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Pharmaceutical composition comprising racetam and carnitine and process for its preparation

A composition, the technology of carnitine, applied in the treatment and/or prevention of mitochondrial disorders, the treatment and/or prevention of mitochondrial disorders, and the field of pharmaceutically acceptable carriers, can solve the problem of combination without beneficial effects of racetam compounds

Inactive Publication Date: 2011-04-13
BIOLAB SANUS FARMACEUTICA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0028] As discussed in the Background of the Invention, to date there is no drug combination that combines the beneficial effects of a racetam (eg, piracetam) with carnitine
In addition, there are no drugs to combine the combination with CoQ10, or with therapeutic agents related to mitochondrial and / or metabolic disorders, to reduce the side effects of treatments based on agents used in the treatment of said disorders, such as cholesterol-lowering drugs, Hypoglycemic drugs, antiepileptic drugs, etc.

Method used

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  • Pharmaceutical composition comprising racetam and carnitine and process for its preparation
  • Pharmaceutical composition comprising racetam and carnitine and process for its preparation
  • Pharmaceutical composition comprising racetam and carnitine and process for its preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] Example 1 - In vitro detection of MPT in response to calcium and simvastatin

[0074] A second protocol different from the above was used in the experiments of this example. Mitochondria were isolated from rat or mouse livers by conventional differential centrifugation using adult animals fasted for 12 hours (see Kaplan RS, Pedersen PL for a description of the method, Characterization of phosphate efflux pathways in rat liver mitochondria. Biochem J 1983; 212: 279-88). Liver was homogenized in 250 mM sucrose, 1 mM EGTA and 10 mM Hepes (pH 7.2) buffer. The mitochondrial suspension was washed twice and the final pellet was resuspended in 250 mM sucrose solution to a final concentration of 80-100 mg / ml protein.

[0075] figure 1 Dose response curves for calcium and simvastatin are illustrated. The results indicated that simvastatin induced MPT. Specifically, 40 μM simvastatin plus 30 μM Ca 2+ Causes a maximal increase in mitochondrial swelling. In the figure, Ca re...

Embodiment 2

[0076] Example 2 - Effect of the combination of L-carnitine and piracetam on mitochondrial swelling induced by statins

[0077] The combination was evaluated at the same concentrations after determining the minimum dose of L-carnitine and the minimum dose of piracetam that showed some protection against mitochondrial swelling caused by statins (simvastatin, pravastatin and lovastatin) (L-Carnitine + Piracetam) Efficiency. Therefore, it was determined that for simvastatin and pravastatin, 0.5 μg / ml L-carnitine + 1.25 μg / ml piracetam would be useful (respectively figure 2 and 3 ); while for lovastatin, 0.5 μg / ml L-carnitine + 1.25 μg / ml piracetam is useful ( Figure 4 ).

[0078] figure 2 In, MFR (0.5 mg / ml) in the presence of simvastatin (line b), simvastatin + 0.5 μg / ml L-carnitine (line c), simvastatin + 1.25 μg / ml piracetam ( Line d) and simvastatin+0.5μg / ml L-carnitine+1.25μg / ml piracetam (line e) were incubated in the standard reaction solution, and compared with th...

Embodiment 3

[0082] Example 3 - Effect of Coenzyme Q10 Alone, or in Combination with L-Carnitine and Piracetam (Piracar) on Mitochondrial Swelling Caused by Simvastatin

[0083] Figure 5 Shows the spectrophotometric profile of MFR (0.5 mg / ml) in the presence of simvastatin (line b), simvastatin+Piracar 0.25 / 0.65 μg / ml (line c), simvastatin+CoQ 5 μg / ml (line d) Incubate with standard reaction solution of simvastatin+CoQ 5 μg / ml+Piracar 0.25 / 0.65 μg / ml (line e), and compare with mitochondria without simvastatin addition (control, line a). These results again confirm the synergistic effect of the combination of L-carnitine and Piracetam (PIRACAR), and the protective effect of the addition of Coenzyme Q10 in avoiding mitochondrial swelling. In the figure, tempo refers to time, and segundos refers to seconds.

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Abstract

The present invention refers to a pharmaceutical composition comprising racetam and carnitine. Said pharmaceutical composition may further comprise coenzyme QlO and / or agent associated with mitochondrial and / or metabolic disturbance,such as hypocholesterolemic agent of the statins group, a hypoglycemic agent, or an antiepileptic agent. The invention also includes a method of treatment for mitochondrial disturbances comprising administration of the pharmaceutical composition of the invention.

Description

field of invention [0001] The present invention relates to a pharmaceutical composition, comprising: (a) a combination of racetam and carnitine, and (b) a pharmaceutically acceptable carrier. Preferably, the pharmaceutical composition of the present invention comprises: (a) a combination of piracetam and carnitine, and (b) a pharmaceutically acceptable carrier. The compositions of the present invention may additionally include Coenzyme Q10, and optionally include therapeutic agents related to mitochondrial and / or metabolic disorders, such as cholesterol-lowering drugs, preferably statins, anti-epileptic drugs, hypoglycemic drugs, and the like. The invention also relates to methods of treatment and / or prevention of mitochondrial disorders, including Alzheimer's and Parkinson's diseases. The present invention also relates to the use of said combination in the preparation of a medicament for the treatment and / or prevention of mitochondrial disorders, including Alzheimer's and Pa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4015A61K31/205A61K31/20
CPCA61K31/4015A61K45/06A61K9/2846A61K31/122A61K9/0095A61K31/205A61K9/0019A61K9/4866A61P21/00A61P25/00A61P25/08A61P25/16A61P25/28A61P3/00A61P3/06A61P43/00A61P5/44A61P3/10A61K2300/00A61K31/40
Inventor J·R·D·C·佩雷拉M·法尔奇M·M·阿拉里奥
Owner BIOLAB SANUS FARMACEUTICA LTD
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