Development and validation of a dissolution method for a BCS class IV drug – tadalafil

Francine Regina Zachow Philippsen, Brunna Ricci Falcão, Letícia de Melo Teixeira, Tiago Rafael Sausen

Abstract


The present study describes the development and validation of a dissolution method for tadalafil, a Biopharmaceutical Classification System class II drug. 0.1 N hydrochloric acid (HCl)+0.5% sodium lauryl sulphate (SLS), pH 4.5-acetate buffer+0.5% SLS and pH 6.8–phosphate buffer+0.5% SLS were tested as dissolution medium, and influences of apparatus, and rotation speed were evaluated. Samples were analyzed by UV spectrophotometric method at 225 nm. The results also shows a better dissolution profile using pH 6.8–phosphate buffer + 0.5% SLS as medium and paddle as apparatus is a speed of 100 rpm.  The conditions that allowed dissolution determination were USP type II apparatus at 100 rpm, containing 900 mL of pH 6.8–phosphate buffer+0.5% SLS as dissolution medium, with analysis at wavelength of 225 nm. Samples were analyzed by UV spectrophotometric method and validated as per ICH guidelines, showing specificity, linearity, precision and accuracy.


Keywords


Dissolution; BCS Class IV drug; Validation

Full Text:

PDF

References


Dissolution Testing of Immediate Release Solid Oral Dosage Forms; Guidance for Industry; U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research (CDER), U.S. Government Printing Office: Washington, DC, 1997.

Brasil. Agência Nacional de Vigilância Sanitária. Resolução no. 31, de 11 de agosto de 2010.

Dressman, JB.; Amidon, GL.; Reppas, C.; Shah, VP. Dissolution testing as a prognostic tool for oral drug absorption: immediate release dosage forms. Pharm. Res., 1998, 15 (1), 11–22.

Emani, J. In vitro - In vivo Correlation: From Theory to Applications. J. Pharm. Pharmaceut. Sci., 2006, 9(2), 169–189.

Farmacopéia Brasileira (2010). 5. ed. Brasília, DF: ANVISA.

Ansari, M; Kazemipour, M.; Talebnia, J. The Development and Validation of a Dissolution Method for Clomipramine Solid Dosage Forms. Dissol. Technology. 2004, 11 (3), 16–24.

Brasil. Agência Nacional de Vigilância Sanitária. Resolução Específica nº 899, de 29 de maio de 2003.

International Conference on Harmonization of Technical Requirements for Registration of Pharmaceuticals for Human Use: Guideline on Validation of Analytical Procedures Q2 (R1). ICH Harmonized Tripartite Guideline: Geneva, Switzerland, 2005

Analytical Procedures and Methods Validation for Drugs and Biologics. Guidance for Industry. U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research (CDER), U.S. Government Printing Office: Washington, DC, 2015.

FIP. Guidelines for dissolution testing of solid oral products. Drug Inf. J, Philadelphia, 1995, 30, 1071–1084.

USP. The United States Pharmacopeia and National Formulary 2016 USP 39–NF 34; The United States Pharmacopeial Convention, Inc.: Rockville, MD.

Shah, R., Patel, S; Patel, H.; Pandey, S.; Shah, S.; Shah, D. Development and validation of dissolution method for carvedilol compression-coated tablets. Brazilian J. Pharm Sci, 2011, 47 (4), 899–906.

Gupta, A.; Gaud, RS.; Ganga, S. Development of Discriminating Dissolution Method for an Insoluble Drug: Nisoldipine. Int. J. PharmTech Res. 2010, 2 (1), 931–939.

Zaid, A.N.; Qaddomi, A.; Ghanem, M.; Shehadeh, L.; Abualhasan, M.; Natur, S.; Khammash,S. Development of a Dissolution Method to Compare Tablet Formulations Containing Valsartan/Amlodipine. Dissol Tech, 2015, 22 (3), 32–38.

Wlodarski K.; Sawicki W.; Haber K.; Knapik J.; Wojnarowska Z.; Paluch M.; Lepek P.; Hawelek L.; Tajber L. Physicochemical properties of tadalafil solid dispersions – Impact of polymer on the apparent solubility and dissolution rate of tadalafil. Eur. J. of Pharm. and Biopharm. 2015, 94, 106–115.

Lobenberg, R.; Amidon, G. Modern bioavailability, bioequivalence and biopharmaceutics classification system. New scientific approaches to international regulatory standards. Eur. J. Pharm. Biopharm. 2000. 50 (1), 3–12.

Kumar, VR.; Sevukarajan M.; Jayasri Vulava, M.; Apavankumar, AG.; Deepthi Y.; Manjunath, M.; Anand, A. Improvement of dissolution characteristics and bioavailability of tadalafil by solid dispersion technique using water-soluble polymers. Int. J. Adv. Pharm. 2012, 2(2), 56–63.

Balakrishnan, AJ; Rege, BD; Amidon, GL.; Polli, JE. Surfactant-mediated dissolution: contributions of solubility enhancement and relatively low micelle diffusivity. J. Pharm. Sci., 2004, 93 (8), 2064–2075.

International Conference on Harmonization of Technical Requirements for Registration of Pharmaceutical for Human Use. Validation of Analytical Procedures: Methodology: ICH4. ICH Harmonized Tripartite Guideline: Geneva, Switzerland, 1996.

Kibbe, A. Handbook of Pharmaceutical Excipients. 6th ed. Washington, DC: American Pharmaceutical Association, 2009.

Goodman, A. The Pharmacological Basis of Therapeutics. Elmsford, NY: McGraw-Hill, 2008

Hanson, R.; Gray, V. Handbook of Dissolution Testing, 3rd ed; Dissolution Technologies, Inc.: Hockessin, DE, 2004.

Fortunato, D. Dissolution Method Development for Immediate Release Solid Oral Dosage Forms. Dissolution Technol. 2005, 12 (3), 12–14.

Priya, MBV; Murthy Soni, TEGK. (2012). Development of Discriminative Dissolution Media for Marketed Gliclazide Modified-Release Tablets. Dissolut. Technol. 15; 38–42.

British Pharmacopoeia. London: Her Majesty’s Stationery Office. London, 2016.

Bakshi, M.; Saranjit, S. (2002) Development of validated stability-indicating assay methods--critical review. J. Pharm. Biomed. Anal. 2002, 28(6), 1011–1040.

Fonseca, LB.; Labastie, M.; de Sousa, VP.; Volpato, NM. Development and Validation of a Discriminative Test for Nimesulide Suspensions. AAPS PharmSciTech 2009, 10(4), 1145–1152.

Li, S.; He, H.; Parthiban, LJ.; Yin, H.; Serajuddin, TM. IV–IVC Considerations in the Development of Immediate-Release Oral Dosage Form. J. Pharm. Sci. 2005, 94 (7), 1396–1417.




DOI: http://dx.doi.org/10.7439/ijapa.v7i2.4155

Article Metrics

Metrics Loading ...

Metrics powered by PLOS ALM

Refbacks

  • There are currently no refbacks.


Copyright (c) 2017 International Journal of Advances in Pharmaceutical Analysis