Chemical Structures and Excipient Profile of Drugs

Chemical Structures and Excipient Profile of Drugs DRUG AND EXCIPIENT PROFILE CAFFEINE Chemical structure: Mol. Weight: Average: 194.1906 Melting point: 238  °C State: solid Water solubility: 2.16E+004 mg/L (at 25  °C) Half Life: 3 7 hours in geriatrics , 65 130 hours in pediatrics Protein Binding: Low protein binding (25 36%) Absorption: absorbed after oral and parenteral 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 used as a CNS stimulant, mild diuretic, and respiratory stimulant (in neonates). Often 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 Action: Caffeine stimulates medullary, 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†²,5†²-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 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) ERGOTAMINE Chemical structure: Mol. Weight: Average: 581.6615 Melting point: 213.5  °C State: solid state Water solubility: Slightly soluble Half Life: 2 hours Absorption: 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 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 pain of a migraine attack is due to increased amplitude of pulsations in the cranial arteries, especially the meningeal branches of the external carotid 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 mechanisms: 1) 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, and 2) 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. CYCLIZINE Chemical structure: Mol. Weight: Average: 266.38 Melting point: 105.5  °C State: solid state Water solubility: 1000 mg/L (at 25  °C) Half Life: 20 hours Pharmacology: 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 partially 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 substances 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 transmission 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 thus 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 PROFILE MANNITOL Synonym: D –mannite, manna sugar, cordycepic acid, pearlitol. Emperical Formula: C6H14O6 Molecular Weight: Approx. 182.17 Description: Mannitol is a white , Odorless, crystalline powder or free flowing granules .It has sweet taste , approximately as sweet as glucose and half as sweet as sucrose, impart the cooling sensation in the mouth. Density, bulk: 0.430 g/cm3 for powder 0.7g/cm3for granules Density, 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 precaution: 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 negative heat of solution, sweetness and mouth feel. MICROCRYSTALLINE CELLULOSE Synonym: Cellulose gel, crystalline cellulose, Avicel PH 101, 102 Empirical Formula: (C6H10O5)n Molecular weight: Approx.36000 Description: 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 ,102 Bulk Density: 0.28gm/cm 3 Tapped Density: 0.43gm/cm3 Solubility: Insoluble in water, dilute acids and most organic solvents .Slightly soluble in sodium 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: Tablet binder / diluents (5-20%), tablet disintegrant (5-15%), tablet glidant (5-15%) antiadherent (5-20%), capsule diluents (10-30%) CROSSCARMELLOSE SODIUM In a cross linked polymer of carboxymethylcellulose sodium. Synonym: Ac-DI-Sol; Molecular formula: C8H16O8 Molecular weight: 240.20784 Description: It occurs as an odorless, white or grayish white powder. Density, bulk: 0.529gm/cm3 Density, tapped: 0.819gm/cm3 Stability and storage condition: It is stable though hygroscopic material, preserve 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 GLYCOLATE Sodium salt of cross linked partly o- carboxymethylated potato starch.. Synonym: Carboxy methyl cellulose, sodium salt, exeplosol, explotab. Description: White or almost white free flowing powder, very hygroscopic. Density, bulk: 0.75gm/cm3 Density, tapped: 0.95gm/cm3 Solubility: Practically insoluble in Methylene 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 dust mask are recommended. Uses: It is use in oral pharmaceutical formulation as a disintegrant for capsule, tablet, and granules. TALC It 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 calcium silicate; powdered talc. Empirical Formula: Mg ­6 (Si2O5) (OH) 4 Description: A very fine, white to grayish-white, impalpable, odorless, crystalline powder. Adheres readily to skin soft to touch and free from grittiness. Density, bulk: 19gm/cm3 Density, tapped: 48gm/cm3 Solubility: 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 STEARATE Synonym: Metallic stearate; octadecanoic acid; magnesium salt; Stearic acid. Nonproprietary Name: Magnesium Stearate (BP); Magnesium Stearate (JP); Magnesium Stearate (USP). Empirical Formula: C36H70MgO4 Molecular Weight: 591.3 Description: 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/cm3 Density, tapped: 0.286gm/cm3 Melting point: 117-1500C Stability And Storage Condition: Stable, non self polymerisable, store in cool and dry place in a well closed container. Incompatibilities: Incompatable with strong acid substances, alkaline 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)

English Language Essay on Spoken Text

Text B is an interview on television show conducted by two presenters with the purpose being to conceive as much information as they can from J. K. Rowling, a famous author on her newest Harry Potter book. The audience here would predominantly be avid young readers of the book who want to know about the book and regular followers of the show. The dominant speaker in this text B would be the interviewers and the chat show is based on adjacency pairs.Using a false-start and contradiction in â€Å"no, I don’t – yes I do† illustrate aspects of spoken language although there are clear elements where the audience might know the interviewers had a basic idea of what was to be asked before-hand. The lack of non-fluency features more clearly suggest the questions were previously prepared, for example, when Richard says â€Å"All the papers that have been promoting this interview today clearly want us†¦Ã¢â‚¬  This tells us research was undertaken on what sort of que stions the audience or readers wanted answered.The change of tone at the end of a sentence suggests spontaneity and cues the other speaker’s turn to speak. For example, â€Å"But of course the last one at the moment is residing in your safe†, portrays the change in tone at the end. Judy, the interviewer used more interrogatives like â€Å"two much loved ones? † while Richard uses ellipsis to try and create spontaneity and confidence, â€Å"you told your husband, obviously you confide in him all things†¦Ã¢â‚¬  allowing turn-taking.The interviewee also seems a little uninterested through her short answers such as â€Å"He did one of the, yeah†; to perhaps show she isn’t in the mood or the fact she’s trying to be careful so as to not reveal any information thus considering her words. Text C is a play script from American Buffalo by David Mamet, with the purpose primarily being to entertain. The audience here would be predominantly educat ed theatre going audience.The play script is structurally organized through the use of adjacency pairs, with interrogatives being a main aspect. Don is portrayed as the dominant speaker as he controls the conversation and asserts his position through speech. Don’s speech is also longer and more authorative to further portray his higher status than Bob. The use of turn-taking and the informal setting gives way to colloquialism such as â€Å"well she was real mad at him†, â€Å"jewed† and â€Å"yup†.Don also uses â€Å"Bobby† to show familiarity with the other character as well as it being a little patronizing to represent their distinctive positions and relationship. Don also instigates topic shifts structurally as he tries to teach Bob about business, â€Å"Things are not always what they seem to be†, shows how a cliche to perhaps portray Don’s maturity and wisdom in comparison to the youth and naivety of Bob.

