Abstract
<p><strong>Objective: </strong>Objective of the present study was to prepare simple single unit gastro-retentive capsules of ofloxacin with the aim to have the gastric retention of the system for longer periods of time (12h) and to study the effect of various polymers on floating behaviour of such single unit gastro-retentive capsules of ofloxacin.</p><p><strong>Methods: </strong>The method used for the preparation of gastro-retentive capsules was a simple physical blending of various low-density hydrophilic polymers alone and in combination with hydrophobic polymers and filling into capsules. These capsules were then subjected to <em>in vitro</em> floatation and matrix integrity study in 0.1N HCl using static volume beaker method and the United States pharmacopoeia (USP) type II dissolution apparatus method at 100rpm.</p><p><strong>Results: </strong>Two grades of hydroxypropyl methylcellulose (HPMC) K4M and K15M used were found suitable for the purpose. Results showed that increase in HPMC level increased colloidal gel barrier strength along with matrix integrity with consequently improved buoyancy. Lactose which was added as release rate modifier decreased matrix integrity and buoyancy. Eudragit a hydrophobic polymer was added so as to have intact, the buoyant formulation for 12 h with desired drug release characteristics. The addition of eudragit enhanced matrix integrity and floatation time to certain levels but higher levels showed negative results. Floatation time of more than 16 h was observed in the formulations containing 2:1 ratio of HPMC K15M and eudragit respectively. 3<sup>2</sup> factorial design was used to study the effect of various formulation variables on buoyancy and matrix integrity. Formulations containing zero level of HPMC were found buoyant for more than 12 h with all levels of eudragit S100 (i.e.,-1, 0,+1 level). It was also observed that matrix integrity consequently buoyancy increased with increase in eudragit with all levels of HPMC.</p><p><strong>Conclusion: </strong>The study concludes that eudragit S100 a hydrophobic polymer increased floatation time of the formulated capsules with all the three levels of HPMC K15M, but at the same time eudragit level should not exceed HPMC, while lactose a release rate enhancer decreased matrix integrity/floatation time of the formulated capsules.</p>
Highlights
Among the various drug delivery routes, oral route has remained the most convenient route due to ease of administration of the dosage forms, patient acceptance and flexibility in formulation [1]
CMC) in different combinations and ratios along with the drug were blended and subjected to buoyancy and matrix integrity study using static volume beaker method. These results showed the suitability of hydroxypropyl methylcellulose (HPMC) K4M and HPMC K15M for the study
The initial combinations of HPMC K15M and the drug used in pre-formulation study are shown in table 1a
Summary
Among the various drug delivery routes, oral route has remained the most convenient route due to ease of administration of the dosage forms, patient acceptance and flexibility in formulation [1]. The success of an oral delivery depends on a number of factors like gastric emptying process, the gastrointestinal transit time of the dosage form, drug release from the dosage form and the site of absorption of drugs [2]. There are many limitations of most of the orally administered dosage forms such as rapid and inconsistent gastrointestinal transit time [3], incomplete drug release from the devices and too short residence time in the absorption region of the gastrointestinal tract, which may lead to lower bioavailability of the dosage form [4, 5]. Even if sustained release of the drug is attained, the drug may be released after the dosage form has passed the absorption site, lowering the efficacy of the drug To solve these problems, oral controlled release gastro-retentive drug delivery system (GRDDS) has been developed. GRDDS prolongs the retention time of dosage forms in the stomach so that there is improved solubility, bioavailability and reduces drug waste [6]; thereby increases the therapeutic efficacy of the drugs
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
