Development of platform technology for gastro-resistant soft gel capsules by using the cross-linking technique

Introduction: Conventional enteric coating is very challenging in soft gel capsules because of shell nature (smooth surfaces and elasticity). Soft gelatin capsules are highly sensitive to temperature, humidity and it can lose their tensile strength during the conventional coating process. Materials and Methods: Enteric soft gel capsules were prepared by addition of enteric polymer in the gelatin shell composition by inducing the cross linking of gelatin through chemical treatment. Results: This dual approach makes the soft gelatin capsules to resist the drug release in stomach and reliably release their contents in the intestine within a predetermined time without affecting the physical properties of soft gel capsules. Conclusions: Enteric effect of soft gel capsules are brought by a specialized synergetic technique which is unique for the molecules which need intestinal drug release.

Formulation and Evaluation of Delayed Release Pellets of Ivabradine Hydrochloride

The aim of preset research work is to formulate and evaluate delayed release pellets of Ivabradine HCl. Pellets are prepared using extrusion-spheronization process and the process parameters are optimized. Polymer coating done with Kollicoat SR 30 D as rate controlling polymer and finally enteric coating done with Eudragit L30D-55. Drug release in formulation F1-F9 studied and it found that the low polymer concentration (2 %) was unable to retard the drug release up to 12 hr so concentration increased batch by batch and finally 12 % coating batch gives desired results which retard the drug release up to 12 hr. also found that the drug release was very low after more % coating than the 12 %. Hence based on that the F5 batch was optimized batch and its found stable during stability study of 1 month.Delayed release pellets of Ivabradine HCl was successfully prepared using Kollicoat SR 30 D as rate controlling polymer.

Stroke Prevention: Little-Known and Neglected Aspects

Combining available therapies has the potential to reduce the risk of stroke by 80% or more. A comprehensive review of all aspects of stroke prevention would be very lengthy; in this narrative review, we focus on some aspects of stroke prevention that are little-known and/or neglected. These include the following: (1) implementation of a Mediterranean diet; (2) B vitamins to lower homocysteine; (3) coordinated approaches to smoking cessation; (4) intensive lipid-lowering therapy; (5) lipid lowering in the elderly; (6) physiologically individualized therapy for hypertension based on renin/aldosterone phenotyping; (7) avoiding excessive blood pressure reduction in patients with stiff arteries; (8) treatment of insulin resistance with pioglitazone in stroke patients with prediabetes and diabetes; (9) impaired activation of clopidogrel in patients with variants of CYP2C19; (10) aspirin pseudoresistance due to enteric coating; (11) rationale for anticoagulation in patients with embolic stroke of unknown source; (12) pharmacologic properties of direct-acting oral anticoagulants that should be considered when choosing among them; (13) the identification of which patients with asymptomatic carotid stenosis are at a high enough risk to benefit from carotid endarterectomy or stenting; and (14) the importance of age in choosing between endarterectomy and stenting. Stroke prevention could be improved by better recognition of these issues and by implementation of the principles derived from them.

Ways to Reduce the Level of Contamination at the Stages of Tableted Chemical Cholera Vaccine Production

Objective of the study was an assessment of the degree of contamination of cholera chemical vaccine at the stages of preparation and determination of the ways to reduce it.Materials and methods. Liquid and lyophilized components of the cholera chemical vaccine used in the study: cholerogen-anatoxin and O-antigens of Vibrio cholerae 569B and V. cholerae M-41 strains, as well as auxiliary substances (sucrose, talc, calcium stearate, starch). Granulation was carried out in a device that works on a fluidized bed principle, GPCG 2 (GLATT, Germany). Subsequent tabletizing of the mixture was performed using MiniTabT compression machine (LUXNER, Germany). Studies were conducted on the evaluation of “microbiological purity” at the stages of manufacturing of the cholera chemical vaccine, tablets coated with an enteric coating. Positive or negative growth of microorganisms on Petri dishes with nutrient media was determined on visual inspection.Results and conclusions. The dynamics of changes in microbial contamination at certain technological stages of vaccine production has been revealed. It is shown that the solutions of antigens in the process of separation are subject to microbial contamination which is associated with the use of ammonium sulfate during precipitation and non-sterile water at the stage of dialysis. Sterility of semi-finished products has been achieved through twophase filtration of choleragen-anatoxin and sterilization of O-antigens of V. cholerae 569B and V. cholerae M-41 strains with flowing steam at (100±1) °C for 30 minutes. In order to decrease microbial contamination at the stage of granulation additional fine filters were installed in the air-supply system. Further on comparative assessment of microbial purity of vaccine batches obtained using both, direct compression and preliminary granulation, was carried out. It has been experimentally demonstrated that granulation of the components of a tablet mixture of cholera vaccine leads to a decrease in the level of bacterial contamination and improves the microbiological purity of the finished dosage form.

Development of Duloxetine Hydrochloride Tablets for Delayed and Complete Release Using Eudragit L 100

The purpose of the research was to optimize the preparation of duloxetine hydrochloride (duloxetine HCl) delayed release tablets. Duloxetine HCl produces a toxic substance called alpha-naphthol when duloxetine HCl is in contact with gastric fluid. Thus, duloxetine HCl when given orally needed a protective enteric coating that disable the delivery of duloxetine HCl in gastric fluid while enabling the drug delivery only in small intestine. Four different core tablets were prepared by direct compression technique, and the one which displayed quick disintegration and dissolution was chosen for enteric coating. The compressed tablets were enteric coated by dip coating technique. Since subcoating is required to safeguard the enteric coating, the core tablets were subcoated by using polymer HPMC K15M and then enteric coated with Eudragit L 100. The prepared tablets were assessed for the entire precompression and postcompression characteristics. FTIR study revealed the existence of all prominent peaks signifying its compatibility and authenticity. The in vitro studies showed that enteric-coated tablets were capable of restricting release in acidic media. The formulation F8 was optimised with 5% and 15% increase in weight of seal coat and enteric coat with good dissolution profile. Stability studies revealed that the optimized formulation was intact without any deterioration for 3 months. In conclusion, the optimized formulation could resist the drug release in acidic environment of gastrointestinal region and release the drug at a time once the tablet reaches the intestine.