Drug Profile of Tizanidine HCl

Drug Profile of Tizanidine HClStructureCategories Analgesics, Anticonvulsants, Parasympatholytics, muscleman Relaxants, Central, Adrenergic aipha-2 Receptor Agonists, Neuromuscular Agents, Muscle relaxant , SkeletalWeight Average 253.711Monoisotopic 253.018893678Chemical Formula C9H8ClN5SIUPAC Name 5-Chloro-N-(4, 5-dihydro-1H-imidazol-2, 1, 3-benzothiadiazol-4-amineTaxonomyKingdom Organic CompoundsSuperclass Heterocyclic CompoundsClass BenzothiadiazolesDirect pargonnt BenzothiadiazolesAlternative pargonnts ChlorobenzenesThiadiazoles Polyamines Aryl Chlorides Guanidines Organochlorides.Substituents Chlorobenzene Aryl chloride Aryl halide Thiadiazole Guanidine Azole Organochloride Organohalogen Polyamine Organonitrogen composite Amine.Classification These belong to Heterocyclic. This compound belongs to the benzothiadiazoles.Description Aromatic compound containing a benzene ring fused to a thiadiazole ring.PharmacologyIndication To manage increase muscle tone associated with spastic ity. For the management of spasticity Tizanidine is a short- acting drug. It is a agonist at a2-adrenergic receptor sites and by increasing presynaptic inhibition of tug neurons presumably decreases spasticity.Pharmacodynamics Tizanidine has no direct effect on neuromuscular junction or skeletal muscle fibers and in monosynaptic spinal reflexes there is no major effect, in beast models. On polysynaptic pathways the effects of Tizanidine are more. To reduce the facilitation of spinal motor neurons the overall effect of these actions are thought.Mechanism of action By increasing the presynaptic inhibition of motor neurons reduces Tizanidine spasticity through agonist action at a2-adrenergic receptor sites.Volume of distribution 2.4L/kgProtein binding 30%Route of elimination Approximately 95% of an administered sexually transmitted disease is metabolized.Half life 2.5 hoursAffected organisms Humans and other mammalsDrug interactions Amlodipine Amlodipine may decrease the clearance and metabolism of Tizanidine During co-administration considers alternate use caution or Therapy.Benazepril With hotshot inhibitor Tizanidine increases the risk of hypotension.Captopril With ACE inhibitor Tizanidine increases the risk of hypotension.SolubilityStorage cool dry office and in well-closed container.4.3. EXCIPIENT PROFILEPharmaceutical excipients are substances, alternative than the pharmacologically effective drug or prodrug, that are indicated in the manufacturing process are hold in the final pharmaceutical compound dosage form. Excipients bring prove practicability to the pharmaceuticals, advancement the alterations in the drug development and aid to advance patent life as well. Excipients arrange the products also practical at bring low cost, they use a lot aim by the pharmaceutical industry which is overflow with pressure to reduce cost. Excipients show a comprehensive change of usable in pharmaceutical dosage forms, along withThe bioavailability and solubilit y of active pharmaceutical ingredients (APIs) have been modulated.In dosage forms stability of the active ingredients have been increased.Preferred polymorphic conformations or forms are maintained by helping active ingredients.Maintaining the pH and/or osmolality of liquid productions.Acting as emulsifying agents, antioxidants, tablet reaper binders, aerosol propellants, and as a tablet disintegrate.Preventing dissociation or aggregation (e.g., polysaccharide and actives protein).Immunogenic responses of active ingredients are modulated (e.g., adjuvant).PolymersHydroxypropyl methyl radicalcellulosesynonyms Hydroxypropyl methyl ether, HPMC, Methocel. Methylcellulose propylene glycol ether, Methyl hydroxypropyl methyl ether 9004-65-3.Non- copyrighted nameBPHypromelloseUSPHydroxypropyl methylcellulose working(a) Category Coating agent, viscosity- increasing agent, tablet binder.Description HPMC is tasteless and an odorless, white fibrous or granular powder, white or creamy.Alkalin ity / sour pH 5.5-8.0 for a 1%w/w sedimentary solution.Melting point Browns at 190-200C, chars at 225-230C, glass transition temperature is 170-180C.Moisture content Hydroxypropyl methyl cellulose consume weture from the atmosphere, the quantity of peeing consumed based on the moisture content and relative humidity and temperature of the surrounding air.Solubility Soluble in forming a viscous colloidal solution, cold water, practically insoluble in neutral spirits (95%), chloroform, and either, but soluble in mixtures of dichloromethane and ethanol and mixtures of dichloromethane and methanol, and mixtures of alcohol and