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Formulation and method for increasing oral bioavailability of drugs

a technology of oral bioavailability and drug bioavailability, which is applied in the direction of biocide, plant/algae/fungi/lichens ingredients, biochemicals, etc., can solve the problems of poor oral bioavailability, many drugs are prone to poor oral bioavailability, so as to improve oral bioavailability, improve oral bioavailability, and improve oral bioavailability

Inactive Publication Date: 2014-11-27
YISSUM RES DEV CO OF THE HEBREWUNIVERSITY OF JERUSALEM LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The invention is about improving the way drugs are absorbed in the body. It is designed to use small particles made of fat to enhance the bioavailability of drugs that have low absorption rates. This technology helps to make drugs more effective and reduces the amount of drug needed. By combining the use of these particles with other chemicals, the invention makes drugs more stable and consistent in their absorption. This results in improved medication for patients.

Problems solved by technology

However, these methods have not been successful in circumventing liver biotransformation and biliary secretion of drugs.
Despite the great advancements in the area of various drug delivery systems such as nano-lipospheres, many drugs are prone to poor oral bioavailability due to biological barriers at the enterocyte level, termed “intestinal first pass metabolism”.
In addition, the poor oral bioavailability is attributed to efflux transporters e.g. permeability-glycoprotein (P-gp) at the enterocyte luminal membrane [3].
P-gp can efflux out a variety of drugs from cells which ultimately lead to unsuccessful drug therapy.
While there are several methods to inhibit metabolic and efflux processes by pharmacological agents, there are limited pharmaceutical solutions to overcome this problem.
Much more difficult is the case of Phase II metabolism, where there are currently no effective technologies that control this biological process in the clinical setting.

Method used

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  • Formulation and method for increasing oral bioavailability of drugs
  • Formulation and method for increasing oral bioavailability of drugs
  • Formulation and method for increasing oral bioavailability of drugs

Examples

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Embodiment Construction

[0162]The present invention is thus based on the realization that it is possible to increase the oral bioavailability of a drug, such as a drug containing a lipophilic compound, by administering the drug in a composition comprising pro-nano lipospheres incorporating piperine.

[0163]The following specific examples illustrate various aspects of the present invention, and are not intended to be limiting in any way. For all examples, all the ingredients were dissolved in the solvent using magnetic stirrer, and heated gently (˜40-45° C.) for 15-45 minutes until the ingredients were completely dissolved. To obtain particles, the concentrate formulation was diluted in at least 10 volumes of water in aqueous solution.

[0164]For all experiments described below, the particle size of the diluted formulation was measured with VLA particle size analyzer (Coulter N4 MD Submicron Particle Size Analyzer), suitable for submicron particle size determination. About 75 μl of the concentrate formulation w...

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Abstract

The application discloses a formulation and method for increasing bioavailability of an orally administered drug.

Description

FIELD OF THE INVENTION[0001]The present invention pertains to a formulation and method for increasing the oral bioavailability of drugs by utilizing advanced pro-nano lipospheres (PNL) and PNL incorporating piperine.BACKGROUND OF THE INVENTION[0002]Many dispersion systems are currently in use as, or being explored for use as carriers of substances, particularly biologically active compounds. These systems are designed to protect the substance from the environment during delivery and to provide a controlled release of the substance to a targeted area. In some cases, the goal is to target specific sites in the body using the dispersion. In other cases, the goal is to prepare a drug carrier system that acts as a reservoir at the site of injection. Dispersion systems used for pharmaceutical and cosmetic formulations can be categorized as either suspensions or particles ranging in size from a few nanometers up to hundreds of microns, dispersed in an aqueous or non-aqueous medium using su...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/436A61K31/05A61K9/10A61K47/22A61K47/24A61K47/14A61K31/343A61K31/17
CPCA61K9/5123A61K31/343A61K31/436A61K31/05A61K9/10A61K47/22A61K47/24A61K47/14A61K31/17A61K9/127A61K9/0019A61K38/00A61K45/06A61K31/352A61K31/366A61K31/7048A61K36/67A61K2300/00
Inventor HOFFMAN, AMNONDOMB, ABRAHAM J.ELGART, ANNACHERNIAKOV, IRINA
Owner YISSUM RES DEV CO OF THE HEBREWUNIVERSITY OF JERUSALEM LTD
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