Enteric-coated Capsules Research Articles

Beneficial effect of probiotics supplements in reflux esophagitis treated with esomeprazole: A randomized controlled trial.

BACKGROUNDReflux esophagitis (RE) is a common digestive disorder, and its frequent recurrences cause significant physical pain and are financially burdensome to patients. However, studies on the natural history of treated RE are few. Although proton pump inhibitors (PPIs) as the first-line treatment provide notable symptomatic relief, disordered gut microbiota has been observed among PPI users. Probiotics are commonly administered to patients to regulate the disordered intestinal flora.AIMTo evaluate the therapeutic effects in RE patients treated with a combination of esomeprazole and probiotics [Bacillus subtilis (B. subtilis) and Enterococcus faecium (E. faecium)].METHODSOne hundred and thirty-four RE patients were randomized into two groups of 67 subjects each. The probiotics group was administered with esomeprazole 20 mg b.i.d. and live combined B. subtilis and E. faecium enteric-coated capsules 500 mg t.i.d. for eight weeks; the placebo group was administered with esomeprazole 20 mg b.i.d. and placebo for eight weeks. Subsequently, 12-wk follow-up was carried out on patients who achieved both endoscopic and clinical cure. Endoscopy, reflux diagnostic questionnaire (RDQ), gastrointestinal symptom rating scale (GSRS), and lactulose hydrogen breath test were performed to evaluate the therapeutic effects. A difference of P < 0.05 was considered statistically significant.RESULTSSixty-six patients in the probiotics group and 64 patients in the placebo group completed the 8-wk treatment. The healing rate and RDQ score had no significant difference between the two groups (P > 0.05). However, the GSRS diarrhea syndrome score was decreased significantly in the probiotics group (P = 0.002), and the small intestinal bacterial overgrowth negative rate in the probiotics group was significantly higher than that in the placebo group (P = 0.002). Of 114 endoscopically and clinically cured patients, 96 completed the follow-up. The log-rank test showed that the time to relapse was shorter in the placebo group than in the probiotics group (P = 0.041). Furthermore, the therapy had a significant influence on relapse time, and the risk of relapse in the probiotics group was lower than that in the placebo group at any time point during the 12-wk follow-up (hazard ratio = 0.52, P = 0.033).CONCLUSIONEsomeprazole combined with probiotics (B. subtilis and E. faecium) have a beneficial effect on RE treatment and patient management.

Preclinical evaluation of the maximum tolerated dose and toxicokinetics of enteric-coated lantibiotic OG253 capsules

Clostridium difficile associated disease (CDAD) is the leading infectious cause of antibiotic-associated diarrhea and colitis in the United States. Both the incidence and severity of CDAD have been increased over the past two decades. We evaluated the maximum tolerated dose (MTD) and toxicokinetics of OG253, a novel lantibiotic in development for the treatment of CDAD. OG253 was orally administered to Wistar Han rats as enteric-coated capsules in a one-day dose escalation study, followed by a seven-day repeated dose toxicokinetics study. All three doses of OG253 (6.75, 27 and 108 mg/day) were generally well-tolerated with no treatment-related clinical signs, alterations in body weight or food consumption in both one-day acute tolerability and seven-days repeated dose tolerability and toxicokinetics study. OG253 capsule administration neither significantly alter the weight of organs nor affect the hematology, coagulation, clinical biochemistry parameters and urine pH compared to placebo capsule administered rats. LC-MS/MS analysis did not detect OG253 in the plasma, indicating that OG253 is not absorbed into the blood from the rat gastrointestinal tract. Glandular atrophy of the rectal mucosa was noticed in two out of six rats administered with a high dose of OG253. Surprisingly, we found that OG253 treatment significantly lowered both serum cholesterol and triglyceride levels in both sexes of rats. Overall, there was a 29.8 and 61.38% decrease in the serum cholesterol and triglyceride levels, respectively as compared to placebo-treated rats. The well-tolerated high dose of OG253 (425.7 mg/kg/day) is recommended as the MTD for safety and efficacy studies. Further preclinical study is needed to evaluate the safety profile of OG253 under longer exposure.

