PHT121- Lecture 1-States of Matter- Summer 2024.pdf

Pharmaceutics Department Physical Pharmacy PHT121 Spring 2024 Lecture (1) States of matter 1  :‫الرسالة‬ ‫ بشراكة‬،‫ كلية الصيدلة جامعة أكتوبر للعلوم الحديثة واالداب معتمدة محليا‬ ‫ تلتزم بتخريج...

Pharmaceutics Department Physical Pharmacy PHT121 Spring 2024 Lecture (1) States of matter 1  :‫الرسالة‬ ‫ بشراكة‬،‫ كلية الصيدلة جامعة أكتوبر للعلوم الحديثة واالداب معتمدة محليا‬ ‫ تلتزم بتخريج صيدلى لادر على المنافسة فى أسواق العمل المحلية و‬،‫بريطانية‬ ‫ و أن يكون عضو فعال فى الفريك الطبى بتمديم أفضل‬،‫الدولية و ريادة االعمال‬ ‫ من خالل برنامج تعليمى متميز و‬،‫ مراعيا أخالليات المهنة‬،‫رعاية صحية‬ ‫ وكذلن تلتزم الكليه بمديم خدمات مجتمعية فعالة و‬،‫أعضاء هيئة تدريس أكفاء‬.‫أبحاث علمية تطبيمية متميزة‬ Mission: The Faculty of Pharmacy of October University for Modern Sciences and Arts is nationally accredited, has British partnership, and is committed to producing graduates who are able to compete in national and international job markets and entrepreneurship, and to be an effective member of the medical team providing best medical care, while heeding professional ethics, through an outstanding academic programme and proficient academic staff. The faculty is devoted also to provide effective community services, and exceptional applied scientific 2 research.  :‫الرؤية‬ ‫كلية رائدة فى‬MSA ) ( ‫كلية الصيدلة جامعة اكتوبر للعلوم الحديثة و االداب‬ ‫مجال التعليم و البحث العلمى و المشاركة المجتمعية على المستوى المومى و‬.‫االلليمى و لها ترتيب متمدم فى التصنيف العالمى لكليات الصيدلة‬ Vision: The Faculty of Pharmacy of October University for Modern Sciences and Arts is a pioneer in tutelage, scientific research, and community service at the local and regional levels, and holds an advanced position among its counterparts in international Pharmacy subject ranking. 3  Aims/Objectives of the course This module aims to provide students with knowledge of physicochemical principles essential for the design and formulation of pharmaceutical products. Students are introduced to the fundamental concepts of states of matter, Phase equilibrium, colligative properties, isotonicity solubility, dissolution, partition coefficient, surface and interfacial phenomena, surface active agents, adsorption and its application in pharmacy and rheological behavior of dosage forms 4 4 Course assessment details for PHT 121 Mid-Term Examination 30 marks (1 hour) Final-term Examination 60 marks (2 hours) Oral Examination none Practical Examination 40 marks (2 exams before and after midterm) Lab evaluation: 5 marks Lecture evaluation: 5 marks Quizzes (average) 5 marks (2 quizzes 1 before and 1 after midterm) Assignment(s) 15 marks Total 150 marks 5  Course learning outcomes design, prepare, analyze, handle, identify, and affecting pharmaceutical and assure quality of preparesynthetic preparations such as solubility, 3. Mapping MLO to programme and NARS key elements synthetic/natural pharmaceutical products. pH, surface and interfacial phenomena, rheology, diffusion NARS Key element Programme Key element Module learning outcome (MLO) pharmaceutical and dissution, colligative 1-1-1 Demonstrate 1-1-1-1 Utilize 1-1-1-1-1 Utilize the physical materials/products. properties and polymers. comprehended principles applied in pharmacy, 2-2-4 Adopt the principles 2-2-4-3 Adopt principles of 2-2-4-3-1 Calculate problems understanding of knowledge knowledge of principles of basic and polymers, and pharmaceutical of pharmaceutical pharmaceutical calculations related to solutions and of pharmaceutical, pharmaceutical sciences. preparations. calculations, biostatistical applied in development of solubility, vapour pressure, biomedical, social, analysis, bioinformatics, rheological properties, ionization behavioral, administrative, different dosage forms and drug pharmacokinetics, and degree, polymers and colligative and clinical sciences. bio-pharmaceutics and delivery systems. properties using the principals of their applications in new pharmaceutical calculations. 1-1-3 Integrate knowledge 1-1-3-1 Consolidate knowledge 1-1-3-1-1 Integrate the drug delivery systems, knowledge dose modification, from the bioequivalence studies, from fundamental sciences from fundamental sciences to physicochemical principles and pharmacy practice. to handle, identify, extract, 4-1-1 Demonstrate 4-1-1-1 Demonstrate effective 4-1-1-1-1 Demonstrate effective responsibility for team communication and team work communication of required work performance and peer skills and enhance time within a monitored time frame. evaluation of other team managementabilities. members, and express time management skills. Weekly plan Week Topic Week Topic  Orientation Lab One  Density  States of matter/Phase Equilibria  Concentration Problems One Two  Solubility Determination