Chemical Structures and Excipient Profile of Drugs

chemic Structures and Excipient Profile of DrugsDRUG AND EXCIPIENT PROFILECAFFEINEChemical mental synthesis Mol. Weight comely 194.1906Melting point 238 CState solidWater solubility 2.16E+004 mg/L (at 25 C)Half deportment 3 7 hours in geriatrics , 65 130 hours in pediatricsProtein Binding Low protein binding (25 36%)Absorption absorbed after(prenominal) oral and parenteral administration. The peak plasma level of caffein ranges from 6 to 10mg/L and the mean time to reach peak concentration ranged from 30 minutes to 2 hours.Pharmacology Caffeine is a naturally occurring xanthine derivative like theobromine and the bronchodilator theophylline. It is used as a CNS stimulant, bats diuretic, and respiratory stimulant (in neonates). a good deal combined with analgesics or with ergot alkaloids, caffeine is used to treat migraine and other types of headache. Over the counter, caffeine is used to treat drowsiness or mild water-weight gain.Mechanism of exercise Caffeine stimulates myelinry, vagal, vasomotor, and respiratory centers, promoting bradycardia, vasoconstriction, and increased respiratory rate. This action was previously believed to be due primarily to increased intracellular cyclic 3,5-adenosine monophosphate (cyclic AMP) following inhibition of phosphodiesterase, the enzyme that degrades cyclic AMP. Xanthines such as caffeine act as antagonists at adenosine-receptors within the plasma membrane of virtually every cell. As adenosine acts as an autocoid, inhibiting the release of neurotransmitters from presynaptic sites but augmenting the actions of nor epinephrine or angiotensin, antagonist of adenosine receptors promotes neurotransmitter release. This explains the stimulatory effects of caffeine. Blockage of the adenosine A1 receptor in the heart leads to the accelerated, pronounced pounding of the heart upon caffeine intake.Indication For wariness of fatigue, orthostatic hypotension, and for the short term treatment of apnea of prematurity in n eonates.Toxicity LD50= 127 mg/kg (oral dose in mice)ERGOTAMINEChemical structure Mol. Weight Average 581.6615Melting point 213.5 CState solid stateWater solubility Slightly solubleHalf Life 2 hoursAbsorption The bioavailability of sublingual ergotamine has not been determined.Pharmacology Ergotamine is a vasoconstrictor and alpha adrenoreceptor antagonist. The pharmacology of ergotamine is extremely complex some of its actions are unrelated to each other, and plane mutually antagonistic. The drug has partial agonist and antagonist activity against tryptaminergic, dopaminergic and alpha adrenergic receptors depending upon the site, and is highly active uterine stimulant. It causes constriction of peripheral and cranial source vessels and producing depression of central vasomotor centers. The pain of a migraine attack is due to increased amplitude of pulsations in the cranial arteries, especially the meningeal branches of the orthogonal carotid artery. Ergotamine overthrows extra cranial profligate flow, causes a decline in the amplitude of pulsation in the cranial arteries, and decreases hyper perfusion of the territory of the basilar artery. It does not reduce cerebral hemispheric blood flow.Mechanism of Action Ergotamine acts on migraine by one of the two proposed mechanisms1) activation of 5-HT1D receptors located on intracranial blood vessels, including those on arteriole-venous anastomoses, leads to vasoconstriction, which correlates with the relief of migraine, and2) Activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system which results in inhibition of pro-inflammatory neuropeptide release.Indication For use as therapy to abort or prevent vascular type of headache, e.g., migraine, migraine variants, or so called histaminic cephalalgia.Toxicity Signs of overexposure including irritation, nausea, vomiting, headache, diarrhea, thirst, coldness of skin, pruritus, weak pulse, numbness, tingling of extremities, and confusion.CYCLIZ INEChemical structure Mol. Weight Average 266.38Melting point 105.5 CState solid stateWater solubility 1000 mg/L (at 25 C)Half Life 20 hoursPharmacology Cyclizine is a piperazine derivative antihistamine used as antivertigo/antiemetic agent. Cyclizine is used in the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness. Additionally, it has been used in the management of vertigo in disease affecting the vestibular apparatus. The mechanism by which cyclizine exerts its antiemetic and antivertigo effects is not been fully elucidated, its central anticholinergic properties are partly responsible. The drug depresses labyrinth excitability and vestibular stimulation, and it may affects medullary chemoreceptor trigger zone. It also possesses anticholinergic, antihistaminic, central nervous system depressant, and local anesthetic effects.Mechanism of Action Vomiting (emesis) is essentially a protective mechanism for removing irritant and harmful subst ances from the upper GI tract. Emesis is controlled by the vomiting centre in the medulla region of the brain, an important part of which is the chemotrigger zone (CTZ). The vomiting centre possesse neurons which are rich in muscarinic cholinergic and histamine containing synapses. These types of neurons are especially involved in contagious disease from the vestibular apparatus to the vomiting centre. Motion sickness involves overstimulation of the pathways due to various sensory stimuli. Hence the action of cyclizine which acts to block the histamine receptors in the vomiting centre and olibanum reducing the activity along these pathways. Furthermore since cyclizine possesses anti-cholinergic properties as well, the muscarinic receptors are similarly blocked.Indication For prevention and treatment of the nausea, vomiting, and dizziness that are associated with motion sickness, and vertigo (dizziness caused by other medical problems).EXCIPIENT PROFILEMANNITOLSynonym D mannite, ma nna sugar, cordycepic window pane, pearlitol.Emperical Formula C6H14O6Molecular Weight Approx. 