DESIGN AND DEVELOPMENT OF SIMVASTATIN GASTRORETENTIVE TABLETS FOR CONTROLLED RELEASE

  • NG Raghavendra Rao Sree Chaitanya Institute of Pharmaceutical Science, L.M.D. Colony, Thimmapur, Karimnagar - 505527, Telangana, India
  • M Laharika Jyothishmathi institute of pharmaceutical sciences, Ramakrishna colony, Karimnagar -505481, Telangana, India
  • C Kistayya St. Johns College of Pharmaceutical Science, Yerrakota, Yemmiganur - 518360, Kurnool, Andhra Pradesh, India

Abstract

Simvastatin is a Hypolipidemic used to control elevated cholesterol or hypercholesterolemia. The primary uses of simvastatin are for the treatment of dyslipidemia and the prevention of cardiovascular disease. Gastroretentive Floating tablets of Simvastatin were developed by direct compression method using HPMC K15M, HPMC K100M, Carbopol, sodium CMC, xanthan gum, sodium alginate polymers used and the mixture of the sodium bicarbonate, citric acid anhydrous as gas generating agents. The results of Pre-compressional and post compression parameters were within IP prescribed limits. The formulation FC1, FC2, FC3, FC4, FC5, FC6, FC8 floated but the lag time was more and floating time is less. For the formulation FC7, the duration of buoyancy was more than 12 hrs, the floating capacity increased in these formulations and floated with less lag time due to the high concentration of gas generating agent sodium bicarbonate-induced CO2 generation in the pressure of dissolution medium (pH 1.2 0.1N HCL). The drug release from the formulations FC1-FC8 was found to be 78.612, 72.66, 87.22, 63.45, 67.26, 73.24, 98.93, and 81.27 in 12hrs. Among all the formulations FC7 floating lag time 7 min with 99% of drug release has better control release of the drug. DSC and FTIR studies revealed that there was no incompatibility of the drug with the excipients used. The stability study conducted as per the ICH guidelines and the formulations were found to be stable. From this study, it can be concluded that the formulation retained for longer periods of time in the stomach and provides controlled release of the drug and may improve bioavailability.

Keywords: Controlled Gastroretentive tablets, Simvastatin, HPMC, Carbopol.

 

Downloads

Download data is not yet available.

Author Biographies

NG Raghavendra Rao, Sree Chaitanya Institute of Pharmaceutical Science, L.M.D. Colony, Thimmapur, Karimnagar - 505527, Telangana, India
Sree Chaitanya Institute of Pharmaceutical Science, L.M.D. Colony, Thimmapur, Karimnagar - 505527, Telangana, India
M Laharika, Jyothishmathi institute of pharmaceutical sciences, Ramakrishna colony, Karimnagar -505481, Telangana, India

Jyothishmathi institute of pharmaceutical sciences, Ramakrishna colony, Karimnagar -505481, Telangana, India

C Kistayya, St. Johns College of Pharmaceutical Science, Yerrakota, Yemmiganur - 518360, Kurnool, Andhra Pradesh, India

St. Johns College of Pharmaceutical Science, Yerrakota, Yemmiganur - 518360, Kurnool, Andhra Pradesh, India

