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Composition and method for improving bioavailability and enhancing brain delivery of 5,5-diphenyl barbituric acid

A technology of diphenylbarbituric acid and sodium diphenylbarbiturate, which is applied in drug combinations, medical preparations containing active ingredients, and pharmaceutical formulas, etc.

Inactive Publication Date: 2007-10-10
TARO PHARMA INDS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

No prior art discloses oral solid dosage forms in the form of DPB salts with enhanced bioavailability

Method used

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  • Composition and method for improving bioavailability and enhancing brain delivery of 5,5-diphenyl barbituric acid
  • Composition and method for improving bioavailability and enhancing brain delivery of 5,5-diphenyl barbituric acid
  • Composition and method for improving bioavailability and enhancing brain delivery of 5,5-diphenyl barbituric acid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0123] The preparation of the DPB of embodiment 1 salt form

[0124] sodium salt

[0125] compound

molecular weight

Weight / grams)

Millimoles

volume

DPB

280

46.35

166

NaOH

40

6.60

165

THF

1,500ml

+150ml

DI water

25ml

[0126] THF: tetrahydrofuran; DI water: deionized water

[0127] operate:

[0128] DPB was dissolved in 1500ml THF. The cloudy solution was filtered through folded filter paper. A sodium hydroxide solution was prepared by dissolving in a mixture of 150 ml THF and 25 ml water. The sodium hydroxide solution was added dropwise to the DPB solution over 0.5 hours. DPB sodium salt formed and precipitated from solution. The mixture was stirred at room temperature for 2 hours, then cooled to 4°C and stirred at this temperature for a further 2 hours. The product was filtered and washed with cold THF. 42.57 g of wet product were obtained. The collec...

Embodiment 2

[0139] Other preparations of embodiment 2 DPB sodium salt

[0140] In Example 1, DPB was dissolved in THF, and then an equimolar amount of aqueous sodium hydroxide solution was added. This example uses a solution of sodium hydroxide in ethanol (ie, a 10% solution of NaOH in ethanol is prepared).

[0141] Operation (synthesized in THF)

[0142] DPB (7.0 g) was dissolved in 70 ml of THF at room temperature. A solution of 1 g NaOH (granules) in 10 ml absolute ethanol was added to the solution. The resulting mixture was stirred at room temperature. Cloudiness was observed immediately and precipitation of material was seen within minutes. The reaction mixture was then stirred for an additional 2 hours at room temperature. The product was filtered and washed with 15ml THF. The wet product was dried under vacuum at 105°C. Quantitative DPB was obtained. The purity of the product was 99.2%, and the water content measured by Karl Fisher method was 1.26%.

[0143] Operation (syn...

Embodiment 3

[0145] The preparation of the MMMDPB of embodiment 3 salt forms

[0146] sodium salt

[0147] 22 g MMMDPB (68 mmol) were suspended in 330 ml tert-butyl methyl ether and 10 ml methanol. The suspension was heated to 60°C and stirred at this temperature for 30 minutes. Then 13 ml of 30% sodium methoxide solution were added dropwise. During the addition, the suspension became a clear solution and after some time the product started to precipitate. After complete addition of the base, the reaction mixture was cooled to room temperature and stirred for an additional 4 hours. Filtration gave very fine crystals of the sodium salt.

[0148] The product (NaMMMDPB) was dried in a vacuum oven at 60°C for 3 hours. 18.4 g of dry sodium salt were obtained with a purity of 98.6% by HPLC analysis. Yield: 78.4%.

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Abstract

The present invention relates to a composition and a method of delivering a barbituric acid derivative to the central nervous system of a mammal in need of treatment for neurological conditions. In particular, the present invention relates to a method of administering an oral dosage form of a sodium salt of 5,5-diphenyl barburtic acid to enhance the bioavailability of 5,5-diphenyl barbituric acid and brain delivery of same.

Description

[0001] Cross References to Related Applications [0002] This application claims priority under 35 U.S.C. §1.119(e) to Provisional Application Serial No. 60 / 600,327, filed August 10, 2004, and to U.S. Serial No. 10 / 735,514, filed December 11, 2003 Continuation-in-Part (CIP) claiming priority to U.S. Provisional Application Serial No. 60 / 432,470, filed December 11, 2002, and U.S. Serial No. 10 / 354,146, filed January 30, 2003 CIP, which claims priority to U.S. Provisional Application Serial No. 60 / 352,273, filed January 30, 2002, and CIP, U.S. Serial No. 10 / 865,428, filed June 10, 2004, which is Continuation of US Serial No. 10 / 333,957 filed on January 27, 2003 and published as US6,765,379, the national phase of PCT / US01 / 23420 filed on July 26, 2001, as claimed in 2000 Priority of US Provisional Application Serial No. 60 / 221,672 filed July 26, the disclosures of which are hereby incorporated by reference in their entirety. technical field [0003] The present invention relates...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/515
CPCA61K31/515C07D239/62C07D239/64A61P17/02A61P25/00A61P25/08A61P25/14A61P25/16A61P25/22A61P27/02A61P39/04A61P43/00A61P9/00A61P9/10
Inventor 丹尼拉·古特曼阿夫拉汉姆·亚科比丹尼尔·莫罗斯巴里·莱维特霍华德·鲁特曼
Owner TARO PHARMA INDS
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