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International Research Journal of Engineering and Technology (IRJET) e-ISSN: 2395-0056
Volume: 07 Issue: 03 | Mar 2020 www.irjet.net p-ISSN: 2395-0072
© 2020, IRJET | Impact Factor value: 7.34 | ISO 9001:2008 Certified Journal | Page 4318
Formulation and Evaluation of Tinidazole Loaded Fast Dissolving Tablets
Pranshu Tangri*, Ng Raghavendra Rao, Akshyay Chauhan, Piyush Chauhan, Tridev Kumar, Surbhi
Verma
Grd(Pg)Imt, Dept of Pharmaceutics, 214, Rajpur Road,Dehradun
-----------------------------------------------------------------------***------------------------------------------------------------------------
Abstract: The current research work deals with the development of fast dissolving tablets of tinidazole using a blend of
natural and synthetic polymers. Six formulations were prepared (T1-T6) by varying the composition of polymers in a ratio of
1:1 to 1:5. All the prepared formulations were evaluated for various parameters like hardness, weight variation, friability,
content uniformity, disintegration time, in-vitro drug release study and also stability study. The study reveals optimum
formulation blends and good in-vitro release profile showing rapid disintegration and rapid dissolution profile. The tablets
showed t80% within 6mins with disintegration time within 1 min. the formulation blends can be used as a model to formulate
other drugs of known potency and bioavailability profile. Fast dissolving tablets are a very ideal dosage form for children and
other patients who have difficulty in swallowing and hence van be used with advantageous benefits to the patient.
Key words: Tinidazole, fast dissolving tablets, rapid dissolving, rapid action
1. Introduction
Oral route is the most preferred route for administration of drugs. Because it provides high patient compliance. Dysphagia is
commonly found among all age groups. Due to this problem, approximately 67% population suffers. The main problem in
swallowing may be due to the taste, size, and surface of dosage forms. The geriatric and pediatric patients experience difficulty
in swallowing conventional tablets, which leads to poor patient compliance. During journey, sometime water is not available
so the patient feels difficulty for intake the solid dosage form. Hence there is an urgent need to developed novel dosage form
that improved the patient compliance. [1,2] The MDT is also known as fast melting, fast dispersing, rapid dissolve, rapid melt,
and or quick disintegrating tablet. All MDTs approved by the Food and Drug Administration (FDA) are classified as orally
disintegrating tablets. Recently, the European Pharmacopeia adopted the term Orodispersible tablet for a tablet that disperses
or disintegrates in less than 3 minutes in the mouth before swallowing. Mouth dissolving of tablet results in quick dissolution
and rapid absorption which provide rapid onset of action. Moreover, drug candidates that undergo pre-gastric absorption
when formulated as MDTs may show increased oral bioavailability. It provides good stability, accurate dosing, and easy
manufacturing. The excipients employed in MDTs are always hydrophilic in nature whereas drug may be either hydrophilic or
hydrophobic. If the drug is hydrophilic, the dosage form is known as fast dissolving tablets otherwise if drug is hydrophobic it
is known as fast disintegrating tablets.[3-5]
1.1 Advantages of MDTs [6,7]
 No need of water to swallow the tablet.
 Apart from it the drug is protected from degradation due to pH and GIT enzymes.
 It improves patient compliance.
 It provides rapid drug delivery from the dosage forms.
 Drug administration through buccal mucosa is easy.
 The large contact area of the oral cavity contributes to rapid and extensive drug absorption.
 Patient compliance is more.
 Having rapid onset of action which may leads to an improved bioavailability.
 Patient having difficulty in swallowing tablet can easily administer this type of dosage form.
 Useful for pediatric, geriatric and psychiatric patients.
International Research Journal of Engineering and Technology (IRJET) e-ISSN: 2395-0056
Volume: 07 Issue: 03 | Mar 2020 www.irjet.net p-ISSN: 2395-0072
© 2020, IRJET | Impact Factor value: 7.34 | ISO 9001:2008 Certified Journal | Page 4319
2. Materials and methods
2.1 Materials
All materials and reagents used were of AR grade and good quality. The drug albendazole was procured from systropic ltd.,
baddi, HP, India. All equipments wrer available and used in the department of pharmaceutics, GRD(PG)IMT, Dehradun.
