PHARM 24
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| What is Pharmaceutical Sciences? | A dynamic and interdisciplinary field that aims to integrate fundamental principles of physical and organic chemistry, engineering, biochemistry, and biology to understand how to optimize delivery of drugs to the body and translate this integrated understanding into new and improved therapies Important points: Integrate fundamental principles of physical and organic chemistry, engineering, biochemistry, and biology Understand how to optimize delivery of drugs to the body and translate this understanding into new and improved therapies |
| What is Physical Pharmacy? | Area of pharmacy dealing with quantitative and theoretical principles of physicochemical science as they apply to the practice of pharmacy Integrates knowledge of mathematics, physics and chemistry and applies them to the pharmaceutical dosage form development. |
| What is the help of Physical Pharmacy course? | Leads to proper understanding of subsequent courses in Pharmaceutics and pharmaceutical technology. Aided the pharmacists and pharmaceutical scientists to predict the solubility, stability, compatibility and biologic action of drug products. |
| Procardia XL | Similar appearance to a conventional tablet Semi-permeable membrane surrounding an osmotically active drug core divided in 2 layers : active & push layers Fluid from GIT increases pressure in the osmotic layer and “push” against the drug layer Designed to provide constant rate over 24 hrs Inert components remain intact during GI transit and eliminated in the feces |
| Patient Counselling on XL tablets | Do not crash, chew or break Swallow the tablet whole with a glass of water Tablet form found in stool may be the outer shell of the tablet only Eventually, outer shell of the depleted tablet passes out through feces |
| Pharmacists must be able to translate the complex scientific principle to a __ | Simple, practical and useful recommendation for a patient |
| 2 types of error | Determinate (constant) Indeterminate (random or accidental) |
| What are constant errors and random/ accidental errors | Constant or determinate errors can be avoided, determined or corrected Random or indeterminate errors occurs by accident or by chance |
| Usually present in each measurement and affect all observations of a series in the same way | Constant errors ex. Errors in calibration, in weighing operations Impurities in the reagents and drugs, in matching colors Personal Errors such as in pouring and mixing, Reading of meniscus, in calculations, etc. Change of volume of solutions with temperature |
| Reducing determinate errors in analytic work | 1. By using a calibrated apparatus 2. Using blanks and controls 3. Using several different analytic procedures and apparatus 4. Eliminating impurities-ex.filtration. purification 5. Carrying out the experiment under varying conditions 6. In manufacturing, eliminate errors by calibrating the weights and apparatus and by checking results and calculations with other workers. |
| How to reduce Pseudo accidental or variable determinate errors | 1. Control the conditions through use of constant temperature baths or ovens 2. Use of buffers. (resist changes in pH) 3. Maintenance of constant humidity and pressure where indicated 4. Careful reading of fractions of units on graduates, balances and other apparatus |
| Inversion relationship of P&V at constant T | • Boyle’s Law |
| Direct relationship of V&T at constant P | • Charles’ Law |
| It states that the amount of gas dissolved in a solution is proportional to the partial pressure of the gas in the equilibrium with the solution. | • Henry’s Law of Gas Solubility |
| The total pressure in a mixture of gases is equal to the sum of the partial pressure of each gas | • Dalton’s Law of Partial Pressure |
| It is the pressure of gas exerted if it alone occupied the whole volume of the mixture | • Partial Pressure |
| States that the rate of effusion of a gas is inversely proportional to the gas’ molar mass | • Graham’s Law |
| Direct relationship of P&T at constant V | • Gay-Lussac’s Law |
| At the same temperature and pressure, Equal volumes of gases contain equal numbers of moles | • Avogadro’s Law |
| Aka Ideal Gas Laws | • Combined Gas Laws |
| Temperature above which liquid can no longer exist | • Critical Temperature (TC) |
| It is the pressure required to liquefy a gas at TC | • Critical Pressure (PC) |
| Methods of Achieving Liquefaction | • Subject to intense cold by the use of freezing mixtures • Adiabatic expansion • Joule-Thomson effect |
| Ideal gas to expand, done in vacuum or dewar flask where it uses its on energy content – drop of temperature can liquefy a gas | • Adiabatic expansion |
| Gas does external work | • Joule-Thomson effect |
| Vapor pressure of liquids | • When a liquid is placed in an evacuated container at a constant temperature, the molecules with the highest energies break away from the surface of the liquid and pass into the gaseous state, and some of the molecules subsequently return to the liquid state, or condense. |
