The aim of present study was to prepare buffered tablets of acid labile drug, Rabeprazole sodium for oral administration using buffering agents to protect a drug from gastric fluid. Rabeprazole belongs to a class of antisecretory compounds (substituted benzimidazole proton-pump inhibitors) that do not exhibit anticholinergic or histamine H2-receptor antagonist properties, but suppress gastric acid secretion by inhibiting the gastric H+, K+ATPase at the secretory surface of the gastric parietal cell. Rabeprazole blocks the final step of gastric acid secretion. The tablets were prepared by direct compression and wet granulation method. The formulations contain water soluble buffers such as sodium bicarbonate and trisodium phosphate as well as water insoluble buffers as magnesium oxide, magnesium hydroxide and calcium carbonate and crospovidone as superdisintegrant. Preformulation studies like angle of repose, bulk density, tapped density, Carr’s index, hausner’s ratios, DSC and drug/excipient compatibility study were conducted and evaluated for hardness, friability, weight variation, drug content, disintegration and in-vitro dissolution. In the present study, pH of F6 batch was found to be optimum and disintegration time is 42 sec. The drug release was found to show maximum drug release in case of F6 with 99.3% in 60 minutes. In case of stability studies study of the optimized batch, all the results were found to be satisfactory and within limits. There were no significant changes after the period of 1 month study. Keywords: Rabeprazole sodium, Proton-pump inhibitors, Buffered tablet, Superdisintegrants, Buffering agents
No abstract
The barrier properties of the topmost layer of the skin, stratum corneum have significant limitations for successful systemic delivery of a wide range of therapeutic molecules, especially macromolecules and genetic material. One solution is to utilize microneedles (MNs), which are capable of painlessly traversing through the stratum corneum and directly translocating protein drugs into the systematic circulation. This strategy involves the use of micron sized needles fabricated from different materials and using different geometries to create transient aqueous conduits across the skin. Microneedles in isolation, or in combination with other enhancing strategies, have been shown to dramatically enhance the skin permeability of numerous therapeutic molecules including biopharmaceuticals either in vitro, ex vivo or in vivo. MNs can be designed to incorporate appropriate structural materials as well as therapeutics or formulations with tailored physicochemical properties. This platform technique has been applied to deliver drugs both locally and systemically in applications ranging from vaccination to diabetes and cancer therap. As an alternative to hypodermic needles, coated polymer microneedles (MNs) are able to deliver drugs to subcutaneous tissues after being inserted into the skin. The dip-coating process is a versatile, rapid fabricating method that can form coated MNs in a short time. However, it is still a challenge to fabricate coated MNs with homogeneous and precise drug doses in the dip-coating process. This review article focuses on recent and potential future developments in microneedle technologies. This will include the detailing of progress made in microneedle design, an exploration of the challenges faced in this field and potential forward strategies to embrace the exploitation of microneedle methodologies, while considering the inherent safety aspects of such therapeutic tools. The clinical potential and future translation of MNs are also discussed.
Background: Aceclofenac is considered to the first line drug in the symptomatic treatment of rheumatoid arthritis, osteoartheritis and ankylosing spondylitis. The successful treatment of arthritis depend on the maintenance of effective drug concentration level in the body, for which a constant and uniform supply of drug is desired. The short biological half-life (about 4 hrs) and dosing frequency more than once a day as well as (70-80%) of dose is excreted by renal transport make aceclofenac an ideal candidate for formulation of niosomal gel. Methodology: The niosomal gel of aceclofenac in order to sustain the release of aceclofenac topically, decreases the side effect of GI disturbance by maintaining the concentration of the drug in the blood and decrease the renal excretion as well as frequency of dosing. Niosomal gel was prepared by coacervation phase separation method. Preformulation studies, structural analysis, in-vitro drug release study, mechanism of drug release kinetic and data analysis (zero order, first order and higuchi’s model), percentage entrapment efficiency and stability study were performed (n=3). Anti-Inflammatory study was performed for final optimized formulation. Result and conclusion: It is revealed from preformulation studies that materials obtained for study did not show any incompatibility. Particle size was determined in the range of 9.46±1.055 to 12.91±3.587μm by using an optical microscope with calibrated eyepiece micrometer. Scanning Electron Microscopy of niosomes was performed to observe surface morphology and percentage entrapment efficiency of niosomes were reported in the range of 63.49±0.265% to 78.55±0.425%. From release kinetic modelling, it was analysed that the drug was released from niosomes by a diffusion-controlled mechanism. Lastly, stability study of all formulations was done in two different temperature and anti inflammatory activity of final optimised formulation was compared with marketed formulation (Voveran Emulgel). Results shows that the aceclofenac Niosomal gel showed fair anti-inflammatory activity but it was not as good as the commercial product.
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