QBD-BASED DEVELOPMENT AND EVALUATION OF TIME-DEPENDENT CHRONOPHARMACEUTICAL DRUG DELIVERY SYSTEM OF AMOXICILLIN TRIHYDRATE FOR MANAGEMENT OF BACTERIAL INFECTION
Abstract
The present studies discuss about the quality by design (QbD)-based development and evaluation of chronomodulated release drug delivery system of amoxicillin trihydrate for management of bacterial infection. Initially, target product profile was defined and critical quality attributes were earmarked. Risk assessment study was performed for identifying the critical material attributes. Preformulation studies were carried out, and direct compression method was employed for the preparation of bilayer matrix tablets containing a delayed and a sustained release layer for preliminary optimization. Systematic formulation optimization was carried out using central composite design by selecting the concentration of Eudragit-L100 D55 and HPMCK4M. Mathematical modeling was performed and optimized compositions of the polymers were identified from the design space. Moreover, the prepared bilayer tablets were evaluated for various tablet properties including in vitro drug release study, release kinetics evaluation and characterized for FTIR, DSC, XRD, SEM studies, in vitro was-off test, antimicrobial assay and accelerated stability studies. In a nutshell, the present studies indicated the supremacy of designing a chronomodulated release bilayer tablet formulations of amoxicillin trihydrate for effective management of bacterial infections.
Keywords:
Amoxicillin, Bilayer tablet, Dissolution, In vitro drug release, Antimicrobial assayDOI
https://doi.org/10.25004/IJPSDR.2018.100311References
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2. Kalantzi LE, Evangelos K, Koutris EX, Bikaris DN. Recent advances in oral pulsatile drug delivery. Recent Pat. Drug Deliv. Formul. 2009; 3(1): 49-63.
3. Hommura Y, Sakamoto Y, Matsukawa J, Shinkawa A. Clinical study on amoxicillin in otorhinolaryngological field. Jpn. J. Antibiot. 1975; 28(3): 353-362.
4. Stillerman M, Isenberg HD, Kacklam RR. Treatment of pharyngitis associated with group A Streptoccous: Comparison of amoxicillin and potassium phenoxymethyl penicillin. J. Infect. Dis. 1974; 129 (Suppl: S1): 69-77.
5. Sherwood PV, Wibawa JI, Atherton JC, Jordan N, Jenkins D, Barrett DA, Shaw PN, Spiller RC. Impact of acid secretion, gastritis, and mucus thickness on gastric transfer of antibiotics in rats. Gut. 2002; 51(4): 490-495.
6. USP 34-NF 29. [Online] Available at: http://www.usp.org/USPNF. (Accessed on 8th February, 2011).
7. Amoxicillin. [Online] Available at: http://en.wikipedia.org/wiki/Amoxicillin. (Accessed on 8th February, 2011).
8. Beauchampa D, Labrecque G. Chronobiology and chronotoxicology of antibiotics and aminoglycosides. Adv. Drug Deliv. Rev. 2007; 59(9-10): 896-903.
9. Breese BB, Disney FA, Talpey WB, Green JL. Treatment of streptococcal pharyngitis with amoxicillin. J. Infet. Dis. 1974; 129(Suppl: S1): 78-80.
10. Beg S, Swain S, Gahoi S, Kohli K. Design, development and evaluation of chronomodulated drug delivery systems of amoxicillin trihydrate with enhanced antimicrobial activity. Curr Drug Deliv. 2013; Apr 10(2):174-87.
11. Leuthner KD, Cheung CM, Rybak MJ. Pulsatile delivery of clarithromycin alone or in combination with amoxicillin against Streptococcus pneumoniae. Antimicrob. Agents Chemother. 2006; 813-816.
12. Sun HK, Lee SY, Banevicius MA, Du X, Maglio D, Nicolau DP. Efficacy of pulsatile amoxicillin and clarithromycin dosing alone and in combination in a murine pneumonia model. J. Antimicrob. Chemother. 2005; 56(3): 559-565.
13. Kurosu M. Multiple-delayed release formulation approach for the treatment of methicillin-resistant Staphylococcus aureus. Expert Opin. Ther. Pat. 2008; 18(11): 1313-1319.
14. Sanchez-Lafuente C, Faucci MT, Fernández-Arévalo M, Álvarez-Fuentes J, Rabasco AM, Mura P. Development of sustained release matrix tablets of didanosine containing methacrylic and ethylcellulose polymers. Int. J. Pharm. 2002; 234(1-2): 213-221.
15. Chang RK, Guo X, Burside BA, Couch RA, Rudnic EM. Formulation approaches for oral pulsatile drug delivery. Am. Pharma. Rev. 1999; 2(1): 51-57.
