FR2641467A2 - Novel laxative compositions and process for obtaining them - Google Patents

Abstract

The invention relates to novel pharmaceutical compositions containing as active principles an ispaghula extract and a lubricant laxative in pulverulent form, wherein the weight ratio of ispaghula extract to microspheres of liquid paraffin ranges from 10 to 20 parts per 1 to 2 parts. Use as an anticholesterolaemic medicament.

Description

NEW LAXATIVE COMPOSITIONS
AND THEIR METHOD OF CBT8NTION
1st addition to French patent application 87.08270
Dens Sa of French patent de 87.08270 of June 15, 1987 entitled "New laxative compositions and their prou of obtaining", the applicant has described and claimed pharmaceutical compositions with laxative action characterized in that they contain as active ingredients a laxative of vegetable origin extracted from Ispaghul and a laxative lubricant in pulverulent form in association or in mixture with excipients or diluents inert.

 Indeed, it had been found that it was possible to add to the pulverulent extract of Ispaghul a laxative lubricant in pulverulent form, namely microspheres including paraffin oil. These microspheres contain from 75 to 95% of paraffin oil in a gelatin envelope possibly hardened by a tanning agent such as formalin or tannin. These microspheres are hard enough to form a perfectly dry powder that does not allow paraffin oil to ooze through the outer shell. These aicrospheres can, therefore, be mixed with the also pulverulent Ispaghul extract and form a perfectly homogeneous powder.

This mixture can then be added with inert excipients such as lactose, mannitol, tricalcium phosphate, magnesium carbonate, colloidal silica, sodium citrate or sodium phosphate. The powder thus formed can also be supplemented with flavoring agents such as inositol or sorbitol, sweetening agents such as saccharin or aspartame, arozatizing agents such as vanillin, ethyl vanillin, furaneol or linalylthiol , preservatives such as sorbic acid or an alkali metal sorbate, ascorbic acid or sodium ascorbate.

In the pharmaceutical compositions according to the invention, the weight ratio between the Ispaghul extract and the paraffin oil microspheres varies from 10 parts per 1 part by weight to 2 parts per 10 parts by weight. The preferred proportions are from 4 parts of Ispaghul to 1 part of paraffin oil in microspheres to 1 part of Ispaghul for 2 parts of paraffin oil.

Preferably, the pharmaceutical compositions according to the invention are present in the form of powder sachets or powder packets, containing from 4 to 10 g of mixture.

A particularly preferred composition is that which contains the Ispaghul extract and the paraffin oil microspheres in equal parts. The administration unit is that which contains 6 to 7 g of the mixture in a polyethylene bag covered with aluminum foil. The mixture according to the invention can also be distributed in well-closed glass vials and the administration of the mixture will be in the form of teaspoons with 50 to 100 ml of water.

The dosage is one or two sachets per day for a period which does not exceed five days.

Now, it has now been found, and this is the basis of the principle of the present request for a certificate of addition, that by varying the weight ratio between the extract of Ispaghul and the microspheres d paraffin oil, new and unexpected therapeutic properties can appear.

In particular, by very significantly increasing the amounts of Ispaghul extract compared to the paraffin oil microspheres, a drug is obtained whose laxative properties are markedly attenuated in favor of hypocholested roleiant properties. It has been found, in particular, that combinations containing from 10 to 20 parts of Ispaghul extract for 1 to 2 parts of paraffin oil microspheres caused by repeated administration a significant reduction in blood cholesterol. It seems indeed, without this being the only explanation, that the extract of Ispaghul by its polysaccharide acids is capable of binding to bile acids and their derivatives by reducing their resorption. Thanks to the presence of a laxative lubricant, they are eliminated by the digestive tract. This reduction in resorption leads to a depletion of the organism into biological precursors of cholesterol and consequently, a progressive decrease in circulating cholesterol.

The reduction in the paraffin oil content is also an element of importance, because while allowing real effectiveness, the microspheres of paraffin oil in small quantities, avoid the occurrence of an undesirable side effect such as laxative effect by administration prolonged.

The present addition therefore relates to new pharmaceutical compositions containing, as active principles, an xspaghul extract and a lubricating laxative in powder form consisting of hardened microspheres characterized in that the weight ratio between the extract of Ispaghul and the paraffin oil microspheres ranges from 10 to 20 for 1 to 2 parts.

These co-compositions according to the present addition may contain, in addition, diluents such as microcrystalline cellulose or lactose, sweetening substances, flavoring agents and / or thinning agents such as colloidal silica or diatomaceous earth, coloring products such as titanium oxide or iron carbonate. These various components are associated with the mixture according to the invention in the proportion of 1 for 2 to 1 for 4 parts.

The compositions according to the invention are distributed in sachets containing from 3 to 6 g of the two active principles in combination or in mixture with an inert non-toxic diluting agent pharma-.

ceutically acceptable.

The useful dosage is generally 1 to 2 sachets per day containing 3 to 6 g of the mixture of constituents and preferably 5 g of the mixture extracted from Ispaghul (10 parts) / paraffin oil microspheres (1 part).

Claims (3)

 paraffin varies from 10 to 20 parts for 1 to 2 parts.  by weight between Ispaghul extract and oil microspheres  hardened microspheres, characterized in that the ratio  lubricant in pulverulent form consisting of  active ingredients, an extract of Ispaghul and a laxative The purpose of this addition is: 1. new pharmaceutical compositions containing, as 2. the new pharmaceutical compositions according to the  claim 1 in which are further incorporated  diluting substances, and / or sweetening substances and / or  flavoring agents and / or thinning agents and / or  coloring substances. 3. the new pharmaceutical compositions according to the  claim 1 or 2 in powder form packaged in  sachets containing 3 to 6 g of the two active ingredients in  combined or mixed with an inert diluent  pharmacologically acceptable noktoxic.