AN EXPERIMENTAL DESIGN IN THE OPTIMIZATION OF VARIOUS TABLET EXCIPIENT FORMULATIONS = A CONCISE REVIEW

IYAN SOPYAN; RETNO WAHYUNINGRUM; INSAN SUNAN K. S.

doi:10.22159/ijap.2022v14i1.43380

Authors

IYAN SOPYAN Department of Pharmaceutical and Technology of Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran, Bandung, Indonesia, Study Center of Dosage Form Development, Faculty of Pharmacy, Universitas Padjadjaran, Bandung, Indonesia https://orcid.org/0000-0001-7616-5176
RETNO WAHYUNINGRUM Department of Pharmacy, Faculty of Science and Technology, Universitas Sembilanbelas November, Kolaka, Indonesia https://orcid.org/0000-0001-7616-5176
INSAN SUNAN K. S. Department of Pharmaceutical and Technology of Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran, Bandung, Indonesia

DOI:

https://doi.org/10.22159/ijap.2022v14i1.43380

Keywords:

Tablet, Excipient, Matrics, Formulation, QBD

Abstract

The use of an experimental design technique in the development of various pharmaceutical preparations, including tablet preparations, has become the latest trend. Because of their ease of use, tablet formulations are popular among both producers and patients. To increase the usage of tablets in diverse circles and settings, researchers are working to develop a variety of tablet excipients for various functions. Fast dissolving tablets (FDT), effervescent tablets, modified-release tablets, oral mucoadhesive tablets, gastroretentive tablets, and colon targeted tablets are some of the tablet formats that have been developed in addition to traditional tablets. This review will look at how formulation optimization in tablet preparations has been done during the previous ten years using specific literacies. The articles for this review were found using the keywords tablet, excipient, matrices, formulation, and QBD in specialized databases such as Elsevier, Pubmed, and Cambridge. Other options include Springer publications, material from the Internet, and articles published online by The Lancet Respiratory Medicine, Medscape, and Statpearls. The formulation design strategy is based on the experimental design approach carried out on the kind of tablet preparation, which has distinct important quality parameters.

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References

Singh S, Prajapati K, Pathak AK, Mishra A. Formulation and evaluation of floating tablet of captopril. Int J PharmTech Res. 2011;3:333-41.

Natoli D, Levin M, Tsygan L, Liu L. Development, optimization, and scale-up of process parameters: tablet compression. In: Developing solid oral dosage forms. Elsevier; 2017. p. 917-51.

Pratiwi PD, Nugroho AK, Lukitaningsih E. Optimasi tablet lepas cepat levofloksasin hidroklorida menggunakan crospovidone sebagai disintegran dan studi disolusi efisiensi. Majalah Farmaseutik. 2020;16(1):58-63. doi: 10.22146/farmaseutik.v16i1.48352.

Akhtar MF, Hanif M, Majeed A, Shah S. Formulation development and optimization of captopril containing tablets through Box-Behnken design. Lat Am J Pharm. 2018;37:1414-23.

Alpizar Ramos S, Gonzalez-de la Parra M. Application of the sequential design of experiments to develop ibuprofen (400 mg) tablets by direct compression. Asian J Chem Pharm Sci. 2017;2:10-5.

Bajwa PS, Sharma J, Bhargava A, Sharma S, Sharma AR, Raina BR. Design and development of immediate-release tablets of terbutaline sulfate using 32 full factorial statistical design. APJHS. 2018;5(1):47-52. doi: 10.21276/apjhs.2018.5.1.11.

Damayanti D, Sari IP, Sulaiman TNS, Bestari AN, Setiawan IM. The formulation of pacing (Costus speciosus) extracts tablet by using Avicel®Ph 200 as filler-binder and amylum as disintegration agent. Indonesian J Pharm. 2018;29(1). doi: 10.14499/indonesianjpharm29iss1pp29.

Huq T, Vu KD, Riedl B, Bouchard J, Han J, Lacroix M. Development of probiotic tablet using alginate, pectin, and cellulose nanocrystals as excipients. Cellulose. 2016;23(3):1967-78. doi: 10.1007/s10570-016-0905-2.

Hadisoewignyo L, Soegianto L, Ervina M, Wijaya I, Santoso SD, Tania N. Formulation development and optimization of tablet containing a combination of Salam (Syzygium Polyanthum) and Sambiloto (Andrographis paniculata) ethanolic extracts. Int J Pharm Pharm Sci. 2016;8:267-73.

Prapajati DB, Rao MS, Barot MT. Development, optimization and evaluation of liquisolid compact tablet of aripiprazole by using factorial design. Int J Pharmacol Res. 2020;12.

