Simvastatin is a lipidlowering agent derived synthetically from a fermentation product of the fungus aspergillus terreus. Page 1 of 47 product monograph prmintsimvastatin simvastatin tablets usp 5 mg, 10 mg, 20 mg, 40 mg and 80 mg lipid metabolism regulator mint pharmaceuticals inc. Prescribing information simvastatin orally disintegrating. What simvastatin 20mg5ml oral suspension is and what it is used for read all of this leaflet carefully before you start taking this medicine because it contains important information for you. Simvastatin is a white to offwhite, nonhygroscopic, crystalline powder that is practically insoluble in water, and freely soluble in chloroform, methanol and ethanol simvastatin oral. The pharmacokinetics of simvastatin and simvastatin acid, following administration of the 80 mg simvastatin orally disintegrating tablet and 240 ml water at 1 minute postdosing, were comparable to those following administration of the simvastatin immediate release 80 mg tablet taken with 240 ml water. Simvastatin by microwave generated solid dispersion techniques. We investigated the influence of sas process parameters pressure, temperature, and solute concentration on the formation of ezetimibehpc solid dispersion particles. Accurately weighed carrier corresponding to different drug. The effect of peg molecular weights on dissolution behavior. The effect of peg molecular weights on dissolution. May 25, 2015 enhancement of solubility and dissolution rate of simvastatin by ternary solid dispersion technique.
Thermal analysis of simvastatin, pvp k30 and the solid dispersion were carried out using differential scanning calorimetry method. It is used along with exercise, diet, and weight loss to decrease elevated lipid levels. It is also used to decrease the risk of heart problems in those at high risk. These simvastatin companies are well known for high quality product delivery. Preparation and characterization of quercetinpolyvinylpyrrolidone k. Labetalol hydrochloride and simvastatin drug interactions a. Pdf preparation and characterization of solid dispersion tablet of. Only select registry of toxic effects of chemical substances rtecs data is presented here. The sd formulation in addition, the thermal behaviors of sfn powder. If, however, a patient who is currently tolerating the 80mg dose of. Simvastatin is an inactive prodrug which is well absorbed 60 to 80% in animal and humans studies, but undergoes extensive first pass hepatic metabolism following oral administration 2,3,11. Full text rapid disintegrating tablets of simvastatin dispersions in.
Statins are hmgcoa reductase inhibitors, which lower the cholesterol level through reversible and competitive inhibition. Rapid disintegrating tablets of simvastatin dispersions in polyoxyethylenepolypropylene block copolymer for maximized disintegration and dissolution gehan f balata,1,2 ahmad s zidan,2. Simvastatin is a drug from the group of statins used to reduce concentrations of total cholesterol, the socalled bad cholesterol ldl and fatty substances called triglycerides circulating in. Factorial design studies and biopharmaceutical evaluation of.
Solid dispersions sds were prepared by spray drying technique at. Formulation and evaluation of simvastatin solid dispersion. Simvastatin is marketed under the trade names zocor, simvastatin, simlup, simcard and others. Then the solvent was allowed to evaporate completely. Labetalol hydrochloride and simvastatin drug interactions. Rapid disintegrating tablets of simvastatin dispersions in. Pharmacokinetic of simvastatin study in malaysian subjects. It is a hypolipidemic drug belonging to the class of pharmaceuticals called statins. Common side effects include constipation, headaches, and nausea. See actual entry in rtecs for complete information. Sustained release of simvastatin from hollow carbonated. Increase in dissolution rate of simvastatin by amorphous solid dispersion system with hydroxypropylmethylcellulose polymer volume 33, number 4 erizal zaini 1, alessandro evert 2 and maria dona octavia 2.
Simvastatin liquid 40mg5ml decision summary 28 april 2011 background until recently, the only option available for patients who could not swallow simvastatin tablets has been to crush the tablets. What simvastatin 20mg5ml oral suspension is and what it is used for read all of this leaflet carefully before you start taking this medicine because it contains. Simvastatin protected the spleen from apoptosis, reduced cytokine production in the serum, and increased the survival rate. Listing here of leading simvastatin manufacturers, simvastatin suppliers, simvastatin exporters from india. Solubility enhancement of poorly water soluble drug simvastatin by. The present study involved preparation of solid dispersions of simvastatin to improve the aqueous solubility and dissolution rate in order to facilitate faster onset of action. See what the interactions are and for which people. Page 1 of 47 product monograph prmint simvastatin simvastatin tablets usp 5 mg, 10 mg, 20 mg, 40 mg and 80 mg lipid metabolism regulator mint pharmaceuticals inc. Preparation, characterization, and dissolution behavior of a solid. To formulate simvastatin orodispersible tablets with high dissolution rate and enhanced bioavailability. In patients taking simvastatin 80 mg for whom an interacting agent is needed, a lower dose of simvastatin or an alternative statinbased regimen with less potential for drugdrug. Rapid disintegrating tablets of simvastatin dispersions in polyoxyethylenepolypropylene block copolymer for maximized disintegration and dissolution gehan f balata,1,2 ahmad s zidan,2 mohamad as abourehab,1,3 ebtessam a essa4 1department of pharmaceutics, faculty of pharmacy, umm alqura university, makkah, saudi arabia.
