Dissolution enhancement and physicochemical characterization of fenofibric acid in surface solid dispersion with croscarmellose sodium

Dissolution enhancement and physicochemical characterization of fenofibric acid in surface solid dispersion with croscarmellose sodium

The dissolution enhancement of the water-insoluble drug fenofibric acid (FA) was conducted by the surface solid dispersion (SSD) technique with croscarmellose sodium (CS) as a carrier. The SSD formulations of FA were prepared by the solvent evaporation method in three different drug-to-carrier weight ratios, evaluated for the dissolutions, and compared to the physical mixtures (PMs). The optimum SSD formulation and its corresponding PM were characterized by Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (PXRD), Differential Thermal Analysis (DTA), and Fourier Transform Infrared Spectroscopy (FTIR) and were compressed into tablets to evaluate the dissolution after compression. The best dissolution was obtained from the SSD 1:1. The recrystallization of FA in the SSD preparation could change the crystal habit of FA and deposited it on the surface of CS. İn addition, there was no chemical interaction observable between both FA and CS in the SSD formulation. No chemical interaction between FA and CS in the SSD. However, a slight reduction was noticed in the crystallinity of FA if compared to that of the pure drug. This study showed that the SSD formulation had the best dissolution compared to the PM, the conventional direct compression, and the reference formulation of FA in its commercial tablets. The SSD preparation with CS could enhance the dissolution of FA from its tablet dosage form.

___

  • Alagona P. Fenofibric acid: A new fibrate approved for use in combination with statin for the treatment of mixed dyslipidemia. Vasc Health Risk Manag. 2010; 6(1): 351-362.
  • Ling H, Luoma JT, Hilleman D. A review of currently available fenofibrate and fenofibric acid formulations. Cardiol Res. 2013; 4(2): 47-55. [CrossRef]
  • Keating GM, Croom KF. Fenofibrate: A review of its use in primary dyslipidaemia, the metabolic syndrome and type 2 diabetes mellitus. Drugs. 2007; 67(1): 121-153. [CrossRef]
  • Davidson MH, Armani A, McKenney JM, Jacobson TA. Safety considerations with fibrate therapy. Am J Cardiol. 2007; 99(6): 3C-18C. [CrossRef]
  • Bays HE, Roth EM, McKenney JM, Kelly MT, Thakker KM, Setze CM, Obermeyer K, Sleep DJ. The effects of fenofibric acid alone and with statins on the prevalence of metabolic syndrome and its diagnostic components in patients with mixed dyslipidemia. Diabetes Care 2010; 33(9): 2113-2116. [CrossRef]
  • Moutzouri E, Kei A, Elisaf MS, Milionis HJ. Management of dyslipidemias with fibrates, alone and in combination with statins: Role of delayed-release fenofibric acid. Vasc Health Risk Manag. 2010; 6(1): 525-539.[CrossRef]
  • Rath NP, Haq W, Balendiran GK. Fenofibric acid. Acta Crystallogr Sect C Cryst Struct Commun. 2005; 61(2): 81-84. [CrossRef]
  • Zhu T, Ansquer JC, Kelly MT, Sleep DJ, Pradhan RS. Comparison of the gastrointestinal absorption and bioavailability of fenofibrate and fenofibric acid in humans. J Clin Pharmacol. 2010; 50(8): 914-921. [CrossRef]
  • Kim KS, Kim JH, Jin SG,Kim DW, Kim DS, Kim JO. Effect of magnesium carbonate on the solubility, dissolution and oral bioavailability of fenofibric acid powder as an alkalising solubilizer. Arch Pharm Res. 2016; 39(4): 531-538. [CrossRef]
  • Kim KS, Jin SG, Mustapha O, Yousaf AM, Kim DW, Kim YH, Kim JO. Novel fenofibric acid-loaded controlled release pellet bioequivalent to choline fenofibrate-loaded commercial product in beagle dogs. Int J Pharm. 2015; 490(1-2): 273-280. [CrossRef]
  • 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): 1068-1075. [CrossRef]
  • Kawabata Y, Wada K, Nakatani M, Yamada S, Onoue S. Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: Basic approaches and practical applications. Int J Pharm. 2011; 420(1): 110. [CrossRef]
  • Vo CL-N, Park C, Lee B-J. Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs. Eur J Pharm Biopharm. 2013; 85(3): 799-813. [CrossRef]
  • Charumanee S, Okonoki S, Sirithunyalug J. Improvement of the dissolution rate of piroxicam by surface solid dispersion. CMU J. 2004; 3(2): 77-84.
  • Pamudji JS, Wikarsa S, Tampara MH. Improvement of gliclazide’s dissolution rate by using surface solid dispersion with avicel PH 101. Int J Pharm Pharm Sci. 2014; 6(11): 461-465.
  • Khatry S, Sood N, Arora S. Surface solid dispersion – a review. Int J Pharm Sci Nanotechnol. 2013; 6(1): 1915-1924.
  • Jain S, Sandhu P, Gurjar M, Malvi R. Solubility enhancement by solvent deposition technique: An overview. Asian J Pharm Clin Res. 2012; 5(4): 15-19.
  • Zhao N, Augsburger LL. Functionality comparison of 3 classes of superdisintegrants in promoting aspirin tablet disintegration and dissolution. AAPS PharmSciTech. 2005; 6(4): E634-640. [CrossRef]
  • Sun T, Hall ML, Isbester PK, Whiteheat BR. Fenofibric acid polymorph; methods of making; and methods of use thereof. United States Patent Application Publication no US 2009/0187040 A1. 2009, July 23.
  • Dixit RP, Nagarsenker MS. In vitro and in vivo advantage of celecoxib surface solid dispersion and dosage form development. Indian J Pharm Sci. 2007; 69(3): 370 – 377.
  • Williams AC, Timmins P, Lu M, Forbes RT. Disorder and dissolution enhancement: Deposition of ibuprofen on to insoluble polymers. Eur J Pharm Sci. 2005; 26(3–4): 288–294. [CrossRef]
  • Kiran T, Shastri N, Ramakrishna S, Sadanandam M. Surface solid dispersion of glimepiride for enhancement of dissolution rate. Int J PharmTech Res. 2009; 1(3): 822-831.
  • 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): 472-477. [CrossRef]
  • Castro SG, Ramirez-Rigo MV, Allemandi DA, Palma SD. New binary solid dispersion of indomethacin and crosscarmellose sodium: physical characterization and in vitro dissolution enhancement. J Excip Food Chem. 2012; 3(4): 121-128.
  • Sharma S, Sher P, Badve S, Pawar AP. Adsorption of meloxicam on porous calcium silicate: characterization and tablet formulation. AAPS PharmSciTech. 2005; 6(4): E618-625. [CrossRef]
  • Rao M, Mandage Y, Thanki K, Bhise S. Dissolution improvement of simvastatin by surface solid dispersion technology. Dissolution Technol. 2010; 17(2): 27-34. [CrossRef]
  • Godfrey AR, DiGiacinto J, Davis MW. Single-dose bioequivalence of 105-mg fenofibric acid tablets versus 145-mg fenofibrate tablets under fasting and fed conditions: a report of two phase i, open-label, single-dose, randomized, crossover clinical trials. Clin Ther. 2011; 33(6): 766-775.[CrossRef]
  • Niraimathi V, Suresh AJ, Alageswaran A. UV spectrophotometric determination of fenofibric acid by using hydrotropy. Int J Pharma Sci Res. 2015; 6(2): 451-458
Journal of research in pharmacy (online)-Cover
  • Yayın Aralığı: Yılda 6 Sayı
  • Yayıncı: Marmara Üniversitesi
Sayıdaki Diğer Makaleler

