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Drug Profile of Tizanidine HCl

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Any opinions, findings, conclusions or recommendations expressed in this material are those of the authors and do not necessarily reflect the views of UK Essays.

Published: Mon, 09 Apr 2018

Structure:

File:Tizanidine.svg

Categories: Analgesics, Anticonvulsants, Parasympatholytics, Muscle Relaxants, Central, Adrenergic aipha-2 Receptor Agonists, Neuromuscular Agents, Muscle relaxant , Skeletal

Weight: Average: 253.711

Monoisotopic: 253.018893678

Chemical Formula: C9H8ClN5S

IUPAC Name: 5-Chloro-N-(4, 5-dihydro-1H-imidazol-2, 1, 3-benzothiadiazol-4-amine

Taxonomy:

Kingdom: Organic Compounds

Superclass: Heterocyclic Compounds

Class: Benzothiadiazoles

Direct parent: Benzothiadiazoles

Alternative parents: Chlorobenzenes:Thiadiazoles; Polyamines; Aryl Chlorides; Guanidines; Organochlorides.

Substituents: Chlorobenzene: Aryl chloride; Aryl halide; Thiadiazole; Guanidine; Azole; Organochloride; Organohalogen; Polyamine; Organonitrogen compound; Amine.

Classification: These belong to Heterocyclic. This compound belongs to the benzothiadiazoles.

Description: Aromatic compound containing a benzene ring fused to a thiadiazole ring.

Pharmacology:

Indication: To manage increased muscle tone associated with spasticity. 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 motor 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 animal 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/kg

Protein binding: 30%

Route of elimination: Approximately 95% of an administered dose is metabolized.

Half life: 2.5 hours

Affected organisms: Humans and other mammals

Drug interactions: Amlodipine: Amlodipine may decrease the clearance and metabolism of Tizanidine During co-administration considers alternate use caution or Therapy.

Benazepril: With ACE inhibitor Tizanidine increases the risk of hypotension.

Captopril: With ACE inhibitor Tizanidine increases the risk of hypotension.

Solubility:

Storage: cool dry place and in well-closed container.

  • 4.3. EXCIPIENT PROFILE:

Pharmaceutical 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 enhance 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 lower cost, they use a lot aim by the pharmaceutical industry which is overflow with pressure to reduce cost. Excipients show a comprehensive change of useful in pharmaceutical dosage forms, along with:

  • The bioavailability and solubility 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 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).

Polymers:

  • Hydroxypropyl methylcellulose

Synonyms: Hydroxypropyl methyl ether, HPMC, Methocel. Methylcellulose propylene glycol ether, Methyl hydroxypropyl methyl ether [9004-65-3].

Non- proprietary name:

  1. BP:Hypromellose
  2. USP:Hydroxypropyl methylcellulose

Functional Category: Coating agent, viscosity- increasing agent, tablet binder.

Description: HPMC is tasteless and an odorless, white fibrous or granular powder, white or creamy.

Alkalinity /acidity: pH 5.5-8.0 for a 1%w/w aqueous solution.

Melting point: Browns at 190-200°C, chars at 225-230°C, glass transition temperature is 170-180°C.

Moisture content: Hydroxypropyl methyl cellulose consume moisture from the atmosphere, the quantity of water 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 ethanol (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 22084000

Methocel K100M Premium2208100000

Methocel K15M Premium220815000

  1. Most 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.
  2. Suitable types of HPMC are the methocel K100M and methocel K4M grades, which have a characteristics of quick hydration and gel formation.
  3. 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 excess dissolution in the 1st stage or initial erosion.

Application in pharmaceutical formulation or technology:

Hypromellose is mostly used in oral and pharmaceutical formulation.

  1. Hypromellose is most primarily used as a binder in tablet for oral products, as an extended release tablet matrix and in film coating.
  2. 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.
  3. Hypromellose at concentration between 0.45-1.0% w/w are may be used for eye drops and artificial tear solution as a thickening agent to vehicles.
  4. Also, used as suspending agent, an emulsifier, and stabilizing agent in topical ointments and gels.
  5. In addition, for manufacture 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 bicarbonate

Non-proprietary names: BP/EP: sodium bicarbonate

Synonym: Baking soda, e-500, and monosodium carbonate.

