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P. Ashok Kumar et al. J Sci Res Pharm, 2018;7(7):74-78

World Inventia Publishers

J

ournal of

S

cientific

R

esearch in

P

harmacy

http://www.jsrponline.com/

Vol. 7, Issue 7, 2018 ISSN: 2277-9469

USA CODEN: JSRPCJ

Research Article

FORMULATION AND INVITRO EVALUATION OF RIZATRIPTAN ORAL THIN FILMS

Perumalla Ashok Kumar 1 _{*, Dr. Deenanath Jhade}2

* 1 _{Research scholar, Department of Pharmaceutics, Sri Satya Sai University of Technology and Medical Sciences, Sehore, Madhya Pradesh, INDIA.}

2 Associate Professor, Department of Pharmaceutics, Sri Satya Sai University of Technology and Medical Sciences, Sehore, Madhya Pradesh, INDIA.

Received on: 11-06-2018; Revised and Accepted on: 16-07-2018

ABSTRACT

I

n present study oral thin films of Rizatriptan was developed to have a faster on set of action. The oral thin films were developed by using

polymers HPMC E5, HPMC E 15 and PVP K90.Oral thin films were prepared by employing solvent casting method. Propylene glycol was selected as permeation enhancer and plasticizer. Drug excipient compatibility studies were carried out by using FTIR, and it was observed that there were no interactions. Formulations were prepared with the varying concentrations polymers ranging from F1-F12, and all the formulations were evaluated for

various physical parameters Physical appearance, Weight variation, Thickness, Folding endurance,Tensile strength, Drug content, Moisture uptake,

Moisture content and all the results were found to be were found to be with in the pharmacopeial limits. Among all the 9 formulations of Rizatriptan F3 formulation which contains HPMC E15 150 mg showed 98.76% cumulative drug release within 30 min by performing dissolution test. Compared to HPMC E15, HPMC E5 and PVP K90, HPMC E 15 showed better drug release profile. Hence it was considered as optimized formulation.

KEYWORDS: Rizatriptan, HPMC E15, HPMC E5, PVP K90 and HPMC E 15.

INTRODUCTION

M

igraine is one of the ten most disabling disorders worldwide, and despite recent developments in the management of migraine, it remains underdiagnosed and undertreated. The new generation anti-migraine drug, Rizatriptan benzoate is an orally active serotonin 5- HT1receptor agonist that potently and selectively binds to 5-HT1B/1D subtypes. Chemically it is N,N-dimethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indole3-ethanamine monobenzoate [1-8]_{. The initial gut}

absorption of Rizatriptan is high (90%); however, the compound undergoes moderate first-pass metabolism, which limits the bioavailability to 47% [9-13]_{. So orally fast dissolving thin films of}

Rizatriptan prevents its first-pass metabolism and eliminates the need of intake of water by the patient during the migraine attack and provide fast onset of action which would be beneficial to migraine sufferers in resuming their functional abilities as soon as possible [14-17]_.

MATERIALS AND METHODS

R

izatriptan, HPMC E15, HPMC E5, PVP K90, Propylene Glycol, Citric Acid, Aspartame all the materials used were lab grade.

Solvent casting method: HPMC E5 and HPMC E15 were weighed in

required ratios and they were then dissolved in water (Cold water) as solvent. Rizatriptan, (20mg), Propylene glycol was added to the above dispersion under continuous stirring. The uniform dispersion was

*Corresponding author:

Perumalla Ashok Kumar

Research scholar,

Department of Pharmaceutics,

Sri Satya Sai University of Technology and Medical Sciences, Sehore, Madhya Pradesh, INDIA.

* E-Mail: [email protected]

DOI: https://doi.org/10.5281/zenodo.1318318

poured in the petri plate. The rate of evaporation of solvent was controlled by inverting cut funnel over the thin films. After 24h, the dried thin film were taken out and stored in desiccator.

Oral thin films are evaluated for the following parameters: Thickness of the film, Disintegration time, Dissolution time, Folding endurance, pH, Percentage of moisture uptake, Tensile strength of the film, Swelling property, Transparency are the various evaluation tests performed for the prepared fast disintegrating thin films.

