Formulation development & invitro evaluation of efavirenz cyclodexprin complexes im-mediate release tablets
Abstract
The study was designed to investigate the effect of cyclodextrins (CDs) on the solubility, dissolution rate, and bioavailability of efavirenz by forming inclusion complexes. Prepared inclusion complexes were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction (XRD) studies. In vitro dissolution study was performed using phosphate buffer pH 6.4, distilled water, and HCl buffer pH 1.2 as dissolution medium. Among all efavirenz–cyclodextrins complexes, efavirenz–DM-β-CD inclusion complex (1:3) prepared by coprecipitation method showed 1.53-fold and 4.11-fold increase in absorption along with 2.1-fold and 2.97-fold increase in dissolution rate in comparison with Pletoz-50 and pure efavirenz, respectively.
Keywords:
Bioavailability, efavirenz–CD inclu-sion complex, dissolution, solubility
Downloads
Download data is not yet available.
References
1. Medical EconomicsPhysicians. Physicians’ desk reference. 59th ed. Stamford: Thomson; 2005. p. 2564–6.
2. Larsen KL. Large cyclodextrins. J Inclusion Phenom Macro Chem. 2002; 43(1–2):1–13.
3. Szejtli J, Osa T. Comprehensive supramolecu-lar chemistry: cyclodextrins, vol 3. Oxford: Pergamon; 1996.
4. Uekama K, Hirayama F, Irie T. Cyclodextrin drug carrier systems. Chem Rev. 1998;98(5):2045–76.
5. Mosher G, Thompson D. Complexation and cyclodextrins. encyclopedia of pharmaceutical technology, Vol. 19. New York: Marcel and Dekker; 1999. p. 49–88.
6. Homans SW. A molecular mechanical force field for the conformational analysis of oligo-saccharides: comparison of the theoretical and crystal structure of Manα1–3Manβ1–4GlcNAc. Biochemistry 1990; 29(39):9110–8.
7. Zuo Z, Kwon G, Stevenson B, Diakur J, Wiebe LI. Flutamide- hydroxypropyl-β-cyclodextrin complex: formulation, physical characteriza-tion, and absorption studies using the Caco-2 in vitro model. J Pharm Pharmceut Sci. 2000; 3(2):220–7.
8. Dollo G, Corre PL, Chollet M, Chevanne F, Bertault M, Burgot JL, et al. Improvement in solubility and dissolution rate of 1,2-dithiole- 3-thiones upon complexation with β-cyclodextrin and its hydrox- ypropyl and sulfobutyl ether-7 derivatives. J Pharm Sci. 1999;88:889–95.
9. Duchene D. New trends in cyclodextrins and derivatives. Paris: Editios de Sante; 1992. p. 351–407.
10. Fromming KH, Szejtli J. Cyclodextrins in pharmacy (Topics in inclusion science). Dor-drecht: Kulwer Academic; 1994.
11. Thompson DO. Cyclodextrin-enabling ex-cipients: their present and future use in pharmaceuticals. Crit Rev Ther Drug Carrier Syst. 1997; 14:1–104.
12. Masson M, Loftsson T, Masson G, Stefansson E. Cyclodextrin as permeation enhancer: some theoretical evaluations and in vitro testing. J Control Release 1999; 59(1):107–18.
13. Govt. of India, Ministry of Health and Fami-ly Welfare. Pharmacopoeia of India, vol I. 4th ed. New Delhi: Controller of Publica-tion; 1996. p. A–144–7
14. Marabathuni VJ, Dinesh P, Ravikumar R, Yamini P, Kiran PS, Hussain SP, Rao CM. Chi-tosan based sustained release mucoadhesive buccal patches containing amlodipine besylate (AMB). Asian J Res Pharm Sci. 2017 Jun 28; 7:97-104.
15. Marabathuni VJ, Bhavani M, Lavanya M, Padmaja K, Madhavi N, Babu P, Rao CM. For-mulation and evaluation of mouth dissolving Tablets of carbamazepine. Magnesium. 2017 Sep 27; 15(30):15.
16. Babu AK, Teja NB, Ramakrishna B, Kumar BB, Reddy GV. Formulation and evaluation of double walled microspheres loaded with pan-toprazole. METHODS. 2011; 15:28.
17. Babu AK, Reddy VR, Reddy N, Vidyasagar J. Evaluating the post compression parameter of ibuprofen by using super disintegrants. An Int J Adv Pharm Sci. 2010; 1(2):247-53.
18. Aruna MS, Babu AK, Thadanki M, Gupta ME. Solid dispersions–an approach to enhance the dissolution rate of Irbesartan. IJRPC. 2011; 1(4):780-7.
19. Babu K, Ramana MV. Development and in vi-vo evaluation of gastro retentive floating tab-lets of antipsychotic drug risperidone. Int J Pharm Pharm Sci. 2016; 11:43-52.