Tong Y, Zhang P, Dang L, Wei H. Monitoring of cocrystallization of ethenzamide–saccharin: insight into the kinetic process by in situ Raman spectroscopy. Chem Eng Res Des. 2016;109:249-57. doi: 10.1016/j.cherd.2016.01.032.

Dhaval M, Jalpa M, Ramesh P, Kalpesh P, Jayant C. Formulation, evaluation and optimization of the felodipine nanosuspension to be used for direct compression to tablet for in vitro dissolution enhancement. Pak J Pharm Sci. 2016;29:1927-36.

Ainurofiq A, Choiri S. The interaction of a binary/ternary interactive mixture of hydrophobic-hydrophilic materials on the drug distribution and drug release performance in the tablet formulation. IOP Conf Ser: Mater Sci Eng. 2017;176. doi: 10.1088/1757-899X/176/1/012006.

Asif M, Yasir M, Bhattacharya A, Bajpai M. Formulation and evaluation of gastroretentive dosage form for fluvastatin sodium. Pharm Glob Int J Comp Pharm. 2010;1:1-4.

Bushra R, Shoaib MH, Ali H, Zafar F, Naeem MI, Aslam N. Formulation design and optimization of aceclofenac tablets (100 mg) using central composite design with response surface methodology. Latin American Journal of Pharmacy. 2014;33:1009-18.

Hanif M, Abbas G. pH-responsive alginate–pectin polymeric rafts and their characterization. Adv Polym Technol. 2018;37(5):1496-506. doi: 10.1002/adv.21808.

Kushare SS, Gattani SG. Design and development of a microwave generated lactose monohydrate-microcrystalline cellulose-based multifunctional excipient composites for tablet formulation using box–Behnken design. J Drug Deliv Ther. 2019;9:1-17.

Oh DJ, Lee BC, Hwang SJ. Solubility of simvastatin and lovastatin in mixtures of dichloromethane and supercritical carbon dioxide. J Chem Eng Data. 2007;52(4):1273-9. doi: 10.1021/je700019h.

Farahiyah D, Sulaiman TNS. Pengaruh kombinasi superdisintegrant crospovidone dan croscarmellose sodium pada sifat fisik dan disolusi fast disintegrating tablet hidroklorotiazid. Maj Farm. 2020;17:140-7.

Lestari ABS, Fudholi A, Nugroho AK, Setyowati EP. Formula optimization of fast disintegrating tablet (FDT) of Centella asiatica (L.) Urb. ethanolic Extract. J Ilmu Kefarmasian Indones. 2018;16:94-9.

Wulandari RS, Fudoli A, Herowati R. Optimasi formula Fdt natrium diklofenak dengan kombinasi Ssuperdisintegrant primojel®, primellose® dan komponen effervescent dengan metode simplex lattice design. Chmk Pharmaceutical Scientific Journal 2019;2:39-47.

Dave V, Yadav RB, Ahuja R, Yadav S. Formulation design and optimization of novel fast dissolving tablet of chlorpheniramine maleate by using lyophilization techniques. Bull Fac Pharm Cairo Univ. 2017;55(1):31-9. doi: 10.1016/j.bfopcu.2016.12.001.

Kumar RK, Diskin Posner I, Goldberg I. Solid-state supramolecular chemistry of porphyrins. Ligand-bridged tetraphenylmetalloporphyrin dimers. J Inclus Phenom Macrocyclic Chem. 2000;37(1):219-30. doi: 10.1023/A:1008118119529

Tafere C, Yilma Z, Abrha S, Yehualaw A. Formulation, in vitro characterization and optimization of taste-masked orally disintegrating co-trimoxazole tablet by direct compression. PLOS ONE. 2021;16(3):e0246648. doi: 10.1371/ journal.pone.0246648, PMID 33725014.

Sarfaraz M, Dhruv RK, Doddayya H, KAA K. Factorial design based optimization of hydroxyzine hydrochloridef dissolving tablets. Indian J Pharm Sci. 2020;82:797-808.

Maroof K, Zafar F, Ali H, Shah SN, Bushira R, Naveed S. Development and optimization of fast dispersible flurbiprofen 100 mg tablets by central composite design. Lat Am J Pharm. 2016;35:685-94.

Mali KK. Design and optimization of modified tamarind gum-based floating-bioadhesive tablets of verapamil hydrochloride. Asian J Pharm. 2016;10(4):239-50. Doi: 10.22377/ ajp.v10i04.862

Okhuelegbe ES, Osayande EP, Amara IM. Optimization of disintegrant blends using box behnken design in the formulation of fast disintegrating tablets of diclofenac sodium. Niger J Pharm Appl Sci Res. 2017;6:1-7.

