Compositions for treatment of gastroesophageal reflux disease (gerd)

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the pharmaceutical industry, in particular to a peroral pharmaceutical composition, which contains polysaccharides from platyclades of Opuntia Ficus Indica, an extract of Olea Europeae leaves, alginate and sodium bicarbonate in a specified ratio. Components of the composition described above act with respect to reduction of gastroesophageal reflux.

EFFECT: peroral pharmaceutical composition is intended for the prevention and treatment of gastroesophageal reflux and GERD.

4 cl, 9 tbl, 6 dwg

 

The present invention relates to pharmaceutical compositions, nutraceutical, diet food and compositions for medical devices for oral administration based on polysaccharides from cladode Opuntia Ficus Indica, which are intended for the prevention or treatment of GERD (gastroesophageal reflux disease), gastroesofagico and related disorders, including dyspepsia, esophagitis, a tumor of the esophagus, gastro-intestinal disorders, chronic pharyngitis, Barret's esophagus, adenocarcinoma of the esophagus, GERD-associated lung, preferably in combination with different active substances used to treat the same diseases. These compositions, which was found to have a synergistic effect, allow the use of lower effective doses of active substances, improving their therapeutic index.

The level of technology

Esophageal reflux is a physiological condition that occurs, particularly in newborns, but when he overcomes the protective mechanism of the mucosa of the esophagus can occur diseases such as GERD.

GERD is a common gastrointestinal disease resulting from gastric or enteric reflux into the esophagus, causing reflux esophagitis, very common the United disease with typical inflammation and lesions (erosions and small ulcers) of the mucous membrane of the esophagus due to reflux of gastric or enteric juice into the esophagus.

In the case of GERD reflux causes symptoms such as esophagitis, but in the absence of lesions.

The pressure gradient between the esophagus and stomach usually prevents the back-flow of stomach contents into the esophagus.

Anatomical structure, ensuring the preservation of the pressure gradient, is the lower esophageal sphincter (LES), the muscle ring at the junction of the esophagus with the stomach, which relaxes during swallowing.

Under physiological conditions, when in the stomach substance (acid up into the esophagus, peristalsis of the esophagus (the muscular contractions of the esophagus) pushes them back into the stomach, while the remains of the acid neutralized swallowed with saliva.

GERD is characterized by the same pressure in the esophagus and stomach. This condition occurs due to:

- lower the tone or no tone LES;

- relaxation of the LES in the absence of swallowing;

- insufficient neutralization of acid caused due to abnormal motility of the esophagus;

- abnormal function of the cardia, the valve between the stomach and esophagus, which suppresses the reflux of stomach contents into the esophagus under physiological conditions.

Incomplete closure of the cardia may occur for various reasons, such as obesity, Smoking, multiple pregnancy, severe physical effort, harmacological treatment or hiatal hernia.

Reflux esophagitis severe can lead to a narrowing of the esophagus (stenosis) after treatment of esophagitis or precancerous lesions (”Barret's esophagus, adenocarcinoma of the esophagus), causing metaplasia of the mucous membrane of the esophagus, which is similar to the mucous membrane of the stomach or duodenum. Some of the subjects of this disease can be caused by other factors, such as reduced salivation, increased acidity, slow release of the stomach, bile salts or reflux of pancreatic enzymes.

Such diseases are characterized by heartburn (severe retrosternal burning, belching and regurgitation of food or acid in the mouth. These symptoms can be associated with abnormalities characteristic of the respiratory system (chronic cough, asthma, hoarseness, chronic laryngitis), teeth (loss of tooth enamel) or ears (ear pain).

GERD and reflux esophagitis, in the case of acid reflux, currently treated 1) proton pump inhibitors (PPI, for example, omeprazole, lanzoprazol), receptor antagonists N2(for example, cimetidine and ranitidine), which reduce the secretion of acid in the stomach and, therefore, reflux; 2) prokinetics agents (e.g. metoclopramide, domperidone, levosulpiride), which increase the tone of the valve is of the cardia and improve the release of the stomach; 3) antacids (e.g., bicarbonate, magnesium hydroxide and aluminum) and cytotoxicity means (for example, sukralfat)which reduces the acidity of the stomach and protects the lining of the esophagus.

Only a few drugs can be used in case of non-acidic (enteral) regurgitation.

Pharmacological treatment is supported by the principles of nutrition, body position and behaviors that help reduce or prevent these symptoms. For example, it is recommended to refrain from alcohol, rich food or fatty, spicy or irritating foods (mint, chocolate, coffee, tea) and sleep on the pillow, raised a few inches.

Pharmacological treatment has no effect on the cause of the disease (improper functioning of the cardia) and should be carried out over long periods of time (even lifelong), since almost all of the subjects, there is a recurrence of the disease in case of interruption of treatment.

