DE10346083A1 - Powdered composition for use as a laxative - Google Patents

Abstract

A laxative based on a pulverulent composition is described, which in addition to plantation seeds (Plantaginis ovatae semen) and / or plantago seed husks and at least one anthranoid compound with laxative effect, in particular at least one sennoside, preferably in the form of anthranoid- or sennoside-containing plants (stock) share , also contains at least one polygalactomannan-based polysaccharide or its derivative. The latter acts on the one hand as a (co) stabilizer in an aqueous suspension of the powdered composition and on the other hand, in particular due to its swelling ability, synergistically with the other components of the composition by supporting their laxative effect, and also facilitates the processability of the invention Composition of a finely divided powder which is readily dispersible in water.

Description

The The present invention relates to a powdered composition for use as a laxative (laxative, Laxative). In particular, the present invention relates to a powdery composition plantation seeds and / or plantago seed husks and anthranoids Compounds, in particular sennosides, preferably in the form of Anthranoidhaltigen, in particular sennosidhaltigen plant parts or Plant components, as well as the use of this composition as a laxative (laxative, Laxative).

Laxativa - synonymous also known as "laxatives" or "laxatives" - there are in most diverse Manifestations, including many herbal laxatives.

So For example, the use of plantago seeds (Plantaginis ovatae semen or Semen plantaginis ovatae, synonymous as Indian Psyllium, Psyllium, Ispaghula, or Psyllium Semen Ispaghulae) or its seed shells (plantago seed husks, Plantaginis ovatae seminis integumentum) for regulatory medicinal products intestinal activity known. Plantago seeds have considerable swelling capacity and practice a physical strain on the sensitive receptors of the intestinal walls out. According to a known method (see DE-PS 11 03 520) finely grind the seeds and add water to a viscous paste and dried in strand form, crushed and finally coated.

The Effect of the senna plant (Senna plant, Cassia senna L. and Cassia angustifolia Vahl), especially its fruits (Fructus sennae, synonymous also known as senna pods or senna bladders) (eg Alexandrian senna fruits = sennae fructus acutifoliae and / or Tinnevelly senna fruits = Sennae fructus angustifoliae) or their fruit pods as well as their pinnate leaves (Folia sennae), as a herbal laxative is also known.

Furthermore Laxatives, which are the two aforementioned principles of action, are also known unite, for example Laxativa, where the physical effect the plantago seeds by the pharmacologically stimulating active principle the sennoside, the ingredients of the senna fruits, is supported, to achieve a better overall effect.

So it is already known mixtures of ground plantation seed and senna fruits as a simple mixture in which the constituents coexist, to assemble. However, in such mixtures the flowability and suspensibility in water not optimally adjust what for the oral Application but desirable would. Also is the processing of these mixtures into ready-to-use powders not or not readily possible.

To remedy the aforementioned disadvantages, is in the DE 30 01 357 C2 a laxative in the form of a laxative granules based on senna fruits, plantation seeds and optionally plantago seed shells having increased sustained release action has been proposed in which the senna particles of plantago seeds, in particular mucilages of the planta seeds, are enclosed or enveloped. The composition described there is an efficient laxative. However, since the composition is present as granules with about 1 to about 3 mm grain size of the granules, ie as asymmetric aggregates of powder particles, it must be taken with plenty of water. Otherwise, there is a risk that it may result in improper oral intake or application, ie ingestion or application with too small amounts of water to the formation of swollen lumps of granules, which in the worst cases to a closure of the esophagus or even the gastrointestinal tract.

On the market laxatives based on psyllium or psyllium or their components often provide sufficient laxative effect and remain after suspension in water due to the rapid onset of the action of the psyllium seed long drinkable, so that they conditions immediately after the production of aq Suspension must be taken. Because after suspension in water, these products gel after just a few minutes and form a thick, ungrainkable lump on the surface. In addition, in most preparations very quickly at least a two-layer phase separation, which no longer ensures the homogeneous distribution of the active components in the stirred preparation. These preparations must be taken with plenty of water who because otherwise there is a risk that it may lead to the formation of swollen lumps that can lead to a closure of the esophagus or even the gastrointestinal tract in the worst cases. Furthermore, these products also the bland taste and artificial appearance is disadvantageous.

Consequently The present invention is based on the object, a composition for use as a laxative, which the pre-described At least largely avoids disadvantages.

A Another object of the present invention is the provision a composition which can be used as a laxative, on the one hand a good laxative Effect shows, but at the same time a facilitated, complication-free Application allows especially without the pre-identified problems or risks.

Finally, another object of the present invention is the further development of the in DE 30 01 357 C2 described laxatives.

