JP2010506855A5

JP2010506855A5 -

Info

Publication number: JP2010506855A5
Application number: JP2009532610A
Authority: JP
Filing date: 2007-10-12
Publication date: 2010-09-30

Claims

A method for selecting a fenofibric acid fast salt formulation comprising:
(a) producing a sustained release oral dosage form comprising (i) a salt of fenofibric acid, (ii) a hydrophilic polymer, and (iii) optionally one or more pharmaceutically acceptable excipients;
(b) selecting a dosage form of step (a) having at least one of the following characteristics:
(i) The release rate of fenofibric acid from the formulation is substantially independent of the ionic strength of the dissolution medium
(ii) 0.5 in (A) 900 mL 0.05 M potassium phosphate buffer (pH 6.0, 37 ° C.) and (B) 900 mL 0.3 M potassium phosphate buffer (pH 6.0, 37 ° C.) The difference in the amount of fenofibrate dissolved in 1, 2, 4, 6 or 8 hours does not exceed about 25%, or
(iii) Difference in disintegration time between (A) 900 mL of 0.05 M potassium phosphate buffer (pH 6.0, 37 ° C.) and (B) 900 mL of 0.3 M potassium phosphate buffer (pH 6.0, 37 ° C.) Is less than about 475 minutes
Including said method .

2. The method of claim 1, wherein the salt of fenofibric acid has a water solubility greater than about 16.1 mg / mL.

The method of claim 1, wherein the salt of fenofibric acid has a water solubility greater than about 19.0 mg / mL.

The salt of fenofibric acid is about 7.09 mg / min / cm in 400 mL of 50 mM sodium citrate buffer (pH 6.8). ²² The method of claim 1 having an intrinsic dissolution rate greater than

The salt of fenofibric acid is about 8.05 mg / min / cm in 400 mL of 50 mM sodium citrate buffer (pH 6.8). ²² The method of claim 1 having an intrinsic dissolution rate greater than

In (A) 900 mL of 0.05 M potassium phosphate buffer (pH 6.0, 37 ° C) and (B) 900 mL of 0.3 M potassium phosphate buffer (pH 6.0, 37 ° C), 0.5, 1, 2, The method of claim 1, wherein the difference in the amount of fenofibrate dissolved in 4, 6 or 8 hours does not exceed about 21.4%.

The difference in disintegration time between 900 mL of 0.05 M potassium phosphate buffer (pH 6.0, 37 ° C.) and (B) 900 mL of 0.3 M potassium phosphate buffer (pH 6.0, 37 ° C.) is less than about 100 minutes. The method of claim 1, wherein:

The hydrophilic polymer is selected from the group consisting of hydroxypropylmethylcellulose, hydroxypropylcellulose, hydroxyethylcellulose, polyethylene oxide, polyethylene glycol, xanthan gum, alginic acid, polyvinylpyrrolidone, starch, cross-linked homopolymer, and acrylic acid copolymer. The method described.

The method of claim 1, wherein the salt of fenofibric acid is present in the formulation in an amount of about 33 to about 75% by weight.

The method of claim 1, wherein the salt of fenofibric acid is present in the formulation in an amount of about 50 to about 75% by weight.

The method of claim 1, wherein the salt of fenofibric acid is present in the formulation in an amount of about 65.5% by weight.

A method for producing a pharmaceutical preparation suitable for oral administration comprising:
(a) selecting a fast salt preparation of fenofibric acid,
  (i) producing a sustained release oral formulation comprising (1) a salt of fenofibric acid, (2) a hydrophilic polymer, and (3) optionally other pharmaceutically acceptable excipients;
  (ii) selecting a formulation of step (a) having at least one of the following characteristics:
    (1) The release rate of fenofibric acid from the preparation is substantially independent of the ionic strength of the dissolution medium
    (2) 0.5 in (A) 900 mL 0.05 M potassium phosphate buffer (pH 6.0, 37 ° C.) and (B) 900 mL 0.3 M potassium phosphate buffer (pH 6.0, 37 ° C.) The difference in the amount of fenofibrate dissolved in 1, 2, 4, 6 or 8 hours does not exceed about 25%, or
    (3) Difference in disintegration time between (A) 900 mL of 0.05 M potassium phosphate buffer (pH 6.0, 37 ° C.) and (B) 900 mL of 0.3 M potassium phosphate buffer (pH 6.0, 37 ° C.) Is less than about 475 minutes
Including, and
(b) a step of producing a pharmaceutical preparation from the fastened salt preparation selected in step (a)
Including said method.

13. The method of claim 12, wherein the salt of fenofibric acid has a water solubility greater than about 16.1 mg / mL.

The salt of fenofibric acid is 7.09 mg / min / cm in 400 mL of 50 mM sodium citrate buffer (pH 6.8). ²² 13. The method of claim 12, having an intrinsic dissolution rate greater than

The difference in disintegration time between (A) 900 mL of 0.05 M potassium phosphate buffer (pH 6.0, 37 ° C.) and (B) 900 mL of 0.3 M potassium phosphate buffer (pH 6.0, 37 ° C.) is about 100. 13. The method of claim 12, wherein the method is less than minutes.