Enteric-coated Tablets Research Articles

Pharmacokinetic and Pharmacodynamic Profile of a Novel Phospholipid Aspirin Formulation.

Aspirin is one of the most widely used medicines. Although aspirin is commonly utilized for the treatment of several medical conditions, its broadest uptake is for the prevention of recurrent ischemic events in patients with atherosclerotic disease. Its mechanism of action of inhibiting platelet activation via blockade of thromboxane A2 production is unique and is not covered by any other antiplatelet agents. While plain, uncoated, immediate-release aspirin is used in acute settings to help assure rapid absorption, enteric-coated aspirin formulations dominate current chronic use, particularly in North America, including for secondary prevention of cardiovascular events. The unmet needs with current aspirin formulations include a high risk of gastrointestinal (GI) adverse events with plain aspirin, which enteric-coated formulations are not able to overcome, and subject to erratic absorption leading to reduced drug bioavailability. These observations underscore the need for aspirin formulations with a more favorable safety and efficacy profile. Phospholipid-aspirin complex (PL-ASA) is a novel formulation designed to address these needs. It is associated with reduced local acute GI injury compared with plain aspirin, and predictable absorption resulting in more reliable platelet inhibition compared with enteric-coated tablets. This review explores the rationale and pharmacologic profile of PL-ASA intended to address the unmet needs for aspirin therapy.

Pharmacokinetics and food impact assessment of ademetionine enteric-coated tablet as an endogenous substance drug in healthy Chinese volunteers.

Ademetionine 1,4-Butanedisulfonate (SAMe) enteric-coated tablets are widely used for treatment of pre-cirrhotic and cirrhotic intrahepatic cholestasis, as well as intrahepatic cholestasis of pregnancy (ICP), but incomplete clinical data and interference from endogenous substances pose numerous challenges for clinical trial of ademetionine. The objective of this study was to evaluate the pharmacokinetic profile of SAMe enteric-coated tablets and to assess its food impact and safety in healthy Chinese subjects. A randomized, open-label, single-dose study was carried out to determine the pharmacokinetics of SAMe enteric-coated tablets administered in both fasted and postprandial conditions. Baseline collection and data adjustment were required to reduce the effect of endogenous substances. Relevant pharmacokinetic data from subjects administered the reference formulation will be disclosed and utilized in this thesis. Twenty-four subjects with a body mass index (BMI) of 19-24kg/m2 were enrolled in the study and all completed the trial. The impact of food on the drug was noticeable, with faster absorption in the fasting group (Tmax , 4.50±1.07 and 7.50±1.58 for the fasting and postprandial groups, respectively) but higher exposure in the postprandial group (AUC0-inf , 4021.02±3377.13 and 5087.28±3539.26 for the fasting and postprandial groups, respectively). No serious adverse effects were observed in the fasted and postprandial conditions. The pharmacokinetic profile of SAMe enteric-coated tablets in healthy Chinese subjects was partially complemented in this study. SAMe enteric-coated tablets showed promising safety in fasted and postprandial conditions. However, the impact of food on the drug was significant and might access to the absorption site and affect biochemical reactions.

Pharmacokinetic Study and Toxicity of Leukovir: A New Combined Drug for the Treatment of Multiple Sclerosis

Leukovir, an enteric-coated tablet, is the original drug product for internal use. The well-known nucleosides cladribine and ribavirin are the active ingredients of the drug product leukovir. Pharmacokinetic parameters of the drug product for the internal use of leukovir active ingredients have been established. The cladribine half-absorption period was t1/2a = 49.5 h, C0 = 276.4 μg/ml, Cmax = 6.0 μg/ml. Distribution and accumulation parameters (Vd, Vss and AUC) have indicated that the drug distribution between the blood cells and blood plasma takes place in the same way, irrespective of the dosage form. Cladribine half-life period is t1/2e = 0.62 hours. The molecule total clearance and average lifetime in the body in the case of subcutaneous drug administration are approximately the same. Ribavirin is characterized by a half-absorption period of t1/2a = 0.71 h, C0 = 115.6 μg/ml and Cmax = 75.5 μg/ml. Ribavirin total volume of distribution (Vd = 1.3 l/kg) and stationary volume of distribution (Vss = 1.64 l/kg) were practically similar to leukovir when administered subcutaneously. The AUC value = 504.2 μg h/ml, which is 2.5 times less than that in the case of drug form administration. Leukovir was regarded as slightly toxic in an acute toxicity study. The risk of cumulation for this drug product is low.