The Applicant has now surprisingly found out that a composition or mixture based on plantago seeds and / or Plantago seed shells, as well as anthranoid compounds with laxatives or laxative Effect, especially sennosides, preferably in the form of anthranoidhaltigen or sennoside-containing plants (stock) (eg fruits or leaflets of senna plants), can be processed to a finely divided powder, which avoids the aforementioned disadvantages in its use as a laxative, when this composition is combined with a polygalactomannan or its derivative formulated.

• (A) Plantagosamen (Plantaginis ovatae Semen) und/oder (A') Plantagosamenschalen; und
• (B) mindestens eine anthranoide Verbindung, insbesondere mindestens ein Sennosid, vorzugsweise in Form von anthranoidhaltigen, insbesondere sennosidhaltigen Pflanzenteilen oder Pflanzenbestandteilen,

enthält, wobei die pulverförmige Zusammensetzung außerdem (C) mindestens ein Polygalactomannan oder dessen Derivat enthält.The present invention thus relates to a powdery composition which

• (A) Plantago seeds (Plantaginis ovatae semen) and / or (A ') plantago seed shells; and
• (B) at least one anthranoide compound, in particular at least one sennoside, preferably in the form of anthranoid-containing, in particular sennosid-containing plant parts or plant constituents,

contains, wherein the powdered composition also contains (C) at least one polygalactomannan or its derivative.

There the at least one anthranoic compound, in particular the sennoside, preferably in the form of an anthranoid or sennoside-containing plant part or plant component (eg fruits or fruit pods / pods or leaflets of senna plants) is generally a complex Mixture of different anthranoider compounds or sennosides in the composition of the invention in front.

Because The Applicant has surprisingly found out that the Polygalactomannan or its derivative as a (co) stabilizer with respect to the previously defined powdered composition, if these are in aqueous suspension is brought; due to the presence of the polygalactomannan-based or -derivatisierten polysaccharide is thus the powdered composition according to the present invention improves suspendable in water or dispersible and remains an aqueous suspension of the powdery composition of the invention via a longer Period stable and thus drinkable, d. H. the suspension gels not prematurely and leads also to no premature phase separation. In addition, the polygalactomannan has but also in an unexpected way the function, in addition, too the effect of the rest Ingredients, in particular the plantago seeds and, where appropriate plantation seed shells, because it is itself a certain Source ability having; it acts synergistically in an unexpected way the other components of the powdered composition together and thus increases their pharmacological activity. After all supports the polygalactomannan or its derivative surprisingly also the Processability of the composition of the invention to a finely divided, free-flowing Powder which is suspendable or dispersible in water.

Advantageously, the polygalactomannan or its derivative is in the form of compounds from the group of guaran (synonymously also called guar gum or Cyamopsis gum) or guar derivatives, in particular partially or completely esterified and / or etherified guar derivatives, in particular guar gum. Ethern added, such as carboxymethyl and hydroxyalkyl derivatives and cationically modified products from the reaction of guar flour with monochloroacetic acid, ethylene or propylene oxide and 2,3-epoxypropyltrimethylammonium chloride in the presence of alkali.

Especially the polygalactomannan or its derivative is preferably in the form of Guar gum and / or guar gum, preferably guar gum. The guar flour and / or The guar gum not only acts as a (co) stabilizer in a special way the composition of the invention in aqueous suspension, but it supports also the formulation of a particularly finely divided powder and increases due to its own swelling ability in a special way the laxative Effect of the rest Ingredients, so acts with the other ingredients in synergistic Way together.

Guar flour is the name for a gray-white powder, which is produced by grinding the endosperm of the endemic plant originally from the Indian and Pakistani areas, now cultivated in other countries, for example in the southern United States, to the legume family (Cyamopsis tetragonoloba) is obtained. The main constituent of the guar flour is guar gum (guar gum, Cyamopsis gum) with up to about 85% by weight of the dry matter; Secondary components are proteins, lipids and cellulose. Guaran itself is a polygalacto mannan, ie a polysaccharide whose linear chain is composed of unsubstituted and substituted in the C ₆ position with a galactose residue mannose units in β-D (1 → 4) -linkage. Guaran itself has an extremely high thickening effect (viscosity of a 1.5 wt .-% aqueous solution to 15,000 mPa · s). The solutions are heavily clouded by insoluble secondary constituents of the guar flour. The solubility can be significantly improved by the derivatization, in particular by etherification or esterification of the guar flour. For further details, reference may be made to Römpp Chemielexikon, 10th edition, volume 2, 1997, pages 1622/1623, keywords "Guar-flour" and "guar derivatives", Georg Thieme Verlag Stuttgart / New York, and the references cited therein , the contents of which are incorporated by reference.