20. Babu AK, Ramana MV. In Vitro and In Vivo Evaluation of Quetiapine Fumarate controlled gastroretentive floating drug delivery system.
2. Larsen KL. Large cyclodextrins. J Inclusion Phenom Macro Chem. 2002; 43(1–2):1–13.
3. Szejtli J, Osa T. Comprehensive supramolecu-lar chemistry: cyclodextrins, vol 3. Oxford: Pergamon; 1996.
4. Uekama K, Hirayama F, Irie T. Cyclodextrin drug carrier systems. Chem Rev. 1998;98(5):2045–76.
5. Mosher G, Thompson D. Complexation and cyclodextrins. encyclopedia of pharmaceutical technology, Vol. 19. New York: Marcel and Dekker; 1999. p. 49–88.
6. Homans SW. A molecular mechanical force field for the conformational analysis of oligo-saccharides: comparison of the theoretical and crystal structure of Manα1–3Manβ1–4GlcNAc. Biochemistry 1990; 29(39):9110–8.
7. Zuo Z, Kwon G, Stevenson B, Diakur J, Wiebe LI. Flutamide- hydroxypropyl-β-cyclodextrin complex: formulation, physical characteriza-tion, and absorption studies using the Caco-2 in vitro model. J Pharm Pharmceut Sci. 2000; 3(2):220–7.
8. Dollo G, Corre PL, Chollet M, Chevanne F, Bertault M, Burgot JL, et al. Improvement in solubility and dissolution rate of 1,2-dithiole- 3-thiones upon complexation with β-cyclodextrin and its hydrox- ypropyl and sulfobutyl ether-7 derivatives. J Pharm Sci. 1999;88:889–95.
9. Duchene D. New trends in cyclodextrins and derivatives. Paris: Editios de Sante; 1992. p. 351–407.
10. Fromming KH, Szejtli J. Cyclodextrins in pharmacy (Topics in inclusion science). Dor-drecht: Kulwer Academic; 1994.
11. Thompson DO. Cyclodextrin-enabling ex-cipients: their present and future use in pharmaceuticals. Crit Rev Ther Drug Carrier Syst. 1997; 14:1–104.
12. Masson M, Loftsson T, Masson G, Stefansson E. Cyclodextrin as permeation enhancer: some theoretical evaluations and in vitro testing. J Control Release 1999; 59(1):107–18.
13. Govt. of India, Ministry of Health and Fami-ly Welfare. Pharmacopoeia of India, vol I. 4th ed. New Delhi: Controller of Publica-tion; 1996. p. A–144–7
14. Marabathuni VJ, Dinesh P, Ravikumar R, Yamini P, Kiran PS, Hussain SP, Rao CM. Chi-tosan based sustained release mucoadhesive buccal patches containing amlodipine besylate (AMB). Asian J Res Pharm Sci. 2017 Jun 28; 7:97-104.
15. Marabathuni VJ, Bhavani M, Lavanya M, Padmaja K, Madhavi N, Babu P, Rao CM. For-mulation and evaluation of mouth dissolving Tablets of carbamazepine. Magnesium. 2017 Sep 27; 15(30):15.
16. Babu AK, Teja NB, Ramakrishna B, Kumar BB, Reddy GV. Formulation and evaluation of double walled microspheres loaded with pan-toprazole. METHODS. 2011; 15:28.
17. Babu AK, Reddy VR, Reddy N, Vidyasagar J. Evaluating the post compression parameter of ibuprofen by using super disintegrants. An Int J Adv Pharm Sci. 2010; 1(2):247-53.
18. Aruna MS, Babu AK, Thadanki M, Gupta ME. Solid dispersions–an approach to enhance the dissolution rate of Irbesartan. IJRPC. 2011; 1(4):780-7.
19. Babu K, Ramana MV. Development and in vi-vo evaluation of gastro retentive floating tab-lets of antipsychotic drug risperidone. Int J Pharm Pharm Sci. 2016; 11:43-52.
20. Babu AK, Ramana MV. In Vitro and In Vivo Evaluation of Quetiapine Fumarate controlled gastroretentive floating drug delivery system.
Published
21/01/2022
Statistics
222 Views | 179 Downloads
Citatons
How to Cite
Bingidoddi , P., V. J. P. Marabathuni, and N. Narapusetty. “Formulation Development & Invitro Evaluation of Efavirenz Cyclodexprin Complexes Im-Mediate Release Tablets ”. International Journal of Pharmacognosy and Chemistry, Vol. 3, no. 1, Jan. 2022, pp. 10-15, doi:10.46796/ijpc.v3i1.263.
Issue
Section
Research Article
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
Copyright © Author(s) retain the copyright of this article.
.