Analysis of Therapeutic Effect of Mesalazine Enteric-coated Tablet Combined with Bifidum Triple Viable Capsule in Treatment of Ulcerative Colitis

Analysis of Therapeutic Effect of Mesalazine Enteric-coated Tablet Combined with Bifidum Triple Viable Capsule in Treatment of Ulcerative Colitis

Development of an orally delivered GLP-1 receptor agonist through peptide engineering and drug delivery to treat chronic disease

Peptide therapeutics are increasingly used in the treatment of disease, but their administration by injection reduces patient compliance and convenience, especially for chronic diseases. Thus, oral administration of a peptide therapeutic represents a significant advance in medicine, but is challenged by gastrointestinal instability and ineffective uptake into the circulation. Here, we have used glucagon-like peptide-1 (GLP-1) as a model peptide therapeutic for treating obesity-linked type 2 diabetes, a common chronic disease. We describe a comprehensive multidisciplinary approach leading to the development of MEDI7219, a GLP-1 receptor agonist (GLP-1RA) specifically engineered for oral delivery. Sites of protease/peptidase vulnerabilities in GLP-1 were removed by amino acid substitution and the peptide backbone was bis-lipidated to promote MEDI7219 reversible plasma protein binding without affecting potency. A combination of sodium chenodeoxycholate and propyl gallate was used to enhance bioavailability of MEDI7219 at the site of maximal gastrointestinal absorption, targeted by enteric-coated tablets. This synergistic approach resulted in MEDI7219 bioavailability of ~ 6% in dogs receiving oral tablets. In a dog model of obesity and insulin resistance, MEDI7219 oral tablets significantly decreased food intake, body weight and glucose excursions, validating the approach. This novel approach to the development of MEDI7219 provides a template for the development of other oral peptide therapeutics.

Effect of acupuncture for regulating spleen and stomach on aspirin resistance in patients with type 2 diabetes mellitus: a randomized controlled trial

To observe the effect of acupuncture for regulating spleen and stomach on aspirin resistance in patients with type 2 diabetes mellitus (T2DM) and explore the effect mechanism. A total of 68 T2DM patients complicated with aspirin resistance were randomized into an observation group and a control group, 34 cases in each one. On the base of the conventional treatment for diabetes, aspirin enteric-coated tablets were prescribed for oral administration, 100 mg each time, once daily in the control group. In the observation group, on the basis of the treatment as the control group, acupuncture was used for regulating spleen and stomach at Zhongwan (CV 12), Zusanli (ST 36), Yinlingquan (SP 9), Hegu (LI 4), etc., once daily. The treatment for 1 week was as one course and 4 courses of treatment were required totally in two groups. Before and After treatment, the indexes of platelet function (platelet aggregation rate [PAG] and salicylic acid concentration), the indexes of vascular endothelial function (6-keone prostaglandin F1α[6-keto-PGF1α], thromin B2 [TXB2] and cyclooxysynthase-2 [COX-2]), blood glucose (fasting plasma glucose [FPG], 2 h plasma glucose [2h PG] and glycosylated hemoglobin [HbA1c]), insulin resistance index (HOMA-IR), blood lipid indexes (total cholesterol [TC], triacylglycerol [TG], high-density lipoprotein cholesterol [HDL-C] and low-density lipoprotein cholesterol [LDL-C]) and the total score of TCM symptoms were observed in the patients of two groups. Clinical therapeutic effect and safety was compared in the patients between the two groups after treatment and the recurrence rate of cardiocerebrovascular events was followed up 6 months after treatment. After treatment, PAG, salicylic acid concentration, TXB2, COX-2, FPG, 2h PG, HbA1c, HOMA-IR, LDL-C, TC, TG and the total scores of TCM symptoms were all reduced as compared with those before treatment in the two groups (P<0.01, P<0.05), and 6-keto-PGF1αand HDL-C were increased as compared with those before treatment in the two groups (P<0.01, P<0.05). In comparison with the control group, the aforementioned indexes in the observation group were all improved significantly (P<0.01). The total effective rate was 91.2% (31/34) in the observation group, higher than 70.6% (24/34) in the control group (P<0.05). In follow up visit, the recurrence rate of cardiocerebrovascular events was 14.7% (5/34) in the observation group, lower than 29.4% (10/34) in the control group (P<0.05). The therapies were safe and had no obvious adverse reactions in both two groups. Acupuncture for regulating spleen and stomach combined with aspirin enteric-coated tablets relieve insulin resistance and reduces blood glucose and lipid as well as the recurrence rate of cardiocerebrovascular events in the patients with T2DM, which is probably related to the regulation of insulin resistance and the improvement of vascular endothelial function. This combined therapy achieves the better effect on aspirin resistance as compared with simple aspirin enteric-coated tablets.