| It is the relationship between the vapor pressure and the absolute temperature of a liquid is expressed by the | • Clausius-Clapeyron Equation |
| • Refers to the quantities of heat that are taken up when the liquids vaporize | Heat of Vaporization |
| SOLIDS characteristics | • Characterized as having fixed/definite shapes • Arranged in units • Nearly incompressible • Have strong intermolecular forces • Very little kinetic energy |
| What are the types of solid? | • Crystalline • Amorphous |
| Occurs by precipitation of the compound out of a solution into an ordered array | • Crystallization • Shows definite melting points |
| Variables that influence crystallization | • Solvents used • Temperature • Pressure • Crystalline array pattern • Purity of material • Salts |
| Have definite geometric forms with 6 common crystalline structures; what are these 6 common structures? | • Cubic • Tetragonal • Hexagonal • Rhombic • Monoclinic • Triclinic |
| What compounds have cubic forms | • Sodium Chloride • Halite • Table Salt • KBr • LiCl • RbI • MgO • CaO • AgCl |
| What compound is a rhombic form? | • Iodine |
| What compounds have monoclinic forms? | • Sucrose • Table sugar • Rectangular prism with a parallelogram as its base • Beet sugar |
| What compounds have triclinic forms? | • Boric acid (aka borax) • 3 axes of different lengths intersecting at oblique angles |
| Theobroma Oil Polymorphic forms | • Unstable gammar form (18C) • Alpha form (22C) • Beta prime form (28C) • Stable beta form (34C) |
| What are the types of Polymorphism? | • Enantiomorphic (change is reversible) • Monotropic (change is unidirectional) • Isotropic (identical in all directions) • Anisotropic (different in all directions) |
| (change is reversible) | • Enantiomorphic |
| (change is unidirectional) | • Monotropic |
| (identical in all directions) | • Isotropic |
| (different in all directions) | • Anisotropic |
| A co-crystal created out of different solvents when a pharmaceutical solid is synthesized through chemical methods, purifications & crystallizations. | • Solvates/Pseudopolymorphs |
| Amorphous Solids characteristics | • Aka glasses or supercooled liquids • Non-crystalline; no definite order • No definite shape and no definite melting poits • Tend to flow when subjected to pressure • Amorphous form of drug is readily absorbed and therpeutically active |
| Temperature at which liquid passes into the solid state | • Freezing point |
| The heat absorbed when 1 g of a solid melts or the heat liberated when it freezes | • Latent Heat of Fusion |
| Latent Heat of Fusion of water at 0C | 80cal/g (1436 cal/mole) |
| States that a system at equilibrium readjusts so as to reduce the effect of an external stress | • Le Chatelier’s Principle |
| It is the liquid crystalline phase | • Mesophase |
| TYPES OF PLASMA | • SMECTIC • NEMATIC • CHOLESTERIC |
| Smectic | • Soap-like / grease-like • Rotate in one axis • Mobile in 2 directions • Most pharmaceutically important |
| Nematic | • Thread-like • Rotate in one axis • Mobile in 3 directions |
| Significance of Smectic | • Solubilization of water insoluble materials will enchanced physical stability of emulsions |
| What are the molecules that form mesophases? | • Organic • Elongated and rectilinear shape • Rigid • Possess strong dipoles and easily polarizable |
| Methods of Formation | • Lyotropic • Thermotropic |
| Liquid crystals are formed using solvents | • Lyotropic |
| Liquid crystals are formed using heat | • Thermotropic |
| Examples of Thermotropic | • Cholesteryl benzoate (145C solid, 179C liquid state turbid) discovered by Reinitzer (1888) |
| • A mesophase formed from the gaseous state where tha gas is held under a combination of temperatures and pressures that exceed the critical point of substance | Supercritical fluids |
| Significance of Supercritical Fluids | • Extraction • Crystallization • Preparation of formulations (Polymer mixtures, micro- and nanoparticles) • Reduces toxicity of gases • Reduced need for hazardos solvents |
| Types of Systems Used to Describe Thermodynamic Properties | Open System Closed System Isolated System |
| States that if two thermodynamic systems are each in thermal equilibrium with a third, then all three are in thermal equilibrium with each other. | Zeroth Law of Thermodynamics |
| First Law of Thermodynamics | Law of Conservation of Energy Energy is constant. cannot be destroyed or created |
| Second Law of Thermodynamics | Law of Entropy Entropy (Disorderliness) |
| Third Law of Thermodynamics | Law of Absolute Zero When a system has a temperature of 0 Kelvin, absolute zero (the lowest temperature), the entropy (energy that cannot be used to do work) is at zero never happens |
| Microscopic Physical States with Different Degree of Orders: | Amorphous state Crystalline state Hydrated state Solvated state |
| Minimal quantity | Crystalline state |
| Property of drug product if it contains water or not. | Hydrated state |
| Ability of drug product to dissolve in a solvent. | Solvated state |
| Physical Change | - Appearance - Melting Point - Clarity and Color of Solution - Moisture - Crystal Modifications (Polymorphism) - Particle Size |
| Consant Heat | Adiabatic |
| Constant Temperature | Isothermic |