water.Methocel productUSP 28 DesignationNormal Viscosity (cps)Methoel K4M Premium 22084000Methocel K100M Premium2208100000Methocel K15M Premium220815000Most influential factors is drug solubility for designing a drug release pattern. Require higher amounts of HPMC in the tablet because they are highly water soluble drugs.Suitable types of HPMC are the methocel K1 00M and methocel K4M grades, which have a characteristics of quick hydration and gel formation.The higher amount of HPMC or viscosity of HPMC can decrease the drug release rate in the tablet. Generally, maximum contended of methocel in the tablet is less 20%. If the contended is below 20%, there is a danger for unembellished dissolution in the 1st stage or initial erosion.Application in pharmaceutical formulation or technologyHypromellose is mostly used in oral and pharmaceutical formulation.Hypromellose is most primarily used as a binder in tablet for oral products, as an extended release tablet matrix and in film coating.Depending upon the viscosity grade, concentration of 2-20% w/w are used in film coating tablets as film-forming solutions. In aqueous film-coating solutions Lower-viscosity grades are used. While in organic solvents higher-viscosity grades are used.Hypromellose at concentration between 0.45-1.0% w/w are may be used for nerve centre drops and artificial tear solu tion as a thickening agent to vehicles. withal, used as suspending agent, an emulsifier, and stabilizing agent in topical ointments and gels.In addition, for fabricate of capsule hyprmellose is used, for hard contact lenses as a wetting agent and as an adhesive in plastic bandages. Also mostly used in food products and cosmetics.Stability and storage Conditions HPMC powder is balanced material, although it is hygroscopic after drying. HPMC powder should be stored in a in a cool, dry place and in well- closed container.Incompatibilities With some oxidizing agents HPMC is incompatible. HPMC will not complex with ionic organic or metallic salts to form insoluble precipitates since it is non-ionic.Safety It is generally considered as a non-irritant and nontoxic material although oral consumption may have a laxative effect39.Sodium bicarbonateNon-proprietary names BP/EP sodium bicarbonateSynonym Baking soda, e-500, and monosodium carbonate.Chemical name carbonic acid, monosodium salt , monosodium carbonate. experiential formula NaHCO3Molecular weight 84.01Category alkalizing agent, therapeutic agent.Description it is an odorless, white crystalline powder with comminuted alkaline taste.Acidity/ alkalinity pH 8.3 for freshly prepared 0.1m aqueous solution at 250C.Density 2.159 g/cm3Solubility Practically insoluble in ethanol and soluble in water,.Stability and storage Sodium bicarbonate is balanced in dry air but still slowly disintegrates in moist air and should accordingly be reserved in a cool dry place and in well-closed container.Safety sodium bicarbonate balance stomachal acid with the change of carbon dioxide orally ingested and that may cause stomach cramps and flatulence.ApplicationsEmployed as a cause of carbon dioxide in effervescent tablets and granules.Also used to buffer the drug molecules that are weak acids. put ond in solutions as buffering agent.Also used as freeze-drying stabilizer.As a bluster forming agent40.Magnesium stearateNonpropr ietary names BP Magnesium Stearate,IP Magnesium Stearate,PhEur Magnesiistearas,USPNF Magnesium Stearate.Synonyms Magnesium octadecananoate Octadecanoic acid Magnesium salt stearic acid magnesium salt.Empirical formula C36H70MgO4Chemical name Octadecanoic acid magnesium saltMolecular weight 591.34Structural FormulaFig 13. Structure of Magnesium SterateFunctional social class Capsule and tablet lubricant.Applications in Pharmaceutical Technology Magnesium stearate is mostly used in pharmaceutical formulations food and cosmetics. Most primarily at the meter of tablet and capsule manufacturing used as a lubricant with concentrations between 0.25% and 0.5% w/w. And also used in barrier creams.Description Magnesium stearate is real(a) accomplished milled or precipitated, light white, impalable powder of less bulk density, having faint smell of stearic acid and a quality taste. The powder quickly be attached to the skin and greasy to touch.Solubility Practically insoluble in ether, eth anol (95%), ethanol, ether and water, approximately. Soluble in impassioned ethanol (95%) and warm benzene41.. crystalline celluloseSynonyms Microcrystalline cellulose, Avicel, Crystalline cellulose, emocel, vivacel, Cellulosum microcrystallinum.Chemical Name CelluloseEmpirical Formula (C6H10O5)n