Effect of Cihang capsule in treatment of vaginal bleeding after artificial abortion

Objective To investigate the clinical efficacy and safety of Cihang capsule in treatment of vaginal bleeding after artificial abortion, and to provide a reference for the related treatment. Methods From January 2016 to December 2016, 1 000 patients with artificial abortion in the No.2 Hospital of Datong Coal Mine Group Co, Ltd were selected and divided into the control group(488 cases) and the observation group(512 cases) by the random number table method. The patients in the two groups were given doxycycline hyclate enteric-coated capsules to prevent postoperative infection, the observation group was given Cihang capsule at the same time, and the control group was treated with oxytocin. The postoperative vaginal bleeding time, normal menstrual recovery time, blood loss and the adverse reactions in the two groups were observed, the clinical efficacy of the two groups was compared. Results The total effective rate of the observation group was 94.14%, which was higher than 89.55% of the control group (χ2=7.076, P<0.05). The cure rate of the observation group was 56.84%, which was higher than 47.95% of the control group (χ2=7.910, P<0.05). The duration of bleeding and the recovery time in the observation group were (5.26±0.41)d and (27.31±4.03)d, respectively, which were shorter than those in the control group[(8.03±0.57)d and (40.16±5.14)d], the differences were statistically significant(t=88.585, 44.106, all P<0.05). During treatment, the observation group had no adverse reactions, the control group found 5 cases with different degrees of abdominal pain, and the incidence rate of adverse reaction between the two groups had statistically significant difference (χ2=5.272, P<0.05). Conclusion Cihang capsule can effectively shorten bleeding time and normal menstrual recovery time in patients with vaginal bleeding after artificial abortion, reduce the amount of vaginal bleeding, and with less adverse reactions, it is worthy of further clinical application. Key words: Abortion, induced; Vagina; Hemorrhage; Cihang capsule; Oxytocin; Bleeding time

Clinical efficacy of Wenweishu granule combined with triple therapy in the treatment of gastric ulcer and its effect on clinical symptoms and serological indexes

Objective To investigate the clinical effect of Wenweishu granule combined with triple therapy on gastric ulcer and its influence on clinical symptoms and serological indexes. Methods From January 2016 to January 2017, 60 patients with gastric ulcer were divided into control group and observation group with 30 cases in each group. The patients in the control group were treated with omeprazole enteric-coated capsule 20 mg + amoxicillin capsule 1 g + clarithromycin 0.5 g, and the patients in the observation group were treated with Wenweishu granule on the basis of the control group. The clinical efficacy, clinical symptom score, serological indexes, and adverse reactions were compared between the two groups after treatment. Results After treatment, the clinical symptom score of abdominal pain, acid reflux, abdominal distension, anorexia of the observation group were (1.07±0.28), (1.54±0.36), (1.03±0.18), (0.93±0.27), which were better than those of the control group (P 0.05). Conclusion Wenweishu granule combined with triple therapy has a good therapeutic effect on gastric ulcer, which can effectively improve the effective rate of treatment, improve the clinical symptoms and serological indicators of the patients, with high safety, worthy of clinical application. Key words: Wenweishu granule; Triple therapy; Gastric ulcer; Clinical efficacy

Clinical study on self-made Jianpi-Yiqi decoction in the treatment of chronic atrophic gastritis

Objective To evaluate the efficacy of self-made Jianpi-Yiqi decoction in the treatment of chronic atrophic gastritis (CAG). Methods A total of 100 patients with CAG who met the inclusion criteria were randomly divided into two groups, 50 in each group. The control group received oral omeprazole enteric-coated capsules and the observation group oral Jianpi-Yiqi decoction. Both groups were treated for 8 weeks. The clinical efficacy, proliferating cell nuclear antigen (PCNA), B cell lymphoma-2 (Bcl-2), TNF-α and PCNA, Bcl-2 mRNA expression were evaluated and compared. Results The total effective rate was 92.0% (46/50) in the observation group and 80.0% (40/50) in the control group. The difference between the two groups was statistically significant (χ2=9.623, P=0.031). The total effective rate of endoscopy was 94.0% (47/50) in the observation group and 74.0% (37/50) in the control group. The difference between the two groups was statistically significant (χ2=11.254, P=0.026). After treatment, the PCNA (4.36 ± 1.95 μg/mg vs. 8.62 ± 2.43 μg/mg, t=8.465), Bcl-2 (3.06 ± 1.63 μg/mg vs. 7.54 ± 1.73 μg/mg, t=9.316), TNF-α (4.13 ± 1.86 μg/mg vs. 7.29 ± 2.14 μg/mg, t=9.473) in the observation group were significantly lower than those in the control group (P<0.05). After treatment, the PCNA (0.053 ± 0.033 vs. 0.074 ± 0.023, t=2.316), Bcl-2 (0.004 ± 0.003 vs. 0.006 ± 0.002, t=5.842) mRNA expression in the observation group were significantly lower than those in the control group (P<0.05). Conclusions The self-made Jianpi-Yiqi decoction can down-regulate the expression of PCNA, Bcl-2 and TNF-α protein and PCNA and Bcl-2 mRNA in gastric mucosa, improve the symptoms of CAG patients and improve clinical efficacy. Key words: Gastritis, atrophic; Jianpi-Yiqi decoction; Proliferating cell nuclear antigen; Bcl-2; Tumor necrosis factor-alpha; Gastroscopy; Gene expression

