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Combinatorial Chemistry & High Throughput Screening

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ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

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Research Article

Natural Plus Synthetic Hydrotropic Solubilization using Response Surface Methodology to Optimize the Solid Dispersion of Hydrochlorothiazide

Author(s): Arun Saharawat, Deepali* and Nidhi Nainwal

Volume 25, Issue 2, 2022

Published on: 17 December, 2020

Page: [307 - 323] Pages: 17

DOI: 10.2174/1386207323666201218115149

Price: $65

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Abstract

Background: Solubility/dissolution is said to be the key factor that influences the oral bioavailability of drug and is also the rate limiting step in formulation development.

Objective: Hydrochlorothiazide (HCZ) is a BCS Class IV drug with low solubility and low permeability. The present work aimed to increase the solubility of hydrochlorothiazide using blends of natural and synthetic hydrotropes.

Methods: Two hydrotropes one from natural (piperazine) and other from the synthetic origin (sodium benzoate) were selected for the formulation of solid dispersion (SD) of HCZ. Preliminary trial batches were prepared by considering the safe dose of both the selected hydrotropes i.e. sodium benzoate (SB) and piperazine (PP). A 32 full factorial design was opted for preparing the optimized solid dispersion of hydrochlorothiazide.

Results: The quadratic models were found to be best fitted for the studied responses, which were percent solubility and in-vitro drug release. The results showed increased solubility and in-vitro drug release of HCZ solid dispersions as a function of increasing levels of both hydrotropes.

Conclusion: In this work, it was concluded that the use of natural hydrotropes along with synthetic hydrotropes gave an effective and safe approach for the solubility enhancement of the HCZ.

Keywords: Hydrochlorothiazide, piperazine, sodium benzoate, 32 full factorial design, solid dispersion, hydrogen bonding.

