Chemical Structures and Excipient Profile of Drugs

chemical Structures and Excipient Profile of DrugsDRUG AND EXCIPIENT PROFILECAFFEINEChemical grammatical construction Mol. exercising incubus Average 194.1906Melting point 238 CState red-bloodedwater dodge solubility 2.16E+004 mg/L (at 25 C)one- half lifespan 3 7 hours in geriatrics , 65 130 hours in paediatricsProtein Binding Low protein binding (25 36%)Absorption absorbed after oral examination and p arnteral administration. The peak plasma level of caffeine 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 use as a CNS stimulant, mild diuretic, and respiratory stimulant (in neonates). Often combined with analgesics or with ergot alkaloids, caffeine is used to track migraine and other types of headache. Over the counter, caffeine is used to treat drowsiness or mild water-weight gain.Mechan ism of Action Caffeine stimulates medullary, vagal, vasomotor, and respiratory centers, promoting bradycardia, vaso density, and increased respiratory rate. This action was previously believed to be due principally to increased intracellular cyclical 3,5-adenosine monophosphate (cyclic AMP) following inhibition of phosphodiesterase, the enzyme that degrades cyclic AMP. Xanthines such as caffeine act as opp cardinalnts at adenosine-sense organs inside the plasma membrane of virtually every cell. As adenosine acts as an autocoid, inhibiting the supply 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. attribute For management of fatigue, orthostatic hypotension, and for the short term treatment of apnea of prematurity in neonates.Toxicity LD50= 127 mg/kg (oral dose in mice)ERGOTAMINEChemical structure Mol. burthen Average 581.6615Melting point 213.5 CState solid positWater solubility Slightly solubleHalf Life 2 hoursAbsorption The bioavailability of sublingual ergotamine has not been determined.Pharmacology Ergotamine is a pressor and alpha adrenoreceptor antagonist. The pharmacology of ergotamine is extremely complex some of its actions are uncorrelated to each other, and even 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 blood vessels and producing depression of central vasomotor centers. The annoyance of a migraine attack is due to increased amplitude of pulsations in the cranial arteries, especially the meningeal branches of the external car otid artery. Ergotamine reduces extra cranial blood 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, mothyness of skin, pruritus, weak pulse, numbness, tingling of extremities, and confusion.CYCLIZINEChemical structure Mol. metric weight unit 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 drift sickness. Additionally, it has been used in the management of vertigo in disease bear upon the vestibular apparatus. The mechanism by which cyclizine exerts its antiemetic and antivertigo effects is not been repletely elucidated, its central anticholinergic properties are partially responsible. The drug depresses labyrinth surliness and vestibular stimulation, and it whitethorn affects medullary chemoreceptor trigger zone. It also possesses anticholinergic, antihistaminic, central nauseated system depressant, and local anesthetic effects.Mechanism of Action Vomiting (emesis) is essential ly a protective mechanism for removing irritant and harmful substances from the upper GI tract. Emesis is controlled by the vomiting inwardness in the medulla division 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 guarding synapses. These types of neurons are especially involved in transmittal from the vestibular apparatus to the vomiting centre. Motion sickness involves overstimulation of the pathways due to motley sensory stimuli. Hence the action of cyclizine which acts to block the histamine receptors in the vomiting centre and thus reducing the activity along these pathways. Furthermore since cyclizine possesses anti-cholinergic properties as rise up, the muscarinic receptors are similarly blocked.Indication For prevention and treatment of the nausea, vomiting, and dizziness that are associated with communicate sickness, and vertigo (dizziness caused by other medical problems).EXCIPIENT PROFILEMANNITOL equivalent word D mannite, manna sugar, cordycepic acid, pearlitol.Emperical Formula C6H14O6Molecular Weight Approx. 182.17Description mannitol is a white , Odorless, crystalline powder or free silklike granules .It has sweet taste , approximately as sweet as glucose and half as sweet as sucrose, impart the calming sensation in the mouth. absorption, masses 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 uncongenial 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 precaution Mannitol may be irritate to eye, eye protection is recommended.Uses Diluents (10-90%w/w), mannitol is used as excipient in the manufac ture of chewable launch pad because of its ostracize heat of solution, sweetness and mouth feel.MICROCRYSTALLINE CELLULOSE equivalent word 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, corrupt acids and most organic solvents .Slightly soluble in atomic number 11 hydroxide solution. stability and storage condition Stable and hygroscopic. Store in a well closed container.Incompatibility None cited in the literature.Handling precautions No restrictions.Uses birth control pill binder / diluents (5-20%), pad disintegrant (5-15%), tablet glidant (5-15%) antiadherent (5-20%), capsule diluents (10-30%)CRO SSCARMELLOSE SODIUMIn a cross linked polymer of carboxymethylcellulose sodium.Synonym Ac-DI-SolMolecular formula C8H16O8Molecular weight 240.20784Description It occurs as an odorless, white or grayish white powder.Density, mess 0.529gm/cm3Density, tapped 0.819gm/cm3Stability and storage condition It is electrostatic though hygroscopic material, stay on in well closed container in cool and dry 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. Eye protection is recommended.Uses It is used in oral pharmaceutical formulation as, a disintegrant for capsule, tablets, and granules.SODIUM STARCH GLYCOLATESodium saltiness of cross linked partly o- carboxymethylated potato starch..Synonym Carboxy methyl cellulose, sodium salt, exeplosol, explotab.Description White or almost w hite free flowing powder, very hygroscopic.Density, bulk 0.75gm/cm3Density, tapped 0.95gm/cm3Solubility Practically insoluble in methylene radical chloride. It gives a translucent suspension 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 spread 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 propose Purified talcum powder (BP), Talc (JP), Talc (USP).Synonym A talc, hydrous magnesium calcium silicate disintegrate talc.Empirical Formula Mg6 (Si2O5) (OH) 4Description A very fine, white to grayish-white, impalpable, odorless, crystalline powder. Adheres readily to skin soft to occupy and free from grittiness.Density, bulk 19gm/cm3D ensity, tapped 48gm/cm3Solubility Insoluble in water, organic solvents, cold acid.Stability and Storage Stable, preserve in well closed container.Incompatibilities It is incompatible with quaternary 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. smelling 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 egotism polymerisable, store in cool and dry place in a well closed container.Incompat ibilities Incompatable with strong acid substances, alkaline substances, iron salts, repress 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)