DESIGN DEVELOPMENT AND EVALUATION OF NANOSUSPENSION OF AZITHROMYCIN
Abstract
The objective of this study is to prepare a formulation of Azithromycin which increase the oral bioavailability as well as increased solubility and dissolution rate. In the present study nine formulations were formulated by using the three different polymers and varying the concentration of PEG and also varying the rotation speed of the stirrer. Results of preformulation studies like melting point 117°C, UV spectroscopy and FTIR studies showed that the drug was pure. The spherical and rough surface of F9 viewed through SEM. In-vitro dissolution study had shown satisfactory results. On the basis of release data and graphical analysis formulation F8 and F9 showed a good controlled zero order release profile.
Keywords:
Azithromycin, polyethylene glycol (PEG), nanosuspension, sustained release, Scanning electron microscopy (SEM), agglomerationDOI
https://doi.org/10.25004/IJPSDR.2015.070502References
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3. Christian L, Jennifer D. Improving drug solubility for oral delivery using solid dispersions. Eur J Pharm Biopharm. 2000; 50(1):47-60.
4. Lenhardt T, Vergnault G, Grenier P, Scherer D, Langguth P. Evaluation of nanosuspensions for absorption enhancement of poorly soluble drugs: In vitro Transport studies Across Intestinal Epithelial Monolayers. AAPS J. 2008 Sep; 10(3):435-438.
5. Amidon GL, Lennernas H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res. 1995; 12:413-420.
6. Verma S. Quality by design principles were explored to maximize the understanding of the unit operation of micro fluidization, for the preparation of nanosuspension using indomethacin as model drug. Adv Drug Deliv Rev. 2009; 56:827-40.
7. Keck CM, Muller RH. Drug nanocrystals of poorly soluble drugs produced by high pressure homoginisation. Eur J Pharm Biopharm. 2006; 62:3-16.
8. Basa S, Muniyappan T, Karatgi P, Prabhu R, Pillai R. Production and in vitro Characterization of solid dosage form incorporating drug nanoparticles. Drug Dev Ind Pharm. 2008; 34(11):1209-18.
9. Kipp JE, Wong J, Doty M, Werling J, Rebbeck C, Brynjelsen S. Method for preparing submicron particle suspensions. US Patent, 2003, 0031719 A1.
10. Banavath H, Sivarama RK, Ansari T, Ali S, Pattnaik G. Nanosuspension: an attempt to enhance bioavailability of poorly soluble drugs. International Journal of Pharmaceutical Sciences and Research 2010; 1(9):1-11.
11. Gambhire MN, Ambade KW, Kurmi SD, Kadam VJ, Jadhav KR. Development and in vitro evaluation of an oral floating matrix tablet formulation of diltiazem hydrochloride. AAPS PharmSciTech. 2007 Sep 7; 8(3):E73.
12. Singhvi G, Singh M. Review: in vitro drug release characterization models. International Journal of Pharmaceutical Studies and Research 2011; 2(1):77-84.
13. Hoepelman MI, Schneider EMM. Azithromycin: The first of the tissue-selective azalides. International Journal of Antimicrobial agents 1995; 5:145-167.
14. Harold C. Clinical microbiological of azithromycin. The American journal of Medicine 1991; 91(3, S1): S12-S18.
15. Page RL, Ruscin JM, Fish D, Lapointe M. Possible interaction between intravenous azithromycin and oral cyclosporine. Pharmacotherapy 2001; 21:1436–43.
16. History Highlights. Pliva, Pharmaceutical Industry. http://www.pliva.hr. Retrieved 20/11/2005.
17. Retsema J, Wench Fu. Macrolides: Structure and microbial targets. International Journal of Antimicrobial Agents 2001; 18:256-263.
18. McCall KL, Glenn AH, Jones AD. Determination of the lack of a drug interaction between Azithromycin and Warfarin. Pharmacotherapy 2004; 24(2):188-194.
19. Coates P, Daniel R, Huston CA. An open study to compare the pharmacokinetics, safety and tolerability of a multiple-dose regimen of Azithromycin in young and elderly volunteers. European Journal of Clinical Microbial Infectious Diseases 1991; 10:850-862.
20. Treadway G, Reisman A. Tolerability of 3-day, once daily Azithromycin suspension versus standard treatments for community-acquired paediatric infectious diseases. International Journal of Antimicrobial Agents 2001; 18:427-431.
21. Drew HR, Gallis AH. Azithromycin-spectrum of activity, pharmacokinetics and clinical applications. Pharmacotherapy 1992; 12(3):161-173.
