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Cucurbitacin E nano suspension composition and preparations thereof
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A technology of nano-suspension and cucurbitacin, which is applied in the field of medicine, can solve the problems of low content of insoluble drugs, increase the incidence of adverse reactions, increase preparations, etc., and achieve fast absorption in the body, easy productization, and loading The effect of large doses
Inactive Publication Date: 2014-07-23
SHENYANG PHARMA UNIVERSITY
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Problems solved by technology
Usually the content of insoluble drugs in the preparation is not high, in order to achieve the therapeutic drug concentration, only increase the dosage of the preparation, which increases the incidence of adverse reactions to a certain extent
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Embodiment 1
[0057] The preparation of embodiment 1 cucurbitacin E nanosuspension
[0058] prescription:
[0059] Cucurbitacin E 5.0mg
[0060] Soy Lecithin 0.75g
[0061] tert-butanol 5.0mL
[0062] Distilled water 45.0mL
[0063] Preparation Process:
[0064] Cucurbitacin E nanosuspension was prepared by probe ultrasonic controlled precipitation method. Dissolve cucurbitacin E in tert-butanol to prepare the organic phase according to the prescription amount, disperse soybean lecithin in water as the water phase, add the organic phase to the water phase in a rapid injection during the ultrasonic working period, and the ultrasonic power is 400W. The ultrasonic time is 6 min, and the ultrasonic process needs to be carried out under an ice bath.
Embodiment 2
[0065] The preparation of embodiment 2 cucurbitacin E nanosuspensions
[0066] prescription:
[0067] Cucurbitacin E 50mg
[0068] Soy Lecithin 50mg
[0069] Distilled water 45.0mL
[0070] Preparation Process:
[0071] Cucurbitacin E nanosuspension was prepared by high pressure homogenization method. Add cucurbitacin E and soybean lecithin into water according to the prescription amount, stir and disperse, and high-pressure homogenize the primary suspension under the conditions of 2 cycles at 200 bar and 10 cycles at 800 bar to obtain cucurbitacin E nanosuspension.
Embodiment 3
[0072] The preparation of embodiment 3 cucurbitacin E nanosuspensions
[0073] prescription:
[0074] Cucurbitacin E 10.0mg
[0075] Soy Lecithin 3.0g
[0076] Poloxamer 188 0.2g
[0077] Ethanol 4.0mL
[0078] Distilled water 45.0mL
[0079] Preparation Process:
[0080] Cucurbitacin E nanosuspension was prepared by probe ultrasonic controlled precipitation method. Dissolve cucurbitacin E in ethanol to prepare the organic phase according to the prescription amount, disperse soybean lecithin in water as the water phase, and add the organic phase to the water phase in the way of rapid injection during the ultrasonic working period, the ultrasonic power is 300W, and the ultrasonic time The sonication process should be carried out in an ice bath for 8 minutes.
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Abstract
The invention discloses a cucurbitacin E nano suspension composition and a preparation method thereof. The cucurbitacin E nano suspension freeze-dried composition is successfully prepared from medicines and a surfactant by a controlled precipitation method and / or a high-pressure homogenizing method in combination with a freeze-drying technique. The cucurbitacin E nano suspension composition comprises cucurbitacin E and a surfactant, wherein the proportion of the cucurbitacin E to the surfactant is 1:300-1:1, and the surfactant is phospholipid or a combination of phospholipid and other surfactants. The composition can be directly applied, or prepared into tablets, capsules, injections and the like after adding forming agents. The nano suspension disclosed by the invention has the advantages of simple preparation technique, stable properties, high drug loading rate and high in-vivo absorption speed, and can easily implement industrial production.
Description
Technical field: [0001] The invention relates to the technical field of medicine, and relates to a cucurbitacin E nanosuspension composition and a preparation thereof. Specifically, a surfactant and a cucurbitacin E are used to form a cucurbitacin E nanosuspension composition and a preparation thereof. Background technique: [0002] The molecular formula of cucurbitacin E is C 32 h 44 o 8 , with a molecular weight of 556.69, has various biological activities such as anti-tumor, liver protection, and improving body immunity, and can also promote the uptake of drug-resistant tumor cells to doxorubicin. Or used alone, and can significantly reduce the cardiotoxicity of doxorubicin. [0003] Cucurbitacin E is a water-insoluble drug, and its solubility in oil is also low. By preparing it into a nanosuspension, its dissolution rate and degree can be improved, thereby increasing its absorption in the body and ensuring the curative effect of cucurbitacin E. [0004] Nanosuspensio...
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