Kadry H. Formulation and optimazation of verdenavil hydrochloride oral disintegrating tablet: effect of superdisntegran. Al-Azhar J Pharm Sci. 2016;53:39-57.

Mohamed S, Tocher DA, Price SL. Computational prediction of salt and cocrystal structures-does a proton position matter? Int J Pharm. 2011;418(2):187-98. doi: 10.1016/j.ijpharm.2011.03.063, PMID 21497185.

Taymouri S, Mostafavi A, Javanmardi M. Formulation and optimization of effervescent tablet containing bismuth sub-citrate. J Rep Pharma Sci. 2019;8(2):236. doi: 10.4103/jrptps.JRPTPS_11_19.

Mahapatra APK, Saraswat R, Botre M, Paul B, Prasad N. Application of response surface methodology (RSM) in statistical optimization and pharmaceutical characterization of a patient compliance effervescent tablet formulation of antiepileptic drug levetiracetam. Future J Pharm Sci. 2020;6:1-14.

Manwar J, Kumbhar DD, Bakal R, Baviskar S, Manmode R. Response surface based co-optimization of release kinetics and mucoadhesive strength for an oral mucoadhesive tablet of cefixime trihydrate. Bull Fac Pharm Cairo Univ. 2016;54(2):227-35. doi: 10.1016/j.bfopcu.2016.06.004.

Sahoo A, Kumar NSK, Suryanarayanan R. Crosslinking: an avenue to develop stable amorphous solid dispersion with high drug loading and tailored physical stability. J Control Release. 2019;311-312:212-24. doi: 10.1016/j.jconrel.2019.09.007, PMID 31499085.

Esim O, Savaser A, Ozkan CK, Bayrak Z, Tas C, Ozkan Y. Effect of polymer type on characteristics of buccal tablets using factorial design. Saudi Pharm J. 2018;26(1):53-63. doi: 10.1016/j.jsps.2017.10.013, PMID 29379333.

Mandal D, Ojha PK, Nandy BC, Ghosh LK. Effect of carriers on solid dispersions of simvastatin (Sim): physicochemical characterizations and dissolution studies. Pharm Lett. 2010;2:47-56.

Ramani V, Sailor GU, Patel MM, Parmar GR, Seth AK. Experimental design approach for the formulation of controlled release buccal bilayer tablets of carvedilol. J Integr Health Sci. 2018;6:54.

Raval J, Yagnik A. Formulation and evaluation of buccoadhesive tablets of buspirone hidrochloride. Highlights Med Sci. 2021;4:128-46.

Meka L, Kesavan B, Chinnala KM, Vobalaboina V, Yamsani MR. Preparation of a matrix type multiple-unit gastro retentive floating drug delivery system for captopril based on gas formation technique: in vitro evaluation. AAPS PharmSciTech. 2008;9(2):612-9. doi: 10.1208/s12249-008-9090-4, PMID 18459051.

Patel D, Sawant KK. Self micro-emulsifying drug delivery system: formulation development and biopharmaceutical evaluation of lipophilic drugs. Curr Drug Deliv. 2009;6(4):419-24. doi: 10.2174/156720109789000519, PMID 19534704.

Saha T, Ahmed N, Hasan I, Reza MS. Preparation, characterization and optimization of mucoadhesive domperidone tablets by box Behnken design. Dhaka Univ J Pharm Sci. 2020;19(1):65-76. doi: 10.3329/dujps.v19i1.47820.

Sugimoto T, Yamazaki N, Hayashi T, Yuba E, Harada A, Kotaka A, Shinde C, Kumei T, Sumida Y, Fukushima M, Munekata Y, Maruyama K, Kono K. Preparation of dual-stimuli-responsive liposomes using methacrylate-based copolymers with pH and temperature sensitivities for precisely controlled release. Colloids Surf B Biointerfaces. 2017;155:449-58. doi: 10.1016/j.colsurfb.2017.04.043, PMID 28463812.

Dehghani F, Farhadian N, Golmohammadzadeh S, Biriaee A, Ebrahimi M, Karimi M. Preparation, characterization and in vivo evaluation of microemulsions containing tamoxifen citrate anti-cancer drug. Eur J Pharm Sci. 2017;96:479-89. doi: 10.1016/j.ejps.2016.09.033, PMID 27693298.

Sopyan I, Sriwidodo WR, Wahyuningrum R, P NA. A review: floating drug delivery system as a tool to improve dissolution rate in gastric. Int J Appl Pharm. 2020;7:51-4. doi: 10.22159/ijap.2020v12i4.38415.

Aleti R, Baratam SR, Jagirapu B, Kudamala S. Formualtion and evaluation of metformin hydrochloride and gliclazide susteined release bilayer tablet: a combination theraphy in management of diabetes. Int J Appl Pharm. 2021;13:343-50.

