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Development a taste-masked acetaminophen solid dispersions using Eudragit® E100 polymer by solvent evaporation technique

Yıl 2023, Cilt: 27 Sayı: 5, 1998 - 2006, 28.06.2025

Sally Shahoud Wassim Abdelwahed Tamim Hammad

Öz

The bitter taste of acetaminophen greatly reduced its formulation in oral dosage forms, so masking the taste was tested using the solid dispersion technique by Eudragit E100 and the solvent evaporation method. The obtained solid dispersions were characterized by FT-IR and DSC. Then, production yield, and drug loading have been determined, and the efficiency of this technique in taste masking by in vitro-in vivo evaluation were investigated by measuring the amount of drug released at pH=6.8 similar to saliva and pH=1.2 similar to stomach. FT-IR demonstrated that absence of interactions between drug and polymer and DSC results showed the complete formation of solid dispersion for F2 and partial formation with F1 and F3. Production yield was more than 96% for all formulations, and drug loading ranged between 99-103% and this increased with special dishes, while in vitro drug release results at pH=1.2 after 15min reached 84.95±0.55,100.89±0.70, and 95.78±0.71 (μg/ml) for F1, F2, and F3 respectively. In another hand, taste-masking evaluation at pH=6.8 showed drug release amount after 2min less than the determination bitterness threshold (900μg/ml) there were 114.98,75.97, and 10.26 μg/ml for F1, F2, and F3 respectively. Therefore, this technique is considered efficient in masking the taste with obtaining a good production yield.

Anahtar Kelimeler

Acetaminophen taste-masking solid dispersion Eudragit E100 solvent evaporation threshold bitterness