A malfunctioning valve in the cardia can be adjusted by means of surgical treatment, which ensures complete recovery, but not good enough when performing the operation, you may experience new symptoms. In addition, surgical treatment is recommended for young actors with good state of health the conditions and subjects, need constant high doses of drugs. Recently Dr. Giga proposed a new surgical method to reduce GERD, but this method is not widespread (http://www.medwatchtoday.com/1113.htm).

There is no clear evidence for choosing one particular method of pharmacological treatment of GERD or reflux esophagitis: physicians tend to be driven by personal experience. Thus, the choice of treatment depends on your doctor's advice and is not objective, so the doctor may try several methods of pharmacological treatment before treatment is chosen that best matches the physiology of the subject.

Subjects with mild or intermittent symptoms antacids are recommended, prokinetics tools, alginates and in the most severe cases, antagonists of N2(anti-H2funds) and proton pump inhibitors (PPI).

In clinical practice, the use of increasing treatment methods are less effective when drugs gradually unite or replaced by more effective drugs with regard to symptoms and reduce treatment - when to begin treatment highly effective drugs, such as proton pump inhibitors, and still less the effect is active drugs (Bytzer P., Goals of therapy and guidelines for treatment success in symptomatic gastroesophageal reflux disease patients, Am. J. Gastroenterol. 2003, 98(3) Suppl: S31-S39).

PPI are very effective drugs, but their prolonged use (necessary in the case of treatment of reflux esophagitis) causes serious side effects associated with prolonged treatment with drugs of this class, such as an increased risk of hip fracture due to migratory absorption of calcium as a result of hypochlorhydria (Yang et al., Long term proton pomp inhibitor therapy and risk of hip fracture, JAMA 2006, 296(94):2947-2953), muscle diseases, as well as polymyositis and rhabdomyolysis (Clark et al., Myopathy including polymyositis: a likely class adverse effect of proton pump inhibitors?, Eur. J. Clin. Pharmacol., 2006, Jun, 62(6):473-479).

Information about the different side effects PPI was obtained on the basis of the data control studies of drugs, held in Spain between 1 January and 31 December 2004, which were presented in the publication Salquiero et al., Safety profile of proton pump inhibitors according to the spontaneous reports of suspected adverse reactions, Int. J. Clin. Pharmacol. Ther., 2006 Nov., 44(11):548-556.

Alginates having a physical mechanism of action (gelation and foaming at acid pH values in the stomach in the presence of HCO3-), are safer than the PPI, but not suitable for the treatment of non-esophageal reflux (Zentlin et al., An valuation of the antireflux properties of sodium alginate by means of combined multichannel intraluminal impedance and pH-metry, Aliment Oil Displayed Pure Pharmacol. Ther. 2005, 21:29-34).

Based on the foregoing and the fact that these diseases such as GERD, reflux esophagitis and related disorders (dyspepsia, esophagitis, a tumor of the esophagus, gastro-intestinal disorders, chronic pharyngitis, Barret's esophagus, adenocarcinoma of the esophagus, GERD-associated lung), are becoming more widespread, it is highly desirable to find a safe and effective way to prevent and treat such diseases, to avoid the simultaneous passage of a subject from different courses of treatment to achieve effective outcomes.

Description of the invention

The present invention relates to pharmaceutical compositions, nutraceutical, diet food and compositions for medical devices for oral administration capable of synergistically interact with the active substances used for the prevention and treatment of acidic and non-acidic oesophageal reflux disease and related clinical complications. These compositions contain a polysaccharide extract from cladode Opuntia Ficus Indica.

Opuntia Ficus Indica (Nopal) is a plant belonging to the family Cactaceae, which grows in Mexico and in the South-Western United States, but widespread even among breeding self-sowing plant the tee of the Mediterranean.

Fruits and young cladode (more tender) since ancient times and used for food (cladode used fresh, salted, pickled, candied, in the form of jam and even as fodder or for the preparation of alcoholic beverages.

In folk medicine the plant is used in different ways: fruit with astringent properties, sailors used to prevent scurvy due to the high content of vitamin C; young cladode used as cataplasm (heated in the oven) and as emollients; application of crushed mass cladode on wounds and ulcers of the skin is a great anti-inflammatory, necrotic and healing tool. This plant is still traditional Sicilian tool to be used in rural areas; the decoction of the flowers has diuretic properties.

