Morphology and buoyancy of oil-entrapped calcium pectinate gel beads

A new emulsion-gelation method to prepare oil-entrapped calcium pectinate gel (CaPG) beads capable of floating in the gastric condition was designed and tested. The gel beads containing edible oil were prepared by either being gently mixed or homogenized an oil phase and a water phase containing pectin, and then extruded into calcium chloride solution with gentle agitation at room temperature. The gel beads formed were then separated, washed with distilled water, and dried at 37 degrees C for 12 hours. A model of the emulsion-gelation process to illustrate the formation of oil-entrapped CaPG beads was proposed. The effect of selected factors, such as type of oil, percentage of oil, and type of pectin on morphology and floating properties was investigated. The oil-entrapped calcium pectinate gel beads floated if a sufficient amount of oil was used. Scanning electron photomicrographs demonstrated very small pores, ranging between 5 and 40 microm, dispersed all over the beads. The type and percentage of oil play an important role in controlling the floating of oil-entrapped CaPG beads. The results suggested that oil-entrapped CaPG beads were promising as a carrier for intragastric floating drug delivery.     

Binding capacity of various fibre to pesticide residues under simulated gastrointestinal conditions

The purpose of this study was to compare the effect of the nature and quantity of various dietary fibre (cellulose, hemicellulose, pectin, lignin) in diets on the binding capacity to pesticides azinphos-methyl (AZM), chlorpropham (CLP), chlorothalonil (CKL), permethrin (PER) as estimated by solubility under conditions of pH and temperature simulating those in the gastrointestinal tract (incubated at pH 2 for 30 min at 37°C, then at pH 7 for 60 min). The ratios of fibre to pesticides were determined in omnivorous diets. In this model, the binding capacity of lignin was equal to hemicellulose for PER, AZM and CLP, but it was significantly higher for CKL. Hemicellulose bound more CKL, AZM and CLP than did cellulose. Although pectin appreciably decreased all pesticides, its effect was lower than other fibres with one exception—cellulose-CKL. In the presence of equal amounts of fibre, lignin exerted the most significant effect on pesticide solubility. Hemicellulose and cellulose bind to the same extent PER and AZM. The effect of pectin was significant only on CKL and AZM when compared to the control.     

Citrus pectin affects cytokine production by human peripheral blood mononuclear cells

Dietary fibers, including pectin, have been shown to exert a favorable effect on a wide spectrum of pathological conditions. Their positive influence on human health is explained by their anti-oxidative, hypocholesterolemic and anti-cancerous effects. However, little has been reported about their activity on the immune system. Therefore, the present study was undertaken to examine the effect of citrus pectin (CP) on cytokine production by human peripheral blood cells (PBMC). PBMC were incubated without or with CP at different degrees of esterification (DE) (∼30, ∼60 and ∼90% esterified pectin, assigned as DE30, DE60 and DE90, respectively) for detection of IL-1β, IL-1ra, TNFα, IL-6 and IL-10 secretion. Incubation with DE60 and DE90 induced a dose-dependent inhibition of the pro-inflammatory cytokine IL-1β secretion, whereas D30 did not affect this function. However, CP at all three esterification degrees did not alter the secretion of the additional pro-inflammatory cytokines examined, i.e. TNFα and IL-6. Conversely, CP at DE60 and DE90 caused a dose-dependent increased secretion of the anti-inflammatory cytokines IL-1ra and IL-10, whereas D30 did not affect the production of IL-1ra and decreased that of IL-10. The findings indicate that CP possesses the capacity to exert an immunomodulatory response in human PBMC which may have a favorable effect on human health.     

Isolation and chemical analysis of a lipopolysaccharide from the outer membrane of the oral anaerobic spirochete Treponema pectinovorum

Isolation of a putative lipopolysaccharide from the surface of the oral treponeme, Treponema pectinovorum, revealed it to contain larger amounts of 3-deoxy-D-manno-octulosonic acid compared with other oral Treponema species. This molecule was isolated from the outer membrane of T. pectinovorum and had chemical characteristics of a putative lipopolysaccharide. The yield of lipopolysaccharide was between 0.6% and to 1.1% of the bacterial dry weight. The purified molecule was resistant to the action of proteinases and consisted of both sugars and lipids. 3-Deoxy-D-manno-octulosonic acid and hexoses accounted for 6.1-8.7% and 17.6-20.2%, respectively of the dry weight. Carbohydrate compositional analysis revealed the presence of glucose, galactose, 2-acetamido-2-deoxy-glucose, rhamnose and 6-deoxy-talose in the molar ratio of 1.00:0.96:0.19:0.88:0.98, respectively. No heptose was detected. The fatty acid analysis determined the presence of straight chain, C13:00, C14:00, C15:00 and C17:00 acids, as well as branched chain, C13:00, C14:00 and two species of C15:00, acids. Electrophoretic analysis indicated that the lipopolysaccharide was present as two major species.     

Decreased bioavailability of propranolol due to interactions with adsorbent antacids and antidiarrhoeal mixtures

The interaction of propranolol (50–160 mg/100 ml) with recommended doses of magnesium trisilicate, kaolin-pectin and bismuth subsalicylate suspensions was studied. Magnesium trisilicate and bismuth subsalicylate were found to adsorb propranolol with a limiting adsorptive capacity of 112 and 97 mg/g, respectively. Kaolin-pectin suspension adsorbed practically all of the drug. The effect of these interactions on the bioavailability of propranolol in rats was determined. The extent, but not the rate. of propranolol absorption was decreased on concomitant administration of the adsorbents. Peak propranolol plasma concentrations decreased by 292 5% and a parallel decrease of 35–44% in AUC values was observed. These interactions suggest possible clinically important differences in propranolol bioavailability.     