Kaynakça

  • [1] Hansen TG, O’Brien K, Morton NS, Rasmussen SN. Plasma paracetamol concentrations and pharmacokinetic following rectal administration in neonates and young infants. Acta Anaesthesiologica Scandinavica. 1999; 43(8): 855-59. https://doi.org/10.1034/j.1399-6576.1999.430813.x
  • [2] Suzuki H, Onishi H, Hisamatsu S, Masuda K, Takahashi Y, Iwata M, Machida Y. Acetaminophen-containing chewable tablets with suppressed bitterness and improved oral feeling. International journal of Pharmaceutics. 2004; 278(1): 51–61. https://doi.org/10.1016/j.ijpharm.2004.02.031
  • [3] Zheng JY, Keeney MP. Taste masking analysis in pharmaceutical formulation development using an electronic tongue. International journal of Pharmaceutics. 2006; 310(1-2): 118–24. https://doi.org/10.1016/j.ijpharm.2005.11.046
  • [4] Udaykumar M, Nageswarao ABN, Kumar VTVS, Giri VV. Fast Dissolving Tablets: New Fangled Drug Delivery System, A Comprehensive Review. International Journal of Research in Drug Delivery. 2012; 2(3): 15-18.
  • [5] WHO. Toolkit for Research and Development of Paediatric Antiretroviral Drugs and Formulations 2018. http://www.who.int/publications/i/item/9789241514361 , (assessed on 30 June 2018).
  • [6] Walsh J, Cram A, Woertz K, Breitkreutz J, Winzenburg G, Turner R, Tuleu C. Playing hide and seek with poorly tasting paediatric medicines: Do not forget the excipients. Advanced Drug Delivery Reviews. 2014; 73: 14-33. https://doi.org/10.1016/j.addr.2014.02.012
  • [7] Sohi H, Sultana Y, Khar RK. Taste masking technologies in oral pharmaceuticals: recent developments and approaches. Drug Development and Industrial Pharmacy. 2004; 30(5): 429-48. https://doi.org/10.1081/ddc-120037477
  • [8] Chiou WL, Riegelman S. Pharmaceutical Applications of Solid Dispersion Systems. Journal of Pharmaceutical Sciences. 1971; 60(9): 1281-1302. https://doi.org/10.1002/jps.2600600902
  • [9] Sekiguchi K, Obi N. Studies on absorption of eutectic mixture. I. A comparison of the behavior of eutectic mixture of sulfathiazole and ordinary sulfathiazole in man. Chemical and Pharmaceutical Bulletin. 1961; 9(11): 866-72.
  • [10] Bindhani S, Mohapata S. Recent approaches of solid dispersion: a new concept towards oral bioavailability. Asian Journal of Pharmaceutical Clincal Research. 2018; 11(3): 72-8.
  • [11] Yi EJ, Kim JY, Rhee YS, Kim SH, Lee HJ, Park CW, Park ES. Preparation of sildenafil citrate microcapsules and in vitro/in vivo evaluation of taste masking efficiency. International Journal of Pharmaceutics. 2014; 466(1-2): 286-95. https://doi.org/10.1016/j.ijpharm.2014.03.001
  • [12] Kulkarni M, Vishwakarma B, Sen S, Anupuram S, Date AA. Development and evaluation of taste masked dry syrup formulation of potassium chloride. American Association of Pharmaceutical Scientists. 2019; 5(1): 1-10. https://doi.org/10.1186/s41120-019-0030-z
  • [13] Brniak W, Maslak E, Jachowicz R. Orodispersible films and tablets with prednisolone microparticles. European Journal of Pharmaceutical Sciences. 2015; 75: 81-90. https://doi.org/10.1016/j.ejps.2015.04.006
  • [14] Shishu, Kamalpreet, Kapoor VR. Development of Taste Masked Oral Formulation of Ornidazole. Indian Journal of Pharmaceutical Sciences. 2010; 72(2): 211-15. https://doi.org/10.4103/0250-474x.65018
  • [15] Jafari E. Preparation, Characterization and Dissolution of Solid Dispersion of Diclofenac Sodium Using Eudragit E-100. Journal of Applied Pharmaceutical Science. 2013; 3(8): 167-70.
  • [16] Al-Kasmi B, Alsirawan MHDB, Paradkar A, Nattouf AH, El-Zein H. Aqueous and pH dependent coacervation method for taste masking of paracetamol via amorphous solid dispersion Formation. Scientific Reports Natural Journal. 2021; 11(8907): 1-11. https://doi.org/10.1038/s41598-021-88312-6
  • [17] Medarevic D, Cvijic S, Dobricic V, Mitric M, Duris J, Ibric S. Assessing the potential of solid dispersions to improve dissolution rate and bioavailability of valsartan: In vitro-in silico approach. European Journal of pharmaceutical sciences. 2018; 124: 188-98. http://doi.org/10.1016/j.ejps.2018.08.026
  • [18] Sharma G, Pawar VK, Garg G, Awasthi R, Kulkarni GT. Taste masking of Promethazine Hydrochloride using Eudragit E100 via solid dispersion technique to develop fast disintegrating tablets. Der Pharmacia Lettre. 2010; 2(3): 83-94.
  • [19] Shiino K, Iwao Y, Miyagishima A, Itai S. Optimization of a novel wax matrix system using aminoalkyl methacrylate copolymer E and ethylcellulose to suppress the bitter taste of acetaminophen. International Journal of Pharmaceutics. 2010; 395: 71–7. http://doi.org/10.1016%2Fj.ijpharm.2010.05.007
  • [20] Albertini B, Cavallari C, Passarini N, Voinovich D, González-Rodriguez ML, Magarotto L, Rodriguez L. Characterization and taste-masking evaluation of acetaminophen granules: comparison between different preparation methods in a high-shear mixer. European Journal of Pharmaceutical Sciences. 2004; 21(2-3): 295–303. https://doi.org/10.1016/j.ejps.2003.10.017
  • [21] Sharma D, Chopra R, Bedi N. Development and evaluation of paracetamol taste masked orally disintegrating tablets using polymer coating technique. International Journal of Pharmaceutical Science. 2012; 3: 129–34.
  • [22] Mamdouh MAA, Badawi AA, Sakaran WS, Elshafeey AH, Elnahas. Different Solid Dispersion Techniques for Dissolution Enhancement Using Paracetamol as a Model Drug. International Journal of Pharmaceutical Phytopharmacol Research. 2015; 4(4): 231-37.
  • [23] Akiladevi D, Basak S. Dissolution enhancement of paracetamol by solid dispersion technique. Journal of Pharmaceutical Research. 2010; 2(12): 2846–49.
  • [24] Khan S, Kataria P, Nakhat P, Yeole P. Taste masking of Ondansetron hydrochloride by polymer carrier system and formulation of rapid-disintegrating tablets. American Association of Pharmaceutical Scientists Pharmaceutical Sciences of Technology. 2007; 8(2): 127-33. https://doi.org/10.1208/pt0802046
  • [25] Al-kasmi B, Al Rahal O, El-zein H, Nattouf A. Structural and in vitro in vivo evaluation for taste masking. Expert Opinion of Drug Delivery. 2018; 15(11): 1105-16. https://doi.org/10.1080/17425247.2018.1535590

