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Biphasic drug release: the permeability of films containing pectin, chitosan and HPMC.

The permeabilities of mixed films of pectin/chitosan/HPMC have been studied to assess their value in producing a dosage form with biphasic drug release characteristics. The inclusion of chitosan enhanced the properties of the films, rendering them stable at all physiological pH values. Pectin/HPMC films were soluble at pH values above 3.0. All pectin/chitosan/HPMC films were permeable to a model drug, paracetamol. HPMC initially increased the permeability of the films and subsequently reduced it at higher concentrations. The minimum permeability was obtained at pH 3 and at an HPMC level of 5% where the potential for polyelectrolyte complex formation between pectin and chitosan exists. The permeabilities of the films increased when they were exposed to pectinolytic enzymes, a system designed to mimic conditions in the colon. The film formulation thus show the potential for biphasic delivery with an initial, controllable slow phase that can be manipulated by changes in the formulation followed by a faster phase under conditions pertaining in the colon.

Acetaminophen↗

Antidiarrhoeal and antiulcerogenic effects of methanolic extract of Asparagus pubescens root in rats.

The effect of methanolic extract of Asparagus pubescens root on experimentally-induced diarrhoea and ulceration was investigated in rats. The extract (500-1500 mg/kg) dose-dependently, reduced significantly the intestinal propulsive movement, castor oil-induced diarrhoea and intestinal fluid accumulation. Yohimbine an alpha(2)-adrenoceptor blocker attenuated the antidiarrhoeal effect of the extract. The extract also reduced the ulcer indices induced by indomethacin and ethanol in a dose-related manner. The results indicate that its antidiarrhoeal and antiulcerogenic effects might in part be due to its alpha(2)-adrenoceptor stimulation and its active constituents respectively.

Anti-Ulcer Agents↗

Anti-diarrheal effect of water extract of Evodiae fructus in mice.

Our previous study showed that Evodiae fructus (the dried, unripe fruit of Evodia rutaecarpa) has an inhibitory effect on the intestinal transit (anti-transit effect) in mice. In the present study, a water extract of Evodiae fructus was used to examine its effect on castor oil-induced diarrhea and to compare with its anti-transit effect in mice. The results indicated that Evodiae fructus had both anti-transit and anti-diarrheal effects with comparable ID(50) (the dose for 50% inhibition) values of 54+/-7 and 76+/-17 mg/kg. The time-courses of Evodiae fructus pretreatment for both anti-transit and anti-diarrheal effects were very similar. Because no significant influences of both nitric oxide (NO) precursor L-arginine (600 mg/kg, i.p.) and NO synthase inhibitor N(G)-nitro-L-arginine methyl ester (25 mg/kg, i.p.) pretreatment, the NO system was not involved in both the anti-transit and anti-diarrheal effects of Evodiae fructus. Like Evodiae fructus, a muscarinic acetylcholine receptor antagonist atropine inhibited castor oil-induced increase in fecal weight and loss of body weight. However, the potencies or time-courses of atropine pretreatment for both anti-transit and anti-diarrheal effects were different. Furthermore, the anti-diarrheal effect of atropine was independent of its anti-transit effect at the lower dose (0.5 mg/kg, i.p.). Therefore, the action of Evodiae fructus appeared to be something different from atropine, suggesting that an action other than the anti-muscarinic action, as previously proposed for Evodiae fructus, may be involved.

Animals↗

Study of antidiarrhoeal activity of four medicinal plants in castor-oil induced diarrhoea.

A study was undertaken to evaluate the effect of aqueous and methanolic plant extracts of Acorus calamus rhizome, Pongamia glabra leaves, Aegle marmelos unripe fruit and Strychnos nux-vomica root bark for their antidiarrhoeal potential against castor-oil induced diarrhoea in mice. The methanolic plant extracts were more effective than aqueous plant extracts against castor-oil induced diarrhoea. The methanolic plant extracts significantly reduced induction time of diarrhoea and total weight of the faeces. The result obtained establish the efficacy of these plant extracts as antidiarrhoeal agents.

Animals↗

Anti-diarrhoeal evaluation of some medicinal plants used by Zulu traditional healers.

