Formulation and in vitro evaluation of theophylline anhydrous bioadhesive tablets

V N Deshmukh, J K Jadhav, D M Sakarkar

Abstract


The aim of the current study was to design oral controlled release (CR) theophylline anhydrous bioadhesive tablets and
to optimize the drug release profile and in vitro bioadhesion strength. Different types of natural hydrophilic polymers
such as xanthun gum, locust bean gum, guar gum, karaya gum, and their combinations were used to formulate matrix
tablets. Tablets of anhydrous theophylline were prepared by the direct compression method and were subjected to in vitro
drug dissolution for 12 hours using the USP dissolution apparatus basket type at a speed of 100 rpm and temperature of 37 ± 0.5°C using gastric fluid (pH 1.2). The bioadhesive strength of the tablets was measured as the force of detachment
against the porcine gastric mucosa. The in vitro release study as well as the retention time of the bioadhesive tablets on
the mucous membrane were investigated to develop a bioadhesive polymer-based CR delivery system and to evaluate the performance of such a delivery device. The combination of karaya gum:guar gum (6:4) tablet showed a greater bioadhesive
strength as compared with a single gum and other gum combination tablets. Karaya gum:guar gum-loaded tablets were not discharged from the mucous membrane and were dissolved in the gastric fluid. An increase in the gum concentration increases the drug release profile beyond 12 hours whereas there is no significant effect of gum concentration on the bioadhesive strength of the tablet.

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References


Ponchel G, Irache J, Specific and non-specific bioadhesive particulate

systems for oral delivery to the gastrointestinal tract. Adv Drug Deliv

Rev 1998;34:191-219.

Peppas N A, Sahlin J J, Hydrogels as mucoadhesive and bioadhesive

materials: A review. Biomaterials 1996;17:1553-61.

Hou SY, Cowles VE, Berner B. Gastric retentive dosage forms: A

review. Crit Rev Ther Drug Carrier Syst 2003;20:459-97.

Lavelle EC. Targeted delivery of drugs to the gastrointestinal tract. Crit

Rev Ther Drug Carrier Syst 2001;18:341-86.

Woodley J. Bioadhesion: New possibilities for drug administration? Clin

Pharmacokinet 2001;40:77-84.

Batchelor H. Novel bioadhesive formulations in drug delivery, Presented

in 2004 at the British pharmaceutical conference on drug delivery to

the upper GI tract, particularly the esophagus: Medicines Research

Unit, Aston University, Birmingham, B47ET, UK, 2004.

Sakagami M, Kinoshita W, Sakon K, Sato JI, Makino Y. Mucoadhesive

beclomethasone microspheres for powder inhalation: Their

pharmacokinetics and pharmacodynamics evaluation. J Control Release

;80:207-18.

Takishima J, Onishi H, Machida Y. Prolonged intestinal absorption of

cephradine with chitosan-coated ethyl cellulose microparticles in rats.

Biol Pharm Bull 2002;25:1498-502.

Lim ST, Forbes B, Berry DJ, Martin GP, Brown MB. In vivo evaluation of

novel hyaluronan/chitosan microparticulate delivery systems for the

nasal delivery of gentamicin in rabbits. Int J Pharm 2002;231:73-82.

Cuna M, Alonso MJ, Torres D, Preparation and in vivo evaluation of

mucoadhesive microparticles containing amoxicillin-resin complexes

for drug delivery to the gastric mucosa. Eur J Pharm Biopharm

;51:199-205.

Gilbert S, Banker, Neil R, Anderson, Lachman L, Liberman HA, et al,

editors. The Theory and practice of Industrial Pharmacy, 3rd ed. Mumbai:

Varghese Publishing House; 1990. p. 88,299.

“United States Pharmacopoeia”, XXIV NF 19. Rockville: United State

Pharmacopoeia Convention; 2000. p. 2388-9.

ICH Harmonized Tripartite Guideline, Validation of analytical

procedures: Text and Methodology Q2(RI), ICH Steering Committee,

Gupta A, Garg S, and Khar R, Measurement of bioadhesive Strength of

mucoadhesive Buccal tablets: Design of in vitro assembly. Indian Drug

;30:152-5.

Ali J, Khar R, Ahuja A, Effect of polymer loading on drug release and

bioadhesion of buccoadhesive carriers for local drug delivery of

triaminocolone acetonitride. East Pharma 1999;46:115-9.

Ali J, Khar R, Ahuja A, Karla R. Buccoadhesive erodible disk for treatment

of orodental infections design and characterization. Int J Pharm

;283:93-103.

Vermani K, Garg S, Lourence JD. Assembly for In vitro measurement of

Bioadhesive strength and retention characteristic in simulated vaginal

environment. Drug Dev Ind Pharm 2002;28:1133-46.

RangaRao KV, Buri PA. Novel insitu method to test polymers and coated

microparticles for bioadhesion. Int J Pharm 1989;52:256-70.

Achar L, Peppas N. Preparation, characterization and mucoadhesive

interactions of poly (methacrylic acid) copolymer with rat mucosa.

J.Control Release 1994;31:271-6.

Elizabeth B, Gennaro AR, editors. Reimington: The science and practice

of pharmacy. 20th ed. Vol. 1, Easton, PA: Mack Publishing Company;

p. 986-7.




DOI: http://dx.doi.org/10.22377/ajp.v3i1.242

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