importance of inorganic in pharmacy

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Slide1:

[BASIC INORGANIC & PHYSICAL CHEMISTRY : PST 04103] LECTURE JAMES D. Bpharm .

COURSE CONTENTS:

COURSE CONTENTS ENABLING OUTCOME SUB – ENABLING OUTCOME RELATED TASKS TO BE TAUGHT. ASSESSMENT CRITERIA Describe concepts of Inorganic & Physical Chemistry in relation to medicines 4.1.1 Describe the relevance of Inorganic & Physical Chemistry in Pharmacy . Explain the Importance of studying Chemistry in Pharmacy. Outline the Chemical and Physical nature of Drugs Explain the application of Chemistry in Pharmacy. Relevance of Chemistry in Medical field is correctly understood. -do- 4.1.2 Write & Balance Chemical Equations and Reactions. Differentiate between Terms used in Chemistry Distinguish different branches of Chemistry Explain Basic concepts and Principles of Chemistry Basic Chemical Equations and Reactions are properly known. -do- 4.1.3 Describe Mixtures, Solutions and Compounds Define Mixtures Define Solutions Define Compounds Mixtures, Solutions and Compounds are correctly described. -do- 4.1.4 Describe Acids, Bases and Salts. Outline Acids Outline Bases Outline salts Acids, Bases and Salts are correctly described.

Introduction to Chemistry:

Introduction to Chemistry BASIC INORGANIC & PHYSICAL CHEMISTRY

Objectives:

Objectives Define chemistry Define matter Classifying pure substances as elements or compounds Describe the characteristics of and element and compound Distinguish pure substance from mixtures Classify mixtures as solutions, suspensions, or colloids

Slide5:

Chemistry Referred to as the “central science” Bridges between physics and biology Biochemistry Material science Friday, October 02, 2015 JAMES D. 5

Slide6:

Chemistry The study of matter and the transformations it undergoes Matter —“stuff” Anything that has mass and occupies space Transformation —“change” Changes in matter Friday, October 02, 2015 JAMES D. 6

Introduction to Chemistry:

Introduction to Chemistry Definition of Chemistry; - study of matter and the changes it undergoes Chemistry is Divided into five major Branches; Organic: study of essential all substances containing carbon Inorganic : study of substances that do not contain carbon Analytical: study of the composition of substances Friday, October 02, 2015 JAMES D. 7

Introduction to Chemistry Cont.:

Introduction to Chemistry Cont. 4. Physical: study of theories and experiments that describe the behavior of chemicals and energy involved. 5. Biochemistry: study of the chemistry of living organisms. Friday, October 02, 2015 JAMES D. 8

Inorganic Chemistry:

Inorganic Chemistry The study of chemicals that do not contain carbon. Friday, October 02, 2015 JAMES D. 9

Organic Chemistry:

Organic Chemistry The study of chemicals that contain carbon. Origin: study of chemicals in living organisms. Friday, October 02, 2015 JAMES D. 10

Organic or Inorganic ?:

Organic or Inorganic ? Sulfuric Acid H 2 SO 4 Methane CH 4 Hydrochloric Acid HCl Ethane C 2 H 6 Friday, October 02, 2015 JAMES D. 11

Analytical Chemistry:

Analytical Chemistry Composition of matter. Ex: Mass Spectrometer Gas Chromatograph Friday, October 02, 2015 JAMES D. 12

Physical Chemistry:

Physical Chemistry The study of : The mechanism The rate The energy transfer that happens when matter undergoes change. Friday, October 02, 2015 JAMES D. 13

Biochemistry:

Biochemistry Study of processes that take place in organisms. Friday, October 02, 2015 JAMES D. 14

Science:

Science What? Why? How? When? A scientist must ask Chemistry 15 Friday, October 02, 2015 JAMES D.

Science and Technology :

Science and Technology Science  Pure Does not necessarily have an application. Technology  Applied Has practical applications in society. Engineering & Pharmaceutical manufacturing Friday, October 02, 2015 JAMES D. 16

Question: Science or Technology?:

Question: Science or Technology? Studying or forming aspirin in a lab in small scale (small amounts). Friday, October 02, 2015 JAMES D. 17

Question: Science or Technology?:

Question: Science or Technology? Producing aspirin tablets so that consumers can use them. Friday, October 02, 2015 JAMES D. 18

Example: Discovery of Nylon by Wallace Carhers in 1930’sot:

Example: Discovery of Nylon by Wallace Carhers in 1930’sot Friday, October 02, 2015 JAMES D. 19

Importance of studying Chemistry in Pharmacy :

Importance of studying Chemistry in Pharmacy Chemistry, a branch of science , is the study of the composition, properties and behavior of matter . Chemistry is concerned with atoms and their interactions with other atoms and molecules. Chemistry is used in medicine quite a lot. All the synthetic medicines that we receive are made from various chemicals and their chemical reactions. Friday, October 02, 2015 JAMES D. 20

