SOLID DISPERSION TECHNIQUE TO ENHANCE THE SOLUBILITY AND BIOAVAILABILITY OF TELMISARTAN AND HYDROCHLOROTHIAZIDE

Main Article Content

Vaishali. Madhukar Vaidya
Dr. Deshraj Shyamkant Chumbhale

Keywords

Telmisartan and hydrochlorothiazide, solid dispersions, PEG 6000 and Gelucire 50/13

Abstract

Objectives: The main objective of the present investigation to develop and evaluate solid dispersions of BCS Class II drugs Telmisartan and hydrochlorothiazide employing various polymers, compatible with conventional manufacturing method to enhance solubility of poorly soluble drugs


Materials and Methods: In this study, Telmisartan and hydrochlorothiazide solid dispersion were prepared using PEG 6000 and Gelucire 50/13 by solvent evaporation method. Solid dispersions and pure Telmisartan in the form of powder were characterized in comparison with pure drug and corresponding physical mixtures in the same ratios by Fourier transform infrared spectroscopy, differential scanning calorimetry (DSC), powder X-ray diffractogram, and in vitro drug release.


Results: SD formulation of both drug Telmisartan and hydrochlorothiazide was prepared by using two different carrier like PEG 6000 and Gelucire 50/13 in 1:1, 1:3, 1:5 and 1:7 drug to polymer ratio by solvent evaporation method & selected for characterization. The DSC study indicated that the crystalline nature of Telmisartan and hydrochlorothiazide was reduced to amorphous. The diffraction pattern of the solid dispersions in each figure indicates that diffraction peaks at 2ɵ values has less intensity than that of pure drugs. This indicated that the crystalline nature of drug sample was converted to amorphous. Scanning electron microscope photographs of solid dispersion seem to be more porous in nature. From the in vitro drug release profile, it can be seen that formulation PSD3 shows higher dissolution rate i.e. 97.54±2.87% compared with other formulations. It is predicted that, increasing concentration of carrier, increases the drug dissolution rate.


Conclusion: This study has shown that the solid dispersion of Telmisartan and hydrochlorothiazide using carrier can be promising formulation for solubility and dissolution enhancement. Synthetic polymers used have shown promising results in the modification of drug release from the formulations

Abstract 113 | pdf Downloads 102

References

1. Zeng Q, Ou L, Zhao G, Cai P, Liao Z, Dong W and Liang X (2020). Preparation and Characterization of PEG4000 Palmitate/PEG8000 Palmitate-Solid Dispersion Containing the Poorly Water-Soluble Drug Andrographolide. Advances in Polymer Technology, 4239207.
2. Xi Z, Zhang W, Fei Y, Cui M, Xie L, Chen L and Xu L (2020). Evaluation of the Solid Dispersion System Engineered from Mesoporous Silica and Polymers for the Poorly Water Soluble Drug Indomethacin: In Vitro and In Vivo. Pharmaceutics., 12: 144.
3. Alshehri S, Imam SS, Altamimi MA, Hussain A, Shakeel F, Elzayat E, Mohsin K, Ibrahim M, Alanazi F (2020). Enhanced Dissolution of Luteolin by Solid Dispersion Prepared by Different Methods: Physicochemical Characterization and Antioxidant Activity. ACS Omega., 5: 6461 - 6471.
4. Yu JY, Kim JA, Joung HJ, Ko JA and Park HJ (2020). Preparation and characterization of curcumin solid dispersion using HPMC. Journal of Food Science., 85(11): 3866-3873.
5. Chavan RB, Lodagekar A, Yadav B and Shastri NR (2020). Amorphous solid dispersion of nisoldipine by solvent evaporation technique: preparation, characterization, in vitro, in vivo evaluation, and scale up feasibility study. Drug Delivery and Translational Research., (10): 903–918.
6. Qushawy M, Nasr A, Swidan S and Mortag Y (2020). Development and Characterization of Glimepiride Novel Solid Nanodispersion for Improving Its Oral Bioavailability. Sci. Pharm., 88(4): 52.
7. Chouhan M, Gupta D, Choukse R and Maheshwari RK (2019) Formulation and evaluation fast dissolving tablets of lovastatin using solid dispersion method. Journal of Drug Delivery & Therapeutics., 9(2-A):29-31.
8. Mohammadi H and Kumar VH (2019) Formulation and Evaluation of Solid Dispersion Incorporated Fast Disintegrating Tablets of Tenoxicam Using Design of Experiment. International Journal of Pharmaceutical Sciences and Drug Research., 11(1): 35-44.
9. Vimalson DC, Parimalakrishnan S, Jeganathan NS and Anbazhagan S (2019). Solid dispersion technique to enhance the solubility and dissolution of febuxostat an BCS Class II drug. Int J App Pharm., 11(1): 241-246.
10. Paul AD, Vinay J and Rajyalakshmi KG (2019). Formulation Design for Poorly Water-Soluble Drug by Using Solid Dispersion of Telmisartan for Solubility and Dissolution Rate Enhancement. Glob J Pharmaceu Sci., 7(3): 555716.
11. Colombo M, Melchiades GL, Michels LR, Figueiró F, Bassani VL, Teixeira HF and Koester LS (2019). Solid Dispersion of Kaempferol: Formulation Development, Characterization and Oral Bioavailability Assessment. AAPS PharmSciTech., 20(3):106.
12. Shirsath NR, Jagtap V and Goswami AK (2019). Formulation and Development of Famotidine Solid Dispersion Tablets for their Solubility Enhancement. Indian Journal of Pharmaceutical Education and Research., 53 (4): 548-553.
13. Dhere M, Majumdar A and Malviya N (2019). Formulation And Evaluation Of Hydrotropic Solid Dispersion Of Eluxadoline. IJPSR., 10(12): 5450-5454.
14. Choudhary H, Yadav B, Patel P, Das P and Pillai S (2019). Formulation and Evaluation of Ramipril Fast Dissolving Tablet using Solid Dispersion. Research J. Pharm. and Tech., 12(8): 3764-3772.
15. Dos Santos KM, Barbosa RM, Vargas FGA, de Azevedo EP, Lins ACDS, Camara CA, Aragão CFS, Moura TFLE and Raffin FN (2018). Development of solid dispersions of β-lapachone in PEG and PVP by solvent evaporation method. Drug Dev Ind Pharm., 44(5):750-756.
16. Christopher VD, Parimalakrishnan S, Jeganathan NS and Anbazhagan S (2018). Enhancement of Solubility And Dissolution Characteristics Of Fenofibrate By Solid Dispersion Technique. Int. Res. J. Pharm., 9(10): 145-150.
17. Sankari T and Hariri S (2018). Preparation and characterization of cefuroxime axetil solid dispersions using poloxamer 188. Braz. J. Pharm. Sci., 54(4):e17644.
18. Laxmi Raj A and Kumar YS (2018). Preparation and Evaluation of Solid Dispersion of Nebivolol Using Solvent Evaporation Method. International Journal of Pharmaceutical Sciences and Drug Research., 10(4): 322-328
19. Sarangi MK and Singh N (2018). A Comparative Study of Solubility Enhancement of Aceclofenac by Solid Dispersion Technique Using Several Polymers. J Appl Pharm., 10(1); 1000259.