Asian Journal of Pharmacy and Technology

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Solubility Enhancement of Ritonavir by using Liquisolid Compact Technique


Affiliations
1 Department of Pharmaceutics, MET’s Institute of Pharmacy, Adgaon, Nashik, Maharashtra, Affiliated to Savitribai Phule Pune University (SPPU), Pune, India
2 Adgaon, Nashik, Maharashtra, India, Affiliated to Savitribai Phule Pune University (SPPU), Pune, India
     

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Novel solubility enhancement technique; liquisolid compact technique is used in present research work. Ritonavir is poorly soluble drug was formulated using Avicel pH 102 and Aerosil 200 as carrier and coating material respectively. Solubility studies were conducted in different liquid vehicles, namely propylene glycol, span 20, PEG 400, tween 20, and PEG 200. From the result of saturation solubility study the liquisolid compacts were formulated using PEG 400 as non volatile vehicle. The ritonavir liquisolid formulations were obtained by allowing liquid vehicle with varying ritonavir concentration to get absorbed onto carrier and coating material taken at different ratio (R=5,10,15,20).Then the ritonavir liquisolid powder system evaluated for flow property determination and then compressed into tablet. Each batch of prepared ritonavir Liquisolid powder compact evaluated for Quality control tests, i.e. uniformity of tablet weight, uniformity of drug content, tablet hardness, friability test, disintegration and dissolution study. Optimized batch of Liquisolid powder compact evaluated for quality control test of tablet along with FTIR, DSC and PXRD study. The tableting properties of the liquisolid compacts were within the acceptable limits and in vitro drug release rate of LS compacts were distinctly higher as compared to directly compressible tablet and pure drug alone. This was due to an increase in wetting properties and surface of drug available for dissolution. FTIR study result indicates that there is no drug excipient interaction..DSC and PXRD study suggested loss of ritonavir crystallinity upon liquisolid formulation, it indicates that drug is held within the power substrate in a solubilized, almost molecularly dispersed state, which lead to enhanced drug solubility. From significant result of solubility of ritonavir, liquisolid technique would be promising solubility enhancement technique for various poorly soluble drugs.

Keywords

Ritonavir, Liquisolid Compact, PEG 400, Carrier Material, Coating Material, Poorly Water Soluble Drugs.
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  • Patil K. J., Surajj M. Sarode, Sathe B.S., Jain P.V., Jain B.V. (2014), Formulation and evaluation of sustained release tablet of Ritonavir, World Journal of Pharmacy and Pharmaceutical Sciences, 3(4),pp. 857-868.

  • Lachmman L, Liberman HA, Konig JL. (1991) The theory and practice of Industrial Pharmacy. 3rdEdn. Vargheese Publishing House, Bombay, pp.430-453

  • 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,vol.11,pp.518-527.

  • Tiong N., Elkordy a., (2009), Effects of liquisolid formulations on dissolution of naproxen, European Journal of Pharmaceutics and Biopharmaceutics, 73, pp.373-384.

  • Savjani K.T, Gajjar A.K., and Savjani J.K.,(2012),Drug Solubility: Importance and Enhancement Techniques, International Scholarly Research Network Pharmaceutics,pp.1-10.

  • Bindu M.B., Kusum B and David Banji,(2010), Novel strategies for poorly water soluble drugs, international Journal of Pharmaceutical Sciences Review and research,4(3),pp.76-84.

  • INDIAN PHARMACOPOEIA 2014,volume III , Government of India , Ministry of Health and Family Welfare, Indian pharmacopoeia commission, Ghaziabad,pp.2677

  • https://aidsinfo.nih.gov/drugs/244/ritonavir/34/professional

  • https://www.drugbank.ca/drugs/DB00503.

  • Nagesh C., Shankaraiah M. M., Attimarad S. L., Patil A. M., Vijay Kumar (2013) ,Improving the solubility and dissolution of Ritonavir by solid dispersion, Journal of Pharmaceutical and Scientific innovation,2(4),pp.30-35.

  • Saran K.,Srujan Kumar M., Subrahmanyam K.V,(2013) Enhancement of solubility of Ritonavir by using Solid dispersion Technique, International Journal of innovative Pharmaceutical Sciences and Research,1(2),pp.266-280.

