Fluvastatin Sodium Research Articles

Screening approach by a combination of computational and in vitro experiments: identification of fluvastatin sodium as a potential SIRT2 inhibitor.

Sirtuins (SIRTs) are NAD+-dependent deacetylases that play various roles in numerous pathophysiological processes, holding promise as therapeutic targets worthy of further investigation. Among them, the SIRT2 subtype is closely associated with tumorigenesis and malignancies. Dysregulation of SIRT2 activation can regulate the expression levels of related genes in cancer cells, leading to tumor occurrence and metastasis. In this study, we used computer simulations to screen for novel SIRT2 inhibitors from the FDA database, based on which 10 compounds with high docking scores and good interactions were selected for in vitro anti-pancreatic cancer metastasis testing and enzyme binding inhibition experiments. The results showed that fluvastatin sodium may possess inhibitory activity against SIRT2. Subsequently, fluvastatin sodium was subjected to molecular docking experiments with various SIRT isoforms, and the combined results from Western blotting experiments indicated its potential as a SIRT2 inhibitor. Next, molecular docking, molecular dynamics (MD) simulations, and binding free energy calculations were performed, revealing the binding mode of fluvastatin sodium at the SIRT2 active site, further validating the stability and interaction of the ligand-protein complex under physiological conditions. Overall, this study provides a systematic virtual screening workflow for the discovery of SIRT2 activity inhibitors, identifies the potential inhibitory effect of fluvastatin sodium as a lead compound on SIRT2, and opens up a new direction for developing highly active and selectively targeted SIRT2 inhibitors.

Formulation and Evaluation of Transdermal Niosomal Gel for Antihyperlipidemic Agent

Aims:: The current study aims to create a formulation of Fluvastatin sodium (FVS) loaded niosome for the treatment of antihyperlipidemia using thin film hydration. The developed formulations were statistically optimized by two factors, three levels by 3-level factorial design and were evaluated for vesicle size, entrapment efficiency, zeta potential, transmission electron microscopy, and in-vitro drug release. Methods:: The optimized FVS niosome being transformed to gel formulation was likewise analyzed for in-vitro skin permeability study, lipase action, and stability study. Results:: The composition of an improved FVS niosome revealed vesicle size, entrapment effectiveness, zeta potential of 105.3 ± 12.4nm, 74.5 ± 0.86% and -36.2 ± 7mV, respectively, with spherical morphology. Conclusion:: The FVS Niosomal gel demonstrated improved skin permeation compared to Orlistat. Furthermore, lipase activity showed better activity when compared with standard Orlistat drugs. Niosomal particles were discovered as a reliable nanovesicular carrier for the transdermal administration of FVS.

Designing, Creating, and Assessing a Modified Pulsincap Delivery System for Intestine Targeting of Fluvastatin in Accordance with Circadian Rhythm

The current study’s objective remains to create the Pulscap delivery system using an insoluble capsule core that contains fluvastatin sodium microspheres. Eudragit RL 100 polymer fluvastatin sodium microspheres were made using the solvent evaporation method. To reduce the possibility of stomach upset, these microspheres were hand-filled into capsules, plugged with hydrogel plugs, then sealed with ethyl cellulose acetate and dipped in an eight: two (vol/vol) Acetone: ethanol solution by butyl pthalate of (0.75%) and 5% cellulose acetate phthalate solution. Formulated dosage form was assessed for in-vivo X-ray imaging studies, in-vitro drug release studies, and in-vivo imaging studies, pharmacokinetic study of the optimized formulation was conducted in a two-way cross-over design with 6 rabbits in each group and the pharmacokinetic parameters (Cmax, Ka, Ke, MRT and AUC0-α) are measured. A Pharmacodynamics study was also performed on lipid profiles in six groups of rabbits. Optimized formulation (F20) which is prepared with a drug and polymer ratio of 1:3, is selected based on a dissolution study which shows a percentage release of 99.98. ± 0.12% at 17th hour. In the in-vivo study, the plasma concentration at 12th hour 53.8 ± 0.02% and at 32nd hour 13.9 ± 0.05%. Pharmacokinetic parameter Cmax (ng/mL): 53.8 ± 0.41, MRT (h): 20.0 ± 0.14, t1/2 (h): 8.52 ± 0.014, Kel (h-1) :0.08 ± 0.014, Ka (h-1):0.25 ± 0.02, AUC0-a (ng h/mL): 944.9. ± 4.05. Serum lipid profile in high cholesterol rabbit after treatment with F20 formulation total cholesterol:240.83 ± 19.76, HDL-C:37.33 ± 2.16, triglycerides:318.67 ± 7.74, VLDL-C:63.73 ± 1.55, LDL-C:139.77 ± 18.74. Compared to lovastatin SR release, lovastatin pulsatile release, and fluvastatin SR release, the results imply that the F20 formulation’s pulsatile drug delivery has established good drug delivery for medications entering the gastrointestinal tract, and it displays superior pharmacokinetic and pharmacodynamic parameters.

