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Application of p-glycoprotein inhibitor gelucire44/14 as oral berberine hydrochloride absorption enhancer

A glycoprotein inhibitor, berberine hydrochloride technology, applied in the field of pharmaceutical preparations, to achieve the effects of inhibiting drug transport, improving bioavailability, and increasing drug absorption

Active Publication Date: 2020-01-10
XI AN JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no report that it can be used as a P-glycoprotein inhibitor to improve the bioavailability of poorly absorbed drug BBR

Method used

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  • Application of p-glycoprotein inhibitor gelucire44/14 as oral berberine hydrochloride absorption enhancer
  • Application of p-glycoprotein inhibitor gelucire44/14 as oral berberine hydrochloride absorption enhancer
  • Application of p-glycoprotein inhibitor gelucire44/14 as oral berberine hydrochloride absorption enhancer

Examples

Experimental program
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Embodiment Construction

[0021] The present invention will be described in further detail below in conjunction with the accompanying drawings and embodiments. The examples are illustrative of the invention, not limiting.

[0022] An ideal absorption enhancer should have a strong absorption-promoting effect, less toxic and side effects, no pharmacological activity, no interaction with other drugs in combination, and no interaction with other tissues or organs except the administration site, and will not affect The normal distribution of the drug and other advantages.

[0023] The fatty acid distribution of Gelucire44 / 14 is shown in Table 1. It can be found that it is relatively safe and has no medicinal effect; in addition, Gelucire44 / 14 was published in the European Pharmacopoeia in 1998 as a pharmaceutical excipient, and has been widely used in pharmaceutical preparations in recent years. The application of Gelucire44 / 14 has great potential in the research field of pharmaceutical excipients; moreove...

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PUM

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Abstract

The invention discloses application of P-glycoprotein inhibitor Gelucire44 / 14 serving as an orally-administrated berberine hydrochloride absorption enhancer. Gelucire44 / 14 serves as a P-glycoprotein inhibitor and can inhibit action of a P-glycoprotein teat pipette, so that absorption of berberine hydrochloride difficult to absorb is improved, and the bioavailability of berberine hydrochloride is improved; toxicity inspection results indicate that Gelucire44 / 14 causes no obvious damage to a mucous membrane on the oral administration absorption part, and thus it can be deduced that Gelucire44 / 14 is a safe orally-administrated absorption enhancer; the oral administration bioavailability of berberine hydrochloride difficult to absorb is improved, and Gelucire44 / 14 can be used for preparing an orally-administrated preparation of berberidaceae isoquinoline alkaloid berberine hydrochloride which is difficult to absorb.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, and relates to improving the oral bioavailability of berberine hydrochloride. Background technique [0002] Oral administration is the most commonly used method of administration in drug therapy. It has attracted widespread attention because of its simple administration method, no direct damage to the skin or mucous membrane, good compliance, easy acceptance by patients, and low production cost of drugs. However, this method of administration is easily affected by many factors such as drug solubility, permeability, intestinal P-glycoprotein efflux, and gastrointestinal environment, resulting in low drug bioavailability and affected drug efficacy. [0003] Berberine hydrochloride (BBR) has a long history as a broad-spectrum antibacterial drug in the treatment of intestinal bacterial infectious diseases. In recent years, researchers have found that BBR has a wide range of pharm...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/14A61K31/4375A61P31/04A61P1/00
CPCA61K9/0053A61K31/4375A61K47/14
Inventor 高阳张海龙孙建梅
Owner XI AN JIAOTONG UNIV
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