  • Dashamukhi R., Kanagala V., Chittimalla A., (2013), Formulation development of Ritonavir tablets containing solid dispersions employing montmorillonite : dissolution rate enhancement, Asian journal of pharmaceutical and clinical research, 6(2), pp.206-208.

  • Yogananda R., Chowdary K.P.,(2013), Formulation Development of Ritonavir Tablets Employing B-cyclodextrins, Hydroxy Propyl B-cyclodextrin and Solutaol Hs15, American Journal of PharmTech Research,3,pp.710-718.

  • Shah K., Borhade S., Londhe V. (2014), Utilization of co-crystallization for solubility enhancement of a poorly soluble antiretroviral drug-Ritonavir, International journal of pharmacy and pharmaceutical sciences,6( 2),pp.556-558.

  • Desai S., Disouza J., Musle K., Hoshmani A.,(2016), Solubility enhancement of Ritonavir by Hot Melt Extrusion, International Journal of Pharmacy and Pharmaceutical Sciences,8(3),pp.309-312 16. Prakash S., Vidyadhara S., Sasidhar R., Abhijit D. and Akhilesh D.(2013),Development and characterization of Ritonavir nanosuspension for oral use, Der Pharmacia Lettre, 5 (6):pp.48-55.

  • Balaji A, M.S. Umashankar and B. Kavitha, (2014), Liquisolid technology- a latest review, International Journal of Applied Pharmaceutics, 6(1),pp. 11-19.

  • Nagabandi K.V, K. N. Jayaveera, T. Ramarao, (2011) LIQUISOLID Compacts: A Novel Approach to Enhance Bioavailability of Poorly Soluble Drugs, Int J Pharm Bio Sci, Volume 1,Issue 3,89-102 19. Kharwade M., and M Sneha., (2015) ,A Review on Pioneering Technique - Liquisolid Compact and Applications., Research Journal of Pharmaceutical, Biological and Chemical Sciences, 6(2), pp.220-227.

  • Kala N. P., Shaikh M. T., Shastri D. H., Shelat P. K., (2014),A Review On Liquisolid Systems, Journal of Drug Delivery and Therapeutics; 4(3),pp. 25-31

  • Spireas et al., Liquisolid Systems and Methods of Preparing Same, United States Patent, 5800834, Sep. 1, 1998.

  • Spireas S, Sadu S (1998), Enhancement of prednisolone dissolution properties using liquisolid compacts , International journal of pharmaceutics , Elsevier, 166, pp.177-188.

  • INDIAN PHARMACOPOEIA, 2007, Government of India, Indian Pharmacopoeia Commission, Ministry Of Health And Family Welfare, Ghaziabad: India, pp.78-80, 177-184, 267-270,495, 897, 1059.

  • Srivastava S., Srivastava D., Nimisha, Prajapat V., (2014), Liquisolid Technique for Enhancement of Dissolution Properties of Lornoxicam, Indo Global Journal of Pharmaceutical Sciences, 4(2), pp. 81-90

  • Gilvert Banker, Christopher T. Rhodes, Modern Pharmaceutics, 4th ed, Informa health care, pp. 178, 544-551.

  • Chella N., Shastria N., Tadikonda R. (2012),Use of the liquisolid compact technique for improvement of the dissolution rate of valsartan, Acta Pharmaceutica Sinica B ,2(5) , pp.502–508

  • Karva G. S., Katariya V. R., Shahi S. R., Spray Drying: A Approach for Solubility Enhancement of Ritonavir by Solid Dispersion, International journal of pharmaceutical sciences and Drug Research ,2015, 7( 4) ,pp.321-328.

  • Shukla D., chakraborty S., singh S., mishra B.,(2008),Mouth dissolving tablets ii:An overview of evaluation techniques, scientia pharmaceutica,77,pp.327-341.

  • Sarraf M., Hussein A., jabbar A.,(2014),Dissolution enhancement of telmisartan by liquisolid compacts, International Journal of Pharmacy and Pharmaceutical Sciences, 6 (2), pp.743-749.