Rectal Diclofenac administration for prevention of post-Endoscopic Retrograde Cholangio-Pancreatography (ERCP) acute pancreatitis. Randomized prospective study.

Post-Endoscopic Retrograde Cholangio-Pancreatography pancreatitis (PEP) is a relevant (1-4%) complication of biliopancreatic operative endoscopy. Rectal nonsteroidal anti-inflammatory drugs (specifically, 100 mg of diclofenac) have shown promising prophylactic activity in PEP. The aim of our prospective study is to report whether prophylactic oral versus rectal suppository versus intramuscular diclofenac versus placebo are able to reduce the incidence and the severity of ERCP-induced pancreatitis. In this randomized, double-blinded, prospective study, 100 patients (49 male, 51 female), similar with regard to indication for ERCP, were enrolled between January 2016 and November 2017 to undergo ERCP in the Section of General and Thoracic Surgery of University Hospital of Palermo. They were randomized into five groups, respectively 20 patients with placebo by mouth; 20 patients with 50 mg diclofenac sodium enteric-coated capsules by mouth; 20 with 100 mg rectal suppository diclofenac, 20 with 75 mg/3 ml intramuscular diclofenac sodium, 20 with 75 mg/3 ml intramuscular diclofenac sodium and 20 with 75 mg/3 ml intravenous diclofenac. All drugs were administered 30 to 90 minutes before ERCP. All clinical data were collected one day before and 2, 12 and 24 hour after ERCP. Data were prospectively collected and to demonstrate the preventive effect of rectal diclofenac on PEP, a two-by-two table and chi-square test with Yates correction were used: the incidence of PEP was significantly lower (p < 0.001) in the rectal diclofenac group respect to other groups and, in the same way, the incidence of post-ERCP pain was significantly lower in the rectal diclofenac group than in the other groups (p = 0.001) and patients discharge was consequently earlier (p < 0.01). 100 mg dose rectal diclofenac administered 30-60 minutes before ERCP can effectively prevent PEP.

Protective Effects of Live Combined B. subtilis and E. faecium in Polymicrobial Sepsis Through Modulating Activation and Transformation of Macrophages and Mast Cells.

