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Oridonin cubic liquid crystal nanoparticle and preparation method thereof

A technology of oridonin A and nanoparticles is applied in the directions of pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. Achieving the problems of therapeutic concentration and low bioavailability, and achieving the effect of improving oral relative bioavailability, good application prospects and high bioavailability

Active Publication Date: 2017-05-31
GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After oral administration, the blood drug concentration in the body is low, and the concentration of oridonin around the tumor cells is even lower, it is difficult to reach a clinically effective therapeutic concentration, which seriously affects the anticancer effect of oridonin
Currently on the market, organic solvents and surface-active substances are mainly used to increase the solubility of oridonin, and intravenous infusion can easily cause adverse reactions such as vasculitis and pain, while oral preparations only have crude oridonin extract tablets. Low content, low bioavailability

Method used

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  • Oridonin cubic liquid crystal nanoparticle and preparation method thereof
  • Oridonin cubic liquid crystal nanoparticle and preparation method thereof
  • Oridonin cubic liquid crystal nanoparticle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1 Preparation of Rubescensin A Cubic Liquid Crystal Nanoparticles and Investigation of Different Liquid Crystal Systems

[0054] The preparation method of the Rubescensin A cubic liquid crystal nanoparticles of the present embodiment comprises the following steps:

[0055] 20mg Rubescensin A was dissolved in propylene glycol to obtain a drug solution; according to each prescription in Table 1 (all by mass percentage), take glycerol monooleate or phytantriol and stabilizer F127 (poloxamer 407) in a 50mL plastic centrifuge tube, melted in a water bath at 60°C, then slowly added it to the above drug solution, vortexed and mixed thoroughly for 5 minutes, then added the prescribed amount of ultrapure water, vortexed for 5 minutes, and the obtained system was cooled at room temperature After equilibrating in the dark for 48 hours, a transparent oridonin cubic liquid crystal gel was obtained. Under the condition of ice bath, the obtained oridonin A cubic liquid crysta...

Embodiment 2

[0061] Example 2 Effects of different mass ratios of F127 and lipids in oridonin A cubic liquid crystal nanoparticles on liquid crystal phase state and drug release behavior

[0062] Only after the oridonin liquid crystal is further prepared into a nanoparticle solution can it be taken orally, and it can pass through the cells of the gastrointestinal tract and be absorbed by the human body; The particles are easy to aggregate and precipitate, adding a stabilizer can support and maintain the network structure of the liquid crystal lattice unit, prevent the aggregation and precipitation of the nanoparticles during the high-pressure homogenization process, and maintain the stability of the liquid crystal nanoparticles during the preparation and storage process.

[0063] (1) The present embodiment investigates the oridonin cubic liquid crystal nanoparticle samples of F127 and lipid (GMO or PYT) with different mass ratios (0%, 9%, 12%, 15%, 20%), Its preparation method is the same ...

Embodiment 3

[0071] Example 3: Effect of drug loading in cubic liquid crystal nanoparticles of oridonin on particle size of cubic liquid crystal nanoparticles and drug encapsulation efficiency

[0072] Drugs with different structures and different contents will affect the internal structure of cubic liquid crystal nanoparticles. Therefore, this embodiment prepares cubic liquid crystal nanoparticles of oridonin A with different drug loadings (raw material prescriptions are shown in Table 2), and the preparation method is as follows: Shown in embodiment 1.

[0073] Table 2 Raw Material Prescription of Oridonin A Cubic Liquid Crystal Nanoparticles

[0074]

[0075]

[0076] The small-angle X-ray scattering patterns (test parameters are the same as those in Example 2), particle size distribution, and encapsulation efficiency of Rubescensin A cubic liquid crystal nanoparticles with different drug loadings in this example were measured.

[0077] The particle size of oridonin cubic liquid cr...

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Abstract

The invention relates to an oridonin cubic liquid crystal nanoparticle and a preparation method thereof. The oridonin cubic liquid crystal nanoparticle is prepared from the following raw materials in percentage by weight: 0.1 to 0.5 percent of oridonin, 7 to 64 percent of amphiphilic lipid material, 6 to 29 percent of solvent, 1 to 8 percent of stabilizer, and 25 to 65 percent of water, wherein the amphiphilic lipid material is glycerol mono-oleate or phytould likeriol; the mass ratio of a liquid crystal material to the stabilizer is 1 to (0.01 to 0.30). The oridonin cubic liquid crystal nanoparticle provided by the invention is smaller in particle size, good in uniformity, and beneficial to endocytosis and transfer of enterocyte; by utilizing a unique structure of cubic liquid crystal, a dissolution barrier and a permeation barrier of the oridonin during an oral absorption process are effectively overcome, the oral relative bioavailability of the oridonin is remarkably improved, and meanwhile, the oridonin can be slowly released.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a cubic liquid crystal nanoparticle of oridonin A and a preparation method thereof. Background technique [0002] Oridonin A is a natural organic compound of kaurene diterpenoids isolated from the Lamiaceae plant Oridonium, which has strong anti-tumor effects on various tumor cells. Clinically, it is mainly used as a new anti-cancer drug or anti-cancer auxiliary drug for the treatment of digestive system cancers such as liver cancer, esophageal cancer, and pancreatic cancer. [0003] Oridonin is a 7,20-epoxy-enantio-kaurane diterpene compound, soluble in methanol, ethanol, propylene glycol, ethyl acetate, acetone and other organic solvents, insoluble in water, and classified as biopharmaceutical For class IV drugs in the system, there are dissolution barriers and permeation barriers during oral administration. After oral administration, the blood drug concentration in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/34A61K31/352A61P35/00
CPCA61K9/0053A61K9/145A61K9/146A61K31/352
Inventor 吴传斌梅丽玲潘昕黄莹陈锦填史旋景卉
Owner GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK
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