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Neuroprotective effect of solubilized UDCA in focal ischemic model

A technology for ischemic stroke and purpose, applied in the field of clear aqueous solution, can solve the problems of lack of therapeutic intervention, nerve damage and so on

Inactive Publication Date: 2012-05-30
柳署弘
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In the absence of therapeutic intervention, nerve damage will result

Method used

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  • Neuroprotective effect of solubilized UDCA in focal ischemic model
  • Neuroprotective effect of solubilized UDCA in focal ischemic model
  • Neuroprotective effect of solubilized UDCA in focal ischemic model

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Example 1: Soluble UDCA formulations

[0061] A clear aqueous solution of dissolved UDCA (s-UDCA) containing intact UDCA and low glucose titer water-soluble starch was prepared. Briefly, 6.48 g of sodium hydroxide granules were dissolved in 500 ml of purified water, followed by dissolving 60 g of UDCA in this sodium hydroxide solution at room temperature with stirring. Then, 400 g of carbohydrate (maltodextrin) was added to the clear solution little by little and stirred. Sweeteners, preservatives (and / or sweeteners and flavoring agents) are added to the resulting clear solution in amounts suitable for pharmaceutical formulations. The pH of the clear solution was adjusted to 7-7.5 with sodium hydrogen phosphate. Purified water was added to bring the total volume to 1000 mL. The clear solution was filtered through a sterile cup filter unit with 0.22 μm and GP plus membrane if necessary.

Embodiment 2

[0062] Example 2: Soluble UDCA formulations

[0063]A clear aqueous solution of dissolved UDCA (s-UDCA) containing intact UDCA and low glucose titer water-soluble starch was prepared. Briefly, 1.1 g of sodium hydroxide particles were dissolved in 500 ml of purified water, and then 10 g of UDCA was dissolved in the sodium hydroxide solution at room temperature with stirring. Then, 500 g of carbohydrate (corn syrup solids) was added to the clear solution little by little and stirred. Sweeteners, preservatives (and / or sweeteners and flavoring agents) are added to the resulting clear solution in amounts suitable for pharmaceutical formulations. The pH of the clear solution was adjusted to 7-7.5 with sodium hydrogen phosphate. Purified water was added to bring the total volume to 1000 mL.

[0064] The Cmax of this composition is 20.4 μg / mL, which is 7 times higher than the reported actigall produced by Novartis Pharmaceuticals, Newark, New Jersey. Data from "Results of a phase ...

Embodiment 3

[0066] Example 3: Soluble UDCA Formulations

[0067] A clear aqueous solution of dissolved UDCA (s-UDCA) containing intact UDCA and low glucose titer water-soluble starch was prepared. Briefly, 2.27 g of sodium hydroxide granules were dissolved in 100 ml of purified water, followed by dissolving 25 g of UDCA in this sodium hydroxide solution at room temperature with stirring. Separately, 745g carbohydrate (maltodextrin) was added little by little into 400mL purified water and stirred until dissolved. The resulting clear carbohydrate solution and UDCA sodium salt solution were combined and stirred. To the resulting clear solution are added sweeteners, preservatives (and / or sweeteners and flavoring agents) in amounts suitable for pharmaceutical formulations. The pH of the clear solution was adjusted to 6.5-7.5 with sodium hydrogen phosphate. Purified water was added to bring the total volume to 1000 mL.

[0068] At 90 to 95°C, vacuum in a rotary evaporator (1.3×10 -1 Pa) dr...

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Abstract

The present disclosure provides compositions and methods for treating, ameliorating, or relieving at least one symptom associated with loss of blood flow to the brain including, without limitation, ischemic stroke. Compositions of the disclosure may comprise a bile acid compound and a carbohydrate, wherein both materials remain in solution for all pH values of the solution within a selected rangeof pH values. Symptoms may include infarct volume, functional recovery, apoptosis, and / or eNOS expression.

Description

technical field [0001] The present disclosure relates to systems and methods for providing a clear aqueous solution of one or more bile acids that can reduce stroke. Background technique [0002] According to recent US statistics, it is estimated that more than 400,000 patients experience a first stroke each year. Furthermore, stroke is the leading cause of disability and the third leading cause of death. Men have a higher risk of stroke than women. About 80% of all strokes may be acute ischemic strokes (due to, eg, intracranial thrombosis or extracranial embolism). With about a quarter of all strokes occurring in individuals under the age of 65, the view that stroke is a disease of old age is somewhat controversial. [0003] The ischemic cascade can occur in the first seconds to minutes after loss of perfusion to the brain. In the absence of therapeutic intervention, nerve damage will result. This injury can be divided into two areas, the infarct area where the damage ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/575A61K9/00A61K47/36A61P25/00A61K36/16
CPCA61K35/413A61K31/723A61K31/554A61K31/58A61K31/715A61K31/727A61K31/575A61K31/4743A61K31/553A61K36/16A61K31/56A61K31/522A61K31/718A61P25/00A61P9/10A61K2300/00
Inventor 柳署弘
Owner 柳署弘
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