Chemical name: carbonic acid, monosodium salt, monosodium carbonate.

Empirical formula: NaHCO3

Molecular weight: 84.01

Category: alkalizing agent, therapeutic agent.

Description: it is an odorless, white crystalline powder with slight alkaline taste.

Acidity/ alkalinity: pH 8.3 for freshly prepared 0.1m aqueous solution at 250C.

Density: 2.159 g/cm3

Solubility: 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 gastric acid with the change of carbon dioxide orally ingested and that may cause stomach cramps and flatulence.

Applications:

  1. Employed as a cause of carbon dioxide in effervescent tablets and granules.
  2. Also used to buffer the drug molecules that are weak acids.
  3. Used in solutions as buffering agent.
  4. Also used as freeze-drying stabilizer.
  5. As a gas forming agent40.
  • Magnesium stearate

Nonproprietary 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: C36H70MgO4

Chemical name: Octadecanoic acid magnesium salt

Molecular weight: 591.34

Structural Formula:

http://upload.wikimedia.org/wikipedia/commons/thumb/8/87/Magnesium_stearate.png/250px-Magnesium_stearate.png

Fig 13. Structure of Magnesium Sterate

Functional category: Capsule and tablet lubricant.

Applications in Pharmaceutical Technology: Magnesium stearate is mostly used in pharmaceutical formulations food and cosmetics. Most primarily at the time 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 actual accomplished milled or precipitated, light white, impalable powder of less bulk density, having faint smell of stearic acid and a quality taste. The powder readily be attached to the skin and greasy to touch.

Solubility: Practically insoluble in ether, ethanol (95%), ethanol, ether and water, slightly. Soluble in warm ethanol (95%) and warm benzene41.

.

  • Microcrystalline cellulose

Synonyms: Microcrystalline cellulose, Avicel, Crystalline cellulose, emocel, vivacel, Cellulosum microcrystallinum.

Chemical Name: Cellulose

Empirical Formula: (C6H10O5)n where n ≈ 220.

Structural formula:

Fig 14: Structure of microcrystalline cellulose

Functional 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 different applications 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 (µm)Moisture content

Avicel pH -10150≤5.0

Avicel pH -102100≤5.0

Uses of microcrystalline cellulose

Use of MCC

Concentration (%)

Adsorbent

20–90

Tablet disintegrant

5-15

Tablet binder/diluent

20–90

Anti-adherent

5–20

Capsulebinder/diluents

20–90

Density (bulk): 0.28-0.32 g/cm3 for Avicel PH 102 and 0.29-0.36 g/cm3 for Avicel PH 200

pH: 5.5-7

Flowability: 1.41 g/s

Melting point: 260–270°C.

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: 1.21–1.30 m2/g for Avicel pH-102, 0.78–1.18 m2/g for Avicel

pH-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 gum

Synonyms:

Bacterial Polysaccharide, Corn Sugar Gum, Xanthan, Gomme desucre de mais, Polysaccharide Xanthane, Gomme Xanthane, Polysaccharide Bactérien, Xanthane, Goma Xantana, Xanthomonas campestris. Gomme de Xanthane,

Description:

Xanthan 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 include:

  • Tablets which slowly break down in the body
  • Liquid drops for the eyes

Xanthan gum is formed by heating a carbohydrate (a substance which consists of sugar) withXanthomonas campestrisbacteria, then processing it.

Uses:

  • Use 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.

Side 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.

Interactions:

Medications 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 dose 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 following doses have been studied. Bymouth: The World Health Organization (WHO) has agreed the maximum pleasing intake for xanthan gum as a laxative of 15 grams per day and as a food additive 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.
  • Aerosil

IUPAC Name: Silicon dioxide

Synonyms: Quartz, Silicic oxide, Silica, Crystalline silica, Silicon (IV) oxide,

Description:

Silicon dioxide, also known assilica (from the Latinsilex), is a chemical compound that is an oxide of silicon with chemical formulaSiO2. It has been known since ancient times. Silica is most usually found in nature as quartz or sand, and also in the cell  walls of diatoms (frustule). Silica is prepared in many forms including fused quartzcrystalfumed silica (or pyrogenic silica), aerogelcolloidal silica, and silica gel49.


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