Formulation and development of Serratiopeptidase enteric coated tablets and analytical method validation by UV Spectroscopy.

Serratiopeptidase (SRP) is a proteolytic enzyme that emerged as one of the most potent anti-inflammatory and analgesic drugs. The purpose of the present study was to formulate and evaluate enteric-coated tablets for SRP and investigate their stability using a simple and validated analytical method by ultraviolet (UV) spectroscopy. The colloidal silicon dioxide (2.50%), sodium starch glycolate (3.44%), and crospovidone (2.50%) were used as appropriate excipients for the development of core part of tablets. To protect the prepared tablets from acidic environment in the stomach, white shellac, castor oil, HPMC phthalate 40, and ethyl cellulose were used. The seal coating and enteric coating attained were 2.75% and 6.74%, respectively. SRP was found to be linear at 265 nm in the concentration range of 25–150 µg/mL. The results revealed that our developed method was linear (R2 = 0.999), precise (RSD % = 0.133), and accurate (% recovery = 99.96–103.34). The formulated SRP tablets were found to be stable under accelerated conditions as well as under room temperature for 6 months (assay %: >97.5%). The in vitro drug release study demonstrated that enteric-coated tablets were able to restrict SRP release in both acidic environments: 0.1 N HCl and simulated gastric fluid (pH 1.2). Moreover, at 60 minutes, the formulated SRP tablets revealed 13.0% and 8.98% higher drug release in phosphate buffer (pH 6.8) and simulated intestinal fluid (pH 6.8), respectively, compared to the marketed tablet formulation. This study concludes that enteric-coated tablets of SRP with higher drug release in the intestine can be prepared and examined for their stability using validated analytical technique of UV spectroscopy.

Enteric-coated bacteriophage tablets for oral administration against gastrointestinal infections

Intestinal Pseudomonas aeruginosa is highly problematic in immunocompromised patients such as those in intensive care units in hospitals. Phage therapy is an attractive alternative or supplementary therapy to antibiotics as it not only kills multidrug-resistant bacteria, but also minimises the disruption of gut microflora. Solid oral dosage forms (i.e., tablets) have the potential to effectively deliver viable phages to the gastrointestinal tract, but formulation studies have been scarce. In this study, Pseudomonas-targeting phage PEV20 was used as a model to produce tablets suitable for oral delivery by utilising industry-scale tablet compression and tablet coating machines. Phage tablets were produced by (i) spray drying of phages, (ii) direct compression of the phage powders into tablets, and then (iii) tablet coating. The resulting phage tablets had negligible phage titre reduction throughout the process and passed the British Pharmacopeia tests, including friability, weight variation, disintegration and dissolution of the tablets as well as weight gain and disintegration (in 0.1 M HCl and pH 7.4 phosphate buffer) of coated tablets. The developed formulation method can be utilised to produce tablets containing other phages and phage cocktails that are effective against enteric bacterial infections.

