improves enalapril maleate stability fluidized bed hot melt ......granules were prepared by hot melt...
TRANSCRIPT
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 1/17
Search
Log inMenu
Log in
Search SpringerLink Search
Research ArticlePublished: 03 August 2016
Fluidized Bed Hot Melt Granulation with Hydrophilic MaterialsImproves Enalapril Maleate Stability
Thiago F. Guimarães1,2,Amanda C. C. Comelli2,Luciana A. Tacón3,Talita A. Cunha4,Ricardo N. Marreto4 &[…]Luís A. P. Freitas 2 - Show fewer authors
AAPS PharmSciTech volume 18, pages1302–1310(2017)Cite this article
263 Accesses
5 Citations
1 Altmetric
Metrics details
Abstract
This work aimed at developing enalapril maleate granules in order to improve its stability in solid dosage form.Granules were prepared by hot melt granulation using a fluidized bed apparatus. Gelucire 50/13®, polyethyleneglycol 6000 e Poloxamer 407® were studied and compared as binders in 2 × 2 factorial designs where theproportions of enalapril maleate, binders and spray dried lactose were varied. The granulation process resulted inhigh yields and granule sizes that indicated the prevalence of particles coating. Furthermore, the granules obtainedshowed adequate flowability and a fast dissolution rate of enalapril maleate with almost 100% of the drug released in10 min. The stability of enalapril maleate in hard gelatin capsules showed that the drug stability was greatly increasedin granules, since for raw drug, the remaining content of enalapril maleate after 91 days was 68.4% and, for granules,the content was always above 93%. This result was confirmed by the quantification of the degradation products,enalaprilat and diketopiperazine, which were found in very low content in granules samples. The results demonstratethat fluidized bed hot melt granulation with hydrophilic binders is a suitable alternative for improving the chemicalstability of enalapril maleate.
This is a preview of subscription content, log in to check access.
Access options
Buy article PDF
B j l b i i
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 2/17
Instant access to the full articlePDF.
Price includes VAT for Brazil
37,40 €
Immediate online access to allissues from 2019. Subscription
will auto renew annually.
This is the net price. Taxes to becalculated in checkout.
99 €
Buy journal subscription
Learn more about Institutionalsubscriptions
Fig. 1
Fig. 2
Fig. 3
Fig. 4
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 3/17
Fig. 5
Fig. 6
Fig. 7
References
1. 1.
Alsante KM, Huynh-Ba K, Baertschi SW, Reed RA, Landis MS, Kleinman MH, et al. Recent trends in productdevelopment and regulatory issues on impurities in active pharmaceutical ingredient (API) and drug products.Part 1: predicting degradation related impurities and impurity considerations for pharmaceutical dosage forms.AAPSPharmSciTech. 2014;15:198–212. doi:10.1208/s12249-013-0047-x.
Google Scholar2. 2.
Regulska K, Stanisz B, Lisiecki P. Optimization of storage and manufacture conditions for imidaprilhydrochloride in solid state as a way to reduce costs of antihypertensive therapy. AAPSPharmSciTech.2013;14:1199–208. doi:10.1208/s12249-013-0010-x.
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 4/17
CASGoogle Scholar
3. 3.
McEvoy GK. AHFS Drug information 1999. 40th Edition Revised American Society of Health-SystemPharmacists, February, 1999.
4. 4.
Sosnowska K, Winnicka K, Czajkowska-Koanik A. Stability of extemporaneous enalapril maleate suspensionsfor pediatric use prepared from commercially available tablets. Acta Pol Pharm - Drug Res. 2009;66:321–6.
CASGoogle Scholar
5. 5.
Wang SL, Lin SY, Chen TF. Reaction kinetics of solid-state cyclization of enalapril maleate investigated byisothermal FT-IR microscopic system. Chem Pharm Bull. 2001;49:402–6.
CASArticlePubMedGoogle Scholar
6. 6.
Stanisz B. Evaluation of stability of enalapril maleate in solid phase. J Pharm Biomed Anal. 2003;31:375–80.
CASArticlePubMedGoogle Scholar
7. 7.
Diego M, Godoy G, Mennickent S, Godoy R. Chemical stability of enalapril maleate drug substance andtablets by a stability-indicating liquid chromatographic method. Quim Nova. 2011;34:450–4.
