Bioenhanced compositions

A technology of composition and enhancer, which is applied in the field of bioenhancement composition, can solve problems such as unacceptable, difficult weight of oral bioavailability, increased solubility, etc., to reduce the degree of absorption, improve bioavailability, and reduce variability Effect

Inactive Publication Date: 2008-07-09
RUBICON RES PTY LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, large amounts of poloxamers are required to achieve a significant increase in solubility
Developing a dosage form of this complex that achieves high oral bioavailability is difficult due to weight constraints
In addition, long-term use of large amounts of poloxamers is not allowed

Method used

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  • Bioenhanced compositions
  • Bioenhanced compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Example 1 - Solubilization of Valsartan

[0075] Solid dispersions of valsartan containing different solubility enhancers in different proportions were prepared by adding valsartan to the molten mass with continuous mixing to obtain a homogeneous dispersion. The solubility of the resulting solid dispersion was determined in 0.1N HCl.

[0076] Table 1: Solubility of valsartan with different solubility enhancers in 0.1N HCl

[0077] Solid dispersion

solubility enhancer

HLB

Solubility mcg / ml

Valsartan

84.60

Valsartan: Stearoyl Macrogol Glyceride USP (Gelucire 50 / 13) 1:0.5

13

73.51 *

Valsartan: Vitamin E T.P.G.S.USP / NF1: 0.5

15

230.40

Valsartan: Vitamin E T.P.G.S.USP / NF1:1

15

337.10

Valsartan: stearoyl macrogol glyceride, USP (Gelucire 50 / 13) 1:1

13

167.19

Valsartan: Polyoxyl (polyoxyl) 40 hydrogenated castor oil, USP (Cremophor

RH40) 1:1

13

181.24

Valsa...

Embodiment 2

[0082] Example 2 - Solubilization of Valsartan Using Surfactant Composition

[0083] Valsartan solid dispersions with different solubility enhancer compositions were prepared by adding valsartan to the fusion mass of the surfactant composition under continuous mixing to obtain a homogeneous dispersion. The solubility of the resulting solid dispersion was determined in 0.1N HCl.

[0084] Table 2: Solubility of valsartan in 0.1N HCl with different solubility enhancer compositions

[0085] Solid dispersion

HLB of Solubility Enhancer Composition

Solubility mcg / ml

Valsartan

84.60

Valsartan: stearyl macrogol

Oily esters, USP (Gelucire 50 /

13): SLS * , USP1:0.5:0.1

17.5

140

Valsartan: stearyl macrogol

Oily esters, USP (Gelucire 50 /

13): SLS, US P1: 1: 0.1

15.5

171.19

Valsartan: Polyoxyethylene 40 hydrogenated

Castor Oil USP (Cremophor

RH40): SLS, USP1: 0.5: 0.1

17.5

123.7

Vals...

Embodiment 3

[0088] The preparation of embodiment 3-valsartan solid dispersion and its dissolution rate research

[0089] Gelucire was melted in a beaker at about 50°C on a hot plate with a thermostat and added to the melted amount of valsartan in a ratio of 1:0.5 (valsartan:Gelucire) and mixed for a while. To this mixture was added 2 parts of microcrystalline cellulose and stirred until it reached room temperature. A weighed amount of disintegrant (here 280 mg) was directly added into the dissolution tank for dissolution.

[0090] In Vitro Dissolution Studies

[0091] In vitro dissolution studies were performed according to the following instructions:

[0092] Dissolution medium: 0.1N HCl with 0.5% SLS

[0093] Dissolution Apparatus: USP Type II

[0094] Temperature: 37.5±0.5℃

[0095] RPM: 50

[0096] Sampling intervals: 5, 10, 15, 30, 60 and 120 minutes

[0097] Sampling volume: 10ml

[0098] Table 3: In vitro dissolution studies of valsartan alone and valsartan solid dispersio...

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PUM

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Abstract

The present invention relates to a method of increasing the bioavailability of angiotensin II receptor blockers (ARBs) by preparing a combination of the ARB and at least one solubility enhancer. The present invention particularly relates to solubility enhancers that not only function as solubility enhancers but also improve the dissolution rate in particular in acidic or weakly acidic media where the dissolution of ARBs is minimal. In the composition, the ARB can be present as a physical mixture, solid dispersion, solid solution or complex with the solubility enhancer. Combinations of ARBs and solubility enhancers can be incorporated into immediate or controlled release or other suitable modified release formulations. Immediate release formulations comprising ARB compositions have an in vitro release of at least 40% in acidic media (pH<3). Thus, the bioavailability of the ARB can be increased by at least 20%, as measured by Cmax, AUC0-t and AUC0-∞.

Description

[0001] This application claims priority from Indian Patent Application No. 477 / MUM / 2005, filed April 18, 2005, and Application No. 0315 / MUM / 2006, filed March 6, 2006, hereby denominated The content of its disclosure is incorporated herein by reference. technical field [0002] The present invention relates to a method of increasing the bioavailability of angiotensin II receptor blockers (ARBs) by preparing a combination of the ARB and at least one solubility enhancer. The present invention is particularly focused on providing a new or improved dissolution profile wherein the release of ARBs in the GI tract is independent of the physiological pH environment. Background of the invention [0003] Angiotensin II is a very potent end-product chemical that causes contraction of the muscles surrounding blood vessels, thereby causing a dramatic narrowing of the blood vessels. This narrowing increases the pressure within the arteries, causing an increase in blood pressure (hypertens...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20
Inventor N·R·帕莱普P·S·皮尔冈卡M·T·鲁斯托姆吉A·S·甘地P·R·贾殷
Owner RUBICON RES PTY LTD
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