Steps involved in dosage development of new drug


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Drug is any substance or product that is used or is intended to be used to modify or explore physiological states for the benefit of the recipient

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Steps involved in dosage development of new drug

  3. 3. Definitions Drug is any substance or product that is used or is intended to be used to modify or explore physiological states for the benefit of the recipient Dosage forms are a mixture of active drug components and nondrug components Dose is defined as quantity of medication that is to be administered at each time to produce a certain degree of response in a patient Bioavailability is defined as the rate and extent of absorption of unchanged drug from its dosage form
  4. 4. Preformulation involves the application of biopharmaceutical principles to the physicochemical parameters of a drug with the goal of designing an optimum drug delivery system.   Characterization of drug molecule is a very important step at the preformulation phase of product development. 
  5. 5. Following studies are conducted as basic preformulation studies, special studies are conducted depending on the type of dosage form and the type of drug molecule Solubility determination pH & pKa determination Partition coefficient Solid state properties ( polymorphism and amorphism) Powder flow properties Stability studies
  6. 6.     Active drug substance (active pharmaceutical ingredient - API) Excipients (inactive pharmaceutical ingredients) ◦ Technological, biopharmaceutical and/or stability reasons ◦ Diluents/fillers, binders, lubricants, desintegrants, coatings, preservants and stabilizers, colorants and flavourings Pharmaceutical dosage form ◦ is a drug delivery system which is formed by technological processing (drug formulation) ◦ determines the physical form of the final pharmaceutical preparation ◦ must reflect therapeutic intentions, route of administrations, dosing etc. Pharmaceutical preparation (PP) ◦ particular pharmaceutical product containing active and inactive pharmaceutical ingredients formulated into the particular dosage form. ◦ Packed and labelled appropriately
  7. 7. Depending on the dosage form selected, various studies are conducted to accomplish the goal. Formulations developed are tested for both physical and chemical stability at accelerated temperatures. Evaluation Tests For Dosage Forms  Weight variation test  Drug Content  Stability  Dissolution  Skin Irritant Test  Viscosity  Clarity
  8. 8. Bioequivalence is a relative term which denotes that the drug substance in two or more identical dosage forms reaches the systemic circulation at the same relative rate and to the same relative extent.  Bioequivalence studies are conducted by pharmacokinetic method and pharmacodynamic method.  Types of bioequivalence studies: 1. In vivo Bioequivalence studies 2. In vitro Bioequivalence studies 
  9. 9. 1. In vivo Bioequivalence studies The following sequence of criteria is useful in assessing the need for in vivo studies  Oral immediate release products with systemic action  Non-oral immediate release products  Modified release products with systemic action 2. In vitro Bioequivalence studies  The drug product has been slightly reformulated by the original manufacturer  An acceptable In-vitro In-vivo correlation and the in vitro dissolution rate of the new product is equivalent with that of the already approved medicinal product
  10. 10.    • • Regulatory affairs (RA), also called government affairs, is a profession within regulated industries, such as pharmaceuticals, medical devices and energy. The regulatory function in healthcare industries is vital in making safe and effective healthcare products available worldwide. The (Healthcare) Regulatory Affairs Profession is still an emergent profession but has two major international professional membership societies: The Regulatory Affairs Professionals Society (RAPS) The Organisation for Professionals in Regulatory Affairs (TOPRA)
  11. 11. Indian-CDSCO (central drug standard control organisation) The CDSCO establishes safety, efficacy, and quality standards for pharmaceuticals and medical devices. It publishes and updates the Indian Pharmacopeia, a list of regulated pharmaceuticals and devices. US-FDA (Food and Drug Administration) FDA is responsible for protecting and promoting public health through the regulation and supervision of food safety, tobacco products, dietary supplements, prescription, cosmetics and OTC products. Canadian-HPFB (The Health Products and Food Branch) minimizing health risk factors to Canadians while maximizing the safety provided by the regulatory system for health products and food; Australian-TGA(The Therapeutic Goods Administration) is responsible for regulating therapeutic goods including medicines, medical devices, blood and blood products,
  12. 12.  Tablets - Compressed product (API+ excipients – e.g., fillers, desintegrants) ◦ Conventional –Desintegration/Desagregation/Dissolution, can be divided (half/quarters) ◦ Coated (not to be divided)  To mask unpleasant taste or smell of API  To avoid of adhesion in oesophagus (to facilitate swallowing and/or avoid release of API and local adverse reactions)  To ensure drug stability
  13. 13.  Capsules - API + excipients - enclosed in the hard/soft water soluble container made of gelatin. - Consist of cap and body – filled with powders, pellets, granules (paste, oil) - In the GIT gelatin shell softens, swells and dissolve particles are dispersed → disintegration → API dissolution → absorption - Hygroscopic
  14. 14.    Solutions (drops) – aqueous, oils ◦ Syrups – aqueous solutions with sugar (or sugar substitute) with/without flavouring agents ◦ Elixirs – sweetened hydroalcoholic solutions which can accomodate less water. ◦ Tinctures – alcoholic or hydroalcoholic solutions – herbal extracts. Emulsions-API+oil+water+emulsifying agent Suspension –API+solvent+suspendig agent - should not be used for drugs with high potency.
  15. 15. Semisolid dosage forms 1.Unshaped (without specific physical shape) •Gels -A semisolid systems in which a liquid phase is constrained within a 3D cross-linked matrix. •Creams – semisolid emulsion systems (o/w, w/o) containing more than 10% of water. o/w creams - more comfortable and cosmetically acceptable as they are less greasy and more easily water washable w/o creams – accommodate and release better lipophilic API, moisturizing, Cold creams •Ointments – semisolid dosage forms with the oleaginous (hydrocarbon), water-soluble or emulsifying base Oleaginous (hydrocabon) base: Petrolatum (Vaseline – white, yellow) Water-soluble base: Polyethylenglycol (PEG)- ointment , macrogol ointments •Pastes – semisolid dispersion system, where a solid particles (> 25%, e.g. ZnO) are dispersed in ointments – mostly oleaginous (Petrolatum)
  16. 16. 2.Shapedsuppositories (for rectal administration) -Solid dosage form under room temperature which are melted at the body temperature. -Different size & shapes– children and adult suppositories -Chemically stable and inert. -Oleaginous (cacao butter, adeps neutralis) or aqueous (PEGs, glycerinated gelatine) Gases dosage forms 1.Gases – medicinal gases, inhalation/volatile anaesthetics (vaporised before administration by inhalation) 2.Aerodispersions of solid particles (e.g., inhalation antiasthmatics) or liquid particles (inhalation antiasthmatics or sprays)
  17. 17.  The above steps are to be followed to formulate an efficient dosge form with maximum therapeutic response and safety with minimum toxicity.
  18. 18. Theory &practice of Industrial pharmacy by Leon lachman  Biopharmaceutics & pharmacokinetics by D.M Brahmankar  Physical pharmacy &pharmaceutical sciences by Martn’s 