Recently it was found that: 1) the fruits of Opuntia Ficus Indica have antioxidant properties (Tesoriere et al., Supplementation with cactus pear (Opuntia Ficus-indica) fruit decreases oxidative stress in healthy humans: a comparative study with vitamin C, Am. J. Clin. Nutr. 2004 Aug; 80(2); 391-395); 2) extract of Opuntia Ficus Indica is an effective treatment for a hangover (J. Wiese et al., Effect of Opuntia Ficus Indica on symptoms of the alcohol hangover, Arch Intern. Med. 2004 Jun 28; 164(12):1334-1340); 3) due to the high content of polysaccharides formed mainly by the polymer of galactose, arabinose and other sugars, cladode Opuntia has the ability to bind eaten fat and sugar (preventing their absorption), improving glycolipids currency and eliminating metabolic disorders; 4) mucilage and pectins of cladode Opuntia Ficus Indica protects the stomach in experimental animal models (Vazquez-Ramirez R. et al., Reversing gastric mucosal alterations during ethanol-induced chronic gastritis in rats by oral administration of Opuntia Ficus Indica mucilage, World J. Gastroenterol. 2006 Jul 21; 12(27):4318-4324). The Trombetta and others (Trombetta D. and al., Effects of polysaccharides from Opuntia Ficus Indica (L.) cladodes on the healing of dermal wounds in the rat, Phytomedicine, 13 (2006) 352-358) found that the polysaccharides extracted from cladode Opuntia Ficus Indica, have a healing effect on the skin at the level of the cell matrix.

Currently, quite unexpectedly it was found that polysaccharides extracted from cladode Opuntia Ficus Indica, have a synergistic effect with the substances used for the prevention and treatment of GERD and its complications caused by this disease.

Thus, the present invention relates to pharmaceutical compositions, nutraceutical, diet food and compositions for medical devices intended for oral administration, on the basis of polysaccharides extracted from cladode Opuntia Ficus Indica, which are preferably in combination with the active substances suitable for the prevention or treatment of diseases of the upper CTD is La gastro-intestinal tract and, in particular, GERD, reflux esophagitis and related disorders (dyspepsia, esophagitis, a tumor of the esophagus, gastro-intestinal disorders, chronic pharyngitis, Barret's esophagus, adenocarcinoma of the esophagus, GERD-associated lung). Active substances used in combination with polysaccharides extracted from cladode Opuntia Ficus Indica, include, but are not limited to, antacids, proton pump inhibitors, antagonists of N2, prokinetics tools, sodium bicarbonate, alginic acid or alginates, chitosans, aluminum hydroxide, calcium carbonate or magnesium, antioxidant and anti-inflammatory flavonoids extracted from plants and leaves of olives or kidney Capparis Spinosa, anthocyanoside of red oranges, black rice or other natural sources, and combinations thereof.

These compositions allow to reduce the dose of the pharmacologically active substances and are therapeutically safe, which is especially important when the treatment of children, pregnant women and the elderly, or in the case of prolonged co-treatment with nonsteroidal anti-inflammatory drugs (NSAID).

These tools allow you to conduct safe and effective local treatment of diseases of the gastrointestinal tract, such as dyspepsia, esophagitis, tumor food the ode, Barret's esophagus, adenocarcinoma of the esophagus, GERD-associated lung lesions, in combination with other methods of treatment of such diseases.

Therefore, the first object of the present invention are pharmaceutical compositions, nutraceutical, diet foods and compositions for medical devices intended for oral administration, which include polysaccharides from cladode Opuntia Ficus Indica, preferably in combination with the active substances used for the prevention or treatment of diseases of the upper section of the gastrointestinal tract, which are presented in the attached claims.

In accordance with the present invention, the term ”combination” refers to a physical or functional Association of extracts and active substances. In the first case (physical Association) active ingredients get in a single composition with carriers, fillers or other ingredients suitable for this purpose. In the second case (functional Association) active ingredients can be introduced in different compositions or different ways to achieve a combined therapeutic effect.

The second object of the present invention is the use of these compositions for the preparation of medicinal products intended for Leche is of GERD dyspepsia, esophagitis, tumors of the esophagus, gastro-intestinal disorders, chronic pharyngitis, Barret's esophagus, adenocarcinoma of the esophagus, GERD-associated pulmonary lesions, in combination with the active substances, which are known to prevent and treat the same disease, the effectiveness of these active substances is enhanced by the synergistic activity of polysaccharides cladode Opuntia Ficus Indica, and such active substances are preferably selected from anti-acid agents, proton pump inhibitors, antagonists of N2, prokinetics funds, sodium bicarbonate, alginic acid or alginates, chitosans, aluminum hydroxide or magnesium, calcium carbonate or magnesium, antioxidant and anti-inflammatory flavonoids extracted from plants and leaves of olives or kidney Capparis Spinosa, anthocyanosides of red oranges, black rice or other natural sources, and their combinations.

