Five-Flavor Sophora flavescens Enteric-Coated Capsules for Ulcerative Colitis: A Systematic Review and Meta-Analysis of Randomized Clinical Trials

Background. Ulcerative colitis (UC), a chronic inflammatory bowel disease, is characterized by abdominal pain, diarrhea, and mucopurulent bloody stool. In recent years, the incidence and prevalence of UC have been increasing consistently. Five-flavor Sophora falvescens enteric-coated capsule (FSEC), a licensed Chinese patent medicine, was specifically used to treat UC. This review was aimed to assess the effectiveness and safety of FSEC for the treatment of UC. Methods. Six electronic databases were searched from inception to March 2021. Randomized clinical trials (RCTs) comparing FSEC or FSEC plus conventional Western medicine with conventional Western medicine in participants with UC were included. Two authors screened all references, assessed the risk of bias, and extracted data independently. Binary data were presented as risk ratios (RRs) with 95% confidence intervals (CIs) and metric data as mean difference (MD) with 95% CI. The overall certainty of the evidence was assessed by GRADE. Results. We included 15 RCTs (1194 participants, 763 in the FSEC group and 431 in the control group). The treatment duration ranged from 42 to 64 days. Twelve trials compared FSEC with conventional Western medicine, and two trials compared FSEC plus conventional medicine with conventional medicine. Another trial compared FSEC plus mesalazine with compound glutamine enteric capsules plus mesalazine. FSEC showed a higher clinical effective rate (improved clinical symptoms, colonoscopy results, and stools) (RR 1.12, 95% CI 1.05 to 1.20; 729 participants; 8 trials; low-quality evidence) as well as the effective rate of traditional Chinese medicine (TCM) syndromes (RR 1.10, 95% CI 1.01 to 1.20; 452 participants; 5 trials; low-quality evidence) compared to mesalazine. There was no significant difference in the adverse events between FSEC and control groups. Conclusions. FSEC may show effectiveness in UC treatment compared to conventional medicine, and the use of FSEC may not increase the risk of adverse events. Due to the limited number of clinical trials and low methodological quality of the included trials, our findings must be interpreted with discretion.

Enteric Coated Oral Delivery of Hydroxyapatite Nanoparticle for Modified Release Vitamin D3 Formulation

Vitamin D3 (VD) and calcium phosphate play a vital role in bone homeostasis. Factors such as obesity or gastrointestinal problems can render the use of pure VD and calcium phosphate supplements ineffective. This study investigated the possibility of using VD-loaded hydroxyapatite nanoparticles for the codelivery of VD and Ca3(PO4)2. Due to the high affinity of Ca3(PO4)2 for bone tissue, HA is an ideal delivery system to deliver VD to target tissue. Herein, HA nanoparticles were synthesized and loaded with VD using a vacuum evaporation method. The synthesized HA-VD nanoparticles were morphologically and chemically characterized by SEM, FTIR, and TGA. The system exhibited a two-stage release pattern, which includes a first-day burst release (35%) and sustained release for a further ten days. The cytocompatibility and cell penetrative ability of the nanoparticle system were assessed in vitro using preosteoblast cells: the system is nontoxic and well-tolerated. Finally, the VD-loaded HA nanoparticles were coated with a gastroresistant polymer, hypromellose phtalate-55 (HP-55) in order to protect the pH-sensitive HA from degradation at lower pHs. A coaxial electrospray technique was employed to achieve this. In all, the tested HA-VD system is a viable alternative for codelivery of VD, Ca2+, and PO43- to their target tissues.

Sport supplements and the athlete’s gut: a review.