NIR-Activatable Heterostructured Nanoadjuvant CoP/NiCoP Executing Lactate Metabolism Interventions for Boosted Photocatalytic Hydrogen Therapy and Photoimmunotherapy.

Near-infrared (NIR) laser-induced photoimmunotherapy has aroused great interest due to its intrinsic noninvasiveness and spatiotemporal precision, while immune evasion evoked by lactic acid (LA) accumulation severely limits its clinical outcomes. Although several metabolic interventions have been devoted to ameliorate immunosuppression, intracellular residual LA still remains a potential energy source for oncocyte proliferation. Herein, an immunomodulatory nanoadjuvant based on a yolk-shell CoP/NiCoP (CNCP) heterostructure loaded with the monocarboxylate transporter 4 inhibitor fluvastatin sodium (Flu) is constructed to concurrently relieve immunosuppression and elicit robust antitumor immunity. Under NIR irradiation, CNCP heterojunctions exhibit superior photothermal performance and photocatalytic production of reactive oxygen species and hydrogen. The continuous heat then facilitates Flu release to restrain LA exudation from tumor cells, whereas cumulative LA can be depleted as a hole scavenger to improve photocatalytic efficiency. Subsequently, potentiated photocatalytic therapy can not only initiate systematic immunoreaction, but also provoke severe mitochondrial dysfunction and disrupt the energy supply for heat shock protein synthesis, in turn realizing mild photothermal therapy. Consequently, LA metabolic remodeling endows an intensive cascade treatment with an optimal safety profile to effectually suppress tumor proliferation and metastasis, which offers a new paradigm for the development of metabolism-regulated immunotherapy.

Formulation development and evaluation of fluvastatin loaded transethosomes: Characterization, stability, in vitro dermal penetration, cytotoxicity and antipsoriatic activity studies

Psoriasis, a common immune-mediated chronic inflammatory disease, may arise from genetic, epigenetic, and immune system factors. Current medications focus on symptom relief, presenting a challenge in discovering new compounds or methods for safe and effective psoriasis management while ensuring patient adherence. Statin drugs like fluvastatin, initially for dyslipidemia, were considered beneficial for treating psoriasis. Thus the objective of this study was to formulate novel topical transethosomes as drug delivery systems for dermal administration of fluvastatin sodium (fluvastatin) in psoriasis treatment. The thin film hydration method was exploited to prepare fluvastatin loaded transethosomes consisted of Phospholipon 90 as the phospholipid, along with Tween 20 or Tween 80 as the edge activators. The physicochemical properties of the transethosomes, including particle size and size distribution, zeta potential, encapsulation efficiency, pH, and conductivity, were evaluated. Attenuated Total Reflectance Fourier Transformed Infrared (ATR-FTIR) analysis was conducted to determine the structural characteristics, while Transmission Electron Microscopy (TEM) and Scanning Electron Microscopy (SEM) analyses were employed to examine the morphological properties. Additionally, the stability of the transethosomes was monitored. Transfersome-type delivery systems were also developed for comparison with the transethosome formulations. The in vitro skin penetration and deposition behavior of fluvastatin transethosomes were assessed using sequential tape stripping, ATR-FTIR Spectroscopy, and Confocal Laser Scanning Microscopy (CLSM) and compared to fluvastatin-loaded transfersomes. Furthermore, in vitro cell culture studies were conducted to evaluate the cytotoxicity and antipsoriatic activities of the fluvastatin-loaded transethosomal carrier systems that exhibited the highest dermal accumulation. The results suggest that fluvastatin-loaded transethosomes inhibit the IL6 and IL8 production in HaCaT cells compared to free fluvastatin. Overall, the aim of this research is to develop innovative, skin-compatible, and stable drug delivery systems that improve the effectiveness of psoriasis treatment. This would be achieved by targeting the active substance, fluvastatin, which is believed to have potential antipsoriatic effects, specifically to the affected area of the skin.

