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INDUSTRIAL PHARMACEUTICAL TECNOLOGY (ESSENTIALS) Part 1

INDUSTRIAL PHARMACEUTICAL TECNOLOGY (ESSENTIALS) Part 1. Yauheni Hryniuk, Associate professor. History. Real birth of industrial Pharmaceutical Technology – first half of XIX century

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INDUSTRIAL PHARMACEUTICAL TECNOLOGY (ESSENTIALS) Part 1

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  1. INDUSTRIAL PHARMACEUTICAL TECNOLOGY (ESSENTIALS) Part 1 Yauheni Hryniuk, Associate professor

  2. History Real birth of industrial Pharmaceutical Technology – first half of XIX century • Merck – established in 1668. But it was only a drugstore, in XIX c. on the drugstore basis factory was established. Today – huge company (~ 40 000 employees). • Shering– drugstore – 1851, factory – 1864. In 2006 – takeover by Bayer. • Bayer – 1863. Today – one of the biggest company with 111500 workers among the world.

  3. Pfizer 182.15 B • Johnson & Johnson 180.88 B • GlaxoSmithKlein 141.87 B • Roche Holding 135.28 B • Novartis 128.65 B • Sanofi-Aventis 122.80 B • Astra Zeneca 75.70 B • Merck 72.71 B • Eli Lilly & Co. 64.67 B • Wyeth 62.78 B Source: Yahoo Finance

  4. Historyin Belarus • JSC “Borisovsky zavod medpreparatov” - 1962 • RUE “Belmedpreparaty” - 1929 • RUE “Minskinterkaps” - 1995

  5. Modern-day drug discovery and development

  6. L eading Pharmaceutical Companies Rankedby R&D Spending (US$ in Billions) in 2010

  7. Advantages of the industrial production • Low prime cost (including innovations) • Large scale production • Unified package (good for transportation) • Quality control processes (standard technical documentation)

  8. Standard technical documentation • Pharmacopoeia • Technology and technical regulations • State standards • Producer Pharmacopoeia articles • SOPs • …

  9. It is extremely needed to provide us with safe, effective and qualitative medicines

  10. Basis of the most tecnological processes – dosage form of drug • Solid dosage forms (tablets, capsules, powders, granules, dragee, …) • Liquid dosage forms (solutions, suspension, emulsion) • Soft dosage forms (ointments, liniments, capsules, patches, gels…) • Gaseous dosage forms (gases, aerosols)

  11. Some special areas of drug production • drugs Galenical (extraction of medicinal plants: tinctures, extracts …) • biotech pharmaceuticals • children's medicines • ophthalmic formulations • geriatric medicines • …

  12. Tecnology of drug production according to the peculiarities of production and dosage form

  13. Drugs Galenical The process of extraction refers to the mass-transfer processes and flows through the diffusion laws

  14. The main factors are: • nature and characteristics of medicinal herbs • Properties of the extracting agent (water, ethanol, ethyl ether, chloroform, acetone, liquefied gases )

  15. Main stages of production: • Raw material preparation • Extraction process • Purification (settling, filtration, centrifugation) • Concentration or drying • Filling and packing

  16. Quality control • Organoleptic characteristics (transparency, chromaticity, taste, flavor) • Ethanol content and dencity (in tinctures) • Dry residue • Heavy metals

  17. Solid dosage forms tablets capsules sugar-coated tablets (dragee) • powders • granules • sachets

  18. Powders latin - pulvis (pulv.) • Powders are drugs or drug extracts that are dried and ground and micronized into fine particles. • According to the division into prescribed doses powders are pulveres indivisi (all doses are given inseparably) and pulveres divisi (they are divides into the prescribed number of doses). • According to the composition are simplex powders (consist one active ingredient) and complex powders (a mixture of more than one active ingredient).

  19. Solid dosage forms Тablets • A tablet is a solid dosage form that is prepared by compressing or molding of the drug into various sizes and shapes. • Dissolution is the rate-limiting step in the delivery of drug from a tablet to the systemiccirculation.

  20. Advantages • Production aspect • Large scale production at lowest cost • Easiest and cheapest to package and ship • High stability • User aspect (doctor, pharmacist, patient) • Easy to handling • Lightest and most compact • Greatest dose precision & least content variability

  21. Disadvantages • Some drugs resist compression into dense compacts • Drugs with poor wetting, slow dissolution, intermediate to large dosages may be difficult or impossible to formulate and manufacture as a tablet that provide adequate or full drug bioavailability • Bitter taste drugs, drugs with an objectionable odor, or sensitive to oxygen or moisture may require encapsulation or entrapment prior to compression or the tablets may require coating

  22. Types of tablets: • Tablets for oral administration • Tablets for vaginal administration • Tablets for implantation (pellets)

  23. Solid dosage forms Tablets for oral administration • Film coated tablets • Entericcoated tablets • Effervescent tablets • Sublingual tablets • Buccal tablets • Troches (lozenges) • Chewable tablets • Controlled release tablets - slow release tablets (SR) and modified release tablets (MR)

  24. Compressed Tablets contains: • Medicinal agent • Diluents or filler • Binders or adhesives • Disintergrants • Lubricants • Miscellaneousadjuncts • Colorants and flavorants

  25. DILUENTS Diluents increase the volume to a formulation to prepare tablets of the desired size. Widely used fillers are lactose, dextrin, microcrystalline cellu-lose starch, pregelatinized starch, powdered sucrose, and calcium phosphate.

