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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 have limited efficacy or tolerability or both

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
Effect test

Embodiment 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 (water was evaporated by a stream of nitrogen) 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 further precipitation occurred. After filtration, the solids were combined and dried in a water extractor. The obtained solid was determined to be pravastatin calcium salt. The resulting salt was 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 Figure 1 . From this PXRD diffraction pattern, it appears that pravastatin calcium salt is weakly crystalline.

[0189...

Embodiment 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 hermetically sealed gelatin capsules. The soft capsules were used at 25°C and the glass vials at 25, 40 and 60°C. Suspensions of salt in oil were periodically measured for 26 weeks. Degradation of pravastatin salts was measured using HPLC.

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

[0198] Figure 7 shows the stability of pravastatin salt in capped vials at 40 and 60°C. Calcium salts again showed significantly lower degradation than sodium or potassium salts at ...

Embodiment 3

[0200] fluvastatin calcium salt

[0201] Dissolve 505.9 mg (1.167 mmol) of fluvastatin Na salt in 15 mL of water. Dissolve 94.2 mg (0.595 mmol) of calcium acetate in 2 mL of water. Immediately after the addition of the calcium acetate solution to the fluvastatin Na solution, a precipitate formed. The solid was collected by filtration, first dried in a vacuum oven at 65°C for 0.5 h, and then placed under a nitrogen stream at room temperature overnight. The dried solids were ground in a mortar and pestle prior to characterization. The resulting solid was characterized using PXRD, DSC, TGA, Raman and IR spectroscopy and was determined to be the calcium salt of fluvastatin. The resulting salt was a 2:1 fluvastatin-calcium salt.

[0202] Solubility measurements of fluvastatin sodium and calcium salts were performed in water at 23°C. Solubility was measured gravimetrically in deionized water. 5.5 mg of fluvastatin sodium salt was dissolved in about 130-150 microliters of water...

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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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