DRUG EXCIPIENT ADSORPTION TECHNIQUE FOR THE PREPARATION OF LOW-DOSE TABLETING
DOI:
https://doi.org/10.22159/ijap.2024v16i5.50991Keywords:
Low-dose tablet, Cetirizine, DAF, Content uniformity, FTIR.Abstract
Objective: This study aimed to improve drug mixability and drug uniformity in low-dose tablet by developing a stable easily mixable drug adsorbed filler.
Methods: The research involved adsorbing drug on filler by using three solvents and drug-to-excipient ratios of 1:50 and 1:75. This drug adsorbed fillers (DAF), drug content uniformity and flow properties were characterized which are crucial for accurate dosing and manufacturing.
Results: Formulations T1 and T2 and T3 showed similar flow properties, including bulk and tapped densities, Carr's indices, and Hausner ratios. T1 had better flowability with a lower angle of repose (23.97 degrees) than T2 (35.42 degrees), T3 (49 degrees), and T4 (39 degrees) and higher drug uniformity (99.89%, 99.54%, 97.12%, 96.83%). Tablet evaluations of TS1, TS2, TS3, TS4 met standard weight variation, friability, and hardness criteria, with TS1 showing a quicker disintegration time (2:58, 3:10, 3:15, 4), indicating faster dissolution and potentially better bioavailability. Dissolution tests showed both exceeded 85% drug release in 30 minutes, with TS1 achieving a higher release (99.98, 99.91%, 98.11%, 97.64%), suggesting more efficient drug release.
Conclusion: The drug adsorbed filler premix technique effectively ensures drug content uniformity and improves low-dose drug mixing, contributing to the development of safe, efficient low-dose pharmaceuticals.
Downloads
References
Alqahtani MS, Kazi M, Alsenaidy MA, Ahmad MZ. Advances in Oral Drug Delivery. Front Pharmacol. 2021;12:618411. doi: 10.3389/fphar.2021.618411, PMID:33679401; PMCID:PMC7933596.
Alyami H, Dahmash E, Bowen J, Mohammed AR. An investigation into the effects of excipient particle size, blending techniques and processing parameters on the homogeneity and content uniformity of a blend containing low-dose model drug. PloS one. 2017;12(6). doi: 10.1371/journal.pone.0178772.
N A Orr, E A Sallam, Content uniformity of potent drugs in tablets. Journal of Pharmacy and Pharmacology.1978;30(1)741–747. doi: 10.1111/j.2042-7158.1978.tb13384.
Kai, Shiino., Takao, Oshima., Ryoichi, Sonoda., Shin-ichiro, Kimura., Shigeru, Itai., Yasunori, Iwao. Controlled-Release Fine Particles Prepared by Melt Adsorption for Orally Disintegrating Tablets. Chemical & Pharmaceutical Bulletin. 2019;67(10):1152-1159. doi: 10.1248/CPB.C19-00554.
Kukkar V, Anand V, Kataria M, Gera M, Choudhury PK. Mixing and formulation of low dose drugs: underlying problems and solutions. Thai J Pharm Sci. 2008;32(3-4):43-58.
Gopinath R, Naidu RA. Pharmaceutical preformulation studies–current review. International Journal of Pharmaceutical and Biological Archives. 2011;2(5):1391-400.
Young JC. True melting point determination. The Chemical Educator. 2013;18:203-8.
Raj SS, Bindu M, Ramyashree D, Sowmya KN. Spectrophotometric method for the estimation of cetirizine hydrochloride in pharmaceutical preparation. Asian Journal of Pharmaceutical Analysis. 2020;10(4):185-8. doi: 10.5958/2231-5675.2020.00034.4.
Nimje HM, Oswal RJ, Kshirsagar SS, Chavan M. Spectrophotometric analysis for estimation of felodipine in tablet dosage form by calibration curve method. Research Journal of Pharmacy and Technology. 2011;4(12):1805-6.