Vigorous or prolonged exercise poses a challenge to gastrointestinal system functioning and is associated with digestive symptoms. This narrative review addresses 1) the potential of dietary supplements to enhance gut function and reduce exercise-associated gastrointestinal symptoms and 2) strategies for reducing gastrointestinal-related side effects resulting from popular sports supplements. Several supplements, including probiotics, glutamine, and bovine colostrum, have been shown to reduce markers of gastrointestinal damage and permeability with exercise. Yet, the clinical ramifications of these findings are uncertain, as improvements in symptoms have not been consistently observed. Among these supplements, probiotics modestly reduced exercise-associated gastrointestinal symptoms in a few studies, suggesting they are the most evidenced-based choice for athletes looking to manage such symptoms through supplementation. Carbohydrate, caffeine, and sodium bicarbonate are evidence-based supplements that can trigger gastrointestinal symptoms. Using glucose-fructose mixtures is beneficial when carbohydrate ingestion is high (>50 g/h) during exercise, and undertaking multiple gut training sessions prior to competition may also be helpful. Approaches for preventing caffeine-induced gastrointestinal disturbances include using low-to-moderate doses (<500 mg) and avoiding/minimizing exacerbating factors (stress, anxiety, other stimulants, fasting). Adverse gastrointestinal effects of sodium bicarbonate can be avoided by using enteric-coated formulations, low doses (0.2 g/kg), or multi-day loading protocols.

Antithrombotic effect of different acetylsalicylic acid drug formulations: is there a difference?

To date, a sufficient volume of clinical studies has been accumulated that have demonstrated a reduced antiplatelet effect of enteric-coated (EC) lowdose acetylsalicylic acid (ASA). Delayed and incomplete absorption from the intestinal alkaline medium, which significantly reduces the bioavailability of drug, is considered the main reason for laboratory aspirin resistance (pseudoresistance) to EC ASA. This phenomenon is of particular importance for patients with acute coronary syndrome, when a quick effect is required, as well as for patients with diabetes and obesity due to additional causes of increased platelet activity, on the one hand, and reduced bioavailability of ASA, on the other. Given the issue of efficacy, the dubious gastroprotective effect and the more pronounced damaging effect on the mucous membrane of small intestine, the use of EC ASA should be avoided, especially in patients with a multifactorial risk of insufficient response to therapy. A good alternative is buffered ASA, which quickly dissolves and is partially absorbed directly in the stomach, having antiplatelet activity comparable to simple ASA and a similar aspirin resistance, is associated with a lower risk of aspirin-induced enteropathy in comparison with ES ASA. In addition, according to a number of small studies and retrospective analyzes, buffered ASA is less likely to cause damage to gastric mucosa compared to EC ASA.

Oral Formulation of Anticancer Agents for Colon Cancer

Aims/Objective: To develop and estimate enteric-coated capsules containing mucoadhesive Microspheres of Capecitabine and Oxaliplatin to treat Colon cancer. Study Design: Box Behnken. Place and Duration of Study: Department of Pharmaceutics, Parul Institute of Pharmacy and Research, Parul University, Vadodara, between 2017 to 2021. Methodology: Capecitabine and Oxaliplatin are used as antineoplastic agents and can be delivered via the oral route of administration. For the estimation of drugs Analytical method has been developed by HPLC. Box Behnken design has been used to optimize Drug: polymer ratio (1:2), Inlet temperature 170ºC, and crosslinking agent with a 0.5 ml 1% Gluteraldehyde solution. The microspheres were successfully prepared by using the spray drying technique and evaluated. Results: The results of optimized Capecitabine microspheres were obtained as Particle size 87.91 µm ± 0.274,% yield 57.21± 1.5,% Mucoadhesion 57.21± 1.5,% entrapment efficiency 82.16± 0.725. The results of optimized Oxaliplatin microspheres were obtained as Particle size 99.88µm±0.034,% yield 56.0± 0.088,% Mucoadhesion 87.0± 0.80,% entrapment efficiency 82.61±0.085. The drug content of Capecitabine and Oxaliplatin in the filled capsule was 94.67% ±0.32 and 93.45%±0.712, respectively. % Drug release of Capecitabine and Oxaliplatin in Phosphate buffer pH 7.4 was found to be 94.83±0.22 and 96.94±0.11 respectively after 8 hrs. Stability study at 400C±20C / 75 ± 5 % RH revealed that there was no significant change in disintegration time, drug content and % CDR during 6 months. So, prepared formulation was stable during stability study. MTT assay has been performed on the formulation of Capecitabine and Oxaliplatin microspheres for assessing the % viability of both the drugs on the Caco-2 cell line. Conclusion: The present study confirmed that prepared mucoadhesive microspheres filled with enteric-coated capsules have an antitumor effect on colon cancer cells. The formulation induced high cell death within 48 hours, and less cell viability was obtained compared to API. Six months accelerated Stability study indicates that formulation is fairly stable at storage conditions.

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.