Preparation and Evaluation of Domperidone Orodispersible Tablets

PRESENTED BY :
Mr. Mahendra Pratap Swain
B.PHARM, 7th SEMESTER,
REGD. NO:- 1103267027
UNDER THE ESTEEMED GUIDANCE OF :
Prof. M.E. Bhanoji Rao
Principal, M.Pharma, Ph.D., HOD of Pharmaceutics
Roland Institute of Pharmaceutical Sciences
Mahendra Pratap Swain Friday, 15-May-2015
PREPARATION BY SOLUBILITY ENHANCEMENT OF DOMPERIDONE
ORO-DISPERSIBLE TABLETS (ODTs) USING SDS WITH INCLUSION
COMPLEXATIONS TECHNIQUE AND THEIR EVALUATION

CONTENTS
Friday, 15-May-2015Mahendra Pratap Swain

Propose Of Work

Plan Of Work

Oro-Dispersible Tablets (ODTs)
 Dispersible Tablets (DTs) are uncoated or film-coated tablets intended to be
dispersed in water before administration giving a homogeneous dispersion.
Dispersible tablets disintegrate within 3 min when examined by the test for
disintegration of tablets and capsules, by using water at 15-25 °C.
 Oro-dispersible tablets (ODTs) are uncoated tablets intended to be placed in
the mouth where they disperse rapidly before being swallowed. ODTs
disintegrate within 30 sec. It is a NDDS because they are easy to administer
and lead to better patient compliance so its should named OD-NDDS.
 E.g.: The trend toward formulation of dispersible tablets is evident in Europe
(159-162) and is becoming more commonplace in the United states with over-
the counter preparation available in the form of the following technologies:
Zydis® (Scerer DDS), Lyoe® (Farmalyoc), WOW® Tab (Yamanouchi),
FlashDose® (Fuisz technologies), OraSolv® (CIMA), and DuraSolv® (CIMA).
These tablets are either placed in mouth where they quickly dissolve or are
placed in a glass of water prior to ingestion and provide consumers with a
dosage form that is both potable and easy to swallow.

 An orally disintegrating tablets or Oro-Dispersible Tablets
(ODTs) is a drug dosage form available for limited amount of
over-the-counter (OTC) & Prescription Medications.
 ODTs serves as an Alternative dosage form those have Dysphagia
(Difficulties in Swallowing).
 Common among all age groups, dysphagia is observed in 35% of
the general population as well as elderly institutionalized
population & 12-18% patient in long term facilities.
 Last decade seen that ODTs are well used in both OTC &
Prescription medication. And important cause to take ODTs
because these are very convenience as it can taken without Water.

Advantages OF ODTs

Drug Selection CriteriaODTs:

Drug Choice:
Pharmacokinetic data:
Bioavailability : High
Protein binding : 91–93%
Metabolism : Hepatic and intestinal (first-pass)
Half-life : 7 hours
Excretion : Breast milk, renal
Chemical data:
Formula : C22H24ClN5O2
Molecular mass : 425.911 g/mol
Domperidone is widely used anti-emetic drug acting by an inhibition of the dopaminergic receptor.
Domperidone does not cross blood brain barrier.
Domperidone is also effective in gastroparesis, pediatrics gastro-esophageal reflux (infant vomiting).
Domperidone also prescribed for the treatment of gastro paresis a stomach motility condition.

Significance of Oro-Dispersible New Drug delivery systems (OD-NDDS):

Important Criteria For Selection Of
Excipients For Used In Formulation Of DTs

Formulationof DTS. :

FORMULATION
Domperidon Domperidon
+ +
INGRADIENTS HP-β-Cyclodextrin PEG-6000
(In mg) (In mg)
F1 F2 F3 F4 F5 F6
1.Domperidon Inclusion Complex
(API)
36.64 36.64 36.64 20 20 20
2. Tween-80 0.2 0.2 0.2 0.2 0.2 0.2
3. SDs
 SSG 18 - - 18 - -
 Crospovidone - 18 - - 18 -
 Croscarmellose - - 18 - - 18
4. Sod. Saccarine 1 1 1 1 1 1
5. Starch-1500 20 20 20 20 20 20
6. Mg-Sterate 1 1 1 1 1 1
7. Talc 1 1 1 1 1 1
8. PVP 10 10 10 10 10 10
9. Flavour & Colour 2 2 2 2 2 2
10. PerLitol 120.16 120.16 120.16 136.8 136.8 136.8
TOTAL (In mg.) 210 210 210 210 210 210

FORMULATION

Technologies Used For Preparing ODTs
 Freeze drying or Lyophilization
 Sublimation
 Mass extrusion
 Melt Granulation
 Spray drying
 Molding
 Nanonization
 Direct compression
 Cotton candy process
 Phase transition process
From that I selected Direct Compression method i.e. given below .