16. Kikuchi A, Okano T. Pulsatile drug release control using hydrogels. Adv. Drug Deliv. Rev. 2002; 54: 53–77.
17. Tekade AR, Gattani SG. Development and evaluation of pulsatile drug delivery system using novel polymer. Pharm. Dev. Technol. 2009; iFirst: 1–8.
18. Gazzanig A, Palugan L, Foppoli A, Sangalli ME. Oral pulsatile delivery systems based on swellable hydrophilic polymers. Eur. J. Pharm. Biopharm. 2008; 68: 11-18.
19. Shiyani B, Gattani S, Surana S. Formulation and evaluation of bilayer tablet of metoclopramide hydrochloride and ibuprofen. AAPS PharmSciTech. 2008; 9(3): 818-827.
20. Patra CN, Kumar AB, Pandit HK, Singh SP, Devi MV. Design and evaluation of sustained release bilayer tablets of propranolol hydrochloride. Acta Pharm. 2007; 57: 479-489.
21. Dhumal RS, Rajmane ST, Dhumal ST, Pawar AP. Design and evaluation of bilayer floating tablets of Cefuroxime axetil for bimodal release. J. Scientific Indust. Res. 2006; 65(10): 812-816.
22. Naeem M, Mahmood A, Khan S, Shahiq Z. Development and evaluation of controlled-release bilayer tablets containing microencapsulated tramadol and acetaminophen. Tropical J. Pharm. Res. 2010; 9(4): 347-354.
23. Atram SC. Formulation of bilayer tablet containing metoprolol succinate and amlodipine besylate as a model drug for antihypertensive therapy. J. Pharm. Res. 2009; 2(8): 1335-1347.
24. Beg S, Hasnain MS, Swain S, Kohli K. Validated stability-indicating LC method for estimation of amoxicillin trihydrate in pharmaceutical dosage forms and time-dependent release formulations. Int. J. Pharm. Sci. Nanotechnol. 2011; 4(2): 1423-1427.
25. Beg S, Kohli K, Swain S, Hasnain MS. Development and validation of RP-HPLC method for quantitation of amoxicillin trihydrate in bulk and pharmaceutical formulations using box-behnken experimental design. J. Liq. Chromatogr. Related Technol. 2012; 35: 393-406.
26. Thummel KE, Shen DD, Isoherranen N, Smith HE. Design and Optimization of Dosage Regimens; Pharmacokinetic data. In: Bruton LL, Laro JS, Parker KL, ed. Goodman and Gilman’s The Pharmacological Basis of Therapeutics, McGraw-Hill Medical Publishing Division, London, 2006, 1863-1875.
27. United States Pharmacopoeia, XXIV NF 19, United States Pharmacopoeia convention, Rockville, 2000, 2388-2389.
28. Higuchi T. Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J. Pharm. Sci. 1963; 52: 1145-1149.
29. Hixson AW, Crowell JH. Dependence of reaction velocity upon surface and agitation. Ind. Eng. Chem. 1931; 23: 923-931.
30. Korsmeyer RW, Gurny R, Doelker EM, Buri P, Peppas NA. Mechanism of solute release from porous hydrophilic polymers. Int. J. Pharm. 1983; 15: 25-35.
31. Peppas NA. Analysis of Fickian and non-Fickian drug release from polymers. Pharm. Acta Helv. 1985; 60: 110-111.
32. Sungthongjeen S, Puttipipatkhachorn S, Paeratakul O, Dashevsky A, Bodmeier R. Development of pulsatile release tablets with swelling and rupturable layers. J. Control. Release 2004; 95: 147-159.
33. Ravi PR, Ganga S, Saha RN. Design and study of lamivudine oral controlled release tablets. AAPS PharmSciTech. 2007; 8(4): E101-E109.
34. Sriamornsak P, Thirawong N, Korkerd K. Swelling, erosion and release behavior of alginate-based matrix tablets. Eur. J. Pharm. Biopharm. 2007; 66: 435-450.
35. Sankalia JM, Sankalia MG, Mashru RC. Drug release and swelling kinetics of directly compressed glipizide sustained-release matrices: Establishment of level A IVIVC. J. Control. Release. 2008; 129: 49-58.
36. Ali J, Khar R, Ahuja A, Kalra R. Buccoadhesive erodible disk for treatment of oro-dental infections. Int. J. Pharm. 1994; 283: 93-103.
37. Bonev B, Hooper J, Parisot J. Principles of assessing bacterial susceptibility to antibiotics using the agar diffusion method. J. Antimicrob. Chemother. 2008; 61(6): 1295-1301.
