Research Journal of Pharmaceutical Dosage Form and Technology

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Solubility Enhancement of Poorly Soluble Drug by using different Techniques


Affiliations
1 Student, Department of Pharmaceutics, Shri. D. D. Vispute College of Pharmacy and Research Center, Panvel., India
2 Assistant Professor, Department of Pharmaceutics, Shri. D. D. Vispute College of Pharmacy and Research Centre, Panvel., India
3 3Principal, Department of Pharmacy, Shri. D. D. Vispute College of Pharmacy and Research Center, Panvel., India
     

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Solubility is the process of a solid dissolving in a liquid phase, resulting in a homogeneous system. Solubility is a crucial characteristic for achieving the appropriate drug concentration in the systemic circulation and demonstrating pharmacological response. Drugs that are poorly water soluble require substantial dosages to achieve therapeutic plasma concentrations following oral administration. Low aqueous solubility is a major issue in the development of novel chemical entities' formulations. Any medicine that needs to be absorbed must be in the form of an aqueous solution at the absorption site. For liquid medicinal compositions, water is the preferred solvent. The majority of medications are weakly acidic and basic, with low water solubility. Micronization, chemical modification, pH adjustment, solid dispersion, complexation, cosolvency, micellar solubilization, hydrotropy, and other procedures are used to increase the solubility of weakly water-soluble pharmaceuticals. The goal of this review paper is to present solubilization approaches for achieving optimal absorption and increased bioavailability.

Keywords

Solubility, solubility enhancement, co-solvent, pH, emulsions.
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  • Harendra. P, Verma.N. (2013). Method Used for Solubility Enhancement Of Poorly Water Soluble Drug: A Review.International Journal of Chemistry and Pharmaceutical Sciences: Vol.1(5): 187-192

  • Bukhari.R, Syed Naiem and Khan, Nisar. (2019). Hydrotrophy: Novel Solubility Enhancement Technique: A Review. International Journal of Pharmaceutical Sciences and Research. 10.13040/IJPSR.0975-8232.10(3).1025-36.

  • Savjani, K. T., Gajjar, A. K., and Savjani, J. K. (2012). Drug Solubility: Importance and Enhancement Techniques. ISRN Pharmaceutics, 195727. https://doi.org/10.5402/2012/195727

  • Chaudhary. A, Nagaich.U, Gulati.N, V. K. Sharma, R. L. Khosa. (2012). Enhancement Of Solubilization and Bioavailability of Poorly Soluble Drugs By Physical And Chemical Modifications: A Recent Review. Journal of Advanced Pharmacy Education and Research 2 (1) 32-67 ISSN 2249-3379

  • Deshmukh, Amol and Tiwari, Kundan and Mahajan, Vijay. (2017). Solubility Enhancement Techniques for Poorly WaterSoluble Drugs. International Journal of Pharmaceutical Sciences and Nanotechnology. 10. 3701-3708. DOI:10.37285/ijpsn.2017.10.3.1

  • Vemula.V.R, Lagishetty.V, Lingala.S. (2010). Solubility Enhancement Techniques. International Journal of Pharmaceutical Sciences Review and Research; Volume 5, Issue 1, November – December 2010; Article-007 ISSN 0976 – 044X

  • ChaumeilJ.C.(2000). Micronisation, A Method of Improving The Bioavailability of Poorly Soluble Drugs, Methods and Findings in Experimental And Clinical Pharmacology, European Journal of Pharmaceutical Sciences ;10, 17–28

  • Kshirsagar.S, Choudhari.M, Sathyan. R, Dhore.S. (2019). Solubility Enhancement by Various Techniques Based on Pharmaceutical and Medicinal Chemistry Approach: an Overview. Asian J. Pharm. Tech.; 9(2):141-146. doi: 10.5958/2231- 5713.2019.00024.2

  • S. S. Mistree, Dr. M. D. Kshirsagar, C. D. Uplenchwar. (2019). CO-Solvency and Hydotropy Technique for solubility Enhancement: an Overview. International Journal of Research in Pharmaceutical Technology. Volume 2(5)

  • Gennaro A.R. editors. Remington, the science and practice of pharmacy, 21st ed. Lippincott, Williams and Wilkins, 2005; 867- 868.

