Drug

Drug is any substance is intended is used as orally applied a topically for the purpose of used of mitigation, treatment, prevention, cure and Diagnosis of disease and disorder and maintain the good quality of health is known has Drug.
Any substance is important to impart or give the therapeutic activity is known has drug.
Drug is important to prevent the disease and disorder and it can give therapeutic activity.
Drug is important to give Pharmacological response and it act has target site of infection and prevent injury or disease and disorder.
Drug was administered in various routes of administration depending on there types.

1. Drug Sunday, December 06, 2015 SAGAR KISHOR SAVALE 1 Mr . Sagar Kishor Savale [Department of Pharmacy (Pharmaceutics)] 2015-016 [email protected]

2. Contents 1.Drug 1.1 drug 1.2 compounding 1.3 dispensing 1.4 dosage from 2. Pharmacokinetics 2.1 Pharmacokinetic parameters 3. Pharmacodynamics parameters 4. Comparision between Pharmacokinetic & pharmacodynamics 5. Plasma concentration curve 6. Process involved in drug Therapeutics 7. Drug moving pattern in body 8. Ideal characteristics of drug Sunday, December 06, 2015 SAGAR KISHOR SAVALE 2

3. Contents 9 . Drug release pattern 10. Drug Classification 11. Types of drug 12. Classification of drug according to BCS 13. Other classes of Drug (A, B, & C) 14. Drug distribution in patient 15. Pharmaceutics 16. Design of drug product 17. Enhancing stability of drug product 18. Standardizations & quality evaluation of drug 19. Types of dosage from 19.1 Types according to physical from 19.2 types according to route of administrations 20. R eferences Sunday, December 06, 2015 SAGAR KISHOR SAVALE 3

4. 1. Drug 1.1 Drug is any substance is intended is used as orally applied a topically for the purpose of used of mitigation, treatment, prevention, cure and Diagnosis of disease and disorder and maintain the good quality of health is known has Drug. Any substance is important to impart or give the therapeutic activity is known has drug. Drug is important to prevent the disease and disorder and it can give therapeutic activity. Drug is important to give Pharmacological response and it act has target site of infection and prevent injury or disease and disorder. Drug was administered in various routes of administration depending on there types. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 4

5. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 5 1.2 Compounding – it is define has the synthesis and preparation of drug and dosage from in laboratory or pharmaceutical industry is known has Compounding. 1.3 Dispensing – it is define has the distribution or dispensing the drug in patient is known has Dispensing. (This two processes are associated with pharmacist)

6. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 6 1.4 Dosage form - Dosage forms are the means by which drug molecules are delivered to sites of action within the body . Drug Active pharmaceutical + Excipients ingredient (API) API – it is Active ingredient can shows therapeutic activity. Excipient – it is chemically inert substance added along with drug. The optimum quantity of drug can shows Therapeutic response but Excess (More than optimum) quantity it can shows Toxicity.

7. 2. Pharmacokinetics The term “ Pharmacokinetics ” is derived from Greek words Pharmakon (drug) and Kinesis ( movement). It is the quantitative study of drug movement in, through and out of the body and their relationship with the pharmacological, therapeutic or toxicological response in man or animals. Dose regimen : The frequency of administration of a drug in a particular dose. It can includes - Absorption, Distribution, Metabolism and Excretion of drug. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 7

8. 2.Pharmacokinetics Absorption : is the process of a movement of a drug from its site of administration to systemic circulation. Distribution : is the dispersion of substances throughout the fluids and tissues of the body i.e. the movement of drug between one compartment and the other. Elimination : process that tends to remove the drug from the body and terminates its action. Metabolism : is the irreversible transformation of parent compounds into daughter metabolites. Excretion : is the elimination of the substances from the body. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 8

9. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 9

10. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 10 2.1.1 Peak Plasma Concentration (C max ) Maximum drug concentration in plasma is know as peak plasma concentration. Expressed in mcg/ml. At C max absorption rate = elimination rate. Peak concentration of any drug is related to it’s pharmacological response. 2.1 Pharmacokinetic parameters

11. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 11 2.1.2 Time of Peak Concentration (t max ) Time taken by the drug to reach the maximum plasma concentration. Expressed in hours. Useful in estimating ate of absorption. Importance in assessing the efficacy of drugs used to treat acute conditions like pain and insomnia.

12. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 12 2.2.3 Bioavailability - the exact rate of absorption of drug from dosage from is represented by serum concentration curve is known has bioavailability. 2.2.4 Bioequivalence – it is define has the bioavailability of drug is same but manufacturing process is not identical is known has Bioequivalence. Area under the curve(AUC) Bioavailability =AUC(Oral )/AUC(Injected)*100

13. 3. Pharmacodynamics parameters 3.1 Maximum Safe Concentration (MSC): Concentration of drug in plasma above which adverse or unwanted effects are precipitated. Also know as minimum toxic concentration (MTC). Concentration of drug above MSC is said to be in toxic level . Sunday, December 06, 2015 SAGAR KISHOR SAVALE 13

14. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 14 3.2 Onset of Action: Beginning of pharmacological response. Occurs as the plasma drug concentration just exceeds required MEC. 3.3 Onset Time: Time required for the drug to start producing pharmacological response. It is the time at which plasma drug concentration reach to MEC

15. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 15 3.4 Duration of Action: Time period during which plasma drug concentration remains above the MEC. 3.5 Intensity of Action: Maximum pharmacological response produce by the peak plasma concentration of drug. Intensity of action depend on the height of peak plasma concentration.

16. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 16 3.6 Therapeutic range: Concentration of drug between MEC and MSC represent therapeutic range. Also know as therapeutic window. 3.7 Therapeutic Index: Ratio of MSC to MEC. Also defined as the ratio of dose required to produce toxic or lethal effects to dose required to produce therapeutic effect .

17. 4. Comparision Sunday, December 06, 2015 SAGAR KISHOR SAVALE 17 Pharmacokinetic Pharmacodynamics Response of Drug in to body Response of Body in to Drug Include absorption, distribution, metabolism and excretion of drug. Includes Pharmacological response and Therapeutic effectiveness.

18. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 18 5. Plasma concentration Curve

19. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 19 6. Process Involved in Drug Therapeutics

20. 7. Drug moving pattern in Body Sunday, December 06, 2015 SAGAR KISHOR SAVALE 20

21. 8. Ideal Characteristics of Drug It is non-toxic Non reactive It is physic chemically stable It is Metabolically stable It is chemically inert It can free from Microbial contamination It can give both rapid as well as sustained activity It was easily available It is inexpensive and economically Sunday, December 06, 2015 SAGAR KISHOR SAVALE 21

22. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 22 9. Drug release pattern

23. 10. Drug Classification Depressants Stimulants Antacids Analgesics Antibacterial Antiviral Mind Altering Drugs Sunday, December 06, 2015 SAGAR KISHOR SAVALE 23

24. 11. Types of Drugs Main Types : (Three Types) Depressants slow down, or depress, the functions of the central nervous system . In moderate doses, depressants can make you feel relaxed. In larger doses, depressants can cause unconsciousness by reducing breathing and heart rate. A person's speech may become slurred and their movements sluggish and uncoordinated. These can include: alcohol; opiates and opioids (heroin) , morphine, codeine, methadone and buprenorphine; cannabis or marijuana; minor tranquillizers diazepam such as Valium, oxazepam (Serepax); some solvents and inhalants such as vapors from petrol, glue, chrome paint and lighter fluid. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 24

25. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 25 Stimulants speed up or stimulate the central nervous system and can make the users feel more awake, alert or confident. Stimulants increase heart rate, body temperature and blood pressure. Other physical effects include reduced appetite, dilated pupils, talkativeness, agitation and sleep disturbance. Types Include: Caffeine Nicotine in tobacco is a stimulant, despite smokers using it to relax Ephedrine, used in medicines for bronchitis, hay fever, asthma Amphetamines and methamphetamines, also known as 'speed', 'ice' and 'crystal meth' Cocaine, also known as 'coke' and 'snow'; slimming tablets: e.g. Duromine and Tenuate;

26. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 26 Hallucinogenic drugs distort the user's perceptions of reality. The main physical effects are dilation of pupils, loss of appetite, increased activity, talking or laughing, jaw clenching, sweating and sometimes stomach cramps or nausea. Drug effects can include a sense of emotional and psychological euphoria and well-being. Visual, auditory and tactile hallucinations may occur, causing users to see or hear things that do not actually exist. These drugs include: LSD, also known as 'trips', 'acid' and 'microdots'; magic mushrooms (psilocybin), also known as 'mushies’ or ‘shrooms’; ecstasy (MDMA/methylenedioxymethamphetamine), also known as 'E', 'XTC' and 'Eccies', produces a combination of hallucinogenic and stimulant effects; and Ketamine, also known as 'K' and 'Special K'.

