DEVELOPMENT AND CHARACTERIZATION OF ORO-DISPERSIBLE TABLETS OF METFORMIN HYDROCHLORIDE USING CAJANUS CAJAN STARCH AS A NATURAL SUPERDISINTEGRANT

Objective: The aim of the research work was to explore the use of Cajanus cajan (Pigeon pea) polysaccharide as a superdisintegrant. The novel superdisintegrant has been evaluated for its action by incorporating it into orodispersible tablets of Metformin Hydrochloride. Methods: Cajanus cajan starch was extracted from its seeds and superdisintegrant was developed by microwave modification of the extract. Various characterization tests such as gelatinization temperature, water absorption index, pH, and viscosity were used to identify the microwave-modified polysaccharide. The orodispersible tablets were made using a direct compression process employing varying concentrations of modified Cajanus cajan starch. Prepared tablets were tested for several pre and post-compression parameters and compared with a well-established synthetic superdisintegrant, sodium starch glycolate. The stability studies were conducted on an optimized formulation. Results: Fourier transform infrared spectroscopy study showed that the drug had no interactions with the microwave-modified Cajanus cajan starch. SEM confirmed that Cajanus cajan starch granules exhibited intact granular structure in oval shapes and smooth surfaces. After microwave modification, the Cajanus cajan starch component lost its granular structure, which further led to the generation of surface pores and internal channels, causing overall swelling responsible for superdisintegrant activity. The optimized formulation (ODF5) containing 15 % modified Cajanus cajan starch performed better in terms of wetting time (22.21 s), disintegration time (53.3 s), and in vitro drug release (92%), as compared to formulation prepared by synthetic superdisintegrant (ODF1). Conclusion: The present investigation concluded that modified Cajanus cajan starch has good potential as a superdisintegrant for formulating oro-dispersible tablets. Furthermore, modified Cajanus cajan starch is inexpensive, non-toxic and compatible in comparison with available synthetic superdisintegrants.

Study of the technological properties of excipients in the development of the composition of orally dispersible tablets

Introduction. The article presents the results of studying the technological properties of individual excipients widely used in the compositions of existing orally dispersed tablets (ODT) for subsequent planning a multifactorial experiment. Samples of excipients were analyzed according to such pharmacopoeial indicators as description, flowability, bulk density, compressibility, fractional composition, solubility in water.Aim. The aim of the work is to create a list and study the technological properties of candidate substances for the role of auxiliary substances in the composition being developed by the ODT.Materials and methods. The technological properties of excipient samples were studied according to the methods of the State Pharmacopoeia of the XIV edition using the flowability tester GTL (ERWEKA, Germany), the bulk density tester SVM 221 (ERWEKA, Germany), the tablet press PGR-10 (LabTools, Russia) and the tablet hardness tester TBH 125 TDP (ERWEKA, Germany).Results and discussion. As a result of the study, experimental data on the technological properties of excipient samples were collected, and the selected samples were compared according to pharmaceutical and technological indicators.Conclusion. In the course of the study, a list of auxiliary substances for the development of the composition of ODT was formed and studies of their technological properties were carried out. The obtained experimental data will allow to develop an optimal matrix of a multifactorial experiment for the development of the composition of ODT and justify the choice of excipients.

Binder Jet 3D Printing of Compound LEV-PN Dispersible Tablets: An Innovative Approach for Fabricating Drug Systems with Multicompartmental Structures

Three-dimensional (3D) printing is an emerging technology that has high application potential for individualized medicines and complex solid dosage forms. This study is designed to explore binder jet 3D printing (BJ-3DP) for the development of high-precision and repeatable compound levetiracetam-pyridoxine hydrochloride (LEV-PN) multicompartmental structure dispersible tablets. PN was dissolved in printing ink directly and accurately jetted into the middle, nested layer of the tablet, and precise control of the drug dose was achieved through the design of printing layers. With modification of the drying method, the “coffee ring” effect caused by drug migration during the curing and molding of the tablets was overcome. Furthermore, 3D topography showed that the tablets have a promising surface morphology. Scanning electron microscopy and porosity results indicated that the tablets have a loose interior and tight exterior, which would ensure good mechanical properties while enabling the tablet to disintegrate quickly in the mouth and achieve rapid release of the two drugs. This study used BJ-3DP technology to prepare personalized multicompartmental structures of drug systems and provides a basis for the development of complex preparations.