Khan MI, Murtaza G, Awan S, Iqbal M, Waqas MK, Rasool A, Fatima U, Asad MH, Kahlid A, Usman F, Najam-us-Saqib Q. Development and validation of stability indicating assay method of cetirizine hydrochloride by HPLC. African Journal of Pharmacy and Pharmacology. 2011;5(2):143-9. doi: 10.5897/AJPP10.283.
Aigner Z, Heinrich R, Sipos E, Farkas G, Ciurba A, Berkesi O, Szabó-Révész P. Compatibility studies of aceclofenac with retard tablet excipients by means of thermal and FT-IR spectroscopic methods. Journal of thermal analysis and calorimetry. 2011;104(1):265-71. Doi: 10.1007/s10973-010-1105-1.
Van Nguyen H, Park C, Oh E, Lee BJ. Improving the dissolution rate of a poorly water-soluble drug via adsorption onto pharmaceutical diluents. Journal of Drug Delivery Science and Technology. 2016;35:146-54. doi: 10.1016/j.jddst.2016.05.008.
Shah, R.B., Tawakkul, M.A. & Khan, M.A. Comparative Evaluation of Flow for Pharmaceutical Powders and Granules. AAPS PharmSciTech 9. 2008;9:250–258. doi: 10.1208/s12249-008-9046-8.
Youness D, Hosseinpoor M, Yahia A, Tagnit-Hamou A. Flowability characteristics of dry supplementary cementitious materials using Carr measurements and their effect on the rheology of suspensions. Powder technology. 2021;378:124-44. doi: 10.1016/j.powtec.2020.09.064.
Saw HY, Davies CE, Paterson AH, Jones JR. Correlation between powder flow properties measured by shear testing and Hausner ratio. Procedia engineering. 2015;102:218-25. doi: 10.1016/j.proeng.2015.01.132.
Geldart D, Abdullah EC, Hassanpour A, Nwoke LC, Wouters IJ. Characterization of powder flowability using measurement of angle of repose. China Particuology. 2006;4(3-4):104-7. doi: 10.1016/S1672-2515(07)60247-4.
Muselík J, Franc A, Doležel P, Goněc R, Krondlová A, Lukášová I. Influence of process parameters on content uniformity of a low dose active pharmaceutical ingredient in a tablet formulation according to GMP. ActaPharmaceutica. 2014;64(3):355-67. doi: 10.2478/acph-2014-0022.
Chen H, Aburub A, Sun CC. Direct compression tablet containing 99% active ingredient—a tale of spherical crystallization. Journal of pharmaceutical sciences. 2019;108(4):1396-400. doi: 10.1016/j.xphs.2018.11.015.
Wahl PR, Peter A, Wolfgang M, Khinast JG. How to measure coating thickness of tablets: Method comparison of optical coherence tomography, near-infrared spectroscopy and weight-, height-and diameter gain. European Journal of Pharmaceutics and Biopharmaceutics. 2019;142:344-52. doi: 10.1016/j.ejpb.2019.06.021.
Patel H, Desai C, Thaker A. Statistical process control as a tool to control weight uniformity of tablets. Journal of Pharmacy and Applied Sciences. 2015;2(1):9
Seitz JA, Flessland GM. Evaluation of the physical properties of compressed tablets I: Tablet hardness and friability. Journal of pharmaceutical sciences. 1965;54(9):1353-7. doi: 10.1002/jps.2600540926.
Zhao H, Yu Y, Ni N, Zhao L, Lin X, Wang Y, Du R, Shen L. A new parameter for characterization of tablet friability based on a systematical study of five excipients. International Journal of Pharmaceutics. 2022;611:121339. doi: 10.1016/j.ijpharm.2021.121339.
Silva DA, Webster GK, Bou-Chacra N, Löbenberg R. The significance of disintegration testing in pharmaceutical development. Dissolution Technol. 2018;25(3):30-8. doi: 10.14227/DT250318P30.
Goodhart FW, McCoy RH, Ninger FC. New in vitro disintegration and dissolution test method for tablets and capsules. Journal of Pharmaceutical Sciences. 1973;62(2):304-10. doi: 10.1002/jps.2600620227.