Enhancement of solubility and dissolution rate of simvastatin. Polyoxyethylenepolypropylene block copolymer poloxamer 188 was employed as a hydrophilic carrier to prepare simvastatin solid dispersions. Increase in dissolution rate of simvastatin by amorphous. Enhancement of simvastatin dissolution by surface solid dispersion. The aim of the present study was to improve the solubility and dissolution rate of a poorly water. Hollow carbonated hydroxyapatite hchap microspheres as simvastatin sv sustainedrelease vehicles were fabricated through a novel and simple onestep biomimetic strategy. Meanwhile, simvastatin induced jnkmediated cjun and atf2 activation.
Hydrolyzed in vivo to an active metabolite, simvastatin competitively inhibits. In dogs, only 7% of an oral dose reached the general circulation 2,3,11. Overexpression of pin1 suppressed simvastatininduced mmp9 downregulation. To prepare and characterize quercetin solid dispersion using polyvinylpyrrolidone pvp k30. The purpose of the present study was to fabricate ezetimibehydroxypropyl cellulose hpc solid dispersion nanoparticles with enhanced dissolution and oral bioavailability using the. The present research work was focussed on the preparation as well as the evaluation of simvastatin solid dispersions for hypolipidemic activity. The related drug information index provides comprehensive access to all drug information related to a specific drug types of content include full prescribing information, drug summaries, full prescribing. Preparation and characterization of simvastatin nanosuspension by homogenization method athul p. It is used to control hypercholesterolemia elevated cholesterol levels and to prevent cardiovascular disease. Simvastatin is a drug from the group of statins used to reduce concentrations of total cholesterol, the socalled bad cholesterol ldl and fatty substances called triglycerides circulating in the blood.
The in vitro drug release of simvastatin through dialysis membrane from simvasln dispersion and dispersion of pure simvastatin was evaluated using modified franz diffusion cell figure 6. The term solid dispersion refers to a grou p of solid products consisting of at least two differe nt components, generally a hydrophilic matrix and a hydrophobic drug. Nandha college of pharmacy and research institute, erode52,india. Hypolipidemic activity of simvastatin solid dispersions in. D3 1department of quality assurance techniques, 2department of pharmaceutics, 3department of pharmaceutics, vjsms vishal institute of pharmaceutical education and research, ale, pune, maharashtra. Preparation of solid dispersion by solvent evaporation method. Samples were examined using a shimadzu tga50 dsc instrument. Altho ugh this is an unlicensed use of a licensed product, it is a recognised solution and has been widely used. The main aim of the study was to formulate and characterize nanosuspension of simvastatin poorly. Enhancement of simvastatin dissolution by surface solid. Pdf preparation and characterization of simvastatin.
The purpose of the present study was to investigate the effect of polyethylene glycol peg molecular weights 6000, 12000 and 20000 as solid dispersion sd carriers on the dissolution behavior of. Samples equivalent to approximately 8 mg simvastatin were placed in aluminum pans and heated from 40 to 250c with a heating rate of 10cmin. Q if you have any further questions, ask your doctor or. Dissolution improvement of simvastatin by surface solid dispersion technology article in dissolution technologies 172.
The objective of the present study was to formulate surface solid dispersions ssd of simvastatin to improve the aqueous solubility and dissolution rate to facilitate faster onset of action. Solid dispersion of simvastatin in starch phosphate was formulated by solvent evaporation technique. Dissolution improvement of simvastatin by surface solid dispersion. Preparation and characterization of solid dispersion of. The solid dispersion system of simvastatin with hpmc provide a promising way to improve its dissolution rate. Simvastatin is a methylated derivative of lovastatin that acts by competitively inhibiting 3hydroxy3methylglutarylcoenzyme a hmgcoa reductase, the enzyme that catalyzes the rate. The term solid dispersion refers to a group of solid products consisting of at least two different components, generally a hydrophilic matrix and a hydrophobic drug. The objective of the present study was to formulate surface solid dispersions ssd of simvastatin to improve the aqueous solubility and dissolution rate to. Polyvinylpyrrolidone pvp and polyethylene glycol peg are the most widely used polymers for the preparation of solid dispersions.