RESULTS AND DISCUSSION

Standard Calibration curve of Rizatriptan:

It was found that the estimation of Rizatriptan by UV spectrophotometric method at λmax259 nm in 6.8 pHsaline phosphate

buffer and had good reproducibility and this method was used in the study. The correlation coefficient for the standard curve was found to be closer to 1, at the concentration range, 0.5-2.5μg/ml.

Evaluation of Rizatriptan oral thin films:

Physical appearance: All the Oral thin films were visually inspected for colour, clarity, flexibility.

Flatness:All the Oral thin films were found to be flat without any foam.

The prepared Rizatriptan Oral thin films were evaluated by physical methods such as Physical appearance, Weight variation, Thickness, Folding endurance, Drug content, Moisture uptake and Moisture content and all the results were found to be with in the pharmacopeial limits.

Tensile strength (F1):The patches (10 samples of each) were dried at

600_{C for 24 hrs. Then they were placed in an isometric transducer and}

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1 2 0.128 2 4 0.267 3 6 0.456 4 8 0.589 5 10 0.762 6 12 0.963

Fig. 1: Standard graph of Rizatriptan in pH 6.8 Phosphate buffer Table No. 3: Evaluation of Oral thin films by physical methods

Formulation Thickness

(mm) endurance Folding content (%) Drug Moisture uptake (%) Moisture content (%) Weight variation F1 0.3432 22 69 14.76 6.02 26.23 F2 0.3287 28 65.8 12.63 5.67 26.17 F3 0.3897 31 79.82 16.68 11.69 25.82 F4 0.3458 29 59.87 18.98 9.76 26.23 F5 0.3218 27 63.42 17.26 6.98 26.73 F6 0.3276 23 57.16 16.25 7.69 26.82 F7 0.3873 26 58.14 18.55 6.91 26.82 F8 0.3452 24 61.19 15.62 8.74 25.93 F9 0.3356 25 58.13 13.88 6.03 24.82 F10 0.3256 25 54.98 14.58 6.38 24.33 F11 0.3372 26 55.76 17.66 7.83 24.38 F12 0.3327 28 58.72 15.38 6.95 25.34

Table No. 4: In-Vitro Drug Release

Time (Min) F1 F2 F3 F4 F5 F6 F7 F8 F9 F10 F11 F12

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Fig. 2: Dissolution graph of all formulations (F1-F3)

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Table No. 5: Disintegration time

S. No. Disintegration Time (Sec)

F 1 39

F 2 47

F 3 43

F 4 56

F 5 59

F 6 68

F7 63

F8 61

F9 54

F10 56

F11 54

F12 58

CONCLUSION

I

n present study oral thin films of Rizatriptan was developed to have a faster on set of action. The oral thin films were developed by using polymers HPMC E5, HPMC E 15 and PVP K90.Oral thin films were prepared by employing solvent casting method. Propylene glycol was selected as permeation enhancer and plasticizer. Drug excipient compatibility studies were carried out by using FTIR, and it was observed that there were no interactions. Formulations were prepared with the varying concentrations polymers ranging from F1-F12, and all the formulations were evaluated for various physical parameters Physical appearance, Weight variation, Thickness, Folding endurance, Tensile strength, Drug content, Moisture uptake, Moisture content and all the results were found to be were found to be with in the pharmacopeial limits. Among all the 9 formulations of Rizatriptan F3 formulation which contains HPMC E15 150 mg showed 98.76% cumulative drug release within 30 min by performing dissolution test. Compared to HPMC E15, HPMC E5 and PVP K90, HPMC E 15 showed better drug release profile. Hence it was considered as optimized formulation.

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How to cite this article:

P. Ashok Kumar, Dr. Deenanath Jhade. FORMULATION AND INVITRO EVALUATION OF RIZATRIPTAN ORAL THIN FILMS. J Sci Res

Pharm 2018;7(7):74-78.DOI: https://doi.org/10.5281/zenodo.1318318

Conflict of interest: The authors have declared that no conflict of interest exists.