Formulation of Carbopol Capsules for Sustained Release of Losartan Potassium
Sustained release formulations have been extensively studied for their benefits in improving various physicochemical and pharmacokinetic properties of large number of drugs. The aim of this study was to develop and evaluate sustained release capsules of losartan potassium in order to provide drug release over a long period of time. This allows the drug much time for absorption in gastrointestinal tract (GIT) and hence may increase the bioavailability of the drug. Carbopol 971 P was used as rate controlling polymer for the preparation of capsules. The capsules were evaluated for matrix integrity and drug release using USP type II dissolution apparatus. The sustained release capsules showed excellent matrix integrity and released more than 90% of the drug over a period of 12 hours. The kinetic studies showed that the drug release from the carbopol matrices followed Korsmeyer Peppas release kinetics and hence the mechanism of drug release was a combination of more than one processes i.e. diffusion and erossion. Hydration volume as well as matrix integrity were affected by the change in the amount of the polymer in the capsules. The study suggests that carbopol 971P capsules can be efficiently used to control and extend the release of losartan potassium over a long period. Thus improved absorption and bioavailability can be achieved which requires further studies in animals in future.
Keywords: Sustained release, Carbopol, Hydration volume, Capsules
2. Neau SH, Loka NC, 15 Pharmaceutical Salts, Water-Insoluble Drug Formulation. 2018:451.
3. Serajuddin AT. Salt formation to improve drug solubility, Advanced drug delivery reviews, 2007; 59(7):603-16.
4. Loftsson T, Hreinsdóttir D, Másson M, Evaluation of cyclodextrin solubilization of drugs, International journal of pharmaceutics, 2005; 302(1-2):18-28.
5. Fine-Shamir N, Beig A, Zur M, Lindley D, Miller JM, Dahan A, Toward successful cyclodextrin based solubility-enabling formulations for oral delivery of lipophilic drugs: solubility–permeability trade-off, biorelevant dissolution, and the unstirred water layer, Molecular pharmaceutics, 2017; 14(6):2138-46.
6. Jambhekar SS, Breen P, Cyclodextrins in pharmaceutical formulations I: structure and physicochemical properties, formation of complexes, and types of complex, Drug Discovery Today, 2016; 21(2):356-62.
7. Raillard SP, Mann A, Manthati SK, Scheuerman RA, Estrada T, Nguyen MQ, et al., Methods of synthesizing a levodopa ester prodrug, Google Patents; 2017.
8. Sharma D, Solubility enhancement strategies for poorly water-soluble drugs in solid dispersions: A review, Asian Journal of Pharmaceutics (AJP): Free full text articles from Asian J Pharm, 2016; 1(1).
9. Vasconcelos T, Marques S, das Neves J, Sarmento B, Amorphous solid dispersions: Rational selection of a manufacturing process, Advanced drug delivery reviews, 2016; 100:85-101.
10. Gao L, Liu G, Ma J, Wang X, Zhou L, Li X, et al., Application of drug nanocrystal technologies on oral drug delivery of poorly soluble drugs, Pharmaceutical research, 2013; 30(2):307-24.
11. Liu Y, Sun C, Hao Y, Jiang T, Zheng L, Wang S, Mechanism of dissolution enhancement and bioavailability of poorly water soluble celecoxib by preparing stable amorphous nanoparticles, Journal of Pharmacy & Pharmaceutical Sciences, 2010; 13(4):589-606.
12. Zhang Y, Huang Z, Omari-Siaw E, Lu S, Zhu Y, Jiang D, et al., Preparation and in vitro–in vivo evaluation of sustained-release matrix pellets of capsaicin to enhance the oral bioavailability, AAPS PharmSciTech, 2016; 17(2):339-49.
13. Lin Q, Fu Y, Li J, Qu M, Deng L, Gong T, et al., A (polyvinyl caprolactam-polyvinyl acetate–polyethylene glycol graft copolymer)-dispersed sustained-release tablet for imperialine to simultaneously prolong the drug release and improve the oral bioavailability, European Journal of Pharmaceutical Sciences, 2015; 79:44-52.
14. Sun Z, Yuan S, Zhao H, Wang Z, Liu Z, Preparation and evaluation of 1-deoxynojirimycin sustained-release pellets vs conventional immediate-release tablets, Journal of microencapsulation, 2017; 34(3):293-8.
15. Ahmed GF, Bathena SPR, Brundage RC, Leppik IE, Conway JM, Schwartz JB, et al., Pharmacokinetics and saturable absorption of gabapentin in nursing home elderly patients, The AAPS journal, 2017; 19(2):551-6.
16. Swearingen D, Aronoff GM, Ciric S, Lal R, Pharmacokinetics of immediate release, extended release, and gastric retentive gabapentin formulations in healthy adults, International journal of clinical pharmacology and therapeutics, 2018; 56(5):231.
17. Meshali M, El-Sayed G, El-Said Y, Abd El-Aleem H, Preparation and evaluation of theophylline sustained-release tablets, Drug development and industrial pharmacy, 1996; 22(4):373-6.
18. Tapia-Albarran M, Villafuerte-Robles L, Assay of amoxicillin sustained release from matrix tablets containing different proportions of Carbopol 971P NF, International journal of pharmaceutics, 2004; 273(1-2):121-7.
19. Radhakrishnan P, Chacko S, Saraswathi R, Krishnan PN, Matrix Based Sustained Release Tablets of Carvedilol: Formulation and In-vitro Characterization, Drug Delivery Letters, 2018; 8(2):153-8.
20. Goa KL, Wagstaff AJ, Losartan potassium, Drugs, 1996; 51(5):820-45.
21. De Paula WX, Denadai ÂM, Braga AN, Shastri VP, Pinheiro SV, Frezard F, et al., A long-lasting oral preformulation of the angiotensin II AT1 receptor antagonist losartan, Drug development and industrial pharmacy, 2018; 44(9):1498-505.
22. Wankhede SB, Raka KC, Wadkar S, Chitlange SS, Spectrophotometric and HPLC methods for simultaneous estimation of amlodipine besilate, losartan potassium and hydrochlorothiazide in tablets, Indian journal of pharmaceutical sciences, 2010; 72(1):136.
23. Gutiérrez-Sánchez PE, Hernández-León A, Villafuerte-Robles L, Effect of sodium bicarbonate on the properties of metronidazole floating matrix tablets, Drug development and industrial pharmacy, 2008; 34(2):171-80.
24. Khan GM, Jiabi Z, Formulation and in vitro evaluation of ibuprofen-carbopol® 974P-NF controlled release matrix tablets III: influence of co-excipients on release rate of the drug, Journal of Controlled Release, 1998; 54(2):185-90.
25. Cedillo-Ramirez E, Villafuerte-Robles L, Hernandez-Leon A, Effect of added Pharmatose DCL11 on the sustained-release of metronidazole from Methocel K4M and Carbopol 971P NF floating matrices, Drug development and industrial pharmacy, 2006; 32(8):955-65.
26. Khan GM, Zhu J-B, Studies on drug release kinetics from ibuprofen–carbomer hydrophilic matrix tablets: influence of co-excipients on release rate of the drug, Journal of Controlled Release, 1999; 57(2):197-203.
27. Dash S, Murthy PN, Nath L, Chowdhury P, Kinetic modeling on drug release from controlled drug delivery systems, Acta Pol Pharm, 2010; 67(3):217-23.
28. Costa P, Lobo JMS, Modeling and comparison of dissolution profiles, European journal of pharmaceutical sciences, 2001; 13(2):123-33.
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported License. that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (SeeÂ The Effect of Open Access).