Under Guar derivatives are understood according to the invention in particular derivatives of Guar flour. Guaran, the main constituent of guar flour, settles as polysaccharide in different ways, for example by full or partial esterification and / or etherification of its hydroxy groups, derivatized. In particular, have gained technical importance the guar ethers, especially the carboxymethyl and hydroxyalkyl derivatives as well as cationically modified products used in the implementation of Guar flour with monochloroacetic acid, Ethylene or propylene oxide and 2,3-epoxypropyltrimethylammonium chloride incurred in the presence of alkali. The guar derivatives, in particular Guar ethers are distinguished the unmodified guar flour by a faster and better solubility in water and an elevated Transparency of the aqueous solution.

Especially it is advantageous if the pulverulent composition according to the invention also (D) at least one silica or their derivative. The silicic acid supports on the one hand the flowability the powdery one Composition and facilitates their processability to a finely divided powder, d. H. has a positive or accelerating effect on the production process, by acting as a flow mediator acts. On the other hand, the silica (co) stabilizing in an aqueous suspension the composition of the invention and thus supports the effect of the polygalactomannan or its derivative, in particular by synergistic interaction with the polygalactomannan or his derivative. After all Adsorbs the silica any moisture that may occur during processing or storage and thus acts as a preventative of clumping Medium.

Particularly suitable silica has been a highly disperse, preferably fumed silica, preferably having an SiO ₂ content of 95% and more, in particular of 99% or more. An example of a suitable silica according to the invention is the product of Aerosil ^® from Degussa. this is a fumed silica of more than 99.8% SiO ₂ content, produced by hydrolysis of silicon tetrachloride in an oxyhydrogen flame (2 H ₂ + O ₂ + SiCl ₄ .fwdarw.SiO ₂ + 4 HCl, flame hydrolysis). Part of the silica or its derivative may be replaced by maltodextrin.

What the one or more used according to the invention As far as sennosides are concerned, these are generally Hydroxyanthracene derivatives, in particular 1,8-Dihydroxyanthronderivate. In general, a complex mixture of different sennosides put to use.

wobei in der allgemeinen Formel (I)

• • der Rest R¹ Wasserstoff oder eine Gruppe -CO-CO₂H darstellt,
• • der Rest R² eine Gruppe -CO₂H oder -CH₂OH darstellt, jedoch mit der Maßgabe, daß, wenn R¹ eine Gruppe -CO-CO₂H bezeichnet, R² eine Gruppe -CO₂H darstellt,
• • die mit dem Zeichen "*" gekennzeichneten Kohlenstoffatome in 9- und 9'-Position des Anthrongerüstes Chiralitätszentren darstellen,

sowie Mischungen und/oder Stereoisomeren, insbesondere Enantiomeren und/oder Diastereoisomeren, und/oder Derivaten der vorgenannten Verbindungen.In particular, the sennoside used according to the invention is selected from the group of the following compounds of the general formula (I):

in the general formula (I)

• The radical R ^{1 represents} hydrogen or a group -CO-CO ₂ H,
• The radical R ^{2 represents} a group -CO ₂ H or -CH ₂ OH, but with the proviso that when R ¹ denotes a group -CO-CO ₂ H, R ^{2 represents} a group -CO ₂ H,
• The carbon atoms in the 9 and 9 position of the anthrone skeleton marked with the symbol "*" represent chiral centers,

and mixtures and / or stereoisomers, in particular enantiomers and / or diastereoisomers, and / or derivatives of the abovementioned compounds.

sowie Mischungen und/oder Derivaten der vorgenannten Verbindungen.Preferably, the sennoside is selected from the group of the following compounds of general formula (I):

and mixtures and / or derivatives of the abovementioned compounds.

advantageously, The sennosides are in the form of fruits (Fructus), in particular z. B. fruit pods, and / or pinnate leaves (Folia), preferably fruits or fruit pods, added by senna plants. The Tinnevelly senna plants are preferred and the Alexandrian senna plant, especially preferred are the Tinnevelly-senna plant, preferably in dried and ground powder to fine powdered form.

All it is particularly preferred to use the sennosides in the form of fruits (Fructus) (in particular, for example, fruit pods / pods) and / or pinnate leaves (Foliae), preferably fruits, the Tinnevelly senna plant (Senna angustifolia, Cassia angustifolia) one.

The Tinnevelly senna plant (Senna angustifolia, Cassia angustifolia) is a shrub up to two meters high, which is native to the countries bordering the Red Sea. However, it is grown to a greater extent in India in field crops, often alternating with rice. This shrub is grown not only around the city of Tinnevelly (drug designation), but also near Bombay and Madras. The Alexandrian senna plant is a subshrub native to North Africa and the middle Nile, up to 60 cm high, which is cultivated in Egypt and Sudan. It owes its name to the former export port of Alexandria, and is therefore also referred to as Khartoum-Senna. Fruits and leaflets of the senna plants contain a complex sennoside mixture, which has laxative effects. For further details reference can be made to German Pharmacopoeia, 10th edition (DAB 10), German pharmacist Verlag Stuttgart, 1991, and the commentary to the DAB 10th edition, 1st Lfg., 1993, T 54, pages 1 to 5, on the Dissertationsschrift of the Gerhard-Mercator-University Duisburg "NIR spectrometry as a method of the quantitative analysis of synthetic and vegetable active substances in tablets and granulates" of Dr. med. Frank Zeyen from 2000 as well as the WHO Monographs on Selected Medicinal Plants "Folium Sennae" (http://www.who.int/medicines/library/trm/medicinalplants/pdf/241to249.pdf).

