Sterculia and Brachychiton: a comprehensive overview on their ethnopharmacology, biological activities, phytochemistry and the role of their gummy exudates in drug delivery.

OBJECTIVES: Sterculia and Brachychiton are two related genera (Malvaceae) containing more than 300 species. Most of these species are ornamental trees that are native to Australia and widely cultivated in many countries. Different members of the two genera were used by various cultures for medicinal and economical purposes. This review sheds light on the medicinal values and chemical composition of various species of these two genera. KEY FINDINGS: Sterculia and Brachychiton species were used traditionally for the treatment of gastrointestinal disorders, microbial infection, skin diseases, inflammation and many other conditions. The seeds of various species were roasted and eaten by many traditional tribes. Plants from the two genera revealed their anti-inflammatory, antioxidant, antimicrobial, antidiabetic, antiulcer, insecticidal and analgesic activity. These activities may be attributed to the presence of a wide range of secondary metabolites as flavonoids, phenolic acids, coumarins, terpenoids particularly sesquiterpenes and triterpenes in addition to sterols and fatty acids. Moreover, the gummy exudates obtained from some members of these genera played an important role in different pharmaceutical dosage forms and drug-delivery systems. CONCLUSIONS: More research is recommended on other species of Sterculia and Brachychiton to discover new molecular entities with potential biological and economic values.

Natural gum as mucoadhesive controlled release carriers: evaluation of cefpodoxime proxetil by D-optimal design technique.

The present study deals with the development of mucoadhesive controlled release tablets of Cefpodoxime Proxetil to increase the gastric residence time and thus prolong drug release, reduce dosing frequency and improve oral bioavailability. Tablets were prepared using sodium alginate and karaya gum, a natural polymer, with a synthetic polymer hydroxypropylmethylcellulose (K100LV) and Karaya gum with HPMC K100LV in various ratios to optimize the drug release profile using D-Optimal technique. Pre- and post-compression parameters of tablets prepared with various formulations (S1-S9, C1-C9) were evaluated. The FTIR and DSC studies revealed that no physiochemical interaction between excipients and drug. The formulation S7 showed prolonged drug release, and the mechanism of drug release from the optimized formulation was confirmed using the Korsmeyer-Peppas model to be non-Fickian release transport and n value was found 0.605 indicating both diffusion and erosion mechanism from these natural gums. The optimized formulation showed mucoadhesive strength >35 g. An in vivo study was performed on rabbits using an X-ray imaging technique. The radiological evidence suggests that the tablets adheres (more than 10 hours) to a rabbit's stomach. No significant changes were found in the physical appearance, drug content, mucoadhesive study and in vitro dissolution pattern after storage at 40 °C/75% relative humidity for 3 months.

Evaluation of Sterculia foetida gum as controlled release excipient.

The purpose of the research was to evaluate Sterculia foetida gum as a hydrophilic matrix polymer for controlled release preparation. For evaluation as a matrix polymer; characterization of Sterculia foetida gum was done. Viscosity, pH, scanning electronmicrographs were determined. Different formulation aspects considered were: gum concentration (10-40%), particle size (75-420 microm) and type of fillers and those for dissolution studies; pH, and stirring speed were considered. Tablets prepared with Sterculia foetida gum were compared with tablets prepared with Hydroxymethylcellulose K15M. The release rate profiles were evaluated through different kinetic equations: zero-order, first-order, Higuchi, Hixon-Crowell and Korsemeyer and Peppas models. The scanning electronmicrographs showed that the gum particles were somewhat triangular. The viscosity of 1% solution was found to be 950 centipoise and pH was in range of 4-5. Suitable matrix release profile could be obtained at 40% gum concentration. Higher sustained release profiles were obtained for Sterculia foetida gum particles in size range of 76-125 microm. Notable influences were obtained for type of fillers. Significant differences were also observed with rotational speed and dissolution media pH. The in vitro release profiles indicated that tablets prepared from Sterculia foetida gum had higher retarding capacity than tablets prepared with Hydroxymethylcellulose K15M prepared tablets. The differential scanning calorimetry results indicated that there are no interactions of Sterculia foetida gum with diltiazem hydrochloride. It was observed that release of the drug followed through surface erosion and anomalous diffusion. Thus, it could be concluded that Sterculia foetida gum could be used a controlled release matrix polymer.

Suppressive effect of viscous dietary fiber on elevations of uric acid in serum and urine induced by dietary RNA in rats is associated with strength of viscosity.

