Dosage Forms and Drug Delivery Systems Pharmaceutics I

1. Dosage Forms and Drug Delivery SystemsPharmaceutics I Dr. Mercedita S. Aquino

2. Chapter 1 Introduction to Drugs and Pharmacy

3. Pharmacy Pharmakon Drugs – it is defined as an agent intended for use in the diagnosis, mitigation, treatment, cure or prevention of disease in man or animals. Drugs have different actions and effects on the body.

4. Different categories of drugs: Ecbolics or oxytocicsagents that stimulate the activity of the uterine muscle Mydriatics agents that dilate the pupil of the eye Mioticsagents that constrict or diminish the pupillary size Emeticsagents that induce vomiting Anti - emetics drugs that stops vomiting

5. Diuretics drugs that increase the flow of urine Expectorantdrugs that increase the respiratory tract fluid Cathartics or laxatives promote evacuation of the bowel Analgesic drugs that relieves pain Antipyreticdrugs that reduce fever Drugs that maybe used to diagnose diabetes, liver malfunction

6. Medicinal agents available today represents one of man’s accomplishments The process of drug discovery and development is complex. Discovery of a potential drug has to undergo definite chemical and physical characterization.

7. Basic Pharmacology • Drug site and rate absorption • It’s pattern of distribution and concentration within the body • Its duration of action • Method and rate of elimination or excretion • Metabolic degradation and the activity of its metabolites • The new drug’s most effective route of administration

8. Appropriate Dosage Forms to facilitate administration of drugs by selected routes • Dosage forms are designed to contain specified quantity of medication for ease and accuracy of dosage administration. • Example: tablets, capsules, syrups, injections • The design, development ,production are prime example of the application of the pharmaceutical sciences – the blending of the basic, applied and clinical sciences with pharmaceutical technology

9. 2 general components of the dosage form: 1. active ingredients or therapeutic ingredients 2. pharmaceutic ingredients To assure stability and effectiveness of the product throughout its usual shelf life the following must be applied: • Principles of chemistry • Physical pharmacy • Microbiology • Pharmaceutical technology

10. What should be considered in the formulation: • Compatibility of all the ingredients including the active component (physically & chemically, including the pharmaceutical ingredients and the packaging materials) • It must be preserved against decomposition due to chemical degradation protected from microbial contamination and destructive influence of excessive heat, light, and moisture

11. The therapeutic ingredients must be released from the dosage form in the proper amount and in such a manner that the onset and duration of the drug’s action is that which is desired. • The pharmaceutical product must lend itself to efficient administration and must possess attractive features of flavor, odor, and texture that enhance patient acceptance • The product must be effectively packaged and clearly and completely labeled.

12. Once prepared: • The pharmaceutical product must be properly administered if the patient is to receive maximum benefit • The medication must be taken in sufficient quantity, at specified intervals, and for an indicated duration of time. • The pharmacist’s intimate knowledge of drug actions, drug therapy, dosage form design and utilization, available pharmaceutical product & drug information sources makes him or her a vital member

13. History of Pharmacy The first apothecary . It was in the preparation of the medicinal materials that the art of the apothecary originated The art of apothecary has always been associated with the mysterious, and its practitioners were believed to have connection with the world of spirits and thus performed as intermediaries between the seen and the unseen.

14. History of Pharmacy • Throughout history the knowledge of drugs and their application to disease has always meant power. • In the Homeric epics, the term pharmakon (Gr.) from which the word pharmacy was derived connotes a charm or a drug that can be used for good or for evil purposes. • As time passed, the art of the apothecary became combined with priestly functions, and among the early civilizations the priest-magician or priest – physician became the healer of the body as well as the soul.

15. History of Pharmacy Pharmacy and Medicine are indistinguishable in their early history, since their practice was generally the function of the tribal religious leaders. Early drugs. • The most common of the memorials is the Papyrus Ebers, a continuous scroll some 60 feet long and a foot wide dating back to the 16th century BC, named after the German Egyptologist, Georg Ebers, who discovered it in the tomb of a mummy.

16. History of Pharmacy • The text to the Ebers Papyrus is dominated by drug formulas with more than 800 formulas or prescriptions are being described and over 700 different drugs being mentioned. Examples of drug mentioned: • Acacia,Castor bean (source of castor oil) • Iron oxide,Sodiumcarbonate,Sodium chloride • Vehicles like: beer, wine, honey and milk

17. History of Pharmacy Hippocrates- was a Greek physician who is credited with the introduction of scientific pharmacy and medicine. His works included the descriptions of hundreds of drugs, and it was during this period that the term pharmakon came to mean a purifying remedy for good only, transcending the previous connotation of a charm or drug for good or evil purposes.