When Anthranoidhaltige plants (existing) parts according to the invention but also those of other anthraquinone-containing drugs with a laxative effect be used, for. B. Rheum palmatum and Rheum officinale (medicinal rhubarb, Root), Rhamnus frangula (buckthorn, bark), Rhamnus purshiana (American Buckthorn, bark), Aloe barbadensis, Aloe ferox (Curacao or Cape Aloe, thickened juice from leaves), Rhamnus catharicus (buckthorn, berries) etc., just to name a few.

According to one particular embodiment The present invention concerns the anthranoids or sennosides, in particular the senna plant particles (fruits or fruit pods and / or Leaflets) in one of the plantation seeds, especially the mucilage plantation seed, at least partially or completely wrapped in the composition of the invention in front. In this way, the composition according to the invention is additionally stabilized.

The Quantities of the individual components are not critical and can vary widely. For example, the salary on plantago seeds in the range of 30 to 80 wt .-%, in particular 40 to 70 wt.%, Preferably 45 to 55 wt .-%, vary. The content of possibly existing Plantagosamenschalen can also in vary widely, namely in the range of 0 to 5 wt .-%, in particular 1 to 4 wt .-%, preferably 1.5 to 3 wt .-%. The content of sennoside (s) can also in wide Ranges vary; in general, it is 0.05 to 1.0 wt .-%, in particular from 0.08 to 0.6% by weight, preferably from 0.1 to 0.5% by weight. The content of senna plant (s), in particular senna fruits or Sennafruchthülsen, may be in the range from 5 to 25% by weight, in particular 7.5 to 15% by weight, preferably 10 to 13 wt.%, vary. The content of polygalactomannan (s), in particular guar and / or guar derivatives (in particular guar flour or guar gum) may range from 5 to 20% by weight, in particular 7 to 15 wt .-%, preferably 7.5 to 12 wt .-%, particularly preferably 8.0 to 10 wt.%, Vary. The content of any existing silica or their derivatives may range from 0 to 5 wt .-%, in particular 0.01 to 2 wt .-%, preferably 0.02 to 1 wt .-%, particularly preferably 0.05 to 0.1 wt .-%, vary. All the above weight percentages are each based on the dry weight of the total composition according to the invention based.

to Improvement of processability and / or appearance and / or the organoleptic properties of the composition of the invention Furthermore be added further additives or additives, for example Dyes (eg natural or nature-identical dyes), flavoring agents, flavor enhancers, flavorings, (Co) stabilizers, fillers, Processing aids, sweeteners etc. and mixtures of the aforementioned compounds.

A pulverulent composition which is preferred according to the invention has the following formulation, the quantities given being based on the dry weight of the total composition: parts by weight • (A) Plantago seeds: 30 to 80, especially 40 to 70, preferably 45 to 55 • (A ') plantation seed shells: 0 to 5, in particular 1 to 4, preferably 1.5 to 3 • (B) Tinnevelly Senna fruits: 5 to 25, in particular 7.5 to 15, preferably 10 to 13 (corresponding to sennosides 0.05 to 1.0, in particular 0.08 to 0.6, preferably 0.1 to 0.5 parts by weight) • (C) Guar Flour and / or Guar Gum: 5 to 20, in particular 7 to 15, preferably 7.5 to 12, particularly preferably 8.0 to 10 • (D) Silica: 0 to 5, in particular 0.01 to 2, preferably 0.02 to 1, particularly preferably 0.05 to 1 • (E) flavorings and colors: 0 to 60, especially 20 to 50, preferably 35 to 45

The Processability of the individual active ingredients to a stable, finely divided, homogeneous powder mixture is the applicant's studies according to only by the incorporation of the polygalactomannan used according to the invention or its derivative, in particular guar gum and / or guar gum, optionally together with a finely divided silica, possible where the polygalactomannan or its derivative, optionally together with a finely divided silica, additionally stabilizing with respect to an aqueous suspension of the powder composition of the invention acts, which makes the oral intake much easier.

Of the Main mass fraction of the composition according to the invention, in particular more than 60 wt .-%, in particular more than 70 wt .-%, preferably before more than 75 wt .-%, has grain sizes in the range of 125 to 250 μm on.