This study was performed to clarify how dietary fiber (DF) with different viscosities would be associated with dietary RNA metabolism. Male Wistar strain rats, four weeks old, were fed diets containing a 3% (w/w) yeast RNA and a 5% (w/w) viscous DF for five days. Viscosity of DF samples used, in order of strength, were xanthan gum (XG) > guar gum (GG) > locust bean gum (LBG) > karaya gum (KG) > pectin (PE) = arabic gum (AG) > CM-cellulose (CMC) = inulin (IN). The serum uric acid concentration in the viscous DF groups significantly decreased as compared with that in the cellulose (CL) group. The urinary excretions of uric acid and allantoin in the respective groups given AG, GG, IN, KG, PE, and XG were significantly suppressed as compared with those in the CL group. The fecal RNA excretion was markedly increased in the IN, KG, PE, and XG groups in comparison to the CL group. The DF with high viscosity significantly suppressed RNA digestion by RNase A and decreased uptakes of 14C-labeled adenosine and adenosine 5'-monophosphate (5'-AMP) in rat jejunum. The results reveal that the suppressive effect of DF on elevation of serum uric acid concentration induced by dietary RNA in rats is associated with the strength of DF viscosity. The mechanism by which this is accomplished is suggested to be attributed to the inhibitions of digestion for dietary RNA and/or absorption of the hydrolyzed compounds.

Compressed xanthan and karaya gum matrices: hydration, erosion and drug release mechanisms.

Directly compressed matrices were produced containing either xanthan gum or karaya gum as a release-controlling agent. These swellable hydrophilic natural gums were used to control the release of varying proportions of two model drugs, caffeine and diclofenac sodium, which have different solubilities in aqueous medium. Gum erosion, hydration and drug release studies were carried out using a dissolution apparatus (basket method) at two agitation speeds. Xanthan gum displayed a high degree of swelling due to water uptake and a small degree of erosion due to polymer relaxation. Neither agitation speed nor drug solubility had any significant effect on water uptake, but matrices with the lower proportion of gum produced a lesser degree of hydration. In contrast, karaya gum displayed a much lower hydration capacity and a higher rate of erosion, both markedly affected by agitation speed. Drug release from xanthan and karaya gum matrices depended on agitation speed, solubility and proportion of drug. Both xanthan and karaya gums produced near zero order drug release with the erosion mechanism playing a dominant role, especially in karaya gum matrices.

Relationship between swelling, erosion and drug release in hydrophillic natural gum mini-matrix formulations.

The swelling, erosion and solvent front penetration properties of mini-matrices containing xanthan (X), locust bean (LB) and karaya (K) gums were examined, analysed and related to the overall in vitro release kinetics of diclofenac sodium, used as a model drug. Mini-matrices were produced with drug:gum ratios of 1:1 as well as formulations of drug and X in combinations of 2:1, 2:3 and 1:2. The rank order of decreasing swelling index (SI) in both axial and radial dimensions was X?K?LB and each gum showed almost Fickian swelling behaviour. The solvent front penetration rates were consistent with the rates of swelling. However, the order of decreasing drug release and erosion rates was LB>X>K and all formulations demonstrated anomalous (non-Fickian) drug release kinetics. Therefore Fickian drug diffusion and polymer erosion were both occurring simultaneously. The dominant mechanism depended on the nature and content of the gum, as well as the stage in the dissolution time period. There was a loss of matrix integrity in formulations containing a high drug:gum ratio.

[Esophageal obstruction after laxative administration]. / Osophagusobstruktion nach Laxantieneinnahme.

Esophageal obstruction caused by food or foreign bodies is not uncommon in elderly patients. The esophageal obstruction is rarely caused by bulk laxatives, even though they are regularly prescribed to elderly patients. We report a case of a 69-year-old woman presenting as an emergency complaining of retrosternal discomfort and the inability to swallow or drink. Directly before contracting the problem, she had taken two teaspoons of Colosan mite, a laxative containing sterculia. We performed a rigid esophagoscopy, which revealed a complete obstruction by a gum like substance in the area of the upper esophagus sphincter. The laxative could be removed and the patient recovered without problems.

Caecal and faecal short-chain fatty acids and stool output in rats fed on diets containing non-starch polysaccharides.

The exact mechanisms by which non-starch polysaccharides increase stool output are unknown. In the present study the hypothesis that the site of fermentation and short-chain fatty acid (SCFA) accumulation is related to the action of non-starch polysaccharides (NSP) on stool output was tested. The basal diet (45 g NSP/kg) of forty-three male Wistar rats was supplemented with 50 g/kg of either guar, karaya, tragacanth, gellan, xanthan or ispaghula for 28 d. A further twenty-three rats were maintained on the basal diet for the same time period. Faeces were then collected over 2 d and caecal contents obtained post-mortem. Caecal and faecal wet and dry weights and SCFA were measured. Each supplement had a different effect on the caecal and faecal contents but they appeared to fall into three groups when compared with the basal diet. In group 1, guar gum affected only caecal SCFA. It had no effect on stool output or faecal SCFA. In group 2, karaya increased caecal SCFA and tragacanth, karaya and xanthan increased faecal SCFA and faecal water. In group 3, ispaghula and gellan had no consistent effect on caecal or faecal SCFA concentrations but increased total faecal SCFA output and increased faecal wet and dry weight. Although the knowledge that SCFA are rapidly absorbed in the large intestine has led us to believe that they play no role in determining faecal output, these results suggest that in some cases where NSP are slowly fermented, and increase faecal SCFA, the role of the SCFA may need to be reassessed.