Development and Optimization of Fluvastatin Sodium Loaded Biodegradable Microspheres

Fluvastatin sodium is a hypolipidemic agent that reduces cholesterol synthesis by inhibiting HMG-COA reductase. The drug has a comparatively short biological half-life (1.2 hours) and low bioavailability (24– 29%), making it an appropriate candidate for a sustained-release drug delivery system. This study aimed to formulate biodegradable microspheres of fluvastatin sodium by optimization through an experimental design approach. Microspheres containing fluvastatin sodium were prepared by o/w emulsification solvent evaporation method using poly (lactic-co-glycolic acid) (PLGA 50:50) as a biodegradable polymer. 32 full factorial design was applied to study the effect of drug to polymer ratio and stirring speed on dependent variables, i.e. particle size, entrapment efficiency, Q1h, t80%. Prepared formulations were subjected to evaluate physicochemical properties and release characteristics. DSC and FTIR proved no interaction between the drug and excipients. Microspheres possessed size in the range of 193 to 344 μm and entrapment efficiency varied from 63.1 to 85.6%. Formulations showed drug release up to 23% within 1-hour. while t80% was found in between 3–9 hours. Regression analysis and ANOVA results suggested a significant effect (p<0.05) of variables on responses. The results of the present study suggested that biodegradable microspheres of fluvastatin sodium prepared using poly (lactic-co-glycolic acid) can be a promising alternative for conventional delivery and suitable for sustained drug release.

Diversity of Solid Forms Promoted by Ball Milling: Characterization and Intrinsic Dissolution Studies of Pioglitazone Hydrochloride and Fluvastatin Sodium Drug-Drug Systems.

Coamorphous salt in a 1:1 ratio prepared by ball milling from Fluvastatin sodium (FLV) and Pioglitazone hydrochloride (PGZ·HCl) can be selectively formed by neat grinding (NG). Furthermore, the salt-cocrystal continuum was preferably formed by employing liquid-assisted grinding (LAG) using ethanol (EtOH). Attempts to prepare the coamorphous salt starting from the salt-cocrystal continuum by NG were unsuccessful. Interestingly, through ball milling by NG or LAG, a great diversity of solid forms (PGZ·HCl-FLV 1:1) could be accessed: NG and hexane (coamorphous); ethyl acetate (physical mixture); EtOH (salt-cocrystal continuum); and water (which presents two Tg, indicating immiscibility of the components). An exploration was performed at different drug-to-drug ratios by NG. By differential scanning calorimetry (DSC), the presence of two endothermic events was observed in this screening: incongruous melting point (solidus) and excess of one of the components (liquidus), except in the 1:1 solid form. From these results, eutectic behavior was observed. Through the construction of a binary phase diagram, it was determined that the 1:1 molar ratio gives rise to the formation of the most stable coamorphous composition. Dissolution profile studies of these solid forms were carried out, specifically on pure FLV and the solid forms of PGZ⋅HCl-FLV (1:2; 1:4; and 1:6), together with the coamorphous 1:1 salt. By itself, pure FLV presented the highest Kint (13.6270 ± 0.8127 mg/cm2⋅min). On the other hand, the coamorphous 1:1 showed a very low Kint (0.0220 ± 0.0014 mg/cm2·min), indicating very fast recrystallization by the FLV, which avoids observing a sudden release of this drug in the solution. This same behavior was observed in the eutectic composition 1:2. In the other solid forms, the value of Kint increases along with the %w of FLV. From the mechanochemical point of view, ball milling by NG or LAG became an important synthetic tool since it allows obtaining a great variety of solid forms to explore the solid-state reactivity of the drug-drug solid-form PGZ HCl-FLV.

