Drug-Excipient Interaction during Formulation Development, in vitro andin vivo Evaluation of Gastroretentive Drug Delivery System for Nizatidine

DOI:

https://doi.org/10.37285/ijpsn.2013.6.4.11

Authors

  • Kishan V
  • Ramireddy Amarnath Reddy
  • Ramesh Bomma

Abstract

The present investigation dealswith the development and evaluation of floating tablets of nizatidine to prolong the gastric residence time, increase local delivery of drug to the H2-receptor of the parietal cell wall to reduce stomach acid secretion. The drug-excipient compatibility studies were conducted by using FTIR, DSC and visual observations. Citric acid inclusion in formulations resulted in incompatibility and the composition was modified to eliminate the problem of incompatibility. Floating matrix tablets of nizatidine were developed by direct compression method using hydroxypropyl methylcellulose (HPMC K4M) and polyox WSR 1105 alone as release retardants and sodium bicarbonate as a gas-generating agent. Alleleven formulations exhibited satisfactory physicochemical characteristics andin vitro buoyancy. Formulations F6 and F10 exhibited controlled and prolonged drug release for 10 h with zero order release. Formulation (F10) was selected as optimized formulation based on physicochemical properties and in vitro drug release and was used inradiographic studies by incorporating BaSO4. The radiographic studies were conducted in comparison with plain controlled release tablets. These studies revealed that gastric retention time of floating and plain controlled release tablets in fasting state were 2 ± 0.86 h and ≤ 0.5 h respectively in human volunteers. Gastric retention time of floating and plain controlled release tablets in fed state were 5.33 ± 0.57 h and 1.66 ± 0.28 h respectively in human volunteers. In conclusion, optimal floating matrix tablet for nizatidine with desired in vitro buoyancy, in vivo gastric retention time and prolonged release could be prepare

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Keywords:

Floating tablets, drug-excipients compatibility, gastric residence time, nizatidine

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Published

2013-12-31

How to Cite

1.
V K, Reddy RA, Bomma R. Drug-Excipient Interaction during Formulation Development, in vitro andin vivo Evaluation of Gastroretentive Drug Delivery System for Nizatidine. Scopus Indexed [Internet]. 2013 Dec. 31 [cited 2024 May 18];6(4):2281-93. Available from: https://www.ijpsnonline.com/index.php/ijpsn/article/view/691

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Research Articles

References

Drug Delivery Systems: A Review. AAPS PharmSciTech 6(3):E372-E390.

Brahma NS and Kim KH (2000). Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J Control Release63:235–259.

Caldwell LJ, Gardner RC and Cargill RC(1988).Drug delivery device which can be retained in the stomach for a controlled period of time.US Patent 4735804.

Chen GL andHao WH (1998).In vitro performance of floating sustained release capsule of verapamil. Drug DevInd Pharm24(11):1067-1072.

Davis AF (1997).Compositions containing histamine-H2-receptor antagonists at low dosage.US Patent 5 656 652.

Fix JA, Cargill R and Engle K (1993). Controlled gastric emptying. III. Gastric residence time of a non-disintegrating geometric shape in human volunteers. Pharm Res10(7):1087–1089.

GargR,Gupta GD (2008). Progress in Controlled Gastroretentive Delivery Systems.Trop J Pharm Res7(3):1055-1066.

Gröning R and Heun G (1989).Dosage forms with controlled gastrointestinal passage - studies on the absorption of nitrofurantoin. Int J Pharm56:111-116.

Higuchi T (1961). Rate of release of medicaments from ointment bases containing drugs in suspension. J Pharm Sci50(10):874-875.

Kokate A, Marasanapalle VP, Jasti BR andXiaoling Li (2006).Physiological and biochemical barriers to the drug delivery. In: Design of Controlled Release Drug Delivery Systems (Jasti BR, Ed.).McGraw-Hill, New York, pp. 41-74.

Korsmeyer RW, Gurny R, Doelker E, Buri P andPeppas NA (1983). Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm15(1):25-35.

Lehr CM (1994). Bioadhesion technologies for the delivery of peptide and protein drugs to the gastrointestinal tract.Crit Rev Ther Drug Carrier Syst11(2-3):119-160.

Malinowski HJ andMarroum PJ (1999).Food and drug administration requirements for controlled release products. In: Encyclopedia of controlled drug delivery, Vol. 1 (Mathiowitz E, Ed.).John Wiley and Sons Inc. 381-395.

Mamajek RC, Moyer ES(1980).Drug-dispensing device and method. US Patent 4 207 890.

Moore JW and Flanner HH (1996). Mathematical comparison of curves with an emphasis on in vitro dissolution profiles. Pharm Tech20(6):64–74.

Physicians’ Desk Reference (2011). 65th ed. PDR Network, Montvale, pp. 1298-3000.

Raval JA, Patel JK, Naihong Li and Patel MM (2007). Ranitidine hydrochloride floating matrix tablets based on low density powder: effects of formulation and processing parameters on drug release. Asian JPharm Sci2(4):130-142.

Ritger PL, Peppas NA (1987). A simple equation for description of solute release I: Fickian and non-fickian release from non-swellable devices in the form of slabs, spheres, cylinder or discs. J Control Release5(1):23-36.

Rosa MJC, Ziaa H and Rhodes CT (1994).Design and testing in-vitro of a bioadhesive and floating drug delivery system for oral application.Int J Pharm105(1):65–70.

Rubinstein A and Friend DR (1994).Specific delivery to the gastrointestinal tract. In: Polymeric Site-Specific Pharmacotherapy (Domb AJ, Ed.).Wiley, Chichester pp.282–283.

Schilling SU, Bruce CD, Shah NH,Malick AW andMcGinity JW (2008). Citric acid monohydrate as a release-modifying agent in melt extrudedmatrix tablets. Int J Pharm361:158–168.

Shah MV, De Gennaro MD andSuryakasuma H (1987). An evaluation of albumin microcapsules prepared using a multiple emulsion technique. J Microencapsul.4(3):223-238.

Sheth PR andTossounian JL (1979). Novel sustained release tablet formulations. US Patent 4 167 558.

Urquhart J and Theeuwes F (1984).Drug delivery system comprising a reservoir containing a plurality of tiny pills.US Patent 4 434 153.

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