ArticleGoogle Scholar
8. 8.
Stanisz B. Kinetics of degradation of enalapril maleate in dosage forms. Acta Pol Pharm - Drug Res.2004;61:415–8.
CASGoogle Scholar
9. 9.
Al-Omari MM, Abdelah MK, Badwan AA, Jaber AMY. Effect of the drug-matrix on the stability of enalaprilmaleate in tablet formulations. J Pharm Biomed Anal. 2001;25:893–902.
CASArticlePubMedGoogle Scholar
10. 10.
Lima DM, Santos LD, Lima EM. Stability and in vitro release profile of enalapril maleate from differentcommercially available tablets: possible therapeutic implications. J Pharm Biomed Anal. 2008;47:934–7.
CASArticlePubMedGoogle Scholar
11. 11.
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 5/17
Resende RLO, Santoro MIRM, Matos JR. Stability and compatibility study on enalapril maleate usingthermoanalytical techniques. J Therm Anal Calorim. 2008;93:881–6.
ArticleGoogle Scholar
12. 12.
Cotton ML, Wu DW, Vadas EB. Drug-excipient interaction study of enalapril maleate using thermal analysisand scanning electron microscopy. Int J Pharm. 1987;40:129–42.
CASArticleGoogle Scholar
13. 13.
Merslavic SM, Jozica Razen NM, Rotar LR. Stable formulation of enalapril salt, a process for the preparationthereof and the use thereof. WO Patent. 1994.
14. 14.
Chen J, Zhang LH, Xu RJ, Bu NJ, Zhang L. Proposal of a new degradation mechanism of enalapril maleateand improvement of enalapril maleate stability in tablet formulation with different stabilizers. Pharmazie.2014;69:277–80.
CASPubMedGoogle Scholar
15. 15.
Cunha TA, Serpa RC, Oliveira APM, Nasser LN, Freitas LAP, Taveira SF, et al. Effect of stearic acid onenalapril stability and dissolution from multiparticulate solid dosage forms. AAPSPharmSciTech.2013;14:1150–7.
CASGoogle Scholar
16. 16.
Oliveira APM, Cunha TA, Serpa RC, Taveira SF, Lima EM, Freitas LAP, et al. Improvement of enalaprilmaleate chemical stability by high shear melting granulation. Pharm Dev Technol. 2014;20(08):1002–8.doi:10.3109/10837450.2014.959178.
ArticleGoogle Scholar
17. 17.
Zoppi A, Garnero C, Linck YG, Chattah AK, Monti GA, Longhi MR. Enalapril: β-CD complex: stabilityenhancement in solid state. Carbohydr Polym. 2011;86:716–21.
CASArticleGoogle Scholar
18. 18.
Thomsen R, Rasmussen HB, Linnet K. In vitro drug metabolism by human carboxylesterase 1: focus onangiotensin-converting enzyme inhibitors. Drug Metab Dispos. 2014;42:126–33.
CASArticlePubMedGoogle Scholar
19. 19.
Borini GB, Andrade TC, Freitas LAP. Hot melt granulation of coarse pharmaceutical powders in a spoutedbed. Powder Technol. 2009;189:520–7.
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 6/17
CASArticleGoogle Scholar
20. 20.
Rantanen J, Jørgensen A, Räsänen E, Luukkonen P, Airaksinen S, Raiman J, et al. Process analysis of fluidizedbed granulation. AAPSPharmSciTech. 2001;2:13–20. doi:10.1007/BF02830561.
Google Scholar21. 21.
Hu X, Li Y, Zhang E, Wang X, Xing M, Wang Q, et al. Preparation and evaluation of orally disintegratingtablets containing taste-masked microcapsules of berberine hydrochloride. AAPSPharmSciTech. 2013;14:29–37.
CASGoogle Scholar
22. 22.
Silva CAM, Taranto OM. Real-time monitoring of gas–solid fluidized-bed granulation and coating process:evolution of particle size, fluidization regime transitions, and psychometric parameters. Drying Technol.2015;33:1929–48. doi:10.1080/07373937.2015.1076000.
ArticleGoogle Scholar
23. 23.