38. Indian Pharmacopoeia, Vol. 1, Controller of Publications, New Delhi, 1996.
39. Govender S, Pillay V, Chetty DJ, Essack SY, Dangor CM, Govender T. Optimization and characterization of bioadhesive controlled release tetracycline microspheres. Int. J. Pharm., 2005; 306: 24-40.
40. Ammar HO, Khalil RM. Preparation and evaluation of sustained release solid dispersions of drugs with Eudragit polymers. Drug Dev. Ind. Pharm. 1997; 23(11): 1043-1054.
41. Katzhendler I, Mader K, Friedman M. Structure and hydration properties of hydroxypropyl methylcellulose matrices containing naproxen and naproxen sodium. Int. J. Pharm. 2000; 200: 161-179.
42. Kim H, Fassihi R. Application of binary polymer system in drug release rate modulation, 2: influence of formulation variables and hydrodynamic conditions on release kinetics. J. Pharm. Sci. 1997; 86: 323-328.
43. Sung KC, Nixon PR, Skoug JW, Ju TR, Gao P, Topp EM, Patel MV. Effect of formulation variables on drug and polymer release from HPMC-based matrix tablets. Int. J. Pharm. 1996; 142: 53-60.
44. Shah N, Zhang G, Apelian V, Zeng F, Infeld MH, Malick AW. Prediction of drug release from hydroxypropyl methylcellulose (HPMC) matrices: effect of polymer concentration. Pharm. Res. 1993; 10: 1693-1695.
45. Bravo SA, Lamas MC, Salomon CJ. Swellable matrices for the controlled-release of diclofenac sodium: formulation and in vitro studies. Pharm. Dev. Technol. 2004; 9: 75-83.
46. York P. A consideration of experimental variables in the analysis of powder compression behaviour. J. Pharm. Pharmacol. 1979; 1: 244-246.
47. Ford JL, Rubinstein MH, Hogan JE. Formulation of sustained release promethazine hydrochloride tablets using hydroxypropyl methylcellulose matrices. Int. J. Pharm. 1985; 24: 327-338.
48. Li S, Shen Y, Li W, Hao X. A common profile for polymer-based controlled release and its logical interpretation to general release process. J. Pharm. Pharmceu. Sci. 2006; 9: 238-244.
49. Beg S, Nayak AK, Kohli K, Swain S, Hasnain MS. Antimicrobial activity assessment of time-dependent release bilayer tablets of amoxicillin trihydrate. Brazil. J. Pharm. Sci. 2012; 48(2): 1-8.
2. Kalantzi LE, Evangelos K, Koutris EX, Bikaris DN. Recent advances in oral pulsatile drug delivery. Recent Pat. Drug Deliv. Formul. 2009; 3(1): 49-63.
3. Hommura Y, Sakamoto Y, Matsukawa J, Shinkawa A. Clinical study on amoxicillin in otorhinolaryngological field. Jpn. J. Antibiot. 1975; 28(3): 353-362.
4. Stillerman M, Isenberg HD, Kacklam RR. Treatment of pharyngitis associated with group A Streptoccous: Comparison of amoxicillin and potassium phenoxymethyl penicillin. J. Infect. Dis. 1974; 129 (Suppl: S1): 69-77.
5. Sherwood PV, Wibawa JI, Atherton JC, Jordan N, Jenkins D, Barrett DA, Shaw PN, Spiller RC. Impact of acid secretion, gastritis, and mucus thickness on gastric transfer of antibiotics in rats. Gut. 2002; 51(4): 490-495.
6. USP 34-NF 29. [Online] Available at: http://www.usp.org/USPNF. (Accessed on 8th February, 2011).
7. Amoxicillin. [Online] Available at: http://en.wikipedia.org/wiki/Amoxicillin. (Accessed on 8th February, 2011).
8. Beauchampa D, Labrecque G. Chronobiology and chronotoxicology of antibiotics and aminoglycosides. Adv. Drug Deliv. Rev. 2007; 59(9-10): 896-903.
9. Breese BB, Disney FA, Talpey WB, Green JL. Treatment of streptococcal pharyngitis with amoxicillin. J. Infet. Dis. 1974; 129(Suppl: S1): 78-80.
10. Beg S, Swain S, Gahoi S, Kohli K. Design, development and evaluation of chronomodulated drug delivery systems of amoxicillin trihydrate with enhanced antimicrobial activity. Curr Drug Deliv. 2013; Apr 10(2):174-87.
