Oral medicament comprising an osmotic laxative incorporated into a matrix based on plant fats with reduced doses of macrogol

Abstract

Oral medicament comprising an osmotic laxative incorporated into a matrix based on plant fats. The present invention relates to an oral pharmaceutical composition comprising: between 30 and 55% by weight of said pharmaceutical composition of micronized anhydrous macrogol; and between 45 and 70% by weight of the pharmaceutical composition of a carrier consisting of an anhydrous hydrophobic lipid coating based on fatty compounds of plant origin, having a melting point of between 36 and 38° C., and to the use thereof as laxative. Said composition enables the reduction in the daily dosage of macrogol by preserving the osmotic pressure thereof as far as the colon, the site of therapeutic action of osmotic laxatives; said carrier protects the macrogol from a reduction, due to the moisture in the digestive tract, in the osmotic pressure.

Claims

1. A method of treatment of constipation in an adult comprising administering an effective amount of an oral pharmaceutical composition as a laxative to an adult in need thereof, wherein said composition is administered in a quantity featuring a reduced dosage of macrogol of 5 g to 15 g per day, wherein the oral pharmaceutical composition comprises: from 30% to 55% by weight of the oral pharmaceutical composition of anhydrous macrogol, the anhydrous macrogol being in the form of a powder; from 45% to 70% by weight of the oral pharmaceutical composition of a carrier consisting of an anhydrous hydrophobic lipid coating surrounding the anhydrous macrogol, the anhydrous hydrophobic lipid coating comprising a fatty compound of plant origin and with a melting point between 36 and 38° C.; and from 0% to 5% by weight of the oral pharmaceutical composition of an excipient selected from the group consisting of thinners, agents that improve homogeneity, sweeteners, aromas, emulsifiers, and combinations thereof, wherein a ratio of a first weight fraction of the anhydrous hydrophobic lipid coating between 45% and 70% of the composition to a second weight fraction of the macrogol between 30% and 55% of the composition is selected such that the anhydrous hydrophobic lipid coating maintains the osmotic pressure of the reduced dosage of the anhydrous macrogol until the oral pharmaceutical composition reaches the colon, thereby localizing administration at the colon.

2. The method of claim 1, wherein the reduced dosage, released in the colon, reduces unwanted side effects selected from stomach cramps, bloating and flatulence.

3. The method of claim 1, wherein the oral pharmaceutical composition localizes the treatment of constipation to the colon, as a result of the oral pharmaceutical composition affording osmotic protection until the pharmaceutical composition reaches the colon.

4. The method of claim 1, wherein the anhydrous hydrophobic lipid coating of said oral pharmaceutical composition comprises: up to 100% by weight of the carrier of shea butter, cocoa butter, or a combination thereof; or from 12% to 25% by weight of the carrier of vegetable wax; and from 25% to 88% by weight of the carrier of a vegetable oil, to a sum total of 100%, providing the melting point of said carrier between 36° C. to 38° C.

5. The method of claim 4, wherein the vegetable oil is selected from the group consisting of sunflower oil, colza oil, corn oil, linseed oil, and a mixture thereof.

Description

EXAMPLES

Examples of Compositions According to the Invention

Composition 1A

(1) TABLE-US-00006 Active ingredient: micronized macrogol 4000 50.00 g  Excipient: Carnauba wax 9.65 g Corn oil 36.70 g  Gylcerol stearate 1.87 g Other excipients 1.78 g (Cholesterol, aroma, aspartame)

Composition 1B

(2) TABLE-US-00007 Active ingredient: micronized macrogol 4000 50.00 g  Excipient: Carnauba wax 6.20 g Corn oil 38.70 g  Gylcerol stearate 1.87 g Other excipients 3.23 g (Cholesterol, aroma, aspartame)

Composition 2A

(3) TABLE-US-00008 Active ingredient: macrogol 3350 55.00 g  Excipients: Carnauba wax 9.35 g Sunflower oil 33.87 g  Other excipients 1.78 g (Aromas, emulsifier, sweetener)

Composition 3A

(4) TABLE-US-00009 Active ingredient: micronized macrogol 4000 35.00 g Excipients: Shea butter 62.00 g Other excipients  3.00 g (Aromas, emulsifier, sweetener, thinner)

Composition 3B

(5) TABLE-US-00010 Active ingredient: micronized macrogol 4000 40.00 g Excipients: Shea butter 35.00 g Cocoa butter  5.00 g Corn oil 17.00 g Other excipients  3.00 g (Aromas, emulsifier, sweetener, thinner)