Andrade TC, Martins RM, Freitas LAP. Granulation of indomethacin and a hydrophilic carrier by fluidized hotmelt method: the drug solubility enhancement. Powder Technol. 2015;270:453–60.
CASArticleGoogle Scholar
24. 24.
Kowalski J, Kalb O, Joshi YM, Serajuddin ATM. Application of melt granulation technology to enhancestability of a moisture sensitive immediate-release drug product. Int J Pharm. 2009;381:56–61.
CASArticlePubMedGoogle Scholar
25. 25.
Walker GM, Holland CR, Ahmad MMN, Craig DQM. Influence of process parameters on fluidized hot meltgranulation and tablet pressing of pharmaceutical powders. Chem Eng Sci. 2005;60:3867–77.
CASArticleGoogle Scholar
26. 26.
Kotyian PN, Yang D, Kulkarini R. Effect of the melt granulation technique on the dissolution characteristics ofgriseofulvin. Int J Pharm. 2007;329:72–80.
ArticleGoogle Scholar
27. 27.
Jivraj M, Martini LG, Thomson CM. An overview of the different excipients useful for the direct compressionof tablets. Pharm Sci Technol Today. 2000;3:58–63.
CASArticle
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 7/17
PubMedGoogle Scholar
28. 28.
Kidokoro M, Haramiishi Y, Sagasaki S, Shimizu T, Yamamoto Y. Application of fluidized hot-melt granulationfor the preparation of granules for tableting; properties of granules and tablets prepared by fluidized hot-meltgranulation. Drug Dev Ind Pharm. 2002;28:67–76.
CASArticlePubMedGoogle Scholar
29. 29.
Sharma VD, Akocak S, Ilies MA, Fassihi R. Solid-state interactions at the core-coat interface: physicochemicalcharacterization of enteric-coated omeprazole pellets without a protective sub-coat. AAPSPharmSciTech.2015;16:934–43. doi:10.1208/s12249-014-0263-z.
CASGoogle Scholar
30. 30.
Morin G, Briens L. A comparison of granules produced by high-shear and fluidized-bed granulation methods.AAPSPharmSciTech. 2014;15:1039–48. doi:10.1208/s12249-014-0134-7.
CASGoogle Scholar
31. 31.
Yamamoto K, Shao ZJ. Process development and scale-up: fluid-bed granulation. Chap 30. In: Qiu Y, Chen Y,Zhang GGZ, editors. Developing solid oral dosage forms. New York: Academic Press (Elsevier); 2009. p. 701–14.
Google Scholar32. 32.
Box GEP, Hunter JS, Hunter WG. Statistics for experimenters: design, innovation and discovery, 2nd edition,Wiley-Interscience, 2005, 633p.
33. 33.
Convention USP. United States Pharmacopeia XXXI. National Formulary, United States PharmacopeiaConvention, Rockville, 2008.
34. 34.
International Conference on Harmonization Guideline Q8(2) Pharmaceutical development. November 2008.(Accessed 8th Jan 2015).http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/UCM073507.pdf.
35. 35.
Wells JI. Pharmaceutical preformulation: the physicochemical properties of drug substances. West Sussex:Ellis Horwood Ltd. Publ; 1988. p. 227.
Google Scholar36. 36.
Shah RB, Tawakkul M, Khan MA. Comparative evaluation of flow for pharmaceutical powders and granules.AAPSPharmSciTech. 2008;9:250–8. doi:10.1208/s12249-008-9046-8.
CASGoogle Scholar
37. 37.
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 8/17
Amidon GE, Secreast PJ, Mudie D. Particle, powder and compact characterization. Chap 8. In: Qiu Y, Chen Y,Zhang GGZ, editors. Developing solid oral dosage forms. New York: Academic Press (Elsevier); 2009. p. 163–86.
Google Scholar38. 38.
Long M, Chen Y. Dissolution testing of solid products. Chap 14. In: Qiu Y, Chen Y, Zhang GGZ, editors.Developing solid oral dosage forms. New York: Academic Press (Elsevier); 2009. p. 319–40.
Google Scholar39. 39.
