Enteric-coated Microspheres Research Articles

PREPARATION AND CHARACTERIZATION OF ENTERIC-COATED DELAYED-RELEASE MICROSPHERE OF PHYTOSOME LOADING ALLICIN-RICH EXTRACT

Objective: Allicin, a natural organosulfur compound, is the main garlic ingredient, which has extensive pharmacological activities. Its unstable under acidic conditions due to alliinase's inactivation causes the need for preparations that delayed-release in the stomach to maximize allicin absorption. This study aimed to prepare and characterize the enteric-coated microsphere of phytosome loading allicin-rich extract to protect it from gastric acid.
 Methods: The allicin-rich extract phytosome (ArE-Ps) was prepared and evaluated for characteristics. Microsphere was made in three formulas with different molar ratios of ArE-Ps and Eudragit L30D-55 (1:1; 1:1.5 and 1:2) by spray dry. The three microspheres compared to particle size, entrapment efficiency, and dissolution test in acid and 7.4 pH medium.
 Results: Optimized ArE-Ps has a size of 251.6 nm, polydispersity index 0.466, zeta potential 34.11, entrapment efficiency of 62.62 %, and specific gravity of 1,005 g/ml. The surface topography of the three formulas shows an almost spherical shape with concave surfaces. The particle size of the microsphere ranges from 215±6.27 nm to 548.8±10.15 nm. Entrapment efficiency increases with an increasing number of polymers with a maximum value of 65.44 % at F3. The results dissolution test in vitro showed no drug release in acidic medium, and drug release occurred at a 7.4 pH medium. Drug release of three microsphere formulations followed the Korsmeyer-Peppas model with a k value of 12.7088±0.1769; 17.9322±1.5621; and 12.958±1.2677; respectively.
 Conclusion: Based on these results, the polymer's increase in three microsphere formulations can affect characteristics and retain drug release under acidic conditions.

Pancreatic enzyme replacement therapy for people with cystic fibrosis.

Most people with cystic fibrosis (CF) (80% to 90%) need pancreatic enzyme replacement therapy (PERT) to prevent malnutrition. Enzyme preparations need to be taken whenever food is taken, and the dose needs to be adjusted according to the food consumed. A systematic review on the efficacy and safety of PERT is needed to guide clinical practice, as there is variability between centres with respect to assessment of pancreatic function, time of commencing treatment, dose and choice of supplements. This is an updated version of a published review. To evaluate the efficacy and safety of PERT in children and adults with CF and to compare the efficacy and safety of different formulations of PERT and their appropriateness in different age groups. Also, to compare the effects of PERT in CF according to different diagnostic subgroups (e.g. different ages at introduction of therapy and different categories of pancreatic function). We searched the Cochrane Cystic Fibrosis and Genetic Disorders Group Trials Register comprising references identified from comprehensive electronic database searches and handsearches of relevant journals and abstract books of conference proceedings. Most recent search: 07 November 2019. We also searched an ongoing trials website and the websites of the pharmaceutical companies who manufacture pancreatic enzyme replacements for any additional trials. Most recent search: 26 December 2019. Randomised and quasi-randomised controlled trials in people of any age, with CF and receiving PERT, at any dosage and in any formulation, for a period of not less than four weeks, compared to placebo or other PERT preparations. Two authors independently assessed trials and extracted outcome data. They also assessed the risk of bias and quality of the evidence (GRADE) of the trials included in the review. 14 trials were included in the review (641 children and adults with CF), two of these were parallel trials and 12 were cross-over trials. Interventions included different enteric and non-enteric-coated preparations of varying formulations in comparison to each other. The number of participants in each trial varied between 14 and 129. 13 trials were for a duration of four weeks and one trial lasted seven weeks. The majority of the trials had an unclear risk of bias from the randomisation process as the details of this were not given; they also had a high risk of attrition bias and reporting bias. The quality of the evidence ranged from moderate to very low. We mostly could not combine data from the trials as they compared different formulations and the findings from individual trials provided insufficient evidence to determine the size and precision of the effects of different formulations. There is limited evidence of benefit from enteric-coated microspheres when compared to non-enteric coated pancreatic enzyme preparations up to one month. In the only comparison where we could combine any data, the fact that these were cross-over trials is likely to underestimate the level of inconsistency between the results of the trials due to over-inflation of CIs from the individual trials.There is no evidence on the long-term effectiveness and risks associated with PERT. There is also no evidence on the relative dosages of enzymes needed for people with different levels of severity of pancreatic insufficiency, optimum time to start treatment and variations based on differences in meals and meal sizes. There is a need for a properly designed trial that can answer these questions.

