|Year : 2012 | Volume
| Issue : 5 | Page : 79-80
Losartan potassium loaded sustained release matrix tablets: Influence of various hydrophilic and hydrophobic polymers on drug release behaviour
DD Vohra, KS Pagi, KS Rajesh
Parul Institute of Pharmacy, PO: Limda, Ta: Waghodiya, Dist.: Vadodara, India
|Date of Web Publication||21-Mar-2012|
K S Rajesh
Parul Institute of Pharmacy, PO: Limda, Ta: Waghodiya, Dist.: Vadodara
Source of Support: None, Conflict of Interest: None
| Abstract|| |
Losartan potassium is an angiotensin II receptor antagonist readily absorbed from the GIT, following oral administration. It has low bioavailability as it undergoes extensive first pass metabolism and low elimination half-life. The present study was aimed at studying sustained release behaviour of the drug using hydrophilic and hydrophobic polymers and to optimise using a 32 full factorial design. Eudragit and HPMC were used to evaluate the effect of hydrophilic and hydrophobic polymers on the release pattern of the drug. A full factorial was implemented at 20, 30 and 40% concentration of hydrophilic polymer and 2.5, 5 and 7.5% of hydrophobic polymer correlating with the release behaviour. Process variables were investigated and the results showed excellent adaptability in releasing drug over prolonged periods. Based on the results, it was found suitable to formulate a dosage form using optimum concentration of hydrophobic polymer along with hydrophilic polymer to vary the release behaviour for over 12 hours.
Keywords: L0 osartan potassium, matrix tablets, hydrophilic and hydrophobic polymers
|How to cite this article:|
Vohra D D, Pagi K S, Rajesh K S. Losartan potassium loaded sustained release matrix tablets: Influence of various hydrophilic and hydrophobic polymers on drug release behaviour. J Pharm Bioall Sci 2012;4, Suppl S1:79-80
|How to cite this URL:|
Vohra D D, Pagi K S, Rajesh K S. Losartan potassium loaded sustained release matrix tablets: Influence of various hydrophilic and hydrophobic polymers on drug release behaviour. J Pharm Bioall Sci [serial online] 2012 [cited 2022 May 29];4, Suppl S1:79-80. Available from: https://www.jpbsonline.org/text.asp?2012/4/5/79/94147
Losartan potassium, an angiotensin II receptor antagonist is used in treatment of hypertension. It is readily absorbed from the GIT following oral administration with poor bioavailability experiencing extensive first pass metabolism and low elimination half-life.
The present work was aimed to control drug delivery and alter the pharmacokinetics and pharmacodynamics of Losartan potassium, to ensure safety, improve efficacy, therapeutic action as well as patient compliance. The influence of variables such as concentration of the hydrophilic and hydrophobic polymers on in-vitro release profiles of tablets prepared by wet granulation was determined.
| Materials and Methods|| |
Identification test for drug
Scanning of Losartan potassium was carried out in 0.1 N HCl and phosphate buffer (pH 6.8) using UV spectrophotometer and the plot of absorbance v/s wavelength was recorded.[Figure 1].
|Figure 1: In vitro release profile of best formulation with HPMC K15M/K100M|
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Drug excipients interaction study
The spectra for the prepared samples was recorded using FTIR spectrophotometer (JASCO 460 plus) and compared with the spectrum of drug to check the chemical interaction.
Formulation of sustained release matrix tablets
Tablets were prepared using different ratios of hydrophilic and hydrophobic polymers along with other excipients by wet granulation method single punch tablet machine.
Evaluation of sustained release matrix tablet
The prepared tablets were evaluated for hardness, thickness, friability, weight variation, drug content, swelling study, in vitro dissolution study, SEM study and stability studies.
| Results and Discussion|| |
Formulation excipients were selected based upon their compatibility with the drug. IR spectra showed that there was no interaction between the drug and the excipient. The tablets prepared from HPMC K15M/K100M with increasing concentration of Eudragit RS 100 showed significant difference between the results. It was clear from in vitro dissolution studies that the tablet with combination of HPMC K15M and Eudragit RS 100 showed better drug release pattern as compared to other batches. The drug release for extended duration is due to the rapid diffusion of dissolved drug through the hydrophilic gel matrix and hydrophobic matrix sustaining the release of the drug.
| Conclusion|| |
Losartan potassium can be formulated as a sustained release dosage form using 20% HPMC K15M with 5% Eudragit RS 100. Hydrophilic matrix of HPMC alone could not control the release of drug effectively for 12 hours and the release pattern was satisfactory. The use of Eudragit along with HPMC proved to show better retarding ability which was clearly seen from the result. ,
| References|| |
|1.||Gupta A, Gaud RS, Ganga S. Development, evaluation and optimization of extended release buccal tablets prepared using progressive hydration technology. Int J Drug Delivery 2010;2:37-48. |
|2.||Behera AK, Nayak AK, Mohanty BR. Development and optimization of losartan potassium tablets. Int J Appl Pharma 2010;2:15-9. |