Simvastatin investigated as a drug, primary irritant, and reproductive effector. In this research different batches were prepared by using the. Learn about drug interactions between isoniazid oral and simvastatin oral and use the rxlist drug interaction checker to check drug combinations. The percentage of the dose retained by the liver is as follows. Feb 27, 2020 simvastatin is a methylated derivative of lovastatin that acts by competitively inhibiting 3hydroxy3methylglutarylcoenzyme a hmgcoa reductase, the enzyme that catalyzes the ratelimiting step in cholesterol biosynthesis. Simvastatin, marketed under the trade name zocor among others, is a lipidlowering medication. Jun 01, 2017 hollow carbonated hydroxyapatite hchap microspheres as simvastatin sv sustainedrelease vehicles were fabricated through a novel and simple onestep biomimetic strategy. Pdf preparation and characterization of solid dispersion. Clinical pharmacokinetic study of simvastatin in malaysian. Preparation and characterization of simvastatin solid dispersion using aqueous solvent 243 j. Simvastatin is a bcs class ii drug having low solubility 1.
Treatment with sp600125 a jnk inhibitor or knockdown of jnk1 reduced mmp2 expression in simvastatintreated cells. Simvastatin powder 1% wv was dispersed in aqueous surfactant solution using magnetic stirrer. Read about common and serious side effects of simvastatin. Solid dispersion technology is a method of dispersing a drug in an inert. Enhanced solubility and dissolution of simvastatin by hpmc. Liver metabolism all statins have the liver as target organ. Solid dispersion and liquisolid dispersion are most likely to be successful. Stability study of simvastatin underhydrolytic conditions.
Atorvastatin, cerivastatin withdrawn from clinical use in 2001. Oct 12, 2015 the purpose of the present study was to fabricate ezetimibehydroxypropyl cellulose hpc solid dispersion nanoparticles with enhanced dissolution and oral bioavailability using the supercritical antisolvent sas process. The dissolution rate of simvastatin from solid dispersion increased with an increased ratio of hpmc polymer. Solid dispersions were formulated using soybean powder as polymer in different ratios. Fast disintegrating crystalline solid dispersions of. This study is created by ehealthme based on reports of 59 people who take labetalol hydrochloride and simvastatin from food and drug administration fda, and is updated regularly. The drug can be dispersed molecularly, in amorphous particles or in crystalline particles.
Drug interactions are reported among people who take labetalol hydrochloride and simvastatin together. Chemical, pharmacokinetic and pharmacodynamic properties. May 09, 2016 therefore, an 80mg dose of simvastatin oral suspension should be used only in patients who have been taking simvastatin 80 mg chronically e. The aim of this work was to improve the aqueous solubility of simvastatin using the surface solid dispersion. Hydrolyzed in vivo to an active metabolite, simvastatin competitively inhibits hepatic hydroxymethylglutaryl coenzyme a hmgcoa reductase, the enzyme which catalyzes the conversion of hmgcoa to mevalonate, a key step. Pharmaceutical dispersion techniques for dissolution and. Preparation and characterization of solid dispersion of simvastatin. Firstly, hollow caco 3 microspheres were precipitated through the reaction of cacl 2 with na 2 co 3 in the presence of aspartic acid and sodium dodecyl sulfate. In addition to the ability of hmgcoa reductase inhibitors to decrease levels of highsensitivity creactive protein. Simvastatin nanosuspension is prepared by high pressure homogenization method. The pharmacokinetics of simvastatin and simvastatin acid, following administration of the 80 mg simvastatin orally disintegrating tablet and 240 ml water at 1 minute postdosing, were comparable.
Pdf preparation and characterization of simvastatin solid. Factorial design studies and biopharmaceutical evaluation. Stability study of simvastatin underhydrolytic conditions assessed by liquid chromatography alejandro alvarezlueje,christian valenzuela,juan arturo squella,andluis joaqu n n ezvergara university of chile, bioelectrochemistry laboratory, chemical and pharmaceutical sciences faculty, po box 233, santiago 1, chile in this work, a liquid. Preparation and evaluation of orodispersible tablets containing. The objective of this study was to use low viscosity grade hydroxypropyl methyl cellulose methocel e3 lv and methocel e5 lv to enhance the solubility and dissolution of poorly water soluble drug simvastatin sim. Chemical, pharmacokinetic and pharmacodynamic properties of. The related drug information index provides comprehensive access to all drug information related to a specific drug types of content include full prescribing information, drug summaries, full prescribing information continuing medication education full pi cme, medication guides, risk evaluation and mitigation strategies rems summaries, rems continuing medication education rems cme, and. Dissolution improvement of simvastatin by surface solid. Two different technologies, hot melt extrusion and spray drying were employed. Among all the solubility enhancement techniques, solid dispersion method, in terms of ease and efficiency is most prom. Spray dried solid dispersion sdp of crystalline simvastatin sim in a fast disintegrating matrix of superdisintegrants was studied as a method to enhance sim dispersibility, rheology, compactibility. Pharmaceutical dispersion techniques for dissolution and bioavailability.
Pdf characterization of solid dispersions of simvastatin. Enhancement of solubility and dissolution rate of simvastatin by ternary solid dispersion technique shete reshma s. Chemical, pharmacokinetic and pharmacodynamic properties of statins. In the case of simvastatin, solid dispersions prepared with either pvp or peg exhibited the largest improvement in wettability and dissolution rate. Being categorized as a class ii drug poorly soluble, highly permeable according to.