DESIGN AND DEVELOPMENT OF LORAZEPAM RECTAL SUPPOSITORIES USING NATURAL POLYMERS.
Main Article Content
Keywords
.
Abstract
The Objective of present Research work was to develop different suppository bases in order to overcome drawbacks of traditional base and to study release of Phenytoin from developed bases. Cocoa butter was used as a base for one of the formulations while for other formulations combinations of suppository bases were prepared by fusion method. Hydrogenated vegetable oil was combined with cocoa butter, poloxamer 407 and polyethylene glycol 2000. Developed bases were evaluated for physicochemical parameters such as appearance, hardness, weight variation, hydroxyl value, etc and used for the preparation of lorazepam suppository. The suppositories of lorazepam were evaluated for physical parameters, drug content and in vitro drug release studies. The optimized suppository base was characterized by infrared spectroscopy and X-ray diffraction analysis. All the combination of suppository bases showed physical parameters within the prescribed range. Hydroxyl value of developed based showed in the range of 89.76-134.64.From the results, it is evident to prefer poloxamer 407 and polyethylene glycol 2000 with hydrogenated vegetable oil for faster release. The lorazepam suppositories also showed physical parameters within the prescribed limit. Formulation containing poloxamer 407 and hydrogenated vegetable oil showed 99.44% drug release at end of 120min with 61.83% dissolution efficiency and 45.38min mean dissolution time. The infrared spectroscopy indicated compatibility of drug with Excipients and X-ray diffraction and differential scanning calorimetry analysis showed reduction in degree of crystallinity of Phenytoin thus improving dissolution rate of drug. It can be concluded that poloxamer 407 and hydrogenated vegetable oil could be combined to deliver poorly soluble drug like Phenytoin
References
2. Salunkhe NH, Jadhav NR, Mali KK, Dias RJ, Ghorpade VS, Yadav a. V. Mucoadhesive microsphere based suppository containing granisetron hydrochloride for management of emesis in chemotherapy. J Pharm Investig. 2014;44(4):253–63.
3. Jadhav UG, Dias RJ, Mali KK, Havaldar VD. Development of in situ-gelling and mucoadhesive liquid suppository of ondansetron. Int J ChemTech Res. 2009;1(4):953–61.
4. Prasanna LJ, Rao RN. Rectal drug delivery: A promising route for enhancing drug absorption. Asian J Res Pharm Sci. 2012;2(4):143–9.
5. Swamy P V, Farhana L, Shirsand SB, Ali Y, Patil A. Design and Evaluation of Rectal Suppositories of Carvedilol. Int J Pharm Sci Nanotechnol. 2009;2(3):654–60.
6. Havaldar VD, Yadav A V., Dias RJ, Mali KK, Ghorpade VS, Salunkhe NH. Rectal suppository as an effective alternative for oral administration. Res J Pharm Technol. 2015;8(6):759.
7. Koliqi R, Polidori C, Islami H. Prevalence of Side Effects Treatment with Carbamazepine and Other Antiepileptics in Patients with Epilepsy. Mater Sociomed. 2015;27(3):167–71.
8. Dias RJ, Mali KK, Ghorpade VS, Havaldar VD, Mohite VR. Formulation and Evaluation of Carbamazepine Liquisolid Compacts Using Novel Carriers. Indian J Pharm Educ Res. 2017;51(S2): S69–78.
9. Lehr CM, Bouwstra JA, Schacht EH, Junginger HE. In vitro evaluation of mucoadhesive properties of chitosan and some other natural polymers. Int J Pharm. 1992;78(1-3):43–8.
10. Jawahar N, Jayaprakash S, Maria GS, Nagarajan M, Moorthi D, Jubie S, et al. Design and evaluation of Sustained release suppositories if nimesulide. Indian J Pharm Sci. 2005;67(5):558– 61.
11. Fleming J. Rapid method for the of hydroxyl values. J Soc Cosmet Chem. 1966; 630(17):625–30.
12. Shinoda M, Akita M, Hasegawa M, Nadai M, Hasegawa T, Nabeshima T, et al. Pharmaceutical evaluation of carbamazepine suppositories in rats. Biosci Biotechnol Biochem. 1995;18(9):1289–91.
13. Patel JK, Patel RP, Amin AF, Patel MM. Formulation and evaluation of mucoadhesive glipizide microspheres. AAPS PharmSciTech. 2005;6(1): E49–55.
14. Swamy PV, Ali MY, Anand Kumar Y, Prasad K, Srinivaslu N. Design and evaluation of rectal drug delivery systems of non- steroidal anti-inflammatory drug. Int. Curr Pharm J. 2012;1(7):165–70.
15. Schmllt M. Influence of the Hydrophilicity of Suppository Bases on Rectal Absorption of Carprofen, a Lipophilic Nonsteroidal Anti-inflammatory Drug. J Pharm Sci. 1990;79(4):359–63.
16. Wakita K, Kuwabara H, Furusho N, Tatebe C, Sato K, Akiyama H. A Comparative Study of the Hydroxyl and Saponification Values of Polysorbate 60 in International Food Additive Specifications. Am J Anal Chem. 2014;05(03):199–204.
17. Hermann TW. Recent research on bioavailability of drugs from suppositories. Int J Pharm. 1995;123(1):1–11.
18. Baria AH, Patel RP, Suthar AM, Parmar RB. Formulation Development and Evaluation of Sustained Release Aceclofenac Suppository. Int J Pharm Sci Drug Res. 2009;1(2):71–3.
19. Saleem M, Taher M, Sanaullah S, Najmuddin M, Ali J, Humaira S, et al. Formulation and evaluation of tramadol hydrochloride rectal suppositories. Indian J Pharm Sci. 2008;70(5):640.
20. Costa P, Sousa Lobo JM. Modeling and comparison of dissolution profiles. Vol. 13, European Journal of Pharmaceutical Sciences. 2001. p. 123–33.
Article Sidebar
Article Details
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
All articles published in JPTCP are licensed under Copyright Creative Commons Attribution-NonCommercial 4.0 International License.
Swapnil R. Nazarkar
Assistant Professor, Vidya Niketan College of Pharmacy, Lakhewadi
Samrat A. Khedkar
Assistant Professor, Vidya Niketan College of Pharmacy, Lakhewadi
Amol A. Ban
Assistant Professor, Vidya Niketan College of Pharmacy, LakhewadiRajendra G. Kharade
Assistant Professor, Vidya Niketan College of Pharmacy, LakhewadiRachana S. Das
Assistant Professor, Vidya Niketan College of Pharmacy, Lakhewadi