Two  Concentration Problems  Phase Equilibria Three  Effect of Electrolytes on Solubility Three  Solubility (1) Definitions, Types of solutions, Four  Solubilization Four  Solubility (2) Gas in liquid, Liquid in Liquid  Colligative properties Five  Partition Coefficient Five  Solubility (3) Solid in Liquid  Colligative properties Six  Colligative Properties Six  Practical Exam 1 Midterm Exams Midterm Exams Seven  Determination of HLB value Seven  Diffusion and Dissolution  Calculation of HLB value Eight  Surface phenomena (surfactants) Eight  CMC determination  Polymer molecular weight Nine  Surface phenomena (Adsorption)  Adsorption Nine  Polymer molecular weight  Rheology Ten  Viscosity Ten  Eleven  Polymers Eleven  Practical Exam 2 Twelve  Revision Final Exams Final Exams Attendance Policy -You are allowed in the lecture 15 min after the beginning of the lecture; after which you are welcome to attend but the attendance will not be recorded. Side talks are not allowed Any activities not related to the course are not allowed. All the faculty’s attendance rules and regulations are strictly applied. Interaction and concentration during the lecture is as important as attendance and will be graded If you don’t understand please make sure that you stop me and ask in a civilised manner; I will always be happy to repeat again but don’t leave the lecture without understanding 8  Course Rules Check the e-learning as all course-related materials, announcements, and lecturer information are present and updated regularly. Ungraded formative quizzes will be offered as a practice on the real quiz Extra lectures will be given every week, you are highly encouraged to attend the extra lecture as we will solve case studies and to ask any questions you might have. After each lecture, a discussion will be available on the forums in the course e- learning page, you can ask any questions related to this lecture and a lecturer will answer your question. The lecturers are always available to answer your questions, If you have any inquiries please reach out: 1) during office hours 2) Via Email. 12 Lecture Evaluation (5 marks) There will be graded activities inside the lectures. A problem will be presented at the end of the lecture, and you have to submit it solved in the lab the following week to receive its grade. Your participation will be graded in the lecture. Each lecture will have an evaluation of 5 marks from coursework grades based on the following: 1) Behavior: 2 marks 2) Submission of Homework problem: 2 marks 3) Lecture activities and participation: 1 mark Each lecture will have several bonus activities that count towards the evaluation The evaluation grade at the end of the semester will be an average of all lecture evaluations As a student you are required to: Work hard Submit the homework on time Interact in the lecture and answer lecture activities Study lectures and labs week by week Any questions you have please reach out via lecture forum discussion, extra hours, office hours and e-mail Submit your assignment on time Solve the previous exams on the e-learning page.  References and recommended books: http://www‐biol.paisley.ac.uk/courses/stfunmac/glossary/front.html http://www.nordicrheologysociety.org http://www.rpi.edu/dept/chem‐eng/Biotech‐Environ/Adsorb/adsorb.ht m http://www.tabletdissolution.com/index.php Martin’s Physical Pharmacy & Pharmaceutical Sciences (6th ed.). Lippincott Williams & Wilkins, ISBN 0781797667, 9780781797665 Florence & David, Physicochemical Principles of Pharmacy (4th edn.), 2011. Alexander.T. AttwoodPharmaceutical Press, 2005 ISBN 085369608X Pharmaceutics. Michael. E. Aulton, Aulton Pharmaceutics The Design and Manufacture of Medicines , 2017 (5th edition), Churchill Livingstone ISBN 9780702070020 1 2  Learning outcomes By the end of the lecture the students should be able to demonstrate knowledge and comprehension of: 1. Gases, liquids and solid are the three primary states of matter or phases 2. solid state , crystallinity, solvates and polymorphism 3. Different physical properties of matter 4. Applications of states of matter in pharmacy 11  Interactive teaching methods Video (https://www.youtube.com/watch?v=lPCeF9KcWh0) Open discussion Student Activity 12 214 What is Physical Pharmacy?? Physical pharmacy is the branch of pharmacy that concentrates on the applications of mathematics, physics and chemistry to the study of pharmacy. In other words: It is the basic science of how dosage forms are affected by their physical and chemical properties It affects all the formulations and dosage forms and it is the basis for your study in pharmaceutics We will study, Solubility, Surface properties, Rheological Properties and Polymers in pharmacy But first, Let’s start by the basics, States of Matter  States of Matter States of matter are determined by the attractive forces between the particles. In order for molecules to exist in aggregates in gases, liquids and solids Intermolecular forces must exist. GASES LIQUID SOLID Week intermolecular forces Van der Waals forces of attraction The intermolecular force between The thermal motions of molecules of leads to some degree of coherence molecules are so strong , so it is substance can overcome the between the molecules of liquid. hardly influenced by thermal attractive force that exist between motions. the molecules. 