326
Views
10
CrossRef citations to date
0
Altmetric
Research Article

Physiological parameters of the gastrointestinal fluid impact the dissolution behavior of the BCS class IIa drug valsartan

ORCID Icon
Pages 1168-1176 | Received 24 Apr 2018, Accepted 05 Oct 2018, Published online: 07 Dec 2018

References

  • Ansari M, Kazemipour M, Talebnia J. 2004. The development and validation of a dissolution method for clomipramine solid dosage forms. Dissolut Technol. 11:16–24.
  • Asare-Addo K, Conway BR, Larhrib H, Levina M, Rajabi-Siahboomi AR, Tetteh J, Boateng J, Nokhodchi A. 2013. The effect of pH and ionic strength of dissolution media on in-vitro release of two model drugs of different solubilities from HPMC matrices. Colloid Surf B. 111:384–391.
  • Bergström CAS, Holm R, Jørgensen SA, Andersson SBE, Artursson P, Beato S, Borde A, Box K, Brewster M, Dressman J, et al. 2014. Early pharmaceutical profiling to predict oral drug absorption: current status and unmet needs. Eur J Pharm Sci. 57:173–199.
  • Chioléro A, Burnier M. 1998. Pharmacology of valsartan, an angiotensin II receptor antagonist. Expert Opin Investig Drugs. 7:1915–1925.
  • Costa P, Manuel J, Lobo S. 2001. Modeling and comparison of dissolution profiles. Eur J Pharm Sci. 13:123–133.
  • Criscione L, Bradley WA, Bühlmayer P, Whitebread S, Glazer R, Lloyd P, Mueller P, Gasparo M. 1995. Valsartan: preclinical and clinical profile of an antihypertensive angiotensin‐II antagonist. Cardiovasc Drug Rev. 13:230–250.
  • Cristofoletti R, Dressman JB. 2016. Matching phosphate and maleate buffer systems for dissolution of weak acids: equivalence in terms of buffer capacity of bulk solution or surface pH? Eur J Pharm Biopharm. 103:104–108.
  • Dressman JB, Amidon GL, Reppas C, Shah VP. 1998. Dissolution testing as a prognostic tool for oral drug absorption: immediate release dosage forms. Pharm Res. 15:11–22.
  • Galia E, Nicolaides E, Hörter D, Löbenberg R, Reppas C, Dressman J. 1998. Evaluation of various dissolution media for predicting in vivo performance of class I and II drugs. Pharm Res. 15:698–705.
  • Garbacz G, Kołodziej B, Koziolek M, Weitschies W, Klein S. 2014. A dynamic system for the simulation of fasting luminal pH-gradients using hydrogen carbonate buffers for dissolution testing of ionisable compounds. Eur J Pharm Sci. 51:224–231.
  • Gu CH, Rao D, Gandhi RB, Hilden J, Raghavan K. 2005. Using a novel multicompartment dissolution system to predict the effect of gastric pH on the oral absorption of weak bases with poor intrinsic solubility. J Pharm Sci. 94:199–208.
  • Hamed R, AlJanabi R, Sunoqrot S, Abbas A. 2017. The effect of pH, buffer capacity, and ionic strength on quetiapine fumarate release from matrix tablets prepared using two different polymeric blends. Drug Dev Ind Pharm. 43:1330–1342.
  • Hamed R, Alnadi SH. 2018. Transfer behavior of the weakly acidic BCS class II drug valsartan from the stomach to the small intestine during fasted and fed states. AAPS PharmSciTech. 19:2213–2225.
  • Hamed R, Awadallah A, Sunoqrot S, Tarawneh O, Nazzal S, AlBaraghthi T, Al Sayyad J, Abbas A. 2016. pH-dependent solubility and dissolution behavior of carvedilol – case example of a weakly basic BCS class II drug. AAPS PharmSciTech. 17:418–426.
  • Jantratid E, Janssen N, Reppas C, Dressman JB. 2008. Dissolution media simulating conditions in the proximal human gastrointestinal tract: an update. Pharm Res. 25:1663–1676.
  • Johnson J, Holinej J, Williams M. 1993. Influence of ionic strength on matrix integrity and drug release from hydroxypropyl cellulose compacts. Int J Pharm. 90:151–159.
  • Johnson JL, Holinej J, Williams MD. 1993. Influence of ionic-strength on matrix integrity and drug release from hydroxypropyl cellulose compacts. Int J Pharm. 90:151–159.
  • Kalantzi L, Goumas K, Kalioras V, Abrahamsson B, Dressman JB, Reppas C. 2006. Characterization of the human upper gastrointestinal contents under conditions simulating bioavailability/bioequivalence studies. Pharm Res. 23:165–176.
