• MOHAMED EL-NABARAWI Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt https://orcid.org/0000-0003-0070-1969
  • DOAA AHMED ELSETOUHY Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt
  • REHAB ABDELMONEM Department of Industrial Pharmacy, Faculty of Pharmacy, Misr University for Science and Technology, 6th of October City, Egypt https://orcid.org/0000-0002-2522-8082
  • AMR EL-HOSSEINI Department of Research and Development, Sedico Pharmaceutical Co., 6th of October City, Egypt




Loratadine, Solid dispersion, Surface solid dispersion, Hydrophilic carriers, On-surface carriers, Dissolution improvement, Co-processed excipient


Objective: The aim of the work in this study is to enhance the dissolution rate of the poorly water-soluble drug; loratadine employing co-precipitated surface solid dispersions (SSDs) prepared using various hydrophilic on-surface carriers namely; Pearlitol® flash, Parteck® ODT, Prosolv® ODT G2 and Pharmaburst® C1.

Methods: Loratadine solid dispersions (SDs) were prepared by co-precipitation method using copovidone, poloxamer 188 and gluconolactone at different ratios. The best formulae were selected, based on dissolution results obtained, to prepare 16 different SSDs. The prepared SSDs were subjected to drug content and in-vitro dissolution studies and the best formulae were further subjected to solid-state characterization, using X-ray powder diffraction (XRPD) and differential scanning calorimeter (DSC). The effect of aging on the best formulae was studied by evaluating the drug content, drug dissolution and the change in the crystalline state using (XRPD).

Results: S1 formula, containing drug: poloxamer 188: pearlitol flash at 1:4:1 ratio, and S9 formula, containing drug: poloxamer 188: prosolv ODT at 1:4:1 ratio showed the highest dissolution efficiency. XRPD and DSC studies of S1 and S9 proved a decrease in drug crystallinity and confirmed solid dispersion formation. The stability study of S1 and S9 showed a slight reduction in the dissolution efficiency (DE) of S1 (from 84.6±0.8 to 81.4±0.7 and 81.4±1.3 at ambient and accelerated conditions, respectively) and a higher reduction in DE of S9 (from 83.5±2.4 to 69.6±1.0 and 57.3±2.9 at ambient and accelerated conditions respectively).

Conclusion: Results obtained obviously confirmed the potential effect of the surface solid dispersion technique, using poloxamer 188 as a hydrophilic carrier and Pearlitol flash as an on-surface carrier, on improving the dissolution of loratadine.


Download data is not yet available.


Li H, Tan Y, Yang L, Gao L, Wang T, Yang X. Dissolution evaluation in vitro and bioavailability in vivo of self-microemulsifying drug delivery systems for pH-sensitive drug loratadine. J Microencapsul. 2015;32(2):175-80. doi: 10.3109/02652048.2014.985340, PMID 25413271.

Kaur L, Kaur T, Singh AP, Singh AP. “Formulation development and solubility enhancement of rosuvastatin calcium by using hydrophilic polymers and solid dispersion method”. Int J Curr Pharm Sci 2021;13(6):50-5. doi: 10.22159/ ijcpr.2021v13i6.1910.

Vasconcelos T, Sarmento B, Costa P. Solid dispersions as strategy to improve oral bioavailability of poor water-soluble drugs. Drug Discov Today. 2007;12(23-24):1068-75. Epub 20071030. doi: 10.1016/j.drudis.2007.09.005. PMID 18061887.

Abd-El Bary A, Louis D, Sayed S. Olmesartan medoxomil surface solid dispersion-based orodispersible tablets: formulation and in vitro characterization. J Drug Delivery Sci Technol. 2014;24(6):665-72. doi: 10.1016/s1773-2247(14)50134-7. PMID: WOS:000350263400016.

Essa EA, Dwaikat M. Enhancement of Simvastatin dissolution by solid surface dispersion: effect of carriers and wetting agents. J Appl Pharm Sci 2015;58:46-53. doi: 10.7324/ JAPS.2015.54.S8.

Chaturvedi M, Kumar M, Pathak K, Bhatt S, Saini V. Surface solid dispersion and solid dispersion of meloxicam: comparison and product development. Adv Pharm Bull. 2017;7(4):569-77. Epub 20171231. doi: 10.15171/apb.2017.068, PMID 29399546, PMCID PMC5788211.

Meka AK, Pola S, Tupally KR, Abbaraju PL. Development, evaluation and characterization of solid surface dispersion for solubility and dissolution enhancement of irbesartan. Int J Drug Dev Res. 2012;4(1):263-73.

Elbary AA, Salem H, Maher M. ’In vitro and in vivo’ evaluation of glibenclamide using solid surface dispersion (SSD) approach. Br J Pharmacol Toxicol. 2011;2(1):51-62.

Essa EA. Enhancement of carvedilol dissolution; solid surface dispersion versus solid dispersion. Asian J Pharm. 2015;9(4):283-9. PMID PubMed PMID. WOS. 000374582500008.

