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HIGH INITIAL BURST RELEASE OF GENTAMICIN FORMULATED AS PLGA MICROSPHERES
HIGH INITIAL BURST RELEASE OF GENTAMICIN FORMULATED AS PLGA MICROSPHERES

... Antibiotic treatment of orthopaedic infection is complicated by systemic toxicity and the need of effective therapeutic concentration necessary to ensure optimum killing of bacteria. To overcome the problem of systemic toxicity and to achieve a high initial release followed by sustained release of a ...
5 1 Prereview - World Health Organization
5 1 Prereview - World Health Organization

... As a central nervous system stimulant, lisdexamfetamine is used as an adjunct in the treatment of attention deficit hyperactivity disorder (ADHD). As a prodrug, lisdexamfetamine was specifically designed as an abuse-resistant product. After oral administration and absorption, enzyme hydrolysis follo ...
Mepivacaine - Academy of General Dentistry
Mepivacaine - Academy of General Dentistry

... potency than lidocaine or prilocaine under in vitro conditions.17 However, these measurements were derived under controlled conditions and do not directly reflect in vivo anesthetic potency. They also do not correctly reflect the clinical end-points of mepivacaine use, where success is measured by a ...
Low Temperature Precursors for SnOx Thin Films
Low Temperature Precursors for SnOx Thin Films

... A brief summary of the work carried out is presented, and conclusions are drawn to compare the different ligand systems utilised in the chemical vapour deposition experiments. A short discussion on potential future investigations is also presented ...
CV - Faculty of Pharmaceutical Sciences
CV - Faculty of Pharmaceutical Sciences

... In order to investigate the suitability of using saliva for therapeutic drug monitoring sensitive assays using GCMS were developed for the acidic anticonvulsant valproic acid and for the basic narcotic analgestic methadone. In the case of valproic acid saliva levels are very pH dependent and vary wi ...
amoxicillin: a broad spectrum antibiotic
amoxicillin: a broad spectrum antibiotic

... Adding an electron withdrawing group onto the 6‐position (located  on the β‐lactam ring) amide group can increase its  acid stability by  making  the  amide  oxygen  less  nucleophillic  as  in  amoxicillin.  This  ensures  that  the  amide  oxygen  will  not  attack  the  β‐lactam  ring's  carbonyl ...
DEVELOPMENT AND VALIDATION OF LIQUID
DEVELOPMENT AND VALIDATION OF LIQUID

... Abstract: An isocratic, reversed phase-liquid-chromatographic method was developed for the quantitative determination of levodopa and carbidopa and entacapone in combined-dosage form. Agilent zorbax sb-C18 (250mm*4.6mm*5µ) column with mobile phase containing water pH 4.0 adjusted with sodium dihydro ...
Ketoconazole and Itraconazole Pharmacokinetic
Ketoconazole and Itraconazole Pharmacokinetic

... respiratory tract caused by H. influenzae and streptococcus pneumoniae (1). Also, it has been found to be effective in the treatment of bronchopulmonary diseases caused by Pseudomonas aeruginosa in patients with cystic fibrosis (2). It may also be used for the treatment of acute exacerbations of bro ...
Blood Coagulation Pathway
Blood Coagulation Pathway

...  Warfarin- sole oral anticoagulant for 60 years.  Limitations- ...
Relationship between Type of Endorser and
Relationship between Type of Endorser and

... The study identified whether there was a difference in responses toward a prescription drug ad based on endorser type. The study accessed allergy patients through an allergy clinic. About 204 patients took part in the study. Each of these patients was randomly assigned to one of the endorser groups ...
NIH Public Access - The Scripps Research Institute
NIH Public Access - The Scripps Research Institute

... The MAP-rFAAH structure remained as the only crystal structure of FAAH for many years. However, the high levels of expression of the h/rFAAH protein offered a new opportunity to solve structures of the enzyme that would be of great relevance to structure-based drug design. Indeed, as noted above, h/ ...
CANADA - CLG.ORG
CANADA - CLG.ORG

... 17. Like other atypical antipsychotics, the ABILIFY Products bind to several different neurotransmitter receptors, but unlike others in its class, it doesn’t block dopamine 2 (specifically, dopamine D2) or serotonin 3 (specifically, 5-HT1A) receptors. Instead, it’s a partial agonist 4 at those recep ...
Dyslipidemia update by Dr Sarma
Dyslipidemia update by Dr Sarma

... My ignorance of even the minute details of HT, DM My indifference to apply the current knowledge My negligence in screening for Lipids, DM, HT, LVH My despondency about preventing TOD and ACS My inadequacy in maintaining my patients ...
blueprint medicines corporation - corporate
blueprint medicines corporation - corporate

... biopharmaceutical company focused on improving the lives of patients with genomically defined diseases driven by abnormal kinase activation. The Company’s approach is to systematically and reproducibly identify kinases that are drivers of diseases in genomically defined patient populations and to cr ...
Renal Drug Metabolism - Pharmacological Reviews
Renal Drug Metabolism - Pharmacological Reviews

“All flesh is coupled by the wave of circular rotational similarity” 1
“All flesh is coupled by the wave of circular rotational similarity” 1

... science consists of several special directions. A fruitful professional dialog does not necessarily occur between experimenters and clinicians. We would like this book to be available not only for representatives of theoretical medicine (pharmacologists, physiologists, and immunologists), but also f ...
Prepared for NCI by Technical Resources International, Inc I.
Prepared for NCI by Technical Resources International, Inc I.

