Novel statin pharmaceutical compositions and related methods of treatment

A composition and drug technology, applied in the direction of pharmaceutical formulations, active ingredients of heterocyclic compounds, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2007-07-04
TRANSFORM PHARM INC (US)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Unfortunately, all of these treatments hav

Method used

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  • Novel statin pharmaceutical compositions and related methods of treatment
  • Novel statin pharmaceutical compositions and related methods of treatment
  • Novel statin pharmaceutical compositions and related methods of treatment

Examples

Experimental program
Comparison scheme
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Example Embodiment

[0185] Example 1

[0186] Pravastatin calcium salt

[0187] To a solution of pravastatin Na salt (1.470 g; 3.292 mmol) in water (15.0 mL) was added a solution of calcium acetate (268 mg; 1.70 mmol) in water (5.0 mL). The resulting solution was concentrated (evaporating water by nitrogen flow) to about 15 mL, and cooled to 0°C. The precipitated white solid was collected by filtration. The filtrate was cooled to 0°C again, and a precipitate further precipitated. After filtration, the solids were combined and dried in a water extractor. It is determined that the solid obtained is pravastatin calcium salt. The salt obtained is a 2:1 pravastatin-calcium salt.

[0188] Figure 1 shows the PXRD diffraction pattern of pravastatin calcium salt (Bruker, data collection). Pravastatin calcium salt can be characterized by any one, any two, any three, or any four or more PXRD peaks in FIG. 1. According to the PXRD diffraction pattern, it seems that pravastatin calcium salt is weakly crystalline....

Example Embodiment

[0194] Example 2

[0195] 26-week solubility data of pravastatin salt in E463808

[0196] Several salts of pravastatin were suspended in E463808 omega-3 oil and placed in capped glass vials or closed gelatin capsules. Soft capsules are used at 25°C and glass vials are used at 25, 40 and 60°C. Periodic measurements of salt in oil suspensions lasted 26 weeks. The degradation of pravastatin salt was measured using HPLC.

[0197] Figure 6 shows the stability data of vials and gelatin capsules (soft capsules) at 25°C. The calcium salt of pravastatin over time shows a significantly lower percentage of impurities than the sodium salt in the soft capsule or the potassium salt in the vial. The calcium salt in the vial showed the least degradation among all the salts in the soft capsule or vial after being placed at 25°C for 26 weeks.

[0198] Figure 7 shows the stability of pravastatin salt in a capped vial at 40 and 60°C. Calcium salt again showed significantly lower degradation than sodi...

Example Embodiment

[0199] Example 3

[0200] Fluvastatin calcium salt

[0201] 505.9 mg (1.167 mmol) of fluvastatin Na salt was dissolved in 15 mL of water. 94.2 mg (0.595 mmol) of calcium acetate was dissolved in 2 mL of water. After adding the calcium acetate solution to the fluvastatin Na solution, a precipitate formed immediately. The solid was collected by filtration, first dried in a vacuum oven at 65°C for 0.5 hours, and then placed in a nitrogen stream at room temperature overnight. The dried solids were placed in a mortar and ground with a mallet before characterization. The obtained solid was characterized by PXRD, DSC, TGA, Raman and IR spectroscopy, and it was determined to be the calcium salt of fluvastatin. The resulting salt is a 2:1 fluvastatin-calcium salt.

[0202] The solubility measurement of fluvastatin sodium and calcium salt was performed in water at 23°C. The solubility is measured gravimetrically in deionized water. 5.5 mg of fluvastatin sodium salt is dissolved in about 130...

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Abstract

The invention provides novel omega-3 oil solutions of one or more statins. These solutions are readily bioavailable. Notably, because the solutions of the invention contain an omega-3 oil as the major ingredient, they not only provide an antihypercholesterolemic effect due to the statin active ingredient, they also provide recommended daily dosages of omega-3 oils (i.e., approximately 1 gram of omega-3 oil per day), or a portion thereof. The invention also provides novel salts of one or more statins.

Description

[0001] This application claims U.S. Provisional Application Serial No. 60 / 599,543, filed August 6, 2004, U.S. Provisional Application Serial No. 60 / 623,518, filed October 29, 2004, and U.S. Provisional Application Serial No. Priority benefit of Provisional Application Serial No. 60 / 655,982, the entire contents of which are hereby incorporated by reference. field of invention [0002] The present invention provides novel omega-3 ester-based oily suspensions of statins. These suspensions basically have no food effect, are effective in small volumes, and are easily bioavailable. Background of the invention [0003] It has been clear for decades that elevated blood cholesterol is a major risk factor for coronary heart disease (CHD), and many studies have shown that the risk of CHD events can be reduced with treatment. Before 1987, lipid-lowering substances were largely limited to foods low in saturated fat and cholesterol, bile acid seque...

Claims

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Application Information

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IPC IPC(8): A61K31/35A61K31/56
Inventor H·古兹曼O·阿尔马森J·雷梅纳
Owner TRANSFORM PHARM INC (US)
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