International Journal of Drug Delivery Technology
Volume 15, Issue 2

Development and Evaluation of Dispersible Tablet comprising Tenofovir, Bictegravir and Emtricitabine 

Nitin Mehetre, Inderbir Singh*

Chitkara College of Pharmacy, Chitkara University, Rajpura 140401, Punjab, India 

Received: 30th Nov, 2024; Revised: 21st Mar, 2025; Accepted: 4th Apr, 2025; Available Online: 25th Jun, 2025 

ABSTRACT

Maximum Anti-HIV Drugs Dosage Forms are available as tablets or capsule dosage forms. Such Dosage Forms are not suitable for patient who is having difficulty to swallowing. Antiretroviral therapy for treatment of HIV Infection contains more than two drugs so dose of drugs are more and most of these drugs are having issues like high bitterness, low solubility, highly moisture sensitivity and drugs incompatibility issue so to formulate HIV drugs into dispersible tablet is challenging. In present research, fixed dose combination of Tenofovir, Bictegravir and Emtricitabine were used to formulate the dispersible bilayer tablet. Bictegravir sodium is BCS class II drug hence with this drug eight different formulation for solubility enhancement was performed. All the physicochemical parameters were evaluated for the granules, Dissolution, assay for the granules were determined. For second layer of Tenofovir, and Emtricitabine, disintegrant concentration was optimized with three different formulations and evaluation was done like flow properties of granules, DT, assay and dissolution. All the results were compared with the marketed product. The formulation F10 showed desirable DT, assay, and dissolution hence it was selected as best formulation.

Keywords: Bictegravir, Emtricitabine, Tenofovir, Anti-cancer Drugs, Dispersible tablet.

How to cite this article: Nitin Mehetre, Inderbir Singh. Development and Evaluation of Dispersible Tablet comprising Tenofovir, Bictegravir and Emtricitabine. International Journal of Drug Delivery Technology. 2025;15(2):605-19. doi: 10.25258/ijddt.15.2.30

REFERENCES

  1. Hannan PA, Khan JA, Khan A, Safiullah S. Oral dispersible system: A new approach in drug delivery system. Indian journal of pharmaceutical sciences. 2016; 78(1):2. doi: 10.4103/0250-474x.180244
  2. Nandhini J, Rajalakshmi A. Dispersible tablets: A review. Journal of Pharmaceutical Advanced Research. 2018; 1(3):148-155. DOI:10.36648/0975-9344.22.1.171
  3. Kumar N, Pahuja S. Dispersible Tablets: An Overview. Journal of Medical Pharmaceutical and Allied Sciences. 2019; 8:2183-2199.
  4. Teżyk M, Milanowski B, Ernst A, Lulek J. Recent progress in continuous and semi-continuous processing of solid oral dosage forms: a review. Drug development and industrial pharmacy. 2016;2;42(8):1195-1214. DOI:10.3109/03639045.2015.1122607
  5. A. AlHusban F, M. El-Shaer A, J. Jones R, R. Mohammed A. Recent patents and trends in orally disintegrating tablets. Recent Patents on Drug Delivery & Formulation. 2010;1;4(3):178-197.
  6. Fulco PP. Crushed bictegravir/emtricitabine/tenofovir alafenamide in a human immunodeficiency virus–positive patient with esophageal cancer. American Journal of Health-System Pharmacy. 2020;1; 77(7):509-510. https://doi.org/10.1093/ajhp/zxaa017
  7. Preethi S, Jain V. Formulation and evaluation of an emtricitabine adjustable pediatric anti-retroviral dosage form. Drug Invention Today. 2019;16;12.
  8. Ray AS, Fordyce MW, Hitchcock MJ. Tenofovir alafenamide: a novel prodrug of tenofovir for the treatment of human immunodeficiency virus. Antiviral research. 2016; 1; 125:63-70. https://doi.org/10.1016/j.antiviral.2015.11.009
  9. Shiyani B, Gattani S, Surana S. Formulation and evaluation of bi-layer tablet of metoclopramide hydrochloride and ibuprofen. Aaps Pharmscitech. 2008; 9(3):818-827. doi: 10.1208/s12249-008-9116-y.
  10. Thompson KC, Kaighn KN, Mukherjee IN, Diimmler CE, Weiser HT, Mancinelli C, inventors; Merck Sharp, Dohme LLC, assignee. Taste-Masked Formulations of Raltegravir. United States patent application US 16/220,064. 2019;6.
  11. Arifa B., Rajini G.Formulation and Evaluation of Taste Masked Oro-dispersible Tablets of an Anti-HIV Drug.International Journal of Pharmaceutical Sciences Review and Research, 2018; 51 (1):76-83.
  12. Pawar DS, Surawase RK. Enhancement of Solubility and Dissolution Rate of Carvedilol by Using Fluidized-bed Granulation Technique.2020; 27, 179-186. DOI: 10.47583/ijpsrr.2020.v65i01.027
  13. Dhoble P, Tekade B, Gorde N, Bodke V. Solubility Enhancement of BCS Class II Antibiotic (Azithromycin) by Solid Dispersion Technique by Using Skimmed Milk. 2024; 14(3):1728-1735. DOI:25258/ijddt.14.3.68
  14. Wadke DA, Serajuddin AT, Jacobson H. Preformulation testing. Pharmaceutical dosage forms: Tablets. 1989;5;1:1-73. https://doi.org/10.1021/js980434g
  15. Takahashi AI, Lourenço FR, Duque MD, Consiglieri VO, Ferraz HG. Using fluid bed granulation to improve the dissolution of poorly water-soluble drugs. Brazilian Archives of Biology and Technology. 2012; 55:477-84. DOI:1590/S1516-89132012000300020