Enhancing the Solubility and Dissolution Rate of Meclizine Hydrochloride by Inclusion Complex
Meclizine Hydrochloride is an Anti-Histamine drugs with very low bioavailability that can be improved by increasing its solubility and dissolution rate. The aim of this study is to enhance dissolution of Meclizine Hydrochloride as a model hydrophobic drug through application of inclusion complex technology. It was formulated as inclusion complex compact, and its dissolution property is evaluated and compared with marketed product of Meclizine Hcl tablet. The newly formulated drug and the interaction between excipients was examined by, Fourier-transform infrared spectroscopy, and differential scanning colorimetry, respectively. Both DSC and SEM results suggested loss of crystallinity of Meclizine Hydrochloride upon conversion into a inclusion complex formulation. The dissolution efficiency of Meclizine Hydrochloride at 45 min was increased from directly compressed tablet to 98.0% for marketed product to 97.2% at 45 minutes for the inclusion complex formulation. The increase in the dissolution rate was also found to be significant compared to the marketed product. The inclusion complex technique appears to be a promising approach for improving the dissolution of poorly soluble drugs like Meclizine Hydrochloride.
Keywords: Meclizine Hydrochloride, inclusion complex, Avicel pH 102, Talc, Lactose, ethanol
2. Loftsson T, Brewster M E et al. Pharmaceutical applications of cyclodextrins Drug solubilisation and stabilization. J Pharm Sci 1996;85:1017–1025.
3. Singh R, Bharti N, Madan J, et al. Characterization of cyclodextrins inclusion complexes – a review. J Pharm Sci Technology 2010; 2:171–183.
4. Nathir A F A, Khaled SA, Mohammad-Bassam AB. Physiochemical study on microencapsulation of hydroxypropyl-beta-cyclodextrins in dermal preparations. Drug Devlopment Industrial Pharm 2010; 36:688–697.
5. Bekerrs O, Uijtendaal E V, Beijnen J H, et al. Cyclodextrins in the pharmaceutical field. Drug Dev Ind Pharm 1991; 17:1503– 1549.
6. Raju KNSL, Kavitha K, Ganesh NS, Ramesh B. Effect of dissolution rate by liquisolid compact approach : An overview. Der Pharmcia Lettre 2011;3(1):71-83.
7. Parakh SR, Gothoskar AV. A review of mouth dissolving tablet technologies. PharmTech 2003;27(11):92-8.
8. Higuchi T, Connors KA. Phase-solubility techniques. Adv Anal Chem Instrum 1961;4:117–212.
9. Chowdary KPR, Nalluri BN. Studies on nimesulide and β-cyclodextrin inclusion complexes. Indian Drugs. June 37(6), 2000, 299-304.
10. Orienti I, Cerchiara T, Zecchi V, et al. Complexation of ursodeoxycholic acid with β-cyclodextrin – choline dichloride coprecipitate. Int. J. of Pharmaceutics. 190, 1999, 139-153.
11. Mura P, Faucci MT, Manderioli A, et.al. Influence of the preparation method on the physicochemical properties of binary system of itraconazole with cyclodextrins. Int. J. of Pharmaceutics 193, 1999, 85-95
12. Srikem Laboratories pvt ltd. Open Part DMF. 2015. 1-155.
13. United State Pharmacopeia. Government of USA. Ministry Of Health.2018; 2541;
14. Subrahmanyam CVS. Textbook of physical pharmaceutics. Delhi: Vallabh Prakashan; 2005 p.28-32.
15. Subrahmanyam CVS, Thimmasetty J, Shivanand KM, Vijayendraswamy SM. Laboratory manual of industrial pharmacy. Delhi: Vallabh Prakashan; 2006 p.32.
16. Saeedi M, Akbari J, Morteza-Semnani K, Enayati-Fard R, Sar-Reshteh-dar S, Soleymani A. Enhancement of dissolution rate of indomethacin: using liquisolid compacts. Iran J Pharm Res 2011; 10:25.
17. Mohammed Asif Husain Mg, T Rama Rao, Maimuna Anjum. Preparation and evaluation of nilvadipine liquisolid compacts. Int J Pharm Pharm Sci 2014; 6:1-8.
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