Formulation and Optimization of Zolmitriptan Orodispersible Tablets

  • T.V. Hari Hara Nadh Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh-522034, India
  • P. Sivaram Kumar Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh-522034, India
  • M. Venkata Ramana Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh-522034, India
  • N. Rama Rao Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh-522034, India

Abstract

Zolmitriptan is a selective 5-hydroxytryptamine receptor agonist reported for the acute migraine treatment, having poor water solubility leads to poor bioavailability. In the present study, attempt to improve the bioavailability of zolmitriptan with the help of PVP K-30 using the microwave irradiation method.  The zolmitriptan and PVP K- 30 in 1:1 ratio was subjected to microwave irradiation for different times such as 60,80,100,120 seconds at 650 watts. Characterization of solid dispersion was done by drug content, XRD, FTIR, DSC. FTIR analysis demonstrated there are no compatibility issues. XRD studies prove that the solid dispersion was in amorphous form. DSC studies prove that solid dispersion was amorphous based on the intensity of peaks. The prepared dispersion was made into orodispersible tablets by direct compression. The optimization of these formulations was carried out by using 32 factorial designs on Design Expert 10.0 software. In order to examine the effect of independent variables Crospovidone (X1), croscarmellose sodium (X2), and combined effect of independent variables 32 factorial design was selected. In this design, two responses such as disintegration time and % drug release were evaluated, and experimental trials are performed for all 9 formulations. For all formulations, the precompression and post-compression parameters were studied. Based upon the model optimized formulation (C1 and C2) was obtained having the disintegration time (34.4±0.84 and 39.8±0.91) and %drug release (98.7±0.42 and 93.2±0.46) respectively.


Keywords: Zolmitriptan, Solid dispersion, Microwave irradiation, Crospovidone, Croscarmellose sodium.

Keywords: Zolmitriptan, Solid dispersion, Microwave irradiation, Crospovidone, Croscarmellose sodium

Downloads

Download data is not yet available.

Author Biographies

T.V. Hari Hara Nadh, Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh-522034, India

Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh-522034, India

P. Sivaram Kumar, Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh-522034, India

Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh-522034, India

M. Venkata Ramana, Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh-522034, India

Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh-522034, India

N. Rama Rao, Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh-522034, India

Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh-522034, India

References

1. Hazee Peera N, Lohithasu D, Sahoo SK, Santhosh Naidu KMK, VAK. Formulation development and evaluation of oral disintegrating tablets of zolmitriptan. Der Pharm Lett. 2013; 5(2):324–32.
2. Dey P, Maiti S. Orodispersible tablets : A new trend in drug delivery. J Nat Sci Biol Med. 2010; 1(1):2–5.
3. Mostafa DAE, Khalifa MKA, Gad SS. Zolmitriptan Brain targeting via intranasal route using solid lipid nanoparticles for migraine therapy : Formulation, Characterization, in-vitro and In-vivo Assessment. Int J Appl Pharm. 2020; 12(2):1–8.
4. Alhalaweh A, Andersson S, Velaga SP. Preparation of zolmitriptan – chitosan microparticles by spray drying for nasal delivery. Eur J Pharm Sci. 2009; 38:206–14.
5. Moneghini M, Bellich B, Baxa P, Princivalle F. Microwave generated solid dispersions containing Ibuprofen. Int J Pharm. 2008; 361(1–2):125–30.
6. Humaira S, Munde MR, Road OJ. Validated UV spectroscopic method for estimation of zolmitriptan from tablet formulations. Int J Biomed Adv Res. 2010; 01(03):82–7.
7. Frizon F, Eloy J de O, Donaduzzi CM, Mitsui ML, Marchetti JM. Dissolution rate enhancement of loratadine in polyvinylpyrrolidone K-30 solid dispersions by solvent methods. Powder Technol [Internet]. 2013; 235:532–9.
8. Maurya D, Belgamwar V, Tekade A. Microwave induced solubility enhancement of poorly water soluble atorvastatin calcium. J Pharm Pharmacol. 2010; 1599–606.
9. Higuchi T CK. Phase-solubility techniques. In: Reilley CN. Adv Anal Chem Instrum. 2018; 7(3):180–2.
10. Ranpise NS, Kulkarni NS, Mair PD, Ranade AN. Improvement of water solubility and in vitro dissolution rate of aceclofenac by complexation with β-cyclodextrin and hydroxypropyl- β-cyclodextrin. Pharm Dev Technol. 2010; 15(April 2009):64–70.
11. Raina A, Sciences P. Microwave induced solubility enhancement of poorly water-soluble drug simvastatin using poloxamer 188 by microwave irradiation method. Int J Pharm Sci Res. 2020; 11(4):1643–52.
12. Morade VB, Daga VR, Malpure PR. Formulation and Evaluation of Mouth Dissolving Tablets of Zolmitriptan. Asian J Pharm Sci Technol. 2018; 8(2):43–51.
13. Gunda RK, Kumar JNS, Satyanarayana V, Batta S, Harika CM. Formulation Development and Evaluation of Carbamazepine Fast Dissolving Tablets. J Pharm Res. 2016; 10(5):216–25.
14. Naga J, Kumar S, Gunda RK. Design , Formulation and Evaluation of Pravastatin Fast Dissolving Tablets . 2018;9(1):15–22.
15. Egla M, Abd SN, Hammid A. Design of Zolmitriptan Liquisolid Orodispersible Tablets and Their In Vitro Evaluation. J Chem Pharm Res. 2016; 8(11):232–42.
16. Nandy BC, Gupta AK, Mittal A, Pradesh M. Design and development of solid dispersion system of zolmitriptan. J Biomed Pharm Res. 2013; 2(5):7–13.
17. Kumar A, Pal D, Santra K. Artocarpus heterophyllus L . seed starch-blended gellan gum mucoadhesive beads of metformin HCl. Int J Biol Macromol. 2014; 65:329–39.
18. Godbole MD, Sabale PM, Mathur VB. Development of lamivudine liposomes by three- level factorial design approach for optimum entrapment and enhancing tissue targeting. J Microencapsul. 2020; 0(0):1–14.
Statistics
145 Views | 311 Downloads
How to Cite
1.
Hari Hara Nadh T, Sivaram Kumar P, Venkata Ramana M, Rama Rao N. Formulation and Optimization of Zolmitriptan Orodispersible Tablets. JDDT [Internet]. 15May2021 [cited 18Sep.2021];11(3):50-7. Available from: https://jddtonline.info/index.php/jddt/article/view/4703