Tečno-čvrsti sistemi: Ispitivanje uticaja faktora formulacije na optimalno opterećenje tečnošću

  • Ivana Aleksić Univerzitet u Beogradu-Farmaceutski fakultet, Katedra za tehnologiju i kozmetologiju
  • Teodora Glišić Univerzitet u Beogradu - Farmaceutski fakultet, Katedra za farmaceutsku tehnologiju i kozmetologiju
  • Sandra Cvijić Univerzitet u Beogradu - Farmaceutski fakultet, Katedra za farmaceutsku tehnologiju i kozmetologiju
  • Jelena Parojčić Univerzitet u Beogradu-Farmaceutski fakultet, Katedra za farmaceutsku tehnologiju i kozmetologiju
DOI: https://doi.org/10.5937/arhfarm72-33130
Ključne reči: tečno-čvrsti kompakti, tabletabilnost, dinamička analiza kompakcije, Fujicalin®, mikrokristalna celuloza

Sažetak


Tečno-čvrsti sistemi predstavljaju novi pristup izradi čvrstih farmaceutskih oblika koji sadrže tečnu lipofilnu lekovitu supstancu ili rastvor/suspenziju slabo rastvorljive lekovite supstance u pogodnom vehikulumu. Imajući u vidu nedostatak literaturnih podataka o ponašanju tečno-čvrstih sistema pri kompresiji, cilj ovog istraživanja je ispitivanje uticaja opterećenja tečnošću, odnosa nosača i sredstva za oblaganje, kao i vrste nosača (mikrokristalna celuloza i bezvodni kalcijum-hidrogenfosfat sušen raspršivanjem (Fujicalin®)) na protočnost i svojstva tečno-čvrstih sistema pri kompresiji, kao i određivanje optimalnog opterećenja tečnošću. Tečno-čvrste smeše sa Fujicalin®-om su pokazale znatno bolju protočnost nego smeše sa mikrokristalnom celulozom. Uočeno je da se sa povećanjem odnosa nosača i sredstva za oblaganje poboljšava protočnost smeša. Kompakti sa Fujicalin®-om su imali dobra mehanička svojstva do udela od 24,7% tečnosti, a kompakti sa mikrokristalnom celulozom do udela od 16,2% tečnosti. Tečno-čvrsti sistemi sa Fujicalin®-om su pokazali slične profile tabletabilnosti onim sa mikrokristalnom celulozom, uprkos tome što sadrže znatno veći udeo tečnosti. Vrednosti pritiska potrebnog za izbacivanje kompakta iz matrice ukazuju da bi dodatak lubrikansa mogao biti potreban u slučaju tečno-čvrstih sistema sa Fujicalin®-om. Dobijeni rezultati ukazuju na superiorna svojstva Fujicalin®-a kao nosača u tečno-čvrstim tabletama, a dinamička analiza kompakcije može predstavljati koristan alat za procenu ponašanja tečno-čvrstih sistema pri kompresiji.

Reference

Spireas S, Bolton SM. Liquisolid systems and methods for preparing same. United States patent 5,800,834, 1998.

Spireas S. Liquisolid systems and methods for preparing same. United States patent 6,423,339 B1, 2002.

De Espíndola B, Beringhs AOR, Sonaglio D, Stulzer HK, Silva MAS, Ferraz HG, Pezzini BR. Liquisolid pellets: A pharmaceutical technology strategy to improve the dissolution rate of ritonavir. Saudi Pharmaceutical Journal. 2019;27(5):702–712.

Barmpalexis P, Grypioti A, Eleftheriadis GK, Fatouros DG. Development of a new aprepitant liquisolid formulation with the aid of artificial neural networks and genetic programming. AAPS PharmSciTech. 2018;19(2):741–752.

Elkadi S, Elsamaligy S, Al-Suwayeh S, Mahmoud H. The development of self-nanoemulsifying liquisolid tablets to improve the dissolution of simvastatin. AAPS PharmSciTech. 2017;18(7):2586–2597.

Pezzini BR, Beringhs AO, Ferraz HG, Silva MAS, Stulzer HK, Sonaglio D. Liquisolid technology applied to pellets: Evaluation of the feasibility and dissolution performance using felodipine as a model drug. Chem Eng Res Des. 2016;110:62–9.

Gong W, Wang Y, Sun L, Yang J, Shan L, Yang M, Gao C. Development of itraconazole liquisolid compact: Effect of polyvinylpyrrolidone on the dissolution properties. Curr Drug Deliv. 2016;13(3):452–461.

Hentzschel CM, Alnaief M, Smirnova I, Sakmann A, Leopold CS. Enhancement of griseofulvin release from liquisolid compacts. Eur J Pharm Biopharm. 2012;80:130-5.

Jhaveri M, Nair AB, Shah J, Jacob S, Patel V, Mehta T. Improvement of oral bioavailability of carvedilol by liquisolid compact: optimization and pharmacokinetic study. Drug Delivery and Translational Research. 2020;10(4):975–985.

Sheta NM, Elfeky YA, Boshra SA. Cardioprotective efficacy of silymarin liquisolid in isoproterenol prompted myocardial infarction in rats. AAPS PharmSciTech. 2020;21:81.

Patel K, Doddapaneni R, Patki M, Sekar V, Bagde A, Singh M. Erlotinib-valproic acid liquisolid formulation: evaluating oral bioavailability and cytotoxicity in erlotinib-resistant non-small cell lung cancer cells. AAPS PharmSciTech. 2019;20:135.