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[1]
Shekhawat, P.B.; Pokharkar, V.B. Understanding peroral absorption: regulatory aspects and contemporary approaches to tackling solubility and permeability hurdles. Acta Pharm. Sin. B, 2017, 7(3), 260-280.
[http://dx.doi.org/10.1016/j.apsb.2016.09.005] [PMID: 28540164]
[2]
Coltescu, A.R.; Butnariu, M.; Sarac, I. The importance of solubility for new drug molecules. Biomed. Pharmacol. J., 2020, 13(2), 577-583.
[http://dx.doi.org/10.13005/bpj/1920]
[3]
Bharti, V.P.; Attal, V.R.; Munde, A.V.; Birajdar, A.S.; Bais, S. Strategies to enhance solubility and dissolution of a poorly water-soluble drug. J. Innov. Pharm., 2015, 2(4), 481-494.
[4]
Jambhekar, S.S.; Breen, P.J. Drug dissolution: significance of physicochemical properties and physiological conditions. Drug Discov. Today, 2013, 18(23-24), 1173-1184.
[http://dx.doi.org/10.1016/j.drudis.2013.08.013] [PMID: 24042023]
[5]
Maheshwari, R.; Shukla, R. Novel method for spectrophotometric analysis of hydrochlorothiazide tablets using niacinamide as hydrotropic solubilizing agent. Asian J. Pharm., 2008, 2(1), 68.
[http://dx.doi.org/10.4103/0973-8398.41570]
[6]
Ghadi, R.; Dand, N. BCS class IV drugs: Highly notorious candidates for formulation development. J. Control. Release, 2017, 248, 71-95.
[http://dx.doi.org/10.1016/j.jconrel.2017.01.014] [PMID: 28088572]
[7]
Bauduin, P.; Renoncourt, A.; Kopf, A.; Touraud, D.; Kunz, W. Unified concept of solubilization in water by hydrotropes and cosolvents. Langmuir, 2005, 21(15), 6769-6775.
[http://dx.doi.org/10.1021/la050554l] [PMID: 16008386]
[8]
Kim, J.Y.; Kim, S.; Papp, M.; Park, K.; Pinal, R. Hydrotropic solubilization of poorly water-soluble drugs. J. Pharm. Sci., 2010, 99(9), 3953-3965.
[http://dx.doi.org/10.1002/jps.22241] [PMID: 20607808]
[9]
Madan, J.R.; Pawar, K.T.; Dua, K. Solubility enhancement studies on lurasidone hydrochloride using mixed hydrotropy. Int. J. Pharm. Investig., 2015, 5(2), 114-120.
[http://dx.doi.org/10.4103/2230-973X.153390] [PMID: 25838997]
[10]
Kamble, R.; Sharma, S.; Mehta, P. Norfloxacin mixed solvency based solid dispersions: an in-vitro and in-vivo investigation. Integr. Med. Res., 2017, 11(3), 512-522.
[11]
Ganesan, P.; Soundararajan, R.; Shanmugam, U.; Ramu, V. Development, characterization and solubility enhancement of comparative dissolution study of second generation of solid dispersions and microspheres for poorly water-soluble drug. Asian J. Pharm. Sci., 2015, 10(5), 433-441.
[http://dx.doi.org/10.1016/j.ajps.2015.05.001]
[12]
Onn, G.; Loh, K.; Tze, Y.; Tan, F.; Peh, K.K. Hydrophilic polymer solubilization on norfloxacin solubility in preparation of solid dispersion. Powder Technol., 2014, 256, 462-469.
[http://dx.doi.org/10.1016/j.powtec.2014.01.089]
[13]
Esim, O.; Savaser, A.; Ozkan, C.K.; Bayrak, Z.; Tas, C.; Ozkan, Y. Effect of polymer type on characteristics of buccal tablets using factorial design. Saudi Pharm. J., 2018, 26(1), 53-63.
[http://dx.doi.org/10.1016/j.jsps.2017.10.013] [PMID: 29379333]
[14]
Pani, N.R.; Nath, L.K.; Bhunia, B. Formulation, development, and optimization of immediate release nateglinide tablets by factorial design. Drug Discov. Ther., 2010, 4(6), 453-458.
[PMID: 22491311]
[15]
Abdelbary, G.A.; Amin, M.M.; Abdelmoteleb, M. Novel mixed hydrotropic solubilization of zaleplon: formulation of oral tablets and in-vivo neuropharmacological characterization by monitoring plasma GABA level. J. Drug Deliv. Sci. Technol., 2016, 33, 98-113.
[16]
Habeeb, P.; Madhavan, N.; Gladis, K.; Anitha, Y.; Mohammed, S.; Raghunath, P. Formulation, optimization and evaluation of solid dispersion tablets of aceclofenac using kollidon 30. Int. J. Biopharmaceutics, 2013, 4(1), 10-17.
[17]
Madan, J.R.; Kamate, V.J.; Dua, K.; Awasthi, R. Improving the solubility of nevirapine using a hydrotropy and mixed hydrotropy based solid dispersion approach; Polymers in Medicine, 2017, pp. 1-8.
[18]
IPC. Ipc Volume 1; 2010.
[19]
Mannaa, M.; Bary, A.A.; El Assal, M.; Abdullah, F. Formulation, optimization, and evaluation of solid dispersions of metformin hcl using factorial design. Int. J. Pharm. Sci. Rev. Res., 2016, 4(2), 154-160.
[20]
Rajpurohit, V.S.; Rakha, P.; Goyal, S.; Dureja, H.; Arorac, G.; Nagpal, M. Formulation and characterization of solid dispersions of glimepiride through factorial design. Indian J. Pharm. Sci., 2011, 7(1), 7-16.
[PMID: 22131616]
[21]
Kamble, R.; Sharma, S.; Mehta, P. Norfloxacin mixed solvency based solid dispersions: an in-vitro and in-vivo investigation. J. Taibah Univ. Sci., 2017, 11(3), 512-522.
[http://dx.doi.org/10.1016/j.jtusci.2016.11.003]
[22]
Mahaveer, T. Formulation and optimization of fast dissolving tablets of norfloxacin., 2014, 6(1), 26-31.
[23]
Segall, A.I. Preformulation: The use of FTIR in compatibility studies. Int. J. Innovations Pharm. Sci., 2019, 4(3), 1-6.
[24]
Li, H.; Ma, L.; Li, X.; Cui, X.; Yang, W.; Shen, S.; Chen, M. A simple and effective method to improve bioavailability of glimepiride by utilizing hydrotropy technique. Eur. J. Pharm. Sci., 2015, 77, 154-160.
[http://dx.doi.org/10.1016/j.ejps.2015.06.016] [PMID: 26093052]
[25]
Elkhodairy, K.A.; Hassan, M.A.; Afifi, S.A. Formulation and optimization of orodispersible tablets of flutamide. Saudi Pharm. J., 2014, 22(1), 53-61.
[http://dx.doi.org/10.1016/j.jsps.2013.01.009] [PMID: 24493974]
[26]
Zhang, W.; Zhang, C.N.; He, Y.; Duan, B.Y.; Yang, G.Y.; Ma, W.D.; Zhang, Y.H. Factors affecting the dissolution of indomethacin solid dispersions. AAPS PharmSciTech, 2017, 18(8), 3258-3273.
[http://dx.doi.org/10.1208/s12249-017-0813-2] [PMID: 28584898]
[27]
El-Houssieny, B.M.; El-Dein, E.Z.; El-Messiry, H.M. Enhancement of solubility of dexibuprofen applying mixed hydrotropic solubilization technique. Drug Discov. Ther., 2014, 8(4), 178-184.
[http://dx.doi.org/10.5582/ddt.2014.01019] [PMID: 25262596]
[28]
Girishpai, K.; Divya, S.; Reddy, M.S. Kumar, Tippavajhala, V.K. Solubility enhancement of norfloxacin by hydrotropy technique. Innovare Acad. Sci., 2014, 6(8), 6-8.
[29]
Dhapte, V.; Mehta, P. Advances in hydrotropic solutions: an updated review. St. Petersburg Polytechnical University Journal. Physics and Mathematics, 2015, 1(4), 424-435.
[30]
Agrawal, G.P.; Maheshwari, R.K.; Mishra, P. Preparation of solid dispersions of ornidazole using mixed hydrotropic solubilization technique and their characterization. Int. J. Green Pharm., 2017, 2017(4), 8-9.
[31]
Nainwal, N.; Jawala, S.; Ranjit, S.; Saharan, V.K. Solubility-permeability interplay of hydrotropic solubilization using response surface methodology. Drug Deliv. Lett., 2020, 10(1)
[http://dx.doi.org/10.2174/2210303110666200220124230]
[32]
Nainwal, N.; Singh, R.; Jawla, S.; Saharan, V.A. The solubility-permeability interplay for solubility-enabling oral formulations. Curr. Drug Targets, 2019, 20(14), 1434-1446.
[http://dx.doi.org/10.2174/1389450120666190717114521] [PMID: 31333138]

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