• • mehr als 95 Gew.-%, insbesondere mehr als 99 Gew.-%, feiner als 500 μm;
• • mehr als 70 Gew.-%, insbesondere mehr als 75 Gew.-%, feiner als 250 μm;
• • mehr als 10 Gew.-%, insbesondere mehr als 15 Gew.-%, feiner als 125 μm.

In general, the composition according to the invention has the following particle size distribution (sieve analysis according to DIN ISO 3310-1):

• More than 95% by weight, in particular more than 99% by weight, finer than 500 μm;
• More than 70% by weight, in particular more than 75% by weight, finer than 250 μm;
• More than 10% by weight, in particular more than 15% by weight, finer than 125 μm.

In Advantageously, the individual components of the composition according to the invention are in an intimate, preferably homogeneous mixture, d. H. the individual components are intimately, preferably homogeneously, with each other processed or mixed.

The Composition according to the invention is extraordinary swellable. This stimulates intestinal activity through physical stimuli. The swelling number (according to DAB 8, German Pharmacopoeia, 8th Edition 1978, official issue, German Pharmacist Verlag Stuttgart / Govi-Verlag GmbH Frankfurt, pages 24 ff.) Is in particular at least 5.0, especially at least 6.0, preferably at least 7.0, especially preferably at least 7.5, most preferably at least 8.0 and more.

As previously described if necessary, the particles of the ground senna fruits from one Protective layer of the mucilages of the plantago seed meal products be surrounded. By this wrapping the sennosides are largely protected from unwanted changes and delayed their release, so that one even longer lasting, retarding and milder effect can be achieved.

Tries, which the Applicant has carried out with the composition according to the invention a delayed one Release of the sennosides from the laxative according to the invention, wherein the retarded However, release of sennosides by no means to a complete blockage the active ingredients leads, but rather to a desired, for a long time practically complete Release. Thus, the Sennosides completely to come into effect.

The powdery composition according to the invention is thus excellently suitable as a laxative (laxative).

Due to the fact that the composition according to the invention is in the form of a finely divided powder, it can be particularly well incorporated or dispersed in water for oral administration and remains very long drinkable after stirring in water, ie in contrast to the products In the prior art, no rapid phase separation takes place. In comparison, prior art products gel after only a few minutes and form a thick, non-drippable lump on the surface.

Furthermore has the composition according to the invention a lifelike appearance and a true-to-life taste.

The Composition according to the invention shows a good laxative Effect and is characterized by a gentle and when used as intended Of unpleasant side effects largely free effect especially through a good compatibility out. Thus, it is suitable for supporting the intestinal activity especially in hemorrhoids or fissure patients and even after a surgical procedure equally can the composition of the invention for clinical regulation for immobilized Patients, d. H. especially patients who are tied to the bed are about longer Time is applied and is also without hesitation during the Pregnancy administrable. The composition of the invention can thus be used in all diseases in which a slight defecation with soft chair desired is (eg in anal fissures, in hemorrhoids, after rectal-anal surgical procedures, for cleaning the bowel before X-ray examinations as well as before and after abdominal surgery or Gastrointestinal tract, in constipations etc.).

For example, the composition of the invention is also particularly suitable for the treatment of patients with drug-induced constipation, z. B. in the treatment with the commonly used loperamide ^® . A study by Ewe et al. (Pharmacology 1993, 47, Suppl. 1, pages 242 to 248) demonstrates the shortened intestinal passage with simultaneous use of Loperamide ^® and sennoside-containing preparations. It has now surprisingly been found that, inter alia, due to the "liquid" administration of the composition according to the invention in the form of an aqueous suspension and the finely divided particles, this effect is better than in the conventional preparations, since the liquid application in the form of an aqueous suspension of very fine particles at temporary restriction of passage from the stomach into the intestine is still possible for solid particulate particles in the context of the "liquid" preparation (aqueous suspension). Consequently, the composition according to the invention is also suitable for facilitating intestinal transit and defecation, in particular as a relief of the side effects, in therapy with medicaments which - although only as unwanted side effects - cause constipation.

toxicity studies prove that the Composition according to the invention neither acute nor chronic if used properly toxicity hazard brings with it. Also, no choleretic effect was observed. There were no incompatibilities detected.

Consequently the powdery composition according to the invention is suitable in an excellent way as an efficient laxative, which at the intended oral Ingestion with no unwanted side effects, especially obstruction of the esophagus or the gastrointestinal tract leads.