2.2 Methods
Following study was done in relation to formulation of fast dissolving tablets. [8-11]
a) Preformulation study of drug:
Particle size, solubility, partition coefficient, melting point and drug excipient compatibility were determined by standard
methods
b) Standard curve of drug tinidazole
Standard curve of tinidazole was prepared in buffer Ph medium 6.8 to mimic the salivary ph and hence give indication of
measurement of drug concentration.
c) Formulation of fast dissolving tablets
Fast dissolving tablets were prepared by direct compression and the composition of the tablets is given as follows
Table No. 1 Formulation Composition
Formulation code
Ingredient/quantity T1 T2 T3 T4 T5 T6
Drug 150 150 150 150 150 150
MCC 100 100 100 100 100 100
Cross povidone 25 50 25 - - 15
Sodium starch
glycolate
- - 25 25 50 15
Cross carmellose
sodium
- - - - - 15
Lactose 75 50 50 75 50 50
Starch 50 50 50 50 50 50
aspartame 10 10 10 10 10 10
Talc 1 1 1 1 1 1
Magnesium stearate 2 2 2 2 2 2
 All ingredients are mg
d) Evaluation parameters
All the prepared batches were evaluated for organoleptic features, hardness, friability, weight variation, disintegration time,
content uniformity and in-vitro drug dissolution study by standard testing methods and procedures.
Results and discussion
The results of the prepared formulations are given as
International Research Journal of Engineering and Technology (IRJET) e-ISSN: 2395-0056
Volume: 07 Issue: 03 | Mar 2020 www.irjet.net p-ISSN: 2395-0072
© 2020, IRJET | Impact Factor value: 7.34 | ISO 9001:2008 Certified Journal | Page 4320
Table No. 2 Results of Evaluation Parameters
Evaluation
parameter
Formulation code
T1 T2 T3 T4 T5 T6
Hardness
(kg/cm2)
3.5 4.3 4.6 3.9 4.5 4.6
Friability (%) 1.3 1.1 0.9 0.8 0.7 0.87
weight
variation (%)
±2.3 ±3.5 ±3.2 ±4.6 ±4.8 ±2.1
Content
uniformity
(%)
97.6% 93.2% 98.6% 98.3% 94.6% 95.8%
Disintegration
time (sec)
37 43 39 36 38 41
T 80% (mins) 6 mins 6.5 mins 6.7 mins 6.4 mins 6.7 mins 6.8 mins
Figure No. 1 Hardness & Friability
Figure No. 2 Weight Variation & Content Uniformity
0
0.5
1
1.5
2
2.5
3
3.5
4
4.5
5
T1 T2 T3 T4 T5 T6
HARDNESS & FRIABILITY
HARDNESS
FRIABILITY
International Research Journal of Engineering and Technology (IRJET) e-ISSN: 2395-0056
Volume: 07 Issue: 03 | Mar 2020 www.irjet.net p-ISSN: 2395-0072
© 2020, IRJET | Impact Factor value: 7.34 | ISO 9001:2008 Certified Journal | Page 4321
Figure No. 3 Disintigration Time
Figure No. 4 In-Vitro Release of Formulations
0
10
20
30
40
50
60
70
80
90
100
T1 T2 T3 T4 T5 T6
WEIGHT VARIATION & CONTENT UNIFORMITY
WEIGHT VARIATION
CONTENT UNIFORMITY
32
34
36
38
40
42
44
T1 T2 T3 T4 T5 T6
TIME(SEC)
DISINTIGRATION TIME
International Research Journal of Engineering and Technology (IRJET) e-ISSN: 2395-0056
Volume: 07 Issue: 03 | Mar 2020 www.irjet.net p-ISSN: 2395-0072
© 2020, IRJET | Impact Factor value: 7.34 | ISO 9001:2008 Certified Journal | Page 4322
Conclusion
All the prepared batches were found to be consistent, stable and show a good rapid release profile. All evaluation parameters
results were found to be within acceptance criteria and the formulations can be further evaluated for stability studies under
long term profile. The results are encouraging and prove the effectiveness of the selected polymeric combinations which can
be successfully utilized of other formulations as well
References
1. Salem I, Lopez K, Galan A, Florey K. Profiles of Drug substances and Excipients 27th Edition., California, USA Academic Press,
2000; pp. 304–16.
2. Dixit AR, Rajput SJ, Patel SG. Preparation and bioavailability assessment of SMEDDS containing valsartan, AAPS Pharm
SciTech 2010; 11:314–21.