where n 220.Structural formulaFig 14 Structure of microcrystalline celluloseFunctional category suspending agent, Adsorbent, tablet disintegrant, tablet and capsule diluent.Applications in pharmaceutical formulation or technology It is primarily used as a diluent/ binder in oral tablet and capsule formulation in both wet granulation processes and direct compression. It has also got some lubricant, antiadherent, and disintegrating properties, which is useful in tableting. Microcrystalline cellulose is used in food products and cosmetics.Description It occurs as a white, tasteless, odourless crystalline powder keeping of porous particles. It is commercially applicable in contrasting appli cations and properties.Solubility Slightly soluble in 5% w/v sodium hydroxide solution insoluble in most organic solvents, water and dilute acids.GradeNominal mean particle size (m)Moisture contentAvicel pH -101505.0Avicel pH -1021005.0Uses of microcrystalline celluloseDensity (bulk) 0.28-0.32 g/cm3 for Avicel PH 102 and 0.29-0.36 g/cm3 for Avicel PH 200pH 5.5-7Flowability 1.41 g/sMelting point 260270C.Moisture content Typically less than 5% w/w.Solubility Insoluble in dilute acids and water, slightly soluble in 5% w/v sodium hydroxide solution.Specific surface area 1.211.30 m2/g for Avicel pH-102, 0.781.18 m2/g for AvicelpH-200.Stability Microcrystalline cellulose is a stable though hygroscopic material.Storage Conditions Storeatambientconditions.Keepcontainers sealed material is very hygroscopic.Incompatibilities Incompatible with strong oxidizing agents43.Xanthum gumSynonymsBacterial polyose, Corn Sugar Gum, Xanthan, Gomme desucre de mais, Polysaccharide Xanthane, Gomme Xanthane, Polysaccharide Bactrien, Xanthane, Goma Xantana, Xanthomonas campestris. Gomme de Xanthane,DescriptionXanthan gum is a sugar-like compound prepared by blending aged (fermented) sugars with assured kind of bacteria. It is used to make medicine.It is used in making some medications and foods. In these products it has different effects. It can keep textures from changing, add thickness, and hold ingredients in place.In many types of medicines Xanthan gum is found. These includeTablets which slowly take apart down in the bodyLiquid drops for the eyesXanthan gum is formed by heating a carbohydrate (a substance which consists of sugar) withXanthomonas campestrisbacteria, then processing it.UsesUse as a bulk-forming laxative to treatconstipation.In people with diabetes it lowers blood sugar.In people with diabetes it lowers cholesterollevels.For dry mouth used as a saliva substitute. human face effects Xanthan gum assume to cause some side effects. A 1987 study, in that five men who are healthy ate roughly 10 to 13gm daily, has commence no adverse effects. It may cause gas.Risks.The FDA has warned against for giving simply thick to premature infants. It has been combined to a danger digestive problem called necrotizing enterocolitis in neonate born prematurely.InteractionsMedications for diabetes (Antidiabetes drugs) interrelates with XANTHAN GUM.By decreasing the absorption of sugars in food Xanthan gum might lower blood sugar. To lower blood sugar Diabetes medications are also used. Blood sugar to be too low may cause by taking xanthan gum with diabetes medications. Guide your blood sugar nearly. The venereal disease of your diabetes medication may need to change. Some medications used for diabetes be composed of glimepiride (Amaryl), chlorpropamide (Diabinese), glyburide, glipizide (Glucotrol), (Micronase, Dia Beta, Pres Tab, Glynase), pioglitazone (Actos), insulin, rosiglitazone (Avandia), tolbutamide (Orinase), and others.Dosing In scientific research the fol lowing sexually transmitted diseases have been studied. Bymouth The World wellness Organization (WHO) has agreed the maximum pleasing intake for xanthan gum as a laxative of 15 grams per day and as a food one-dimensional of 10 mg/kg /day. Xanthan gum require extra fluids for effectiveness and safety, bulk laxatives such as.For diabetes As an ingredient in muffins a typical dose is 12grams per day44.AerosilIUPAC Name Silicon dioxideSynonyms Quartz, Silicic oxide, Silica, Crystalline silica, Silicon (IV) oxide,DescriptionSilicon dioxide, also known assilica (from theLatinsilex), is achemical compoundthat is anoxideofsiliconwithchemical formulaSiO2. It has been known since antediluvian patriarch times. Silica is most usually found in nature asquartz or sand, and also in thecell wallsofdiatoms(frustule). Silica is prepared in many forms including fused quartz,crystal,fumed silica(or pyrogenic silica), aerogel,colloidal silica, and silica gel49.