Araştırma Makalesi
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Yıl 2025, Cilt: 29 Sayı: 4, 1437 - 1450, 05.07.2025

Ali Mohammed Hussein Ghaidaa Hameed , Fitua M. Aziz

https://doi.org/10.12991/jrespharm.1734450

Öz

Kaynakça

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Improve the solubility of cefpodoxime proxetil by amorphous solid dispersion technique

Yıl 2025, Cilt: 29 Sayı: 4, 1437 - 1450, 05.07.2025

Ali Mohammed Hussein Ghaidaa Hameed , Fitua M. Aziz

https://doi.org/10.12991/jrespharm.1734450

Öz

This research aimed to improve the solubility and stabilize cefpodoxime proxetil (CP), a class IV drug, by amorphous solid dispersion (ASD) technique. Four formulations were prepared by dispersing amorphous CP in soluplus, polyvinylpyrrolidone (PVP K30), and ethyl cellulose (EC) blends in different compositions and ratios. The optimum formulation was stored in accelerated conditions at 40 °C and 75% relative humidity for six months. The drug's solubility and dissolution rate in different systems were explored. Furthermore, Differential Scanning Calorimetry (DSC), X-ray Powder Diffractometry (PXRD), Fourier Transform Infrared spectroscopy (FTIR), and Field Emission Scanning Electron Microscopy (FESEM) were used to examine the physical state of the drug. The antibacterial activity of the drug was evaluated during the experiment. When mixing CP with soluplus and PVP K30 in a 1:1:1 ratio as ASD, the drug solubility at pH 1.2 enhanced about 28 folds than a pure drug, and the dissolution rate increment was observed. The DSC, FTIR, and PXRD data confirmed the drug is amorphous and miscible with these polymers. FESEM revealed particle size reduction. The antibacterial activity was raised. After storage in the accelerated condition, physical investigations indicated that no recrystallization occurred, and this condition had little effect on in vitro drug dissolution and antibacterial activity. This can be a good indicator of the drug's solubility enhancement and physical stability optimization that will make the possibility of preparing this drug in the future as an oral solid dosage form with the possibility of manufacturing with a drug company due to the promising results.

Anahtar Kelimeler

Amorphous solid dispersion (ASD) technique cefpodoxime proxetil physical stability solubility

Kaynakça

  • [1] Solomon S, Iqbal J, Albadarin AB. Insights into the ameliorating ability of mesoporous silica in modulating drug release in ternary amorphous solid dispersion prepared by hot melt extrusion. Eur J Pharm Biopharm. 2021;165:244-258. https://doi.org/10.1016/j.ejpb.2021.04.017
  • [2] Pignatello R, Corsaro R, Bonaccorso A, Zingale E, Carbone C, Musumeci T. Soluplus® polymeric nanomicelles improve solubility of BCS-class II drugs. Drug Deliv Transl Res. 2022;12(8):1991-2006. https://doi.org/10.1007/s13346-022-01182-x
  • [3] Han R, Xiong H, Ye Z, Yang Y, Huang T, Jing Q, Lu J, Pan H, Ren F, Ouyang D. Predicting physical stability of solid dispersions by machine learning techniques. J Control Release. 2019;311:16-25. https://doi.org/10.1016/j.jconrel.2019.08.030
  • [4] Kim J-S, Park H, Kang K-T, Ha E-S, Kim M-S, Hwang S-J. Micronization of a poorly water-soluble drug, fenofibrate, via supercritical-fluid-assisted spray-drying. J Pharm Investig. 2022;52(3):353-366. http://dx.doi.org/10.1007/s40005-022-00565-z
  • [5] Quan W, Kong S, Ouyang Q, Tao J, Lu S, Huang Y, Li S, Luo H. Use of 18ƒÀ-glycyrrhetinic acid nanocrystals to enhance anti-inflammatory activity by improving topical delivery. Colloids Surf B Biointerfaces. 2021;205:111791. https://doi.org/10.1016/j.colsurfb.2021.111791
  • [6] Tekade AR, Yadav JN. A review on solid dispersion and carriers used therein for solubility enhancement of poorly water soluble drugs. Adv Pharm Bull. 2020;10(3):359-369. https://doi.org/10.34172%2Fapb.2020.044
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  • [9] Bansal SS, Kaushal AM, Bansal AK. Enthalpy relaxation studies of two structurally related amorphous drugs and their binary dispersions. Drug Dev Ind Pharm. 2010;36(11):1271-1280. https://doi.org/10.3109/03639041003753847
  • [10] Czajkowski M, Jacobsen A-C, Bauer-Brandl A, Brandl M, Skupin-Mrugalska P. Hydrogenated phospholipid, a promising excipient in amorphous solid dispersions of fenofibrate for oral delivery: Preparation and in-vitro biopharmaceutical characterization. Int J Pharm. 2023; 644:123294. https://doi.org/10.1016/j.ijpharm.2023.123294
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  • [12] Lust A, Strachan CJ, Veski P, Aaltonen J, Heinamaki J, Yliruusi J, Kogermann K. Amorphous solid dispersions of piroxicam and SoluplusR: Qualitative and quantitative analysis of piroxicam recrystallization during storage. Int J Pharm. 2015;486(1-2):306-314. https://doi.org/10.1016/j.ijpharm.2015.03.079
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  • [16] Luebbert C, Wessner M, Sadowski G. Mutual impact of phase separation/crystallization and water sorption in amorphous solid dispersions. Mol Pharm. 2018;15(2):669-678. https://doi.org/10.1021/acs.molpharmaceut.7b01076
  • [17] Zeng A, Yao X, Gui Y, Li Y, Jones KJ, Yu L. Inhibiting surface crystallization and improving dissolution of amorphous loratadine by dextran sulfate nanocoating. J Pharm Sci. 2019;108(7):2391-2396. https://doi.org/10.1016/j.xphs.2019.02.018
  • [18] Bhujbal SV, Mitra B, Jain U, Gong Y, Agrawal A, Karki S, Taylor LS, Kumar S, Tony Zhou Q. Pharmaceutical amorphous solid dispersion: A review of manufacturing strategies. Acta Pharm Sin B. 2021;11(8):2505-2536. https://doi.org/10.1016%2Fj.apsb.2021.05.014
  • [19] Mendonsa N, Almutairy B, Kallakunta VR, Sarabu S, Thipsay P, Bandari S, Repka MA. Manufacturing strategies to develop amorphous solid dispersions: An overview. J Drug Deliv Sci Technol. 2020;55:101459. https://doi.org/10.1016%2Fj.jddst.2019.101459
  • [20] Saha SK, Joshi A, Singh R, Jana S, Dubey K. An investigation into solubility and dissolution improvement of alectinib hydrochloride as a third-generation amorphous solid dispersion. J Drug Deliv Sci Technol. 2023;81:104259. http://dx.doi.org/10.1016/j.jddst.2023.104259
  • [21] Singh A, Van den Mooter G. Spray drying formulation of amorphous solid dispersions. Adv Drug Del Rev. 2016;100:27-50. https://doi.org/10.1016/j.addr.2015.12.010 [22] Mishra DK, Dhote V, Bhargava A, Jain DK, Mishra PK. Amorphous solid dispersion technique for improved drug delivery: Basics to clinical applications. Drug Deliv Transl Res. 2015;5:552-565. https://doi.org/10.1007/s13346-015-0256-9
  • [23] Shi X, Xu T, Huang W, Fan B, Sheng X. Stability and bioavailability enhancement of telmisartan ternary solid dispersions: the synergistic effect of polymers and drug-polymer (s) interactions. AAPS PharmSciTech. 2019;20(4):143. https://doi.org/10.1208/s12249-019-1358-3
  • [24] Thompson SA, Davis Jr DA, Miller DA, Kucera SU, Williams III RO. Pre-processing a polymer blend into a polymer alloy by KinetiSol enables increased ivacaftor amorphous solid dispersion drug loading and dissolution. Biomedicines. 2023;11(5):1281. https://doi.org/10.3390/biomedicines11051281
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Toplam 63 adet kaynakça vardır.

