OPTIMIZATION OF FAST-DISSOLVING TABLETS OF CARVEDILOL USING 23 FACTORIAL DESIGN
DOI:
https://doi.org/10.22159/ijap.2024v16i1.49535Keywords:
Carvedilol, Factorial design, Superdisintegrant, Antihypertensive, In vivo studyAbstract
Objective: Optimization of carvedilol fast-dissolving tablets through a 23 factorial design employing starch hyaluronate as a new superdisintegrating agent.
Methods: The esterification method was used for producing starch hyaluronate. A direct compression process was used to develop carvedilol tablets utilizing a mix of starch hyaluronate (SH) as a novel superdisintegrant, crospovidone, and sodium starch glycolate. The prepared tablets are analyzed for physical characteristics, drug dissolution, in vivo pharmacokinetic, and stability studies.
Results: New superdisintegrant synthesized was a fine, free-flowing crystalline powder. In the DSC study, starch hyaluronate had no interaction with the drug. NMR and FTIR investigations supported the ester connection between starch and hyaluronic acid. CF2, the optimized formulation, had the shortest disintegration time of 26±2 seconds. The percentage of drugs dissolved in ten minutes from the optimized composition was 93.4±1.32%. The optimized composition achieved peak plasma concentration in a short time and demonstrated higher relative bioavailability for the drug.
Conclusion: A formula containing a 5% concentration of starch hyaluronate was optimized and has a proper potential for application in the formulation of rapidly disintegrating tablets, in addition to improving clinical obedience throughout the efficacious treatment of hypertension.
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Hiremath SP, Makanapur C. Formulation and evaluation of orodispersible tablets of a model anti-hypertensive drug. Int J Pharm Pharm Sci. 2017;9(10):34. doi: 10.22159/ijpps.2017v9i11.18967.
Bhide P, Nachinolkar R. Formulation development and characterisation of meclizine hydrochloride fast dissolving tablets using solid dispersion technique. Int J App Pharm. 2018;10(4):141. doi: 10.22159/ijap.2018v10i4.26493.
Jayapal N, Vamshi Vishnu Y. Formulation and in vivo evaluation of self-nanoemulsifying drug delivery system of ramipril in wistar rats. Asian J Pharm Clin Res. 2021;14(7):126-36. doi: 10.22159/ajpcr.2021.v14i7.42003.
Chauhan K, Solanki R, Sharma S. A review on fast dissolving tablet. Int J App Pharm. 2018;10(6):10(6):1. doi: 10.22159/ijap.2018v10i6.28134.
Radha GV, Sastri KT, Prathyusha P, Bhanu P, Rajkumar J. Formulation and evaluation of aceclofenac proniosome loaded orabase for management of dental pain. Int J App Pharm. 2018;10(6):204. doi: 10.22159/ijap.2018v10i6.29143.
Patel SS, Patel NM. Development of directly compressible co-processed excipient for dispersible tablets using 32 full factorial design. Int J Pharm Pharm Sci. 2009;1:125-48.
Hossain MS, Hossain MA, Anisuzzman M. Formulation development and evaluation of carvedilol tablet. Int Res J Pharm. 2013;4(8):96-100. doi: 10.7897/2230-8407.04816.
Jire DS, Gosavi NS, Badhe RB, Jagdale DH. Mouth dissolving tablet: a novel drug delivery system. Asian J Pharm Res. 2021;14:180-6. doi: 10.52711/2231-5691.2021.00033.
Prakash Rao AHO, Rada SK, Kandukuri S. Optimization of starch crotonate as a novel superdisintegrant in the formulation of fast dissolving tablets through 23 factorial design. Int J App Pharm. 2021;7:247-56. doi: 10.22159/ijap.2021v13i4.41335.
Kumar SR, Annu K. Design, optimization, and evaluation of acyclovir fast dissolving tablets employing starch phthalate–a novel superdisintegrant. Asian J Pharm Chem Res. 2019;7:132-42. doi: 10.22159/ajpcr.2019.v12i11.35474
Kumar RS, Yagnesh TNS, Kumar VG. Optimisation of ibuprofen fast dissolving tablets employing starch xanthate using 23 factorial design. Int J App Pharm. 2017;9(5):51. doi: 10.22159/ijap.2017v9i5.19707.
Preethi GB, Banerjee S, Shivakumar HN, Ravi Kumar M. Formulation of fast-dissolving tablets of doxazosin mesylate drug by direct compression method. Int J App Pharm. 2017;9(5):22. doi: 10.22159/ijap.2017v9i5.18168.
Chatwal GR, Anand SK. Instrumental methods of chemical analysis. 5th ed. Himalaya Publishing House; 2009. p. 2.49-51.
