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Pharmaceutical composition for enhancing intestinal absorption of danshensu, preparation and preparation method thereof

A technology for intestinal absorption and danshensu, applied in the field of medicine, can solve the problems of poor gastrointestinal membrane permeability of danshensu, reduced oral bioavailability of danshensu, low oral bioavailability of danshensu, etc. Absorb, improve bioavailability, improve bioavailability effect

Inactive Publication Date: 2019-04-02
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some studies have found that regardless of the administration of various preparations made of compound Danshen recipes or a single component of Danshensu, Danshensu has poor oral absorption, slow elimination, and low oral bioavailability. Related studies have shown that Danshensu with low oral bioavailability There are two possible reasons: one is that the gastrointestinal membrane of Danshensu has poor permeability and absorption is difficult; the other is that the transport of Danshensu is mainly active transport mediated by P-gp transporter, and the efflux of P-gp may be Will reduce the oral bioavailability of Danshensu in rats

Method used

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  • Pharmaceutical composition for enhancing intestinal absorption of danshensu, preparation and preparation method thereof
  • Pharmaceutical composition for enhancing intestinal absorption of danshensu, preparation and preparation method thereof
  • Pharmaceutical composition for enhancing intestinal absorption of danshensu, preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 Selection of Danshensu Absorption Intestinal Segment in Eversioned Intestinal Sac Experiment

[0037] 1. Test material

[0038] SPF-grade male SD rats, 180-200 g, were provided by the Animal Center of Guangzhou University of Traditional Chinese Medicine; Danshensu was purchased from Nanjing Zelang Pharmaceutical Technology Co., Ltd.

[0039] 2. Test method

[0040] Take 6 of the above-mentioned rats, fasting without water for 12 hours before the experiment, anesthetize with 0.3mL / 100g intraperitoneal injection of 10% chloral hydrate, fix the rats after anesthesia, open the abdominal cavity about 3cm along the abdominal midline, and quickly cut off the twelve fingers Intestine (starting at 1 cm from the pylorus), jejunum (starting at about 15 cm from the pylorus) and ileum (starting at 10 cm from the small end of the cecum) were each placed in K-R solution (ice bath) for 10 cm, and the rat intestinal mesentery was carefully peeled off. Drain the content and w...

Embodiment 2

[0050] Example 2 Effect of menthol on intestinal absorption of danshensu in eversion intestinal sac test

[0051] 1. Test material

[0052] The test animals were the same as in Example 1, and menthol was purchased from Aladdin.

[0053] 2. Test method

[0054] Take 36 rats and divide them into 6 groups randomly, 6 rats in each group. Each group is given the following concentrations of Danshensu: 10, 20, 40, 80, 150, 200 mg / mL, with the jejunum section as the test site, according to the implementation The method described in Example 1 was tested, samples were taken for HPLC content determination, cumulative absorption capacity and absorption rate were calculated, intestinal length and internal diameter were measured, drug intestinal absorption rate constant was calculated, and the optimal absorption concentration of danshensu was screened out. After determining the optimal administration concentration of Danshensu in the eversion intestinal sac experiment, another 30 rats wer...

Embodiment 3

[0065] Example 3 Caco-2 cells detect the effect of menthol on the intestinal absorption of danshensu

[0066] 1. Test material

[0067] Caco-2 cell line was purchased from ATCC, Manassas, VA.

[0068] 2. Test method

[0069] Rinse the Transwell plate growing Caco-2 with PBS, then rinse with pre-warmed HBSS, pH 7.4, then add pre-warmed HBSS, at 37°C, 5% CO 2 Incubate under the condition for 20min, suck off the HBSS, repeat 2 times.

[0070] For the transfer from the cell villi surface (AP side) to the base surface (BL side): add 1ml of Danshensu solution to the AP side as the drug supply pool, and add 2ml of blank pH7.4 HBSS to the BL side as the drug receiving pool; for the BL side Transfer to the AP side: Add 2ml of Danshensu solution to the BL side as a drug supply pool, and add 0.5ml of blank pH7.4HBSS to the AP side as a drug receiving pool. Place the Transwell culture plate in a 37°C air bath constant temperature shaker with a rotation speed of 60r / min, and absorb the...

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Abstract

The invention relates to a pharmaceutical composition capable of enhancing intestinal absorption of tanshinol as well as a preparation and a preparation method of the pharmaceutical composition. The pharmaceutical composition takes the tanshinol and menthol as active ingredients; rat everted gut sacs model and Caco-2 cell test results indicate that through the combined application of the tanshinol and the menthol, the intestinal absorption rate of the tanshinol can be significantly improved, and the bioavailability of the tanshinol can be improved. Preferably, the pharmaceutical composition is applied in the form of a micro-capsule, wherein the micro-capsule is composed of a capsule core and a capsule material; the capsule core consists of the tanshinol and the menthol; and the capsule material consists of chitosan and xanthan gum. The average drug loading capacity of the micro-capsule reaches 60% or above and the encapsulation efficiency of the micro-capsule reaches 90% or above; and the micro-capsule is good in dispersity and liquidity, relatively narrow in particle size distribution and is dense and smooth in surface, and the micro-capsule is represented as a relatively regular spherical form. Based upon a dissolution rate test, the micro-capsule is good in sustained-release effect; and by prolonging a drug release time, the intestinal absorption of the tanshinol is further enhanced and the bioavailability of the tanshinol is improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pharmaceutical composition for enhancing intestinal absorption of danshensu, its preparation and a preparation method. Background technique [0002] The main route of administration of traditional Chinese medicine is oral administration. In oral administration, the absorption of drugs is affected by many factors, such as drug solubility, dissolution rate, mucosal permeability, first-pass effect and so on. There are two main ways to improve its oral bioavailability, one is to carry out structural modification, and the other is to use intestinal absorption enhancers. The current intestinal absorption enhancers can be mainly divided into bioadhesive polymers, amino acid derivatives, cholates, acylcarnitines and surfactants. [0003] Danshensu, also known as salvianic acid A, is one of the water-soluble phenolic acids of Danshen, which has the functions of reducing my...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/10A61K31/192A61K9/50A61P9/10A61P9/00A61P29/00A61P7/02
CPCA61K9/5036A61K31/192A61K47/10
Inventor 王晖刘文彬薛漫清恽昊王爱娟
Owner GUANGDONG PHARMA UNIV