Aims: Clinical studies showed that the use of probiotics during critical illness reduced nosocomial infection and improved clinical outcome. However, the functional mechanisms of probiotics is remains unclear. Therefore the aim of current study is to explore the protective effects and understand the underlying mechanisms for the beneficial effects of live combined Bacillus subtilis and Enterococcus faecium (LCBE) in cecal ligation puncture (CLP)-induced sepsis.Methods and Results: Seven-week-old C57BL/6J mice were divided into three groups: sham group (6 mice), CLP-control group (20 mice, pretreatment with saline for 7 days before CLP surgery) and CLP-probiotics group (14 mice, pretreatment with LCBE enteric-coated capsules for 7 days before CLP surgery). In survival experiment, mice were monitored for 7 days after CLP. After the procedure, mice were sacrificed, and, serum, and peritoneal lavage fluid were collected and intestinal ileal samples were harvested.Results: Our results showed that the mortality was significantly reduced in mice CLP-probiotics group vs. CLP-control group (P < 0.05). Also, treatment CLP-probiotics group decreased the injury scores CLP-probiotics group when compared to CLP-control group. Additionally, levels of pro-inflammatory cytokines IL-6 and TNF-α levels in the serum and intestinal ileal tissues of CLP-probiotics group were reduced when compared to CLP-control group (P < 0.05). However, no significant differences in anti-inflammatory levels of IL-10 and TGF-β1 were observed between CLP-control and CLP-probiotic groups. Furthermore, our experiments showed that that probiotic treatment suppressed the macrophage activation and transformation from M-type to M1-type, inhibited the mast cells (MCs) degranulation, and activation of AKT (kinase B) pathway.Conclusion: In conclusion, our data shows that probiotics have a protective role in CLP septic mice through reducing intestinal inflammation, altering macrophage polarization and MCs degranulation, and regulating AKT signaling.Significance and Impact of Study: This study demonstrated the protective effects and mechanisms involved in the protective role of live combined Bacillus subtilis and Enterococcus faecium (LCBE) in CLP-induced septic mice model.

New formulation of ibuprofen on absorption-rate: A comparative bioavailability study in healthy volunteers.

Background:Enteric-coated capsules are solid dosage forms which are designed to bypass the stomach and release the drug in the small intestine. This study was done to compare pharmacokinetics of ibuprofen tablet and ibuprofen as enteric-coated capsule using sodium alginate beads.Methods:A crossover randomized study was performed on 12 healthy volunteers receiving a single dose of regular ibuprofen tablet (200 mg) and enteric-coated capsule (200 mg). The washout time between the periods was one month. Pharmacokinetic and pharmacodynamic blood samples were collected for 16 hours following treatment. High-performance liquid chromatography (HPLC) method used the following specifications: C18 column with 4.6 mm diameter & 25 mm length, the fluorescent detector of excitation and emission wavelengths were 224 and 290 nm, respectively.Results:After a single oral dose of ibuprofen formulations, the median times to maximum concentration were 60 and 240 minutes in ibuprofen tablet (200 mg) and enteric-coated capsule, respectively. The maximum levels for the participants receiving ibuprofen tablet and enteric-coated capsule were 11.71±1.3 and 10.32±4.19 µg/mL, respectively. The pharmacokinetic (PK) modeling data showed the area under curve (AUC) to be 61.51 hours & 86.62 hours for the group receiving the tablet and the capsule, respectively.Conclusion:According to the results, in is concluded that enteric coating may delay the onset of ibuprofen effect and increases the duration of action. This formulation has advantages over the conventional drug delivery systems as it lengthens the dosing intervals and also increases patient compliance for chronic pain.

Tremella polysaccharide: The molecular mechanisms of its drug action.

Tremella fuciformis is an edible medicinal mushroom well known as "Yiner" or "Baimuer" in China and has been used as a Chinese herb for many years. T. fuciformis polysaccharide (TFPS) has been identified as a major bioactive component. Different experimental conditions can obtain different TFPS fractions, which makes TFPS a mixture of different polysaccharides with the molecular weight ranging from 5.82×105Da to 3.74×106Da. The monosaccharides detected in TFPS include mannose, xylose, fucose, glucuronic acid, glucose, and galactose. One characterized TFPS chemical structure consists of a linear (1→3)-linked α-d-mannose backbone with highly branched β-d-xylose, α-d-fucose and β-d-glucuronic acid as the side chains. TFPS shows multiple physiological and healthy promoting effects including immunomodulation, antitumor, anti-oxidation, anti-aging, hypoglycemic, hypolipidemic, neuroprotection, and other effects. As a result, "Tremella Polysaccharide Enteric-coated Capsules" was approved by Chinese Food and Drug Administration (SFDA) in 2002 for treating cancer patients with leukopenia induced by chemotherapy and radiotherapy. It is also used as adjuvant drug for treating chronic persistent hepatitis and chronic active hepatitis. In this chapter, 113 independent studies involving in biochemical, pharmacological, and clinical studies of TFPS during the past 46 years (1972-2018) on the base of PubMed, CNKI (China National Knowledge Infrastructure) and Wanfang database search are summarized. TFPS shows efficacy for all types of human diseases in the reported clinical studies. The structure, molecular mechanisms of the immunomodulation, antitumor, anti-oxidation, anti-aging, hypoglycemic, hypolipidemic, preclinical and clinical efficacy are discussed to provide a general picture of TFPS as a clinically used drug.