In accordance with the present invention polysaccharides cladode Opuntia Ficus Indica, which does not necessarily contain maltodextrins (up to 50%)can be obtained in the form of mucus, which can be selected in the extraction of cladode or process water at room temperature. Alternative cladode press under pressure, the resulting juice is centrifuged and the liquid supernat the NT is subjected to ultrafiltration, thus obtaining an aqueous solution with a high content of polysaccharides (molecular weight of more than 104Yes). Then an aqueous solution centrifuged and dried. The content of polysaccharides in the extract cladode Opuntia Ficus Indica is usually from 1 to 70 wt.%. Chemical structure and composition of the polysaccharide cladode Opuntia Ficus Indica were investigated and are described in the following publications (D. McGarvie, H. Parolis, Methylation analysis of the mucilage of Opuntia ficus indic. Carbohydrate Research, (1981) 88:305-314; M. S. Karawya et al. Mucilages and Pectines of Opuntia, Tamarindus and Cydonia. Planta Medica (1980) Supplement:68-75; M. E. Malainine et al. Structure and morphology of cladodes and spines of Opuntia ficus indica. Cellulose extraction and characterization. Carbohydrate polymers (2003) 51:77-83).

Mucus consists of the residues of 1,4-α-D-galactopyranoside acid and 1,2-β-L-rhamnopyranoside that are attached to short chains 1,6-β-D-galactopyranose in position 4 all residues rhamnopyranose. Most residues galactoside have the chain in position O-3 or O-4, which mainly consist of arabinofuranoside residues, arabinofuranoside-xylopyranoside (D. McGarbie, H. Parolis, Methylation analysis of the mucilage of Opuntia ficus indic. Carbohydrate Research, (1981) 88:305-314). The mucus contained in cladode Opuntia Ficus Indica, usually isolated by extraction (D. Trombetta et al., Effect of polysaccharides from Opuntia ficus-indica (L.) cladodes on the healing of dermal wounds in the rat. Phytomedicine (2006) 13:352-358) or processing water (R. Vazquez-Ramirez et al., Reversing gastric mucosal alterations during ethanol-induced chronic gastritis in rats by oral administration of Opuntia Ficus Indica mucilage. Wold J. Gastroenterol (2006) 12(27):4318-4324).

The compositions of the present invention can be solid or liquid suitable for oral administration, preferably in the form of oral solutions, oral suspensions, oral emulsions, tablets, powders and tablets for preparation according to the individual recipe. In this sense, the term ”medical device” means an active medical device (class I) according to the classification defined by Directive 93/42/EEC, Annex IX.

The compositions of the present invention may include preservatives, ionic and non-ionic buffers and additives normally used to obtain compositions for oral administration.

For liquid compositions for oral administration such as solutions, suspensions or emulsions, the solvent preferably use water or multicomponent aqueous solution suitable for oral administration.

Active substances suitable for the treatment or prevention of diseases of the upper section of the gastrointestinal tract, which can be used in combination with an extract of cladode Opuntia Ficus Indica of the present invention, include: (1) substances used to treat the same diseases, such as proton pump inhibitors, antagonists of N2, prokinetics tools, antaci the ing funds sodium bicarbonate, alginic acid or alginates, chitosan, sodium bicarbonate, and combinations thereof; 2) natural substances, such as antioxidant and anti-inflammatory flavonoids, isolated from plants, for example, kidney Capparis Spinosa, anthocyanoside of red oranges, black rice or other natural sources, and preferably extracts of the leaves of the olive tree; 3) combination of the substances referred to in paragraphs 1) and 2).

The leaves of Olea europeae can be extracted water or hydropyrolysis solvents (10-80% ethanol) at room temperature or when heated to 60-70°C, when processing in the microwave, ultrasound or by solvent extraction with overheating (O.H. Lee et al. Assessment of phenolics-enriched extract and fractions of olive leaves their antioxidant activities Bioresour Technol (2009)Epub ahead of print; Mylonaki S. et al. Optimisation of the extraction of olive (olea europaea) leaf phenolics using water/ethanol-based solvent systems and response surface methodology.Anal Bioanal Chem. (2008) 392(5):977-85; Japn-Lujan R, Luque de Castro MD. Small branches of olive tree: a source of biophenols complementary to olive leaves.J Agric Food Chem. (2007) 30; 55(11):4584-8; Vassiliki T Papoti, Maria Z. Tsimidou. Impact of sampling parameters on the radical scavening potential of olive (Olea europeae L.) leaves.J Agric Food Chem. 2009, 57, 3470-3477; Japn-Lujn R, Luque de Castro MD. The Superheated liquid extraction of oleuropein and related biophenols from olive leaves.J Chromatogr A. (2006) 1136(2):185-91). Water-alcohol extraction can be repeated several times to obtain a high content of befunolol. After the extraction is odny or water-alcohol solvent is removed in vacuum at 40°C. For further enrichment befinally, dry extract can be introduced into the polystyrene and subjected to elution with a solution of ethanol and water with a ratio of 50:50.

