Felodipine nano suspension and preparation method thereof

A nano-suspension, Dipin nano technology, applied in the field of medicine, can solve problems such as difficult large-scale preparation, and achieve the effect of mild preparation method conditions and low preparation cost

Active Publication Date: 2013-08-21
江苏一南生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The felodipine nanosuspension reported in the literature is prepared

Method used

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  • Felodipine nano suspension and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0021] Dissolve 0.1 g of felodipine and 0.01 g of copovidone PVP S 630 in 80 mL of absolute ethanol, slowly add 0.01 g of PVP K-90 into 1000 mL of water, and evaporate at 40 °C to evaporate the ethanol. The felodipine nanosuspension was obtained, and the concentration of felodipine was 0.1 mg / ml. The average particle diameter of the felodipine nanosuspension was measured, and the result was 385 nm, and the suspension remained stable within 48 h.

Embodiment 2

[0023] Dissolve 0.1 g of felodipine and 0.04 g of copovidone PVP S 630 in 100 mL of 95% ethanol, slowly add 0.04 g of PVP K-90 into 400 mL of water, evaporate at 40 °C, and evaporate the ethanol. The felodipine nanosuspension was obtained, and the concentration of felodipine was 0.25 mg / ml. Measure the average particle diameter of felodipine nano-suspension, the result is 126 nm (the transmission electron microscope figure of felodipine nano-suspension is shown in figure 1 ), the suspension remained stable within 48 h.

Embodiment 3

[0025] Dissolve 0.1 g of felodipine and 0.02 g of copovidone PVP S 630 in 80 mL of absolute ethanol, slowly add 0.02 g of PVP K-90 into 200 mL of water, and evaporate at 40 °C to evaporate the ethanol. The felodipine nanosuspension was obtained, and the concentration of felodipine was 0.5 mg / ml. The average particle diameter of the felodipine nanosuspension was measured, and the result was 338 nm, and the suspension remained stable within 48 h.

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Abstract

The invention belongs to the technical field of medicine, and discloses a felodipine nano suspension and a preparation method thereof. Due to low water solubility and low oral bioavailability, the popularization and application of felodipine are restricted. The felodipine nano suspension disclosed by the invention is characterized by containing felodipine, copovidone PVPS630 and povidone PVPK-90, wherein the mass ratio of the felodipine to the copovidone PVPS630 to the povidone PVPK-90 is (10-5):(1-2):(1-2). According to the invention, the preparation method of the nano suspension is moderate in conditions, simple and controllable; and the felodipine achieves high oral bioavailability.

Description

technical field [0001] The invention relates to a felodipine nano-suspension and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Felodipine is a selective dihydropyridine calcium ion channel blocker developed by Sweden's Astra Company. It was first listed in Denmark in 1988. It is a highly effective, safe and well-tolerated drug for treating hypertension. It is effective for the elderly Or patients with coronary heart disease, heart failure, renal insufficiency, asthma, peripheral vascular disease, gout or diabetes are relatively safe. [0003] Felodipine belongs to the second class of drugs in the biopharmaceutical classification system. Its solubility is small, and its transmembrane rate is normal. The dissolution rate is the rate-limiting step of its bioavailability. effective way of utilization. On the other hand, felodipine has a first-pass effect in the absorption process. If the drug dissolves slowly, the met...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/4422A61K47/32A61P9/12
Inventor 罗瑞雪张振海
Owner 江苏一南生物科技有限公司
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