniposide nanosuspension of this embodiment contains 5 mg of teniposide, 10 mg of polyethylene glycol vitamin E succinate (TPGS) per 1 ml of the nanosuspension, and the balance is water for injection.

[0059] The preparation method of the teniposide nanosuspension of the present embodiment comprises the following steps:

[0060] 1) Dissolve 100 mg of polyethylene glycol vitamin E succinate in water for injection to form an aqueous phase; take methanol as organic phase A for later use;

[0061] 2) Dissolve 50 mg of teniposide in organic phase A to form organic phase B;

[0062] 3) Under the conditions of room temperature and ultrasound (400W), fully mix the organic phase B obtained in step 2) with the aqueous phase obtained in step 1) to form a translucent teniposide emulsion with blue opalescence, and then rotary evaporate Remove methanol, and dry in a vacuum oven at 40°C for 12 hours to further remove the organic solvent, dilute to 10ml with water for injection,...

Embodiment 3

[0067] The teniposide nanosuspension of this embodiment contains 2 mg of teniposide, 1 mg of lecithin, and 0.5 mg of vitamin E per 1 ml of the nanosuspension, and the balance is water for injection.

[0068] The preparation method of the teniposide nanosuspension of the present embodiment comprises the following steps:

[0069] 1) Dissolve 1000mg of lecithin and 500mg of vitamin E in chloroform to form an organic phase A; take water for injection as the water phase and set aside;

[0070] 2) Dissolve 2000mg of teniposide in the organic phase A to form the organic phase B;

[0071] 3) Rotate the organic phase B obtained in step 2) to remove chloroform under reduced pressure, and dry it in a vacuum oven at 35°C for 10 hours to form a thin film; hydrate the thin film with the water phase, vortex it with 400W ultrasound for 4 minutes, and inject it with Dilute to 1000ml with water, and homogenize with a high-pressure homogenizer (20MPa, cycle 5 times) to obtain teniposide nanosus...

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Abstract

The invention discloses a teniposide nanosuspension and a preparation method thereof. Each 1ml of the nanosuspension contains 0.1-50mg of teniposide, 0.1-500mg of a stabilizer, 0-500mg of an additive, and the balance of water. Compared with commercially available teniposide injections (VUMON), teniposide intravenous emulsions, teniposide solid lipid nanoparticles and phospholipid complex liposomes, the teniposide nanosuspension has the advantages of high drug load, good stability, no carriers or co-solvents, avoiding of the use of organic solvents, low toxic side effects, reduction of the untoward reactions of patients, good patient compliance; high-efficiency low-toxicity performance of the antitumor activity of teniposide, good clinical curative effect and good application prospect.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a teniposide nano-suspension, and also relates to a preparation method of the teniposide nano-suspension. Background technique [0002] Teniposide is made from podophyllotoxin extracted from the plant of the genus Cephalophyllum through condensation, reduction, and condensation. It is also known as thienin and podophylloside. Desmethyl-epipodophyllotoxin-β-D-thiophenylidene glucopyranoside. Teniposide is a white or off-white crystalline powder, a neutral lipophilic substance, insoluble in water and ether, slightly soluble in methanol, and better soluble in dichloromethane. [0003] Teniposide is a cell cycle-specific antitumor drug. Its mechanism of action is to prevent cells from entering mitosis, making cells stagnate in late S or early G2, inhibiting eukaryotic protein synthesis, and making polyribose Body depolymerization, interfering with the function o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/7048A61P35/00
Inventor 和素娜牛永防李杰刘玲王淑英
Owner HENAN UNIV OF SCI & TECH
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