Pamudji JS, Wikarsa S, Tampara MH. Improvement of gliclazide’s dissolution rate by using solid surface dispersion with avicel PH 101. Int J Pharm Pharm Sci. 2014;6(11):461-5.

Lalitha Y, Lakshmi P. Enhancement of dissolution of nifedipine by surface solid dispersion technique. Int J Pharm Pharm Sci. 2011;3(3):41-6.

Patel B, Parikh RH, Swarnkar D. Enhancement of dissolution of telmisartan through use of solid dispersion technique–surface solid dispersion. J Pharm Bioallied Sci. 2012;4Suppl 1:S64-8. doi: 10.4103/0975-7406.94142, PMID 23066211, PMCID PMC3467836.

Singh D, Pathak K. Hydrogen bond replacement-unearthing a novel molecular mechanism of solid surface dispersion for enhanced solubility of a drug for veterinary use. Int J Pharm. 2013;441(1-2):99-110. doi: . PMID 23261857.

Chanda R, Nallaguntla L. Formulation and evaluation of medicated lozenges for sore throat. Asian J Pharm Clin Res. 2020;13(10):62-7. doi: 10.22159/ajpcr.2020.v13i10.38660.

Loratadine. In: British Pharmacopoeia. London: TSO; 2016.

Moffat AC, Osselton MD, Widdop B, Watts J. Clarke’s analysis of drugs and poisons. London: Pharmaceutical Press; 2005.

Nokhodchi A, Al-Hamidi H, Antonijevic MD, Owusu Ware S, Kaialy W. Dissolution and solid state behaviours of carbamazepine-gluconolactone solid dispersion powders: the potential use of gluconolactone as dissolution enhancer. Chem Eng Res Des. 2015;100:452-66. doi: 10.1016/j.cherd.2015.04.018. PMID PubMed. WOS. 000359956900040.

Uniformity of dosage units. In: United States Pharmacopeia and national formulary (USP 40-NF 35). Rockville, MD: the United States pharmacopeial convention; 2017.

de Oliveira MA, Yoshida MI, Silva DC. Quality evaluation of pharmaceutical formulations containing hydrochlorothiazide. Molecules. 2014;19(10):16824-36. Epub 20141020. doi: 10.3390/molecules191016824, PMID 25335110, PMCID PMC6271651.

Zhang Y, Huo M, Zhou J, Zou A, Li W, Yao C. DD Solver: an add-in program for modeling and comparison of drug dissolution profiles. AAPS J. 2010;12(3):263-71. Epub 20100406. doi: 10.1208/s12248-010-9185-1, PMID 20373062, PMCID PMC2895453.

Ryan JA. Compressed pellet X-ray diffraction monitoring for optimization of crystallinity in lyophilized solids: imipenem: cilastatin sodium case. J Pharm Sci. 1986;75(8):805-7. doi: 10.1002/jps.2600750817, PMID 3464737.

Moore JW, Flanner HH. Mathematical comparison of dissolution profiles. Pharm Technol. 1996;20:64-74.

Polli JE, Rekhi GS, Augsburger LL, Shah VP. Methods to compare dissolution profiles and a rationale for wide dissolution specifications for metoprolol tartrate tablets. J Pharm Sci. 1997;86(6):690-700. doi: 10.1021/js960473x.

Lomuscio S, Ma H, Matchett MA, Sandhu HK, Shah NH, Zhang YE, Inventors. Assignee. Pharmaceutical composition with improved bioavailability. Hoffmann Roche. Patent WO2014114575; 2014.

Langham ZA, Booth J, Hughes LP, Reynolds GK, Wren SA. Mechanistic insights into the dissolution of spray-dried amorphous solid dispersions. J Pharm Sci. 2012;101(8):2798-810. Epub 20120516. doi: 10.1002/jps.23192, PMID 22592919.

Ajay S, Harita D, Tarique M, Amin P. Solubility and dissolution rate enhancement of curcumin using Kollidon VA64 by solid dispersion technique. Int J Pharm Tech Res. 2012;4:1055-64.

Homayouni A, Sadeghi F, Nokhodchi A, Varshosaz J, Garekani HA. Preparation and characterization of celecoxib solid dispersions; comparison of poloxamer-188 and PVP-K30 as carriers. Iran J Basic Med Sci. 2014;17(5):322-31. PMID 24967060, PMCID PMC4069839.

Zhai X, Li C, Lenon GB, Xue CCL, Li W. Preparation and characterisation of solid dispersions of tanshinone IIA, cryptotanshinone and total tanshinones. Asian J Pharm Sci. 2017;12(1):85-97. doi: . PMID 32104317, PMCID PMC7032082.

Taniguchi C, Kawabata Y, Wada K, Yamada S, Onoue S. Microenvironmental pH-modification to improve dissolution behavior and oral absorption for drugs with pH-dependent solubility. Expert Opin Drug Deliv. 2014;11(4):505-16. Epub 20140128. doi: 10.1517/17425247.2014.881798, PMID 24472170.