The United States Pharmacopoeia 29, national formulary 24, Asian edition. Rockville, MD: United States pharmacopoeia convention, Inc; 2006. p. 1890.
Aboud HM, El komy MH, Ali AA, El Menshawe SF, Abd Elbary A. Development, optimization, and evaluation of carvedilol-loaded solid lipid nanoparticles for intranasal drug delivery. AAPS PharmSciTech. 2016;17(6):1353-65. doi: 10.1208/s12249-015-0440-8, PMID 26743643.
Hazarika JNR, Deb P. Formulation evaluation and optimization of immediate release tablet of aceclofenac by direct compression method. Int J Curr Pharm Sci 2017;9(3). doi: 10.22159/ijcpr.2017.v9i3.19972.
Preethi GB, Banerjee S, Shivakumar HN, Ravi Kumar M. Formulation of fast-dissolving tablets of doxazosin mesylate drug by direct compression method. Int J App Pharm. 2017;9(5):22. doi: 10.22159/ijap.2017v9i5.18168.
Subhashis D, Gampa VK, Satyanarayana SV. Preparation and evaluation of solid dispersion of terbinafine hydrochloride. Asian J Pharm Technol. 2013;3:9-15.
Karakucuk A, Celebi N, Teksin ZS. Preparation of ritonavir nanosuspensions by microfluidization using polymeric stabilizers: I. A Design of experiment approach. Eur J Pharm Sci. 2016;95:111-21. doi: 10.1016/j.ejps.2016.05.010, PMID 27181836.
Anusha K, Rada S. Oral disintegrating tablets: best approach for faster therapeutic action of poorly soluble drugs. Egypt Pharmaceut J. 2021;20(2). doi: 10.4103/epj.epj_63_20.
Marshall K, Lachman L, Liberman H, Kanig J. The theory and practice of industrial pharmacy. 3rd ed. India: Varghese publishing house; 1987. p. 66-99, 293-345.
Deliang Gu LH. A novel approach to formulate and optimize orally disintegrating tablets of bambuterol hydrochloride. Pharmaceut Anal Acta. 2013;4(3). doi: 10.4172/2153-2435.1000216.
Malaquias LFB, Sa-Barreto LCL, Freire DO, Silva ICR, Karan K, Durig T. Taste masking and rheology improvement of drug complexed with beta-cyclodextrin and hydroxypropyl-β-cyclodextrin by hot-melt extrusion. Carbohydr Polym. 2018;185:19-26. doi: 10.1016/j.carbpol.2018.01.011, PMID 29421056.
Pabari RM, Ramtoola Z. Application of face centred central composite design to optimise compression force and tablet diameter for the formulation of mechanically strong and fast disintegrating orodispersible tablets. Int J Pharm. 2012;430(1-2):18-25. doi: 10.1016/j.ijpharm.2012.03.021, PMID 22465631.
Abdelbary AA, Li X, El-Nabarawi M, Elassasy A, Jasti B. Comparison of nanomilling and coprecipitation on the enhancement of in vitro dissolution rate of poorly water-soluble model drug aripiprazole. Pharm Dev Technol. 2014;19(4):491-500. doi: 10.3109/10837450.2013.800107, PMID 23731085.
Jaya S, Amala V. Formulation and in vitro evaluation of oral disintegrating tablets of amlodipine besylate. Int J App Pharm. 2019;11(1):49. doi: 10.22159/ijap.2019v11i1.28457.
Kumari A, Kumar RS. Synthesis and characterization of starch malonate: development of fast dissolving tablets of aceclofenac by 23 factorial designs. Int J App Pharm. 2021;13(3):87-102. doi: 10.22159/ijap.2021v13i3.40538.
Malode LL, Atram SC, Patil SR, Talwekar PD. Formulation and evaluation of natural gum based fast dissolving tablet. AJPTR. 2020;10(1):211-20. doi: 10.46624/ajptr.2020.v10.i1.016.
Parfati N, Rani KC, Charles N, Geovany V. Preparation and evaluation of atenolol-β-cyclodextrin orally disintegrating tablets using co-process crospovidone-sodium starch glycolate. Int J App Pharm. 2018;10(5):190. doi: 10.22159/ijap.2018v10i5.27982.
Aboud HM, El komy MH, Ali AA, El Menshawe SF, Abd Elbary A. Development, optimization, and evaluation of carvedilol-loaded solid lipid nanoparticles for intranasal drug delivery. AAPS PharmSciTech. 2016;17(6):1353-65. doi: 10.1208/s12249-015-0440-8, PMID 26743643.
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