Doppler Ultrasound under Image Denoising Algorithm in the Diagnosis and Treatment of Fetal Growth Restriction Using Aspirin Combined with Low-Molecular-Weight Heparin.

Objective This study explored the clinical application value of image denoising algorithm combined with Doppler ultrasound imaging in evaluation of aspirin combined with low-molecular-weight heparin (LMWH) on fetal growth restriction (FGR). Method A two-stage image denoising by principal component analysis (PCA) with local pixel grouping (LPG-PCA) denoising algorithm was constructed in this study. Eighty FGR pregnant women were included in the study, and they were rolled into an experimental group (aspirin enteric-coated tablets + LMWH calcium injection) and a control group (LMWH calcium injection) according to the different treatment plans, with 40 cases in each group. All patients were performed with Doppler ultrasound imaging. The blood flow parameters (BFPs) were recorded and compared before and after the treatment in two groups, including power index (PI), resistance index (RI), high systolic blood flow velocity (S), high diastolic blood flow velocity (D), S/D value, and peak systolic velocity (PSV). In addition, the middle cerebral artery (MCA) BFPs, cerebral placental rate (CPR), amniotic fluid index (AFI) and perinatal outcome (PO) of the two groups were compared. Results The total effective rate of treatment in group A (87.5%) was greatly higher than that in group B (62.5%), showing statistical difference (P < 0.05). The PI (0.72 ± 0.19), RI (0.57 ± 0.17), and S/D values (2.26 ± 0.43) in group A were dramatically lower than those in group B, which were 0.92 ± 0.21, 0.75 ± 0.14, and 2.64 ± 0.45, respectively (P < 0.05), and the AFI was higher (13.71 ± 2.2 cm vs 11.38 ± 2.16 cm) (P < 0.05). The Apgar score (9.17 ± 0.26), weight (3.57 ± 1.08), and gestational age (38.85 ± 2.50) of group A were all higher in contrast to those of group B, which were 7.33 ± 0.25, 2.61 ± 1.13, and 36.18 ± 2.25, respectively (P < 0.05). In addition, the fetal double parietal diameter (2.4 ± 0.9 mm), femur diameter (2.2 ± 0.6 mm), head circumference (1.2 ± 0.4 mm), abdominal circumference (1.3 ± 0.7 mm), and uterine height (0.8 ± 0.3 mm) in group A were obviously superior to those in group B, which were 1.8 ± 0.4 mm, 1.7 ± 0.5 mm, 0.8 ± 0.2 mm, 0.9 ± 0.4 mm, and 0.4 ± 0.6 mm, respectively, showing statistically observable differences (P < 0.05). Conclusion Doppler ultrasound based on image denoising algorithm can accurately evaluate the effect of aspirin combined with LMWH on the improvement of FGR and showed good application value.

Effect of Protamine Zinc Recombinant Human Insulin Mixed Injection Combined with Metformin Enteric-coated Tablet in the Treatment of Type 2 Diabetes Mellitus

Effect of Protamine Zinc Recombinant Human Insulin Mixed Injection Combined with Metformin Enteric-coated Tablet in the Treatment of Type 2 Diabetes Mellitus

Effect of Compound Lactobacillus Acidophilus Tablet Combined with Omeprazole Enteric-coated Tablet on Acute Gastroenteritis

Effect of Compound Lactobacillus Acidophilus Tablet Combined with Omeprazole Enteric-coated Tablet on Acute Gastroenteritis

Efficacy and safety of the Chinese herbal formula Hewei Jiangni recipe for NERD with cold-heat complex syndrome: study protocol for a double-blinded randomized controlled trial

