Preparation and characterization of Selfdisintegrating fast dissolving valsartan tablets using novel hybridized polymer comprising Hydroxypropyl methylcellulose and Acacia gum.
https://doi.org/10.51412/psnnjp.2022.36
Keywords:
Valsartan, Hydroxypropyl methyl cellulose, self-disintegrating tabletAbstract
Background: Automation of pharmacotherapy is a recently emerging therapeutic approach that depends on advanced dosage form design engineered through carefully fabricated carriers from two or more excipients The study seeks to develop and characterised in a solid dosage form, a novel, highly functional composite polymer using a hydrophilic natural (Acacia gum) and synthetic Hydroxypropyl methyl cellulose (HPMC) polymer via cross-linking
Methods: HPMC and Acacia gum (AG) ratio 4:0; 3:1; 2:2; 1:3 and 0:4 were cross linked using citric acid. The batches were characterised by FTIR, welling index, viscosity and pH. Five batches of powder blends were prepared using the hybridized HPMC-AG composite polymer 'F1, F2, F3, F4, and F5 as binder in the valsartan (VAL) powder blends. The blends were evaluated for bulk density, angle of repose and compressibility index. Tablets were formulated by direct compression method using Cadmach rotary tableting machine, 12.5 mm die and compression pressure of 10 KN. The tablets parameters such as thickness, diameter, weight variation test, drug content, hardness, friability, and in vitro release studies in phosphate buffer solution (pH 6.8).
Results: The presence of the major functional groups of both polymers after cross-linking proved that there was no complex interaction after the reaction. The powder flow properties and tablets analysis for all batches F1 – F5, showed promising characteristics for an ideal tablet formulation, with average powder flow rate, tablet disintegration time, crushing strength and T90% as follow: F1 (0.10 gs-1, 16.00 min, 135 N, and 20.0 min.) respectively; F2 (0.254 gs-1, 8.48 min, 60 N, and 15.0 min.) respectively; F3 (0.269 gs-1, 10.30 mi, 85 N, and 12.0 min.) respectively; F4 (0.200 gs-1, 4.30 min, 65, and 8.0 min.) respectively; F5 ( 0.315 gs-1, 10.54 mi, 12 N, and 17.0 min.) respectively. The compact formulation 'F4'containing 80 mg VAL 50 mg HPMC, 150 mg AG and 120 mg cellactose have the best property for Self-Disintegrating Fast Dissolving VAL Tablet, better T90 % than the marked generic VALtablets.
Conclusion: A new 2-component composite polymer highly hydrophilic was formed from citric acid cross-linked HPMC and AG. When used with cellactose to formulate VAL tablets it compressed directly and is suitable for formulation of a new Self-Disintegrating Fast Dissolving Oral Solid Dosage Form with improved bioavailability.
References
Acacia Gum Information. Drug .com; MedFacts Natural Products. Updated October 4, 2011. Accessed October 24 , 2011 .
http://www.drug.com/zyrtec.html.http://www.drugs.com/npp/acacia-gum.
Ford J.L, Rubinstein M.H and Hogan J.E (2007) Formation of sustained release promethazine hydrochloride tablet using
hydroxypropylmethylcellulose matrix, Int J Pharm. 24, 327-338.
Ke W, Hsu T, Ho H, and Sheu M (2006). Physical and chemical characterization of ambroxol SR matrix tablets containing melt-coated granules ofambroxol with Compritol 888, Asian J Pharm Sci 1, 35-42.
Feely L.C, and Davis S.S (1988). Infuence of surfactants on the drug release from hydroxyl propyl methyl cellulose, Int J Pharm 41, 83-90.
Eddington N.D,Ashraf M,Augsburger L.L, Leslie J.L, Fossler M.J, Lesko L.J, Shah V.P, and Rekhi G.S (1998). Identifcation of formulation and
manufacturing variables that infuence in vitro dissolution and in vivo bioavialability of propranolol hydrochloride tablets, Pharm Dev
Tech 3, 535- 547.