  • Fiese E.F, Hagen T.A. Preformulation. In: Lachman L, Liberman H.A, Kanig J.L, editors. The theory and practice of industrial pharmacy. 3rd ed. Bombay: Varghees Publication House, 1990; 171-196.

  • Allen L.V, Popovich, N.G, Ansel H.C., Ansel’s Pharmaceutical Dosage Forms and Drug Delivery Systems, Lippincott, Williams and Wilkins 2005; 100- 101.

  • Venkatesh S, Y, Rao V, Anderson B. D, Intrinsic solubility estimation and pH-solubility behavior of cosalane (NSC 658586), an extremely hydrophobic diproticacid, Pharmaceutical Research, 1996; 13(10), 1453-1459.

  • Savjani, K. T., Gajjar, A. K., and Savjani, J. K. (2012). Drug solubility: importance and enhancement techniques. ISRN pharmaceutics, 2012, 195727. https://doi.org/10.5402/2012/195727

  • Patil, A. N., D. M. Shinkar, and R. B. Saudagar. (2017). “Review Article: Solubility Enhancement by Solid Dispersion”. International Journal of Current Pharmaceutical Research, vol. 9, no. 3, May 2017, pp. 15-18.doi:10.22159/ijcpr.2017.v9i3.19583.

  • Gupta P, Kakumanu VK, Bansal AK. (2004). Stability and solubility of celecoxib-PVP amorphous dispersions: a molecular perspective. Pharmaceutical Research. 21(10):1762–1769. [PubMed] [Google Scholar]

  • Abdul-Fattah AM, Bhargava HN. (2002) Preparation and in vitro evaluation of solid dispersions of halofantrine. International Journal of Pharmaceutics. 235(1-2):17–33. [PubMed] [Google Scholar]

  • Sinha S, Ali M, Baboota S, Ahuja A, Kumar A, Ali J. (2010). Solid dispersion as an approach for bioavailability enhancement of poorly water-soluble drug ritonavir. AAPS PharmSciTech.11(2):518–527. [PMC free article] [PubMed] [Google Scholar]

  • Chiou WL, Riegelman S. (1971). Pharmaceutical applications of solid dispersion systems. Journal of Pharmaceutical Sciences.;60(9):1281–1302. [PubMed] [Google Scholar]

  • Tachibana T, Nakamura A. (1965). A methodfor preparing an aqueous colloidal dispersion of organic materials by using watersoluble polymers: dispersion of β-carotene by polyvinylpyrrolidone. Colloid and Polymer Science. ;203(2):130– 133. [Google Scholar]

  • Uekama K, Hirayama F, Irie T. (1998). Cyclodextrin drug carrier systems. Chemical Reviews. ;98(5):2045–2076. [PubMed] [Google Scholar]

  • Parikh RK, Mansuri NS, Gohel MC, Soniwala MM. Dissolution enhancement of nimesulide using complexation and salt formation techniques. Indian Drugs. 2005;42(3):149–154. [Google Scholar]

  • Cao F, Guo J, Ping Q. (2005). The physicochemical characteristics of freeze-dried scutellarin- cyclodextrin tetracomponent complexes. Drug Development and Industrial Pharmacy. ;31(8):747–756. [PubMed] [Google Scholar]

  • Wen X, Tan F, Jing Z, Liu Z. (2004). Preparation and study the 1:2 inclusion complex of carvedilol with β-cyclodextrin. Journal of Pharmaceutical and Biomedical Analysis.;34(3):517–523. [PubMed] [Google Scholar]

  • Kevin C Garala, Anil J Shinde, Harinath N More. Solubility Enhancement of Aceclofenac Using Dendrimer. Research J. Pharma. Dosage Forms and Tech. 2009; 1(2): 94-96.

  • K Ravi Sankar, NL Prasanthi, SS Manikiran and N Rama Rao, Research Journal of Pharmaceutical Dosage Forms and Technology. 2(2): March – April. 2010, 184-188.