Zhou D, Porter WR, Zhang GGZ. Drug stability and degradation studies. Chap 5. In: Qiu Y, Chen Y, ZhangGGZ, editors. Developing solid oral dosage forms. New York: Academic Press (Elsevier); 2009. p. 87–124.
Google Scholar40. 40.
Ip DP, Brenner GS, Stevenson JM, Lindenbaum S, Douglas AW, Klein SD, et al. High resolution spectroscopicevidence and solution calorimetry studies on the polymorphs of enalapril maleate. Int J Pharm. 1986;28:183–91.
CASArticleGoogle Scholar
41. 41.
Pandey P, Hamey R, Bindra DS, Huang Z, Mathias N, Eley T, et al. From bench to humans: formulationdevelopment of poorly water soluble drug to mitigate food effect. AAPSPharmSciTech. 2014;15:407–16.doi:10.1208/S12249-013-0069-4.
CASGoogle Scholar
42. 42.
Sundeep S. Dhareshwar. Case study: enalapril: a prodrug of enalaprilat. In: Prodrugs, Chap 5. Springer Int PublAG. pp 1221–1229. 2007. doi:10.1007/978-0-387-49785-3-39.
43. 43.
Khawam A, Flanagan DR. Solid-state kinetic models: basics and mathematical fundamentals. J Phys Chem B.2006;110:17315–28. doi:10.1021/jp062746a.
CASArticlePubMedGoogle Scholar
44. 44.
Khawam A, Flanagam DR. Basics and applications of solid-state kinetics: a pharmaceutical perspective. JPharm Sci. 2006;95:472–98.
CASArticlePubMedGoogle Scholar
Download references
ACKNOWLEDGMENTS
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 9/17
The financial support from FAPESP (2005/05191-2 and 2011/20872-7), CNPq (PQ-2), CAPES (PhD scholarship toT.F. Guimarães) and FAPEG is gratefully acknowledged. Authors would like to thank Rudolf Barth ElectronMicroscopy Platform of the Oswaldo Cruz Institute/FIOCRUZ for the SEM operation and micrographs.
Author information
Affiliations
1. Fundação Oswaldo Cruz (FIOCRUZ), Farmanguinhos - Manguinhos, Avenida Sizenando Nabuco 100, Rio deJaneiro, RJ, 21045-900, Brazil
Thiago F. Guimarães2. Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Avenida do Café s/n,
14040-903, Ribeirão Preto, SP, BrazilThiago F. Guimarães, Amanda C. C. Comelli & Luís A. P. Freitas
3. Labmaq do Brasil Ltda, Ribeirão Preto, Via Anhanguera km 304, CEP 140140125, SP, BrazilLuciana A. Tacón
4. Faculdade de Farmácia, Universidade Federal de Goiás, Setor Universitário, Goiânia, GO, 74605-220, BrazilTalita A. Cunha & Ricardo N. Marreto
Authors
1. Thiago F. GuimarãesView author publicationsYou can also search for this author in
PubMedGoogle Scholar
2. Amanda C. C. ComelliView author publicationsYou can also search for this author in
PubMedGoogle Scholar
3. Luciana A. TacónView author publicationsYou can also search for this author in
PubMedGoogle Scholar
4. Talita A. CunhaView author publicationsYou can also search for this author in
PubMedGoogle Scholar
5. Ricardo N. MarretoView author publicationsYou can also search for this author in
PubMedGoogle Scholar
6. Luís A. P. FreitasView author publicationsYou can also search for this author in
PubMedGoogle Scholar
Corresponding author
Correspondence to Luís A. P. Freitas.
Rights and permissions
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 10/17
Reprints and Permissions
About this article
Cite this article
Guimarães, T.F., Comelli, A.C.C., Tacón, L.A. et al. Fluidized Bed Hot Melt Granulation with Hydrophilic MaterialsImproves Enalapril Maleate Stability. AAPS PharmSciTech 18, 1302–1310 (2017). https://doi.org/10.1208/s12249-016-0593-0
Download citation
Received: 18 May 2016
Accepted: 18 July 2016
Published: 03 August 2016
Issue Date: May 2017
DOI: https://doi.org/10.1208/s12249-016-0593-0
KEY WORDS
chemical stabilitydegradation kineticsdissolution ratefluid bedtop spray
Access options
Instant access to the full article PDF.