Management of Pain, Exocrine and Endocrine Insufficiency in Chronic Pancreatitis

Chronic pancreatitis is the progressive and inflammatory disease which will result in the irreversible destruction and fibrosis of the pancreas. These processes cause chronic pain and pancreatic dysfunctions such as exocrine and endocrine insufficiency. Medical treatment for chronic pancreatitis would be reviewed in this article. Abdominal pain should be accessed by using multidimensional approach including pain intensity, pattern, impact on daily function and quality of life. Abstinence from alcohol and smoking should be strong recommendation. The guideline for analgesic therapy follows the principles of the “pain relief ladder” by World Health Organization. The pancreatic enzyme replacement should be considered when exocrine insufficiency is suspected. Enteric-coated microspheres or mini-microspheres of <2 mm in size with a minimum lipase dose of 40,000–50,000 United States Pharmacopeia are the recommended preparations. These preparations should be taken with main meals. Increasing the oral enzyme dose and the addition of a proton pump inhibitor could be considered in cases of unsatisfactory clinical response. Diabetes mellitus secondary to chronic pancreatitis is classified as Type IIIc diabetes mellitus. Optimal pharmacological treatment has not been established yet but should promote life-style changes, which may improve glucose control and avoid hypoglycemia. In patients with severe malnutrition, insulin therapy is recommended as a first choice. Treatment for chronic pancreatitis can include medication, therapeutic endoscopy, interventional radiology, and surgery. Among them, medical treatment is the most important and should be well understood.

The sinomenine enteric-coated microspheres suppressed the TLR/NF-κB signaling in DSS-induced experimental colitis

Sinomenine is a pure alkaloid with immunosuppressive effects that is extracted from the Chinese medicinal plant Sinomenium acutum. We studied the therapeutic effects of sinomenine on inflammatory bowel disease. In this study, we randomly divided mice into the following ten groups: Control group; DSS-induced colitis group; Salicylazosulfapyridine (SASP)-treated group; Chitosan-treated group; low-, medium-, and high-dose sinomenine-treated and sinomenine enteric-coated microspheres-treated groups. We recorded changes in colon length, disease activity index (DAI), and colon pathology, measured TLR4, MyD88, SIGIRR, NF-κB p65 protein levels and inflammatory serum cytokine levels.Except for the Control group, the weight of mice in each group decreased, the DAI of the DSS-induced colitis group was significantly higher than the other groups, and the DAIs of the sinomenine- and sinomenine enteric-coated microspheres-treated groups were significantly lower than that of the SASP-treated group. TLR4, MyD88, NF-κB p65 and proinflammatory cytokine expressions decreased dose dependently in the sinomenine and sinomenine enteric-coated microspheres-treated groups and were generally lower in the sinomenine enteric-coated microspheres groups. However, SIGIRR and anti-inflammatory IL-10 expressions exhibited the opposite pattern. Based on the superior therapeutic effect, sinomenine enteric-coated microspheres might regulate TLR/NF-κB signaling and would be beneficial for an effective and safe therapy of inflammatory bowel disease.

Pancreatic enzyme replacement therapy for people with cystic fibrosis.