22. Lalak NJ, Morris DL. Azithromycin clinical pharmacokinetics. Clinical Pharmacokinetics. 1993; 25(5):370-374.
23. Wilson and Gisvold’s textbook of organic medicinal and pharmaceutical chemistry 11th Edition. J.H. Lippincot Williams and Wilkins. London. 2004, pp. 352.
24. Rowe RC, Sheskey PJ, Martin CE. Handbook of Pharmaceutical Excipients. 2009, 6, pp. 518-522
25. Backett AH, Stenlake JB. Practical pharmaceutical chemistry.CBS publishers and distributors, New Delhi. 1997, 1, pp. 72–74.
26. Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. ActaPoloniae Pharmacy Drug Research 2010; 67(3):217-223.
27. Wongmekiat A, Tozuka Y, Oguchi T, Yamamoto K. Formation of fine drug particles by co-grinding with cyclodextrin: I: The use of β-cyclodextrin anhydrate and hydrate. Pharm Res. 2002; 19:1867–1872.
28. Itoh K, Pongpeerapat A, Tozuka Y, Oguchi T, Yamamoto K. Nanoparticle formation of poorly water soluble drugs from ternary ground mixtures with PVP and SDS. Chem Pharm Bull. 2003; 51:171–174.
29. Mura P, Cirri M, Faucci MT, Gines-Dorado JM, Bettinetti GP. Investigation of the effects of grinding and co-grinding on physicochemical properties of glisentide. J Pharm Biomed Anal. 2002; 30:227–237.
30. Murray JJ, Emparanza P, Lesinskas E, Tawadrous M, Breen JD. Efficacy and safety of a novel, single-dose Azithromycin Microsphere formulation versus 10 days of levofloxacin for the treatment of acute bacterial sinusitis in Adults. Otolaryngol Head Neck Surg. 2005 Aug; 133(2):194-200.
31. Rainbow B, Kipp J, Papadopoulos P, Wong J, Glosson J, Gass J, et al. Itraconazole IV nanosuspension enhances efficacy through altered pharmacokinetic in the rat. Int J Pharm. 2007; 339:251–60.
32. Sharma SA, Shirolkar SV. Development and Evaluation of In-Situ Gelling Otic Formulations of Azithromycin Dihydrate using Poloxamer. The Bioscan 2013; 8(1): 33-36.
2. Riaz M. Stability and uses of liposomes. Pak Pharm Sci. 1995; 8(2):69-79.
3. Christian L, Jennifer D. Improving drug solubility for oral delivery using solid dispersions. Eur J Pharm Biopharm. 2000; 50(1):47-60.
4. Lenhardt T, Vergnault G, Grenier P, Scherer D, Langguth P. Evaluation of nanosuspensions for absorption enhancement of poorly soluble drugs: In vitro Transport studies Across Intestinal Epithelial Monolayers. AAPS J. 2008 Sep; 10(3):435-438.
5. Amidon GL, Lennernas H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res. 1995; 12:413-420.
6. Verma S. Quality by design principles were explored to maximize the understanding of the unit operation of micro fluidization, for the preparation of nanosuspension using indomethacin as model drug. Adv Drug Deliv Rev. 2009; 56:827-40.
7. Keck CM, Muller RH. Drug nanocrystals of poorly soluble drugs produced by high pressure homoginisation. Eur J Pharm Biopharm. 2006; 62:3-16.
8. Basa S, Muniyappan T, Karatgi P, Prabhu R, Pillai R. Production and in vitro Characterization of solid dosage form incorporating drug nanoparticles. Drug Dev Ind Pharm. 2008; 34(11):1209-18.
9. Kipp JE, Wong J, Doty M, Werling J, Rebbeck C, Brynjelsen S. Method for preparing submicron particle suspensions. US Patent, 2003, 0031719 A1.
10. Banavath H, Sivarama RK, Ansari T, Ali S, Pattnaik G. Nanosuspension: an attempt to enhance bioavailability of poorly soluble drugs. International Journal of Pharmaceutical Sciences and Research 2010; 1(9):1-11.
11. Gambhire MN, Ambade KW, Kurmi SD, Kadam VJ, Jadhav KR. Development and in vitro evaluation of an oral floating matrix tablet formulation of diltiazem hydrochloride. AAPS PharmSciTech. 2007 Sep 7; 8(3):E73.
12. Singhvi G, Singh M. Review: in vitro drug release characterization models. International Journal of Pharmaceutical Studies and Research 2011; 2(1):77-84.