3. Raja RK, Abbulu K, Sudhakar M. Development, characterization and solubility study of solid dispersion of valsartan. J Chem
Pharm Res 2011; 3:180–7.
4. Blagden N, Matas M, Gavan P, York P. Crystal engineering of active pharmaceutical ingredients to improve solubility and
dissolution rates. Adv Drug Deliv Rev 2007; 59:617–30.
5. Jin X, Zhang Z, Sun E, Li S, Jia X. Statistically designed enzymatic hydrolysis of an icariin/b-cyclodextrin inclusion complex
optimized for production of icaritin. Acta Pharma 2012; 2:83–9.
6. Cappello B, Maio DC, Iervolino M, Miro A. Improvement of solubility and stability of valsartan by hydroxypropyl -
bcyclodextrin. J Inclusion Phenomena Macrocyclic Chem 2005; 54:289–94.
7. Ibrahim HK, El-Setouhy DA. Valsartan orodispersible tablets: formulation, in vitro/in Vivo characterization. AAPS
PharmSciTech 2010; 11:89–96.
8. Abbas KA, Mohamed A, Abdulamir AS, Abas HA. A review on supercritical fluid extraction as new analysis method. American
J. Biochem Biotech 2008; 4:345–53.
9. Agnivesh R, Shrivastava, Bhalchandra, Ursekar, Chhanda J, Kapadia. Design, optimization, preparation and evaluation of
dispersion granules of valsartan and formulation into tablets. Current Drug Del 2009; 6:28–37.
10. Habib W, Khankari R, Hontz J. Fast-dissolving drug delivery systems. Crit Re Ther Drug Carrier Systems 2000; 17:61–72.
11. Deepak S, Dinesh K, Mankaran S, Gurmeet S, Rathore MS. Fast disintegrating tablets: A new era in novel drug delivery
system and new market opportunities. J Drug Deliv Ther 2012; 2(3):74–86.
0
20
40
60
80
100
120
0 1 2 3 4 5 6 7 8 9
%DRUGRELEASE
TIME(MINS)
%IN-VITRO DRUG RELEASE
T1
T2
T3
T4
T5
T6

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IRJET - Formulation and Evaluation of Tinidazole Loaded Fast Dissolving Tablets

  • 1. International Research Journal of Engineering and Technology (IRJET) e-ISSN: 2395-0056 Volume: 07 Issue: 03 | Mar 2020 www.irjet.net p-ISSN: 2395-0072 © 2020, IRJET | Impact Factor value: 7.34 | ISO 9001:2008 Certified Journal | Page 4318 Formulation and Evaluation of Tinidazole Loaded Fast Dissolving Tablets Pranshu Tangri*, Ng Raghavendra Rao, Akshyay Chauhan, Piyush Chauhan, Tridev Kumar, Surbhi Verma Grd(Pg)Imt, Dept of Pharmaceutics, 214, Rajpur Road,Dehradun -----------------------------------------------------------------------***------------------------------------------------------------------------ Abstract: The current research work deals with the development of fast dissolving tablets of tinidazole using a blend of natural and synthetic polymers. Six formulations were prepared (T1-T6) by varying the composition of polymers in a ratio of 1:1 to 1:5. All the prepared formulations were evaluated for various parameters like hardness, weight variation, friability, content uniformity, disintegration time, in-vitro drug release study and also stability study. The study reveals optimum formulation blends and good in-vitro release profile showing rapid disintegration and rapid dissolution profile. The tablets showed t80% within 6mins with disintegration time within 1 min. the formulation blends can be used as a model to formulate other drugs of known potency and bioavailability profile. Fast dissolving tablets are a very ideal dosage form for children and other patients who have difficulty in swallowing and hence van be used with advantageous benefits to the patient. Key words: Tinidazole, fast dissolving tablets, rapid dissolving, rapid action 1. Introduction Oral route is the most preferred route for administration of drugs. Because it provides high patient compliance. Dysphagia is commonly found among all age groups. Due to this problem, approximately 67% population suffers. The main problem in swallowing may be due to the taste, size, and surface of dosage forms. The geriatric and pediatric patients experience difficulty in swallowing conventional