Cucurbitacin oral lipid nano emulsion and preparation method

A technology of lipid nanometer and cucurbitacin, which is applied in the directions of pharmaceutical formulations, emulsion delivery, medical preparations of inactive ingredients, etc.

Inactive Publication Date: 2013-06-26
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Aiming at the defects of low dissolution rate and large fluctuation of cucurbitacin B tablets, low oral bioavailability, and the consequent nausea, loss of appetite and side effects of diarrhea

Method used

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  • Cucurbitacin oral lipid nano emulsion and preparation method
  • Cucurbitacin oral lipid nano emulsion and preparation method
  • Cucurbitacin oral lipid nano emulsion and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Example 1 Preparation of Cucurbitacin B Oral Lipid Nanoemulsion

[0076] Prescription:

[0077] Cucurbitacin B 3mg

[0078] MCT 1.66 g

[0079] RH40 0.37 g

[0080] SPC 0.15g

[0081] VE 0.30 g

[0082] Glycerin 0.30 g

[0083] Appropriate amount of purified water

[0084] Preparation:

[0085] Weigh the prescribed amount of cucurbitacin B (the purity determined by HPLC area normalization method is greater than 99%), MCT, SPC, RH40 and VE to form the oil phase; weigh the prescribed amount of glycerin dissolved in purified water as the water phase, two-phase Heat to 50~55°C respectively. After the substances in the oil phase were completely dissolved, under the condition of magnetic stirring, the water phase was slowly added to the oil phase, and the stirring was continued for 10 min to obtain colostrum, which was homogenized 6 times with a microfluidizer at 14000 psi, and diluted with pure water to Pass 30 mL through a 0.22 μm microporous membrane to obtain ...

Embodiment 2

[0092] Example 2 Cucurbitacin D Oral Lipid Nanoemulsion

[0093] Prescription:

[0094] Cucurbitacin D 3mg

[0095] MCT 1.66 g

[0096] RH40 0.37g

[0097] SPC 0.15g

[0098] VE 0.30g

[0099] Glycerin 0.30 g

[0100] Appropriate amount of purified water

[0101] Preparation:

[0102] Weigh the prescribed amount of cucurbitacin D (the purity determined by HPLC area normalization method is greater than 98%), MCT, SPC, RH40 and VE to form the oil phase; weigh the prescribed amount of glycerin dissolved in purified water as the water phase, two-phase Heat to 50~55°C respectively. After the substances in the oil phase were completely dissolved, under the condition of magnetic stirring, the water phase was slowly added to the oil phase, and the stirring was continued for 15 min to obtain colostrum, which was homogenized 5 times with a microfluidizer at 15000 psi, and diluted with pure water to Pass 30 mL through a 0.22 μm microporous membrane to obtain the final milk; d...

Embodiment 3

[0108] Example 3 Cucurbitacin E Oral Lipid Nanoemulsion

[0109] Prescription:

[0110] Cucurbitacin E 3mg

[0111] MCT 1.66 g

[0112] RH40 0.37g

[0113] SPC 0.15 g

[0114] VE 0.30 g

[0115]Glycerin 0.30 g

[0116] Appropriate amount of purified water

[0117] Preparation:

[0118] Weigh the prescribed amount of cucurbitacin E (the purity determined by HPLC area normalization method is greater than 99%), MCT, SPC, RH40 and VE to form the oil phase; weigh the prescribed amount of glycerin dissolved in purified water as the water phase, two-phase Heat to 50~55°C respectively. After the substances in the oil phase were completely dissolved, under the condition of magnetic stirring, the water phase was slowly added to the oil phase, and the stirring was continued for 12 minutes to obtain colostrum, which was homogenized 4 times with a microfluidizer at 15000 psi, and diluted with pure water to Pass 30 mL through a 0.22 μm microporous membrane to obtain the final mi...

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Abstract

The invention discloses a prescription for preparing a cucurbitacin oral lipid nano emulsion and a preparation method. The cucurbitacin oral lipid nano emulsion contains cucurbitacin, medium chain triglyceride, soya lecithin, polyoxyethylene 40 hydrogenated castor oil, an antifreezing agent, vitamin E and water. The prepared cucurbitacin oral lipid nano emulsion has good antifreezing capability, Compared with the tablet in the market, the disintegration of the tablet in the gastrointestinal tract is not existed, the dissolution of the medicine is fast, the cucurbitacin oral lipid nano emulsion is widely and uniformly distributed in a easy mode, the acting time is fast, and the bioavailability of the cucurbitacin oral lipid nano emulsion is obviously enhanced. The preparation technology is simple, and can be used for industrial production.

Description

technical field : [0001] The invention belongs to the field of pharmaceutical preparations and discloses a prescription process for preparing cucurbitacin oral lipid nanoemulsion. Background technique : [0002] Cucurbitacins are a class of highly oxidized tetracyclic triterpenoids extracted from plants, and more than 40 kinds have been discovered so far. In ancient my country, the traditional Chinese medicine melon stalk was used to treat jaundice, and it can induce vomiting and eliminate phlegm. It can be used to treat severe water evil, edema of limbs, cough and asthma, and those who accidentally ingest poisons that have not yet been absorbed in the gastric cavity. This shows that cucurbitacins have a long history of curing diseases and saving lives in our country. Most of these components exist in Cucurbitaceae plants, and some of them exist in other plants. With the development of spectroscopic technology, the structure of cucurbitacins has been comprehensively under...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/575A61K47/44A61K47/10A61P1/16A61P35/00
Inventor 邓意辉程晓波佘振南
Owner SHENYANG PHARMA UNIVERSITY
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