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Aqueous Suspensions

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Long Acting Injections and Implants

Part of the book series: Advances in Delivery Science and Technology ((ADST))

Abstract

A good formulation of coarse particles dispersed in a liquid vehicle is facilitated by an understanding of the theory of particle technology and methodologies to assess physical properties of the resulting product. Formulation parameters include particle–vehicle interactions, sedimentation/flocculation kinetics, particle size and crystal form identity and stability, and appropriate suspension rheology to aid flocculation and minimize caking. The vehicle and stabilizers added must allow for creation of a flocculated system, prevent caking, and promote rapid redispersion. Additional delivery considerations include irritation and pain potential, in vitro vs. in vivo release methodologies, and the targeted delivery profile.

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References

  1. Kayes JB (1977) Pharmaceutical suspensions: relation between zeta potential, sedimentation volume and suspension stability. J Pharm Pharmacol 29:199–204

    Article  PubMed  CAS  Google Scholar 

  2. Kuentz M, Roethlisberger D (2002) Sedimentation analysis of aqueous microsuspensions based on near infrared transmission measurements during centrifugation – determination of a suitable amount of gelling agent to minimize settling in the gravitational field. STP Pharma Sci 12:391–396

    CAS  Google Scholar 

  3. Briceno MI (2000) Rheology of suspensions and emulsions. In: Drugs and the pharmaceutical sciences (pharmaceutical emulsions and suspensions), vol 105. Dekker, New York, pp 557–607

    Google Scholar 

  4. Tripathi DK, Ghosal SK, Panda D (1994) Rheological characterization of CMC for formulating some pharmaceutical suspensions. J Polym Mater 11:141–146

    CAS  Google Scholar 

  5. Graham DT, Pomeroy AR (1978) The effects of freezing on commercial insulin suspensions. Int J Pharm 1:315–322

    Article  CAS  Google Scholar 

  6. Deicke A, Suverkrup R (1999) Dose uniformity and redispersibility of pharmaceutical suspensions. I: Quantification and mechanical modeling of human shaking behavior. Eur J Pharm Biopharm 48:225–232

    Article  PubMed  CAS  Google Scholar 

  7. Han J, Beeton A, Long PF, Wong I, Tuleu C (2006) Physical and microbiological stability of an extemporaneous tacrolimus suspension for paediatric use. J Clin Pharm Ther 31:167–172

    Article  PubMed  CAS  Google Scholar 

  8. Wong J, Papadopoulos P, Werling J, Rebbeck C, Doty M, Kipp J, Konkel J, Neuberger D (2006) Itraconazole suspension for intravenous injection: determination of the real component of complete refractive index for particle sizing by static light scattering. PDA J Pharm Sci Technol 60:302–313

    PubMed  CAS  Google Scholar 

  9. Duro R, Souto C, Gomez-Amoza JL, Martinez-Pacheco R, Concheiro A (1999) Interfacial adsorption of polymers and surfactants: implications for the properties of disperse systems of pharmaceutical interest. Drug Dev Ind Pharm 25:817–829

    Article  PubMed  CAS  Google Scholar 

  10. de Villiers MM, Mahlatji MD, Malan SF, van Tonder EC, Liebenberg W (2004) Physical transformation of niclosamide solvates in pharmaceutical suspensions determined by DSC and TG analysis. Pharmazie 59:534–540

    PubMed  Google Scholar 

  11. Macek TJ (1963) Preparation of parenteral dispersions. J Pharm Sci 52:694–699

    Article  CAS  Google Scholar 

  12. Buckwalter FH, Dickison HL (1958) The effect of vehicle and particle size on the absorption, by the intramuscular route, of procaine penicillin G suspensions. J Pharm Sci 47:661–666

    Article  CAS  Google Scholar 

  13. Butterstein GM, Castracane VD (2000) Effect of particle size on the prolonged action of ­subcutaneous danazol in male and female rats. Fertil Steril 74:356–358

    Article  Google Scholar 

  14. Deshpande AP, Krishnan JM, Kumar PBS (2010) Rheology of complex fluids. Springer, New York, NY

    Google Scholar 

  15. Gupta RK (2000) Polymer and composite rheology, 2nd edn. Dekker, New York, NY

    Google Scholar 

  16. Larson RG (1999) The structure and rheology of complex fluids. Oxford University Press, New York, NY

    Google Scholar 

  17. Macosko CW (1993) Rheology: principles, measurements, and applications. Wiley-VCH, New York, NY

    Google Scholar 

  18. Matthews BA, Rhodes CT (1968) Flocculation phenomena in pharmaceutical suspensions. J Pharm Sci 57:569–573

    Article  PubMed  CAS  Google Scholar 

  19. Speiser P (1966) Galenic aspects of drug actions. Pharm Acta Helv 41:321–342

    PubMed  CAS  Google Scholar 

  20. Apelian HM, Coffin-Beach D, Huq AS (1992) Pharmaceutical composition of florfenicol. US Patent 5,082,863

    Google Scholar 

  21. Patterson A, Holmes D (1996) Long acting oxytetracycline composition. PCT Int Appl, p 13. CODEN: PIXXD2 WO 9601634 A1 19960125 CAN 124:185632 AN 1996:150381

    Google Scholar 

  22. Mosher GL, Thompson DO (2002) Formulations containing propofol and a sulfoalkyl ether cyclodextrin. PCT Int Appl, p 56. CODEN: PIXXD2 WO 2002074200 A1 20020926 CAN 137:253005 AN 2002:736046

