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Dried forms of aqueous solubilized bile acid dosage formulation, preparation and uses thereof

A technology of bile acids and bile salts, which is applied in the direction of bulk delivery, antibacterial drugs, digestive system, etc., and can solve problems such as insufficient bioavailability, unstable water-based dosage forms, and limited uses

Inactive Publication Date: 2007-10-31
柳署弘
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The few aqueous formulations available are unstable and have very limited use due to pH control and maintenance issues
Also, some commercially available pharmaceutical dosage forms of bile acids have been found to have insufficient bioavailability

Method used

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  • Dried forms of aqueous solubilized bile acid dosage formulation, preparation and uses thereof
  • Dried forms of aqueous solubilized bile acid dosage formulation, preparation and uses thereof
  • Dried forms of aqueous solubilized bile acid dosage formulation, preparation and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment I

[0078] The first series of solution formulations prepared according to the instructions below using soluble bile acids (as free acids) and high molecular weight water-soluble starch conversion products did not exhibit any precipitation at any of the pHs tested.

[0079] Soluble bile acids Starch conversion products (min)

[0080] If it is 200mg CDCA about 30g

[0081] If it is 200mg UDCA about 5g

[0082] If it is 200mg KLCA about 12g

[0083] If it is 200mg cholic acid, about 10g

[0084] If it is 200mg deoxycholic acid, about 50g

[0085] If it is 200mg hyodeoxycholic acid about 3.5g

[0086] Add pure water to 100mL

[0087] An aqueous solution (100 mL) in which one of the above-mentioned soluble bile acids was dissolved was prepared. Maltodextrin (as a high molecular weight conversion product of water-soluble starch) is dissolved with stirring at about 60-80°C to obtain a clear solution. The pH of the resulting clear solution is adjusted with acid to prepare oral dos...

Embodiment II

[0090] A second series of solution formulations prepared according to the instructions below using soluble bile acids (as free acids) and high molecular weight water-soluble starch conversion products did not exhibit any precipitation at any of the pHs tested.

[0091] Soluble bile acids Starch conversion products (min)

[0092] If it is 200mg CDCA about 18g

[0093] If it is 200mg UDCA about 3g

[0094] If it is 200mg KLCA about 7.2g

[0095] If it is 200mg cholic acid, about 6g

[0096] If it is 200mg deoxycholic acid, about 30g

[0097] If it is 200mg hyodeoxycholic acid about 2.1g

[0098] Add pure water to 100mL

[0099] An aqueous solution (100 mL) in which one of the above-mentioned soluble bile acids was dissolved was prepared. To the resulting solution was added maltodextrin (as a high molecular weight water-soluble starch conversion product) and dissolved with stirring at room temperature to give a clear solution. Oral dosage forms, topical formulations and so...

Embodiment III

[0102] The first series of solution formulations prepared according to the instructions below using soluble bile acids (as free acids) and high molecular weight water-soluble starch conversion products did not show any precipitation at pH 6.5-8.

[0103] Soluble bile acids Starch conversion products (min)

[0104] If it is 200mg CDCA about 15g

[0105] If it is 200mg UDCA about 1.5g

[0106] If it is 200mg KLCA about 3.6g

[0107] If it is 200mg bile acid, about 3g

[0108] If it is 200mg deoxycholic acid, about 15g

[0109] If it is 200mg hyodeoxycholic acid about 3.5g

[0110] Add pure water to 100mL

[0111] An aqueous solution (100 mL) in which one of the above-mentioned soluble bile acids was dissolved was prepared. To the resulting solution was added maltodextrin (as a high molecular weight water-soluble starch conversion product) and dissolved with stirring at room temperature to give a clear solution. Injectable, colon-localized, topical, and eye drop dosage for...

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Abstract

The ionic conjugates include an inorganic particle electrostatically associated with a macromolecule which can interact specifically with predetermined chemical species or biological targets.

Description

Background of the invention [0001] Bile salts, organic acids derived from cholesterol, are natural ionic detergents that play key roles in the absorption, transport and secretion of lipids. The term primary bile acids refers to those synthesized de novo by the liver. In humans, primary bile acids include cholic acid (3α,7α,12α-trihydroxy-5β-cholanic acid) (“CA”) and chenodeoxycholic acid (3α,7α-dihydroxy-5β-cholanic acid) (“CDCA”). Dehydroxylation of these bile acids by gut bacteria produces more hydrophobic secondary bile acids such as deoxycholic acid (3α,12α-dihydroxy-5β-cholanic acid) (“DCA”) and lithocholic acid (3α-hydroxy -5β-cholanic acid) ("LCA"). These four bile acids CA, CDCA, DCA, and LCA generally account for more than 99% of the bile acid pool in the human body. Secondary bile acids that are further metabolized by the liver are sometimes called tertiary bile acids. [0002] Keto bile acids are produced in the second place in humans as a result of the oxidati...

Claims

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Application Information

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IPC IPC(8): A61K9/16
CPCA61K9/1652A61P1/16A61P31/04
Inventor 柳署弘
Owner 柳署弘
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