... phenol/furfural novolak-type resins (Brode, 1982). In this application, HMF is produced from glucose in the presence of phenol, with which it is polymerized using a basic catalyst. Acid-catalyzed dehydration of HMF yields OMBF (5,5'-oxydimethylenebis(2furfural)), an intermediate in the synthesis of ...
M P D U
M P D U

... wet AMD. 16 It also found evidence that Avastin and Lucentis could be administered effectively at longer intervals than the normal once-per-month schedule. Finally, NEI found that “serious adverse events (primarily hospitalizations)” occurred at a rate of 24 percent for patients receiving Avastin an ...
Dosage Adjustment for Cytotoxics in Renal Impairment
Dosage Adjustment for Cytotoxics in Renal Impairment

... impaired patients. Caution is recommended in this group. Glaxo Wellcome – although very little unmetabolised drug is excreted in the urine, a complex range of metabolites are excreted by this route. The administration of high-dose busulphan has been evaluated in 15 patients with multiple myeloma (4 ...
Dosage Adjustment for Cytotoxics in Renal Impairment
Dosage Adjustment for Cytotoxics in Renal Impairment

... impaired patients. Caution is recommended in this group. Glaxo Wellcome – although very little unmetabolised drug is excreted in the urine, a complex range of metabolites are excreted by this route. The administration of high-dose busulphan has been evaluated in 15 patients with multiple myeloma (4 ...
Dosage Adjustment for Cytotoxics in Renal Impairment
Dosage Adjustment for Cytotoxics in Renal Impairment

... impaired patients. Caution is recommended in this group. Glaxo Wellcome – although very little unmetabolised drug is excreted in the urine, a complex range of metabolites are excreted by this route. The administration of high-dose busulphan has been evaluated in 15 patients with multiple myeloma (4 ...
FETAL MORPHINE METABOLISM AND CLEARANCE ARE
FETAL MORPHINE METABOLISM AND CLEARANCE ARE

... a backpack and sham tethered. This allowed proper adjustment of the backpack straps and assessment of acceptance of the animal to the tether system. Only those animals who readily adapted to the system were studied. Surgery was performed under general anesthesia (isoflurane, nitrous oxide) using ste ...
ASD v2.0: updated content and novel features
ASD v2.0: updated content and novel features

... changes in its conformation and dynamics in response to the perturbation of an effector at a site distinct from the active site, also termed the allosteric site (1). The mechanisms of allosteric perturbation in cells are diverse, ranging from binding scenarios (with ions, lipids, small molecules, et ...
overview of comments received on community - EMA
overview of comments received on community - EMA

... For several of the extracts mentioned above, published data do not support a lower limit of hyperforin of 2 %. This applies to the extracts C) and G), as documented in the publications of Melzer et al. 1998, Wurglics et al. 2001a, Wurglics et al. 2001b, Volz and Zeller 2000) which mention hyperforin ...
Annex 1 - Emcdda
Annex 1 - Emcdda

... iodine atom is normally associated with the 4-position (Figure 1) which reflects historical developments explored by Shulgin and colleagues since the 1960s (Brandt, 2014). The "NBOMe" component refers to the N-(2-methoxybenzyl) part of the molecule (Figure 1). Two more isomers are possible that carr ...
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Drug discovery



In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which new candidate medications are discovered. Historically, drugs were discovered through identifying the active ingredient from traditional remedies or by serendipitous discovery. Later chemical libraries of synthetic small molecules, natural products or extracts were screened in intact cells or whole organisms to identify substances that have a desirable therapeutic effect in a process known as classical pharmacology. Since sequencing of the human genome which allowed rapid cloning and synthesis of large quantities of purified proteins, it has become common practice to use high throughput screening of large compounds libraries against isolated biological targets which are hypothesized to be disease modifying in a process known as reverse pharmacology. Hits from these screens are then tested in cells and then in animals for efficacy.Modern drug discovery involves the identification of screening hits, medicinal chemistry and optimization of those hits to increase the affinity, selectivity (to reduce the potential of side effects), efficacy/potency, metabolic stability (to increase the half-life), and oral bioavailability. Once a compound that fulfills all of these requirements has been identified, it will begin the process of drug development prior to clinical trials. One or more of these steps may, but not necessarily, involve computer-aided drug design. Modern drug discovery is thus usually a capital-intensive process that involves large investments by pharmaceutical industry corporations as well as national governments (who provide grants and loan guarantees). Despite advances in technology and understanding of biological systems, drug discovery is still a lengthy, ""expensive, difficult, and inefficient process"" with low rate of new therapeutic discovery. In 2010, the research and development cost of each new molecular entity (NME) was approximately US$1.8 billion. Drug discovery is done by pharmaceutical companies, with research assistance from universities. The ""final product"" of drug discovery is a patent on the potential drug. The drug requires very expensive Phase I, II and III clinical trials, and most of them fail. Small companies have a critical role, often then selling the rights to larger companies that have the resources to run the clinical trials.Discovering drugs that may be a commercial success, or a public health success, involves a complex interaction between investors, industry, academia, patent laws, regulatory exclusivity, marketing and the need to balance secrecy with communication. Meanwhile, for disorders whose rarity means that no large commercial success or public health effect can be expected, the orphan drug funding process ensures that people who experience those disorders can have some hope of pharmacotherapeutic advances.
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