Effects of Xiaoshuan Enteric-Coated Capsule on White and Gray Matter Injury Evaluated by Diffusion Tensor Imaging in Ischemic Stroke

Xiaoshuan enteric-coated capsule (XSECC) is a drug approved by the Chinese State Food and Drug Administration for the treatment of stroke. This study was to investigate the effects of XSECC on white and gray matter injury in a rat model of ischemic stroke by diffusion tensor imaging (DTI) and histopathological analyses. The ischemia was induced by middle cerebral artery occlusion (MCAO). The cerebral blood flow measured by arterial spin labeling was improved by treatment with XSECC on the 3rd, 7th, 14th and 30th days after MCAO. Spatiotemporal white and gray matter changes in MCAO rats were examined with DTI-derived parameters (fractional anisotropy, FA; apparent diffusion coefficient, ADC; axial diffusivity, λ//; radial diffusivity, λ⊥). The increased FA was found in the XSECC treatment group in the corpus callosum, external capsule and internal capsule, linked with the decreased λ//, λ⊥ and ADC on the 3rd day and reduced ADC on the 30th day in the external capsule, suggesting XSECC reduced the axon and myelin damage in white matter after stroke. The relative FA in the striatum, cortex and thalamus in XSECC treatment group was significantly increased on the 3rd, 7th, 14th and 30th days accompanied by the increased λ// on the 3rd day and reduced relative ADC and λ⊥ on the 30th day, indicating that XSECC attenuated cell swelling and membrane damage in the early stage and tissue liquefaction necrosis in the late stage in gray matter after stroke. Additionally, XSECC-treated rats exhibited increased mean fiber length assessed by diffusion tensor tractography. Moreover, histopathological analyses provided evidence that XSECC relieved nerve cell and myelin damage in white and gray matter after stroke. Our research reveals that XSECC could alleviate white and gray matter injury, especially reducing nerve cell damage and promoting the repair of axon and myelin after ischemic stroke.

Dermatophagoides farinae allergen encapsule for oral immunotherapy with HDM allergic rhinitis

It is well known that the house dust mites (HDMs) are the most common and potent inhalant allergens world-wide and the allergen immunotherapy (AIT) can efficaciously and safely ameliorate the allergic symptoms. Different formulations and routes of HDMs AIT have been achieved symptomatic improvement with mite allergic rhinitis (AR) and/or asthma. The object of the present article is to observe the efficacy and safety of oral immunotherapy (OIT) by enteric-coated capsules (EC) of Dermatophagoides farinae allergen (Df) with mite AR. A year of single blind placebo trial was applied. A total of 54 AR patients aged 25.8 in average with/without asthma and skin prick test (SPT) positive in HDMs were selected into either active or placebo groups. The OIT started with 5 days of dose rush induction, succeeded by a maintenance dose for 12 months. The efficacy of the treatment was assessed by symptomatic evaluation and laboratory in vivo and in vitro parameters of pre-immunotherapy (pre-IT) and post-immunotherapy (post-IT) statistically. The patients each received a total accumulative dose of 16 715BU Df protein nitrogen, and 87.5% (21/24) subjects achieved symptomatic improvement. The post-IT symptom scores decreased (t=11.07, P&lt;0.001); visual analog scale (VAS) decreased (t=10.68, P&lt;0.001); number of patients required symptom-medication decreased from 23/24 to 3/24 cases (c2=33.57, P&lt;0.001); SPT wheal sizes of both Df and Dp significantly reduced (Df t=2.64, P=0.015 and Dp t=6.01, P&lt;0.001); nasal provocation test (NPT) with the antigen tolerance elevated more than 3 times (c2=9.65, P=0.008). The only unchanged parameter was the tIgE levels (P=0.07). The parameters of placebo group were changed but not significant statistically or negligible. There were no local or general adverse reactions in both groups happened in the one year course of OIT. It is concluded that the newly designed formulation and route of clinical administration by Df EC OIT with AR were comparable to that of Df sublingual IT. The new formulation is more convenient and promising approach to treat AR.