The Composition according to the invention thus effectively combines the physical effect of Plantago seeds due to source properties and pharmacological stimulating active principle of the ingredients of the senna fruits, the Sennoside, to achieve an improved overall effect in this way.

by virtue of their powdered Characteristics of the composition according to the invention for oral use suspended in water. The easy suspendability and subsequent stabilization of the suspension thus prepared is characterized by the polygalactomannan-based or -derivatized polysaccharide, in particular in the form of guar gum and / or guar gum, optionally together with the silicic acid, So that the oral intake takes place automatically with sufficient amounts of water, since it is an aqueous suspension supplied becomes.

advantageously, is the composition of the invention For this purpose already packed in sachets, each of which contained amount of inventive composition preferably corresponds to a single dose (eg, in each case 5 to 10 g of the composition according to the invention or z. B. such amounts of composition, the 5 to 20 mg sennosides correspond). To the composition of the invention sufficient to protect, the sachets are preferably at least substantially airtight and / or at least substantially waterproof (eg. by welding or sticking). Advantageously, the sachets protect the Composition according to the invention also against exposure to light, in particular UV light.

The Composition according to the invention is generally taken orally, especially in amounts of 1 to 50 g, in particular 1 to 20 g, preferably 5 to 10 g of the Composition by diem. A daily dose of 60 mg, preferably 30 mg sennoside (s) advantageously not exceeded become. On the other hand, to achieve a sufficient laxative effect, should the composition according to the invention but administered in such amounts that the daily dose of sennoside (s) at least 5 mg, especially at least 10 mg, preferably at least 15 mg. It may be advantageous to set the total daily amount to several Divide single doses, z. B. to two to three single doses each 5 to 25 g, especially 5 to 20 g, preferably, 5 to 10 g of the Composition per single dose or with 5 to 20 mg, in particular 5 to 10 mg sennoside (s).

The oral intake should be accompanied by sufficient intake of water, on the one hand to ensure an efficient effect (= swelling) and on the other hand undesirable Side effects (such as occlusion of the esophagus) too avoid; this is generally ensured by the oral Ingestion in the form of an aqueous suspension the powder composition of the invention takes place, since the composition of the invention due to Otherwise it is not possible to take the finely divided powder form. In general should be taken at least 40 ml of water per 1 g when taken orally the composition of the invention be provided, wherein the inventive composition before oral Ingestion in the water is brought into suspension and then in Form of an aqueous suspension is administered orally.

The Preparation of the powdery composition according to the invention can be done in a conventional manner. The production takes place in general, according to the usual Manufacturing process for Powder compositions. This can be done, for example, by that the individual constituents (if appropriate after drying) initially fine are ground, the degree of grinding targeted to the desired granulometry the final composition can be adjusted, and then a intimate homogeneous mixture of the individual components in the desired proportions will be produced. The grinding of the individual components can but alternatively also done only in the state of the mixture.

Further The present invention relates to the use of the composition according to the invention for Preparation of a pharmaceutical or pharmaceutical composition to promote and / or relief and / or regulation of defecation or intestinal activity. Thus, the present invention relates to the use of the composition of the invention for prophylactic and / or curative (therapeutic) treatment the aforementioned disease states, where a slight defecation with soft chair desired is.

Finally, concerns the present invention also provides a therapeutic method for Promotion and / or Relief and / or regulation of bowel movement or intestinal activity (eg for the treatment of constipation or constipation) from other disorders where a slight defecation with soft chair desired is as described above), wherein the above-described inventive composition in therapeutically effective amounts, generally by oral administration, preferably oral administration of an aqueous suspension the powdery one Composition according to the present invention.

Further Configurations, modifications and variations as well as advantages of present invention are for the person skilled in the art readily discernible when reading the description and realizable without him the scope of the present invention leaves. The following embodiments are merely illustrative of the present invention, but without restricting it to this.

embodiments

example 1

A Composition according to the invention and two comparative products of the prior art are in a transferred aqueous suspension. To For this purpose, each 6 g of the compositions in each about 240 ml of tap water stirred.

The composition according to the invention is a finely divided powder (more than 70% by weight of the particles with average diameters in the range from 125 to 250 μm), which contains 52% by weight of plantation seed, 2.2% by weight. Plantago seed shells, 12.3% by weight Tinnevelly senna fruits (corresponding to about 0.3% by weight sennosides), 8.3% by weight guar gum, 0.07% by weight finely divided silica, 0.03% by weight .-% maltodextrins and 25.1 wt .-% of other ingredients (natural flavoring, coloring, flavoring and sweetening substances) contains.

The first comparative composition is a composition of 52 % By weight of plantation seed, 2.2% by weight of plantago seed husks, 10 to 13.2 Wt% Tinnevelly senna fruits (corresponding to about 0.3% by weight of sennosides) and from 32.6 to 35.8% by weight other ingredients (talc, gum arabic, iron oxides, paraffin, Flavorings, sucrose), but is free of guar gum and silica.

