Drug Res (Stuttg) 2020; 70(12): 576-582
DOI: 10.1055/a-1249-8186
Original Article

Development and Optimization of Methscopolamine Bromide Gastroretentive Floating Tablets Using 32 Factorial Design

Maninder Pal Singh
1   CT Institute of Pharmaceutical Sciences, Shahpur, Jalandhar Punjab
2   MM College of Pharmacy, Maharishi Markandeshwar (Deemed to be University) Mullana –Ambala
,
Manish Kumar
2   MM College of Pharmacy, Maharishi Markandeshwar (Deemed to be University) Mullana –Ambala
,
Ravi Shankar
3   SHEAT College of Pharmacy, Varanasi
› Author Affiliations

Abstract

Purpose The aim of this study was to formulate methscopolamine floating drug delivery system to increase its gastro retention for further enhancement of absorption and overall bioavailability.

Method Direct compression method was used to formulate floating drug delivery system of methscopolamine bromide. Different amount of HPMC, PVP K25, and MCC were used for preparation of tablets.

Result The prepared tablets were evaluated for thickness, hardness, weight variation, floating lag time, swelling index and in-vitro drug release. All the formulations showed less than 10% of weight variation. The hardness and thickness of all the formulations were within the range of 3.7−4.2 kg/cm2 and 3.63−3.83 mm respectively. Floating lag time for all the formulations was reported in seconds. The degree of swelling was reported in range of 82.10−85.83%. In vitro release was carried out for 24 h. The maximum release was shown by F1 (93.947%) while the minimum release was observed for F4 (90.420%). The best formulation was optimized on the basis of percentage cumulative drug release, floating lag time and swelling index. F1 found to be the best formulation. Further on analyzing the drug release mechanism, F1 found to exhibit korsmeyer peppas model of drug release.

Conclusion Floating gastroretentive tablet of methscopolamine bromide was successfully developed using direct compression method with potential to enhance the drug absorption and effective treatment of peptic ulcer.



Publication History

Received: 23 June 2020

Accepted: 19 August 2020

Article published online:
29 September 2020

© 2020. Thieme. All rights reserved.

Georg Thieme Verlag KG
Rüdigerstraße 14, 70469 Stuttgart, Germany

 
  • References

  • 1 https://pubchem.ncbi.nlm.nih.gov/compound/methscopolamine_bromide
  • 2 https://www.parpharm.com/products/assets/pdf/Methscopolamine-Bromide-2018.pdf
  • 3 Whitehead L, Fell JT, Collett JH. et al. Floating dosage forms: An in vivo study demonstrating prolonged gastric retention. J Controlled Release 1998; 55: 3-12
  • 4 Singh NB, Kim KH. Floating drug delivery systems: An approach to oral controlled drug delivery via gastric retention. J Controlled Release 2000; 63: 235-259
  • 5 Arora S, Ali J, Ahuja A. et al. Floating drug delivery systems: A review. AAPS Pharm SciTech 2005; 3: E372-E390
  • 6 Bardonnet PL, Faivre V, Pugh WJ. et al. Gastroretentive dosage forms: overview and special case of Helicobacter pylori. J Controlled Release 2006; 111: 1-18
  • 7 Moes AJ. Gastroretentive dosage forms. Crit Rev Ther Drug Carrier Syst 1993; 10: 143-195
  • 8 Singh S, Pathak K. Assessing the bioadhesivity of Acconon MC8-2EP/NF for gastroretention of floating microsponges of loratidine and achieving controlled drug delivery. Pharm. Biomed Res 2016; 2: 58-74
  • 9 Srikanth MV, Rao NS, Sunil SA. et al. Statistical design and evaluation of a propranolol HCl gastric floating tablet. Acta Pharm Sin B 2012; 2: 60-69
  • 10 Sato Y, Kawashima Y, Takeuchi H. et al. In vitro and in vivo evaluation of riboflavin-containing microballoons for a floating controlled drug delivery system in healthy humans. Int J Pharm 2004; 275: 97-107
  • 11 Klausner EA, Lavy E, Friedman M. et al. Expandable gastroretentive dosage forms. J Controlled Release 2003; 90: 143-162
  • 12 Chen RN, Ho Ho, Yub YC. Development of swelling/floating gastroretentive drug delivery system based on a combination of hydroxyethyl cellulose and sodium carboxymethyl cellulose for Losartan and its clinical relevance in healthy, volunteers with CYP2C9 polymorphism. Eur J Pharm Sciences 2010; 39: 82-89
  • 13 Adebisi A, Conway BR. Gastroretentive microparticles for drug delivery applications. J Microencapsul 2011; 28: 689-708
  • 14 Streubel A, Siepmann J, Bodmeier R. Gastroretentive drug delivery systems. Exp Opin Drug Deliv 2006; 3: 217-233
  • 15 Rajani S, Panna T, Rajendra NS. In vitro and in vivo evaluation of gastroretentive floating drug delivery system of ofloxacin. Asian J Pharma Sciences 2013; 8: 191-198
  • 16 Rahman Z, Ali M, Khar RK. Design and evaluation floating labeled. Act pharm 2006; 56: 49-57
  • 17 United states Pharmacopeia 24-NF 19. 2000. Page No.296-297
  • 18 Indian Pharmacopeia 9th Ed, 1996. Page no. 135-136
  • 19 Roy P, Shahiwala A. Statistical optimization of ranitidine hydrochloride floating pulsatile delivery system for chronotherapy of nocturnal acid breakthrough. Eur J Pharm Sci 2009; 37: 363-369
  • 20 Gambhire MN, Ambade KW, Kurmi SD. et al. Development and in vitro evaluation of an oral floating matrix tablet formulation of diltiazem hydrochloride. AAPS Pharm SciTech 2007; 8: E73
  • 21 Reddy LH, Murthy RS. Floating dosage systems in drug delivery. Crit Rev Ther Drug Carr Syst 2002; 19: 553-585
  • 22 Gaikwad VD, Yadav VD, Gaikwad D. Novel sustained release and swellable gastroretentive dosage form for ciprofloxacin hydrochloride. Int J Pharm Investig 2014; 4: 88-92
  • 23 Pawar HA, Gharat PR, Dhavale RV. et al. Development and evaluation of gastroretentive floating tablets of an antihypertensive drug using hydrogenated cottonseed oil. ISRN Pharm 2013; 1-9
  • 24 Lingam M, Bhaskar K, Krishna C. et al. Preparation of a matrix T type multiple-unit gastro retentive floating drug delivery system for captopril based on gas formation technique: In Vitro evaluation. AAPS Pharm Sci Tech 2008; 9: 612-619
  • 25 Streubel A, Siepmann J, Bodmeier R. Floating matrix tablets based on low density foam powder: Effects of formulation and processing parameters on drug release. Eur J Pharm Sci 2003; 18: 37-45