Importance of studying Chemistry in Pharmacy:

Importance of studying Chemistry in Pharmacy Chemistry is important to medicine because it helps in finding the cure to most diseases. Understanding chemistry also helps us to understand how vitamins, supplements and drugs can help or harm us. Chemical reactions occur when you breathe, eat or even sleep. Friday, October 02, 2015 JAMES D. 21

Importance of studying Chemistry in Pharmacy:

Importance of studying Chemistry in Pharmacy What about laboratory tests which doctors run on sick patients? What about radiation therapies? Chemotherapy is used to treat patients that have cancer. Where do you think medicinal drugs and therapies come from? In diagnosis and in understanding the environmental issues which may have effect of imposing impurities in medicines through their irreversible reactions like hydrolysis, polymerization and oxidation. Friday, October 02, 2015 JAMES D. 22

Importance of studying Chemistry in Pharmacy:

Importance of studying Chemistry in Pharmacy You need to know also that chemistry is good for the animal health. Chemistry is important in medicine because most diseases, injuries, and treatments involve chemicals and chemical processes. By understanding chemistry, we are able to develop drugs that fight disease, develop better nutrition, and develop healthier environments to avoid disease. Friday, October 02, 2015 JAMES D. 23

How do you use chemistry in a pharmacy? :

How do you use chemistry in a pharmacy? Pharmacies deal with medicines, and most medical compounds are small molecules like aspirin or ethanol, to larger biological molecules, mostly proteins like insulin or prolactin. So a pharmacist is doing a fair bit of chemistry, in addition to doing biology, medicine, and retail sales. Friday, October 02, 2015 JAMES D. 24

How do you use chemistry in a pharmacy?:

How do you use chemistry in a pharmacy? Pharmacists are not just concerned with how their chemicals affect the body of the patient, but they are also concerned with how the molecules interact with one another, how they affect the body in combination, and how they are delivered. To make a pill that survives the stomach acid, and is delivered into the intestines, can be complicated without chemistry background. Friday, October 02, 2015 JAMES D. 25

How do you use chemistry in a pharmacy?:

How do you use chemistry in a pharmacy? Some drugs must be injected or delivered through the skin in some other way, because they can’t pass through the digesting tract unaltered - most proteins are in this category. Some are inhaled for the same reason, or because they act faster that way. Knowing how chemistry affects drug delivery is an important part of designing pills, capsules, injectables , and inhalants. Friday, October 02, 2015 JAMES D. 26

How do you use chemistry in a pharmacy?:

How do you use chemistry in a pharmacy? In other cases, a drug might cause the body to produce an enzyme that breaks down another drug the patient might be taking. Understanding chemistry allows the pharmacist to suggest that the pills be taken at different times, or that another drug be substituted for one of the originals. Friday, October 02, 2015 JAMES D. 27

How do you use chemistry in a pharmacy?:

How do you use chemistry in a pharmacy? Chemistry helps us understand; Physicochemical Properties of Drugs useful in dosage forms designing and in achieving Drug Stability Drugs-Receptor Binding Interaction useful in managing bioavailability and Mechanism of Action of medicines and their Side Effects. Friday, October 02, 2015 JAMES D. 28

Physical and chemical Properties and Drug:

Physical and chemical Properties and Drug Physicochemical Properties and Drug depend on; Ionisation ( hydrophilicity ) Acidity or Basicity of a compound Lipophilicity Hydrogen bonding ( Partition coefficients) Molecular size Friday, October 02, 2015 JAMES D. 29

Ionisation (hydrophilicity) :

Ionisation (hydrophilicity) Ionisation = protonation or deprotonation resulting in charged molecules , about 85% of marketed drugs contain functional groups that are ionised to some extent at physiological pH (pH 1.5 – 8). Ionisation constants: pKa Friday, October 02, 2015 JAMES D. 30

Ionisation:

Ionisation The extent of ionisation of a compound can have a large effect on many biological properties, such as receptor/enzyme binding, binding to plasma proteins, CNS penetration, solubility and absorption. Once the pKa value of a molecule is known, then it is possible to calculate the proportion of ionised and neutral species at any pH. Friday, October 02, 2015 JAMES D. 31

Ionisation:

Ionisation So the same compound will be ionised to different extents in different parts of the body. This means that, for example, basic compounds will not be so well absorbed in the stomach than acidic compounds since it is generally the unionised form of the drug which diffuses into the blood stream. Friday, October 02, 2015 JAMES D. 32

2. Acidity or Basicity of a compound :

2. Acidity or Basicity of a compound The acidity or basicity of a compound plays a major role in controlling: Absorption and transport to site of action Solubility, bioavailability, absorption and cell penetration, plasma binding, volume of distribution Friday, October 02, 2015 JAMES D. 33

Acidity or Basicity of a compound :

Acidity or Basicity of a compound Binding of a compound at its site of action un-ionised form involved in hydrogen bonding ionised form influences strength of salt bridges or H-bonds Elimination of compound Biliary and renal excretion CYP P 450 metabolism Friday, October 02, 2015 JAMES D. 34

