Extracts, fractions and compositions comprising acetogenins and their applications

A solid oral dosage form for treatment of inflammation, made by:

• 1) providing an ethyl acetate extract of Annona squamosa leaves, said ethyl acetate extract being prepared by a process comprising:
• a) pulverizing said Annona squamosa leaves;
• b) extracting said pulverized Annona squamosa leaves with hexane to obtain a first solution;
• c) separating said first solution from a spent raw material;
• d) extracting said spent raw material with ethyl acetate to obtain a second solution;
• e) concentrating said second solution to obtain said ethyl acetate extract;
• and
• 2) incorporating an effective amount of said extract into a solid oral dosage form.

A solid oral dosage form for treatment of inflammation, comprising;

• i) an organic solvent extract of Annona squamosa seeds in an amount effective for treatment of inflammation, said organic solvent extract comprising acetogenins and being prepared by a process comprising:
• a) pulverizing said Annona squamosa seeds;
• b) extracting said pulverized Annona squamosa seeds with ethyl acetate or hexane to obtain a solution;
• c) separating said solution from a spent raw material;
• d) concentrating said solution to obtain said organic solvent extract;
• and
• ii) a second anti-inflammatory agent which is an organic solvent extract of Annona squamosa leaves or an anti-inflammatory extract of a plant other than Annona squamosa;
• wherein said solid oral dosage form is a tablet, soft capsule, hard capsule, soft gel capsule, pill, or a dosage form comprising a controlled release polymer-based coating.

A solid oral dosage form for treatment of inflammation, comprising:

• i) an organic solvent extract of Annona squamosa leaves in an amount effective for treatment of inflammation, said organic solvent extract comprising acetogenins and being prepared by a process comprising:
• a) pulverizing said Annona squamosa leaves;
• b) extracting said pulverized Annona squamosa leaves with alcohol or ethyl acetate to obtain a solution;
• c) separating said solution from a spent raw material;
• d) concentrating said solution to obtain said organic solvent extract;
• and
• ii) a second anti-inflammatory agent which is an ethyl acetate or hexane extract of Annona squamosa leaves or an anti-inflammatory extract of a plant other than Annona squamosa;
• wherein said solid oral dosage form is a tablet, soft capsule, hard capsule, soft gel capsule, pill, or a dosage form comprising a controlled release polymer-based coating.

A solid oral dosage form for treatment of inflammation, comprising:

• an organic solvent extract of Annona squamosa in an amount effective for treatment of inflammation, said extract being prepared by a process comprising:
• a) pulverizing Annona squamosa seeds or Annona squamosa leaves;
• b) extracting said pulverized Annona squamosa seeds or Annona squamosa leaves with an organic solvent to obtain a solution;
• c) separating said solution from a spent raw material;
• d) concentrating said solution to obtain said organic solvent extract;
• wherein said solid oral dosage form is a tablet, soft capsule, hard capsule, soft gel capsule, pill, or a dosage form comprising a controlled release polymer-based coating;
• wherein said organic solvent extract is selected from the group consisting of:
• an organic solvent extract of Annona squamosa leaves having an IC50 for inhibition of TNFα of between about 8 and about 29 ng/ml;
• an ethyl acetate extract of Annona squamosa seeds;
• and
• a mixture thereof.