Leaf extract Olea europeae contains phenols (tyrosol, hydroxytyrosol and derivatives thereof), cinnamic acids, flavonoids (apigenin, luteolin and their glucoside derivatives, rutin, quercetin), lignans, secoiridoid (oleoresin, oleuropein and derivatives thereof, linolevuyu acid) and has the following polyphenolic profile: 2-40% flavonoids (apigenin, luteolin and their derivatives), 0.5 to 10% oleuropein, 1-30% hydroxytyrosol and their derivatives.

In this area known methods of producing pharmaceutical or food compositions. The content of polysaccharides extracted from Opuntia Ficus Indica, is preferably from 0.5 to 50% wt./wt. calculated on the total weight of the compositions; other active substances can be 1-30%.

Polysaccharides Opuntia Ficus Indica, which is currently used in foods are safe for certain categories of entities, such as the elderly, children or pregnant women.

The present invention further relates to the use of these compositions for the treatment and prevention of diseases of the upper section of the gastrointestinal tract by introducing the needy to the subject a therapeutically effective amount of polysaccharides Opunta, preferably in combination with the active substances used to treat or prevent those diseases.

Pathological conditions that can be successfully treated with compositions of the present invention, include gastroesophageal reflux, GERD, dyspepsia, esophagitis, a tumor of the esophagus, gastro-intestinal disorders, chronic pharyngitis, Barret's esophagus, adenocarcinoma of the esophagus, GERD-associated lung.

Brief description of drawings

Other features and advantages of the present invention will be more apparent from the following description of the invention and non-limiting examples with reference to the accompanying drawings, where:

- Figa: photograph of cladode and fruits of Opuntia Ficus Indica;

- Figure 2: model of mucoadhesive in vitro;

- Figure 3: comparison of the synergistic action of polysaccharides extracted from cladode Opuntia Ficus Indica, with sodium alginate in respect of the individual components in a model in vitro using epithelial cells of the buccal mucosa;

- Figure 4: mucoadhesive (percentage of inhibition of binding lectin after exposure) of each tested substance compared in figure 3.

- Figure 5: effect on peptic ulcer different substances or combination of substances tested in different experimental models of gastric ulcer in rats, caused by the Oh chemical method. Data are presented as mean value ± SD for 6 animals; in parentheses are the percentage of inhibition compared with the control group.

- 6: effects on esophageal ulcer different substances or combination of substances tested in the model of gastroesophageal reflux, caused by the surgical method. Data are presented as mean value ± SD for 6 animals; in parentheses are the percentage of inhibition compared with the control group.

The following tables provide non-limiting examples of compositions according to the present invention.

Table 1
Suspension 1 for oral administration
Components%
Polysaccharides from cladode Opuntia Ficus Indica2 g (1-20 g)
Waterto 100 ml

Table 2
Suspension 2 for oral administration
Components%
Sodium alginate 5 g
Sodium bicarbonate2.67 g
Polysaccharides from cladode Opuntia Ficus Indica2.0 g (1-20 g)
Waterto 100 ml

Table 3
Powder (sachet) 1 for oral administration
Components%
Sodium alginate10-20 g
Sodium bicarbonate5-10 g
Polysaccharides from cladode Opuntia Ficus Indica1-20 g

Table 4
Powder (sachet) 2 for oral administration
Components%
Sodium alginate10-20 g
Sodium bicarbonate5-10 g
The extract from the leaves of olives5-20 g
Polish the IDA from cladode Opuntia Ficus Indica 1-20 g

Table 5
Capsule 1
Componentsmg/capsule
Cimetidine200 mg
Polysaccharides from cladode Opuntia Ficus Indica100-200 mg
The extract from the leaves of olives100-200 mg
Lactoseto fill capsules

Table 6
Capsule 2
Componentsmg/capsule
Hydrochloride ranitidine84 mg
Alginic acid500.0 mg
Polysaccharides from cladode Opuntia Ficus Indica200 mg
The extract from the leaves of olives200 mg
Sodium bicarbonate165,25 mg
The magnesium stearate is 0.75 mg
Filler350 mg

Determining in vitro mucoadhesive polysaccharides from cladode Opuntia Ficus Indica, used separately and in combination with alginic acid on epithelial cells of the buccal mucosa

To assess mucoadhesive ability of polysaccharides from cladode Opuntia Ficus Indica was the analysis of mucoadhesive in vitro, described in the publication Patel (Patel D. and al., An in vitro mucosal model predictive of bioadhesive agents in the oral cavity. J. Control Release, 1999, 61(1-2):175-183), using the weighted epithelial cells from the buccal mucosa. When performing this analysis mucoadhesive (adhesive ability of the tested substances in the cells of the mucous membrane) is determined as the inhibition of binding lectin with membrane glycoprotein induced by masking the surface of the cell mucoadhesive substance.

