Andrographolide nano suspension and preparation method thereof

A technology of andrographolide and nanosuspension, applied in the field of medicine, can solve the problems of limited clinical application, low stability, low encapsulation rate, etc., achieve high penetration through cell membrane, increase dissolution rate, and reduce efflux. effect of function

Inactive Publication Date: 2017-02-08
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the bioavailability of andrographolide has been improved to a certain extent, its low drug loading, low encapsulation efficiency and low stability limit its clinical application

Method used

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  • Andrographolide nano suspension and preparation method thereof
  • Andrographolide nano suspension and preparation method thereof
  • Andrographolide nano suspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Box-Behnken central combination design test optimization of andrographolide nanosuspension preparation process

[0028] Main experimental materials:

[0029]

[0030]

[0031] On the basis of single factor, choose 4 factors that have significant influence on the preparation process of andrographolide nanosuspension, namely stabilizer concentration (A), TPGS and SDS ratio (B), media grinder speed (C) and grinding time (D) is the independent variable, with the particle size and polydispersity coefficient as the dependent variable (response value), the Box-Behnken central combination design is carried out, and the mathematical model is established to optimize the preparation process.

[0032] In this experiment, the particle size and polydispersity coefficient (PI) of andrographolide nanosuspension were used as evaluation indicators, stabilizer concentration (A), TPGS and SDS ratio (B), media grinder speed (C) and grinding time ( D) Investigate the factors, use the Bo...

Embodiment 2

[0041] Example 2: Weigh 1g of andrographolide, add 200mL of water (containing 0.600g TPGS, 0.620g SDS), homogenizer 16000rpm high-speed shear for 5min, and then pour the above suspension into a media grinder (0.3- 0.4mm zirconia beads (850g) were milled at 1056 rpm for 68 minutes to prepare andrographolide nano-suspension. Add 1% (W / V) mannitol and put them into vials of 5 mL each. Pre-frozen at -80℃ for 12h, and then placed in a freeze dryer, -30℃ for 10h, -10℃ for 5h, 0℃ for 2h, 25℃ for 2h to prepare andrographolide nanosuspension jelly Dry powder.

Embodiment 3

[0042] Example 3: Preparation of andrographolide nanosuspension (without TPGS): Weigh 1 g of andrographolide, add 200 mL of water (without adding TPGS, only containing 0.620 g SDS), and the rest are prepared according to the process of Example 2 above to obtain Andrographolide nanosuspension freeze-dried powder (without TPGS) (standby).

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Abstract

The invention belongs to the field of pharmaceutical preparations, and provides an andrographolide nano suspension and a preparation method thereof. The andrographolide has low solubility in water, can be easily excreted by P-gp, has high metabolism rate, and thus, has lower dissolution rate and lower in-vivo bioavailability. In order to enhance the dissolution rate and bioavailability of the drug, a P-gp inhibitor TPGS and an ionic stabilizer SDS are selected to prepare the andrographolide nano suspension by using a medium grinding technique; by using the particle size and distribution as evaluating indicators, a Box-Behnken center combined degisn test optimized preparation technique is utilized to prepare the andrographolide nano suspension; and freeze-drying is used for solidifying. After carrying out the characterization, the research in short-term stability, Caco-2 permeability and in-vitro dissolution, and the in-vivo pharmacokinetic and pharmacodynamic research, the results indicate that the andrographolide nano suspension can increase the dissolution rate of andrographolide and enhance the oral-administration bioavailability and anti-inflammatory action.

Description

Technical field [0001] The invention relates to the technical field of medicine, in particular to andrographolide nano suspension and a preparation method. Background technique [0002] Andrographolide (andrographolide) is one of the main effective ingredients extracted from the Acanthaceae plant Andrographis paniculata. It is a diterpene lactone compound and the content in andrographolide leaves is as high as 1.84%. Modern studies have found that andrographolide has a wide range of pharmacological activities, and it has good anti-inflammatory, anti-infective, anti-cancer, and liver-protecting effects. However, it has strong hydrophobicity and low solubility in water (0.07mg / mL) (Chen LL, Wang ZH. Investigation of basic physical and chemical properties of andrographolide[J].Pharm Today,2010,20(1):41-43 .), easy to be excreted by P-gp, fast metabolism, leading to its low dissolution rate and low bioavailability (2.67%) (Ye L, Wang T, TangL et al. Poor oral bioavailability of a pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/365A61K9/19A61K47/22A61P29/00
CPCA61K31/365A61K9/10A61K9/19A61K47/22
Inventor 李俊松蒋爱狄留庆王静娴陈婷芮天奇
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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