11. Leuthner KD, Cheung CM, Rybak MJ. Pulsatile delivery of clarithromycin alone or in combination with amoxicillin against Streptococcus pneumoniae. Antimicrob. Agents Chemother. 2006; 813-816.
12. Sun HK, Lee SY, Banevicius MA, Du X, Maglio D, Nicolau DP. Efficacy of pulsatile amoxicillin and clarithromycin dosing alone and in combination in a murine pneumonia model. J. Antimicrob. Chemother. 2005; 56(3): 559-565.
13. Kurosu M. Multiple-delayed release formulation approach for the treatment of methicillin-resistant Staphylococcus aureus. Expert Opin. Ther. Pat. 2008; 18(11): 1313-1319.
14. Sanchez-Lafuente C, Faucci MT, Fernández-Arévalo M, Álvarez-Fuentes J, Rabasco AM, Mura P. Development of sustained release matrix tablets of didanosine containing methacrylic and ethylcellulose polymers. Int. J. Pharm. 2002; 234(1-2): 213-221.
15. Chang RK, Guo X, Burside BA, Couch RA, Rudnic EM. Formulation approaches for oral pulsatile drug delivery. Am. Pharma. Rev. 1999; 2(1): 51-57.
16. Kikuchi A, Okano T. Pulsatile drug release control using hydrogels. Adv. Drug Deliv. Rev. 2002; 54: 53–77.
17. Tekade AR, Gattani SG. Development and evaluation of pulsatile drug delivery system using novel polymer. Pharm. Dev. Technol. 2009; iFirst: 1–8.
18. Gazzanig A, Palugan L, Foppoli A, Sangalli ME. Oral pulsatile delivery systems based on swellable hydrophilic polymers. Eur. J. Pharm. Biopharm. 2008; 68: 11-18.
19. Shiyani B, Gattani S, Surana S. Formulation and evaluation of bilayer tablet of metoclopramide hydrochloride and ibuprofen. AAPS PharmSciTech. 2008; 9(3): 818-827.
20. Patra CN, Kumar AB, Pandit HK, Singh SP, Devi MV. Design and evaluation of sustained release bilayer tablets of propranolol hydrochloride. Acta Pharm. 2007; 57: 479-489.
21. Dhumal RS, Rajmane ST, Dhumal ST, Pawar AP. Design and evaluation of bilayer floating tablets of Cefuroxime axetil for bimodal release. J. Scientific Indust. Res. 2006; 65(10): 812-816.
22. Naeem M, Mahmood A, Khan S, Shahiq Z. Development and evaluation of controlled-release bilayer tablets containing microencapsulated tramadol and acetaminophen. Tropical J. Pharm. Res. 2010; 9(4): 347-354.
23. Atram SC. Formulation of bilayer tablet containing metoprolol succinate and amlodipine besylate as a model drug for antihypertensive therapy. J. Pharm. Res. 2009; 2(8): 1335-1347.
24. Beg S, Hasnain MS, Swain S, Kohli K. Validated stability-indicating LC method for estimation of amoxicillin trihydrate in pharmaceutical dosage forms and time-dependent release formulations. Int. J. Pharm. Sci. Nanotechnol. 2011; 4(2): 1423-1427.
25. Beg S, Kohli K, Swain S, Hasnain MS. Development and validation of RP-HPLC method for quantitation of amoxicillin trihydrate in bulk and pharmaceutical formulations using box-behnken experimental design. J. Liq. Chromatogr. Related Technol. 2012; 35: 393-406.
26. Thummel KE, Shen DD, Isoherranen N, Smith HE. Design and Optimization of Dosage Regimens; Pharmacokinetic data. In: Bruton LL, Laro JS, Parker KL, ed. Goodman and Gilman’s The Pharmacological Basis of Therapeutics, McGraw-Hill Medical Publishing Division, London, 2006, 1863-1875.
27. United States Pharmacopoeia, XXIV NF 19, United States Pharmacopoeia convention, Rockville, 2000, 2388-2389.
28. Higuchi T. Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J. Pharm. Sci. 1963; 52: 1145-1149.
29. Hixson AW, Crowell JH. Dependence of reaction velocity upon surface and agitation. Ind. Eng. Chem. 1931; 23: 923-931.
30. Korsmeyer RW, Gurny R, Doelker EM, Buri P, Peppas NA. Mechanism of solute release from porous hydrophilic polymers. Int. J. Pharm. 1983; 15: 25-35.
31. Peppas NA. Analysis of Fickian and non-Fickian drug release from polymers. Pharm. Acta Helv. 1985; 60: 110-111.
32. Sungthongjeen S, Puttipipatkhachorn S, Paeratakul O, Dashevsky A, Bodmeier R. Development of pulsatile release tablets with swelling and rupturable layers. J. Control. Release 2004; 95: 147-159.