米邦塔仙人掌果胶对小鼠慢性不可预知温和应激所致抑郁样症状的改善作用

目的:研究米邦塔仙人掌果胶(milpa alta cactus pectin,MCP)对小鼠慢性不可预知温和应激(CUMS)后体重和糖水偏好的影响。方法:健康雄性昆明种小鼠60只随机分为5组:正常对照组、CUMS组、MCP低剂量组(50 mg/kg)、MCP中剂量组(100 mg/kg)、MCP高剂量组(200 mg/kg),各10只。采用11种应激因子,建立CUMS模型,给予小鼠应激6周。通过测量糖水摄入和小鼠体重变化率,评价MCP对抑郁样症状的改善作用。结果:CUMS组小鼠体重增长率、糖水摄入量都显著低于正常对照组(P0.05);与CUMS组比较,MCP中、高剂量组小鼠体重变化率、糖水摄入量明显增加(P0.05)。结论:MCP对CUMS所致抑郁样症状具有一定的改善作用。     

Standard triple, bismuth pectin quadruple and sequential therapies for Helicobacter pylori eradication

AIM: To compare the effectiveness of standard triple, bismuth pectin quadruple and sequential therapies for Helicobacter pylori (H. pylori ) eradication in a randomized, double-blinded, comparative clinical trial in China. METHODS: A total of 215 H. pylori -positive patients were enrolled in the study and randomly allocated into three groups: group A (n = 72) received a 10-d bismuth pectin quadruple therapy (20 mg rabeprazole bid , 1000 mg amoxicillin bid , 100 mg bismuth pectin qid , and 500 mg levofloxaci...     

Pectin/Kollicoat SR30D isolated films for colonic delivery [I]: a comparison of normal and colitis‐induced models to assess the efficiency of microbially triggered drug delivery

Objectives The purpose of the study was to evaluate digestion of pectin/Kollicoat SR30D free films for colonic delivery in vitro and in vivo. Methods Free films containing different ratios of pectin to Kollicoat SR30D were prepared by casting/solvent evaporation method. An in‐vitro comparison of swelling, degradation and permeability of the free films was carried out in simulated colon fluids containing caecal contents from normal rats with colitis induced by 2,4,6‐trinitrobenzene sulfonic acid (TNBS) or oxazolone. A comparative in‐vivo evaluation of degradation was also conducted in normal and colitis‐induced model rats. Key findings The pectin within the mixed films was susceptible to rat colonic bacterial enzymes. The extent of digestion correlated with the amount of pectin present within the film. In vitro, the swelling index, drug permeability and extent of film digestion in simulated colon fluids with caecal contents obtained from normal rats were higher than from TNBS‐ or oxazolone‐induced model rats, whereas in‐vivo degradation was similar in the three groups of rats. The pectin/Kollicoat SR30D free films were completely degraded in the colitis‐induced rats. Conclusions Pectic/Kollicoat SR30D films may be useful as coatings to target delivery of drugs to the colon.     

Effect of Pectin Type and Plasticizer on In Vitro Mucoadhesion of Free Films

The objective was to measure and compare the specific and general mucin interaction of plasticized and unplasticized pectin films. The pectin types differed in the type and degree of substitution. Mucoadhesive properties were measured by using a texture analyzer. Pectin with an intermediate degree of methoxylation (36%) displayed substantially higher general and specific mucin interaction than amidated, acetylated, and high methoxylated pectin. This was explained with extensive hydrogen bonding in addition to favorable wetting properties. When comparing all plasticized films to all unplasticized films, a consistent and statistically significant increase in the peak force was observed on adding an effective plasticizer.     

A New Ternary Polymeric Matrix System for Controlled Drug Delivery of Highly Soluble Drugs: I. Diltiazem Hydrochloride

Purpose. The purpose of this study was to develop a new ternary polymeric matrix system that is easy to manufacture and that delivers a highly soluble drug over long periods of time. Methods. Pectin, hydroxypropylmethylcellulose (HPMC), and diltiazem HC1 granulated with gelatin at optimized ratios were blended at different loading doses and directly compressed. Swelling behavior, dissolution profiles and the effect of hydrodynamic stress on release kinetics were evaluated. Results. Diltiazem release kinetics from the ternary polymeric system was dependent on the different swelling behavior of the polymers and varied with the drug loading dose and hydrodynamic conditions. Drug release followed either non-Fickian or Case II transport kinetics. The relative influence of diffusion and relaxational/dissolution effects on release profiles for different drug loadings was calculated by a nonlinear regression approach. Photographs taken during swelling show that the anisotropic nature of the gel structure, drug loading dose, swelling capacity of polymers used, and the design of delivery system all play important roles in controlling the drug release and dissolution/ erosion processes. Conclusions. Zero-order delivery of diltiazem HC1 from a simple tablet matrix was achieved. The ternary polymeric system developed in this study is suitable for controlled release of highly soluble drugs. It offers a number of advantages over existing systems, including ease of manufacturing and of release modulation, as well as reproducibility of release profiles under well defined hydrodynamic conditions. Our delivery system has the potential to fully release its drug content in a controlled manner over a long time period and to dissolve completely.