The second comparative composition is a commercial product based of Indian psyllium husks (psyllium), which next to it Ingredients (including natural and artificial Colorants, flavorings, flavorings and sweeteners, Citric acid, Iron oxides, calcium), but is free of sennosides and also no guar gum and no silica contains.

To Suspension of the three compositions in water remains only the composition of the invention over more stable as a quarter of an hour while the two comparative suspensions after only a few minutes Phase separation show (sedimentation of solids). The second Comparative composition, which also by their threadbare taste and the artificial one Appearance detrimental, also gels after fifteen minutes and forms a thick, undrinkable lumps on the surface while the suspension of the composition according to the invention even after an hour remains drinkable.

Also in their laxative effect, the three compositions differ significant: While the second comparison composition based on Indian psyllium husk (Psyllium) only a moderately laxative effect shows that in more severe cases of constipations is not always sufficient, shows the first comparative composition a much better laxative Effect due to the combination of physical effect of Plantago seeds / plantago seed shells as a result of swelling on the one hand and pharmacologically stimulating effect of sennosides on the other hand. This combination effect is in the composition of the invention even increased due to the synergistic mode of action of the guar gum.

Example 2

A Composition according to the invention was prepared as follows:

Starting mixture:

Sieving and mixing:

The individual components were - respectively in finely ground form - by means of Vacuum in a double cone mixer (two-sided pointed mixer) introduced with 2,500 l capacity. Lumps or larger components were separated during loading of the mixer via a 3-mm sieve. The materials were then run at a speed for 30 minutes mixed at 16 rpm. Subsequently, the homogenized, mixed product down in two polypropylene bigbags with Polyethylene inner bags equipped were filled. This resulted in a mixture or composition according to the invention.

Sachets filling and Pack process:

A machine for the simultaneous filling of four Sachets (sachets) was using Vacuum supplied the previously prepared powder product. The individual sachets were each loaded with a predetermined dose of 6 g via a screw dispenser. The batch no. and the expiration date were stamped on the fold of the sachets. Subsequently, the sachets were welded over welding or heating jaws, so that the contents were packed air- and waterproof. The loaded and sealed sachets were then stacked in pairs to a total of 20 sachets and transported to a cartoning or packaging machine, where they were packed together with the leaflet in a box, with the respective batch no. and the expiration date was printed. The units were then checked for correct weight and any deviating units were discarded. A fixed number of loaded cartons can then be further packed into large packages.

Claims (18)

Powdered composition containing (A) Plantago seeds (Plantaginis ovatae Semen) and / or (A ') Plantago seed shells; and (B) at least one anthranoide compound, in particular at least one sennoside, preferably in the form of anthranoid-containing, in particular sennoside-containing plant parts or plant components, characterized in that the composition also contains (C) at least one polygalactomannan or its derivative. Composition according to Claim 1, characterized in that it additionally contains (D) at least one silica or its derivative, in particular a highly dispersed, preferably pyrogenic silica, preferably having an SiO ₂ content of 95% and more, in particular of 99% and more, in particular wherein a part of the silica or its derivative may be replaced by a maltodextrin. Composition according to Claim 1 or 2, characterized that this Polygalactomannan or its derivatives are selected from the group of Guaran (guar gum, Cyamopsis gum) and guar derivatives, in particular partial or complete esterified and / or etherified guar derivatives, in particular guareths, such as carboyxymethyl and hydroxyalkyl derivatives and cationically modified Products from the conversion of guar flour with monochloroacetic acid, ethylene or propylene oxide and 2,3-epoxypropyltrimethylammonium chloride in Presence of alkali. Composition according to one or more of the preceding Claims, characterized in that the Polygalactomannan or its derivative in the form of guar flour and / or Guar gum is added. Composition according to one or more of the preceding Claims, characterized in that the Composition a mixture of different anthranoider compounds, especially sennosides. Composition according to one or more of the preceding claims, characterized in that the sennoside is a Hydroxyanthracenderivat, in particular a 1,8-Dihydroxanthronderivat, and / or that the sennoside is selected from the group of the following compounds of general formula (I):

wherein in the general formula (I) • the radical R ^{1 represents} hydrogen or a group -CO-CO ₂ H, • the radical R ^{2 represents} a group -CO ₂ H or -CH ₂ OH, but with the proviso that when R ¹ denotes a group -CO-CO ₂ H, R ^{2 represents} a group -CO ₂ H, • the carbon atoms labeled with the symbol "*" in the 9 and 9 'positions of the anthrone skeleton represent chiral centers, and mixtures and / or stereoisomers, in particular enantiomers and / or diastereoisomers, and / or derivatives of the abovementioned compounds. Composition according to Claim 6, characterized in that the sennoside is chosen from the group of the following compounds of general formula (I):