In vitro and in vivo evaluation of coated capsules for colonic delivery

The aim of the present study was to design and evaluate the combination of pH-dependent and time-dependent polymers for colon-specific drug delivery using response surface methodology (RSM). Theophylline was selected as a model drug and Eudragit® FS 30D (pH-dependent), Eudragit® RL 30D and Eudragit® RS 30D (as time-dependent) were used as coating polymers. Dissolution test was carried out in different pH media mimicking the transit of capsules from stomach to colon. The morphology of coated capsules was evaluated by scanning electron microscopy (SEM). In vivo studies were performed using fluorescent imaging in order to trace the movement of capsules in gastrointestinal (GI) tract. The results of in vitro studies showed that optimized formulation had suitable release profile at different pH values, which were in agreement with the predicted value by RSM. The SEM images revealed that surface coated capsules were smooth and also fluorescent imaging indicated that coated capsules disintegrated at the targeted colon region. These findings provide novel insights for the development of enteric coated capsule in order to specify drug delivery to colon.

Dual route vaccination for plague with emergency use applications

Here, we report a dual-route vaccination approach for plague, able to induce a rapid response involving systemic and mucosal immunity, whilst also providing ease of use in those resource-poor settings most vulnerable to disease outbreaks. This novel vaccine (VypVaxDuo) comprises the recombinant F1 and V proteins in free association. VypVaxDuo has been designed for administration via a sub-cutaneous priming dose followed by a single oral booster dose and has been demonstrated to induce early onset immunity 14 days after the primary immunisation; full protective efficacy against live organism challenge was achieved in Balb/c mice exposed to 2 × 104 median lethal doses of Yersinia pestis Co92, by the sub-cutaneous route at 25 days after the oral booster immunisation. This dual-route vaccination effectively induced serum IgG and serum and faecal IgA, specific for F1 and V, which constitute two key virulence factors in Y. pestis, and is therefore suitable for further development to prevent bubonic plague and for evaluation in models of pneumonic plague. This is an essential requirement for control of disease outbreaks in areas of the world endemic for plague and is supported further by the observed exceptional stability of the primary vaccine formulation in vialled form under thermostressed conditions (40 °C for 29 weeks, and 40 °C with 75% relative humidity for 6 weeks), meaning no cold chain for storage or distribution is needed.In clinical use, the injected priming dose would be administered on simple rehydration of the dry powder by means of a dual barrel syringe, with the subsequent single booster dose being provided in an enteric-coated capsule suitable for oral self-administration.

Multiple Oral Insulin (ORMD-0801) Doses Elicit a Cumulative Effect on Glucose Control in T2DM Patients

Efforts to overcome the narrow therapeutic index of subcutaneously delivered insulin, have propelled the development of orally delivered alternatives. The enteric-coated ORMD-0801 oral insulin capsule has been shown to provide effective glucose control in both type 1 and type 2 diabetes patients. In this single-center, randomized, double-blind, placebo-controlled, three-way crossover study, 31 adult T2DM patients were treated with a placebo capsule during the first three days of three 1-week treatment periods, followed by five days of treatment with an oral placebo (n=31) or a 460 IU insulin capsule, delivered one (qd; n=20), two (bid; n=21) or three (tid; n=20) time per day. Run-in (Days 1-3) vs. treatment (Days 4-8) period continuous glucose monitoring (CGM) data were compared, as were pre- vs. post-treatment insulin and c-peptide levels. Patients were of a mean age of 57.5±7.8, and most were male (61.3%) and Caucasian (80.6%). Mean placebo-adjusted change from baseline in 24-hour glucose (all run-in days vs. all treatment days) ranged from -7.65 mg/dL for qd to -9.91 mg/dL for tid, with a more dramatic change observed in subjects with higher glucose (&amp;gt;190 mg/dL; n=17) at baseline (-12.44 mg/dL (qd) and -18.43 (tid)). Pre- vs. posttreatment and placebo vs. active treatment c-peptide and insulin ratios were similar across all regimens. ORMD-0801 was well tolerated and did not elicit any serious adverse effects. The vast majority of hyperglycemic events were recorded during placebo treatment (n=27), while hypoglycemic events were evenly distributed across treatment groups (≤5/group). Thus, multiple-dose ORMD-0801 regimens safely provide for improved glucose control, which is expected to be enhanced with more extended treatment. Its impact may be of particular benefit to patients uncontrolled by current drug regimens. Disclosure R. Eldor: Consultant; Self; Oramed Pharmaceuticals, Inc.. Speaker's Bureau; Self; AstraZeneca, Sanofi, Boehringer Ingelheim Pharmaceuticals, Inc., Merck Sharp &amp; Dohme Corp., Novo Nordisk Inc., Medtronic. J. Neutel: None. K.E. Homer: None. M. Kidron: Employee; Self; Oramed Pharmaceuticals, Inc..

