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Complex nano particle of ginsenoside Rh2 albumin and preparation method thereof

A technology of ginsenosides and human serum albumin, which is applied in the directions of pharmaceutical formulations, drug combinations, and medical preparations with inactive ingredients, etc., can solve the problems of low bioavailability, large particles, and insolubility in water.

Inactive Publication Date: 2014-05-07
WUXI MATERNAL & CHILD HEALTH HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

A large number of basic and clinical studies have shown that drugs containing ginsenosides have broad application prospects in the treatment of tumors, but there are still many problems in traditional preparations, such as large particles, insoluble in water, and low bioavailability, which limit their use. Clinical application

Method used

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  • Complex nano particle of ginsenoside Rh2 albumin and preparation method thereof
  • Complex nano particle of ginsenoside Rh2 albumin and preparation method thereof
  • Complex nano particle of ginsenoside Rh2 albumin and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0020] The albumin composite nanoparticles of ginsenoside Rh2 involved in the present invention are prepared through the following steps:

[0021] Preparation of albumin composite nanoparticles of ginsenoside Rh2: Dissolve ginsenoside Rh2 in a small amount of absolute ethanol, weigh 250 mg of albumin and dissolve it in 25 ml deionized water, add ginsenoside Rh2 after complete dissolution, and place on a magnetic stirrer Mix well, adjust the pH to be slightly alkaline (pH9.0), slowly (drop by drop about 1ml / 1min) add an appropriate amount of absolute ethanol, stir for half an hour until the solution becomes turbid, then slowly add about 50ul of glutaraldehyde solution, Continue to stir and solidify for 12 hours, centrifuge the reaction solution in a centrifuge tube (21000rpm) for half an hour, wash with water three times, filter through 220um, vacuum dry and store at 4°C for later use.

[0022] The optimal conditions were explored through various conditions such as the ratio of...

Embodiment 2

[0031] Example 2: The effect of absolute ethanol amount and the ratio pH of the aqueous phase on the stability of albumin composite nanoparticles of ginsenoside Rh2

[0032] Weigh 250mg of albumin and dissolve it in 25ml of deionized water, add ginsenoside Rh2 after completely dissolving, mix well on a magnetic stirrer, slowly (drop by drop about 1ml / 1min) add about 150ml of absolute ethanol to prepare ginsenoside Rh2 white Compared with the nanoparticles added with 100ml and 200ml of absolute ethanol, the protein composite nanoparticles have a more uniform particle size and a moderate size, which is suitable for relevant animal experiments and clinical use, and has a higher encapsulation efficiency and drug loading capacity.

Embodiment 3

[0033] Example 3: Effect of buffer pH on the stability of albumin composite nanoparticles of ginsenoside Rh2

[0034] Using pH 9.0 deionized aqueous solution to reconstitute this product, in terms of encapsulation efficiency and particle size, there is no significant difference between pH 7.0 and 5.0. However, after several months of storage at 4°C, the drug release rate was significantly different from that at pH 7.0 and 5.0. The product reconstituted at pH 5.0 is easy to settle and is not suitable for long-term storage.

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Abstract

The invention discloses a complex nano particle of ginsenoside Rh2 albumin and a preparation method thereof. According to the invention, albumin is adopted to wrap ginsenoside Rh2 to prepare a soluble albumin nano particle drug administration system. The nano particle is good in dispersion, and has a sustained release effect, so that more drugs can be accumulated near a tumor tissue, the anti-tumor effect is improved, the toxic and side effects of the drugs on normal tissues can be reduced, and the tolerance of a patient is improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and specifically relates to an albumin composite nanoparticle of an antitumor drug ginsenoside Rh2 and a preparation method thereof. Background technique [0002] Ginsenoside Rh2 belongs to the secondary aglycon of ginseng, with extremely low content and strong anti-tumor activity. Now it is mostly obtained by degradation and transformation of ginsenosides with high content. Many studies have shown that ginsenoside Rh2 can slow down the proliferation rate of tumor cells or induce cell death by interfering with the cell cycle of tumor cells. A large number of basic and clinical studies have shown that drugs containing ginsenosides have broad application prospects in the treatment of tumors, but there are still many problems in traditional preparations, such as large particles, insoluble in water, and low bioavailability, which limit their use. Clinical application. It will ha...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/704A61K47/48A61K9/08A61K9/20A61K9/16A61K9/48A61K9/06A61K9/107A61P35/00
Inventor 陈道桢唐秋莎陈钰杨蕊李向东陈万瑛田新梅
Owner WUXI MATERNAL & CHILD HEALTH HOSPITAL
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