    Google Scholar 

  23. Spiegel AJ, Noseworthy MM (1963) Use of nonaqueous solvents in parenteral products. J Pharm Sci 52:917–927

    Article  PubMed  CAS  Google Scholar 

  24. Yalkowsky SL, Roseman TJ (1981) Solubilization of drugs by cosolvents. In: Yalkowsky SH (ed) Techniques of solubilization of drugs. Dekker, New York, NY, pp 91–134

    Google Scholar 

  25. Higuchi T, Lach JL (1954) Study of possible complex formation between macromolecules and certain pharmaceuticals. III. Interaction of polyethylene glycols with several organic acids. J Am Pharm Assoc 43:465–470

    CAS  Google Scholar 

  26. Aguiar AJ, Armstrong WA, Desai SJ (1987) Development of oxytetracycline long acting injectable. J Control Release 6:375–385

    Article  CAS  Google Scholar 

  27. Kwon GS, Okano T (1996) Polymeric micelles as new drug carriers. Adv Drug Deliv Rev 21:107–116

    Article  CAS  Google Scholar 

  28. Tubetskoy VS (1999) Polymeric micelles as carriers of diagnostic agents. Adv Drug Deliv Rev 37:81–88

    Article  Google Scholar 

  29. Bader H, Ringsdorf H, Schmidt B (1984) Water-soluble polymers in medicine. Angew Makromol Chem 123:457–485

    Article  Google Scholar 

  30. La SB, Okana T, Kataoka K (1996) Preparation and characterization of the micelle-forming polymeric drug indomethacin-incorporated poly(ethylene oxide)-poly(beta-benzyl L-aspartate) block copolymer micelles. J Pharm Sci 85:85–90

    Article  PubMed  CAS  Google Scholar 

  31. Burgess DJ, Hussain AS, Ingallinera TS, Chen MI (2002) Assuring quality and performance of sustained and controlled release parenterals: AAPS workshop report, co-sponsored by FDA and USP. Pharm Res 19:1761–1768

    Article  PubMed  CAS  Google Scholar 

  32. Burgess DJ, Crommelin DJA, Hussain AS, Chen MI (2004) Assuring quality and performance of sustained and controlled release parenterals: EUFEPS workshop report. AAPS Pharm Sci 6:100–111

    Article  Google Scholar 

  33. Martinez M, Rathbone M, Burgess D, and Huynh M (2008) In vitro and in vivo considerations associated with parenteral sustained release products: A review based upon information ­presented and points expressed at the 2007 Controlled Release Society Annual Meeting. J. Controlled Release 129:79–87

    Google Scholar 

  34. Ostergaard J, Larse SW, Parshad H, Larsen C (2005) Bupivacaine salts of difilunisal and other aromatic hydroxycarboxylic acids: aqueous solubility and release characteristics from solutions and suspensions using a rotating dialysis cell model. Eur J Pharm Sci 26:280–287

    Article  PubMed  CAS  Google Scholar 

  35. Chien UW (1981) Long acting parenteral drug formulations. J Parenter Sci Technol 35:106–139

    PubMed  CAS  Google Scholar 

  36. Hornish RE, Kotarski SF (2002) Cephalosporins in veterinary medicine – ceftiofur use in food animals. Curr Top Med Chem 2:717–731

    Article  PubMed  CAS  Google Scholar 

  37. Brown SA, Hanson BJ, Mignot A, Millerioux L, Hamlow PJ, Hubbard V, Callahan JK, Kausche FM (1999) Comparison of plasma pharmacokinetics and bioavailability of ceftiofur sodium and ceftiofur hydrochloride in pigs after a single intramuscular injection. J Vet Pharmacol Ther 22:35–40

    Article  PubMed  CAS  Google Scholar 

  38. McCarty DJ, Faires JS (1936) A comparison of the duration of local anti-inflammatory effect of several adrenocorticosteroid esters – a bioassay technique. Curr Ther Res Clin Exp 5:284–290

    Google Scholar 

  39. Blyth T, Hunter JA, Stirling A (1994) Pain relief in the rheumatoid knee after steroid injection: a single-blind comparison of hydrocortisone succinate and triamcinolone acetonide or hexacetonide. Br J Rheumatol 33:461–463

    Article  PubMed  CAS  Google Scholar 

  40. Derendorf H, Mollmann H, Voortman G, Van den Ouwelan FA, Van de Putte LBA, Gevers G, Dequeker J, van Vliet-Daskalapoulou E (1990) Pharmacokinetics of rimexolone after intra-articular administration. J Clin Pharmacol 30:476–479

    PubMed  CAS  Google Scholar 

  41. Nieuwenhuyse H, Lewis AJ (1980) The persistence and effects of rimexolone in arthritic and normal rabbit knee joints. Arzneimittelforschung 30:1646–1649

    PubMed  CAS  Google Scholar 

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Author information

Authors and Affiliations

  1. Pharmaceutical Sciences Veterinary Medicine R&D, Pfizer Inc., Kalamazoo, MI, USA

    Susan M. Machkovech & Todd P. Foster

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  1. Susan M. Machkovech
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  2. Todd P. Foster
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Correspondence to Susan M. Machkovech .

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Editors and Affiliations

  1. Cuesta Drive 631, Los Altos, 94024, USA

    Jeremy C. Wright

  2. Browns Road 626, Storrs, 06268, Connecticut, USA

    Diane J. Burgess

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© 2012 Controlled Release Society

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Machkovech, S.M., Foster, T.P. (2012). Aqueous Suspensions. In: Wright, J., Burgess, D. (eds) Long Acting Injections and Implants. Advances in Delivery Science and Technology. Springer, Boston, MA. https://doi.org/10.1007/978-1-4614-0554-2_8

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