  • Asija R., Bhatt S., Asija S., Yadav A., Shah I., (2014), Enhancement of solubility and dissolution of lercanidipine by liquisolid technique, Journal of Chemical and Pharmaceutical Research, 6(6),pp.2680-2686.

  • Pavia, D.L., Lampman, G.M., Kriz, G.S. and Vivyan, J.R. 2011, Spectroscopy, 7th ed. New Delhi, Cengage Learning India Pvt. Ltd., pp.26-92.

  • Komala D.R., Janga K.Y., Jukanti R., Bandarri S., Vijaygopal M. (2015), Competence of Raloxifene hydrochloride loaded liquisolid compacts for improved dissolution and intestinal permeation, Journal of Drug Delivery Science and Technology, Elsevier, 30, pp.232-241.

  • Sanka K., Poienti S., Mohd A., Diwan P.(2014), Improved oral delivery of clonazepam through liquisolid powder compact formulations: In-vitro and Ex-vivo characterization, Powder technology256,Elsevier,pp.336-344.

  • Patel J. B. Patel K. J.,(2015), Enhancement of solubility of lornoxicam using novel liquisolid technique, Pharma Science Monitor, 6(2), pp.196-206.

  • Lachmman L, Liberman HA, Konig JL. (2013) The theory and practice of Industrial Pharmacy. 4th Edn. Vargheese Publishing House, Bombay, pp.244-247

  • Chandel P. Kumar R., Kapoor A.,(2013), Liquisolid Technique: An approach for enhancement of solubility, Journal of drug Delivery and Therapeutics, 3(4), pp.131-137.


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  • Solubility Enhancement of Ritonavir by using Liquisolid Compact Technique

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Authors

Sapana Ahirrao
Department of Pharmaceutics, MET’s Institute of Pharmacy, Adgaon, Nashik, Maharashtra, Affiliated to Savitribai Phule Pune University (SPPU), Pune, India
Bhagyashree D. Gangode
Department of Pharmaceutics, MET’s Institute of Pharmacy, Adgaon, Nashik, Maharashtra, Affiliated to Savitribai Phule Pune University (SPPU), Pune, India
Sanjay Kshirsagar
Adgaon, Nashik, Maharashtra, India, Affiliated to Savitribai Phule Pune University (SPPU), Pune, India

Abstract


Novel solubility enhancement technique; liquisolid compact technique is used in present research work. Ritonavir is poorly soluble drug was formulated using Avicel pH 102 and Aerosil 200 as carrier and coating material respectively. Solubility studies were conducted in different liquid vehicles, namely propylene glycol, span 20, PEG 400, tween 20, and PEG 200. From the result of saturation solubility study the liquisolid compacts were formulated using PEG 400 as non volatile vehicle. The ritonavir liquisolid formulations were obtained by allowing liquid vehicle with varying ritonavir concentration to get absorbed onto carrier and coating material taken at different ratio (R=5,10,15,20).Then the ritonavir liquisolid powder system evaluated for flow property determination and then compressed into tablet. Each batch of prepared ritonavir Liquisolid powder compact evaluated for Quality control tests, i.e. uniformity of tablet weight, uniformity of drug content, tablet hardness, friability test, disintegration and dissolution study. Optimized batch of Liquisolid powder compact evaluated for quality control test of tablet along with FTIR, DSC and PXRD study. The tableting properties of the liquisolid compacts were within the acceptable limits and in vitro drug release rate of LS compacts were distinctly higher as compared to directly compressible tablet and pure drug alone. This was due to an increase in wetting properties and surface of drug available for dissolution. FTIR study result indicates that there is no drug excipient interaction..DSC and PXRD study suggested loss of ritonavir crystallinity upon liquisolid formulation, it indicates that drug is held within the power substrate in a solubilized, almost molecularly dispersed state, which lead to enhanced drug solubility. From significant result of solubility of ritonavir, liquisolid technique would be promising solubility enhancement technique for various poorly soluble drugs.

Keywords


Ritonavir, Liquisolid Compact, PEG 400, Carrier Material, Coating Material, Poorly Water Soluble Drugs.

References