Price includes VAT for Brazil
37,40 €
Buy article PDF
This is the net price. Taxes to be calculated incheckout.
99 €
Buy journal subscription
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 11/17
Immediate online access to all issues from 2019.Subscription will auto renew annually.
Learn more about Institutional subscriptions
SectionsFiguresReferences
AbstractReferencesACKNOWLEDGMENTSAuthor informationRights and permissionsAbout this article
Fig. 1
Fig. 2
Fig. 3
Fig. 4
Fig. 5
Fig. 6
Fig. 7
1. Alsante KM, Huynh-Ba K, Baertschi SW, Reed RA,Landis MS, Kleinman MH, et al. Recent trends inproduct development and regulatory issues onimpurities in active pharmaceutical ingredient (API)and drug products. Part 1: predicting degradationrelated impurities and impurity considerations forpharmaceutical dosage forms. AAPSPharmSciTech.2014;15:198–212. doi:10.1208/s12249-013-0047-x.
Google Scholar
2. Regulska K, Stanisz B, Lisiecki P. Optimization ofstorage and manufacture conditions for imidaprilhydrochloride in solid state as a way to reduce costsof antihypertensive therapy. AAPSPharmSciTech.2013;14:1199–208. doi:10.1208/s12249-013-0010-x.
CASGoogle Scholar
3. McEvoy GK. AHFS Drug information 1999. 40thEdition Revised American Society of Health-SystemPharmacists, February, 1999.
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 12/17
4. Sosnowska K, Winnicka K, Czajkowska-Koanik A.Stability of extemporaneous enalapril maleatesuspensions for pediatric use prepared fromcommercially available tablets. Acta Pol Pharm -Drug Res. 2009;66:321–6.
CASGoogle Scholar
5. Wang SL, Lin SY, Chen TF. Reaction kinetics ofsolid-state cyclization of enalapril maleateinvestigated by isothermal FT-IR microscopic system.Chem Pharm Bull. 2001;49:402–6.
CASArticlePubMedGoogle Scholar
6. Stanisz B. Evaluation of stability of enalapril maleatein solid phase. J Pharm Biomed Anal. 2003;31:375–80.
CASArticlePubMedGoogle Scholar
7. Diego M, Godoy G, Mennickent S, Godoy R.Chemical stability of enalapril maleate drug substanceand tablets by a stability-indicating liquidchromatographic method. Quim Nova. 2011;34:450–4.
ArticleGoogle Scholar
8. Stanisz B. Kinetics of degradation of enalaprilmaleate in dosage forms. Acta Pol Pharm - Drug Res.2004;61:415–8.
CASGoogle Scholar
9. Al-Omari MM, Abdelah MK, Badwan AA, JaberAMY. Effect of the drug-matrix on the stability ofenalapril maleate in tablet formulations. J PharmBiomed Anal. 2001;25:893–902.
CASArticlePubMedGoogle Scholar
10. Lima DM, Santos LD, Lima EM. Stability and invitro release profile of enalapril maleate fromdifferent commercially available tablets: possibletherapeutic implications. J Pharm Biomed Anal.2008;47:934–7.
CASArticlePubMed
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 13/17
Google Scholar
11. Resende RLO, Santoro MIRM, Matos JR. Stabilityand compatibility study on enalapril maleate usingthermoanalytical techniques. J Therm Anal Calorim.2008;93:881–6.
ArticleGoogle Scholar
12. Cotton ML, Wu DW, Vadas EB. Drug-excipientinteraction study of enalapril maleate using thermalanalysis and scanning electron microscopy. Int JPharm. 1987;40:129–42.
CASArticleGoogle Scholar
13. Merslavic SM, Jozica Razen NM, Rotar LR. Stableformulation of enalapril salt, a process for thepreparation thereof and the use thereof. WO Patent.1994.
14. Chen J, Zhang LH, Xu RJ, Bu NJ, Zhang L. Proposalof a new degradation mechanism of enalapril maleateand improvement of enalapril maleate stability intablet formulation with different stabilizers.Pharmazie. 2014;69:277–80.
