Session 1: Drug metabolism.
One of the most challenging advanced research areas in pharmacology with in the new millennium is to know why every individual respond differently to drug therapy and to what extent that individual variability in disposition is liable for the observed differences in therapeutic efficacy and adverse reactions. Drug metabolism reactions are of two stages: stage 1 (functionalization) reactions like oxidation, hydrolysis; and stage II (conjugation) reactions like glucuronidation, sulfate conjugation. Newly introduced drugs are associated with 551 bioactivity points from ChEMBL (65.5%), manual curation from literature (24.14%), the Guide to Pharmacology (6.17%) and approved drug labels (4.17%), respectively; as well as 109 mechanism of action (MoA or Tclin proteins—vide infra) targets, with kinases (26%) and enzymes (21%) representing the major target categories, followed by G-protein-coupled receptors—GPCRs (17%) and tumor-associated antigens (9%).
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Session 2: Absolute & Relative bioavailability
Absolute Bioavailability:
Compares the bioavailability of the active drug in systemic circulation following Non-intravenous administration with an equivalent drug following intravenous administration for drugs administered intravenously, bioavailability is 100%. Determination of the best administration route
Relative Bioavailability:
Compares the bioavailability of a formulation (A) of particular drug in comparison with another formulation (B) of an equivalent drug.
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Session 3: Factors affecting Bioavailability of a Drug
Factors affecting bioavailability are differentiated into pharmaceutical and pharmacological factors. Disintegration, dissolution and absorption affects the bioavailability of drugs. Pharmaceutical factors are particle size, nature of excipients and adjuvants, degree of ionization...Pharmacological factors are gastric emptying and gastrointestinal motility, gastro intestinal diseases, food and other substances, first pass metabolism, drug-drug interactions, and route of administration.
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Session 4: First pass metabolism.
The first pass effect is a phenomenon in which a drug gets metabolized at a specific location in the body that results in a reduced concentration of the active drug upon reaching its site of action or the circulation. The first pass effect is usually related to the liver, as this is often a serious site of drug metabolism. Let’s take a example of 100 drug molecules that are ingested in pill form. Only 90 of those molecules survive the alimentary canal . Then 81 make it past the gut wall and into the hepatic portal vein . Of the 81 that enters the liver, only 41 can make it to the systemic circulation. Thus the bioavailability is 41/100 = 41%. We also know the fraction that was passed through the gut (90/100 = 90%), the gut wall (81/90 = 90%), and the liver (41/81 = 50%). If you multiply each of these fractions together (90% * 90% * 50% = 41%) you reach the overall bioavailability for the drug. However, the primary pass effect also can occur within the lungs, vasculature, GI tract, and other metabolically active tissues within the body. This effect can become augmented by various factors like plasma protein concentrations, enzymatic activity, and gastrointestinal motility. The extent to which a patient may experience the first pass effect varies from patient to patient, and this must even be taken into consideration when determining appropriate dosing. If the first-pass effect is exceptionally prominent in patient, the drug may require administration via different route to bypass the first-pass effect.
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Session 5: Concept of Equivalents & Pharmaceutical equivalents.
Pharmaceutical equivalents are drug products in identical dosage forms and route(s) of administration that contain identical amounts of the identical active drug ingredient, i.e., an equivalent salt or ester of the same therapic moiety, or, with in the case of modified-release dosages that need a reservoir, such forms as prefilled syringes where the volume may vary, that delivers identical amounts of the active ingredient over the identical dosing period; it don't necessarily contain an equivalent inactive ingredients; and meet the identical compendial or other applicable standard of identity, strength, quality, and purity, including potency and, where applicable, content uniformity, disintegration times, and/or dissolution rates.2 They will differ in characteristics like shape, scoring configuration, release mechanisms, packaging, excipients (including colours, flavours, preservatives), expiration date/time, and, within certain limits, labelling.
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Session 6: Pharmacokinetic and pharmacodynamics.
Pharmacokinetics is the study of absorption, distribution, metabolism and excretion of drug. The main concept of pharmacokinetics is elimination of chemical xenobiotic from the body.Pharmacodynamics is that the study of the biochemical and physiological effects of drug with the body. The interaction of drug with the receptors located either in the cell membrane or intercellular fluids.