Patient counseling, risk factors and comorbidity assessment in diabetic foot ulcer

Smithamol SUNNY, Anita ANN SUNNY, Rama PARTHASARATHY, Shanmugasundaram RAJESHKUMAR, Swathy PRADEEP

Anti-inflammatory properties of the ruthenium polypyridyl complex, K314, on the in vitro activated macrophages

Furkan AYAZ

Scylla serrata Forskal as natural source of glucosamine hydrochloride

Muammar FAWWAZ, Indah MUTMAINNAH, Muzakkir BAITS, Pipin VEMILIA

Oxoaporphine alkaloids from the barks of Platymitra siamensis Craib (Annonaceae) and their cytotoxicity against MCF-7 cancer cell line

Saripah Salbiah SYED ABDUL AZZIZ, Mohamad Syahrizal AHMAD, Yumi Zuhanis Has-Yun HASHIM, Phirdaous ABBAS, Mohd Azlan NAFIAH, Shieh Ting KAN, Yuhanis MHD BAKRI, Khalijah AWANG

Peruvian pharmacist employment and wage: Gender, university and type of job influences

Alfredo OYOLA, Josefa PARI, Pompeyo CUBA, Luzmila HERNANDEZ, Melisa QUISPE, Luz CHACALTANA, Juana LA ROSA

Zingiber officinale mitigates diazinon-induced testicular toxicity via suppression of oxidative stress and apoptosis in mice model

Abbasali KARIMPOUR, Maedeh HAMZEH, Saeed YAGHUBİ BEKLER, Fereshteh TALEBPOUR AMİRİ

Synthesis, characterization and antitubercular evaluation of some new isoxazole appended 1-carboxamido-4,5- dihydro-1H-pyrazoles

Kishor PALLEAPATI, Afzal Basha SHAIK, Venkataramana KALIKIVAYI

In vitro bioavailability studies on phytochemical profile and antioxidant activity potential of Clematis viticella L.

Esra ACAR ŞAH, Engin CELEP, Erdem YEŞİLADA

The percentage of depressive symptoms in patients with type 2 Diabetes Mellitus in M Djamil General Hospital Padang, Indonesia

Dwisari DILLASAMOLA, Alexander KAM, Eva DECROLİ

Water fraction of Sonchus arvensis (Linn.) leaves protects heart upon isoproterenol-induced myocardial infarction in rats and promotes survival of cardiomyocytes in vitro

Neng Fisheri KURNIATI, Yasushi FUJIO, Rahmayati RUSNEDY, Dhyan Kusuma ATUNINGTYAS, Nova SULISKA, Elin Yulinah SUKANDAR