Most people with cystic fibrosis (80% to 90%) need pancreatic enzyme replacement therapy to prevent malnutrition. Enzyme preparations need to be taken whenever food is taken, and the dose needs to be adjusted according to the food consumed. A systematic review on the efficacy and safety of pancreatic enzyme replacement therapy is needed to guide clinical practice, as there is variability between centres with respect to assessment of pancreatic function, time of commencing treatment, dose and choice of supplements. This is an updated version of a published review. To evaluate the efficacy and safety of pancreatic enzyme replacement therapy in children and adults with cystic fibrosis and to compare the efficacy and safety of different formulations of this therapy and their appropriateness in different age groups. Also, to compare the effects of pancreatic enzyme replacement therapy in cystic fibrosis according to different diagnostic subgroups (e.g. different ages at introduction of therapy and different categories of pancreatic function). We searched the Cochrane Cystic Fibrosis and Genetic Disorders Group Trials Register comprising references identified from comprehensive electronic database searches and handsearches of relevant journals and abstract books of conference proceedings. Most recent search: 15 July 2016.We also searched an ongoing trials website and the websites of the pharmaceutical companies who manufacture pancreatic enzyme replacements for any additional trials. Most recent search: 22 July 2016. Randomised and quasi-randomised controlled trials in people of any age, with cystic fibrosis and receiving pancreatic enzyme replacement therapy, at any dosage and in any formulation, for a period of not less than four weeks, compared to placebo or other pancreatic enzyme replacement therapy preparations. Two authors independently assessed trials and extracted outcome data. They also assessed the risk of bias of the trials included in the review. One parallel trial and 12 cross-over trials of children and adults with cystic fibrosis were included in the review. The number of participants in each trial varied between 14 and 129 with a total of 512 participants included in the review. All the included trials were for a duration of four weeks. The included trials had mostly an unclear risk of bias from the randomisation process as the details of this were not given; they also mostly had a high risk of attrition bias and reporting bias.We could not combine data from all the trials as they compared different formulations. Findings from individual studies provided insufficient evidence to determine the size and precision of the effects of different formulations. Ten studies reported information on the review's primary outcome (nutritional status); however, we were only able to combine data from two small cross-over studies (n = 41). The estimated gain in body weight was imprecise, 0.32 kg (95% confidence interval -0.03 to 0.67; P = 0.07). Combined data from the same studies gave statistically significant results favouring enteric-coated microspheres over enteric-coated tablets for our secondary outcomes stool frequency, mean difference -0.58 (95% confidence interval -0.85 to -0.30; P < 0.0001); proportion of days with abdominal pain, mean difference -7.96% (95% confidence interval -12.97 to -2.94; P = 0.002); and fecal fat excretion, mean difference -11.79 g (95% confidence interval -17.42 to -6.15; P < 0.0001). Data from another single small cross-over study also favoured enteric-coated microspheres over non-enteric-coated tablets with adjuvant cimetidine in terms of stool frequency, mean difference -0.70 (95% confidence interval -0.90 to -0.50; P < 0.00001). There is limited evidence of benefit from enteric-coated microspheres when compared to non-enteric coated pancreatic enzyme preparations up to one month. In the only comparison where we could combine any data, the fact that these were cross-over studies is likely to underestimate the level of inconsistency between the results of the studies due to over-inflation of confidence intervals from the individual studies.There is no evidence on the long-term effectiveness and risks associated with pancreatic enzyme replacement therapy. There is also no evidence on the relative dosages of enzymes needed for people with different levels of severity of pancreatic insufficiency, optimum time to start treatment and variations based on differences in meals and meal sizes. There is a need for a properly designed study that can answer these questions.

Development of enteric-coated microspheres of embelin for their beneficial pharmacological potential in ulcerative colitis

The aim of the present study is to develop embelin-loaded enteric-coated microspheres and investigate their pharmacological potential in acetic acid induced ulcerative colitis. The optimized formulation of embelin-loaded microspheres has shown significant sustained release of embelin. Further this formulation significantly reduced the ulcer activity score and oxidative stress, and attenuated the inflammatory changes. Thus it may be concluded that embelin-loaded enteric-coated microspheres have shown delayed release capacity than plain embelin and exerts colon ulcer protective effect in rats.

