A kind of pharmaceutical composition and its preparation method and application

A technology for medicines and uses, applied in the field of pharmaceutical compositions, can solve the problems of affecting bioavailability, increasing the solubility and permeability of puerarin, and increasing the absorption of puerarin, so as to increase oral bioavailability and increase intestinal permeability. , the effect of increasing the solubility

Active Publication Date: 2020-09-04
SOUTHERN MEDICAL UNIVERSITY
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Problems solved by technology

[0005] However, these methods for increasing the absorption of puerarin are mostly realized by improving the solubility and permeability of puerarin by using pharmaceutical theory. Poor bioavailability and poor biological permeability. Studies have shown that there are biological reasons for the low bioavailability of puerarin, that is, puerarin is the substrate of the intestinal efflux transport protein P-gp (Cui Shengmiao et al. Rat intestinal eversion model to Research on the absorption mechanism of puerarin[J]. Shizhen Guoyue Guoyao, 2008,19(7):1715-16), puerarin absorbed into enterocytes can be effluxed out of the cells by intestinal efflux transporter P-gp , leading to a decrease in the amount of puerarin entering the systemic circulation, thereby affecting its bioavailability
Therefore, simply relying on pharmaceutical methods to increase the solubility and permeability of puerarin cannot maximize the absorption of puerarin

Method used

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  • A kind of pharmaceutical composition and its preparation method and application
  • A kind of pharmaceutical composition and its preparation method and application
  • A kind of pharmaceutical composition and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1 increases the solubility of puerarin with Ligustrazine

[0026] Puerarin solutions of different concentrations (1600, 800, 400, 320, 200, 160, 80, 40, 20, 10, 5 μM) were prepared in HBSS (Hank’s Balanced Salt Solution) medium, and 100 μl of internal standard testosterone solution (100 μM) was added , vortex, and centrifuge. At the same time, prepare the above-mentioned mixed solution of Ligustrazine and Puerarin with concentration gradient in HBSS, the concentration ratio of Ligustrazine and Puerarin is 1:1, add 100 μl internal standard testosterone solution (100 μM), vortex, and centrifuge. The samples were analyzed by ultra-high performance liquid chromatography. The solubility curve was drawn with the theoretical concentration of puerarin as the abscissa and the peak area ratio of puerarin and testosterone as the ordinate. see results figure 1 , the results showed that when the concentration of puerarin in HBSS was low, puerarin dissolved linearly wit...

Embodiment 2

[0027] Example 2 Ligustrazine and Puerarin Medicinal Combination Improve Puerarin Penetration

[0028] The apparent permeability coefficient (Peff) of different concentrations (20μM, 40μM, 160μM) of puerarin in four intestinal segments of rat duodenum, jejunum, ileum and colon was investigated by rat in vivo intestinal perfusion model. The formula for calculating the apparent permeability coefficient is as follows: where Co and Cm are the inlet and outlet concentrations, respectively; Gz=πDL / 2Q, where Q is the perfusion velocity, L is the length of the intestinal segment, and D is the diffusion coefficient.

[0029]The results of the study showed that under the investigated concentration conditions (Co=40μM), the effective permeability coefficient of puerarin in the duodenum, jejunum, ileum, and colon were 0.21±0.05, 0.26±0.09, and 0.21±0.07, respectively. , 0.20±0.09. When ligustrazine and puerarin were used together, the effective permeability coefficients of puerarin in ...

Embodiment 3

[0031] Example 3 The medicinal combination of ligustrazine and puerarin reduces the effect of intestinal transport proteins on the efflux of puerarin. The effect of different concentrations of puerarin on the duodenum, jejunum, ileum, and colon of rats was investigated using a rat in vivo intestinal perfusion model. Percent absorption of four intestinal segments. The results of the study showed that under the investigated concentration conditions, the percentage absorption rate of puerarin in the four intestinal segments of duodenum, jejunum, ileum and colon were 5.47±1.87, 6.15±2.03, 5.11±1.61, 4.20±1.83 . In addition, the absorption of puerarin when puerarin was combined with verapamil (P-gp specific inhibitor) and when puerarin was combined with ligustrazine was investigated. The results showed that when verapamil was combined with puerarin, At the same concentration, the percent absorption rate of puerarin in the duodenum, jejunum, ileum and colon were 12.57±3.77, 14.41±3...

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Abstract

The invention relates to a pharmaceutical composition, and a preparation method and application thereof. The pharmaceutical composition disclosed in the invention contains puerarin and Ligusticum wallichii extract used as active components; preferably, the pharmaceutical composition does not contain other active components. The Ligusticum wallichii extract in the pharmaceutical composition can improve the dissolving capability of puerarin, enhance the intestinal permeability of puerarin, reduce the influence of intestinal efflux transport protein P-gp on efflux of puerarin, improve the oral absorption of puerarin from a plurality of links and enhance the oral bioavailability of puerarin, so synergistic effect is exerted on treatment of cardiovascular and cerebrovascular diseases.

Description

technical field [0001] The invention relates to a pharmaceutical composition, in particular to a pharmaceutical composition comprising chuanxiong extract and puerarin. Background technique [0002] Cardiovascular and cerebrovascular diseases generally refer to heart and brain ischemic or hemorrhagic diseases caused by hyperlipidemia, hypertension, atherosclerosis, etc. With the change of people's diet structure, at present, cardiovascular and cerebrovascular diseases have become the number one killer threatening the lives of Chinese residents. The disease has a high mortality rate, which brings great pain and heavy burden to patients, families and society. Since the occurrence and development of cardiovascular and cerebrovascular diseases is a gradual process, early prevention and early treatment become an effective way to reduce the harm of cardiovascular and cerebrovascular diseases. [0003] Traditional Chinese medicine is a treasure of the Chinese nation. Many traditi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61K36/488A61K36/236A61K31/4965A61P9/00A61P9/10
CPCA61K31/352A61K31/4965A61K36/236A61K36/488A61K2300/00
Inventor 赵洁吴芃蔡铮陈润芝杨娜
Owner SOUTHERN MEDICAL UNIVERSITY
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