Yıl 2023, Cilt: 27 Sayı: 5, 1998 - 2006, 28.06.2025

Sally Shahoud Wassim Abdelwahed Tamim Hammad

Öz

Kaynakça

  • [1] Hansen TG, O’Brien K, Morton NS, Rasmussen SN. Plasma paracetamol concentrations and pharmacokinetic following rectal administration in neonates and young infants. Acta Anaesthesiologica Scandinavica. 1999; 43(8): 855-59. https://doi.org/10.1034/j.1399-6576.1999.430813.x
  • [2] Suzuki H, Onishi H, Hisamatsu S, Masuda K, Takahashi Y, Iwata M, Machida Y. Acetaminophen-containing chewable tablets with suppressed bitterness and improved oral feeling. International journal of Pharmaceutics. 2004; 278(1): 51–61. https://doi.org/10.1016/j.ijpharm.2004.02.031
  • [3] Zheng JY, Keeney MP. Taste masking analysis in pharmaceutical formulation development using an electronic tongue. International journal of Pharmaceutics. 2006; 310(1-2): 118–24. https://doi.org/10.1016/j.ijpharm.2005.11.046
  • [4] Udaykumar M, Nageswarao ABN, Kumar VTVS, Giri VV. Fast Dissolving Tablets: New Fangled Drug Delivery System, A Comprehensive Review. International Journal of Research in Drug Delivery. 2012; 2(3): 15-18.
  • [5] WHO. Toolkit for Research and Development of Paediatric Antiretroviral Drugs and Formulations 2018. http://www.who.int/publications/i/item/9789241514361 , (assessed on 30 June 2018).
  • [6] Walsh J, Cram A, Woertz K, Breitkreutz J, Winzenburg G, Turner R, Tuleu C. Playing hide and seek with poorly tasting paediatric medicines: Do not forget the excipients. Advanced Drug Delivery Reviews. 2014; 73: 14-33. https://doi.org/10.1016/j.addr.2014.02.012
  • [7] Sohi H, Sultana Y, Khar RK. Taste masking technologies in oral pharmaceuticals: recent developments and approaches. Drug Development and Industrial Pharmacy. 2004; 30(5): 429-48. https://doi.org/10.1081/ddc-120037477
  • [8] Chiou WL, Riegelman S. Pharmaceutical Applications of Solid Dispersion Systems. Journal of Pharmaceutical Sciences. 1971; 60(9): 1281-1302. https://doi.org/10.1002/jps.2600600902
  • [9] Sekiguchi K, Obi N. Studies on absorption of eutectic mixture. I. A comparison of the behavior of eutectic mixture of sulfathiazole and ordinary sulfathiazole in man. Chemical and Pharmaceutical Bulletin. 1961; 9(11): 866-72.
  • [10] Bindhani S, Mohapata S. Recent approaches of solid dispersion: a new concept towards oral bioavailability. Asian Journal of Pharmaceutical Clincal Research. 2018; 11(3): 72-8.
  • [11] Yi EJ, Kim JY, Rhee YS, Kim SH, Lee HJ, Park CW, Park ES. Preparation of sildenafil citrate microcapsules and in vitro/in vivo evaluation of taste masking efficiency. International Journal of Pharmaceutics. 2014; 466(1-2): 286-95. https://doi.org/10.1016/j.ijpharm.2014.03.001
  • [12] Kulkarni M, Vishwakarma B, Sen S, Anupuram S, Date AA. Development and evaluation of taste masked dry syrup formulation of potassium chloride. American Association of Pharmaceutical Scientists. 2019; 5(1): 1-10. https://doi.org/10.1186/s41120-019-0030-z
  • [13] Brniak W, Maslak E, Jachowicz R. Orodispersible films and tablets with prednisolone microparticles. European Journal of Pharmaceutical Sciences. 2015; 75: 81-90. https://doi.org/10.1016/j.ejps.2015.04.006