CASPubMedGoogle Scholar
15. Cunha TA, Serpa RC, Oliveira APM, Nasser LN,Freitas LAP, Taveira SF, et al. Effect of stearic acid onenalapril stability and dissolution frommultiparticulate solid dosage forms.AAPSPharmSciTech. 2013;14:1150–7.
CASGoogle Scholar
16. Oliveira APM, Cunha TA, Serpa RC, Taveira SF,Lima EM, Freitas LAP, et al. Improvement ofenalapril maleate chemical stability by high shearmelting granulation. Pharm Dev Technol.2014;20(08):1002–8.doi:10.3109/10837450.2014.959178.
ArticleGoogle Scholar
17. Zoppi A, Garnero C, Linck YG, Chattah AK, MontiGA, Longhi MR. Enalapril: β-CD complex: stabilityenhancement in solid state. Carbohydr Polym.2011;86:716–21.
CASArticleGoogle Scholar
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 14/17
18. Thomsen R, Rasmussen HB, Linnet K. In vitro drugmetabolism by human carboxylesterase 1: focus onangiotensin-converting enzyme inhibitors. DrugMetab Dispos. 2014;42:126–33.
CASArticlePubMedGoogle Scholar
19. Borini GB, Andrade TC, Freitas LAP. Hot meltgranulation of coarse pharmaceutical powders in aspouted bed. Powder Technol. 2009;189:520–7.
CASArticleGoogle Scholar
20. Rantanen J, Jørgensen A, Räsänen E, Luukkonen P,Airaksinen S, Raiman J, et al. Process analysis offluidized bed granulation. AAPSPharmSciTech.2001;2:13–20. doi:10.1007/BF02830561.
Google Scholar
21. Hu X, Li Y, Zhang E, Wang X, Xing M, Wang Q, etal. Preparation and evaluation of orally disintegratingtablets containing taste-masked microcapsules ofberberine hydrochloride. AAPSPharmSciTech.2013;14:29–37.
CASGoogle Scholar
22. Silva CAM, Taranto OM. Real-time monitoring ofgas–solid fluidized-bed granulation and coatingprocess: evolution of particle size, fluidization regimetransitions, and psychometric parameters. DryingTechnol. 2015;33:1929–48.doi:10.1080/07373937.2015.1076000.
ArticleGoogle Scholar
23. Andrade TC, Martins RM, Freitas LAP. Granulationof indomethacin and a hydrophilic carrier by fluidizedhot melt method: the drug solubility enhancement.Powder Technol. 2015;270:453–60.
CASArticleGoogle Scholar
24. Kowalski J, Kalb O, Joshi YM, Serajuddin ATM.Application of melt granulation technology toenhance stability of a moisture sensitive immediate-release drug product. Int J Pharm. 2009;381:56–61.
CASArticlePubMedGoogle Scholar
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 15/17
25. Walker GM, Holland CR, Ahmad MMN, Craig DQM.Influence of process parameters on fluidized hot meltgranulation and tablet pressing of pharmaceuticalpowders. Chem Eng Sci. 2005;60:3867–77.
CASArticleGoogle Scholar
26. Kotyian PN, Yang D, Kulkarini R. Effect of the meltgranulation technique on the dissolutioncharacteristics of griseofulvin. Int J Pharm.2007;329:72–80.
ArticleGoogle Scholar
27. Jivraj M, Martini LG, Thomson CM. An overview ofthe different excipients useful for the directcompression of tablets. Pharm Sci Technol Today.2000;3:58–63.
CASArticlePubMedGoogle Scholar
28. Kidokoro M, Haramiishi Y, Sagasaki S, Shimizu T,Yamamoto Y. Application of fluidized hot-meltgranulation for the preparation of granules fortableting; properties of granules and tablets preparedby fluidized hot-melt granulation. Drug Dev IndPharm. 2002;28:67–76.
CASArticlePubMedGoogle Scholar
29. Sharma VD, Akocak S, Ilies MA, Fassihi R. Solid-state interactions at the core-coat interface:physicochemical characterization of enteric-coatedomeprazole pellets without a protective sub-coat.AAPSPharmSciTech. 2015;16:934–43.doi:10.1208/s12249-014-0263-z.