Role of Fluvastatin sodium loaded polymeric nanoparticles in the treatment of Hyperlipidemia: Fabrication and Characterization

The present work is focused on the formulation and evaluation of polymeric nanoparticles (NPs) loaded by Fluvastatin sodium (FLS). This drug has many disadvantages, including bioavailability of up to 24 to 44% and a half-life of approximately 30 min to 60 min. Also, it comes under Biopharmaceutical classification system (BCS) class III, but it is sparingly soluble in water. Polymeric NPs were prepared using gum rosin and chitosan as polymers which Solvent Evaporation and Inotropic Gelation method prepared. Prepared polymeric NPs were characterized for respective parameters like drug entrapment efficiency, particle size, zeta potential, Differential Scanning Calorimetry, X-Ray Diffraction, Scanning Electron Microscopy, Transmission Electron Microscopy, In vitro and In vivo drug release study. The average Particle size was lay within the range of 271 nm to 313.3 nm for the Solvent Evaporation method (SE) and 123.3 nm to 382 nm for the Inotropic gelation method (IG). Drug entrapment efficiency (DEE) of SE3 was found to be 86.1%, and IG3 had 70.2%. In vitro release study showed sustained action for both methods at the end of 48 h; an increase in the polymer resulted in decreased drug release. From the study, it can be concluded that prepared polymeric NPs from both methods show significant hypolipidemic activity. Stability studies showed that formulations are stable at the end of 3 months.

Application of Central Composite Design for Formulation and Optimization of Solid Dispersion for Dissolution Rate Enhancement of BCS Class II Drug

The objective of this research work was to develop solid dispersion of Fluvastatin sodium (FLS-SD) by solvent evaporation technique for dissolution enhancement of Fluvastatin sodium (FLS). Furthermore, central composite design (CCD) was applied for studying the effect of drug: polymer (w/w) (X1) and surfactant concentration (% w/v) (X2) on dependent variables T50% (Minutes) (Y1), Q90(%) (Y2) and percentage drug content (Y3). Thirteen experimental runs were performed as per CCD design layout and analyzed. The model was exceptional fitted in quadratic model as indicated by lack of fit of p-value more than 0.05. An optimized FLS-SD composition having 0.998 desirability function was explored using Design-Expert software. The theoretical values of t50%, Q90 and % drug content for optimized FLS-SD given by software were 23 min, 94.289% and 88.515%, respectively. The percentage cumulative drug release from FLS, physical mixture and FLS-SD was found 25.43%, 27.54%, and 93.6% within 2 hour which demonstrated superior and significant dissolution enhancement of FLS (*p < 0.05). The r2 for the Zero-order, First-order, Korsmeyer-peppas (K-P), and Higuchi models for FLS-SD were 0.8336, 0.7594, 0.9539 and 0.9234, respectively. K-P model was found superior (y = 0.426x +1.1259, r2 = 0.9539) and ‘n’ value was 0.426(n <0.45) which revealed fickian drug release from FLS-SD. This research work concluded that solid dispersion formulation by solvent evaporation technique could be successfully utilized for dissolution enhancement of BCS class II drug.

Identification of nafamostat mesylate as a selective stimulator of NK cell IFN-γ production via metabolism-related compound library screening

Natural killer (NK) cells play important roles in controlling virus-infected and malignant cells. The identification of new molecules that can activate NK cells may effectively improve the antiviral and antitumour activities of these cells. In this study, by using a commercially available metabolism-related compound library, we initially screened the capacity of compounds to activate NK cells by determining the ratio of interferon-gamma (IFN-γ)+ NK cells by flow cytometry after the incubation of peripheral blood mononuclear cells (PBMCs) with IL-12 or IL-15 for 18 h. Our data showed that eight compounds (nafamostat mesylate (NM), loganin, fluvastatin sodium, atorvastatin calcium, lovastatin, simvastatin, rosuvastatin calcium, and pitavastatin calcium) and three compounds (NM, elesclomol, and simvastatin) increased the proportions of NK cells and CD3+ T cells that expressed IFN-γ among PBMCs cultured with IL-12 and IL-15, respectively. When incubated with enriched NK cells (purity ≥ 80.0%), only NM enhanced NK cell IFN-γ production in the presence of IL-12 or IL-15. When incubated with purified NK cells (purity ≥ 99.0%), NM promoted NK cell IFN-γ secretion in the presence or absence of IL-18. However, NM showed no effect on NK cell cytotoxicity. Collectively, our study identifies NM as a selective stimulator of IFN-γ production by NK cells, providing a new strategy for the prevention and treatment of infection or cancer in select populations.