BackgroundProton pump inhibitor (PPI) is effective for the treatment of nonerosive gastroesophageal reflux (NERD), but long-term use of PPI is prone to have complications and recurrence after withdrawal. Traditional Chinese medicine (TCM) can relieve the symptoms of reflux and improve the quality of life. The purpose of this study is to evaluate the safety and efficacy of Hewei Jiangni recipe (HWJNR) in the treatment of NERD with cold-heat complex syndrome, and clarify the mechanism of HWJNR on NERD based on the correlation analysis of intestinal flora and metabolites.MethodsThis is a single-center, randomized controlled, double-blind, placebo-controlled clinical trial in which 72 eligible participants with NERD and TCM syndrome of intermingled heat and cold will be randomly allocated in the ratio of 1:1 to two groups: TCM group and western medicine group. The TCM group will receive HWJNR with omeprazole enteric-coated tablets placebo, while the western medicine group will receive omeprazole enteric-coated tablets with HWJNR placebo. Each group will be treated for 8 weeks. The primary outcome is the score of gastroesophageal reflux disease (GERD) health-related quality of life questionnaire (GERD-Q). Secondary outcomes include SF-36 quality of life scale (SF-36), patient-reported outcomes (PRO) self-rating scale score, syndrome score of TCM, and adverse events. Mechanistic outcome is the correlation analysis of intestinal flora and metabolites from healthy individuals and NERD participants before and after the treatment respectively.DiscussionThe goal of this trial is to investigate the efficacy and safety of HWJNR in the treatment of NERD with cold-heat complex syndrome, and to study the composition structure and metabolite expression profile of intestinal flora in patients with NERD through 16SrRNA sequencing and metabolomic correlation analysis of fecal flora, which makes us identify the dominant links of treatment and reveal the potential mechanism of HWJNR.ChiCTR2000041225. Registered on 22 December 2020

Efficacy of a Viokace Pancreatic Enzyme Protocol for Clearing Occluded Enteral Feeding Tubes: A Quality Assurance Evaluation

Background: A previous retrospective study documented restored patency to 48.2% of occluded enteral feeding tubes using alkalinized Creon pancreatic enzyme capsules. In light of the low efficacy rate, the institutional enteral feeding tube clearance protocol was subsequently revised to incorporate a newly marketed non–enteric-coated Viokace pancreatic enzyme tablet, despite the lack of published data for this indication. Objective: This study aims to evaluate the effectiveness of a Viokace-based alkalinized pancreatic enzyme protocol to clear occluded enteral feeding tubes in a university health system. Methods: This retrospective, cohort quality assurance study included adult and pediatric patients receiving a Viokace-based pancreatic enzyme protocol for enteral feeding tube occlusions in a university health system during a 12-month period. The primary outcome was effectiveness in enteral tube clearance as documented in the electronic medical record. Efficacy of the new protocol was also compared with a Creon-based alkalinized solution using historical data. Results: The Viokace protocol successfully cleared 176 of the 277 (63.5%) occluded enteral feeding tubes occurring in 205 patients included in the analysis. The revised protocol was significantly more effective at clearing occluded enteral feeding tubes (P = 0.0056) than a protocol using Creon pancreatic enzyme capsules. Conclusion: According to this retrospective evaluation, an alkalinized Viokace pancreatic enzyme protocol was effective in clearing 63.5% of occluded enteral feeding tubes. This significantly higher success rate than previously documented with a Creon-based protocol supports the change in pancreatic enzyme formulations in the institutional protocol.

Electronic focusing high-nergy extracorporeal shockwave combined with conventional oral medicine for the treatment of ankylosing spondylitis