In vitro cytotoxicity and in vivo efficacy of 5-fluorouracil-loaded enteric-coated PEG-crosslinked chitosan microspheres in colorectal cancer therapy in rats

Purpose: Microspheres of chitosan (CS) crosslinked with polyethylene glycol (PEG) were prepared by emulsion crosslinking followed by solvent evaporation technique. The formulations were characterized and subjected to in vitro and in vivo tests to assess cell growth, changes in cell morphology and activities by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on human HT-29 colon cancer cell lines.Methods: In vivo activity was evaluated for dimethyl hydrazine-induced colorectal cancer in albino male Wistar rats. Biochemical and histological parameters were evaluated to understand their effectiveness for colon cancer therapy.Results: The 5-FU immediate release (IR) formulations suspended in sodium carboxymethyl cellulose (SCMC) produced an immediate cytotoxic effect, whereas microspheres inhibited the proliferation of tumor cells to induce apoptosis over an extended time. Minimum inhibitory concentration (IC50) values for both standard plain 5-FU and 5-FU-loaded microspheres were, respectively, 5.00 ± 0.004 µg/mL and 165 ± 1.9 µg/mL which showed the improved safety profile of the microsphere formulation. Tissue distribution showed high concentration of 5-FU in colon that was higher than IC50 required to stop the growth or death of colon cancer cells from the colonic dysplasia in Duke’s Stage A. Significant reduction in tumor volume and multiplicity was observed with increased levels of liver enzymes in animals when treated with standard 5-FU formulation compared to 5-FU-loaded microspheres. Elevated levels of serum albumin, creatinine, leukocytopenia and thrombocytopenia were observed in animals for the standard 5-FU formulation.Conclusion: The PEG-crosslinked CS microspheres of this study slowly released 5-FU up to 24 h to colonic region and enhanced the antitumor activity.

Pancreatic enzyme replacement therapy for pancreatic exocrine insufficiency in the 21(st) century.

Restitution of normal fat absorption in exocrine pancreatic insufficiency remains an elusive goal. Although many patients achieve satisfactory clinical results with enzyme therapy, few experience normalization of fat absorption, and many, if not most, will require individualized therapy. Increasing the quantity of lipase administered rarely eliminates steatorrhea but increases the cost of therapy. Enteric coated enzyme microbead formulations tend to separate from nutrients in the stomach precluding coordinated emptying of enzymes and nutrients. Unprotected enzymes mix well and empty with nutrients but are inactivated at pH 4 or below. We describe approaches for improving the results of enzyme therapy including changing to, or adding, a different product, adding non-enteric coated enzymes, (e.g., giving unprotected enzymes at the start of the meal and acid-protected formulations later), use of antisecretory drugs and/or antacids, and changing the timing of enzyme administration. Because considerable lipid is emptied in the first postprandial hour, it is prudent to start therapy with enteric coated microbead prior to the meal so that some enzymes are available during that first hour. Patients with hyperacidity may benefit from adjuvant antisecretory therapy to reduce the duodenal acid load and possibly also sodium bicarbonate to prevent duodenal acidity. Comparative studies of clinical effectiveness of different formulations as well as the characteristics of dispersion, emptying, and dissolution of enteric-coated microspheres of different diameter and density are needed; many such studies have been completed but not yet made public. We discuss the history of pancreatic enzyme therapy and describe current use of modern preparations, approaches to overcoming unsatisfactory clinical responses, as well as studies needed to be able to provide reliably effective therapy.

Preparation and characterization of biodegradable or enteric-coated microspheres containing the protease inhibitor camostat

We have produced biodegradable or enteric-coated microspheres containing camostat mesylate, a protease inhibitor, using a water-oil-water emulsion solvent evaporation method. The characteristics of the microspheres were determined. When polylactic acid, a biodegradable polymer, was used as a wall material, the optimized microsphere obtained showed a loading efficiency of almost 95% and had a mean diameter of 30 microm. This microsphere showed a sustained-release profile, with nearly 25% of drug being released at seven days in a dissolution test. When hypromellose acetate succinate (AS-HG type, with a high content of succinyl group) was used as an enteric wall material, optimized microspheres showed a loading efficiency of almost 80%. In this case, pH 3.0 citrate buffer was used as an internal aqueous phase, and citrate buffer containing 0.5% polyvinylalcohol was used as the external aqueous phase. These microspheres showed a rapid release profile in pH 6.8 buffer, whereas the release was extremely slow in pH 1.2 buffer. Hypromellose acetate succinate microspheres were also prepared containing 10% (w/w) N-benzoyl-dl-arg-4-nitroanilide as a model substrate for trypsin, with or without 5% (w/w) camostat. These microspheres were incubated in pH 6 or 7 buffer containing trypsin at 37 degrees C. When camostat was included in the microspheres, the substrate was protected from attack by trypsin, while in the absence of camostat, the released substrate was immediately attacked by trypsin to produce the degradation product N-benzoyl-dl-arginine.

