Enteric-coated proliposomal formulations for poorly water soluble drugs

a technology of oral medicaments and proliposomes, which is applied in the field of entericcoated proliposome formulations for poorly water soluble drugs, can solve the problems of instability, leakage and potential destruction, and reduced therapeutic efficacy of many drugs, and achieves the effects of enhancing stability and bioavailability of pharmaceutically active agents, facilitating oral administration of medicaments, and simple and inexpensiv

Inactive Publication Date: 2005-02-10
BETAGERI GURU V
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0009] The current invention relates to a drug delivery system comprising at least one pharmaceutically active agent, at least one phospholipid and an enteric coating material. A particular advantage of the current invention is that it provides a simple and inexpensive system to facilitate the oral administration of medicaments. In many embodiments, this drug delivery system enhances the stability and bioavailability of pharmaceutically active agents.

Problems solved by technology

Although they represent an improvement over the prior art, oral liposome formulations have been criticized because of their instability, leakage and potential destruction in gastric fluids.
Although the oral ingestion of drugs represents a safe and versatile method of pharmaceutical delivery, the therapeutic efficacy of many drugs is reduced because many pharmaceuticals are labile or inactivated under the acidic conditions of the stomach.
For example, the utility of previous systems for orally administering labile pharmacological substances has been limited by the need to use toxic amounts of delivery agents, the instability of the systems, the inability to protect the active ingredient, the inability to effectively deliver drugs that are poorly water soluble or labile, the inadequate shelf life of the systems, the failure of the drug delivery systems to promote absorption of the active agent and the difficulties inherent to manufacturing the systems.

Method used

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  • Enteric-coated proliposomal formulations for poorly water soluble drugs
  • Enteric-coated proliposomal formulations for poorly water soluble drugs

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0039] Halofantrine and distearoyl phosphatidylcholine (1:3 ratio) were dissolved in chloroform and the solvent was evaporated using nitrogen gas. The dry powder was passed through a # 60 mesh screen. Cellulose acetate phthalate (50 mg) was dissolved in acetone (6 ml) and sprayed on the halofantrine and distearoyl phosphatidylcholine mixture.

[0040] Dissolution was carried out using 40 mg of the formulation using a Type II USP dissolution apparatus. The dissolution medium (250 ml) was phosphate buffered saline (pH 7.4). The temperature of the dissolution media was maintained at 37±0.5° C. and the rotation of the paddle was set at 50 rpm. Samples (5 ml) were withdrawn at 5, 10, 15, 30, 45, 60, 90, 120, 180 and 240 minutes. Equal volumes of phosphate buffered saline were added to maintain a constant volume of dissolution media.

[0041] The samples were analyzed by high performance liquid chromatography (HPLC). In the mobile phase, 46.5:53.5 (0.025 M potassium phosphate / sulfuric acid / tr...

example 2

[0045] Testosterone and phospholipid (DMPC, DPPC or DSPC; 1:1 ratio) were dissolved in chloroform. Chloroform was evaporated using nitrogen gas.- The dry powder was passed using a # 60 mesh sieve. Cellulose acetate phthalate (40 mg) was dissolved in acetone (5 ml) and the resulting solution was sprayed on the solid dispersion containing the testosterone and phospholipid. Nitrogen gas was used to dry the powder.

[0046] Dissolution was carried out using 45 mg of the formulation using a Type II USP dissolution apparatus. The dissolution medium (300 ml) was phosphate buffered saline (pH 7.4). The temperature of the dissolution media was maintained at 37±0.5° C. and rotation of the paddle was set at 50 rpm. The samples (5 ml) were withdrawn at 2, 5, 8, 10, 15, 20, 25, 30, 40, 50, 60, 80, 100, and 120 minutes. Equal volumes of phosphate buffered saline were added to maintain a constant volume of dissolution media. Dissolution samples were analyzed by measuring the absorbance at 254 nm.

[0...

example 3

[0048] Famotidine and distearoyl phosphatidylcholine (DSPC; 1:3 ratio) were dissolved in chloroform. Chloroform was evaporated using nitrogen gas. The dry powder was passed using a # 60 mesh sieve. Cellulose acetate phthalate (50 mg). was dissolved in acetone (5 ml) and the resulting solution was sprayed on the solid dispersion containing testosterone and phospholipid. Nitrogen gas was used to dry the powder.

[0049] Dissolution was carried out using 87 mg of the formulation using a Type II USP dissolution apparatus. The dissolution medium (300 ml) was phosphate buffered saline (pH 7.4). The temperature of the dissolution media was maintained at 37±0.5° C. and the paddle rotation was set at 50 rpm. The samples (5 ml) were withdrawn at .2, 5, 8, 10, 15, 20, 25, 30, 40, 50, 60, 80, 100, and 120 minutes. Equal volumes of phosphate buffered saline were added to maintain a constant volume of dissolution media. Dissolution samples were analyzed by measuring the absorbance at 285 nm.

[0050]...

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Abstract

This invention relates to enteric-coated proliposomal formulations for oral medicaments. In particular, it relates to an enteric-coated proliposomal oral drug delivery system for poorly water soluble drugs and methods for making the same. The drug delivery system comprises a pharmaceutical agent, a phospholipid and an enteric coating material. The present invention provides enhanced stability and bioavailability for orally administered drugs.

Description

BACKGROUND OF THE INVENTION [0001] 1. Field of the Invention [0002] This invention relates to enteric-coated proliposomal formulations for oral medicaments. In particular, it relates to enteric-coated proliposomal formulations for poorly water soluble drugs. [0003] 2. Description of the Related Art [0004] Among the various routes of drug administration, the oral route is preferred because of its versatility, safety and patient comfort. The encapsulation of pharmaceuticals in liposomes is useful in reducing toxicity and improving the therapeutic effectiveness of certain drugs. For example, compounds such as insulin, factor VIII, tryptophan, phenylalanine, heparin, vitamin K etc., have been investigated for their effectiveness orally, after encapsulation into liposomes. Although they represent an improvement over the prior art, oral liposome formulations have been criticized because of their instability, leakage and potential destruction in gastric fluids. [0005] The use of proliposom...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/06A61K9/10A61K9/127A61K9/20A61K9/30A61K9/32A61K9/36A61K9/50A61K9/54A61K9/58A61K9/60A61K31/133A61K31/426A61K31/568A61K35/64A61K45/00A61K47/04A61K47/12A61K47/14A61K47/24A61K47/32A61K47/36A61K47/38
CPCA61K9/1277A61K31/568A61K31/426A61K9/5042
Inventor BETAGERI, GURU V.
Owner BETAGERI GURU V
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