Pharmaceutical gallium compositions and methods

A composition and drug technology, applied in the direction of drug combination, pharmaceutical formula, active ingredients of heavy metal compounds, etc., can solve problems such as blood pressure drop

Inactive Publication Date: 2011-04-13
GENTA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Also, nitrates alone and in combination with certain medications (such as sildenafil) can cause a severe drop in blood pressure (ie, hypotension)

Method used

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  • Pharmaceutical gallium compositions and methods
  • Pharmaceutical gallium compositions and methods
  • Pharmaceutical gallium compositions and methods

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] 1 to 6 equivalents of ammonium citrate are gradually added to the aqueous solution containing 1 equivalent of Ga(NO3)3.9H2O at room temperature. At this time, spontaneous crystallization quickly appeared. Agitated at room temperature to form a mixture of precipitates (fine gelatinous substances) to reach a pH of about 3-4.5. The reaction was allowed to cool to room temperature. The nitrate in the solution was stripped from the precipitated gallium citrate by filtration through Whatman 3M filter paper. Then, the gallium citrate was washed with 50% isopropanol dissolved in water and 190 alcohol alcohol in sequence and rotary evaporated under high vacuum at 60-100° C. to produce a gallium citrate preparation in fine powder form.

Embodiment 2

[0079] Before drying, the two separate batches of gallium citrate in Example 1 were mixed with standard excipients, wet granulated and compressed into two different batches of ~725 mg tablets containing 30 mg of gallium. The tablets from each of these batches contained approximately 22 μg of nitrate. For comparison, two batches of Ga(NO 3 ) 3 ·9H 2 O Prepared into 2 different batches of 750 mg tablets containing 30 mg of gallium. The tablets from each of these batches contained approximately 80 mg of nitrate.

Embodiment 3

[0081] The properties of each batch of tablets in Example 2 were directly compared with single-dose dog studies. The tablets were orally administered to a group of four dogs and the gallium plasma levels were measured at different time points after administration. The results of the two gallium citrate batches and the better performing batch of gallium nitrate (clinical prototype) are shown in Table 1 below.

[0082] Table 1

[0083]

[0084] The bioavailability of two batches of gallium citrate tablets and one batch of gallium nitrate (clinical prototype) tablets with better performance after oral administration to dogs is graphically depicted in figure 1 in. The figure clearly shows that the oral absorption of gallium from each batch of gallium citrate tablets (Tmax≈30-60min) is significantly faster than that of gallium nitrate tablets (Tmax≈90-180min). In this respect, the oral administration of gallium citrate is similar to the IV administration of gallium nitrate. See Le...

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PUM

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Abstract

The present invention provides novel pharmaceutical gallium compositions, as well as methods for their preparation and methods for treating conditions and diseases such as cancer, hypercalcemia, osteoporosis, osteopenia, Paget's disease, and infections.

Description

Technical field [0001] The present invention generally relates to pharmaceutical gallium compositions, particularly those suitable for therapeutic oral, inhalation or intravenous administration. Background technique [0002] It has been proven that gallium is used in the treatment of many human and animal diseases, including hypercalcemia, cancer, metastatic bone disease, infection, and especially certain common degenerative or metabolic bone diseases such as osteoporosis and wearers. The medicinal value of Kitt disease. For example, many clinical studies have shown that gallium has anti-tumor activity and reduces abnormally high bone turnover in Paget’s disease (reviewed in Bernstein, gallium compounds for treatment, in metal therapeutic drugs and metal-based diagnostics : The use of metals in medicine 259-277 (edited by Gielen and Tiekink, 2005)). Gallium is currently approved in the U.S. as gallium nitrate for intravenous injection (Ga(NO 3 ) 3 ·9H 2 O) Solution To treat ma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C51/41C07C55/10C07C57/145C07C57/15C07C59/245C07C59/255C07C59/265C07C69/70C07C69/704A61P19/08A61P19/00A61P31/04A61P11/00A61K31/194A61K31/225
CPCA61K31/28A61P11/00A61P19/00A61P19/08A61P19/10A61P3/14A61P31/00A61P31/04A61P35/00
Inventor B·D·布朗R·P·小沃伦
Owner GENTA INC
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