Preparation and In Vivo Efficacy Study of Pancreatin Microparticles as an Enzyme Replacement Therapy for Pancreatitis

Deficiency manifestations because of pancreatic insufficiency are treated by oral administration of pancreatic enzymes. As pancreatic enzymes get denatured in hostile acidic conditions of stomach, this investigation was aimed at formulating multiparticulates of pancreatic enzymes coated with enteric polymers such as eudragit L100, cellulose acetate phthalate, and hydroxyl propyl methyl cellulose phthalate, which will circumvent gastric inactivation in addition to providing optimal mixing with chyme. Pancreatin microspheres were prepared by emulsification phase separation by nonsolvent addition and solvent evaporation techniques. This process was optimized for core : coat ratio (1:0.5), stirrer speed (350–400 rpm), dispersant concentration, and amount of nonsolvent added to precipitate microspheres. Optimized formulations were assessed for % enzyme content, acid resistance, flow properties, particle size, particle morphology (by standard electron microscopy), compatibility of drug and polymer in formulation (by differential scanning calorimetry), in vitro release kinetics, and in vivo efficacy study in pancreatitis-induced animal model. Capsules containing enteric-coated pancreatin microspheres offered adequate protection to enzymes and prevented their denaturation in acidic environment. Developed multiparticulate dosage forms promoted effective mixing, instant and complete in vitro release compared with marketed tablets.

Dietary Counseling Versus Dietary Supplements for Malnutrition in Chronic Pancreatitis: A Randomized Controlled Trial

Up to 50% of patients with chronic pancreatitis (CP) are malnourished. There are limited data on the role of dietary intervention in improving the nutritional status of such patients. The aim was to compare the efficacy of medium chain triglyceride (MCT)-enriched commercial dietary supplements with dietary counseling for homemade food in the management of malnutrition in patients with CP. In a randomized controlled trial, consecutive undernourished patients with CP (body mass index [BMI] <18.5 kg/m(2)) at a tertiary care hospital were randomized to receive either dietary counseling for regular homemade food or commercial MCT-enriched dietary supplements for a period of 3 months to compensate for the dietary calorie deficit. All patients received standard management for CP including pancreatic enzyme supplements. Primary outcome measure was improvement in BMI. Sixty malnourished patients with CP were randomized to counseling group (n = 29; mean age, 32 +/- 10 years; male, 83%) and supplementation group (n = 31; mean age, 28 +/- 10 years; male, 84%). BMI increased in both the counseling group and supplementation group (17.2 +/- 1.7 vs 18.1 +/- 1.8 kg/m(2), P = .001; 16.7 +/- 1.6 vs 18.2 +/- 1.6 kg/m(2), P = .001). There were similar improvements in triceps skinfold thickness, dietary intake, fecal fat, and pain score during a period of 3 months in both groups. There was, however, no significant difference between the counseling and supplementation groups with regard to any of the outcome measures. Dietary counseling for a balanced homemade diet is as good as commercial food supplements in improving malnutrition in patients with CP.

Immunity development following oral vaccination against Actinobacillus pleuropneumoniae in a mouse model

Porcine contagious pleuropneumonia caused by Actinobacillus pleuropneumoniae (Ap) is a deadly disease in pigs. In this work, we attempt to determine immunogenic properties of an oral Ap vaccine in a mouse model. Formalin-inactivated, whole-cell Ap suspension is included in two vaccine formulations: the classic injectable form with aluminium adjuvant and the oral form encapsulated into enteric-coated polymer microspheres. Two groups of mice, each vaccinated with one of the vaccines, are subjected to immunomorphology investigations in comparison with the non-vaccinated control group. Experimental results reveal pronounced systemic immunity and serum antibodies in the group vaccinated by injection. The orally vaccinated group demonstrated more expressed local immunity and mucous antibodies than control group. However, in this group, some tolerance induction occurred in the lungs during the first two vaccinations. We thus developed the means of overcoming primary tolerance, which might become a highly promising approach in improving the potency of oral vaccines.