Effects of enalapril folic acid combined with levamlodipine on incidence of cardiovascular and cerebrovascular events in patients with essential hypertension

Essential hypertension (EP) is a chronic disease. Effective treatment of hypertension is one of most crucial preventions of cardiovascular (CV) and cerebrovascular (CBV) events. Enalapril folic acid combined with levamlodipine is an effective therapy to treat EP, but its effect on CV and CBV events in hypertensive patients is unknown. This study set out to assess the effects of enalapril folic acid combined with levamlodipine on incidence of CV and CBV events in patients with EP. We randomly assigned 172 patients with EP enrolled in our hospital between April 2017 and September 2018 to receive Levoamlodipine Maleate Dispersible Tablets alone (the control group, n = 85) or Levoamlodipine Maleate Dispersible Tablets combined with Enalapril Maleate and Folic Acid Tablets (the combination group, n = 87). All patients received basic treatment. After 4 weeks of treatment, we recorded the clinical outcomes and adverse reactions of all patients and compared the blood pressure before and after the treatment. The CV and CBV events happening in the two groups within 3 months after the treatment were also recorded. After 4 weeks of treatment, in contrast to the control group, the combination group had a higher marked response rate and lower moderate response rate and non-response rate (P <0.05). The two groups displayed no great disparity in complication rate (P >0.05). Before treatment, the two groups did not differ in pulse pressure (PP), diastolic blood pressure (DBP), and systolic blood pressure (SBP) (P >0.05). After 4 weeks of treatment, both groups showed decreased PP, DBP, and SBP (P <0.05), with lower PP, DBP, and SBP in the combination group (P <0.05). The main CV and CBC events happening in the two groups during the 3-month follow-up included heart failure, stroke, unstable angina pectoris, transient cerebral hemorrhage, acute coronary syndrome, and accelerated heart rate, devoid of fatality. The control group obtained 22 cases (25.88%) of CV and CBC events, which was remarkably higher than the combination group that had 8 cases (9.20%) (P <0.05). In conclusion, the enalapril folic acid combined with levamlodipine therapy is clinically valuable since it can better control blood pressure and reduce the incidence of CV and CBC events in patients without increasing the risk of adverse reactions.

FORMULATION AND EVALUATION OF VALSARTAN CONTAINING SURFACE SOLID DISPERSIONS FOR THE DEVELOPMENT OF ORODISPERSIBLE TABLET

In this postulations we think about Surface Solid Dispersion and Oro dispersible tablet for upgrade of disintegration rate of valsartan. The medications having low solvency, the disintegration of these medications is rate constraining advance in their bioavailability in oral measurements frames. To defeat this number of innovations are accessible. Among them surface solid dispersion and oro dispersible tablets are two promising systems. Surface solid dispersion is a method for scattering at least one xing on a water solvent transporter of to a great degree high surface territory to accomplish expanded bioavailability and disintegration rates of insoluble medications, and oro dispersible tablets are one of the novel oral medication conveyance framework that break down or scatter rapidly in almost no time after situation in month without water.