Direct compression
 Easiest way to Mfg. Of tablets by this technique.
 Low mfg. cost, conventional equipments & limiting no. of processing steps
led this technique to be a preferable one. How over disintegration & dissolution of
directly compressed tablets depends on single or combine effect of disintegrant,
water soluble excipients & effervescing agents.
 It is essential to choose a suitable & optimum concen. Of disintgrants to ensure
quick disintegration & dissolution.
 Superdisintgrants are newer substances which are more effective at lower
concen. At greater disintgrating efficiency & mechanical strength.
 Studied revealed that water insoluble Superdisintgrants like Sod. Starch
glycolate & Croscarmellose sod. Show better disintegration properties then the
slightly water soluble agents like Crospovidone sod. they do not have tendency to
Swell.

Evaluation Study:
Evaluation of powder blends/Pre Formulation study :
 Bulk density
 Tapped density
 Angle of repose
 Compressibility index
 Melting point test
 Compatibility study
 Flow property of API’s
 Solubility study
Evaluation of Dispersible Tablets (DTs/ODTs) :
 Hardness Test
 Friability
 Thickness
 Weight Variation Test
 Disintegration test
 Water Absorption Ratio
 Wetting time
 Dissolution test

Pre-Formulation Studies
Bulk Tapped Flow Properties determination
Batch No. Density Density
(ρb=M/Vb) (ρt=M/Vt) Angle of Repose Compressibility
index
Hausner’s Ratio
F1 1 1.18 24 (Excellent) 15.25 (Good) 1.18
(Excellent)
F2 0.8 1.15 25 (Good) 30.43 (Poor) 1.43 (Poor)
F3 1 1.18 30 (Good) 15.25 (Good) 1.18
(Excellent)
F4 1.01 1.28 33 (Passable) 20.31
(Passable)
1.26 (Passable)
F5 1.02 1.3 33 (Passable) 21.53 (Poor) 1.27 (Passable)
F6 1.03 1.26 43 (Poor) 18.25
(Passable)
1.22 (Passable)

Result & Discussion on Pre-formulation Studies:

Post-FormulationStudies
Batch No. Disintegra
tion
Wetting
time (sec.)
Hardness Friability Weight Drug
Release
time (sec.) (n=10)
kg/cm
2
(%) variation Q30 (%)
F1 29 32 3.9 ±0.122 0.39 199±1.33 96.21
F2 27 30 3.9 ±0.128 0.41 200±1.56 92.21
F3 30 33 4.0 ±0.365 0.41 200±1.59 89.65
F4 31 34 4.2 ±0.126 0.4 198±1.33 96
F5 30 35 3.9 ±0.152 0.38 210±1.62 91.54
F6 29 32 4.9 ±0.360 0.41 302±1.57 92.53

Result and Discussion Post-formulation i.e. ODTs:

Conclusion

REFERENCE:
Conted.
 Ainley Wade and Paul J weller, Hand book of pharmaceutical Excipients, 2nd Edition, published by The American pharmaceutical Association Washington: 1994; 84,143,280,519.
 Bhowmik D, Krishnakanth CB, Pankaj, Chandira RM. Fast dissolving tablet: An Overiew. Journal of Chemical and Pharmaceutical Research 2009; 1(1): 163-77.
 British Pharmacopoeia. Vol. I and II: 1993; 755.
 British Pharmacopoeia.British Pharmacopoeial commission. A- 290, Vol. 4. London: The stationary office, 2005.
 E. Norris and M. Guttadauria, Eur. J. Rheumatol. Inflamm., 8(1), 94 (1987).
 European Pharmacopoeia, 5th Edi.,vol 1. European Department for the Quality of Medicines within the Council of Europe, Strasbourg, 2005, 234.
 Gandhi GS, Dharmendra R, Mundhada, Bhaskaran S. Levocetrizineorodispersible tablet by direct compression method. Journal of Applied Pharmaceutical Science 2011; 1(5):145-50.
 Gaur K, Tyagi LK, Kori ML, Sharma CS, Nema RK. Formulation and characterization of fast disintegrating tablet of aceclofencac using sublimation method. IJPSR 2011; 3(1):19-22.
 Geraro AR, Remington’s pharmaceutical sciences. 18th Edition. Mack publishing co, Eastern pennsylvania, 1990; 560, 1996 and 6006.
 Goodman and Gilman’s, the pharmacological basis of therapeutics. 10th edition, edited by Joel G Hardman, lee E Limberd, mcgraw Hill Medical Publishing Division, New York, 10th edition: 2002; 2001-
1206.
 ICH Harmonized Tripartite Guidelines, 2003. Stability testing of New Drug Substances and Products. Q1A (R2).
 Indhumati D, Prabha KS. Formulation and evaluation of orodissolving tablet of fluoxetine using superdisintegrants. International Journal of Pharma and Bio Sciences 2011; 2(1):833-47.
 Jadhav SB, Kaudewar DR, Kaminwar GS, Jadhav AB, Kshirsagar RV, Skarkar DM. Formulation and evaluation of dispersible tablets of Diltiazem hydrochloride. Int J pharmtech Res 2011; 3(3):1314-21.
 Japanese Pharmacopoeia, 15th ed. Tokyo, The stationary office, society of Japanese Pharmacopoeia; 2007. 1730.
 Kamboj M, Goyal S, Rakha P, Arora G, Dureja H, Nagpal M. Formulation and evaluation of metformin oro-dispersible tablets.Acta poloniaepharmaceutica ñ Drug Research 2011; 68(5)717-23.
 Kohli DPS, Shah DH, Drug formulations manual, New Delhi, India, Eastern publishers, 2000; 4-10.
 Kundu S, Sahoo PK. Recent trends in the developments of orally disintegrating tablet technology. Pharma Times 2008; 40(4):11-5.
 Lachman L, Lieberman HA, Kanig LJ, Theory and practice of industrial pharmacy, 3rd edition, Varghese publishing house, Bombay, India, Varghese publishing house, 1991;
 Lachman L, Lieberman HA, Pharmaceutical Dosage Forms: Tablets, New York, Marcel Dekker Inc, 1:1980; 110-184.
 Lachman L, Liebermann HA, et al. The Theory and Practice of Industrial Pharmacy. Mumbai, Varghese publishing house 69; 1991.
 Lakshmi CSR, Patel NJ, Patel HP, Akul S. Formulation and evaluation of oral dispersible tablets of Cinnarizine using sublimation technique. International Journal of Pharmaceutical Sciences Review and
Reaearch. 2011; 6(2):178-82.