Combining unprotected pancreatic enzymes with pH-sensitive enteric-coated microspheres does not improve nutrient digestion in patients with cystic fibrosis

To assess the efficacy of combining unprotected powder enzymes and oral enteric-coated microsphere (ECM) and to ECM alone in treating nutrient maldigestion in patients with cystic fibrosis. Patients were randomly assigned into 2 consecutive, 2-week phases; ECM alone, and ECM plus unprotected powder enzymes. Fecal fat, energy, and nitrogen output were compared with intake at the end of each phase. Two-tailed, paired t tests were performed to compare outcomes. The mean age of the 14 patients (3 girls) was 5.7 +/- 3.2 years (range, 1.9 to 13.4 years). There was no significant difference in percent malabsorption of fat (15.6% vs 18.2%), energy (13.3% vs 13.4%), or nitrogen (11.8% vs 11.3%) between phases. The addition of powder enzymes to ECM did not improve nutrient maldigestion compared with ECM alone.

Treatment of pancreatic exocrine deficiency.

In treating pancreatic exocrine insufficiency the diagnosis of a cause, wherever possible, is a first step. If there is an obstructing lesion, then its relief may be curative. Adequate management depends on dietary manipulation and enzyme replacement. A reduction in fat intake, with accentuation of protein and carbohydrate consumption, is recommended. For enzyme replacement, enteric-coated microspheres are required, taken with adequate acid-suppression with a proton-pump inhibitor. The enzyme supplements, using standard preparations of pancreatin, usually of porcine source, may be as much as 4 to 8 tablets per meal and should be taken with food. Endocrine insufficiency usually requires insulin.

Recognizing and diagnosing pancreatic insufficiency in infants.

1. Peter Francis Belamarich, MD 1. Einstein College of Medicine-Children’s Hospital at Montefiore Bronx, NY 1. Exocrine Pancreatic Dysfunction. Cystic Fibrosis. Gaskin K. In: Walker WA, Durie PR, Hamilton JR, Walker-Smith JA, Watkins JB, eds.Pediatric Gastrointestinal Disease, Hamilton, Ontario, Canada: BC Decker Inc;.2000;:1353–1369 2. Pancreatic Function Tests. Huynh H, Couper R. In: Walker WA, Durie PR, Hamilton JR, Walker-Smith JA, Watkins JB, eds.Pediatric Gastrointestinal Disease, Hamilton, Ontario, Canada: BC Decker Inc.2000;:1515–1528 3. Hereditary and Childhood Disorders of the Pancreas. Lopez MJ, Grand RJ. In: Feldman MH, Sleisenger MH, Scharschmidt BF, eds.Sleisenger and Fordtran’s Gastrointestinal and Liver Disease Philadelphia, Pa: WB Saunders.1998;:782–808 Pancreatic insufficiency (PI) is uncommon among infants, but it is important to recognize. Early diagnosis followed by oral enzyme replacement therapy can avert the significant morbidity that follows upon severe malnutrition in infancy. In addition, for the majority of infants who have PI and subsequently are found to have cystic fibrosis, early diagnosis allows genetic counseling to be offered and can help prevent progression of associated pulmonary disease. The pathophysiology of pancreatic insufficiency is complex. Malabsorption results from inadequate secretion of the approximately 20 enzymes and cofactors derived from the pancreatic acini as well as from insufficient bicarbonate secretion from the ductal epithelium. Without adequate bicarbonate to neutralize gastric acid, whatever limited pancreatic lipase is available cannot function optimally, and bile salt micellization of dietary fat droplets also is impaired. Thus, fat digestion takes a “double hit,” and fat malabsorption becomes a prominent clinical feature of PI. Protein maldigestion and malabsorption are also substantial, but they are more commonly subclinical. Quantitative studies of pancreatic enzyme secretion have shown that the pancreas has a tremendous functional reserve. Significant fat malabsorption does not occur until lipase secretion is below 2% of normal values. Thus, clinically apparent PI represents not mild or …

Pancreatic dysfunction and treatment options.