Mali S, Oza N. Centeral composite design for formulation and optimization of longacting injectable (LAI) mikrospere of paliperidone. Int J Appl Pharm. 2021;13(5):87-98. doi: 10.22159/ijap.2021v13i5.42297

Patel MB, Shaikh F, Patel V, Surti NI. Application of simplex centroid design in formulation and optimization of floating matrix tablets of metformin. Int J Appl Pharm Sci. 2017;7:23-30.

Kamere K, Gopalakrishna SV, Subbareddy GV. Formulation and optimization of gastroretentive glimepiride floating matrix tablet. Int J Life Sci Pharm Res. 2021;11:136-47.

Maddiboyina B, Hanumanaik M, Nakkala RK, Jhawat V, Rawat P, Alam A, Foudah AI, Alrobaian MM, Shukla R, Singh S, Kesharwani P. Formulation and evaluation of gastro-retentive floating bilayer tablet for the treatment of hypertension. Heliyon. 2020;6(11):e05459. doi: 10.1016/j.heliyon. 2020.e05459, PMID 33241144.

Raza A, Bukhari NI, Karim S, Hafiz MA, Hayat U. Floating tablets of minocycline hydrochloride: formulation, in vitro evaluation and optimization. Future J Pharm Sci. 2017;3(2):131-9. doi: 10.1016/j.fjps.2017.05.001.

Moinuddin SM, Ruan S, Huang Y, Gao Q, Shi Q, Cai B, Cai T. Facile formation of co-amorphous atenolol and hydrochlorothiazide mixtures via cryogenic-milling: enhanced physical stability, dissolution and pharmacokinetic profile. Int J Pharm. 2017;532(1):393-400. doi: 10.1016/j.ijpharm.2017.09.020, PMID 28893583.

Yang Y, Waring JF. Genomic approaches to drug-drug interactions. In: CEO APLPDP and, editor. Drug-drug interactions in pharmaceutical development [Internet]. John Wiley and Sons, Inc; 2007. p. 113-30.

Syed SM, Lahoti S, Syed AA. Controlled porosity osmotic tablet of atenolol: in vitro and in vivo evaluation. Marmara Pharm J. 2016;20(3):325-32. doi: 10.12991/mpj.20162040694.

Moin A, Roohi NKF, Rizvi SMD, Ashraf SA, Siddiqui AJ, Patel M, Ahmed SM, Gowda DV, Adnan M. Design and formulation of polymeric nanosponge tablets with enhanced solubility for combination therapy. RSC Adv. 2020;10(57):34869-84. doi: 10.1039/D0RA06611G.

Gunda RK, Manchineni PR. Statistical design and optimization of sustained-release formulations of pravastatin. Turk J Pharm Sci. 2020;17(2):221-7. doi: 10.4274/tjps.galenos.2019.70048, PMID 32454783.

Iffat W, Shoaib MH, Yousuf RI. Hydrophillic and hydrophobic polymer combination: formulation development and optimatization of nicorandil sustained release tablet. Lat Am J Pharm. 2017;36:907-17.

Kraisit P. Impact of hydroxypropyl methylcellulose (HPMC) type and concentration on the swelling and release properties of propranolol hydrochloride matrix tablets using a simplex centroid design. Int J App Pharm. 2019;11:143-51. doi: 10.22159/ijap.2019v11i2.31127.

Morovati A, Ghaffari A, Erfani Jabarian L, Mehramizi A. Single layer extended-release two-in-one guaifenesin matrix tablet: Formulation method, optimization, release kinetics evaluation and its comparison with mucinex® using box-behnken design. Iran J Pharm Res. 2017;16(4):1349-69. PMID 29552045.

Parmar K, Patel J, Sheth N. Self nano-emulsifying drug delivery system for Embelin: Design, characterization and in vitro studies. Asian J Pharm Sci. 2015;10(5):396-404. doi: 10.1016/j.ajps.2015.04.006.

Bharti C, Nagaich U, Pandey J, Jain S, Jain N. Development of nitazoxanide-loaded colon-targeted formulation for parasitic intestinal infections: centre composite design-based optimization and characterization. Future J Pharm Sci. 2020;6:1-17.

Kotadiya RM, Savant NP, Upadhyay UM. Colon targeted Moringa gum compression coated tablets of capecitabine: A factorial approach. Pharmacophore. 2019;10(1).

Kim MS, Kim JS, Hwang SJ. Enhancement of wettability and dissolution properties of cilostazol using the supercritical antisolvent process: effect of various additives. Chem Pharm Bull (Tokyo). 2010;58(2):230-3. doi: 10.1248/cpb.58.230, PMID 20118585.