To observe the progress of disease activity and sacroiliac joint imaging in patients with ankylosing spondylitis treated by extracorporeal shockwave combined with conventional oral medicine, and find a new safe and effective therapeutic method. The clinical data of 30 patients with ankylosing spondylitis treated from January 2018 to December 2018 were retrospectively analyzed. Including 20 males and 10 females, aged from 18 to 50 years with an average of (34.50±9.60) years. All 30 patients had different degrees of sacroiliac joint bone marrow edema on MRI before treatment. Thirty patients were divided into treatment group and control group according to different treatment methods. Among them, 15 cases in control group were treated with non-steroidal anti-inflammatory drugs and sulfasalazine enteric-coated tablets, for the 15 cases in treatment group, in addition to oral medicine in line with control group, electronic focusing high-energy extracorporeal shockwave therapy was added. The course of disease, age, pre- and post-treatment erythrocyte sedimentation rate, C-reactive protein in the two groups were analyzed; and visual analogue scale (VAS) and spondyloarthritis research consortium Canada (SPARCC) scoring system were used to evaluate the pain of the sacroiliac joint and the structural damage of the sacroiliac joint;Bath ankylosing spondylitis disease activity index (BASDAI) was calculated. All patients were followed up for at least 3 months. One month after treatment, VAS, and SPARCC scores in treatment group were significantly better than in control group (P<0.05). After 1 month of treatment, there was no significant difference in BASDAI, erythrocyte sedimentation rate and C-reactive protein between two groups(P>0.05). VAS, BASDAI, SPARCC, erythrocyte sedimentation rate, and C-reactive protein of all patients after treatment were significantly improved compared with those before treatment (P< 0.01). Electronic focusing high-energy extracorporeal shockwave combined with conventional oral medicine in the treatment of ankylosing spondylitis has a good clinical effect in rapidly relieving pain, improving disease activity, and preventing imaging progress. In addition, it is safe and non-invasive, which is worthy of clinical application.

Efficacy of simvastatin on carotid atherosclerotic plaque and its effects on serum inflammatory factors and cardiocerebrovascular events in elderly patients.

To investigate the efficacy of simvastatin on carotid atherosclerotic plaque (CAP) and its effects on serum inflammatory factors and cardiocerebrovascular events in elderly patients, 130 elderly patients with CAP were randomly divided into observation (n=65) and control groups (n=65). The control group was treated with 75 mg/day aspirin enteric-coated tablets, and the observation group was administered additional 20 mg/day simvastatin. Serum total cholesterol, triglyceride, and high- and low-density lipoprotein cholesterol levels (evaluated via the endpoint method) were determined in both groups. Furthermore, the length, thickness and number of CAPs was measured using color Doppler ultrasonography. In addition, levels of inflammatory biomarkers including high-sensitivity C-reactive protein (hs-CRP), tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), nitric oxide, D-dimer and fibrinogen, as well as change in microemboli count, were also compared After treatment, the observation group exhibited a significant reduction in size, thickness, and number of CAP and intima-media thickness compared with before treatment. However, no significant difference was found in the indicators of CAPs in the control group before and after treatment. The levels of total cholesterol, triglyceride, and low-density lipid cholesterol decreased, while high-density lipid cholesterol increased in the observation group after treatment, with notable changes in the observation group compared with in the control group. Overall response rate was higher in the observation group compared with the control group. TNF-α, IL-6, and hs-CRP levels in the observation group decreased after treatment compared with those before treatment and those in the control group. Furthermore, the rate of microemboli positivity was lower in the observation group than in the control group. Moreover, the overall incidence of acute cardiocerebrovascular events was lower in the observation group than in the control group. Therefore, it was demonstrated that simvastatin can reduce blood lipid levels, decrease the quantity and size of plaques, alleviate inflammatory response, reduce microemboli formation and reduce the risk of cardiocerebrovascular events in elderly patients with CAP.

Clinical Study on Treatment to Ankylosing Spondylitis with Fengshi Qutong Capsule-Diclofenac Sodium Combination

Objective: To discuss the clinical study on Fengshi Qutong capsules combined with diclofenac sodium in the treatment of ankylosing spondylitis. Methods: 80 patients who were treated for ankylosing spondylitis from June 2019 to June 2020 were selected and divided into two groups. The experimental group was treated with Fengshi Qutong capsules combined with diclofenac sodium, and the control group was treated with sulfasalazine enteric-coated tablets. Results: The treatment efficacy, VAS score, BASDAI score, BASFI score, CRP level, TNF-? level, IL-I? level, and the incidence of adverse reactions between the two groups were significantly different (P&lt;0.05). Conclusion: The application of Fengshi Qutong capsules combined with diclofenac sodium in the treatment of patients with ankylosing spondylitis is beneficial to improve the treatment efficacy, reduce the levels of CRP, TNF-?, and IL-I?, reduce the incidence of adverse reactions, and reduce the VAS, BASDAI and BASFI scores, rendering it of important clinical value.