18. History of Pharmacy Because of his pioneering work in medicinal science and his inspirational teachings, and advanced philosophies that have become a part of modern medicine, Hippocrates is honored by being called the ‘’Father of Medicine’’

19. History of Pharmacy Dioscorides, a Greek physician and botanist was the first to deal with botany as an applied science of pharmacy. His work, De MateriaMedicais considered a milestone in the development of pharmaceutical botany and in the study of naturally occurring medicinal materials. This study today is known as Pharmacognosy- a term in formed from two Greek words, pharmakondrug, and gnosis, knowledge.

20. History of Pharmacy Drugs discovered by Dioscorides: • Opium, Ergot, hyoscyamos Claudius Galen – a Greek pharmacist-physician His medical writings include: • descriptions of numerous drug formulas and methods of compounding; • originated commonly referred to as ‘’ Galenic pharmacy’’, the most common the cold cream called Galen’s Cerate.

21. History of Pharmacy • Pharmacy remained a function of medicine until the increasing variety of drugs and the growing complexity of compounding demanded specialists who could devote full attention to the art. • Pharmacy was officially separated from medicine for the first time in 1240 A.D. When the decree of German Emperor Frederick II regulated the practice of pharmacy within that part of his kingdom called the Two Sicilies.

22. History of Pharmacy • His edict separating the two professions acknowledged that pharmacy required special knowledge, skills, initiative and responsibility if adequate care to the medical needs of the people was to be guaranteed. • Pharmacists were obliged by oath to prepare reliable drugs of uniform quality according to their art.

23. Drug Standards • As the scientific basis for drugs and drug products developed, so did the need for uniform standards to ensure quality. • The United States Pharmacopeia(USP) and National Fomulary (NF) – two official compendia

24. Drug Standards • Pharmacopeia comes from the Greek word Pharmakon, meaning “Drug ‘’and “Poiein” meaning “make” and the combination indicates any recipe or formula or other standards required to make or prepare a drug. • The first combined compendium, representing the USPXX and NFXV became official on July 1, 1980. • All monograph of therapeutically active drug substances appeared in USP whereas monographs on pharmaceutically active appeared in NF section

25. Drug Standards • The monograph gives information about the drug. • The initial part consist of the official title (generic of nonproprietary name) of the drug substance • Followed by its structural formula, empirical formula, molecular weight, chemical names, and the drug’s Chemical Abstract Service (CAS) registry number. • Next statement of chemical purity, a cautionary statement which reflects the toxic nature of the agent, packaging and storage recommendations, chemical and physical test and the prescribed method of assay to substantiate the identification and purity of the chemical

26. Classification of Drugs • Drugs approved for marketing by the Bureau of Food & Drug (BFAD) are categorized according to the manner in which they may be legally obtained by the patient: 1. OTC(Over –the-counter) drugs – maybe sold without physician’s prescription • These are drugs deemed safe enough for the use by the layman in the self-treatment of simple conditions for which competent medical care us not generally sought.

27. Classification of Drugs 2. Prescription drugs – referred to as “Legend drugs” , are made available only on the prescription of the licensed practitioner. • They are useful after expert diagnosis or too dangerous for use in self-medication. • These drugs may not be refilled (dispensed again after initial filling of the prescription)without the consent of the prescriber.

28. The Role of the Pharmacist • The pharmacist is competent to perform numerous setting that applies: • The basic pharmaceutical sciences • Clinical sciences • Professional training and experiences

29. The Role of the Pharmacist • 1. Community Pharmacy • Has active role in the patient’s use of the prescription and non-prescription medication, diagnostic agents, durable medication equipment and devices • Develops patient medication profiles and counsels patients on their health status and use of drug and nondrug measures • Source of drug information to the patients and other allied health professionals • Enjoys the opportunity to influence directly or indirectly the selection and use of drug therapies

30. The Role of the Pharmacist • 2. Institutional settings – Hospitals, Extended Health Facilities & Health Maintenance Organization (HMO) • Provision of professional and clinical services example: intravenous admixture services, nuclear pharmacy, patient monitoring, • Provision of education and technological services example: drug information and poison control • Provision of research and support services example: pharmacokinetic consult services investigational drug studies division.