Damour D, François A, Lefevre P, Chesnoy S, Neves S. Optimising excipient properties for ODT formulation; 2015. Available from: https://www.pharmaexcipients.com/news/optimising-excipient-properties-for-odt-formulation-whitepaper-roquette/.roquette. [Last accessed on 28 Jul 2022]

Maulvi FA, Dalwadi SJ, Thakkar VT, Soni TG, Gohel MC, Gandhi TR. Improvement of dissolution rate of aceclofenac by solid dispersion technique. Powder Technol. 2011;207(1-3):47-54. doi: 10.1016/j.powtec.2010.10.009.

Alam A. Formulation of solid dispersion and surface solid dispersion of nifedipine: a comparative study. Afr J Pharm Pharmacol. 2013;7(25):1707-18. doi: 10.5897/AJPP12.1180.

Comoglu T, Inal O, Kargili A, Pehlivanoglu B. Formulation, in vitro and in vivo evaluation of taste masked rasagiline orally fast disintegrating tablets (ODTS). Res Rev J Pharm Pharm Sci. 2017;6(2):27-38.

Ganapuram BR, Alle M, Dadigala R, Kotu GM, Guttena V. Development, evaluation and characterization of surface solid dispersion for solubility and dispersion enhancement of irbesartan. J Pharm Res. 2013;7(6):472-7. doi: 10.1016/ j.jopr.2013.06.012.

Fathima N, Mamatha T, Qureshi HK, Anitha N, Rao JV. Drug-excipient interaction and its importance in dosage form development. J Appl Pharm Sci. 2011;1(06):66-71.

Steele DF, Edge S, Tobyn MJ, Moreton RC, Staniforth JN. Adsorption of an amine drug onto microcrystalline cellulose and silicified microcrystalline cellulose samples. Drug Dev Ind Pharm. 2003;29(4):475-87. doi: 10.1081/ddc-120018382, PMID 12737540.

Daraghmeh N, Chowdhry BZ, Leharne SA, Al Omari MM, Badwan AA. Co-processed chitin-mannitol as a new excipient for oro-dispersible tablets. Mar Drugs. 2015;13(4):1739-64. Epub 20150330. doi: 10.3390/md13041739, PMID 25830680, PMCID PMC4413185.

Gondane P, Sapkal NP, Jaiswal N. Synthesis and evaluation of taste-masked ionic liquid salts of loratadine. Int J Pharm Pharm Sci. 2020;12(11):71-9. doi: 10.22159/ijpps. 2020v12i11.38965.

Verma S, Singh SK, Verma PRP. Solidified SNEDDS of loratadine: formulation using hydrophilic and hydrophobic grades of Aerosil®, pharmacokinetic evaluations and in vivo–in silico predictions using GastroPlus™. RSC Adv. 2016;6(4):3099-116. doi: 10.1039/C5RA21796B.

Mansury MA, Jatav RK, Jatav RK. Determination and identification of loratadine by various analytical methods using UV-visible, FT-IR, and HPLC chromatographic techniques. Indo Am J Pharm Res. 2015;5(9):2899-909.

El-Badry M, Hassan MA, Ibrahim MA, Elsaghir H. Performance of poloxamer 407 as the hydrophilic carrier on the binary mixtures with nimesulide. Farmacia. 2013;61(6):1137-50.

Loratadine. In: United States Pharmacopeia and national formulary (USP 40-NF 35). Rockville, MD: the United States pharmacopeial convention; 2017.

Collett J. Poloxamer. In: Rowe RC, Sheskey PJ, Quinn ME, editors. Handbook of pharmaceutical excipients. London: Pharmaceutical Press; 2009. p. 506-9.

Mannitol. In: United States Pharmacopeia and national formulary (USP 40-NF 35). Rockville, MD: United States pharmacopeial convention; 2017.

Yamashita K, Nakate T, Okimoto K, Ohike A, Tokunaga Y, Ibuki R. Establishment of new preparation method for solid dispersion formulation of tacrolimus. Int J Pharm. 2003;267(1-2):79-91. doi: 10.1016/j.ijpharm.2003.07.010. PMID 14602386.

Weerapol Y, Limmatvapirat S, Nunthanid J, Konthong S, Suttiruengwong S, Sriamornsak P. Development and characterization of nifedipine-amino methacrylate copolymer solid dispersion powders with various adsorbents. Asian J Pharm Sci. 2017;12(4):335-43. Epub 20170118. doi: 10.1016/j.ajps.2017.01.002. PMID 32104344, PMCID PMC7032161.

ICH guidelines. (R2): stability testing of new drug substances and products. Q1A. ICH; 2003.

Kanaujia P, Lau G, Ng WK, Widjaja E, Schreyer M, Hanefeld A. Investigating the effect of moisture protection on solid-state stability and dissolution of fenofibrate and ketoconazole solid dispersions using PXRD, HSDSC and Raman microscopy. Drug Dev Ind Pharm. 2011;37(9):1026-35. Epub 20110321. doi: 10.3109/03639045.2011.558091, PMID 21417604.



How to Cite




Original Article(s)

Most read articles by the same author(s)