Composition according to one or more of the preceding Claims, characterized in that the or the sennoside (s) in the form of fruits (Fructus), in particular Fruit pods, and / or pinnate leaves (Folia), preferably fruits, especially fruit pods, of senna plants, in particular the alexandrine and / or the Tinnevelly senna plant, preferably the Tinnevelly senna plant, preferably in a dried and finely ground powdered form. Composition according to Claim 8, characterized that this or the sennosides in the form of fruits and / or pinnules, preferably fruits, especially fruit pods, the Tinnevelly senna plant (Senna angustifolia, Cassia angustifolia) are added. Composition according to one or more of the preceding Claims, characterized in that the or the sennosides, in particular the senna plant particles, of the plantago seed, in particular the mucilage of the plantago seeds, at least partially or completely wrapped are. Composition according to one or more of the preceding claims, characterized by a content of plantago seeds of 30 to 80 wt .-%, in particular 40 to 70 wt .-%, preferably 45 to 55 wt .-%, and / or by a content of Plantagosamenschalen from 0 to 5 wt .-%, in particular 1 to 4 wt .-%, preferably 1.5 to 3 wt .-%, and / or by a content of sennoside (s) from 0.05 to 1.0 wt .-%, in particular 0.08 to 0.6 Wt .-%, preferably 0.1 to 0.5 wt .-%, and / or by a content of Sennapflanze (s), in particular Senna fruits or Sennafruchthülsen, from 5 to 25 wt .-%, in particular 7.5 to 15 Wt .-%, preferably 10 to 13 wt .-%, and / or by a content of Polygalactomannan (s), in particular guar gum and / or guar derivatives of 5 to 20 wt .-%, in particular 7 to 15 wt .-%, preferably 7.5 to 12 wt .-%, particularly preferably 8.0 to 10 wt .-%, and / or a content of silica or its derivatives of 0 to 5 wt .-%, in particular 0.01 to 2 wt. -%, preferably 0.02 to 1 wt .-%, particularly preferably 0.05 to 0.1 wt .-%, wherein all abovementioned Gewich percentages are each based on the dry weight of the total composition. Composition according to one of the preceding claims, characterized characterized in that they Furthermore contains at least one further additive and / or additive, in particular selected from the group of dyes such as natural or nature-identical Dyes, flavorings, flavor enhancers and flavorings, stabilizers and (co) stabilizers, fillers and processing aids, as well as mixtures of the aforementioned Links. Composition according to one or more of the preceding claims, characterized by the following formulation, wherein the quantities are in each case based on the dry weight of the total composition: parts by weight • (A) Plantago seeds: 30 to 80, especially 40 to 70, preferably 45 to 55 • (A ') plantation seed shells: 0 to 5, in particular 1 to 4, preferably 1.5 to 3 • (B) Tinnevelly Senna fruits: 5 to 25, in particular 7.5 to 15, preferably 10 to 13 (corresponding to sennosides 0.05 to 1.0, in particular 0.08 to 0.6, preferably 0.1 to 0.5 parts by weight) • (C) Guar Flour and / or Guar Gum: 5 to 20, in particular 7 to 15, preferably 7.5 to 12, particularly preferably 8.0 to 10 • (D) Silica: 0 to 5, in particular 0.01 to 2, preferably 0.02 to 1, particularly preferably 0.05 to 1 • (E) flavorings and colors: 0 to 60, especially 20 to 50, preferably 35 to 45 Composition according to one or more of the preceding Claims, characterized, that the Composition having the following particle size distribution: • more than 95 wt .-%, in particular more than 99 wt .-%, finer than 500 microns; • more than 70 wt .-%, in particular more than 75 wt .-%, finer than 250 microns; • more than 10% by weight, in particular more than 15% by weight, finer than 125 μm, in which all aforementioned weight data in each case on the dry weight the total composition, and / or that the main mass fraction the composition, in particular more than 60 wt .-%, in particular more than 70 wt .-%, preferably more than 75 wt .-%, grain sizes in the range from 125 to 250 μm exhibit. Composition according to claims 1 to 14 for use as laxative (laxative). Use of the composition according to claims 1 to 14 for the manufacture of a pharmaceutical or pharmaceutical Composition for promotion and / or relief and / or regulation of defecation and / or intestinal activity. Use according to claim 16 for prophylactic or curative treatment of diseases in which a slight defecation with soft chair desired is, especially hemorrhoidal diseases, conditions after rectal-anal surgery and before and after surgery Surgery of the abdomen as well as constipation, or for relief intestinal transit and defecation, especially as a relief of side effects, in therapy with Medications that cause constipation. Composition according to claims 15 and 16 or use according to claim 17, characterized in that the composition is administered orally is taken, preferably as an aqueous suspension, in particular in daily doses of a total of 1 to 50 g, in particular 1 to 20 g, preferably 5 to 10 g, of the composition.