2  Intermolecular forces Ion-Ion interactions Strongest Intermolecular forces Ion-dipole interactions Dipole-dipole (H-Bonding) Van der Waals Forces=London Dispersion forces Weakest Pure substances are either Elements or Compounds Mixtures Mixtures tend to retain the properties of their individual substances. Homogeneous Mixtures In a homogeneous mixture, the parts of the mixture look the same and appears to contain only one substance. A solution is a homogeneous mixture in which one substance in dissolved into another. (will be discussed the next lecture) Do you know an example of a solution?  Heterogeneous Mixtures In a heterogeneous mixture, the parts of the mixture are noticeably different from one another. Particles are suspended not Particles are suspended and dissolved into another not dissolved into another substance. substance. Colloids appear to They will separate into layers homogeneous, but under a over time microscope they are not. They do not separate into layers Example: sand in water. over time. Example: Milk Suspension Colloid Homogoneous Mixture Hetrogenous Mixture Physical Vs. Chemical Change Changing states of matter is an example of physical change Changing states of matter 28 Changing states of matter Effect of Temperature As the temperature of a solid, liquid or gas increases, the energy of the particles increases and particles move more rapidly and further from each other As the temperature falls, the particles slow down. If a liquid is cooled sufficiently, it forms a solid. (condensation) If a liquid is heated sufficiently, it forms a gas. (evaporation) Changing states of matter Effect of Pressure Pressure bring the particles of matter closer and closer by applying pressure on them. So, liquids can be converted into solids by applying pressure and When we apply pressure on a gas enclosed in a cylinder, it starts compressing and converting into liquid.  Liquefaction of Gases (Condensation) · When a gas is cooled, it loses some of its kinetic energy, and the velocity of the molecules decreases--- --Changes to liquid · critical temperature: Above which it is impossible to liquefy a gas irrespective of the pressure applied · critical pressure: The pressure required to liquefy a gas at its critical temperature · The further a gas is cooled below its critical temperature, the less pressure is required to liquefy it. Activity: Can you find out what is the critical temperature and pressure of water? (373°C at 217 atm)  Melting point of solids · The temperature at which a liquid passes into the solid state is known as the freezing point. It is also the melting point of a pure solid · Normal freezing or melting point (at 1 atm) · heat of fusion: the heat required to increase the intermolecular distances in solids, thus allowing melting. · Molecular weight, type of intermolecular bonds and molecular configuration, all can affect melting and freezing point of compounds. ·How intermolecular forces affect the heat of fusion??? ·The stronger the intermolecular forces the higher the heat of fusion.  Boiling (Evaporation) · The temperature at which the pressure of the vapour above the liquid equals the atmospheric pressure (1 atm) is known as the boiling point. · The boiling point may be considered the temperature at which thermal agitation can overcome the attractive forces between the molecules of a liquid. · Therefore, the boiling point of a compound, provides a rough indication of the magnitude of the attractive forces. · Activity: Polar molecules usually have higher boiling point than nonpolar. WHY?? · As polar compounds have stronger intermolecular forces than non polar compounds ( polar bonds are stronger) 33 Activity Identify as physical or chemical change When wood is burnt is this considered Chemical Compression of a powder to a tablet form. Physical Changing of states of matter Physical Rusting of silver Chemical Pharmaceutical Applications for different states of matter  Gases in Pharmaceuticals: Aersols · Aerosols are products that depend on the power of a liquified gas to expel the contents of the container. · They are a mixture of the drug formula and a propellant. · Propellant: material that is liquid under the pressure conditions existing inside the container but that forms a gas under normal atmospheric conditions. · If the drug is nonvolatile, it forms a fine spray as it leaves the valve orifice; · at the same time, the liquid propellant vaporizes off and turns to gas · Examples of propellants: Chlorofluorocarbons · Activity: What are Metered dose inhalation products??? · Device that delivers a specific amount of medication to the lungs in the form of aerosol. 