False positive technetium-99m pyrophosphate scintigraphy in a patient with cardiac amyloidosis light chain

Introduction:Patients with cardiac amyloidosis light chain (AL) present with negative Tc-99m pyrophosphate (PYP) scintigraphy (absent or mild heart uptake). On the contrary, patients with cardiac amyloidosis transthyretin (ATTR) present with positive Tc-99m PYP scanning (intensive heart uptake). We present a false positive Tc-99m PYP scintigraphy (grade 2, the heart-to-contralateral ratio is 1.65) in a patient with AL.Patient concerns:A 42-year-old Chinese man complained of effort intolerance, chest discomfort, and short of breath progressively over 1 year. New York Heart Association Class III. Physical examination showed legs swelling. Laboratory revealed elevated brain natriuretic peptide of 23,031 ng/mL (0–88) and Troponin-T of 273.4 ng/mL (0–14).Diagnosis:Cardiac amyloidosis light chain. Evidences: free light chains (FLCs): decreased serum free kappa/lambda ratio of 0.043 (0.31–1.56). Immunofixation electrophoresis: a positive lambda light chain monoclonal protein. Cardiac biopsy: HE: Ambiguity Congo red strain. Myocardial immunofluorescence: positive lambda light chain. Myocardial immunohistochemistry: positive lambda light chain, negative kappa light chain, and TTR.Interventions:Furosemide 40 mg qd, torasemide 20 mg qd, spirolactone 20 mg qd, potassium chloride 10 mL per 500 mL urine, atorvastatin calcium tablet 20 mg qd, aspirin enteric-coated tablets 100 mg qd during the 2-weeks in-hospital.Outcomes:The patient died 2 months later after discharge.Conclusion:False positive Tc-99m PYP scintigraphy may rarely presented in patients with cardiac amyloidosis light chain. So, the clonal plasma cell process based on the FLCs and immunofixation is a base to rule out AL cardiac amyloidosis when we interpret a positive Tc-99m PYP scintigraphy.

Effect of acupuncture on intestinal flora and TLR4 in brain and intestinal tissues in rats with stress gastric ulcer

To observe the effect of acupuncture at "Guanyuan" (CV 4) and "Xiajuxu" (ST 39) on intestinal flora and Toll-like receptors-4 (TLR4) in brain and intestinal tissue in rats with stress gastric ulcer (SGU), and to explore the possible mechanism of acupuncture for SGU. Thirty-one male SD rats were randomly divided into a blank group (n=7), a model group (n=8), an acupuncture group (n=8) and a drug group (n=8). The rats in the model group, acupuncture group and drug group were treated with modified restraint plus water-immersion stress method to establish SGU model. After modeling, the rats in the acupuncture group were treated with acupuncture at "Guanyuan" (CV 4) and "Xiajuxu" (ST 39), 20 min each time, and the needles were twirled for 30 s every 5 min. The rats in the drug group were treated with intragastric administration of 2 mL omeprazole enteric-coated tablets (20 mg/mL). Both the treatments were given once a day for 5 days. After the intervention, the gastric mucosal damage index was calculated by Guth method; the morphological changes of gastric mucosa were observed by HE staining; the diversity of intestinal flora was detected by 16S rDNA high-throughput sequencing; TLR4 contents in brain and intestinal tissues were determined by ELISA. Compared with the blank group, the gastric mucosal damage index was significantly increased in the model group (P<0.01); the morphological changes of gastric mucosa were obvious; the Observed Species index and Shannon index of α diversity index of intestinal flora were decreased (P<0.05); the β diversity showed that the spatial distance between the model group and the blank group was far; the TLR4 contents in the brain and intestinal tissue were increased (P<0.05, P<0.01). Compared with the model group, the gastric mucosal damage index was decreased in the acupuncture group and the drug group (P<0.05); the morphology of gastric mucosa was improved; the Observed Species index and Shannon index of α diversity index of intestinal flora in the acupuncture group was increased (P<0.05), and the Shannon index in the drug group was increased (P<0.05); the β diversity showed that the spatial distance between the acupuncture group and the blank group was close; the TLR4 contents in the brain and intestinal tissues of the acupuncture group were decreased (P<0.01). Compared with the drug group, the contents of TLR4 in the intestinal tissue of the acupuncture group were decreased (P<0.05). Acupuncture at "Guanyuan" (CV 4) and "Xiajuxu" (ST 39) could alleviate SGU in rats, and its mechanism may be related to increasing the diversity of intestinal flora, promoting the disorder of intestinal flora to normal, and reducing the overexpression of TLR4 in brain and intestinal tissues.