Materials and methods

As a result of processing cells of the mucous membrane of the biotinylated lectin and streptomycinresistant the sample turns yellow; pre-treatment of mucosal cells mucoadhesive substance (30°C, for 15 minutes before treatment with lectin) allows you to mask the binding site of the lectin, which in turn decreases the intensity of the yellow color

Lectin is a protein found in some plants of the Leguminosae (Canavalia ensiformis), which has the ability to contact glycoside and mannoside residues of glycoproteins membrane; Biotin (vitamin H) binds to the lectin using streptavidine, which is added to the suspension of cells to create complex protein-glucose-lectin-Biotin-streptavidine.

Adding to the suspension of cells dihydrochloride o-phenylenediamine (o-pd) and hydrogen peroxide dihydrochloride o-phenylenediamine is oxidized by complex protein-glucose-lectin-Biotin-streptavidine with the formation of 2,3-diaminobenzene, the sample becomes yellow (figure 2).

The interaction block after 1 minute, adding a 1 M solution of H2SO4. The color intensity, which is determined by an proportional to the binding lectin with glycosidic residues on the cell membrane.

Cells of the buccal mucosa were obtained from healthy volunteers, male and female, by gently scraping the inside of the cheeks with a wooden spatula. Then the cells were collected and suspended in 10 ml of 0.05 M (TBS) isotonic Tris buffer, pH 7,6 (D. Patel et al., An in vitro mucosal model predictive of bio-adhesive agents in the oral cavity. J. Control Release, 1999, 61(1-2):175-183). Then added the sample suspension (0.1 ml Trypanosoma blue, 0,5% (the AC./about.)) and using hemocytometer determined the total number of cells: each sample contained 48×10 4cells of the buccal mucosa. Polysaccharides from cladode Opuntia Ficus Indica and sodium alginate was dissolved in 0.9% isotonic NaCl to a concentration of 0.5% wt./about., and then used for pre-treatment of cells of the buccal mucosa. The results are expressed as percentage of binding of the tested substances with the cells of the mucous membrane, which is inversely proportional to the percentage value of reducing the color of the sample compared with the control sample.

The entire experiment was repeated 5 times for the control sample and for each tested substance.

Statistical analysis was performed using univariate ANOVA analysis in accordance with hoc criterion of Bonferroni.

Results

As shown in figure 3 and 4, the result of this analysis, it was found that 55,81% polysaccharides Opuntia Ficus Indica concatenated with suspended cells of the buccal mucosa, which is significantly higher compared to sodium alginate (mucoadhesive are 5.36%; p<0,05). In addition, it was found that the addition of sodium alginate to the polysaccharides cladode Opuntia Ficus Indica mucoadhesive reaches 74,83%.

Conclusion

The results obtained from the analysis of mucoadhesive in vitro, showed that polysaccharides cladode Opuntia Ficus Indica are characterized by a higher mucoadhesive compared on the Yu with sodium alginate. In addition, it was unexpectedly discovered that the combination of these substances has a synergistic effect, which ensures stronger mucoadhesive activity.

Evaluation of in vivo anti-ulcer activity of the composition containing sodium alginate/antacid/polysaccharides from cladode Opuntia Ficus Indica/extract from the leaves of Olea Europeae

The aim of this study was to evaluate the antiulcer activity of the combination of sodium alginate/antacid, polysaccharides from cladode Opuntia Ficus Indica extract from the leaves of Olea Europeae in an animal model ulcers (in rats)induced by ethanol and indomethacin.

Materials and methods

When performing this experiment were evaluated 5 of the tested compositions, which were compared with filler: the combination of alginate/antacid (A), polysaccharides from cladode Opuntia Ficus Indica (V), the extract from the leaves of Olea Europeae (C), the combination of alginate/antacid/polysaccharides from cladode Opuntia Ficus Indica (D), the combination of alginate/antacid/polysaccharides from cladode Opuntia Ficus Indica/extract from the leaves of Olea Europeae (S) and suspension of carbopol 919 of 0.3% wt./about. in water as a filler (F).

Each sample obtained in the form of an aqueous suspension (concentration indicated in table 7), was injected using a pump for oral administration (1 ml per 100 g body weight).