  26. BINDERS • Binders promote the adhesion of particles of the formulation. Such adhesion enables preparation of granules and maintains the integrity of the final tablet.Commonly used binding agents include: water, ethanol, starch, gelatin and sugars (sucrose, glucose, dextrose, and lactose).

  27. DISINTEGRANTS • The breakup of the tablets to smaller particles is important for dissolution of the drug and subsequent bioavailability. Disintegrators promote such breakup. To rupture or breakup of tablets, disintegrating agents must swell or expand on exposure to aqueous solution. Thus, the most effective disintegrating agents in most tablet systems are those with the highest water uptake property. In general, the more hydrophilic, the better disintegrating agents are therefore highly hydrophilic.

  28. LUBRICANTS • Lubricant is a substance capable of reducing or preventing friction, heat, and wear when introduced as a film between solid surfaces. It works by coating on the surface of particles, and thus preventing adhesion of the tablet material to the dies and punches. • Lubricants play more than one role in the preparation of tablets. • Commonly used lubricants include: talc, magnesium stearat, calcium stearate ,stearic acid, hydrogenated vegetable oils and PEG.

  29. wet granulation: suitable for drugs that are stable to moisture and heat dry granulation: suitable for drugs that are sensitive to moisture and heat powder compression : suitable for drugs that are sensitive to moisture and heat, fill material possessing, good flowability and compressibility granulation direct compression Compressed tablet manufacturing • The classification of manufacturing methods crystal compression：suitable for drugs with proper crystal form and good flowability

  30. The classification of tablet presses • Tablet presses: a. single-punch presses b. multi-station rotary presses

  31. The main components of single-punch tablet presses Core components: die lower punch upper punch

  32. The compression cycle of a rotary tablet press

  33. Tablet coating The reasons for tablet coating 1) to protect the medicinal agent against destructive exposure to air and/or humidity; 2) to mask the taste of the drug; 3) to provide special characteristics of drug release; 4) to provide aesthetics or distinction to the product; 5) to prevent inadvertent contact by nonpatients with the drug substance

  34. Tablet coating The general methods involved in coating tablets are as follows 1) sugarcoating tablets 2) film-coating tablets 3) fluid-bed or air suspension coating 4) compression coating

  35. Quality standards and compendial requirements The apparent physical features of compressed tablets: 1) shape: round, oblong, unique 2) thickness: thick or thin 3) diameter: large or small 4) flat or convex 5) unscored or scored in halves, thirds and quadrants 6) engraved or imprinted with an identifying symbol and/or code number 7) coated or uncoated 8)colored or uncolored 9) number of layers.

  36. Quality standards and compendial requirements • Other physical specifications and quality standards: tablet weight weight variation content uniformity tablet thickness tablet hardness tablet disintegration drug dissolution • in-process controls • verification after the production

  37. Quality standards and compendial requirements Tablet hardness 1)The greater the pressure applied, the harder the tablets. 2) The hardness required by different tablets a) lozenges and buccal tablets: hard (dissolve slowly) b) the tablets for immediate drug release: soft 3) Measurement a) special dedicated hardness testers b) multifunctional equipment

  38. Quality standards and compendial requirements Friability 1) It is used to determine a tablet’s durability 2) Method: allowing the tablets to roll and fall within the rotating apparatus (friabilator); determine the loss in weight; 3) requirement: weight loss ≤1%

  39. Quality standards and compendial requirements — tablet dissolution 1) The importance of in vitro dissolution test a) to guide the formulation and product development process toward product optimization b) to monitor the performance of manufacturing process c) to assure bioequivalence from batch to batch d) as a requirement for regulatory approval for product marketing for products registered with the FDA and regulatory agencies of other countries.

  40. 2) The goal of in vitro dissolution is to provide a reasonable prediction of the product’s in vivo bioavailability. Basis: The combinations of a drug’s solubility and its intestinal permeability are supposed as a basis for predicting the likelihood of achieving a successful in vivo – in vitro correlation (IVIVC).

  41. 3) The formulation and manufacturing factors affecting the dissolution of a tablet a) the particle size of the drug substance b) the solubility and hygroscopicity of the formulation c) the type and concentration of the disintegrant, binder, and lubricant used d) the manufacturing method, particularly, the compactness of the granulation and the compression force e) the in-process variables

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