27. 12. Classification according to Biopharmaceutical Classification System (BCS) The Biopharmaceutical Classification System has been developed to provide a scientific approach to allow for to prediction in vivo pharmacokinetics of oral immediate release (IR) drug product by classifying drug compound based on their – 1. Solubility 2. Permeability 3. Dissolution Sunday, December 06, 2015 SAGAR KISHOR SAVALE 27

28. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 28 CLASS SOLUBILITY PERMEABILITY Class – I (Metaprolol, Atenolol) High High Class – II (cimetidine, naproxen) Low High Class – III (nifidipine, metformin) High Low Class – IV (Taxol, Chlorthiazole) Low Low

29. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 29 13. Other Classes of Drug Class Example Possession Dealing Class A Ecstasy, LSD, heroin, cocaine, crack, magic mushrooms Up to 7 years in prison or an unlimited fine or both Up to life in prison or an unlimited fine or both Class B Amphetamines, Methylphenidate (Ritalin),Pholcodine Up to 5 years in prison an unlimited fine or both Up to 14 years in prison or an unlimited fine or both Class C Cannabis, tranquilizers, some painkillers, Gammahydroxybutyrate (GHB),Ketamine Up to 2 years in prison or an unlimited fine or both. Up to 14 years in prison or an unlimited fine or both

30. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 30 14. Drug Distribution in patient Therapeutic Target Discovery/ Literature serve Research and Development Approval Manufacture Final Dosage form Distribution Patient

31. 15. Pharmaceutics Pharmaceutics is the science of dosage form design. There are many chemicals with known pharmacological properties but in a raw form it is worth less for patient. Pharmaceutics deals with the formulation of a pure drug substance into a dosage form. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 31

32. 16. Design of Drug Products Effectiveness Safety Reliability Stability Physical Chemical Microbiological Sunday, December 06, 2015 SAGAR KISHOR SAVALE 32 Pharmaceutical elegance Appearance Organoleptic properties Convenience Ease of use Dosing frequency Consumer acceptance

33. 16. Enhancing Stability of Drug Products Excipients may be added to protect the drug & increases stability of Drug : Antioxidants Preservatives Chelating agents Buffering agents Binding agent Diluents Adhesives Disintegrate Surfactant Polymers Coloring agent Wetting agent Sunday, December 06, 2015 SAGAR KISHOR SAVALE 33

34. 17. Adverse Effects / Side effects List of possible unpleasant or dangerous secondary effects other than the desired effects Causes of ADRs - Interactions Drug/Drug Drug/Food Drug/Herb Toxic potential Sunday, December 06, 2015 SAGAR KISHOR SAVALE 34

35. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 35 QUALITY EVALUATION OF HERBAL DRUGS CHEMICAL BIOLOGICAL ORGANOLEPTIC BOTANICAL PHYSICAL Moist. Cont. Extrac. Values Ash Values Fluores. Analy. Macroscopic Microscopic Qualitative Quantitative SEM Studies Powder Studies Shape External Marking Colour Odour Taste Texture Fracture Antagonistic Microbial Contamination Toxicological Pharmacological Other specific activities Bacterial Fungal Qualitative Quantitative Chromatography Heavy metal Pesticide residue Mycotoxin HPTLC GLC HPLC HPTLC Finger printing Sec. Metabolites DNA Finger printing 18. Standardization & Quality Evaluation of Drug

36. 19. Types of Dosage from Definition: Dosage forms are the means by which drug molecules are delivered to sites of action within the body. The need for dosage forms: 1- Accurate dose. 2- Protection e.g. coated tablets, sealed ampules. 3- Protection from gastric juice. 4- Masking taste and odour. 5- Placement of drugs within body tissues. 6- Sustained release medication. 7- Controlled release medication. 8- Optimal drug action. 9- Insertion of drugs into body cavities (rectal, vaginal) 10- Use of desired vehicle for insoluble drugs. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 36