Ayrıntılar

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

Ali Mohammed Hussein

Ghaidaa Hameed

Fitua M. Aziz

Yayımlanma Tarihi 5 Temmuz 2025
Gönderilme Tarihi 15 Temmuz 2024
Kabul Tarihi 20 Ağustos 2024
Yayımlandığı Sayı Yıl 2025 Cilt: 29 Sayı: 4

Kaynak Göster

APA Hussein, A. M., Hameed, G., & M. Aziz, F. (2025). Improve the solubility of cefpodoxime proxetil by amorphous solid dispersion technique. Journal of Research in Pharmacy, 29(4), 1437-1450. https://doi.org/10.12991/jrespharm.1734450
AMA Hussein AM, Hameed G, M. Aziz F. Improve the solubility of cefpodoxime proxetil by amorphous solid dispersion technique. J. Res. Pharm. Temmuz 2025;29(4):1437-1450. doi:10.12991/jrespharm.1734450
Chicago Hussein, Ali Mohammed, Ghaidaa Hameed, ve Fitua M. Aziz. “Improve the Solubility of Cefpodoxime Proxetil by Amorphous Solid Dispersion Technique”. Journal of Research in Pharmacy 29, sy. 4 (Temmuz 2025): 1437-50. https://doi.org/10.12991/jrespharm.1734450.
EndNote Hussein AM, Hameed G, M. Aziz F (01 Temmuz 2025) Improve the solubility of cefpodoxime proxetil by amorphous solid dispersion technique. Journal of Research in Pharmacy 29 4 1437–1450.
IEEE A. M. Hussein, G. Hameed, ve F. M. Aziz, “Improve the solubility of cefpodoxime proxetil by amorphous solid dispersion technique”, J. Res. Pharm., c. 29, sy. 4, ss. 1437–1450, 2025, doi: 10.12991/jrespharm.1734450.
ISNAD Hussein, Ali Mohammed vd. “Improve the Solubility of Cefpodoxime Proxetil by Amorphous Solid Dispersion Technique”. Journal of Research in Pharmacy 29/4 (Temmuz 2025), 1437-1450. https://doi.org/10.12991/jrespharm.1734450.
JAMA Hussein AM, Hameed G, M. Aziz F. Improve the solubility of cefpodoxime proxetil by amorphous solid dispersion technique. J. Res. Pharm. 2025;29:1437–1450.
MLA Hussein, Ali Mohammed vd. “Improve the Solubility of Cefpodoxime Proxetil by Amorphous Solid Dispersion Technique”. Journal of Research in Pharmacy, c. 29, sy. 4, 2025, ss. 1437-50, doi:10.12991/jrespharm.1734450.
Vancouver Hussein AM, Hameed G, M. Aziz F. Improve the solubility of cefpodoxime proxetil by amorphous solid dispersion technique. J. Res. Pharm. 2025;29(4):1437-50.