PREPARATION AND EVALUATION OF METOLAZONE SOLID DISPERSIONS AND FAST DISSOLVING TABLETS USING STERCULIA FOETIDA SEED STARCH AND PLASDONE K-29/32 AS SUPERDISINTEGRANTS
DOI:
https://doi.org/10.22159/ijap.2020v12i4.37975Keywords:
Metolazone, Solid dispersions, Plasdone K-2932, Sterculia foetida, Fast dissolving tabletsAbstract
Objective: The objective of the current study is to improve the solubility of the Biopharmaceutical Classification System (BCS) Class-II drug, Metolazone, using various superdisintegrants.
Methods: Starches were extracted from Sterculia foetida seed powder by water and alkali techniques i.e., sodium hydroxide at 0.1%, 0.25% and 0.5% concentrations. Several phytochemical and physicochemical parameters were evaluated on the extracted starches. Solid dispersions of Metolazone were prepared by the solvent evaporation technique using plasdone K-29/32 alone and by mixing plasdone K-29/32 with Sterculia foetida seed starch. Various physical parameters were evaluated for the prepared solid dispersions. Tablets were prepared using Metolazone solid dispersions and varying concentrations of Sterculia foetida seed starch by direct compression technique. Pre and post-compression parameters were evaluated along with in vitro drug release studies, characterization using Scanning Electron Microscopy (SEM) and stability studies.
Results: Phytochemical tests showed the presence of starch in all extracts. Starch prepared from 0.1% sodium hydroxide (SFS2) showed best physicochemical properties. In vitro dissolution studies revealed that solid dispersion MS4 containing Metolazone and plasdone K-29/32 in 1:3 ratios showed better drug release. Formulation MPT6 containing MS5 solid dispersion with 15% w/w of SFS2 showed enhanced drug release. SEM studies revealed no major interactions between drugs and excipients. Accelerated stability studies showed that all tablets were stable.
Conclusion: Sterculia foetida seed starch and plasdone K-29/32 have enhanced the solubility of Metolazone.
Downloads
References
Khan GM. Controlled release oral dosage forms: some recent advances in matrix type drug delivery systems. J Med Sci 2001;1:350-4.
Jin Xi K, Jeong SP, Phuong T, Yong CP, Dong HK, Sang EL. Overview of the manufacturing methods of solid dispersion technology for improving the solubility of poorly water-soluble drugs and application to anticancer drugs. MDPI Pharm 2019;11:1-26.
Argade PS, Magar DD, Sudagar RB. Solid dispersion: solubility enhancement technique for poorly water soluble drugs. J Adv Pharm Educ Res 2013;3:427-39.
Iswarya S, Abha D, Bhagyashri J, Vandana W, Jesal D. Solid dispersions: an approach to enhance solubility of poorly water soluble drug. J Sci Innovative Res 2013;2:685-94.
Garima Y, Anupriya K, Shilpi B. Fast dissolving tablets recent advantages: a review. Int J Pharm Sci Res 2012;3:728-36.
Mohanachandran PS, Sindhumol PG, Kiran TS. Superdisintegrants: an overview. Int J Pharm Sci Rev Res 2011;6:105-9.
Kusum K, Ram BS, Shweta A. Natural polymers and their applications. Int J Pharm Sci Rev Res 2016;37:30-6.
Rajeswari S, Prasanthi T, Navya S, Ranjit PS, Satyajit P, Vinusha G. Natural polymers: a recent review. World J Pharm Pharm Sci 2017;6:472-94.
Swarnalatha K, Venkata KB, Hari BB. Phytochemical screening, anti-diabetic and antioxidant activities of Kigelia Africana (LAM.) and Sterculia foetida L. Rasayan J Chem 2019;12:907-14.
Xueqing Li, Rutao W, Yang L, Yun L, Heng Z, Yabo F. Pharmacokinetic study of single-and multiple-dosing with metolazone tablets in healthy Chinese population. BMC Pharmacol Toxicol 2017;18:1-10.
Vidyadhara S, Sasidhar RL, Lakshmi HD, Vijetha P, Vijetha K. Studies on jack fruit seed starch as a novel natural superdisintegrant for the design and evaluation of Irbesartan fast-dissolving tablets. Integr Med Res 2017;6:280-91.
Rubina NS, Mubeen MA, Kiran N, Vijay P, Asma BS, Imad UM. Phytochemcial screening and in vitro anti-inflammatory activity of methanolic extract of Sterculia foetida L. IOSR J Pharm Biol Sci 2016;11:28-34.
Sundeep M, Vidyadhara S, Sailaja Y, Sandeep D, Sasidhar RL, Ramu A. Formulation and evaluation of dolutegravir sodium solid dispersions and fast dissolving tablets using poloxamer-188 and jack fruit seed starch as excipients. Asian J Pharm Clin Res 2019;12:1-10.
Prashant B, Reeshwa N. Formulation, development and characterization of Meclizine hydrochloride fast dissolving tablets using solid dispersion technique. Int J Appl Pharm 2018;10:141-6.
Pinak K, Mansi S, Niketkumar P, Shashank J, Namrata V, Senshang L. Preparation and characterization of pyrimethamine solid dispersions and an evaluation of the physical nature of pyrimethamine in solid dispersions. J Drug Delivery Sci Tech 2018;45:110-23.
Vikaas B, Ritika MB, Sandeep K, Nitesh C, Manjusha C. Formulation and evaluation of fast disintegrating tablet of telmisartan. J Chem Pharm Res 2016;8:61-7.
Manimaran V, Damodharan N. Development of fast dissolving tablets of nisoldipine by solid dispersion technology using poloxamer 407 and poloxamer 188. J Young Pharm 2016;8:341-9.
Mahmoud EM, Mahmoud MA, Khalid AK, Hatem AS. Accelerated physical stability testing of tolmetin sodium fast dissolving tablets prepared by direct compression method. Int J Pharm Pharm Res 2017;8:42-51.
Bhairav BA, Jagtap LR, Saudagar RB. Solubility and dissolution enhancement of pioglitazone using solid dispersion technique. Int J Curr Pharm Res 2017;9:186-93.
Shirsath NR, Jagtap V, Goswami AK. Formulation and development of Famotidine solid dispersion tablets for their solubility enhancement. Indian J Pharm Educ Res 2019;53:548-53.
Pinak K, Mansi S, Niketkumar P, Shashank J, Namrata V, Senshang L. Preparation and characterization of pyrimethamine solid dispersions and an evaluation of the physical nature of pyrimethamine in solid dispersions. J Drug Delivery Sci Tech 2018;45:110-23.
Gagandeep S, Navjot S, Randeep K, Neena B. Development and characterization of nevirapine loaded amorphous solid dispersions for solubility enhancement. Asian J Pharm Clin Res 2019;12:176-82.
Uday KM, Kishore BM. Design and evaluation of fast dissolving tablets containing diclofenac sodium using fenugreek gum as a natural superdisintegrant. Asian Pac J Trop Biomed 2014;4:329-34.
Emmanuel OO, Musiliu OA, Ekaete IA. Evaluation of callinectes chitosan as a superdisintegrant in metronidazole tablet. Int J Pharm Pharm Sci 2017;9:111-8.
Sanjaymitra PS, Ganesh GN. Dissolution and solubility enhancement strategies: current and novel prospectives. J Crit Rev 2018;5:1-10.
Madaan R, Bala R, Vasisht T, Sharma R, Garg S. Formulation and characterization of matrix tablets using mucilage of Tinospora cordifolia as natural binder. Int J Pharm Pharm Sci 2018;10:22-7.