tablets, which leads to poor patient compliance. During journey, sometime water is not available so the patient feels difficulty for intake the solid dosage form. Hence there is an urgent need to developed novel dosage form that improved the patient compliance. [1,2] The MDT is also known as fast melting, fast dispersing, rapid dissolve, rapid melt, and or quick disintegrating tablet. All MDTs approved by the Food and Drug Administration (FDA) are classified as orally disintegrating tablets. Recently, the European Pharmacopeia adopted the term Orodispersible tablet for a tablet that disperses or disintegrates in less than 3 minutes in the mouth before swallowing. Mouth dissolving of tablet results in quick dissolution and rapid absorption which provide rapid onset of action. Moreover, drug candidates that undergo pre-gastric absorption when formulated as MDTs may show increased oral bioavailability. It provides good stability, accurate dosing, and easy manufacturing. The excipients employed in MDTs are always hydrophilic in nature whereas drug may be either hydrophilic or hydrophobic. If the drug is hydrophilic, the dosage form is known as fast dissolving tablets otherwise if drug is hydrophobic it is known as fast disintegrating tablets.[3-5] 1.1 Advantages of MDTs [6,7]  No need of water to swallow the tablet.  Apart from it the drug is protected from degradation due to pH and GIT enzymes.  It improves patient compliance.  It provides rapid drug delivery from the dosage forms.  Drug administration through buccal mucosa is easy.  The large contact area of the oral cavity contributes to rapid and extensive drug absorption.  Patient compliance is more.  Having rapid onset of action which may leads to an improved bioavailability.  Patient having difficulty in swallowing tablet can easily administer this type of dosage form.  Useful for pediatric, geriatric and psychiatric patients.
  • 2. International Research Journal of Engineering and Technology (IRJET) e-ISSN: 2395-0056 Volume: 07 Issue: 03 | Mar 2020 www.irjet.net p-ISSN: 2395-0072 © 2020, IRJET | Impact Factor value: 7.34 | ISO 9001:2008 Certified Journal | Page 4319 2. Materials and methods 2.1 Materials All materials and reagents used were of AR grade and good quality. The drug albendazole was procured from systropic ltd., baddi, HP, India. All equipments wrer available and used in the department of pharmaceutics, GRD(PG)IMT, Dehradun. 2.2 Methods Following study was done in relation to formulation of fast dissolving tablets. [8-11] a) Preformulation study of drug: Particle size, solubility, partition coefficient, melting point and drug excipient compatibility were determined by standard methods b) Standard curve of drug tinidazole Standard curve of tinidazole was prepared in buffer Ph medium 6.8 to mimic the salivary ph and hence give indication of measurement of drug concentration. c) Formulation of fast dissolving tablets Fast dissolving tablets were prepared by direct compression and the composition of the tablets is given as follows Table No. 1 Formulation Composition Formulation code Ingredient/quantity T1 T2 T3 T4 T5 T6 Drug 150 150 150 150 150 150 MCC 100 100 100 100 100 100 Cross povidone 25 50 25 - - 15 Sodium starch glycolate - - 25 25 50 15 Cross carmellose sodium - - - - - 15 Lactose 75 50 50 75 50 50 Starch 50 50 50 50 50 50 aspartame 10 10 10 10 10 10 Talc 1 1 1 1 1 1 Magnesium stearate 2 2 2 2 2 2  All ingredients are mg d) Evaluation parameters All the prepared batches were evaluated for organoleptic features, hardness, friability, weight variation, disintegration time, content uniformity and in-vitro drug dissolution study by standard testing methods and procedures. Results and discussion The results of the prepared formulations are given as