Aqueous and methanolic extracts of several medicinal plants, Psidium guajava (leaves), Aristea spp., Iridaceae family (stem), Bridelia micrantha (bark) and Eleutherina bulbosa (bulb), used by Zulu traditional healers were evaluated for anti-diarrhoeal activity against different experimental models of diarrhoea in rats as well as for anti-microbial activity against different pathogenic microorganisms that cause diarrhoea. The methanolic extract of P. guajava (leaves) was the only agent showing significant inhibitory activities against the growths of Salmonella spp. (two isolates), Shigella spp. (S. flexneri, S. virchow and S. dysenteriae) and enteropathogenic Escherechia coli (two isolates). The methanolic extract of B. micrantha (Bark) demonstrated weak inhibitory activities against S. flexneri and S. plesiomonas. Based on the results in experimental rat models, there were significant reductions in faecal output and frequency of droppings when plant extracts were administered compared with castor-oil treated rats. All plant extracts also significantly retarded the propulsion of charcoal meal and significantly inhibited the PGE(2)-induced enteropooling. The results have confirmed the effectiveness of all these Zulu medicinal plants as anti-diarrhoeal agents.

Africa↗

Intestinal anti-spasmodic effect of a phytodrug of Psidium guajava folia in the treatment of acute diarrheic disease.

Ancestral medicinal use of guava (Psidium guajava L. Fam. Myrtaceae) is today supported by numerous biomedical studies concerning the properties of leaf extracts. However, insufficient clinical studies are reported on the use of this plant resource in the treatment of gastrointestinal ailments. The present work reports a randomized, double-blinded, clinical study performed to evaluate the safety and efficacy of a phytodrug (QG-5) developed from guava leaves, standardized in its content of quercetin and orally administered to a group of adult patients with acute diarrheic disease. Capsules containing 500 mg of the product were administered to 50 patients every 8 h during 3 days. Results obtained showed that the used guava product decreased the duration of abdominal pain in these patients.

Acute Disease↗

Evaluation of anti-diarrhoeal activity in seed extracts of Mangifera indica.

Mangifera indica is commonly grown in many parts of the world. Its seeds have been used for anti-diarrhoeal activity in Indian traditional medicine. This study evaluates the potential anti-diarrhoeal activity of methanolic (MMI) and aqueous (AMI) extracts of seeds of M. indica in experimental diarrhoea, induced by castor oil and magnesium sulphate in mice. Both MMI and AMI were given orally in the dose of 250 mg/kg, showed significant anti-diarrhoeal activity comparable with that of the standard drug loperamide. However, only MMI significantly reduced intestinal transit in charcoal meal test as compared with atropine sulphate (5 mg/kg; im). The in vitro antimicrobial activity of MMI and AMI showed variable results. While, AMI significantly inhibited growth of Streptococcus aureus and Proteus vulgaris, both MMI and AMI did not show any significant effect on growth of E. coli and Klebsiella. The results illustrate that the extracts of M. indica have significant anti-diarrhoeal activity and part of the activity of MMI may be attributed to its effect on intestinal transit.

Animals↗

Evaluation of antidiarrhoeal activity Rumex maritimus root.

The partitioned n-hexane, ethylacetate and residual methanol extracts of the root of Rumex maritimus were evaluated for antidiarrhoeal activity in mice using castor oil and serotonin induced diarrhoea and also charcoal motility test at 50, 100 and 200 mg/kg body weight dose. Among these, the methanol extract most significantly prolonged the time for induction of diarrhoea, reduced the frequency of diarrhoeal episodes and also decreased the propulsion of charcoal meal through the gastrointestinal tract.

Animals↗

Gastrointestinal effects of Mebarid, an ayurvedic formulation, in experimental animals.

Mebarid, an ayurvedic formulation, was tested for its anti-diarrhoeal, anti-ulcer and anti-motility activities in animals. Mebarid was investigated at four dose levels of 125, 250, 500 mg/kg BW and 1g/kg BW The methods of castor oil-induced diarrhoea and pylorus-ligation-induced ulcers in rats were used to evaluate the anti-diarrhoeal and anti-ulcer activity, respectively, while charcoal meal test in mice was the method used for testing its anti-motility effect. Mebarid was found to have significant activity in all the three models. Thus, it can be concluded that Mebarid possesses anti-diarrhoeal, anti-motility and anti-ulcer activities and can prove beneficial in the treatment of above gastrointestinal disorders.