Jyoti J, Anandhakrishnan NK, Singh SK, Kumar B, Gulati M, Gowthamarajan K, et. al. A three-pronged formulation approach to improve oral bioavailability and therapeutic efficacy of two lipophilic drugs with gastric lability. Drug Deliv and Transl Res. 2019;9:848–865.

Bonthagarala B, Dasari V, Kotra V, Swain S, Beg S. Quality-by-Design based development and characterization of pioglitazone loaded liquisolid compact tablets with improved biopharmaceutical attributes. J Drug Deliv Sci Technol. 2019;51: 345–355.

Khames A. Investigation of the effect of solubility increase at the main absorption site on bioavailability of BCS class II drug (risperidone) using liquisolid technique. Drug Deliv. 2017;24(1):328–338.

Khames A. Formulation and characterization of eplerenone nanoemulsion liquisolids, an oral delivery system with higher release rate and improved bioavailability. Pharmaceutics. 2019;11(1):40.

Nokhodchi A, Hentzschel CM, Leopold CS. Drug release from liquisolid systems: speed it up, slow it down. Expert Opinion on Drug Delivery. 2011;8(2):191–205.

Spireas S, Jarowski C, Rohera B. Powdered solution technology: principles and mechanism. Pharm Res. 1992;9(10):1351-8.

Vranikova B, Gajdziok J, Vetchy D. Determination of flowable liquid retention potential of aluminometasilicate carrier for liquisolid systems preparation. Pharm Dev Technol. 2015;20:839–844.

Vranikova B, Gajdziok J. Evaluation of sorptive properties of various carriers and coating materials for liquisolid systems. Acta Ploniae Pharmaceutica – Drug Research. 2015;72(3):539-549.

Komala DR, Janga KY, Jukanti R, Bandary S. Competence of raloxifene hydrochloride loaded liquisolid compacts for improved dissolution and intestinal permeation. J Drug Deliv Sci Technol. 2015;30:232-241.

Anzilaggo D, Beringhs AO, Pezzini BR, Sonaglioa D, Stulzera HK. Liquisolid systems: Understanding the impact of drug state (solution or dispersion), nonvolatile solvent and coating material on simvastatin apparent aqueous solubility and flowability. Colloids Surf B Biointerfaces. 2019;175:36–43.

Badawy МА, Kamel АО, Sammour ОА. Use of biorelevant media for assessment of a poorly soluble weakly basic drug in the form of liquisolid compacts: in vitro and in vivo study. Drug Delivery. 2016;23(3):818–827.

Kurek M, Woyna-Orlewicz K, Khalid MH, Jachowicz R. Optimization of furosemide liquisolid tablets preparation process leading to their mass and size reduction. Acta Poloniae Pharmaceutica – Drug Research. 2016;73(5):1325–1331.

Lu M, Xing H, Yang T, Yu J, Yang Z, Sun Y, Ding P. Dissolution enhancement of tadalafil by liquisolid technique. Pharm Dev Technol. 2017;22:77–89.

Jaipakdee N, Limpongsa E, Sripanidkulchai B, Piyachaturawat P. Preparation of Curcuma comosa tablets using liquisolid techniques: In vitro and in vivo evaluation. Int J Pharm. 2018;553:157–168.

Jadhav NR, Irny PV, Patil US. Solid state behavior of progesterone and its release from Neusilin US2 based liquisolid compacts. J Drug Deliv Sci Technol. 2017;38: 97–106.

Aleksić I, German Ilić I, Cvijić S, Parojčić J. An Investigation into the Influence of Process Parameters and Formulation Variables on Compaction Properties of Liquisolid Systems. AAPS PharmSciTech. 2020;21(7):242.

Fuji Chemical Industry Co., Ltd., Brochure: The unique DCPA Fujicalin®; c2021 [cited 2021 Feb 20]. Available from: http://www.fujichemical.co.jp/english/medical/medicine/fujicalin/index.html

Fell JT, Newton JM. Determination of tablet strength by the diametral-compression test. J Pharm Sci. 1970;59:688–691.

Armstrong NA, Haines-Nutt RF. Elastic recovery and surface area changes in compacted powder systems. J Pharm Pharmacol. 1972;24:135–136.

Hentzschel CM, Sakmann A, Leopold CS. Suitability of various excipients as carrier and coating materials for liquisolid compacts. Drug Dev Ind Pharm. 2011; 37(10):1200–1207.

European Pharmacopoeia 10th edition, Strasbourg: Council of Europe; 2019.

Thoorens G, Krier F, Leclercq B, Carlin B, Evrard B. Microcrystalline cellulose, a direct compression binder in a quality by design environment—A review. Int J Pharm. 2014;473:64–72.

McCormick D. Evolutions in direct compression. Pharmaceutical Technology. 2005;17(4):52–62.

Ragnarsson G. Force–displacement and network measurements. In: Alderborn G, Nystrom C, editors. Pharmaceutical Powder Compaction Technology. New York: Marcel Dekker In; 1996; p. 77–97.

Pitt KG, Webber RJ, Hill KA, Dey D, Gamlen MJ. Compression prediction accuracy from small scale compaction studies to production presses. Powder Technology. 2015;270:490-3.

Objavljeno
2022/02/19
Broj časopisa
Vol. 72 Br. Notebook 1 (2022): Arhiv za farmaciju
Rubrika
Originalni naučni rad
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