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Pharmaceutical compositions containing beta-lapachone, or derivatives or analogs thereof, and methods of using same

A composition and analog technology, which can be applied in the directions of medical preparations containing active ingredients, drug combinations, medical preparations without active ingredients, etc., can solve the problems of low solubility of beta-paradone and the like

Inactive Publication Date: 2005-01-05
阿奎利公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] However, one obstacle in the development of pharmaceutical formulations containing β-paradrone suitable for parenteral and topical administration is the low solubility of β-paradrone in pharmaceutical solvents

Method used

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  • Pharmaceutical compositions containing beta-lapachone, or derivatives or analogs thereof, and methods of using same
  • Pharmaceutical compositions containing beta-lapachone, or derivatives or analogs thereof, and methods of using same
  • Pharmaceutical compositions containing beta-lapachone, or derivatives or analogs thereof, and methods of using same

Examples

Experimental program
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Effect test

Embodiment Construction

[0150] 1. Evaluation of known solvent systems that increase the solubility of hydrophobic pharmaceutical substances and are acceptable

[0151] a. Preparation of β-paradone and hydroxypropyl-β-cyclodextrin (HPBCD) solution

[0152] Various acceptable and well-known pharmaceutical solvent systems were evaluated for increasing the solubility of hydrophobic pharmaceutical substances using β-paradone. As shown in Table 5 below, among the various solutions evaluated, the solutions reached the lowest concentration targeted (10 mg / ml). However, none of these solvent systems could be diluted 5-fold with sterile saline without significant precipitation of β-paradone in solution. In addition, most co-solvents and surfactants have their own toxicity and tolerance issues that need to be addressed during high-dose administration.

[0153] table 5

[0154] Solvent system Undiluted 5 times diluted *

[0155] (mg / ml) (mg / ml)

[0156] Poloxa...

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PUM

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Abstract

It has been confirmed that β-paradone has potent antitumor activity and inhibits human cancer lines, but its solubility in most pharmaceutical solvents is poor. The present invention overcomes this important defect by adopting a novel pharmaceutical composition, which contains an effective amount of β-paradone or its derivatives, analogs and pharmaceutical solubilizing carrier molecules, and the solubilizing carrier molecules can be It is a water-solubilizing carrier molecule, such as hydroxypropyl-β-cyclodextrin, or an oil-based solubilizing carrier molecule to enhance the solubility of β-paradone in an aqueous solution. An effective amount of β-paradone or its derivatives and analogs can be mixed with pharmaceutical solubilizing carrier molecules in an aqueous solution. The novel pharmaceutical compositions can be administered with a second anticancer agent, or in combination with radiation therapy. The invention also discloses a formula, which mixes pharmaceutical solubilizing carrier molecules with β-paladone or its derivatives and analogues, and after the mixture is freeze-dried, it is reconstituted in an aqueous solution to have effective solubility. The invention also provides the β-paladone emulsion in the excipient of the medicinal fat emulsion. The invention also discloses a method for treating cancer by administering the novel pharmaceutical composition and formulation to a sick body. The invention also provides a pharmaceutical kit.

Description

field of invention [0001] The present invention relates to pharmaceutical compositions and formulations, and methods of administering these pharmaceutical compositions and formulations, comprising β-lapachone or derivatives, analogs thereof, in admixture with solubilized carrier molecules, Used to enhance the solubility of β-paradone in different solvent systems. Background of the invention [0002] More than 1.22 million new cases of cancer were diagnosed in the United States in 2001 alone. With more than 563,000 deaths per year, cancer has become the second leading cause of death after heart disease (UBS Warburg "Disease Dynamics: The Cancer Market", Nov. 8, 2000). If the cancer is caught early, both surgery and radiation therapy may be helpful, but for metastatic cancer, existing drug treatments generally only relieve symptoms and rarely lead to long-term cures. Even if it is a new chemotherapy that enters the market, the prolongation of the survival period of the patie...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/19C07D311/78A61K31/337A61K31/352A61K47/10A61K47/24A61K47/30A61K47/32A61K47/34A61K47/40A61K47/44A61P17/06A61P35/00
CPCY10S514/97A61K47/24A61K31/337Y10S514/937A61K47/10A61K31/352A61K9/0019A61K47/32Y10S514/941A61P17/00A61P17/06A61P35/00A61K2300/00
Inventor 江志伟达谢瑞瑟·G·瑞蒂
Owner 阿奎利公司
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