Acidity or Basicity of a compound :

Acidity or Basicity of a compound Fluid pH Aqueous humour 7.2 Blood 7.4 Colon 5-8 Duodenum (fasting) 4.4-6.6 Duodenum (fed) 5.2-6.2 Saliva 6.4 Small intestine 6.5 Stomach (fasting) 1.4-2.1 Stomach (fed) 3-7 Sweat 5.4 Urine 5.5-7.0 Friday, October 02, 2015 JAMES D. 35

Acidity or Basicity of a compound :

Acidity or Basicity of a compound Drugs are only absorbed passively when they are unionised. This is because the compound has to pass through a lipophilic (‘fat loving’) membrane and this process will be unfavourable for charged molecules. . In a more acidic medium, such as the stomach, the percentage ionised for an acidic compound will be less than at pH 7.4 and so more compound will have the capacity to be passively absorbed. In comparison, a basic compound in an acidic medium will be more ionised and so less of the compound will be in the neutral form and have the capacity to undergo passive absorption. Friday, October 02, 2015 JAMES D. 36

Acidity or Basicity of a compound :

Acidity or Basicity of a compound This may well be the reason for the observation that acidic compounds generally have better fraction absorbed (hence bioavailability) than bases with neutral compounds lying between them. Friday, October 02, 2015 JAMES D. 37

3. Lipophilicity :

3. Lipophilicity Lipophilicity (‘fat-liking’) is the most important physical property of a drug in relation to its absorption, distribution, potency and elimination. Lipophilicity is often an important factor in all of the following, which include both biological and physicochemical properties Solubility Absorption Plasma protein binding CNS penetration Bioavailability Friday, October 02, 2015 JAMES D. 38

3. Lipophilicity :

3. Lipophilicity bind too strongly to plasma proteins and therefore the free blood concentration will be too low to produce the desired effect .   Conversely, if the compound is too polar (hydrophilic), it may not be absorbed through the gut wall due to lack of membrane solubility. So it is important that the lipophilicity of a potential drug molecule is correct in design. Friday, October 02, 2015 JAMES D. 39

Slide40:

Hydrophobic means ‘water hating’. This principle also applies to the physical properties of drug molecules. If a compound is too lipophilic, it may be insoluble in aqueous media (e.g. gastrointestinal fluid or blood) Friday, October 02, 2015 JAMES D. 40

4. Hydrogen bonding :

4. Hydrogen bonding Hydrogen bonding is the attractive force between a hydrogen atom covalently bound to an electronegative atom (the donor) and a second electropositive atom (the acceptor). You don’t want too many hydrogen bond donors or acceptors, otherwise the drug won’t get from the gut into the blood. Friday, October 02, 2015 JAMES D. 41

5. Molecular size :

5. Molecular size Molecular size is one of the most important factors affecting biological activity, but it’s also one of the most difficult to measure. There are various ways of investigating the molecular size, including measurement of: Molecular weight (most important) Polar surface area Friday, October 02, 2015 JAMES D. 42

5. Molecular size :

5. Molecular size Molecular weight is probably the most useful measure of molecular size as it is very easy to calculate, but you may also come across other measures. Polar surface area, for example, is a measure of what proportion of the surface of the molecule is comprised of polar groups, compared to the proportion of hydrophobic groups. Friday, October 02, 2015 JAMES D. 43

The application of Chemistry in Pharmacy :

The application of Chemistry in Pharmacy The most obvious is that pharmacy is dealing with chemicals. It is pure chemistry and understanding how the chemicals interact with a living being. To know what medicines are made of and how they interact with each other and environment . To know how medicines interact with each other once prescribed as a daily regime or otherwise. Friday, October 02, 2015 JAMES D. 44

The application of Chemistry in Pharmacy :

The application of Chemistry in Pharmacy To know of potential side effects a patient may incur due to the specific medication or a combination of medicines. To calculate the correct dosage prescribed by a physician. To know the storage conditions for drug stability To conduct quality control tests for drug efficacy certification. Friday, October 02, 2015 JAMES D. 45

The application of Chemistry in Pharmacy :

The application of Chemistry in Pharmacy How accurate are the batches ? Measuring the active ingredients in medicines can be achieved by titration and other simple laboratory techniques The precise quantities of ingredients for any batch of medicine are measured and recorded THROUGH Q.C on random samples from each batch being selected and tested. Friday, October 02, 2015 JAMES D. 46

The application of Chemistry in Pharmacy:

The application of Chemistry in Pharmacy Separation of drugs mixtures by various chromatography methods in which Both the random samples and the standard solution are passed through a high performance liquid chromatography (HPLC) and the quantities are compared. HPLC is widely used to check the quantities of active ingredients in medicines. The result of this process show if the average content of the medicine lies within the accepted limits of variation as an application of Chemistry. Friday, October 02, 2015 JAMES D. 47

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