Formulation and Evaluation of Triclosan Dispersible Tablets for Oral Hygiene

In human anatomy mouth is the earliest segment of alimentary canal which receives food and fabricates saliva, and is one of the foundation for bacterial development due to accretion of sugars form food chunks. There have been more than 300 kinds of bacteria set up in the mouth. The purpose of the present study is to investigate the number of microbes’ grown-up at different timings of the day by collecting the samples from individual volunteer oral cavities and counting the colonies; the utmost count was noted as in the range of 190-200 in the evening samples. The same samples were used to calculate minimum inhibitory concentration of Triclosan, the antibiotic formulated for oral hygiene. Triclosan dilutions were prepared and analyzed for the inhibition zones, it resulted that 300mg of the drug have shown satisfactory results. Triclosan was formulated into a dispersible tablet to enable dispersion of tablet into water for rinsing the oral cavity to remove the contaminants. The Dispersion time of the tablet was within the range of 43.66-111.33 second and it was observed that formulation was acceptable with reasonable limits of standard required for dispersible tablets. Addition of superdisintegrant enhanced the dispersion time which facilitates easy mixing of tablet in water. It concludes that superdisintegrant addition technique is a useful method for preparing dispersible tablets by wet granulation method, and Triclosan dispersible tablet further reduces the microbial attack on tooth by rinsing each time after meals, upon doing so on long term basis the dental decays will probably be eradicated.

Pharmacological and clinical evaluation of deferasirox formulations for treatment tailoring

Deferasirox (DFX) is the newest among three different chelators available to treat iron overload in iron-loading anaemias, firstly released as Dispersible Tablets (DT) and more recently replaced by Film-Coated Tablets (FCT). In this retrospective observational study, pharmacokinetics, pharmacodynamics, and safety features of DFX treatment were analyzed in 74 patients that took both formulations subsequently under clinical practice conditions. Bioavailability of DFX FCT compared to DT resulted higher than expected [Cmax: 99.5 (FCT) and 69.7 (DT) μMol/L; AUC: 1278 (FCT) and 846 (DT), P < 0.0001]. DFX FCT was also superior in scalability among doses. After one year of treatment for each formulation, no differences were observed between the treatments in the overall iron overload levels; however, DFX FCT but not DT showed a significant dose–response correlation [Spearman r (dose-serum ferritin variation): − 0.54, P < 0.0001]. Despite being administered at different dosages, the long-term safety profile was not different between formulations: a significant increase in renal impairment risk was observed for both treatments and it was reversible under strict monitoring (P < 0.002). Altogether, these data constitute a comprehensive comparison of DFX formulations in thalassaemia and other iron-loading anaemias, confirming the effectiveness and safety characteristics of DFX and its applicability for treatment tailoring.

Formulation and Characterization of Dispersible Tablets of Cefpodoxime Proxetil: A Cephalosporin Antibiotic

The objective was to formulate rapid dispersible tablets of Cefpodoxime Proxetil using various types of superdisintegrants viz., Croscarmellose sodium (CCS), Sodium starch glycolate (SSG) and Crospovidone (CP) in varied concentrations (1-5%). The model drug for current investigation, Cefpodoxime Proxetil, a broad spectrum third generation Cephalosporin antibiotic belongs to BCS class IV. The preformulation studies were accomplished by determining the compatibility of model drug with respective excipients by FTIR studies. These studies, revealed no chemical interaction of excipients with the model drug. The formulation development was achieved in phases comprising of preliminary screening, pre-optimization and optimization studies. The bitter taste of model drug was masked by addition of flavors and sweeteners to make it pleasant for pediatric patients upon oral administration. The formulations (F1-F6) were prepared by direct compression method. The percent released from all formulations showed release of more than 90% of drug within 30 min with drug content of more than 95%. The study showed that formulation containing CCS as superdisintegrants furnished best results. Formulation F5 showed maximum (99.6%) drug release within 30 minutes which is prerequisite for dispersible tablets. It also possessed a rapid release of drug from the formulation. The F5 formulation showed comparative dissolution profile vis-a-vis a commercialized formulation. The study concluded that dispersible tablets of Cefpodoxime Proxetil can be an alternative to conventional dosage form for the treatment of urinary tract infection, skin infection, and upper respiratory tract infections.