McCullough JP, Waddington G. Melting-point purity determinations: Limitations as evidenced by calorimetric studies in the melting region. Analytica Chimica Acta. 1957;17:80-96. doi: 10.1016/S0003-2670(00)87001-4.
S. Subramanya Raj Urs, Bindu M., Ramyashree D., Sowmya K. N. Spectrophotometric method for the Estimation of Cetirizine Hydrochloride in Pharmaceutical preparation. Asian J. Pharm. Ana. 2020; 10(4):185-188. doi: 10.5958/2231-5675.2020.00034.4.
Wamorkar V, Manjunath S, Varma MM. Development and validation of UV spectroscopic method for determination of metoclopramide hydrochloride in bulk and tablet formulation. Int J Pharm Pharm Sci. 2011;3(3):171-4.
Lashkarbolooki M, Hezave AZ. Comparison between Modeling of Cetirizine Solubility Using Different Approaches: Semi-Empirical Density Based Correlations vs. Peng-Robinson EoS. Open Access Library Journal. 2015;2(9):1-6. doi: 10.4236/oalib.1101715.
Segall AI. Preformulation: The use of FTIR in compatibility studies.
Van Nguyen H, Park C, Oh E, Lee BJ. Improving the dissolution rate of a poorly water-soluble drug via adsorption onto pharmaceutical diluents. Journal of Drug Delivery Science and Technology. 2016;35:146-54. doi: 10.1016/j.jddst.2016.05.008.
Emery EM. Flow properties of selected pharmaceutical powders (Doctoral dissertation, University of Saskatchewan.
Zaid AN, Rowa’J AR, Ghoush AA, Qaddumi A, Zaaror YA. Weight and content uniformity of lorazepam half-tablets: A study of correlation of a low drug content product. Saudi Pharmaceutical Journal. 2013;21(1):71-5. doi: 10.1016/j.jsps.2011.12.009.
Bushra R, Shoaib MH, Aslam N, Hashmat D, Rehman M. Formulation development and optimization of ibuprofen tablets by direct compression method. Pak. J. Pharm. Sci. 2008;21(2):113-20.
Chaturvedi H, Garg A, Rathore US. Post-compression evaluation parameters for tablets-an overview. Eur J Pharm Med Res [Internet]. 2017;4(11):526-30.
Singhvi G, Singh M. In-vitro drug release characterization models. Int J Pharm Stud Res. 2011;2(1):77-84.
Qothrunnadaa, t., & hasanah, a. N. (2021). Patches for acne treatment: an update on the formulation and stability test. International Journal of Applied Pharmaceutics. 2021;13(4), 21–26. doi: 10.22159/ijap.2021.v13s4.43812.
Nurdianti, l., clara, r., suhendy, h., setiawan, f., & idacahyati, k. (2021). Formulation, characterization, and determination of the diffusion rate study of antioxidant serum containing astaxanthin nanoemulsion. International Journal of Applied Pharmaceutics, 2021;13(4), 200–204. doi: 10.22159/ijap.2021.v13s4.43859.
Damle, m. C., r. R. Pardeshi, and s. R. Bidkar. “development and validation of stability indicating hptlc method for pimavanserin tartrate”. International Journal of Pharmacy and Pharmaceutical Sciences. 2023;15(10),17-23. doi: 10.22159/ijpps.2023v15i10.48820.
Silva, l. P. D. A., and e. M. Boldo. “optimization of albendazole 400 mg tablet compression process using design of experiment (doe) approach”. International Journal of Pharmacy and Pharmaceutical Sciences. 2021;13(2),1-6. doi: 10.22159/ijpps.2021v13i2.40382.
Published
How to Cite
Issue
Section
Copyright (c) 2024 Arun Radhakrishnan, NIKHITHA KS, RAMYA G
![Creative Commons License](http://i.creativecommons.org/l/by/4.0/88x31.png)
This work is licensed under a Creative Commons Attribution 4.0 International License.