13. Hoepelman MI, Schneider EMM. Azithromycin: The first of the tissue-selective azalides. International Journal of Antimicrobial agents 1995; 5:145-167.
14. Harold C. Clinical microbiological of azithromycin. The American journal of Medicine 1991; 91(3, S1): S12-S18.
15. Page RL, Ruscin JM, Fish D, Lapointe M. Possible interaction between intravenous azithromycin and oral cyclosporine. Pharmacotherapy 2001; 21:1436–43.
16. History Highlights. Pliva, Pharmaceutical Industry. http://www.pliva.hr. Retrieved 20/11/2005.
17. Retsema J, Wench Fu. Macrolides: Structure and microbial targets. International Journal of Antimicrobial Agents 2001; 18:256-263.
18. McCall KL, Glenn AH, Jones AD. Determination of the lack of a drug interaction between Azithromycin and Warfarin. Pharmacotherapy 2004; 24(2):188-194.
19. Coates P, Daniel R, Huston CA. An open study to compare the pharmacokinetics, safety and tolerability of a multiple-dose regimen of Azithromycin in young and elderly volunteers. European Journal of Clinical Microbial Infectious Diseases 1991; 10:850-862.
20. Treadway G, Reisman A. Tolerability of 3-day, once daily Azithromycin suspension versus standard treatments for community-acquired paediatric infectious diseases. International Journal of Antimicrobial Agents 2001; 18:427-431.
21. Drew HR, Gallis AH. Azithromycin-spectrum of activity, pharmacokinetics and clinical applications. Pharmacotherapy 1992; 12(3):161-173.
22. Lalak NJ, Morris DL. Azithromycin clinical pharmacokinetics. Clinical Pharmacokinetics. 1993; 25(5):370-374.
23. Wilson and Gisvold’s textbook of organic medicinal and pharmaceutical chemistry 11th Edition. J.H. Lippincot Williams and Wilkins. London. 2004, pp. 352.
24. Rowe RC, Sheskey PJ, Martin CE. Handbook of Pharmaceutical Excipients. 2009, 6, pp. 518-522
25. Backett AH, Stenlake JB. Practical pharmaceutical chemistry.CBS publishers and distributors, New Delhi. 1997, 1, pp. 72–74.
26. Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. ActaPoloniae Pharmacy Drug Research 2010; 67(3):217-223.
27. Wongmekiat A, Tozuka Y, Oguchi T, Yamamoto K. Formation of fine drug particles by co-grinding with cyclodextrin: I: The use of β-cyclodextrin anhydrate and hydrate. Pharm Res. 2002; 19:1867–1872.
28. Itoh K, Pongpeerapat A, Tozuka Y, Oguchi T, Yamamoto K. Nanoparticle formation of poorly water soluble drugs from ternary ground mixtures with PVP and SDS. Chem Pharm Bull. 2003; 51:171–174.
29. Mura P, Cirri M, Faucci MT, Gines-Dorado JM, Bettinetti GP. Investigation of the effects of grinding and co-grinding on physicochemical properties of glisentide. J Pharm Biomed Anal. 2002; 30:227–237.
30. Murray JJ, Emparanza P, Lesinskas E, Tawadrous M, Breen JD. Efficacy and safety of a novel, single-dose Azithromycin Microsphere formulation versus 10 days of levofloxacin for the treatment of acute bacterial sinusitis in Adults. Otolaryngol Head Neck Surg. 2005 Aug; 133(2):194-200.
31. Rainbow B, Kipp J, Papadopoulos P, Wong J, Glosson J, Gass J, et al. Itraconazole IV nanosuspension enhances efficacy through altered pharmacokinetic in the rat. Int J Pharm. 2007; 339:251–60.
32. Sharma SA, Shirolkar SV. Development and Evaluation of In-Situ Gelling Otic Formulations of Azithromycin Dihydrate using Poloxamer. The Bioscan 2013; 8(1): 33-36.
Published
01-09-2015
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“DESIGN DEVELOPMENT AND EVALUATION OF NANOSUSPENSION OF AZITHROMYCIN”. International Journal of Pharmaceutical Sciences and Drug Research, vol. 7, no. 5, Sept. 2015, pp. 384-9, https://doi.org/10.25004/IJPSDR.2015.070502.
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How to Cite
“DESIGN DEVELOPMENT AND EVALUATION OF NANOSUSPENSION OF AZITHROMYCIN”. International Journal of Pharmaceutical Sciences and Drug Research, vol. 7, no. 5, Sept. 2015, pp. 384-9, https://doi.org/10.25004/IJPSDR.2015.070502.