  • Dinesh Pardhi, Umesh Shivhare, Pravin Suruse and GeetuChabra, Liquisolid Technique for Solubility Enhancement of Poorly Water Soluble Drugs, Research Journal of Pharmaceutical Dosage Forms and Technology. 2(5): Sept.-Oct. 2010, 314-322.

  • Tapan Kumar Giri, Manish Desmukh, Animesh Jaiswal and Dulal Krishna Tripathi, β-Cyclodextrin and Its Derivatives Based Drug Delivery, Research Journal of Pharmaceutical Dosage Forms and Technology. 2(6): Nov.-Dec. 2010, 361-369.

  • Nakkala Balaji, V. Sai Kishore and Kasani Hari Krishna Gouda, Formulation and Evaluation of Simvastatin Solid Dispersions for Dissolution Rate Enhancement, Research Journal of Pharmaceutical Dosage Forms and Technology. 3(4): July-Aug. 2011, 152-156.

  • Atul Phatak, Pallavi Jorwekar and P.D. Chaudhari, Nanosuspensions: A Promising Nanocarrier Drug Delivery System, Research Journal of Pharmaceutical Dosage Forms and Technology. 3(5): Sept.-Oct. 2011, 176-182.

  • Amit J. Raval and Madhabhai M. Patel, Techniques to Improve Bioavailability of Poorly Water Soluble Drugs – A review, Research Journal ofPharmaceutical Dosage Forms and Technology. 3(5): Sept.-Oct. 2011, 183-192.

  • Gannu Praveen Kumar and S. Kiran Kumar, Drug Dissolution Enhancement by Salt Formation: Current Prospects, Research Journal of Pharmaceutical Dosage Forms and Technology. 3(6): Nov.- Dec., 2011, 251-259.

  • P. Sabitha Reddy*, C. Swetha and K. Ravindra Reddy, Effect of Hydrotropes and Physical Properties on Solubility of Glibenclamide, Research Journal of Pharmaceutical Dosage Forms and Technology. 3(6): Nov.- Dec., 2011, 294-297.

  • Patil MD, Keny RV, Pimprikar RB, Yashwante SB, Saindane DS, Mandlik SK, MujawarTabrej, Kale MK and Firke BM, Physicochemical Characterization of Solid Dispersion of Telmisartan with Alkaliser by Hot Melt Method, Research Journal of Pharmaceutical Dosage Forms and Technology. 1(3): Nov. – Dec. 2009, 250-253.


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  • Solubility Enhancement of Poorly Soluble Drug by using different Techniques

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Authors

Supriya Vinod Pote
Student, Department of Pharmaceutics, Shri. D. D. Vispute College of Pharmacy and Research Center, Panvel., India
Kedar Bavaskar
Assistant Professor, Department of Pharmaceutics, Shri. D. D. Vispute College of Pharmacy and Research Centre, Panvel., India
Ashish Jain
3Principal, Department of Pharmacy, Shri. D. D. Vispute College of Pharmacy and Research Center, Panvel., India

Abstract


Solubility is the process of a solid dissolving in a liquid phase, resulting in a homogeneous system. Solubility is a crucial characteristic for achieving the appropriate drug concentration in the systemic circulation and demonstrating pharmacological response. Drugs that are poorly water soluble require substantial dosages to achieve therapeutic plasma concentrations following oral administration. Low aqueous solubility is a major issue in the development of novel chemical entities' formulations. Any medicine that needs to be absorbed must be in the form of an aqueous solution at the absorption site. For liquid medicinal compositions, water is the preferred solvent. The majority of medications are weakly acidic and basic, with low water solubility. Micronization, chemical modification, pH adjustment, solid dispersion, complexation, cosolvency, micellar solubilization, hydrotropy, and other procedures are used to increase the solubility of weakly water-soluble pharmaceuticals. The goal of this review paper is to present solubilization approaches for achieving optimal absorption and increased bioavailability.

Keywords


Solubility, solubility enhancement, co-solvent, pH, emulsions.

References