Animals↗

Screening of anti-diarrhoeal profile of some plant extracts of a specific region of West Bengal, India.

Ethanol extract of four different plants of the Khatra region of the Bankura district of West Bengal, India were evaluated for anti-diarrhoeal activity against different experimental models of diarrhoea in rats. The extracts of Ficus bengalensis Linn. (hanging roots), Eugenia jambolana Lam. (bark), Ficus racemosa Linn. (bark) and Leucas lavandulaefolia Rees (aerial parts) showed significant inhibitory activity against castor oil induced diarrhoea and PGE2 induced enteropooling in rats. These extracts also showed a significant reduction in gastrointestinal motility in charcoal meal tests in rats. The results obtained establish the efficacy of all these plant materials as anti-diarrhoeal agents.

Animals↗

Antidiarrhoeal activity of Waltheria americana, Commelina coelestis and Alternanthera repens.

The antidiarrhoeal activity of the hexane, chloroform, methanol and aqueous extracts of Waltheria americana, Commelina coelestis and Alternathera repens, was tested on mice with diarrhoea induced by castor oil and MgSO4. The methanol extract of C. coelestis and A. repens and aqueous extract of A. repens, presented antidiarrhoeal effect, monitored by number of liquid feces defecated and intestinal transit of a suspension of graphite with castor oil in Wistar rats.

Administration, Oral↗

Antiamoebic and phytochemical screening of some Congolese medicinal plants.

Results from the in vitro antiamoebic activity of some Congolese plant extracts used as antidiarrhoeic in traditional medicine indicated that of 45 plant extracts tested, 35 (77.78%) exhibited an antiamoebic activity and 10 (22.22%) were inactive. The highest activity (MIC < 100 microg/ml) was obtained with extracts from root bark of Paropsia brazzeana, Cryptolepis sanguinolenta, Alchornea cordifolia, Hensia pulchella, Maprounea africana, Rauwolfia obscura and Voacanga africana, leaves and stem bark of Psidium guajava, stem bark of Dialum englerianum, Harungana madagascariensis and Mangifera indica, mature seeds of Carica papaya, and leaves of Morinda morindoides and Tithonia diversifolia. Metronidazole used as reference product showed a more pronounced activity than that of all plant extracts tested.

Amebicides↗

Antidiarrhoeal effects of Ocimum gratissimum leaf extract in experimental animals.

The aqueous extract of the leaves of Ocimum gratissimum was screened for antidiarrhoeal effects. The extract inhibited castor oil-induced diarrhoea in rats as judged by a decrease in the number of wet faeces in the extract-treated rats. In addition, the extract inhibited the propulsive movement of intestinal contents. On the isolated ileum of guinea-pig, the extract showed no direct action; however, it reduced the responses of the guinea-pig ileum to acetylcholine, nicotine and histamine. Phytochemical tests revealed the main constituents as tannins, steroids, triterpenoid and carbohydrates. These findings suggested that the aqueous extract of the leaves of O. gratissimum might elicit an antidiarrhoeal effect by inhibiting intestinal motility, partly via muscarinic receptor inhibition.

Acetylcholine↗

Studies on antidiarrhoeal activity of Punica granatum seed extract in rats.

Methanol extract of Punica granatum seed was evaluated for antidiarrhoeal activity against different experimental models of diarrhoea in rats. P. granatum seed extract treated animals showed significant inhibitory activity against castrol-oil induced diarrhoea and PGE2 induced enteropooling in rats. The extract also showed a significant reduction in gastro-intestinal motility in charcoal meal test in rats. The results obtained established the efficacy of P. granatum seed extract as an antidiarrhoeal agent.

Animals↗

Anti-diarrhoeal evaluation of Clerodendrum phlomidis Linn. leaf extract in rats.

A study was undertaken to evaluate the effect of methanolic extract of leaves of Clerodendrum phlomidis Linn. (MECP) (Family: Verbenaceae) for its anti-diarrhoeal potential against several experimental models of diarrhoea in Wistar albino rats. MECP showed significant inhibitory activity against castor oil induced diarrhoea and PGE2 induced enteropooling in rats. The extract also showed a significant reduction in gastrointestinal motility in charcoal meal test in rats. The results obtained establish the efficacy and substantiated the folklore claim as an anti-diarrhoeal agent.

Animals↗