References

1. Hoffman A. Pharmacodynamic aspects of sustained release prepara¬tions. Adv Drug Deliv Rev. 1998; 33:185–199.
2. Baumgartner S, Kristl J, Vrecer F, Vodopivec P, Zorko B. Optimisation of floating matrix tablets and evaluation of their gastric residence time. Int J Pharm. 2000; 195:125–135.
3. Singh BN, Kim KH. Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J Control Release. 2000; 63(3):235–259.
4. Streubel A, Siepmann J, Bodmeier R. Drug delivery to the upper small intestine window using gastroretentive technologies. Curr Opin Pharmacol. 2006; 6:501–508.
5. Nayak AK, Maji R, Das B. Gastroretentive drug delivery systems: a review. Asian J Pharm Clin Res. 2010; 3:2–10.
6. Lee TW, Robinson JR. Controlled release drug delivery systems. In: Gennaro AR, editor. The Science and Practice of Pharmacy. Vol I. 20th ed. Remington: Mack Publishing Company; 2000:1676-1693.
7. Kagan L, Lapidot N, Afargan M, et al. Gastroretentive accordion pill: enhancement of riboflavin bioavailability in humans. J Control Release. 2006; 113:208–215.
8. Murphy CS, Pillay V, Choonara YE, Du Toit LC. Gastroretentive drug delivery systems: current developments in novel system design and evaluation. Curr Drug Deliv. 2009; 6:451-460.
9. Xiaoqiang X, Minjie S, Feng Z, Yiqiao H. Floating matrix dosage form for phenoporlamine hydrochloride based on gas forming agent: in vitro and in vivo evaluation in healthy volunteers. Int J Pharm. 2006; 310:139-145.
10. Hwang SJ, Park H, Park K. Gastric retentive drug-delivery systems. Crit Rev Ther Drug Carrier Syst. 1998; 15(3):243–284.
11. Chavanpatil MD, Jain P, Chaudhari S, Shear R, Vavia RR. Novel sus¬tained release, swellable and bioadhesive gastroretentive drug delivery system for ofloxacin. Int J Pharm. 2006; 316(1–2):86–92.
12. Deshpande AA, Shah NH, Rhodes CT, Malick W. Development of a novel controlled release system for gastric retention. Pharm Res. 1997; 14:815-819.
13. Davis DW. Method of swallowing a pill. US Patent. 1968; 3(418):999.
14. Rouge N, Buri P, Doelker E. Drug absorption sites in the gastroin¬testinal tract and dosage forms for site-specific delivery. Int J Pharm. 1996; 136:117–139.
15. Brahma N, Kwon HK. Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J Controlled Release. 2000; 63:235–259.
16. Seth PR, Tossounian J. The hydrodynamically balanced system, a novel drug delivery system for oral use. Drug Dev Ind Pharm. 1984; 10:313–339.
17. Hilton AK, Deasy PB. In vitro and in vivo evaluation of an oral sustained-release floating dosage form of amoxycillin trihydrate. Int J Pharm. 1992; 86(1):79–88.
18. Rubinstein A, Friend DR. Specific delivery to the gastrointestinal tract. In: Domb AJ, editor. Polymeric Site-Specific Pharmacotherapy. Chichester: Wiley; 1994:282-283.
19. Raghavendra Rao NG, Vijaya Kumar G, Akhlaaq Ahmad. Formulation and Evaluation of Gas Powered System of captopril tablets. American Journal of Pharmacy and Health Resaerch. AJPHR: 2015; 3(9):40 - 56.
20. Raghavendra Rao NG, Vijaya Kumar G, Priyanka V. Design and Development of Niveripine Gas powered systems for controlled release. Asian Journal of Biochemical and Pharmaceutical Research. AJBPR. 2015; 5(3):146-157.
21. Raghavendra Rao NG, Sunil Firangi, Keyur Patel. Formulation And In-Vitro Evaluation Of Zidovudine Gastroretentive Floating Drug Delivery System For Prolong Release. International Journal of Current Biomedical and Pharmaceutical Research. IJCBPR: 2011; 1(4):226-233.
22. Raghavendra Rao NG, Sunil Firangi, Keyur Patel. Formulation and Evaluation Of Gastroretentive Effervescent Floating Drug Delivery System Of Zidovudine. American Journal of Pharma Tech Research. AJPTR: Feb: 2012; 2(1):513-529.
23. Raghavendra Rao NG, Shrishail Ghurghure. Formulation and Evaluation of Zidovudine Controlled Release Gas Powered System Using hydrophilic Polymer. International Research Journal of Pharmacy. IRJP 2 (3), March-2011:86-94.
24. Raghavendra Rao NG, Harsh A Panchal, Pentewar Ram. Formulation And In-Vitro Evaluation Gastroretentive Drug Delivery System Of Cefixime For Prolong Release. Der Pharmacia Sinica, 2011, 2 (2):236-248.
Statistics
114 Views | 138 Downloads
How to Cite
Rao, N., Laharika, M., & Kistayya, C. (2017). DESIGN AND DEVELOPMENT OF SIMVASTATIN GASTRORETENTIVE TABLETS FOR CONTROLLED RELEASE. Journal of Drug Delivery and Therapeutics, 7(1), 30-36. https://doi.org/10.22270/jddt.v7i1.1353