Xiaoshuan enteric-coated capsule alleviates cognitive impairment by enhancing hippocampal glucose metabolism, hemodynamics and neuroplasticity of rat with chronic cerebral hypoperfusion

Chronic cerebral hypoperfusion (CCH) is identified as a critical risk factor of dementia in patients with cerebrovascular disease. Xiaoshuan enteric-coated capsule (XSECC) is a compound Chinese medicine approved by Chinese State Food and Drug Administration for promoting brain remodeling and plasticity after stroke. The present study aimed to explore the potential of XSECC to improve cognitive function after CCH and further investigate the underlying mechanisms. CCH was induced by bilateral common carotid artery occlusion (BCCAO) in rats. XSECC (420 or 140 mg/kg) treatment remarkably reversed BCCAO-induced cognitive deficits. Notably, after XSECC treatment, magnetic resonance angiography combined with arterial spin labeling noninvasively demonstrated significantly improved hippocampal hemodynamics, and 18F-FDG PET/CT showed enhanced hippocampal glucose metabolism. In addition, XSECC treatment markedly alleviated neuropathologies and improved neuroplasticity in the hippocampus. More importantly, XSECC treatment facilitated axonal remodeling by regulating the phosphorylation of axonal growth related proteins including protein kinase B (AKT), glycogen synthase kinase-3β (GSK-3β) and collapsin response mediator protein-2 (CRMP2) in the hippocampus. Taken together, the present study demonstrated the beneficial role of XSECC in alleviating BCCAO-induced cognitive deficits by enhancing hippocampal glucose metabolism, hemodynamics and neuroplasticity, suggesting that XSECC could be a useful strategy in cerebral hypoperfusion state and dementia.

Effect of different course of omeprazole in the treatment of laryngopharyngeal reflux

Objective:To compare the efficacy and safety of omeprazole in the treatment of laryngopharyngeal reflux. Method:One hundred and sixty patients with laryngopharyngeal reflux in our hospital from March 2015 to January 2017 (diagnosis treatment for 8 weeks) were selected and randomly divided into group A, B, C, D, with 40 cases in each group. Each group of patients were treated with omeprazole enteric-coated capsules (20mg, Bid) for 1, 2, 3 and 4 months, respectively. The reflux symptom index(RSI), reflux finding score(RFS) score, and 24h intraesophageal pH-metry , pepsin detection were compared between the four groups before treatment, at the end of treatment, at 1 month and 2 months after treatment. The efficacy and side effects were evaluated.Result:With the increase of treatment course, patient's RSI and RFS score, 24h pH-metry <4.0 percentage, pepsin positive rate decreased gradually, and there was a significant difference between before and after treatment. After treatment, there was a statistical significance in group B and group A, group C and group B. There was no significant difference between group D and group C. After the end of treatment and up to 2 months of follow-up, the RSI and RFS scores gradually increased and 24h Ph-metry <4.0 percentage, pepsin positive rate increased in group A and B,and those were not significantly different in group C and group D. With the increase of treatment duration, the effective rate of treatment increased, which was 67.5%, 80.0%, 90.0% and 95.0%, respectively. The difference was statistically significant, but the adverse effects did not increase (P>0.05).Conclusion:Omeprazole is safe and effective in the treatment of laryngopharyngeal reflux. The symptoms and signs of the patients are obviously improved during the 5 months of the course, and the condition is relatively stable and the recurrence rate is low.