33. Ravi PR, Ganga S, Saha RN. Design and study of lamivudine oral controlled release tablets. AAPS PharmSciTech. 2007; 8(4): E101-E109.
34. Sriamornsak P, Thirawong N, Korkerd K. Swelling, erosion and release behavior of alginate-based matrix tablets. Eur. J. Pharm. Biopharm. 2007; 66: 435-450.
35. Sankalia JM, Sankalia MG, Mashru RC. Drug release and swelling kinetics of directly compressed glipizide sustained-release matrices: Establishment of level A IVIVC. J. Control. Release. 2008; 129: 49-58.
36. Ali J, Khar R, Ahuja A, Kalra R. Buccoadhesive erodible disk for treatment of oro-dental infections. Int. J. Pharm. 1994; 283: 93-103.
37. Bonev B, Hooper J, Parisot J. Principles of assessing bacterial susceptibility to antibiotics using the agar diffusion method. J. Antimicrob. Chemother. 2008; 61(6): 1295-1301.
38. Indian Pharmacopoeia, Vol. 1, Controller of Publications, New Delhi, 1996.
39. Govender S, Pillay V, Chetty DJ, Essack SY, Dangor CM, Govender T. Optimization and characterization of bioadhesive controlled release tetracycline microspheres. Int. J. Pharm., 2005; 306: 24-40.
40. Ammar HO, Khalil RM. Preparation and evaluation of sustained release solid dispersions of drugs with Eudragit polymers. Drug Dev. Ind. Pharm. 1997; 23(11): 1043-1054.
41. Katzhendler I, Mader K, Friedman M. Structure and hydration properties of hydroxypropyl methylcellulose matrices containing naproxen and naproxen sodium. Int. J. Pharm. 2000; 200: 161-179.
42. Kim H, Fassihi R. Application of binary polymer system in drug release rate modulation, 2: influence of formulation variables and hydrodynamic conditions on release kinetics. J. Pharm. Sci. 1997; 86: 323-328.
43. Sung KC, Nixon PR, Skoug JW, Ju TR, Gao P, Topp EM, Patel MV. Effect of formulation variables on drug and polymer release from HPMC-based matrix tablets. Int. J. Pharm. 1996; 142: 53-60.
44. Shah N, Zhang G, Apelian V, Zeng F, Infeld MH, Malick AW. Prediction of drug release from hydroxypropyl methylcellulose (HPMC) matrices: effect of polymer concentration. Pharm. Res. 1993; 10: 1693-1695.
45. Bravo SA, Lamas MC, Salomon CJ. Swellable matrices for the controlled-release of diclofenac sodium: formulation and in vitro studies. Pharm. Dev. Technol. 2004; 9: 75-83.
46. York P. A consideration of experimental variables in the analysis of powder compression behaviour. J. Pharm. Pharmacol. 1979; 1: 244-246.
47. Ford JL, Rubinstein MH, Hogan JE. Formulation of sustained release promethazine hydrochloride tablets using hydroxypropyl methylcellulose matrices. Int. J. Pharm. 1985; 24: 327-338.
48. Li S, Shen Y, Li W, Hao X. A common profile for polymer-based controlled release and its logical interpretation to general release process. J. Pharm. Pharmceu. Sci. 2006; 9: 238-244.
49. Beg S, Nayak AK, Kohli K, Swain S, Hasnain MS. Antimicrobial activity assessment of time-dependent release bilayer tablets of amoxicillin trihydrate. Brazil. J. Pharm. Sci. 2012; 48(2): 1-8.
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01-05-2018
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“QBD-BASED DEVELOPMENT AND EVALUATION OF TIME-DEPENDENT CHRONOPHARMACEUTICAL DRUG DELIVERY SYSTEM OF AMOXICILLIN TRIHYDRATE FOR MANAGEMENT OF BACTERIAL INFECTION”. International Journal of Pharmaceutical Sciences and Drug Research, vol. 10, no. 3, May 2018, pp. 173-85, https://doi.org/10.25004/IJPSDR.2018.100311.
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How to Cite
“QBD-BASED DEVELOPMENT AND EVALUATION OF TIME-DEPENDENT CHRONOPHARMACEUTICAL DRUG DELIVERY SYSTEM OF AMOXICILLIN TRIHYDRATE FOR MANAGEMENT OF BACTERIAL INFECTION”. International Journal of Pharmaceutical Sciences and Drug Research, vol. 10, no. 3, May 2018, pp. 173-85, https://doi.org/10.25004/IJPSDR.2018.100311.