PH-Regulating Nanoplatform for the "Double Channel Chase " of Tumor Cells by the Synergistic Cascade between Chlorine Treatment and Methionine-Depletion Starvation Therapy.

During rapid proliferation and metabolism, tumor cells show a high dependence on methionine. The deficiency of methionine exhibits significant inhibition on tumor growth, which provides a potential therapeutic target in tumor therapy. Herein, ClO2-loaded nanoparticles (fluvastatin sodium&metformin&bupivacaine&ClO2@CaSiO3@MnO2-arginine-glycine-aspatic acid (RGD) (MFBC@CMR) NPs) were prepared for synergistic chlorine treatment and methionine-depletion starvation therapy. After outer layer MnO2 was degraded in the high glutathione (GSH) tumor microenvironment (TME), MFBC@CMR NPs released metformin (Me) to target the mitochondria, thus interfering with the tricarboxylic acid (TCA) cycle and promoting the production of lactate. In addition, released fluvastatin sodium (Flu) by the NPs acted on monocarboxylic acid transporter 4 (MCT4) in the cell membrane to inhibit lactate leakage and induce a decrease of intracellular pH, further prompting the NPs to release chlorine dioxide (ClO2), which then oxidized methionine, inhibited tumor growth, and produced large numbers of Cl- in the cytoplasm. Cl- could enter mitochondria through the voltage-dependent anion channel (VDAC) channel, which was opened by bupivacaine (Bup). The disruption of Cl- homeostasis promotes mitochondrial damage and membrane potential decline, leading to the release of cytochrome C (Cyt-C) and apoptosis inducing factor (AIF) and further inducing cell apoptosis. To sum up, the pH-regulating and ClO2-loaded MFBC@CMR nanoplatform can achieve cascade chlorine treatment and methionine-depletion starvation therapy toward tumor cells, which is of great significance for improving the clinical tumor treatment effect.

Development and validation of a stability-indicating RP-HPLC method for the estimation of Fluvastatin sodium in bulk and tablet dosage form

A simple and gradient RP- HPLC method has been validated and developed for Fluvastatin Sodium in bulk and tablet dosage form. The proposed method was validated to obtain official requirements including stability, accuracy, precision, linearity and selectivity. The method was developed on Hypersil ODS C18 column (150 x 4.6 mm, 5micron) using the mobile phase consists of methanol: 20mM Phosphate buffer (pH 3.2 adjusted with Phosphoric acid): acetonitrile (55: 30: 15 v/v) was delivered at a flow rate of. The flow rate was set as 1.1 ml/minute and the maximum absorption were observed at 234 nm. The Fluvastatin Sodium drug showed a precise and good linearity at the concentration ranges of 3-15 µg/ml. The RP-HPLC, assay showed the highest purity ranging 99.88 % to 100.09 % for Fluvastatin Sodium tablet formulation and 100.02 % was the mean percentage purity. The Fluvastatin Sodium retention time was found to be 5.5 minutes. The method accuracy was showed by statistical analysis. The developed RP-HPLC method can be adopted for the routine analysis of Fluvastatin Sodium in bulk and pharmaceutical dosage forms in quality control laboratories. The developed method was validated according to the ICH guidelines.

Green Atomic Absorption Spectroscopic Methods for the Determination of Rabeprazole Sodium and Fluvastatin Sodium in Pure and Pharmaceutical Dosage Forms

Aims: Novel green analytical methods have been proposed for the assay of Rabeprazole sodium and Fluvastatin sodium in their pure and formulated dosage forms.
 Study Design: The methods determine each drug through the estimation of its sodium content, using Flame Atomic Absorption Spectroscopy at wavelength 589 nm. 
 Place and Duration of Study: Central laboratory at Faculty of Pharmacy, Damanhour University. Time duration January-March, 2020.
 Methodology: Methods are developed and optimized for maximum sensitivity, selectivity and degree of greenness. Linearity is achieved in the range of 8.29- 66.33 ppm of Rabeprazole sodium (equivalent to 0.5- 4 ppm Na) and 14.13- 141.32 ppm of Fluvastatin sodium (equivalent to 0.75 -7.5 ppm Na). The proposed assays are fully validated regarding ICH guidelines. 
 Results: Atomic spectroscopic assays are compared to reported spectrophotometric ones for each drug separately using Student t-test and F-variance ratio. 
 Conclusion: Satisfactory values indicate good agreement and the insignificant difference between both methods. The obtained percentages of recovery (99-101%) indicate no interference from excipients in formulation matrices.

