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Parenteral controlled release drug delivery system - by varsha phirke

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Parenteral controlled release drug delivery system - by varsha phirke

  1. 1. Parenteral Controlled Release System Seminar By: Varsha Phirke M Pharm (Pharmaceutics) Guided by: Mrs. Pallavi Chaudhari Padm. Dr. D. Y. Patil College of Pharmacy, Akurdi1
  2. 2. Contents:  Terminology  Approaches  Mechanism  Injectable drug delivery system  Long acting contraceptive formulations  Implantable drug delivery  Quality Control  Case study  References 2
  3. 3. Terminology Parenteral is the introduction of nutrition, a medication, or other substance into the body via a route other than the mouth, especially via infusion, injection or implantation. Controlled Release drug delivery systems aim to maintain plasma concentration of drugs within the therapeutic window for a longer period of time 3
  4. 4. Difference between IR-SR-CR in terms of plasma concentration 4
  5. 5. Approaches: 1) Use of viscous, water miscible vehicles, such as an aqueous solution of gelatin or polyvinyl pyrrolidone. Change in solubility characteristics of drug Change in time of release once drug is administered Change in state of drug post administration 2) Utilization of water immiscible vehicles, such as vegetable oil, some water repelling agents, like aluminium monostearate. 3) Formation of thixotropic suspension Structural break point Change in flow properties Change in dissolution characteristics 5
  6. 6. Approaches: 4) Preparation of water insoluble drug derivatives such as salts, complexes and esters. Chemical modification without affecting therapeutic activity Kinetics are influenced Stability is enhanced 5) Dispersion in polymeric microspheres, or microcapsules such as lactides-glycolides homopolymers or copolymers Use of Surface active agent Polymerization insitu or through reaction Microcapsules using various techniques 6) Co-administration of vasoconstrictors 6
  7. 7. Mechanism: On the basis of different mechanism, depot formulation categories into four types 1) Dissolution controlled depot formulation 2) Adsorption type depot formulation 3) Encapsulation type depot formulation 4) Esterification type depot formulation 7
  8. 8. Class Mechanism Rate limiting step Examples Dissolution controlled depot Drug absorption is controlled by slow dissolution of drug particle. Dissolution of drug particles. Formation of salt or complexes with low aqueous solubility, Suspension of Macrocrystals. Adsorption type depot Binding of drug molecules to adsorbent [Al(OH)3] Rate of absorption. Vaccine preparations Encapsulation type depot Encapsulating drug within permeation barrier /dispersing drug particles in a diffusion matrix. Permeation across the permeation barrier & the rate of biodegradation. Naltrexone pamoate- releasing biodegradable microcapsule, liposome, & Norethindrone-releasing biodegradable beads. Esterification type depot Esterifying drug to form bioconvertible Prodrug-type ester & then into injection. Number of enzyme present, Interfacial partitioning of drug esters. Fluphenazine enanthate, nandrolone decanoate in oleaginous solution. 8
  9. 9. Injectable drug delivery system In situ forming drug delivery systems (ISFD) Classified into five categories according to their mechanism of depot formation: Thermoplastic pastes In situ cross linked systems In situ polymer precipitation Thermally induced gelling system In situ solidifying organogels. Microspheres Liposomes Suspension Solid lipid nanoparticles 9