Donner Company Case Solution Essay - 899 Words

1. The process flow diagram of the production system at Donner. Preparation Stage Imagine Transfer Fabrication 2. What size orders would you schedule on the CNC drill? On the CNC router? Time taken to process the orders depends on the selected drilling method either a) Manual drilling or CNC OR b) Using CNC Drill Assumption 1: Manual Drilling is not done on all the available Manual Drill Presses in parallel. Calculating time taken for Manual drilling and CNC Drilling: = Setup Time + Run Time (Per Hole) * No. of Holes drilled on each circuit board * No. of boards Time taken for Manual drilling =15 + 0.08*500*x where x= number of circuit boards Time taken for CNC drilling = 240 + 0.004*500*x where x= number of†¦show more content†¦of Boards (n) Parallel Process allowed Manual Drill 6 n ≠¤ 56 No Parallel Processing CNC Drill n 56 CNC Drill What Size orders can be scheduled on CNC Router? Using the steps used in previous part, calculating the time taken by each method Time taken for Punch Press =50 + x Time taken for CNC Router = 150+ 0.5x To figure out whether CNC Router to be used, 50 + x ≠¥ 150+ 0.5x Hence x ≠¥ 200. [x= number of circuit boards] Conclusion for CNC Router: n 200 Use Punch Press Total no. of Boards (n) n 200 For Use CNC Router 3. Would you recommend adding another CNC drill? Perform a net-present value calculation to help make the decision. Price of the CNC machine is $80,000. The additional assumption we need to add to assumption already given is that: Arthur Dief will run all the small orders (8 circuit boards or less) and other boards will be done on a CNC machine despite of the shop floor policy which states that only orders for more than 100 boards be drilled on a CNC machine. The company is currently using a CNC machine for orders for equal or greater than 140 boards due to capacity of a CNC machine; however, they would be able to process all orders with CNC machines if they add one more machine. In this case, if we calculate the current cost in drilling process:Show MoreRelatedBenihana of Tokyo Case8219 Words   |  33 PagesMedaille College MBA-621 Operations Management Case Study #2 Donner Company 3/8/2006 Amr Abbas Problem Definition The three-year old Donner Company has positioned itself well within both the small volume, customized (contract) printed circuit boards market as well as the large volume, generic (captive) printed circuit boards market. 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Legal Analysis of Indirect Expropriation Claim Under...

WRITING SAMPLE Kiho Kim 101 Cherry Ave. Bethpage, NY 11714 (070) 8624-1462 The attached writing sample is an excerpt from a research paper submitted for the international business transaction course of Hofstra School of Law. This research paper addresses potential controversies arising from the investment provisions of KOR-US FTA, particularly focusing on indirect expropriation claims under KOR-US FTA. The beginning chapter provides a brief history of expropriation provisions in bilateral investment treaty. The second chapter discusses indirect expropriation provisions of the NAFTA Chapter 11 and the relevant case law. The final chapter analyzes detailed criteria to review indirect expropriation claims in the context of†¦show more content†¦In the next chapter, the Article will evaluate the influence of the NAFTA Chapter 11 on the expropriation provisions of KOR-US FTA, and attempt to discover discrepancies between the NAFTA Chapter 11 jurisprudence and the U.S. Taking Clause jurisprudence. Particularly, this chapter’s analysis will offer a helpful insight on understanding of the textual improvement made in KOR-US FTA because the investment provisions of KOR-US FTA are basically modeled on the NAFTA Chapter 11. Finally, the Article will explore the concrete standard for determining an indirect expropriation articulated in KOR-US FTA, and analyze each considerable factor under customary international law. II HISTORY OF INVESTMENT TREATIES AND EXPROPRIATION Industrialized countries have long made efforts to achieve a global consensus about the principle that foreign investments cannot be nationalized without appropriate compensation. Particularly, the United State has strongly endorsed the â€Å"Hull Formula,† which requires a state to provide â€Å"prompt, adequate, and effective† compensation for the expropriation of foreign investments. 1However, continuous attempts to incorporate the Hull Formula into multilateral 1 See Andreas F. Lowenfeld, International Economic Law, 397-402 (2002). 3 treaty were frustrated because theShow MoreRelatedLegal Analysis of Indirect Expropriation Claim Under Korea-Us Fta3577 Words   |  15 Pagesof KOR-US FTA, particularly focusing on indirect expropriation claims under KOR-US FTA. The beginning chapter provides a brief history of expropriation provisions in bilateral investment treaty. The second chapter discusses indirect expropriation provisions of the NAFTA Chapter 11 and the relevant case law. The final chapter analyzes detailed criteria to review indirect expropriation claims in the context of KOR-US FTA. 0 LEGAL ANAYSIS OF INDIRECT EXPROPRIATION CLAIMS UNDER KOR-US FTA Kiho Kim