Formulation and Evaluation of Orodispersible Tablet of Fluvastatin Sodium

The purpose of this research work is to formulate and evaluate the Orodispersible tablet of Fluvastatin Sodium to enhance the bioavailability and effectiveness of the drug. The objectives of the drug work were to formulate and evaluate Orodispersible tablets of Fluvastatin Sodium, having adequate mechanical strength, rapid disintegration, and fast action. Precompression parameters like angle of repose, bulk density, tapped density, compressibility index & post-compression parameters like wetting time, water absorption ratio, in-vitro disintegration, and in-vitro dispersion time were studied. The hardness, friability, and drug content of all the formulations were found to be within the limits. The best formulation PK09 has shown good disintegration time, dissolution time, and dispersion time. The optimized formulation of batch PK9 gave the best in-vitro release of 99.60% in 3min in phosphate buffer pH 6.8. The release of the drug followed the matrix diffusion mechanism as compared to the commercial formulation. Formulation PK9 gives quick disintegration and better drug release. Hence it can be concluded that the formulation of PK9 is stable and effective for quick action and it is an alternative to the conventional tablets.
 Keywords: Orodispersible Tablets, Fluvastatin Sodium, Fast dissolving/disintegrating tablets, GIT, bioavailability, first-pass metabolism, superdisintegrants

Development of Sustained Release Eudragit Based Matrix Tablet of Fluvastatin Sodium Microspheres

The purpose of this research is to investigate the suitability of acquiring improved dissolution profile and sustained release of Fluvastatin sodium to reduce dosage frequency via a novel combination of freeze dried microspheres and Eudragit polymers-based matrix tablet technologies. Fluvastatin sodium microspheres were prepared using polyvinyl pyrollidone K-30 and Poloxamer 407 through solvent evaporation via freeze drying. We adopted a central composite design to examine the influence of independent variables viz. drug:polymer (X1) and surfactant (X2) on the t50 % (Y1), Q90 (Y2) and percentage drug content (Y3) along with determination of an optimized composition for production of an optimal Fluvastatin sodium microspheres. Design expert software illustrated that an optimized Fluvastatin sodium microspherescould be achieved using 1:3.496 drug:polymer and 3.102 % poloxamer 407 which would illustrates t50 % (36.33 min), Q90 (79.99 %) and percentage drug content (81.589 %). The mean diameter and polydispersity index of Fluvastatin sodium microspheres using dynamic light scattering was found 0.78 μm and 0.287, respectively. Sustained release tablet of optimized Fluvastatin sodium microspheres (Fluvastatin sodium microspheres-sustained release tablet) was manufactured using Eudragit RS 100 and Eudragit RL 100 based granules by wet granulation technique. In vitro drug release kinetics studies were executed to assess the drug release mechanism from optimized Fluvastatin sodium microspheres and Fluvastatin sodium microspheres-sustained release tablet. The dissolution level of Fluvastatin sodium was 3.58-fold improved wthin 2 h through the freeze dried microspheres. Fluvastatin sodium microspheres-sustained release tablet showed sustained drug release over 24 h and was matched properly to Korsmeyer-Peppas model with release exponent of 0.5318, which indicated drug release through diffusion and erosion mechanism. Conclusively, it has been demonstrated that novel combination of freeze dried microspheres and their Eudragit polymers-based matrix tablet techniques could find great potential for improving drug dissolution and sustained release of water insoluble drugs along with reduced dosage frequency.