CASGoogle Scholar
30. Morin G, Briens L. A comparison of granulesproduced by high-shear and fluidized-bed granulationmethods. AAPSPharmSciTech. 2014;15:1039–48.doi:10.1208/s12249-014-0134-7.
CASGoogle Scholar
31. Yamamoto K, Shao ZJ. Process development andscale-up: fluid-bed granulation. Chap 30. In: Qiu Y,Chen Y, Zhang GGZ, editors. Developing solid oraldosage forms. New York: Academic Press (Elsevier);2009. p. 701–14.
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 16/17
Google Scholar
32. Box GEP, Hunter JS, Hunter WG. Statistics forexperimenters: design, innovation and discovery, 2ndedition, Wiley-Interscience, 2005, 633p.
33. Convention USP. United States Pharmacopeia XXXI.National Formulary, United States PharmacopeiaConvention, Rockville, 2008.
34. International Conference on Harmonization GuidelineQ8(2) Pharmaceutical development. November 2008.(Accessed 8th Jan 2015).http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/UCM073507.pdf.
35. Wells JI. Pharmaceutical preformulation: thephysicochemical properties of drug substances. WestSussex: Ellis Horwood Ltd. Publ; 1988. p. 227.
Google Scholar
36. Shah RB, Tawakkul M, Khan MA. Comparativeevaluation of flow for pharmaceutical powders andgranules. AAPSPharmSciTech. 2008;9:250–8.doi:10.1208/s12249-008-9046-8.
CASGoogle Scholar
37. Amidon GE, Secreast PJ, Mudie D. Particle, powderand compact characterization. Chap 8. In: Qiu Y,Chen Y, Zhang GGZ, editors. Developing solid oraldosage forms. New York: Academic Press (Elsevier);2009. p. 163–86.
Google Scholar
38. Long M, Chen Y. Dissolution testing of solidproducts. Chap 14. In: Qiu Y, Chen Y, Zhang GGZ,editors. Developing solid oral dosage forms. NewYork: Academic Press (Elsevier); 2009. p. 319–40.
Google Scholar
39. Zhou D, Porter WR, Zhang GGZ. Drug stability anddegradation studies. Chap 5. In: Qiu Y, Chen Y,Zhang GGZ, editors. Developing solid oral dosageforms. New York: Academic Press (Elsevier); 2009.p. 87–124.
Google Scholar
40. Ip DP, Brenner GS, Stevenson JM, Lindenbaum S,Douglas AW, Klein SD, et al. High resolutionspectroscopic evidence and solution calorimetrystudies on the polymorphs of enalapril maleate. Int JPharm. 1986;28:183–91.
CASArticleGoogle Scholar
41. Pandey P, Hamey R, Bindra DS, Huang Z, Mathias N,Eley T, et al. From bench to humans: formulation
23/03/2020 Fluidized Bed Hot Melt Granulation with Hydrophilic Materials Improves Enalapril Maleate Stability | SpringerLink
https://link.springer.com/article/10.1208/s12249-016-0593-0 17/17
development of poorly water soluble drug to mitigatefood effect. AAPSPharmSciTech. 2014;15:407–16.doi:10.1208/S12249-013-0069-4.
CASGoogle Scholar
42. Sundeep S. Dhareshwar. Case study: enalapril: aprodrug of enalaprilat. In: Prodrugs, Chap 5. SpringerInt Publ AG. pp 1221–1229. 2007. doi:10.1007/978-0-387-49785-3-39.
43. Khawam A, Flanagan DR. Solid-state kinetic models:basics and mathematical fundamentals. J Phys ChemB. 2006;110:17315–28. doi:10.1021/jp062746a.
CASArticlePubMedGoogle Scholar
44. Khawam A, Flanagam DR. Basics and applications ofsolid-state kinetics: a pharmaceutical perspective. JPharm Sci. 2006;95:472–98.
CASArticlePubMedGoogle Scholar
Over 10 million scientific documents at your fingertips
Switch Edition
Academic EditionCorporate Edition
HomeImpressumLegal informationPrivacy statementHow we use cookiesAccessibilityContact us
Not logged in - 143.208.144.131
Not affiliated
Springer Nature
© 2020 Springer Nature Switzerland AG. Part of Springer Nature.