  10. 10. Class Mechanism of depot formation Examples Thermoplastic pastes Semisolid polymers which injected as a melt and form a depot upon cooling to body temperature. D,L-lactide, glycolide, E-caprolactone, dioxanone and orthoesters In situ cross linked polymer systems Cross-linked polymer network can be found in situ by free radical reactions initiated by heat (thermosets) /absorption of photon / ionic interactions between small cation & polymer anions. Benzoyl pero PEG(polyethylene glycol)-oligo-glycol-acrylate, using a photo initiator, such as eosinxide( banned) In situ polymer precipitation Water-insoluble and biodegradable polymer in biocompatible organic solvent. Phase separation and precipitation of the polymer forming the depot at the site of injection Atrigel Thermally induced gelling system Gelation at body temperature when highly concentrated polymer solution >15% w/w were injected PEO-PPO-PEO (pluronics or poloxamers) In situ solidifying organogels Water insoluble amphiphilic lipids, which swell in water and forms various types of lyotropic liquid crystals. Glycerol monooleate/ monopalmitostearate/ monolinoleate, sorbitan monostearate (SMS) & different gelation modifiers (polysorbates 20 10
  11. 11. Generic name Trade name Dosage form Penicillin & Procaine Duracillin Squibb Suspension injection Medroxyprogesterone acetate Depo-Provera, Upjohn Suspension injection Fluphenazine enanthate and decanoate Prolixin enanthate and Prolixin decanoate; Squibb oil solutions Microcrystalline deoxycorticosone pivalate Percortan pivalate; Ciba oleaginous suspension Nandrolone decanoate Decadurabolin, Organon injection Insulin Zinc Utralente, Lente and semilente, Novo suspensions Testosterone enanthate / estradiol valerate in ethyl oleate B Ditate - DS, Savage repository vehicle 11
  12. 12. Long acting contraceptives formulations: (A)Injectables: Depo-Provera C-150 (Depot Medroxyprogesterone acetate injection) Deladroxate Norethindrone releasing biodegradable polymer based suspension Norethindrone enanthate in oleaginous solutions Norgestrel 17 beta fatty acid esters (B)IUD’s and subdermal implants: Hormonal intrauterine device (Mirena - also known as IUC or IUS) Nonhormonal intrauterine device with copper (US -Paragard) Subdermal contraceptive implant (US - Nexplanon/ Implanon/ Implanon NXT); internationally– Norplant- Jadelle 12
  13. 13. Implants 13
  14. 14. Approaches: A Controlled drug release by diffusion 1) Membrane permeation-controlled release system Non porous membranes, Porous membranes Semiporous membranes eg. - Norplant subdermal implants of levonorgestrel 2) Matrix diffusion-controlled release system Lipophilic polymers Hydrophilic polymers Porous polymers eg. - Compudose implant of estradiol 3) Micro-reservoir dissolution-controlled release system Hydrophilic reservoir in lipophilic matrix Lipophilic reservoir in hydrophilic matrix eg. - Synchro-mate implant of norgestomet 4) Membrane matrix hybrid type-controlled release system Lipophilic membrane with hydrophilic matrix Hydrophilic membrane with lipophilic matrix eg.- Norplant II subdermal implant of Levonorgesterl (4 years) 14
  15. 15. Approaches: B Controlled drug release by activation Osmotic pressure activated eg.- Alzet pump Vapour pressure activated eg.- Infusaid pump Magnetically activated Phonophoresis Hydrolysis activated eg.- for control release of levonorgestrel (poly ortho esters used) Hydration activated eg.- Hydron implant C Controlled drug delivery by feedback regulated mechanism Bioerosion regulated drug delivery system Bioresponse activated drug delivery system 15
  16. 16. Approach Mechanism example Membrane permeation- controlled release Drug encapsulated in capsule / spherical compartment Norplant subdermal implant Matrix diffusion-controlled release Homogenous dispersion of drug in lipophilic/ hydrophilic polymer matrix Compudose implant Micro-reservoir dissolution- controlled release Drug in suspension in aqueous solution of water miscible polymer forms dispersion of drug reservoir in polymer matrix Syncro mate implant Membrane matrix hybrid type-controlled release Hybrid of polymer membrane permeation controlled DDS and Polymer matrix diffusion controlled DDS Norplant II A. Controlled drug release by diffusion 16