36 Liquids in Pharmacy Liquid dosage forms are pourable pharmaceutical formulations which contain a mixture of active drug components and nondrug components (excipients) dissolved or suspended in a suitable solvent or mixtures of solvents. Activity: What are the examples of liquid dosage forms: Such as: Syrup. Suspension. Solutions. Drops. Emulsion. Mixture. Linctus. Elixir.  SOLIDS & CRYSTALLINE STATE more than 80% of pharmaceuticals are solid formulations 38  Polymorphism When a substance has more than one molecular arrangement, they are designated as polymorphs and the phenomenon as polymorphism. Polymorphs: when one substance have the same chemical composition but different internal structure (Molecular arrangement) Crystalline Form Amorphous form The solids in which the particles of matter are The solids in which the constituent particles arranged and organized in a specific manner. of matter are arranged in a random manner The crystalline form a has a lower energy at The absence of crystalline structure leads to the molecular level with stronger bonding weak bonds intermolecular bonds and higher (mostly ionic) between molecules that require molecular energy higher energy to break. More stable Less stable Lower Solubility Higher Solubility Higher melting point Lower melting point 40  Why we study polymorphism? · Depending upon their relative stability, one of the several polymorphic form will be physically more stable than others. · Stable polymorph represents the lowest energy state, has highest melting point and least aqueous solubility. · Metastable form represent the higher energy state, have lower melting point and high aqueous solubility · Metastable form shows better bioavailability and therefore preferred in formulations. · Metastable form converts to the stable form due to their higher energy state. The reversible change between polymorphs is called enantiotropic (by varying temperature and pressure) The irreversible change between polymporphs is called monotropic (usually from metastable to stable form) 19  The most common example of polymorphism Carbon carbon atoms diamond Graphite in sheet graphite of a hexagonal carbon: diamond in a cubic (tetrahedral lattice lattice arrangement ) Diamond is metastable and converts very slowly to graphite which is more stable  Cocrystal  A co-crystal is a crystalline structure made up of two or more components in a definite ratio, where each component is defined as either an atom, ion, or molecule.  Solvates  Solvates are cocrystals formed when the solvent is trapped inside crystal lattice  When the trapped solvent is water, it is termed Hydrate.  When the water is removed from hydrate, it will be in anhydrous form Polymorphism affects many physical properties in drugs such as:  Melting point  Color  Solubility  Bioavailability  Stability Solubility is very important in pharmaceutical processes including dissolution and formulation. Activity: Does polymorphism affect chemical properties? Answer: No, as the chemical structure is the same  Polymorphism in Pharmaceutics  The crystalline from of the antibiotic novobiocin is poorly absorbed and has no activity, where the amorphous form is readily absorbed and therapeutically active, due to different dissolution rate.  Fluoxetine HCl, the active ingredient in the antidepressant drug Prozac. is amorphous which will have increased solubility compared to the crystalline form  CELECOXIB is a nonsteroidal anti-inflammatory drug with the higher bioavailability was shown by the amorphous state Activity: What is the disadvantage of using a drug in an amorphous state? Answer: It will be less stable Homework Problem: A pharmaceutical company is developing a new drug, Compound A. During the early stages of development, they discover that Compound A can exist in two different polymorphic forms: Form I and Form II. The company conducts a series of experiments to characterize the physical and chemical properties of the two polymorphs. They find that Form I is more soluble in water than Form II and Form II is more stable than Form I. 1) Predict the type of polymorph of each form and justify your answer. 2) Which polymorph would be more suitable for formulation in an immediate-release dosage form?  Any Questions See you in lecture 2 For Next Lecture, Answer the following Questions What is a saturated solution? Do solids have vapour pressure? 37 49