182.17Description Mannitol is a white , Odorless, cobwebby powder or free flowing granules .It has sweet taste , approximately as sweet as glucose and half as sweet as sucrose, gestate the cooling sensation in the mouth.Density, bulk 0.430 g/cm3 for powder 0.7g/cm3for granulesDensity, tapped 0.734gm /cm3for powder, 0.8gm/cm3 for granules.Solubility Freely soluble in water, very slightly soluble in ethanol (96 per cent). It shows polymorphism.Incompatibility Mannitol is incompatible with xytilol infusion and may form complexes with some metals such as aluminum, copper and iron. Mannitol was found to reduce bioavailability of cemitidine compared to sucrose.Handling vigilance Mannitol may be irritate to eye, eye protection is recommended.Uses Diluents (10-90%w/w), mannitol is used as excipient in the manufacture of chewable tablet because of its proscribe heat of solution, sweetness an d mouth feel.MICROCRYSTALLINE CELLULOSESynonym Cellulose gel, crystalline cellulose, Avicel PH 101, 102Empirical Formula (C6H10O5)nMolecular weight Approx.36000Description Purified, partially depolymerised cellulose occurs as a white, tasteless odorless, crystalline, powder that is composed of porous particles available in different particle size grades with different properties , i.e. 101 ,102Bulk Density 0.28gm/cm 3Tapped Density 0.43gm/cm3Solubility Insoluble in water, dilute acids and most organic solvents .Slightly soluble in sodium hydroxide solution.stableness and storage condition immutable and hygroscopic. Store in a well closed container.Incompatibility None cited in the literature.Handling precautions No restrictions.Uses Tablet binder / diluents (5-20%), tablet disintegrant (5-15%), tablet glidant (5-15%) antiadherent (5-20%), enfold diluents (10-30%)CROSSCARMELLOSE SODIUMIn a cross linked polymer of carboxymethylcellulose sodium.Synonym Ac-DI-SolMolecular formula C 8H16O8Molecular weight 240.20784Description It occurs as an odorless, white or hoary white powder.Density, bulk 0.529gm/cm3Density, tapped 0.819gm/cm3Stability and storage condition It is stable though hygroscopic material, preserve in well closed container in cool and juiceless place.Incompatibilities The efficacy of disintegration may be slightly reduced in tablet formulation prepared by either the wet granulation or direct compression that contains hygroscopic excipients such as Sorbitol.Handling precautions It may be irritant to eye. gist protection is recommended.Uses It is used in oral pharmaceutical formulation as, a disintegrant for capsule, tablets, and granules.SODIUM STARCH GLYCOLATESodium salt of cross linked partly o- carboxymethylated potato starch..Synonym Carboxy methyl cellulose, sodium salt, exeplosol, explotab.Description exsanguine or almost white free flowing powder, very hygroscopic.Density, bulk 0.75gm/cm3Density, tapped 0.95gm/cm3Solubility Practically insoluble in Methylene chloride. It gives a translucent fracture in water.Stability and Storage It is stable and should be stored in a well closed container in cool and dry place.Incompatibilities It is incompatible with ascorbic acid.Handling precautions Eye protection, glove and a dust mask are recommended.Uses It is use in oral pharmaceutical formulation as a disintegrant for capsule, tablet, and granules.TALCIt is hydrous magnesium silicate may contain a small amount of aluminium silicateand iron.Nonpropritery Name Purified Talc (BP), Talc (JP), Talc (USP).Synonym A talc, hydrous magnesium atomic number 20 silicate powdered talc.Empirical Formula Mg6 (Si2O5) (OH) 4Description A very fine, white to grayish-white, abstract, odorless, crystalline powder. Adheres readily to skin soft to smear and free from grittiness.Density, bulk 19gm/cm3Density, tapped 48gm/cm3Solubility Insoluble in water, organic solvents, cold acid.Stability and Storage Stable, preserve in well closed con tainer.Incompatibilities It is incompatible with quatern ammonium compounds.Handling Precaution Eye protection, gloves, and respirator are recommended.Uses It is use a s glidant, lubricant (1-10%), Diluents5-30%, Dusting powder 90-99%MAGNESIUM STEARATESynonym Metallic stearate octadecanoic acid magnesium salt Stearic acid.Nonproprietary Name Magnesium Stearate (BP) Magnesium Stearate (JP) Magnesium Stearate (USP).Empirical Formula C36H70MgO4Molecular Weight 591.3Description Fine, white, precipitated or milled, impalpable powder of low bulk density. Odour and taste are slight but characteristic. The powder is readily adheres to the skin.Density, bulk 0.519 gm/cm3Density, tapped 0.286gm/cm3Melting point 117-1500CStability And Storage Condition Stable, non self polymerisable, store in cool and dry place in a well closed container.Incompatibilities Incompatable with strong acid substances, alkalic substances, iron salts, avoid mixing with strong oxidizing materials. Use with caution with drugs , which are incompatible with alkali.Uses tablet and capsule lubricant, glidant or antiadherent (0.25-2.0%).(Brunye et al., 2010) (Mohammadi and Kanfer, 2005) (Shapiro and Cowan, 2006) (Tsutsumi et al., 2002)