37. 19.1 Types according to physical from Liquid dosage form (solutions, syrups, suspensions, drops, injection) Solid dosage form(Capsule , tablets , powder) Semisolid dosage form(Ointments, Creams, pastes, Gels) Sunday, December 06, 2015 SAGAR KISHOR SAVALE 37

38. 19.2 Types according to route of administration Oral Topical Rectal Parenteral Vaginal Inhaled Ophthalmic Otic Intanasal Pulmonary Sunday, December 06, 2015 SAGAR KISHOR SAVALE 38

39. 19.1.1 Solid dosage from Capsules It contain one or more medicinal substances enclosed with in a shell or container prepared from suitable form of gelatin Capsule has two types Hard gelatin capsules Soft gelatin capsules Sunday, December 06, 2015 SAGAR KISHOR SAVALE 39

40. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 40 Hard gelatin capsules It is made up of gelatin ,sugar and water. They are physically hard. The hard-shell gelatin capsules contain solid drugs (made by hard Gelatin core) Soft gelatin capsule It is made up of gelatin. Glycerin Or sorbitol are added to render gelatin elastic. The soft-shell gelatin capsules contain oils. These capsules are easily swallowed due to tasteless shell .( Soft gelatin core) (

41. 2.Tablet A tablet is a hard, compressed medication in round, oval or square shape. The excipients include: Binders, glidants (flow aids) and lubricants to ensure efficient tabletting. Disintegrants to ensure that the tablet breaks up in the digestive tract. -Sweeteners or flavours to mask the taste of bad-tasting active ingredients. Pigments to make uncoated tablets visually attractive. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 41

42. 2.1Types of tablet Immediate release tablet: Release the drug substance immediate after ingestion Delayed release tablet : The drug substance is not released until a physical event has occurred e.g. change in gut flora. Chewable tablet : The tablets are placed in the mouth, chewed and swallowed e.g. Lozenges Buccal tablet: These are designed to be placed in buccal cavity of mouth for rapid action. Sublingual tablets : these are placed under tongue for rapid dissolution. Effervescent tablets : The tablet contain sodium bicarbonate in addition to the drug substance. Before use they are dissolve in water.e.g. Acetylsalicylic acid Sunday, December 06, 2015 SAGAR KISHOR SAVALE 42

43. 19.1.2 Powders Powders are drugs or drug extracts that are dried and ground and converted into fine particles. Advantage Use both internally and externally Good chemical stability as compared to fluids Rapid onset of action Easy to swallow even in large bulk, espacially mixed with drink food Economic Safe to children and elderly patients Sunday, December 06, 2015 SAGAR KISHOR SAVALE 43

44. 19.1.3 Types of Powders Oral powder : They are intended to be suspended or dissolve in water or mixed with foods e.g. Antacid and laxatives Dentifrices : They contain soap or detergent, mild abrasive and anticariogenic agent Dusting powder : They are locally applying non toxic preparation that is intended to be dissolved in water prior to use as an antiseptic. They may be formulated for nasal, optic and vaginal use. Insufflations : They are introduced in body cavity such as ear ,nose, throat, tooth socket.Insuffaltor is used to administer these products. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 44

45. 19.1.4 Liquid dosage form Liquid dosage forms are prepared: (1) By dissolving the active drug substance(s) in an aqueous or no aqueous (e.g. alcohol, ether, glycerin) solvent. (2) By suspensing the drug in appropriate medium. (3) by incorporating the drug substance into an oil or water phases. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 45

46. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 46 Liquid dosage forms can be administered : Topically - lotions or suspension applied to the skin, eye drops, nasal drops, ear drops Orally (p.o.) - oral suspension and solution Parenterally - subcutaneous injection (s.c.), intramuscular injection (i.m.) and intravenous administration (i.v.)

47. 19.1.5 Solution Oral solution: Oral solutions are clear Liquid preparations for oral use containing one or more active ingredients dissolved in a suitable vehicle. b- Oral emulsion: Oral emulsions are stabilized oil-in-water dispersions, either or both phases of which may contain dissolved solids. c-Oral suspension: - Oral suspensions are Liquid preparations for oral use containing one or more active ingredients suspended in a suitable vehicle. - Oral suspensions may show a sediment which is readily dispersed on shaking to give a uniform suspension which remains sufficiently stable to enable the correct dose to be delivered. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 47

48. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 48 d- Syrup: It is a concentrated aqueous solution of a sugar, usually sucrose. Flavored syrups are a convenient form of masking disagreeable tastes. e- Elixir: -It is pleasantly flavored clear liquid oral preparation of potent or nauseous drugs. - The vehicle may contain a high proportion of ethanol or sucrose together with antimicrobial preservatives which confers the stability of the preparation.

49. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 49 h- Gargles: They are aqueous solutions used in the prevention or treatment of throat infections. Usually they are prepared in a concentrated solution with directions for the patient to dilute with warm water before use. i- Mouthwashes : These are similar to gargles but are used for oral hygiene and to treat infections of the mouth.

50. 19.2.1 Topical dosage forms OINTMENTS They are composed of fluid hydrocarbon meshed in a matrix of higher melting solid hydrocarbon, e.g. pertrolatum. According the place of application they are: 1) unguentum dermaticum 2) unguentum ophthalmicum 3) unguentum nasale Sunday, December 06, 2015 SAGAR KISHOR SAVALE 50

51. 1.Characteristics a)Smooth texture b) Elegant in appearance c) Non dehydrating d) Non greasy e) Non hygroscopic f) Non irritating g) Do not alter membrane / skin functioning Sunday, December 06, 2015 SAGAR KISHOR SAVALE 51

52. 19.2.2 Creams These are either oil-in-water (O/W) or water-in-oil (W/O) emulsions and contain preservatives to prevent bacterial and fungal growth. Easier to spread & remove. The commonest preservatives are parabens Oil-in-water emulsions rub into the skin and are easily washed off Water-in-oil emulsions are greasier Sunday, December 06, 2015 SAGAR KISHOR SAVALE 52

53. 19.2.3 Gels Gels are semi-colloids which liquefy on contact with the skin Gels are transparent or translucent non-greasy semisolid gels . Gels are a common form for acne preparations (e. g. Acnederm) They are used as lubricant . Sunday, December 06, 2015 SAGAR KISHOR SAVALE 53

54. 20. References Brahmankar D.M., Jaiswal S.B., First edition, “Absorption of Drugs” Biopharmaceutics and Pharmacokinetics – A treatise, Vallabh Prakashan, Delhi 1995. Shargel L., Andrew B.C., Fourth edition “Physiologic factors related to drug absorption” Applied Biopharmaceutics and Pharmacokinetics, Prentice Hall International, INC., Stanford 1999. Aulton M.E. Pharmacetutics “The Science of Dosage Form Design”, 2 nd Ed.; Churchill Livingstone. Swarbrick J., Boylan J.C., “Absorption” Encyclopedia of Pharmaceutical Technology, Third Edition Marcel Dekker, INC., New York 1988:1:1-32. Biopharmaceutics & pharmacokinetics by G.R.Chatwal. Human anatomy & physiology by Tortora . Leon shargel, Susanna wu-pong, Andrew B.C.Yu , Applied Biopharmaceutics & Pharmacokinetics , 5 th edition 2005, published by the Mc Graw hills companies, page no. 431-436 & 482-484. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 54

55. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 55 Leon Lachman, Herbert A lieberman,The theory and practice of industrial pharmacy 2009. G . Banker and C.T. Rhodes, Modern Pharmaceutics, Marcel Dekker, Inc., 2000. H . Brittain, Physical Characterization of Pharmaceutical Solids, Marcel Dekker, Inc., 1995. H . Brittain, Polymorphism in Pharmaceutical Solids, Marcel Dekker, Inc., 1999. S.R . Byrn, R.R. Pfeiffer and J.G. Stowell, Solid State Chemistry of Drugs, Second Edition, SSCI, Inc.,1999. M . Gibson, Pharmaceutical Preformulation and Formulation, HIS Health Group, Englewood, CO, 2001. D.J.W . Grant and T. Higuchi, Solubility Behavior of Organic Compounds, John Wiley & Sons, Inc., 1990. L.J . Ravin and G.W. Radebaugh, “Preformulation”, Chapter 75 in Remington’s Pharmaceutical Sciences, 18th edition, Mack Publishing Company, Easton, Pennsylvania, 1990. S . Yalkowsky, Solubility and Solubilization in Aqueous Media, American Chemical Society, Washington D.C. 1999.

56. Sunday, December 06, 2015 SAGAR KISHOR SAVALE 56 Thank you