Neuroprotective effect of solubilized UDCA in focal ischemic model

An ischemic stroke and solution technology, which can be used in nervous system diseases, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. It can solve problems such as nerve damage and lack of therapeutic intervention.

Inactive Publication Date: 2007-09-12
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 inte

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 Formulation

[0061] A clear aqueous solution of solubilized UDCA (s-UDCA) containing intact UDCA and low glucose titer water-soluble starch was prepared. Briefly, 6.48 g of sodium hydroxide particles 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 little by little to the clear solution and stirred. Sweetening agents, preservatives (and / or sweetening 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 make the total volume 1000 mL. If necessary, the clear solution was filtered through a sterile cup filter unit of 0.22 μm and GP plus membrane.

Embodiment 2

[0062] Example 2: Soluble UDCA Formulation

[0063]A clear aqueous solution of solubilized 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 next, 10 g of UDCA was dissolved in this sodium hydroxide solution at room temperature with stirring. Then, 500 g of carbohydrate (corn syrup solids) was added little by little to the clear solution and stirred. Sweetening agents, preservatives (and / or sweetening 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 make the total volume 1000 mL.

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

Embodiment 3

[0066] Example 3: Soluble UDCA Formulation

[0067] A clear aqueous solution of solubilized UDCA (s-UDCA) containing intact UDCA and low glucose titer water-soluble starch was prepared. Briefly, 2.27 g of sodium hydroxide particles 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, 745 g of carbohydrate (maltodextrin) was added little by little to 400 mL of 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 flavors) in amounts suitable for pharmaceutical formulation. The pH of the clear solution was adjusted to 6.5-7.5 with sodium hydrogen phosphate. Purified water was added to make the total volume 1000 mL.

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

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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 range of 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 U.S. statistics, it is estimated that there are more than 400,000 first-time stroke patients 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 or extracranial embolism). About a quarter of all strokes occur in individuals under the age of 65, and the notion that stroke is a disease of old age is somewhat controversial. [0003] The ischemic cascade can occur in the first few seconds to minutes after the loss of perfusion to the brain. Without therapeutic intervention, nerve damage will result. The injury can be divided into two areas, the infarct area where irreversible damage is p...

Claims

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Application Information

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