Improvement of Development and Validation of an RP-HPLC Method for The Fluvastatin Sodium Using QbD Approach and Its Application to Forced Degradation Studies

The current examination portrays the improvement of the QbD way to deal with Reverse Phase-High Performance Liquid Chromatography (RP-HPLC) framework utilizing Design of Experiments.Each of the three principle parts of the RP-HPLC measure (Buffer pH, Organic Step-percent acetonitrile, Organic Modifier-Methanol) are introduced in a successful test configuration zeroed in on methodical exploring. Through measurable investigation devices, for example, Analysis of Variance (ANOVA) and plots that uncovered the last chromatographic states of the strategy, the criticalness and communication impacts of these boundaries on the reaction factors (maintenance time and following component) were assessed. The chromatographic detachment was accomplished on Thermo Hypersil BDS RP C18 (250 × 4.6 mm, 5μ) section utilizing Buffer (pH 6.8): Acetonitrile (60:40v/v) as portable stage and discovery was finished utilizing Photo-Diode Array (PDA) identifier at 288 nm. The created fluvastatin sodium technique is direct with coefficients of relationship over a scope of 10-80μg/ml. The (R2) estimation of the connection coefficient is 0.999. The percent RSD for the strategy's exactness and accuracy was discovered to be under 2 percent. Investigations of Forced Degradation uncovered that the method was found to show security. The outcomes indicated that the strategy proposed is proper for the exact and precise assurance and detailing of fluvastatin sodium in mass.

Optimization of Process Parameters for Formulation of Fluvastatin Tablet by Using Dry Granulation Method

The manufacturing process of the tablet is a very complex process; it can be affected by the several process parameters or variables. The aim of this study was to understand and optimize the process parameters such as mixing, granulation, lubrication and tablets compression processes using quality by design (QbD) approach for a model Anti- Hyperlipidemic drug Fluvastatin sodium. During the processes there are several parameters which may influence or affect product quality. So the main objective of present work was to identify various process parameters and optimize this parameter, for the formulation of good quality product which needs to optimize Blending time, Roller force, Compression force and machine speed. A scale up batch was taken to evaluate and optimize the parameters. Critical quality attributes (CQA) such as flow behavior, granules parameters, Blend uniformity, tablet appearance, effect on tablet quality like physical appearance (surface, weight etc.) and tablet dissolution time as well as drug release. The test results of following parameters at various in-process phases are complies with the specified limits and finished product sample results were found to be within specified limits. This study results assures the manufacturing process is reproducible, robust and will yield consistent product, which meets specification.
 Keywords: Process Parameters, Quality by Design, Fluvastatin, Granulation, Blending, Compression etc,.

New Validated Analytical Method for Determination of Simvastatin in Tablet Formulations by RP–HPLC

RP–HPLC method has been developed and validated for the determination of simvastatin (SVS) in pure form and in tablets. Fluvastatin sodium was used as internal standard. The determination was performed on Nucleodur column C8 (250×4.6 mm i.d., 5 µm particle size); the mobile phase consisted of a mixture of phosphate buffer solution (KH2PO4 0.05 M, pH 4.83) and methanol (20:80, v/v), pumped at a flow rate 1.0 mL min−1 . Analyte was monitored by UV detection at 230 nm. The mean retention times for fluvastatin and simvastatin were about 4.40 and 9.00 min, respectively. The method was proved linear in the range of 3.5– 550.0 µg mL-1 and exhibited good correlation coefficient (r>0.9998) and excellent mean recovery (100.71– 102.18%). Very good limit of detection of 0.63 µg mL-1 was found for SVS. The method was validated statistically and by recovery studies for linearity, precision, repeatability, and reproducibility. This method was successfully applied to the determination of simvastatin content in four marketed brands from Syria. A good agreement between this method with the pharmacopoeial method for the determination of simvastatin in some real samples demonstrates that the proposed method is suitable to quantify simvastatin in pharmaceutical formulations.

Formulation and evaluation of fluvastatin sodium drug-in-adhesive transdermal system

Formulation and evaluation of fluvastatin sodium drug-in-adhesive transdermal system

Central composite designed solid dispersion for dissolution enhancement of fluvastatin sodium by kneading technique.

Aim: This research is focused on enhancing aqueous solubility and dissolution of fluvastatin sodium (FSS) through solid dispersion (FSS-SD) production using polyethylene glycol 6000 and polyvinyl pyrollidone K-30 by kneading technique. Methodology & results: Central composite design explored the influence of polyethylene glycol 6000 and polyvinyl pyrollidone K-30 on T50% and Q90. The aqueous saturation solubility of FSS (8.7±1.12μg/ml) was amplified 20-fold in FSS-SD (179±4.16μg/ml). Cumulative drug release from FSS and optimized FSS-SD were 27.49 and 87.4% within 90min, respectively. Conclusion: FSS-SD production using kneading technique offers great prospective in maximizing FSS's solubility and dissolution.