Keywords: Bioavailability Congress | Bioequivalence Congress | Bioavailability Meetings | Bioequivalence Meetings | Bioavailability Workshops | Bioequivalence Events | Bioavailability & Bioequivalence Conferences | Bioavailability Conferences
Introduction
The pharmaceutical industry is comprised of companies engaged in researching, developing, manufacturing and distributing drugs for human or veterinary use. New drugs have an enormous positive influence on global health, prosperity and economic productivity by saving lives, increasing life spans, reducing suffering, preventing surgeries and shortening hospital stays. Advances in medicine have eliminated deadly diseases and have brought other life-threatening conditions under control. Drug therapy is now an integral part of nearly every facet of healthcare, and new breakthroughs promise to revolutionize the treatment of non-communicable diseases.
Industry Overview and Competitiveness:
Large, diversified and global, the U.S. pharmaceutical industry is one of the most critical and competitive sectors in the economy. According to the Pharmaceutical Research and Manufacturers Association (PHRMA), more than 810,000 people work in the biopharmaceutical industry in the United States across a broad range of occupations, such as scientific research, technical support and manufacturing. Directly and indirectly, the industry supports over 3.4 million jobs across the United States and added an estimated $790 billion to the economy in 2014. Although manufacturing jobs supported by the industry are expected to decline over the next decade due to continued productivity gains, it will remain an important source of high paying jobs, providing salaries way above the national average.
Research and development (R&D)
The pharmaceutical sector has consistently been one of the most R&D intensive industries in the United States. The research-based industry generally allocates around 15 to 20 per cent of revenues to R&D activities and invests over $50 billion on R&D annually. Although the United States remains the global leader in innovative R&D investment, producing more than half the world’s new molecules in the last decade, its continued leadership cannot be taken for granted. R&D performed in the United States has become increasingly expensive relative to emerging economies in Asia, such as China and Singapore, where governments have enacted policies to attract investment and are poised for future growth. Conditions that limited R&D offshoring in the past, such as market proximity and availability of talent, are rapidly shifting.
The worldwide market for pharmaceuticals is projected to grow from around $1 trillion in 2015 to $1.3 trillion by 2020, representing an annual growth rate of 4.9 per cent. Several global demographic and economic trends are driving pharmaceutical consumption, including a rapidly aging world population and an associated rise in chronic diseases, increased urbanization and higher disposable incomes, greater government expenditure on healthcare and growing demand for more effective treatments.
Scope and Importance:
FDA ensure that the drug product for marketing should be safe, effective and meet all applicable standards, for this FDA requires bioavailability/pharmacokinetic studies and, where necessary, bioequivalence studies for all drug products (FDA Guidance for Industry, 2003). The U.S. Food and Drug Administration (FDA) define bioavailability as "the rate and extent to which the active drug ingredient or therapeutic moiety is absorbed from a drug product and becomes available at the site of drug action". Generally direct and indirect methods use to assess drug bioavailability.
Societies/Industries/Universities Associated with Pharmaceutical Technology and Development:-
International Society of Pharmaceutical Compounding (ISPhC)
Major Pharmaceutical Associations around the Globe
Conclusion:
The bioavailability of medicine in recent years has become interesting subject in drug development and also within the early stages of drug discovery. This is a tool to finding that the majority of the candidate drugs that failed in clinical trials due to problems with toxicology and absorption, distribution, metabolism, excretion i.e. ADME, rather than through lack of efficacy. The very hard efforts are being made within the pharmaceutical industry to enhance success rates by taking under consideration the toxicology and ADME aspects in drug discovery. Therefore, it's not surprising to envision that the amount of publications on bioavailability of drug has been highly increasing steadily for some times. In this review, attention is targeted to briefly discuss some terms of bioavailability, absolute bioavailability, and relative bioavailability, measurement of bioavailability and in-vitro dissolution and bioavailability, in-vitro in-vivo correlation, biopharmaceutical classification system, bioequivalence.