  17. 17. Approach Mechanism Examples Osmotic pressure activated Drug reservoir solution or semisolid placed within semipermeable housing with controlled water permeability Alzet osmotic pump Vapour pressure activated Drug reservoir is solution is placed inside infusate chamber Infusaid pump Magnetically activated Magnetic wave triggering mechanism is incorporated into drug delivery device Hydrolysis activated Solid drug is homogenously dispersed throughout polymer matrix of bioerodible or biodegradable polymer Levonorgestrel using Poly ortho esters biodegradable polymer Hydration activated Solid drug is coated by hydrophilic polymer Hydron implant B. Controlled drug release by activation 17
  18. 18. C. Controlled drug delivery by feedback regulated mechanism Approach Mechanism Bioerosion regulated Drug dispersed bioerodible matrix fabricated with polymer coated with immobilised urease Bioresponse activated Drug enclosed in bioresponsive polymer whose permeability is controlled by concentration of biochemical agent in tissue 18
  19. 19. Quality Control of Parenterals 1) Sterility Tests. 2) Pyrogen Tests. 3) Leaker Tests. 4) Particulate matter testing. 5) Weight variation or content uniformity 6) Bacterial endotoxin test 19
  20. 20. 20 Case study Patel D. B. et al in Journal of Global Pharma Technology, 2010; 2(2): 85-90 has presented an article on Atrigel® system describing it as a proven sustained-release drug delivery platform that delivers therapeutic levels of a wide spectrum of drugs over a few days to several months with a single injection. Atrigel system is used for both Parenterals and site- specific drug delivery. The ease of manufacture of the Atrigel system and its relatively pain-free subcutaneous injection into the body provide significant advantages over both solid implants and micro particles. Most of the standard biodegradable polymers can be used in the Atrigel technology. The hydrophilic solvents employed in the Atrigel system to dissolve the polymers. The low- molecular- weight polymers at low polymer concentrations can be easily injected into the body using standard needles. The high molecular- weight polymers at high polymer concentrations may be used as gels or putties that can be placed into sites in the body where they solidify and provide support. Atrigel technology provides a more stable, ready-to-use formulation.
  21. 21. References: Yie W. Chien, Marcel Dekker Inc.; Novel Drug Delivery Systems- New York, Volume 50, 381:517 J. R. Robinson, V. H. Lee; Controlled drug delivery- fundamentals and applications- Marcel Dekker Inc., volume-20, 2nd edition, 5:58, 179:208, 484:515 K. E. Avis, H. A. Lieberman, L. Lachman; Pharmaceutical Dosage forms: Parenteral medications- Marcel Dekker Inc., Volume 1, 2nd edition, 1:-55, 5:106 Xiaoling Li, Bhaskara Jasti; Design of Controlled Release Drug delivery systems- McGraw-Hill Publications, 107:124, 139:168, 203:229 Vasant Ranade, Mannfred Hollinger; Drug delivery systems-CBS Publications, Second Edition, 115:135 G. S. Banker, C. T. Rhodes; Modern Pharmaceutics- Marcel Dekker Inc., 4th edition, 381:414, 501:528 21
  22. 22. References: N. K. Jain; Advances in Controlled and novel drug delivery-CBS Publications, 1st edition 2010, 204:229 Vyas S. P., Khar R. K. In; Controlled Drug Delivery Concepts and Advances- CBS Publication, 1st edition 2002, 452:457 Vyas S. P., Khar R. K. In; Targeted and Controlled Drug Delivery- CBS Publication, 4th edition, 2005, 213:215 Michael J. Akers, D. S. Larrimore, D. M. Guazzo; Parenteral Quality Control-CBS Publications, 2008, 3:17, 124:183, 287:354 Hitesh Bari; A prolonged release Parenterals drug delivery system – an overview, International Journal of Pharmaceutical Sciences Review and Research, Volume 3, Issue 1, July – August 2010; Article 001 Patel D. B. et al., Journal of Global Pharma Technology. 2010; 2(2): 85-90 22

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