DESIGN AND DEVELOPMENT OF TOPICAL HYDROGEL FORMULATION OF IRBISARTAN
Objective: Irbesartan is an antihypertensive with limited bioavailability. The objective of the study was to develop controlled release matrix tablets of irbisartan drug.
Methods: Tablets were prepared by wet granulation process. Result: In vitro drug release study revealed that HPMC causes initial burst release of drug hence combining HPMC sustained the action for 8 h (95.92±0.57% release). Fitting the in vitro drug release data to Korsmeyer equation indicated that diffusion along with erosion could be the mechanism for drug release. Compared to conventional tablets, the release of model drug from these HPMC matrix tablets was prolonged, leading to achieve an effective therapy with a low dosage of the drug, to reduce the frequency of medication. The pharmacological and clinical properties of irbesartan, a noncompetitive angiotensin II receptor type 1 antagonist, successfully used for more than a decade in the treatment of essential hypertension.
Results: Compatibility Studies In order to investigate the possible interactions between irbesartan and distinct polymers and/or diluents, FT-IR and DSC studies were carried out. FT-IR results proved that the drug was found to be compatible with excipients as wave numbers are almost similar for pure drug and also drug excipients mixture. In picture 1 and 2. DSC studies indicate that chosen excipients for the formulation were found to be compatible with the active ingredient as the melting endothermic peaks are in the range of 250-320 °C which is same as the melting point of irbisartan.
Conclusion: Irbesartan exerts its antihypertensive effect through an inhibitory effect on the pressure response to angiotensin II. Irbesartan 150–300 mg once daily confers a lasting effect over 24 h, and its antihypertensive efficacy is further enhanced by the coadministration of hydrochlorothiazide.
2. Toti US, Aminabhavi TM. Modified guar gum matrix tablet for controlled release of diltiazem hydrochloride. J Controlled Release 2004;95:567-77.
3. Shruti Chopra GV Patil, Motwani SK. Release modulating hydrophilic matrix systems of losartan potassium: optimization of formulation using statistical experimental design. Eur J Pharm Biopharm 2007;66:73-82.
4. Lachman L, Lieberman HA, Kanig editors JL. The theory and practice of industrial pharmacy. 1st edition. Varghee publishing house, Bombay; 1991. p. 293-430.
5. Bravo SA, Lamas MC, Salomon CJ. In vitro studies of diclofenac sodium controlled release from bio-polymeric hydrophilic matrices. J Pharm Pharm Sci 2002;5:213-9.
6. Al-Saidan SM, Krishnaiah YS, Patro SS, Satyanaryana V. In vitro and in vivo evaluation of guar matrix tablets for oral controlled release of water-soluble Diltiazem HCl. AAPS PharmSciTech 2005;6:14-21.
7. Khullar P, Khar RK, Agarwal SP. Evaluation of hydrogel-based controlled release niacin tablets. Drug Dev Ind Pharm 1998;24:479-83.
8. Rokade AP, Kulkarni PV, Mallikarjuna NN, Aminabhavi TM. Preparation and characterization of novel semi-interpenetrating polymer network hydrogel microspheres of chitosan and hydroxyl propyl cellulose for controlled release of chlorothiazide. J Microencapsulation 2009;26:27-36.
9. Elkheshen S, Yassin AE, Alkhaled F. Per-oral extended release bioadhesive tablet formulation of Verapamil Hcl hydrogel tablets. Boll Chim Farm 2003;142:226-31.
10. Atul Kuksal, Tiwary AK, Jain NK, Jain S. Formulation and in vitro, in vivo evaluation of extended release matrix tablets of Zidovudine: influence of the combination of hydrophilic and hydrophobic matrix formers. AAPS PharmSciTech 2006;7:1-8.
11. Chen Chih Ming, Chiao, Charles SL. Controlled release hydrogel formulation, U. S. Patent US 5419917; 1995.
12. Gupta NV, Satish CS, Shivakumar HG. Preparation and characterization of gelatin-poly (methacrylic acid) interpenetrating polymer network hydrogels as a pH-sensitive delivery system for Glipizide. Indian J Pharm Sci 2007;69:64-8.
13. Changez M, Burugapalli K, Koul V, Choudhary V. The effect of the composition of poly (acrylic acid)-gelatin hydrogel on gentamycin sulphate release: in vitro. Bio-materials 2003;24:527-36.
14. Hemant YKS, Satish CS, Shivakumar HG. Preparation and evaluation of chitosan-poly (acrylic acid) hydrogels as stomach specific delivery for amoxicillin and metronidazole. Ind J Pharm Sci 2007;69:91-5.
This work is licensed under a Creative Commons Attribution 4.0 International License.