  • [14] Shishu, Kamalpreet, Kapoor VR. Development of Taste Masked Oral Formulation of Ornidazole. Indian Journal of Pharmaceutical Sciences. 2010; 72(2): 211-15. https://doi.org/10.4103/0250-474x.65018
  • [15] Jafari E. Preparation, Characterization and Dissolution of Solid Dispersion of Diclofenac Sodium Using Eudragit E-100. Journal of Applied Pharmaceutical Science. 2013; 3(8): 167-70.
  • [16] Al-Kasmi B, Alsirawan MHDB, Paradkar A, Nattouf AH, El-Zein H. Aqueous and pH dependent coacervation method for taste masking of paracetamol via amorphous solid dispersion Formation. Scientific Reports Natural Journal. 2021; 11(8907): 1-11. https://doi.org/10.1038/s41598-021-88312-6
  • [17] Medarevic D, Cvijic S, Dobricic V, Mitric M, Duris J, Ibric S. Assessing the potential of solid dispersions to improve dissolution rate and bioavailability of valsartan: In vitro-in silico approach. European Journal of pharmaceutical sciences. 2018; 124: 188-98. http://doi.org/10.1016/j.ejps.2018.08.026
  • [18] Sharma G, Pawar VK, Garg G, Awasthi R, Kulkarni GT. Taste masking of Promethazine Hydrochloride using Eudragit E100 via solid dispersion technique to develop fast disintegrating tablets. Der Pharmacia Lettre. 2010; 2(3): 83-94.
  • [19] Shiino K, Iwao Y, Miyagishima A, Itai S. Optimization of a novel wax matrix system using aminoalkyl methacrylate copolymer E and ethylcellulose to suppress the bitter taste of acetaminophen. International Journal of Pharmaceutics. 2010; 395: 71–7. http://doi.org/10.1016%2Fj.ijpharm.2010.05.007
  • [20] Albertini B, Cavallari C, Passarini N, Voinovich D, González-Rodriguez ML, Magarotto L, Rodriguez L. Characterization and taste-masking evaluation of acetaminophen granules: comparison between different preparation methods in a high-shear mixer. European Journal of Pharmaceutical Sciences. 2004; 21(2-3): 295–303. https://doi.org/10.1016/j.ejps.2003.10.017
  • [21] Sharma D, Chopra R, Bedi N. Development and evaluation of paracetamol taste masked orally disintegrating tablets using polymer coating technique. International Journal of Pharmaceutical Science. 2012; 3: 129–34.
  • [22] Mamdouh MAA, Badawi AA, Sakaran WS, Elshafeey AH, Elnahas. Different Solid Dispersion Techniques for Dissolution Enhancement Using Paracetamol as a Model Drug. International Journal of Pharmaceutical Phytopharmacol Research. 2015; 4(4): 231-37.
  • [23] Akiladevi D, Basak S. Dissolution enhancement of paracetamol by solid dispersion technique. Journal of Pharmaceutical Research. 2010; 2(12): 2846–49.
  • [24] Khan S, Kataria P, Nakhat P, Yeole P. Taste masking of Ondansetron hydrochloride by polymer carrier system and formulation of rapid-disintegrating tablets. American Association of Pharmaceutical Scientists Pharmaceutical Sciences of Technology. 2007; 8(2): 127-33. https://doi.org/10.1208/pt0802046
  • [25] Al-kasmi B, Al Rahal O, El-zein H, Nattouf A. Structural and in vitro in vivo evaluation for taste masking. Expert Opinion of Drug Delivery. 2018; 15(11): 1105-16. https://doi.org/10.1080/17425247.2018.1535590
Toplam 25 adet kaynakça vardır.