Bacillus subtilis and Enterococcus faecium enteric-coated capsules combined with mesalazine for treatment of patients with ulcerative colitis: Efficacy and impact on serum levels of SOD, MDA, interleukins, and TNF-α

<i>Bacillus subtilis</i> and <i>Enterococcus faecium</i> enteric-coated capsules combined with mesalazine for treatment of patients with ulcerative colitis: Efficacy and impact on serum levels of SOD, MDA, interleukins, and TNF-α

A Randomized Double-Blind Placebo-Controlled Trial to Evaluate Prophylactic Effect of Traditional Chinese Medicine Supplementing Qi and Hemostasis Formula on Gastrointestinal Bleeding after Percutaneous Coronary Intervention in Patients at High Risks.

Objective To evaluate the clinical efficacy of traditional Chinese medicine (TCM) supplementing Qi and hemostasis formula on gastrointestinal (GI) bleeding after percutaneous coronary intervention (PCI) and thus find out the optimal therapeutic regimen to reduce incidence of GI bleeding without increase of major adverse cardiovascular events (MACEs). Methods In the randomized, double-blinded, controlled trial, 117 participants who underwent PCI were enrolled and evenly distributed into treatment arm (59) and control arm (58). Numerous end points were assessed including the primary endpoint of GI bleeding and MACEs and secondary endpoint of thromboelastogram (TEG) (mainly MAadp, inhibition of ADP, and inhibition of AA) and TCM syndrome score during the follow-up phase of 90 days. Results Incidence of bleeding including GI bleeding and MACE did not differ significantly between two arms (28.82% in treatment arm versus 24.44% in control). However, on both days 30 and 90, TCM treatment remarkably reduced the TCM syndrome total score with notable alteration (P<0.05) except for some parameters such as pulse manifestation. When it came to TEG, however, MAADP increased significantly on day 30 in control arm, accompanied by a notable descending in inhibition rate of ADP pathway (both P<0.01). Conclusion (1) Supplementing Qi and hemostasis formula is equal to Pantoprazole Sodium Enteric-Coated Capsule in hemostasis and gastric mucosal protection; (2) supplementing Qi and hemostasis formula is superior to Pantoprazole Sodium Enteric-Coated Capsule in improving TCM syndrome manifestation possibly through the multitarget mechanism; (3) interference on clopidogrel of supplementing Qi and hemostasis formula might be much less than Pantoprazole Sodium Enteric-Coated Capsule due to the potential CYP450-independent mechanism. This trial is registered with ChiCTR1800014485.

A Study on the Curative Effect of Omeprazole in the Treatment of Ulcerative colitis

Objective:to study the clinical efficacy of Omeprazole in the treatment of ulcerative colitis. Methods: 40 cases of ulcerative colitis were randomly divided into two groups, each with 20 cases. The control group was treated with Mesalazine granules, and the treatment group was treated with above-mentioned medicine and oral Omeprazole enteric-coated capsules at the same time. Results: the treatment effect of ulcerative colitis in the treatment group was significantly superior to that in the control group; the time of colitis symptom disappeared was significantly shorter than that in the control group, and the recurrence number after treatment was significantly less than that in the control group. Conclusion: Omeprazole has very obvious treatment effect in the treatment of ulcerative colitis.

Liquid Nanosize Emulsion-Filled Enteric-Coated Capsules for Colon Delivery of Immunosuppressant Peptide.

Present study aims at solubilizing slightly water-soluble peptide into a nanosize emulsion which is filled into a hard gelatin capsule in the form of preconcentrate. Further, liquid-filled capsule was dip-coated with ethyl cellulose and Eudragit S100 for colon targeting. An in vitro release profile was studied for selected formulations, i.e., Formulation A (5mg ethyl cellulose and 40mg Eudragit S100), Formulation B (10mg ethyl cellulose and 30mg Eudragit S100), and Formulation C (10mg ethyl cellulose and 20mg Eudragit S100). Formulations B and A showed an immediate release after 5 and 6h, respectively, which represents ileo-ceacal transit time. The nanosize of emulsion, i.e., below 100nm, was confirmed by transmission electron microscopy. Also, a phase transition of nanosize emulsion from water in oil to oil in water on dilution with water was observed through TEM. This novel approach of filling poorly water-soluble protein in solubilized form of nanosize emulsion preconcentrate into coated hard gelatin capsules for colon targeting has been reported first time. This approach could be a breakthrough for the better management of local intestinal pathologies.