Pancreatic steatorrhea and pancreatic diabetes are the dominant symptoms of patients in the decompensated stage of chronic pancreatitis (CP). In this stage, the nutritional state is greatly disturbed and hypoglycemia and labile infection are involved. Pancreatic enzyme replacement therapy is the principal treatment method for pancreatic steatorrhea. Before initiating this therapy, dietary fat intake must be determined and pancreatic lipase and bicarbonate secretion function must be evaluated. Upper small intestinal pH is regulated by gastric acid secretion, and abnormal gastric emptying changes lipolysis. In addition, precipitation of bile acids in the upper small intestine and ileal brakes due to undigested fats and carbohydrates must be considered. Porcine pancreatin, bacterial lipase, and acid-resistant fungal lipase are used as enzymes for replacement therapy. Conventional, entero-coating, and enteric-coated microsphere preparations of porcine pancreatin are available for treatment and are formulated to protect against gastric acids, to dissolve enzymes at optimum pH, and to be emptied simultaneously with food from the stomach. Gastric acid secretion suppressants, such as H2 blockers or a proton pump inhibitor, can also be used concomitantly with pancreatin preparations. In consideration of both strengths and weaknesses of these preparations, types and dosages of enzyme replacement therapy should be carefully prescribed, and fecal fats should be examined repeatedly by a simple and rapid method during treatment. Attention should also be paid to changes in body weight and nutritional indices (e.g., nutritional parameters, fat-soluble vitamins). The relationship between carbohydrate maldigestion/malabsorption in CP patients and treatment of pancreatic diabetes are topics for future research.

A new experimental chronic pancreatitis model in the dog: Effect of enzymatic replacement with an enteric-coated microsphere formulation (Eurobiol® 25.00 I.U.)

A new experimental chronic pancreatitis model in the dog: Effect of enzymatic replacement with an enteric-coated microsphere formulation (Eurobiol® 25.00 I.U.)

Effect of Superdisintegrant on Antigen Release from Enteric-Coated Antigen Microspheres

AbstractThe effect of incorporation of a superdisintegrant into an oral enteric-coated antigen microsphere (EW) delivery system was studied. The mixture of antiken and sodium starch glycolate (SSG, Explotab®) was applied onto 25- to 30-mesh nonpareil beads followed by coating with polymethacrylic acid-ethylacrylate. (PMA-EA, Eudragit® L-30D). Lipopolysaccharide (LPS) was used as a model antigen. The amount of antigen released from the ECAMs in dissolution medium as a function of time was determined by a size-exclusion HPLC method with UV detection. The level of superdisintegrant incorporated was optimized by adding different amount of SSG onto the beads. Study results indicated 12% (w/w) SSG provided the significantly faster release of LPS than other formulations. The time of the beads with SSG incorporated began to break apart the enteric film was 1.24, 1.26, 1.34, 1.58 and 1.86 min for 12%. 9%, 5%, 3%, and 1% superdisintegrant added formulation, respectively. The disintegrating time of SSG incorporated ...

A double-blind, placebo-controlled randomized trial evaluating the efficacy of enteric-coated pancreatin microsphere therapy in patients with non-resectable malignant tumours of the pancreatic head region

A double-blind, placebo-controlled randomized trial evaluating the efficacy of enteric-coated pancreatin microsphere therapy in patients with non-resectable malignant tumours of the pancreatic head region

Plasma lipid concentrations in children with cystic fibrosis: the value of a high-fat diet and pancreatic supplementation

Impaired digestion of dietary fat is an almost universal feature of cystic fibrosis (CF) which results in low concentrations of essential fatty acids in plasma lipids. We have evaluated the effect of a high-lipid diet and pancreatic enzyme supplementation, using enteric-coated microsphere preparations, on plasma lipid concentrations in paediatric CF patients. Absorption of dietary lipid was comparable between control and CF subjects. This resulted in plasma cholesterol, triacylglycerol, total phosphatidylcholine and individual phosphatidylcholine molecular species concentrations in CF patients which were in the same range as those in controls. Normal values for these variables were also found in patients with clinically detectable liver disease. These results show that present dietary management of CF patients supports normal plasma lipid concentrations.