Identification and genotoxicity evaluation of potential impurities in rabeprazole sodium using in silico and in vitro analyses

Rabeprazole sodium is a widely used drug for gastrointestinal disorders. Several analytical methods for identifying rabeprazole sodium and its impurities have been reported. However, the genotoxicity of rabeprazole sodium and its impurities is still unclear. Thus, it is necessary to develop analytical methods that can identify the structures of its impurities and evaluate their genotoxicity. Here, we used high-performance liquid chromatography-quadrupole time-of-flight mass spectrometry for identifying the impurities in rabeprazole sodium enteric-coated tablets. Impurities in the samples were matched with synthesized impurities based on the exact mass and secondary mass spectrometry characteristics and then subjected to in silico analysis using the Derek and Sarah software, as well as in vitro genotoxicity evaluations. Our method successfully identified the impurities as 2-[[4-(3-methoxy propane)-3-methyl-N-oxido-2-pyridyl] methyl sulfonyl]-1H-benzimidazole (impurity I), 2-[[4-(3-methoxy propane)-3-methyl-2-pyridyl]methyl sulfonyl]-benzimidazole (impurity II), 2-[[4-(3-methoxy propane)-3-methyl-2-pyridyl] methionyl]-1H-benzimidazole (impurity III), and 2-mercapto benzimidazole (impurity IV). In silico analysis predicted that impurity III demonstrated a structural alert; thus, this impurity was evaluated for in vitro genotoxicity using the Ames test and chromosomal aberration assay. Impurity III at concentrations of 7.5–30 μg/mL had an aberration rate of over 5% with or without S-9 mix. Furthermore, impurity III at concentrations of 40–1000 μg/plate significantly increased the number of mutagenic colonies with or without S-9 mix. These results indicated that impurity III should be regulated to the limit of 0.01%.

Knowledge, Attitude, and Practice of Community Pharmacists Toward Tablet Splitting and Crushing at Omdurman Locality

Background: The splitting or crushing of tablets has many advantages, such as dose flexibility, cost reduction, and ease of swallowing. Despite these benefits, there are many drawbacks to this practice. Pharmacists should be able to make decisions and counsel patients concerning these techniques. Our study aimed to evaluate their knowledge, attitude, and practice about tablet splitting and crushing. Methods: A descriptive cross-sectional survey was carried out among 150 community pharmacists using a validated self-administered questionnaire. A stratified random sampling technique was used to select the participants. The knowledge, attitude, and practice were evaluated. Associations between the variables were tested using the Chi-square method. Results: Out of 147 participants, 67.1% were females. The majority of subjects were between 20 and 30 years of age. About 48% of respondents scored a fair knowledge level and 23% of them were knowledgeable of the subject matter. Furthermore, 51% of pharmacists showed good attitudes, as they do not usually recommend the splitting and crushing of tablet dosage. Moreover, more than half of the participants used alternative formulations for patients who were unable to swallow. Nearly 65% of participants did not encourage tablet splitting to help patients to save money. Almost 80% of them declared that they never advised a patient to split or crush enteric-coated or sustained-release tablets. Moreover, a significant association was found between participants' knowledge and their professional experience. On the other hand, the participants' attitude was significantly associated with their age and training levels. Conclusion: The study showed variable knowledge levels among participants. Nearly 51% of the participating pharmacists showed good attitudes regarding the study subject. Experience, age, and training have a positive effect on the knowledge and attitude of participants.