A kind of gambogic acid nanosuspension and preparation method thereof

A technology of nano-suspension and gambogic acid, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problems of unsafe clinical use, low bioavailability, and allergic reactions. and other issues, to achieve the effect of improving bioavailability, improving solubility and high safety

Active Publication Date: 2021-03-05
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, in the existing preparations of gambogic acid, solubilizers or co-solvents are often added to improve the solubility of gambogic acid, but the addition of solubilizers will cause a series of side effects, such as allergic reactions, nephrotoxicity, cardiotoxicity and neurotoxicity
Some researchers have also studied new dosage forms of gambogic acid, but most of them have defects such as poor stability and unsafe clinical use, so it is imminent to study a new preparation of gambogic acid to solve its defects such as poor solubility and low bioavailability

Method used

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  • A kind of gambogic acid nanosuspension and preparation method thereof
  • A kind of gambogic acid nanosuspension and preparation method thereof
  • A kind of gambogic acid nanosuspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1 a kind of gambogic acid nano-suspension

[0024] The specific preparation method is as follows:

[0025] 1) Completely dissolve 30 mg of gambogic acid in 1 ml of absolute ethanol to obtain an organic phase.

[0026] 2) Dissolving 20 mg of poloxamer 188 in 40 ml of purified water to obtain an aqueous phase.

[0027] 3) Under the conditions of ice-water bath and stirring, slowly drop the organic phase into the water phase to make it evenly dispersed, stir magnetically for 20 minutes, and then spin off the ethanol to obtain a coarse suspension.

[0028] 4) Use a high-speed shearing machine to shear the obtained coarse suspension at 20000rpm for 5min to make it evenly dispersed, pass the obtained mixed solution through the micro jet, first pre-homogenize at 5460psi for 3 times, and then pre-homogenize at 0psi, 6990psi, 9320psi, Homogenize 15 times under the conditions of 11650psi, 13980psi and 16310psi to obtain the gambogic acid nanosuspension. Three batche...

Embodiment 2

[0032] Embodiment 2 a kind of gambogic acid nano-suspension

[0033] Concrete method is the same as embodiment 1, step 4) middle and high pressure homogenization pressure is selected as 11650psi, keeps other conditions constant, just changes the number of times of high pressure homogenization, that is, step 4) utilizes the mixed solution after high-speed shearing, first 5460psi pre-homogenization Massage 3 times, and then use 11650psi to homogenize 2, 4, 8, 12, 18, 24 times respectively to obtain the gambogic acid nanosuspension. Three batches of samples were prepared in the same way, and the particle size of the obtained preparation was measured by a particle size analyzer. The results are shown in Table 2.

[0034] Table 2

[0035]

[0036] As can be seen from Table 2, the size of the particle size of the nanosuspension is correlated with the number of homogenization, which decreases with the increase of the number of times, and after reaching a certain number of times, ...

Embodiment 3

[0037] Embodiment 3 a kind of gambogic acid nano-suspension

[0038] The specific method is the same as in Example 1, the high-pressure homogeneous pressure in step 4) is selected as 11650psi, and other conditions are kept unchanged, only the amount of surfactant poloxamer 188 is changed, and in step 2), poloxamer 188 is changed. Amounts of 8, 12, 16, 20, 24 and 28 mg were dissolved in 40 ml of purified water to obtain an aqueous phase. Gambogic acid nano-suspension was obtained, and the particle size of the obtained preparation was measured by a particle size analyzer, and the results are shown in Table 3.

[0039] table 3

[0040] No. Poloxamer 188(mg) Particle size (nm) PDI 1 8 329.9 0.311 2 12 314.4 0.227 3 16 303.2 0.205 4 20 301.5 0.194 5 24 268.8 0.181 6 28 272.2 0.215

[0041] It can be seen from Table 3 that when the amount of poloxamer 188 is 24 mg, the particle size is smaller and the PDI is the smalles...

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Abstract

The invention discloses a gambogic acid nano-suspension, which is prepared from gambogic acid and a surfactant, and the surfactant is poloxamer 188. The preparation method is as follows: 1) Weigh gambogic acid crude drug and dissolve it with absolute ethanol to obtain an organic phase; 2) Dissolve a surfactant in pure water to obtain an aqueous phase; 3) Under conditions of ice-water bath and stirring, the Add the dehydrated ethanol solution of gambogic acid to the water phase, stir magnetically, so that the gambogic acid is evenly dispersed in the aqueous solution of the surfactant, and the ethanol is removed by rotary evaporation to obtain a coarse suspension; 4) the coarse suspension is sequentially Perform high-speed shearing treatment and high-pressure homogenization treatment to obtain gambogic acid nano-suspension. The preparation of the gambogic acid nano-suspension in the present invention can improve the solubility of the drug, improve the safety of the drug, change the distribution of the drug in the body, reduce the dosage of the drug, reduce the toxic and side effects, improve the safety and compliance, and play a better role in the treatment. Effect.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a gambogic acid nano-suspension and a preparation method thereof. Background technique [0002] Gambogic acid (gambogic acid, GA) is obtained from the acidic resin of Gambogic, a natural compound with significant anti-tumor activity, and it has a certain inhibitory effect on cell lines such as human lung adenocarcinoma and human gastric cancer. It can play an anti-tumor effect by inhibiting the synthesis of DNA in the organism, inhibiting the phosphorylation of tyrosine kinase, etc., and is a tumor cell apoptosis inducer with multiple targets. Although gambogic acid has strong anti-tumor ability, its poor water solubility (less than 0.5 μg / mL) is a major problem to be solved in its clinical application. Gambogic acid has a high plasma clearance rate and a wide range of distribution in the body, resulting in low bioavailability, which greatly limits the clinical promoti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K9/19A61K31/352A61K47/10A61P35/00
CPCA61K9/10A61K9/19A61K31/352A61K36/185A61K47/10
Inventor 陈立江李丽张金凤张文君刘宇梁啸
Owner LIAONING UNIVERSITY
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