Table 7
The subjects of songs
Composition (% wt./about.)
ComponentsAndInWithDEF
Sodium alginate5--55-
Sodium bicarbonateto 2.67--to 2.67to 2.67-
Polysaccharides from cladode Opuntia Ficus Indica-2-22-
The extract from the leaves of Olea Europeae--1-1-
The carbopol 9190,3

This experiment was performed using adult male Wistar rats (Rattus norvegicus) weighing from 180 to 200, the Animals were housed under conditions of natural illumination (alternating cycle of light and dark 12:12 hours), controlled temperature (24±1°C) and humidity (60±4%)received standard feed (feed for rats GLP Morini Mill) and water needs for one week. Then, animals were deprived of feed for 24 hours and water for 2 hours before the start of the experiment (F. Vitali, Antiulcer potential of a standardized extract of red orange juice in the rat, Int. J. Food Properties, 10, 331-344, 2007).

Experimental model of ulcers induced by ethanol

Animals were randomly distributed into 6 groups (1-6) for 6 animals in each group. Group 1 was used as the control group, which was introduced filler (sample F, a solution of 0.3% wt./about. of carbopol 919 and 1% wt./about. calcium carbonate in distilled water, neutralized with NaOH, 1 ml/100 g body weight) and after 1 hour of ulcerogenic agent: absolute ethanol (1 ml/rat; animals in groups 2-6 oral injected samples And (767 mg/kg body weight, group 2) (200 mg/kg body weight, group 3), C (100 mg/kg body weight, group 4), D (967 mg/kg of body weight those who and, group 5) and E (1067 mg/kg body weight, group 6). Within 1 hour after injection of the samples a-E animals in groups 2-6 were administered 1 ml of absolute ethanol to cause an ulcer. Within 1 hour after alcohol administration all animals were anestesiologi diethyl ether and was slaughtered. All animals were removed stomachs, which cut at the large curve and gently washed with 0.9% NaCl solution without deleting the superficial mucosa.

Experimental model of ulcers induced by indomethacin

Animals were randomly distributed into 6 groups (1-6) for 6 animals in each group. Animals in group 1 (control group) orally injected with a filler (sample F, a solution of 0.3% wt./about. of carbopol 919 and 1% wt./about. calcium carbonate in distilled water, neutralized with NaOH, 1 ml/100 g body weight) and after 1 hour was subcutaneously injected ulcerogenic substance indomethacin (suspension in distilled water containing 1% carboxymethyl cellulose) in an amount of 0.03 g/kg of body weight (1 ml/kg body weight). Animals in groups 2-4 were injected samples a-E as in the above experimental models of ulcers induced by ethanol, and after 1 hour, the suspension was injected indomethacin. After 5 hours after administration of indomethacin animals were anestesiologi diethyl ether and was slaughtered. All animals were removed stomachs that were analyzed in the same way as in experimental is those with ethanol.

Evaluation of the effectiveness of the tested compositions

Visually analyzed the mucosal surface of the stomach. Length (mm) of each lesion on the mucous membrane was determined on the basis of an arbitrary scale (table 8).

In both experimental models for each stomach was calculated index ulceration (figure U.I.), adding the evaluation assigned to the ulcer, and the percentage of inhibition of ulceration (P.I.U.) [(figure U.I.control- Figure U.I.sample)/Figure U.I.control]*100. Data are expressed as arithmetic mean ± standard error of the mean for each group; the significance of the data was analyzed on the basis of the criterion of the Kruskal-Wallis and then criterion Dunn. The value of p<0,05 was considered significant.

Evaluation of the ulcer for 2 models are shown in table 8.

Results

The results of these experiments are shown in figure 5. In both experimental models, the percentage of inhibition of ulceration (.I.U.)obtained for group D (animals, which have introduced a combination of sodium alginate/antacid/polysaccharides from cladode Opuntia Ficus Indica), was higher compared to the same value obtained with the individual components use the same combination, and higher than the sum of P.I.U, indicating a synergistic effect of the combination of individual substances. The addition of an extract of Olea Europeae (group E) increases P.I.U. by an amount exceeding the amount P.I.U. with the individual use of the extract from the leaves of Olea Europeae and combinations of sodium alginate/antacid/polysaccharides from cladode Opuntia Ficus Indica, which indicates the presence of synergistic action.

Table 8
Assessment ulcers in models of chemically induced ulcer
AssessmentDefeat
0The absence of ulcers
0,5Hyperemia
1Hemorrhagic spots
21-5 small ulcers
3Many small ulcers
41-5 small ulcers and 1-3 large sores
5Many small and large ulcers
6The stomach is full of ulcers along with perforation

Conclusion

This study in vivo allowed us to identify unexpected synergistic potentiation of the effects of sodium alginate/antaci is a, can be achieved with the use of polysaccharides from cladode Opuntia Ficus Indica. Specified synergistic effect enhances the extract from the leaves of Olea Europeae. Ulcerative lesions, had the animals were subjected to standard treatment (sodium alginate and sodium bicarbonate), was assigned a very high score compared to animals that were administered the combination of the present invention, indicating a synergistic effect of the individual components.

