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Oral formulations for picoplatin

A preparation, the technology of picoplatin, applied in this field, can solve the problems of low solubility, uncomfortable infusion, difficult to prepare oral dosage forms, etc.

Inactive Publication Date: 2010-08-18
PONIARD PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Intravenous infusion is uncomfortable due to the need for insertion of a needle into the vein and the fact that the patient must remain still for a considerable period of time while administering a relatively large volume of picoplatin solution
Picoplatin is orally bioavailable, but its low solubility in water makes it difficult to prepare an effective oral dosage form

Method used

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  • Oral formulations for picoplatin
  • Oral formulations for picoplatin
  • Oral formulations for picoplatin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0139] Example 1: HPLC method for picoplatin

[0140] condition:

[0141] column:

Luna 5u C18(2)250×4.6mm 00G-4252-E0

(Phenomenex)

Mobile phase A:

0.2% TFA in deionized water (v / v)

Mobile phase B:

Methanol HPLC grade

Flow rate:

1.0mL / min

Detection wavelength:

267nm

Column temperature:

35℃

Sample temperature:

25℃

[0142] Time to go:

25 minutes

Sample diluent:

normal saline

[0143] Table I - Gradient

[0144]

Embodiment 2

[0145] Example 2: Determination of the solubility of picoplatin at various pH values.

[0146] The goals of this study were to determine the solubility of picoplatin in aqueous solutions and to measure the effect of pH on picoplatin solubility.

[0147] Table II - pH Buffers

[0148]

[0149]

[0150] step:

[0151] Picoplatin (10 mg) was weighed into 0.5 mL Eppendorf tubes, 10 tubes in total, and 250 μL of buffer or water was added to these picoplatins. The tubes were mixed for 1 minute. Measure the pH of each tube. The tubes were then placed on a shaker at 25°C in the dark for 16 hours and the pH was measured again. These solutions were centrifuged through 0.45 uM Spin-X filters, and 50 mg of each filtrate was transferred to individual HPLC tubes. 1.5 mL of 0.9% NaCl solution (physiological saline) was added to these HPLC tubes, followed by HPLC analysis immediately to determine the concentration of each sample.

[0152] Table III - pH of picoplatin in bu...

Embodiment 3

[0155] Example 3: Determination of the pH-stability profile of picoplatin.

[0156] The goals of this study were to determine the effect of pH on the stability of picoplatin in aqueous solution and to evaluate the overall stability of picoplatin in aqueous solution.

[0157] Table IV - pH Buffers

[0158]

[0159] step:

[0160]Picoplatin (10 mg + / - 0.1 mg) was weighed into a 5 mL volumetric flask, then saline was added to the 5 mL volume and the sample was mixed by inversion to dissolve all solids to obtain a 2 mg / mL stock solution. Then, 0.375 mL of the stock solution was added to 1.125 mL of the indicated pH buffer, deionized water, or saline in the HPLC tube and mixed by swirling for 10 seconds to obtain a 0.5 mg / mL test solution. Two tubes were made for each pH for checking.

[0161] Samples were then injected for HPLC analysis, one analysis per tube in the following order: pH 6, pH 5, pH 4, pH 3, pH 2, deionized water, saline.

[0162] Then, for each solutio...

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Abstract

The invention provides formulations for the organoplatinum anticancer drug picoplatin. Self emulsifying compositions, stabilized nanoparticulate compositions, solid dispersions, and nanoparticulate suspensions in oils are provided, along with methods for preparation of the formulations. The formulations can provide improved oral availability of picoplatin relative a to a simple solution of picoplatin such as in water or normal saline solution and can be used in combination therapy.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to U.S. Provisional Application 60 / 950,033, filed July 16, 2007, and U.S. Provisional Application 61 / 043,962, filed April 10, 2008, both titled "Oral Formulations for Picoplatin" The entire content of is incorporated herein by reference. Background technique [0003] Picoplatin, a new generation of organoplatinum drugs, has shown promise for the treatment of a variety of malignancies, including those already resistant to existing organoplatinum drugs such as cisplatin and carboplatin. resistant malignancies. Picoplatin has shown promise for the treatment of a variety of cancers or tumors, including small cell lung cancer, colorectal cancer, and hormone-resistant prostate cancer. [0004] The structure of picoplatin is: [0005] [0006] It is named cis-amminedichloro(2-picoline)platinum(II), or [SP-4-3]-ammine(dichloro)(2-picoline)platinum(II) . The compound is a planar complex of...

Claims

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Application Information

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IPC IPC(8): C07F15/00
CPCA61K31/282A61K9/145A61K9/19A61K9/1075A61K9/10A61P35/00A61P35/02
Inventor A·X·陈C·郭C·A·普罗西夏伊
Owner PONIARD PHARMA INC
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