Ayrıntılar

Birincil Dil İngilizce
Konular Eczacılık ve İlaç Bilimleri (Diğer)
Bölüm Articles
Yazarlar

Sally Shahoud 0000-0001-9753-1606

Wassim Abdelwahed 0000-0002-6353-8831

Tamim Hammad 0000-0001-5234-1817

Yayımlanma Tarihi 28 Haziran 2025
Yayımlandığı Sayı Yıl 2023 Cilt: 27 Sayı: 5

Kaynak Göster

APA Shahoud, S., Abdelwahed, W., & Hammad, T. (2025). Development a taste-masked acetaminophen solid dispersions using Eudragit® E100 polymer by solvent evaporation technique. Journal of Research in Pharmacy, 27(5), 1998-2006.
AMA Shahoud S, Abdelwahed W, Hammad T. Development a taste-masked acetaminophen solid dispersions using Eudragit® E100 polymer by solvent evaporation technique. J. Res. Pharm. Temmuz 2025;27(5):1998-2006.
Chicago Shahoud, Sally, Wassim Abdelwahed, ve Tamim Hammad. “Development a Taste-Masked Acetaminophen Solid Dispersions Using Eudragit® E100 Polymer by Solvent Evaporation Technique”. Journal of Research in Pharmacy 27, sy. 5 (Temmuz 2025): 1998-2006.
EndNote Shahoud S, Abdelwahed W, Hammad T (01 Temmuz 2025) Development a taste-masked acetaminophen solid dispersions using Eudragit® E100 polymer by solvent evaporation technique. Journal of Research in Pharmacy 27 5 1998–2006.
IEEE S. Shahoud, W. Abdelwahed, ve T. Hammad, “Development a taste-masked acetaminophen solid dispersions using Eudragit® E100 polymer by solvent evaporation technique”, J. Res. Pharm., c. 27, sy. 5, ss. 1998–2006, 2025.
ISNAD Shahoud, Sally vd. “Development a Taste-Masked Acetaminophen Solid Dispersions Using Eudragit® E100 Polymer by Solvent Evaporation Technique”. Journal of Research in Pharmacy 27/5 (Temmuz 2025), 1998-2006.
JAMA Shahoud S, Abdelwahed W, Hammad T. Development a taste-masked acetaminophen solid dispersions using Eudragit® E100 polymer by solvent evaporation technique. J. Res. Pharm. 2025;27:1998–2006.
MLA Shahoud, Sally vd. “Development a Taste-Masked Acetaminophen Solid Dispersions Using Eudragit® E100 Polymer by Solvent Evaporation Technique”. Journal of Research in Pharmacy, c. 27, sy. 5, 2025, ss. 1998-06.
Vancouver Shahoud S, Abdelwahed W, Hammad T. Development a taste-masked acetaminophen solid dispersions using Eudragit® E100 polymer by solvent evaporation technique. J. Res. Pharm. 2025;27(5):1998-2006.