Evaluation of in vivo combination of sodium alginate/antacid/polysaccharides from cladode Opunta Ficus Indica/extract from the leaves of Olea Europeae in reducing gastroesophageal reflux caused by surgery (ligation of the pylorus)

The aim of this study was to evaluate the effectiveness of the combination of sodium alginate/antacid/polysaccharides from cladode Opuntica Ficus Indica with the extract from the leaves of Olea Europeae in reducing gastroesophageal reflux caused by surgery as the result of ligation of the pylorus in rats.

Reducing gastroesophageal Relaxa was measured in the presence of ulcers of the esophagus in animals that were administered the active combination after surgical induction of ulcers.

Adult male Wistar rats (Rattus norvegicus) weighing 180-200 grams were randomly divided into 6 groups (1-6) for 6 animals in each gr is the group. In accordance with the Protocol of the experiment described in the publication Mina (Min et al.: The effects of apigenin-7-O-β-D-glucurono-pyranoside on reflux oesophagitis and gastritis in rats, Autonomic &autacoid Pharmacology 2005 Jul; 25(3):85-91; T. Hayakawa et al.: Roles of cyclooxygenase 2 and microsomal prostaglandin E synthase 1 in rat acid reflux oesophagitis, Gut 2006, 55:450-456), animals were anestesiologi pentobarbital and called esophagitis due to acid reflux by ligating the transition region between the cardiac Department of the stomach and the glandular part and wrapping the duodenum near the pylorus. Group 1 (not exposed to any effect) was the positive control group. Animals in groups 2-6 intraduodenal was administered compositions a-E immediately after ligating the pylorus and the limiting protrusion in the same quantities that the previous models of chemically induced ulcers. Then at the junction of the stomach to the esophagus performed a longitudinal cardiomyotomy length of about 1 cm to enhance the reflux from the stomach into the esophagus. After 6 hours the animals were anestesiologi diethyl ether and was slaughtered, the esophagus was removed and evaluated the total area of lesions on the basis of the estimates are given in table 9.

End index ulceration (figure U.I.) and P.I.U. for each group was calculated as described above.

Table 9
Evaluation poraj the deposits of the mucous membrane of the esophagus
AssessmentTotal area (mm2)
0No visible lesions
1Rare lesions
2The total area of lesions ≤30 mm2
3The total area of lesions ≥30 mm2
4The perforation

Results

The results of the described experiment is shown in Fig.6. This experimental model has confirmed a higher percentage of inhibition of ulceration (P.I.U.)obtained in group D (which was introduced sodium alginate/antacid/polysaccharides from cladode Opuntia Ficus Indica), compared with the same value obtained in the experimental groups, which were introduced individual components, and this figure was even higher amounts P.I.U, indicating a significant synergistic effect of the combination of sodium alginate/antacid/polysaccharides from cladode Opuntia Ficus Indica in reducing gastroesophageal reflux. Then add the extract from the leaves of Olea Europeae to the specified combination (group E) increased P.I.U. what about the level which was higher than P.I.U. used separately extract from the leaves of Olea Europeae and combinations of D, confirming the results obtained in models of chemically induced gastric ulcers.

Conclusion

This test in vivo shows that the extract from cladode Opuntia Ficus Indica has a potentiating effect on the reduction of gastroesophageal reflux. The effect is further increased by the addition of extract from the leaves of Olea Europeae.

1. Oral pharmaceutical composition comprising polysaccharides from cladode Opuntia Ficus Indica extract from the leaves of Olea Europeae, alginate and sodium bicarbonate, where the mass ratio of alginate to sodium bicarbonate, the leaf extract Olea Europeae, polysaccharides from cladode Opuntia Ficus Indica is from 2:1:1:0.2 to 4:2:4:4, for the prevention and treatment of gastroesophageal reflux and GERD.

2. The composition according to claim 1, in which the mentioned polysaccharides cladode are in the form of mucus, juice cladode or aqueous solution (ultra)filtered juice cladode, which is not necessarily concentrated and dried.

3. The composition according to claim 1, which is represented in the form of a solution, suspension, emulsion, tablet, capsule, powder or sachet for the preparation of suspensions or emulsions for oral administration.

4. Composition according to any one of paragraphs. 1-3, in the form of powder, including:

Alginat sodium10-20 g
Sodium bicarbonate5-10 g
Leaf extract Olea Europeae5-20 g
Polysaccharides from cladode Opuntia Ficus Indica1-20 g



 

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25 cl, 3 tbl, 163 ex

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2 cl, 1 tbl, 2 ex

FIELD: medicine.

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19 cl, 2 dwg, 7 tbl, 4 ex

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