  • Klein S, Rudolph M, Dressman J. 2002. Drug release characteristics of different mesalazine products using USP apparatus 3 to simulate passage through the GI tract. Dissolut Technol. 9:6–12.
  • Klein S, Wempe MF, Zoeller T, Buchanan NL, Lambert JL, Ramsey MG, Edgar KJ, Buchanan CM. 2009. Improving glyburide solubility and dissolution by complexation with hydroxybutenyl-beta-cyclodextrin. J Pharm Pharmacol. 61:23–30.
  • Klein S. 2010. The use of biorelevant dissolution media to forecast the in vivo performance of a drug. AAPS J. 12:397–406.
  • Kostewicz ES, Wunderlich M, Brauns U, Becker R, Bock T, Dressman JB. 2004. Predicting the precipitation of poorly soluble weak bases upon entry in the small intestine. J Pharm Pharmacol. 56:43–51.
  • Krieg BJ, Taghavi SM, Amidon GL, Amidon GE. 2015. In vivo predictive dissolution: comparing the effect of bicarbonate and phosphate buffer on the dissolution of weak acids and weak bases. J Pharm Sci. 104:2894–2904.
  • Lindahl A, Ungell AL, Knutson L, Lennernas H. 1997. Characterization of fluids from the stomach and proximal jejunum in men and women. Pharm Res. 14:497–502.
  • Marques MRC, Loebenberg R, Almukainzi M. 2011. Simulated biological fluids with possible application in dissolution testing. Dissolut Technol. 18:15–28.
  • Ozturk SS, Palsson BO, Dressman JB. 1988. Dissolution of ionizable drugs in buffered and unbuffered solutions. Pharm Res. 05:272–282.
  • Pradhan R, Kim SY, Yong CS, Kim JO. 2016. Preparation and characterization of spray-dried valsartan-loaded Eudragit® E PO solid dispersion microparticles. Asian J Pharm Sci. 11:744–750.
  • Prior A, Frutos P, Correa C, editors. 2010. Comparison of dissolution profiles: current guidelines. VI Congreso SEFIG y.
  • Sa‘ib JK. 2015. Titrimetric study of the solubility and dissociation of benzoic acid in water: effect of ionic strength and temperature. Am J Analyt Chem. 6:429.
  • Sheng JJ, Kasim NA, Chandrasekharan R, Amidon GL. 2006. Solubilization and dissolution of insoluble weak acid, ketoprofen: effects of pH combined with surfactant. Eur J Pharm Sci. 29:306–314.
  • Tsume Y, Langguth P, Garcia-Arieta A, Amidon GL. 2012. In silico prediction of drug dissolution and absorption with variation in intestinal pH for BCS class II weak acid drugs: ibuprofen and ketoprofen. Biopharm Drug Dispos. 33:366–377.
  • Tsume Y, Mudie DM, Langguth P, Amidon GE, Amidon GL. 2014. The Biopharmaceutics Classification System: subclasses for in vivo predictive dissolution (IPD) methodology and IVIVC. Eur J Pharm Sci. 57:152–163.
  • Van Den Abeele J, Brouwers J, Mattheus R, Tack J, Augustijns P. 2016. Gastrointestinal behavior of weakly acidic BCS class II drugs in man-case study of diclofenac potassium. J Pharm Sci. 105:687–696.
  • Vertzoni M, Dressman J, Butler J, Hempenstall J, Reppas C. 2005. Simulation of fasting gastric conditions and its importance for the in vivo dissolution of lipophilic compounds. Eur J Pharm Biopharm. 60:413–417.
  • Vidyadhara S, Viswanadh K, Shetiya P, Ramu A, Sasidhar RL. 2015. Development and characterization of a novel nanosuspension based drug delivery system of valsartan: a poorly soluble drug. Asian J Pharm. 9:29–34.
  • Wei H, Löbenberg R. 2006. Biorelevant dissolution media as a predictive tool for glyburide a class II drug. Eur J Pharm Sci. 29:45–52.
  • Xu W-J, Xie H-J, Cao Q-R, Shi L-L, Cao Y, Zhu X-Y, Cui J-H. 2016. Enhanced dissolution and oral bioavailability of valsartan solid dispersions prepared by a freeze-drying technique using hydrophilic polymers. Drug Deliv. 23:41–48.
  • Zhou Z, Dunn C, Khadra I, Wilson CG, Halbert GW. 2017. Statistical investigation of simulated fed intestinal media composition on the equilibrium solubility of oral drugs. Eur J Pharm Sci. 99:95–104.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.