REFERENCE:
 Malik K, Arora G, Singh I, Arora S. Lallemantiareylenne seeds assuperdisintegrant: Formulation and evaluation of nimesulide orodispersible tablets. International Journal of Pharmaceutical Investigation
2011; 1(3):192-8.
 Martindale, The complete drug reference, 34th edition, Pharmaceutical press, Royal pharmaceutical society of Great Britian, 2005; 172- 173.293-345.
 Masareddy RS, Kadia RV, Manvi FV. Development of mouth dissolving tablets of clozapine using two different techniques. Indian J Pharm Sci 2008; 70(4):526-28.
 Patel KB, Shete SN, Belgamwar VS, Tekade AR. Formulation design and optimization of taste-masked mouth-dissolving tablets of tramadolol hydrochloride. Asian J Pharm 2010; 239-45.
 Patel NJ, Lakshmi CSR, Patel HP, Akul S. Formulation and evaluation of Oral dispersible tablets of cinnarizine using direct compression technique. IJPSR 2011; 2(4):961-67.
 Paul Y, Tyagi S, Singh B. Formulation and evaluation of oral dispersible tablets of zidovudine with different super disintegrants. International Journal of Current
 Pharmaceutical Review and Research 2011; 2(2):81-91.
 Pfister WR, Ghosh TK. Orally Disintegrating Tablets: Products, Technologies and Development issues. Pharm Technol 2005: 136-50.
 Ratnaparkhi MP, Mohanta GP, Upadhyay. Review on: Fast dissolving tablet. Journal of Pharmacy Research 2009; 2(1):5-12.
 S. Coveleyn J.P. Remon, Drug Dev. Ind. Pharm., 25(9), 1005(1999)
 S. Coveleyn J.P. Remon, Int. J. Pharm., 166, 65(1997)
 S. Coveleyn J.P. Remon, Int. J. Pharm., 173, 49(1998) Senthil A, Sivakumar T, Narayanaswamy VB, Ashish SP, Viral GP. Formulation and evaluation of Metoprololtartarate by directcompression using
super disintegrants. International Journal of Research in Ayurveda and Pharmacy 2011;2(1):224-29.
 Shankar DG, UV and visible spectropotometric methods for determination of cefixime, Indian drug: 2001; 38.
 Simone Schiermeier, Peter Christian Schmidt, Fast dispersible Ibuprofen tablets, European Journal of Pharmaceutical Sciences, 15:2002; 295-305.
 T. Ishikawa, Y. Watanabe, N. Utoguchi, and M. Matsumoto, Chem. Pharm. Bull. (Tokyo), 47(10), 1451 (1999).
 The United States pharmacopoeia, USP 29/NF 24, Asian edition, Twin brook parkway, Rockvillie, printed in Canada, 2005; 411-412.
 Tony Nunn, Julie Williams, Formulation of medicines for children, British journal of pharmacology, 2004; 674-676.
 USP/NF. Asian Edition, Twinbrookparkway, Rockwillas.2006: 411-412.
 Y. Bi, Y. Yonezawa, and H. Sunda, J. Pharm. Sci., 88(10) 1004(1999).
 Y.X. Bi, H. Sunda, Y. Yonezawa, and K. Danjo, Drug Dev. Ind. Pharm., 25(5) 571(1999).

Mahendra pratap Swain
MPS-JSR-MP
Mr. Mahendra pratap Swain

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