31. The Role of the Pharmacist • 3. Industry Pharmacists working for pharmaceutical research, manufacturing and distributing firms involves in: • Drug product development • Clinical testing • Production • Marketing • Management functions Requires knowledge in basic and pharmaceutical sciences, dosage form designs & technical aspects of production

32. The Role of the Pharmacist • 4. Post graduate residency and/or fellowship program to enhance their practice and/or research skills. • Pharmacy residency is defined as an organized, directed postgraduate training program in a defined area of practice. • The chief purpose of pharmacy residencies us to train pharmacists in professional practice and management skills.

33. The Role of the Pharmacist • 5. Government Services • Pharmacists performs professional and administrative functions as in the development and implementation of health care program • Government supported hospitals, clinics and specialized health care institutions.

34. The Mission of Pharmacy • The mission of Pharmacy is to serve society as the profession responsible for the appropriate use of medications, device and services to achieve optimal therapeutic outcomes.

35. The Mission of Pharmacy • Elements in the statement defined: • Pharmacy is the health profession that concerns itself with the knowledge system that results to the discovery, development, and use of medications and medication information in the care of patients. • It encompasses: • Clinical • Economic • Educational aspects

36. The Mission of Pharmacy • Society encompasses patients, other than health care providers, health-policy decision makers, corporate health benefits managers, the healthy public. • Appropriate refers to the pharmacist’s responsibility to ensure that a medication regimen is specifically tailored for the individual patient, based on accepted clinical and pharmacological parameters.

37. The Mission of Pharmacy • Medication refers to the legend and nonlegend agents used in the diagnosis and treatment, prevention, and/or cure of disease. The term is specifically and purposefully used and is distinguished from the term drug, which has a negative and nontherapeutic public image. • Devices refers to the equipment, process, biotechnological entities, diagnostic agents, or other products that are used to assist in effective management of the medication regimen.

38. The Mission of Pharmacy • Services refers to patient, health professional and public education services, screening and monitoring programs, medication-regimen management and related activities that contribute to effective medication use by patients. • Optimal therapeutic outcomes declares the profession’s ultimate contribution to public health. Pharmacy asserts it unique rights, privileges, and responsibilities-and accepts the attendant liabilities-associated with medication us.

39. Pharmaceutical Care • The role of the pharmacist in practice is the delivery of pharmaceutical care. • Definition of Pharmaceutical Care (Hepler and Strand) • Pharmaceutical care is the responsible provision of drug therapy for the purpose of achieving definite outcomes that improve a patient’s quality of life.

40. Pharmaceutical Care • Outcomes are: • cure of disease • Elimination of reduction of patient’s symptomatology • Arresting or slowing of a disease process • Preventing a disease or symptomatology

41. Pharmaceutical Care • 3 major functions: • Identifying potential and actual drug-related problems • Resolving actual drug-related problems • Preventing potential drug-related problems

42. Pharmacy Practice Standards

43. Chapter 2 New Drug Development and Approval Process

44. New Drug Development Process • New Chemical Entity • Sources: • Organic Synthesis • Molecular Modification • Isolation from plants

45. New Drug Development Process • Preclinical studies • Including: • Chemistry • Physical properties • Biological • Pharmacology • ADME • Toxicology • Preformulation • Plus: • Long-term Animal Toxicity • Product Formulation • Manufacturing and Controls • Package and Label Design

46. New Drug Development Process • Investigational New Drug Application (IND) • Submission • BFAD review

47. New Drug Development Process • Clinical Trials • Phase I – initial introduction of investigational drugs to human volunteer, primarily assessing for the purpose of assessing safety • Phase II- to determine the efficacy of the new drug in treating the disease against which it is being tested and to detect side effects or toxicity symptoms not manifested in the animal studies or with healthy volunteers • Phase III – involves the participation of additional clinicians with the objective of determining the usefulness of the drug in the expanded patient base.

48. New Drug Development Process • New Drug Application(NDA) • Submission • FDA REVIEW • Pre-approval plant inspection • FDA Action

49. New Drug Development Process • Post Marketing • Phase IV Clinical Studies • Clinical Pharmacology/Toxicology • Additional Indications • Adverse Reaction Reporting • Product Defect Reporting • Product Line Extension

50. New Drug Development Process