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Curcumenol nanosuspension, and preparation method and application thereof

A technology of nano-suspension and curcumol, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of limited experimental research and clinical use, low solubility of curcumol, biological Problems such as poor utilization rate can achieve the effect of promoting further research and development, improving bioavailability and low cost

Active Publication Date: 2017-01-25
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Due to the extremely low solubility of curcumol in water, resulting in incomplete absorption or poor bioavailability, which greatly limits experimental research and clinical use, there is currently no preparation product on the market

Method used

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  • Curcumenol nanosuspension, and preparation method and application thereof
  • Curcumenol nanosuspension, and preparation method and application thereof
  • Curcumenol nanosuspension, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 conditional screening

[0034] Curcumol nano-suspension preparation method is as follows:

[0035] 1) Dissolve 50 mg of curcumol completely in 1 ml of absolute ethanol to obtain an organic phase.

[0036] 2) Dissolve 25mg of PVP and 25mg of lecithin in 50ml of purified water to obtain an aqueous phase.

[0037] 3) In an ice-water bath (0°C), under stirring (3×10 3 r·min-1), slowly drop the organic phase into the water phase to make it evenly dispersed. After the dropwise addition, spin off the ethanol to obtain a coarse suspension.

[0038] 4) Dilute the obtained coarse suspension in 2×10 4 High-speed shearing at rpm for 4min, 13.6×10 7 Homogenize 15 times under Pa pressure to obtain curcumol nanosuspension.

[0039] (1) Show the influence of the active agent

[0040] Other conditions remain unchanged, as shown in Table 1, the surfactant in step 2) is changed.

[0041] Table 1 Effect of Surfactant

[0042]

[0043] Note:-.No surfactant added.

[0...

Embodiment 2

[0059] Embodiment 2 curcumol nanosuspension

[0060] Curcumol nano-suspension preparation method is as follows:

[0061] 1) Dissolve 50 mg of curcumol completely in 1 ml of absolute ethanol to obtain an organic phase.

[0062] 2) Dissolving 12.5-200mg of PVP and 25mg of lecithin in 50ml of purified water to obtain an aqueous phase.

[0063] 3) In an ice-water bath (0°C), under stirring (3×10 3 r·min -1 ), slowly drop the organic phase into the water phase to make it evenly dispersed. After the dropwise addition, spin off the ethanol to obtain a coarse suspension.

[0064] 4) Dilute the obtained coarse suspension in 2×10 4 High-speed shearing at rpm for 4min, 13.6×10 7 Homogenize 15 times under Pa pressure to obtain curcumol nanosuspension. The results are shown in Table 4.

[0065] Table 4 Effect of Surfactant

[0066]

[0067] As can be seen from Table 4, when curcumol: lecithin: PVP=1:0.5:0.5, the particle size is the smallest, which is the optimum surfactant dos...

Embodiment 3

[0068] Embodiment 3 curcumol nanosuspension lyophilized powder

[0069] Curcumol nano-suspension lyophilized powder preparation method is as follows:

[0070] 1) Dissolve 50 mg of curcumol completely in 1 ml of absolute ethanol to obtain an organic phase.

[0071] 2) Dissolve 25mg of PVP and 25mg of lecithin in 50ml of purified water to obtain an aqueous phase.

[0072] 3) In an ice-water bath (0°C), under stirring (3×10 3 r·min -1 ), slowly drop the organic phase into the water phase to make it evenly dispersed. After the dropwise addition, spin off the ethanol to obtain a coarse suspension.

[0073] 4) Dilute the obtained coarse suspension in 2×10 4 High-speed shearing at rpm for 4min, 13.6×10 7 Homogenize 15 times under Pa pressure to obtain curcumol nanosuspension.

[0074] 5) As shown in Table 5, add the lyophilized powder into the prepared curcumol suspension, shake well, freeze in a -80°C refrigerator for 24 hours, and freeze-dry in a freeze dryer for 8 hours to ...

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Abstract

The invention relates to a curcumenol nanosuspension, and a preparation method and application thereof, and belongs to the field of pharmaceutical preparations. According to the invention, the curcumenol nanosuspension is prepared by adopting a precipitation method in combination with high-speed shearing and high-pressure homogenization. The prescription is optimized by using particle size and polydispersity index (PDI) as indicators, the form of the preparation is inspected by means of a transmission electron microscope, and the dissolution of the drug is inspected by means of in-vitro release experiments. The curcumenol nanosuspension provided by the invention is characterized in that the curcumenol nanosuspension comprises curcumenol, lecithin and PVP (polyvinyl pyrrolidone), wherein the mass ratio of the curcumenol to the lecithin to the PVP is 1:(0.4-0.6):(0.25-4); the particle size of drug in the suspension is 50-500 nm; and the curcumenol concentration in the suspension is 0.25-1 mg / ml. The nanosuspension preparation method provided by the invention is simple, controllable and suitable for industrial production, and improves the drug dissolution.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a preparation method of curcumol nano-suspension and freeze-dried powder thereof. Background technique [0002] Curcumol is an important component extracted from the volatile oil of Curcuma Phaeocaulis Val. Curcumol is considered to be the characteristic component of Curcuma, and it is one of the important material bases for the antitumor efficacy of Curcuma oil. Compared with chemically synthesized anticancer drugs, curcumol has less adverse reactions and is suitable for long-term medication. Traditional Chinese medicine believes that curcumol has obvious curative effects on various cancers such as liver cancer, gastric cancer, ascites cancer, leukemia, and gynecological tumors, and has great development prospects in the application of anti-tumor drugs. [0003] Nanosuspensions (nanosuspensions, NS) are submicron colloidal dispersions of pure drug nanoparticles, whic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K47/32A61K47/24A61K9/19A61K47/26A61K31/352A61P35/00
CPCA61K9/10A61K9/19A61K31/352A61K47/24A61K47/26A61K47/32
Inventor 刘宇吴浩天陈立江
Owner LIAONING UNIVERSITY
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