  • 3. International Research Journal of Engineering and Technology (IRJET) e-ISSN: 2395-0056 Volume: 07 Issue: 03 | Mar 2020 www.irjet.net p-ISSN: 2395-0072 © 2020, IRJET | Impact Factor value: 7.34 | ISO 9001:2008 Certified Journal | Page 4320 Table No. 2 Results of Evaluation Parameters Evaluation parameter Formulation code T1 T2 T3 T4 T5 T6 Hardness (kg/cm2) 3.5 4.3 4.6 3.9 4.5 4.6 Friability (%) 1.3 1.1 0.9 0.8 0.7 0.87 weight variation (%) ±2.3 ±3.5 ±3.2 ±4.6 ±4.8 ±2.1 Content uniformity (%) 97.6% 93.2% 98.6% 98.3% 94.6% 95.8% Disintegration time (sec) 37 43 39 36 38 41 T 80% (mins) 6 mins 6.5 mins 6.7 mins 6.4 mins 6.7 mins 6.8 mins Figure No. 1 Hardness & Friability Figure No. 2 Weight Variation & Content Uniformity 0 0.5 1 1.5 2 2.5 3 3.5 4 4.5 5 T1 T2 T3 T4 T5 T6 HARDNESS & FRIABILITY HARDNESS FRIABILITY
  • 4. International Research Journal of Engineering and Technology (IRJET) e-ISSN: 2395-0056 Volume: 07 Issue: 03 | Mar 2020 www.irjet.net p-ISSN: 2395-0072 © 2020, IRJET | Impact Factor value: 7.34 | ISO 9001:2008 Certified Journal | Page 4321 Figure No. 3 Disintigration Time Figure No. 4 In-Vitro Release of Formulations 0 10 20 30 40 50 60 70 80 90 100 T1 T2 T3 T4 T5 T6 WEIGHT VARIATION & CONTENT UNIFORMITY WEIGHT VARIATION CONTENT UNIFORMITY 32 34 36 38 40 42 44 T1 T2 T3 T4 T5 T6 TIME(SEC) DISINTIGRATION TIME
  • 5. International Research Journal of Engineering and Technology (IRJET) e-ISSN: 2395-0056 Volume: 07 Issue: 03 | Mar 2020 www.irjet.net p-ISSN: 2395-0072 © 2020, IRJET | Impact Factor value: 7.34 | ISO 9001:2008 Certified Journal | Page 4322 Conclusion All the prepared batches were found to be consistent, stable and show a good rapid release profile. All evaluation parameters results were found to be within acceptance criteria and the formulations can be further evaluated for stability studies under long term profile. The results are encouraging and prove the effectiveness of the selected polymeric combinations which can be successfully utilized of other formulations as well References 1. Salem I, Lopez K, Galan A, Florey K. Profiles of Drug substances and Excipients 27th Edition., California, USA Academic Press, 2000; pp. 304–16. 2. Dixit AR, Rajput SJ, Patel SG. Preparation and bioavailability assessment of SMEDDS containing valsartan, AAPS Pharm SciTech 2010; 11:314–21. 3. Raja RK, Abbulu K, Sudhakar M. Development, characterization and solubility study of solid dispersion of valsartan. J Chem Pharm Res 2011; 3:180–7. 4. Blagden N, Matas M, Gavan P, York P. Crystal engineering of active pharmaceutical ingredients to improve solubility and dissolution rates. Adv Drug Deliv Rev 2007; 59:617–30. 5. Jin X, Zhang Z, Sun E, Li S, Jia X. Statistically designed enzymatic hydrolysis of an icariin/b-cyclodextrin inclusion complex optimized for production of icaritin. Acta Pharma 2012; 2:83–9. 6. Cappello B, Maio DC, Iervolino M, Miro A. Improvement of solubility and stability of valsartan by hydroxypropyl - bcyclodextrin. J Inclusion Phenomena Macrocyclic Chem 2005; 54:289–94. 7. Ibrahim HK, El-Setouhy DA. Valsartan orodispersible tablets: formulation, in vitro/in Vivo characterization. AAPS PharmSciTech 2010; 11:89–96. 8. Abbas KA, Mohamed A, Abdulamir AS, Abas HA. A review on supercritical fluid extraction as new analysis method. American J. Biochem Biotech 2008; 4:345–53. 9. Agnivesh R, Shrivastava, Bhalchandra, Ursekar, Chhanda J, Kapadia. Design, optimization, preparation and evaluation of dispersion granules of valsartan and formulation into tablets. Current Drug Del 2009; 6:28–37. 10. Habib W, Khankari R, Hontz J. Fast-dissolving drug delivery systems. Crit Re Ther Drug Carrier Systems 2000; 17:61–72. 11. Deepak S, Dinesh K, Mankaran S, Gurmeet S, Rathore MS. Fast disintegrating tablets: A new era in novel drug delivery system and new market opportunities. J Drug Deliv Ther 2012; 2(3):74–86. 0 20 40 60 80 100 120 0 1 2 3 4 5 6 7 8 9 %DRUGRELEASE TIME(MINS) %IN-VITRO DRUG RELEASE T1 T2 T3 T4 T5 T6