USE OF COLOSTRUM FOR THE TREATMENT OF CONSTIPATION

Abstract: Gastro-resistant pharmaceutical formulations containing animal colostrum for the treatment of constipation, and the use of colostrum for the treatment of constipation.

Description: Use of colostrum for the treatment of constipation The present invention relates to gastro-resistant pharmaceutical formulations containing animal colostrum for the treatment of constipation, and the use of colostrum for the treatment of constipation. Constipation is a widespread problem in adults and children, consisting in the difficult or infrequent passage of the stool mass through the colon, which mass accumulates becoming hard following water reasdorption. Constipation can be acute or chronic, due to organic, traumatic, functional, neurogenic conditions and the like. The treatment of constipation involves various alternatives: Enrichment in the vegetable fibres content of the diet, use of agents increasing stool bulk (natural or semisynthetic polysaccharides and cellulose derivatives, such as bran, psyllium and methylcellulose) or mineral oils, to increase stool bulk and keep it softer, thanks to an increased adsorption of liquids in the intestinal tract. Such an approach, however, is not always sufficient to overcome the problem. Use of saline or osmotic laxatives, such as salts (magnesium; sodium and potassium sulfates, phosphates and tartrates); lactulose, sorbitol: they transit rapidly in the bowel, where they cause an increase in osmotic pressure and therefore an increase in water adsorption in the feces and the peristalsis stimulation. This laxatives act rapidly and are generally used to empty the bowel prior to diagnostic procedures and surgery; they are contraindicated in case of renal failure and heart failure. Use of stimulant laxatives (phenolphthalein, castor oil, anthraquinone derivatives such as senna and cascara), which promote an increase in peristalsis and intraluminal fluid. They can cause a remarkable irritation of bowel and electrolyte balance disturbances. Therefore, a medicament promoting elimination without causing the above mentioned side-effects is much needed. The present invention aims at overcoming the above cited problems, by the use of gastro-resistant pharmaceutical formulations containing equine, bovine or anyhow animal, but preferably equine, colostrum, for the treatment of constipation. The present invention further relates to the use of equine, bovine or anyhow animal, but preferably equine, colostrum, as a laxative. It has surprisingly been found that colostrum, administered to patients suffering from constipation, acts favourably inducing elimination of stool mass without causing irritation, cramps or electrolyte disturbances. In fact, during the clinic trials, 11 out of 12 treated patients showed a favourable response to the treatment with colostrum, obtaining an effective, natural laxative action. It should be stressed that colostrum exerts and effective action in the treatment of women suffering from pregnancy or post-partum constipation, which are delicate conditions difficult to treat, as the response to the treatment with both bulking agents and common laxatives is poor, and contraindications to pharmacological treatment are remarkable, since drugs can induce uterus contractions in the pregnant woman (as is the case with castor oil) or they can be present in breast milk in amounts adversely affecting the breast¬ fed infant (particularly anthraquinone laxatives). The colostrum treated patients obtained an effective, physiological laxative effect without any side-effects. The gastro-resistant pharmaceutical formulations of invention contain powder or liquid colostrum in amounts of 10 mg to 5 g per unitary dose. More particularly, the formulations of the invention comprise gastro-resistant tablets containing powdered, freeze-dried or sprayzed colostrum, or gastro- resistant pearls containing liquid colostrum. The gastro-resistant tablets or pearls of invention are prepared according to the conventional pharmaceutical techniques for the preparation of gastro- resistant formulations, for example an enteric coating can be applied to a colostrum core by means of fluidized bed coating or pan coating techniques. The enteric coating is used to protect colostrum against the gastric acid environment, such a coating can consist of copolymerized methacrylic acid/methacrylic acid methyl esters, such as those known under the names Eudragit R (commercialized by Rohm Pharma), polymers such as cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, water-based polymer dispersions, such as Eudragit* (by Rohm Pharma), Aquateric R (PMC Corp.). The enteric coating can optionally contain plasticizers such as triacetin, cetanol, citric and phthalic acids esters. The formulations of the invention can optionally contain other active ingredients known to have a beneficial effect on the condition to treat, particularly vegetable extracts. According to a further aspect of the invention, the formulations can contain colostrum mixed with milk. The following examples further illustrate the invention. Example 1 One enteric-coated tablet contains: Powder colostrum 145 mg Hydroxypropyl methylcellulose phthalate 6 mg Cetyl alcohol 0.5 mg The enteric coating solution is applied on the colostrum core by fluidized bed coating. Example 2 One enteric-coated tablet contains: Powder colostrum 64 mg Powder milk 45 mg Hydroxypropyl methylcellulose phthalate 32 mg Cetyl alcohol 5 mg The enteric coating solution is applied on the colostrum core by fluidized bed coating. Example 3 One 400 mg capsule contains: Freeze-dried colostrum 12 mg Cassia acutifolia dried leaves 25 mg Aloe vera 40 mg Gelidum e Gracilaria 120 mg Rheum Rhaponticum rhizome 85 mg Carbo ligni 118 mg The whole mass is mixed thoroughly, then placed into a gastro-resistant capsule. Example 4 One 400 mg capsule contains: Freeze-dried colostrum 60 mg Cassia acutifolia dried leaves 25 mg Aloe vera 40 mg Gelidum e Gracilaria 105 mg Rheum Rhaponticum rhizome 80 mg Carbo ligni 90 mg The whole mass is mixed thoroughly, then placed into a gastro-resistant capsule.

Claims: CLAIMS 1. Gastro-resistant pharmaceutical formulations containing colostrum for the treatment of constipation. 2. Pharmaceutical formulations according to claim 1, wherein the colostrum is equine, bovine or anyhow animal, but preferably equine, colostrum. 3. Formulations according to claims 1 and 2, in the form of gastro-resistant tablets or pearls, containing respectively powder or liquid colostrum. 4. Formulations according to the above claims, containing 10 mg to 5 g of powder or liquid colostrum per unitary dose. 5. Formulations according to claims 3 and 4, wherein the powder colostrum is freeze-dried or sprayzed. 6. Formulations according to the above claims, further containing powder milk. 7. The use of colostrum for the preparation of a medicament for the treatment of constipation.

Inventors: FERRARIO GIANLUIGI, FERRARIO, GIANLUIGI
Applicants: FERRARIO GIANLUIGI, SYLVIE LIMITED, FERRARIO, GIANLUIGI
Application year: 1997
Main classification: A61K35
IPC codes: A61K35