Vlachou M, Hani N, Efentakis M, Tarantili P.A, Andreopoulos A.G (2000). Polymers for use in controlled release system: the effect of surfactants on their swelling properties, J Biomater Appl 15, 65-77.
Nokhodchi A, Norouzi-Sani S, Siahi-Shadbad M.R and Lotfpoor M (2002). The effect of various surfactants on the release rate of propranolol hydrochloride from hydroxyl propyl methyl cellulose (HPMC)-Eudragit matrix, Eur J PharmSci 54, 349-356.
Lahdenpaa E, Niskanen M and Yliruusi J (1997). Crushing strength disintegration time and weight variation of tablets compressed from three MCC pH grades and their mixtures, Eur J Pharm Biopharm 42, 315-322.
Li J.Z, Rekhi G.S, Augsburger L.L and Shangraw R.F (1996). The role of intra and extragranular microcrystalline cellulose in tablet dissolution, Pharm Dev Tech 1, 343-355.
Pao-Chu Wu (2004). Once-daily propranolol extended release tablet dosage form: formulation design and in vitro/in vivo investigation, Eur J Pharm Biopharm, 58, 607-614.
Highlights or Prescribing Information . Diovan® (valsartan) tablets, for oral use. Initial U.S . Approval: 1996
Griffith L. (2000). Polymeric biomaterials. Actamaterialia, 48, 263-277.
Richardson G, Langton M, Bark A, Hermansson A.M, (2003). Wheat starch gelatinization – the effects of sucrose emulsifier and the physical state of the emulsifier. Starch; 55 (3-4): 150 - 161.
Shah R.B, Tawakkul M.A, and Khan M.A (2008). C o m p a r a t i v e E v a l u a t i o n o f F l o w f o r Pharmaceutical Powders and Granules. AAPS PharmSciTech.: 9(1) 250-258.
L i e b e r m a n H . A , L a c h m a n L ( 1 9 8 9 ) .Pharmaceutical dosage forms tablets. 2nd ed. New York: Marcel Dekker; 198: 9-15.
United States pharmacopeia. National formulary USP 29-NF 24. Dissolution<711> physical tests and determinations. United States Pharmacopeia Convention, Inc. Rockville, MD, 2006, pp.2673- 2682.
Banker G.S, Anderson N.R. In: Lachman L, Lieberman H.A, Kanig J.L, eds. The Theory and Practice of Industrial Pharmacy. 3rd ed. Mumbai: Varghese Publishing House (1987) 293-399.
Schramm C, Vukusic C.S.B, and Katovic L (2002). Non-formaldehyde durable press finishing of dyed fabrics: Evaluation of cottonbound polycarboxylic acids, Coloration Technology 118, 244–249
Shinde, A. J. (2017). Formulation and optimization of expandable gastroretentive tablet of diltiazem hydrochloride using factorial design. Asian Journal of Pharmaceutics (AJP), 11 (01).
OlsonA, Liu F, TuckerA, Goshe M, and Cavanagh J (2013). Chemical crosslinking and LC/MS analysis to determine protein domain orientation. Biochemical and Biophysical Research Communications; 431 (2), 253-257.
Krumova M, Lopez D, Benavente R, Mijangos C and Perea J.M (2000). Effect of crosslinking on the mechanical and thermal properties of poly(vinyl alcohol). Polymer; 41: 9265-9272.
Rivero S, García M.A, Pinotti A (2010). Crosslinking capacity of tannic acid in plasticized chitosan films. Carbohydrate Polymers; 82: 270-
Rivero S. (2012). Ph.D. Thesis. Study and application of active films based on chitosan. University of La Plata.
Xie X, and Liu Q (2004). Development and physicochemical characterization of new resistantcitrate starch from different corn starches. Starch; 56: 364.
ZhouY, Luner Pand Caluwe P(1995). Mechanism of crosslinking of papers with polyfunctional carboxylic acids. Journal of Applied Polymer Science; 58 (9): 1523–1534.
Published
How to Cite
Issue
Section
License
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
