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Tripterine nanosuspension and preparation method thereof

A technology of nano-suspension and tripterine, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the limitations of drug delivery methods, low bioavailability, and toxicity. Problems such as large side effects, to achieve the effects of economical, safe and easy-to-obtain excipients, high tumor cell inhibition rate, and simple prescription

Active Publication Date: 2017-01-11
INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] CSL is poorly soluble in water, which greatly limits the way of drug delivery in in vivo studies
Existing in vivo studies mostly use suspension gavage or intraperitoneal administration, but it is difficult to maximize the curative effect due to low bioavailability
Moreover, CSL has relatively large toxic and side effects, and has certain toxicity to reproductive, endocrine and digestive systems.

Method used

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  • Tripterine nanosuspension and preparation method thereof
  • Tripterine nanosuspension and preparation method thereof
  • Tripterine nanosuspension and preparation method thereof

Examples

Experimental program
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Embodiment 1

[0031] Dissolve 5mg tripterine (CSL) and 5mg PEG2000-PCL2000 in 0.2mL methanol, slowly instill in 5mL deionized water at room temperature at 250HZ, continue to sonicate for 3min, remove methanol by rotary evaporation, and obtain CSL nanosuspension agent. The average particle size is 67.1nm ( figure 1 ), the polydispersity index (PDI) was 0.232, and the potential value was -10.4mV.

Embodiment 2

[0033] Dissolve 5mg of tripterine (CSL) and 5mg of PEG2000-PCL1140 in 0.2mL of methanol, slowly instill in 5mL of deionized water with 250HZ ultrasound at room temperature, continue to sonicate for 3min, remove methanol by rotary evaporation, and obtain CSL nanosuspension agent. The average particle diameter is 74.2nm, the polydispersity index (PDI) is 0.201, and the potential value is -12.6mV.

Embodiment 3

[0035] Dissolve 5mg tripterine (CSL) and 5mg PEG5000-PCL2000 in 0.2mL methanol, slowly instill in 5mL deionized water with 250HZ ultrasound at room temperature, continue to sonicate for 3min, remove methanol by rotary evaporation, and obtain CSL nanosuspension agent. The average particle size is 76.4nm, the polydispersity index (PDI) is 0.192, and the potential value is -13.8mV.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a preparation method of tripterine nanosuspension and application thereof, which are used for preparation of amphipathic stabilizers including mPEG-PCL, mPEG-DSPE, Bianze78, SPC, Tween80, BSA, TPGS and the like. The tripterine nanosuspension is prepared by adopting a solvent precipitation-ultrasonic injection method, and the formulation composition is as follows: the combination ratio of tripterine to the stabilizer is 1:(0.1-1) (weight ratio); the maximal drug loading capacity can reach 85%, the minimum grain size can reach 67.1nm, the polydispersity is good; the nanosuspension is steady in both gastrointestinal fluid and plasma, can be used by oral administration and intravenous injection; the nanosuspension has a good sustained-release effect in vitro, and burst release cannot happen; the nanosuspension is remarkable in tumor cell inhibition ratio in vitro in comparison with a raw medicine liquor; and in vivo pharmacological experiment also shows excellent anti-tumor efficacy, thus having wide application and development prospect.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a tripteryglide nanosuspension prepared with amphiphilic stabilizers such as mPEG-PCL, mPEG-DSPE, Benzaze 78, SPC, Tween80, BSA, TPGS, and the like. Preparation method and application. Background technique [0002] Celastrol (CSL for short) is derived from the roots, leaves and flowers of Euonymus plant Tripterygium wilfordii. It is a triterpene monomer component of Tripterygium wilfordii. Studies have found that CSL has a significant effect on a variety of immune system diseases. In recent years Studies have found that its anti-tumor effect is also relatively significant. It has been found that its anti-tumor effect on rat adrenal medulla pheochromoma differentiation cell line PC12, rat glioma C6 cell line, nasopharyngeal carcinoma cell line CNE-1, SHG-44 Glioma cell lines, cervical cancer HeLa cells, human prostate cancer cell PC-3, leukemia cells U937, human lung ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/56A61K9/19A61K47/34A61K47/24A61K47/26A61K47/22A61P35/00A61P35/02
Inventor 王向涛张明珠韩美华郭一飞
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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