PRODUCT DEVELOPMENT AND EVALUATION OF AN ORALLY DISINTEGRATING ANTI-EMETIC TABLET

M.PHARM DISSERTATION PROTOCOL SUBMITED TO

SUBMITTED TO

RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES

KARNATAKA

BY

ARBIND KUMAR YADAVB.Pharm

Under the guidance of:

DR. DEHGHAN MOHAMMED HUSSANM.Pharm Ph.D.

PROFESSOR

PG Deptof Pharmaceutics

LUQMAN COLLEGE OF PHARMACY, GULBARGA.

DEPARTMENT OF PHARMACEUTICS

LUQMAN COLLEGE OF PHARMACY, GULBARGA.

2013-2014

RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES,BANGALORE,KARNATAKA,

ANNEXTURE –II

PROFORMA OF REGISTRATION OF SUBJECT OF DISSERTATION

1. / Name of the candidate and permanent
address ( in block letters) / ARBIND KUMAR YADAV
Luqman college of Pharmacy,
P.Box No. 86, Behind P & T Colony, old Jewargi road, Gulbarga - 585 102.
2. / Name of the institution / Luqman college of PharmacyGulbarga
3. / Course of study and subject / M.PHARMA (PHARMACEUTICS)
4. / Date of admission to the course / 12/06/2013
5. / Title of Topic / “PRODUCT DEVELOPMENT AND EVALUATION OF AN ORALLY DISINTEGRATING ANTI-EMETIC TABLET”
6. / Brief Resume of the intended work
6.1 Need for the study:
Difficulty in swallowing (dysphagia) is a common problem of all age groups, especially the elderly and pediatrics, because of physiological changes associated with these groups. Other categories that experience problems using conventional oral dosage forms include are the mentally ill, uncooperative and nauseated patients, those with condition of motion sickness, sudden episodes of allergic attack or coughing. Sometimes it may be difficult to swallow conventional products due to unavailability of water. These problems led to the development of a novel type of solid dosage form called mouth dissolving tablets, which disintegrate and dissolve rapidly in saliva without the need of drinking water. They are also known as fast dissolving tablets, melt-in-mouth tablets, rapimelts, porous tablets, oro-dispersible tablets, quick dissolving tablets or rapidly disintegrating tablets. Upon ingestion of these dosage forms, the saliva rapidly dissolves the drug in it and then swallowed and absorbed in the normal way. Some drugs are absorbed from the mouth, pharynx and oesophagus as the saliva passes down in to the stomach. In these cases, the bioavailability of drugs is significantly greater than those observed from standard dosage forms1.
Antiemetic drugs like Domperidone, Ondensetron hydrochloride, Granisetron hydrochloride have the oral problems like difficulty in swallowing, less oral bioavailability, first pass metabolism in conventional tablet dosage forms. To overcome such problems the antiemetic drugs can be formulated in the form of fast dissolving tablets where the drug is rapidly disintegrated in mouth within fraction of seconds and improves the oral drug bioavailability. Fast dissolving tablets can be prepared by methods like direct compression, wet granulation, sublimation, effervescent methods along with superdisintegrants to increase invitro dispersion time. Some of the newer methods to formulate quick release dosage forms include Zydis, Orasolv, Flashtab, Wowtab, oraquick, Ziplet2.
Hence, in this present study a suitable antiemetic drug is selected to formulate rapid dissolving tablets for improving its bioavailability and to meet patient compliance.
6.2 Review of Literature
  1. Parmar RB et al., worked on formulation and evaluation of domperidone fast dissolving tablets by using superdisintegrants Avicel PH 102 and sodium starch glycolate by direct compression and they found a good hardness of 3kg/cm2, disintegration time of 27 seconds and in vitro drug release is 95% within 30 minutes as compared to the marketed product, which gives quick release from emesis3.
  2. Gnanaprakash K et al., carriedout formulation and evaluation of fast dissolving tablets ofvaldecoxib with β-cyclodextrin using superdisintegrants polyvinyl pyrrolidine, sodium carboxy methyl cellulose and crospovidone by direct compression and they reported thatincreased proportion of polymers, superdisintegrants and solubilizing agents have shown enhanced cumulative drug release rate 99.88% within 10 minutes4.
  3. Jashanjit singh et al., developed optimization and formulation of orodispersible tablets of meloxicam by non-aqueous wet granulation using crospovidone and mannitol and they showed disintegration time of 32seconds, drug content 98.5% and fast drug release rate of 99.5%within 30 minutes as compared with conventional tablet5.
  4. Bhalero AV et al., carried out development and evaluation of clonazepam fast dissolving tablets using superdisintegrants and solid dispersion technique by using PVP K-30 and combination of 5% w/w crosscaramellode sodium and 5% w/w sodium starch glycolate and they reported that so formulated tablets showed least dispersion time of 8seconds and faster dissolution rate6.
  5. Shahi SR et al., worked on formulation and in vitro evaluation of orodispersible tablets of etoricoxib with superdisintegrants crospovidone, croscaramellose sodium and sodium starchglycolate and they reported that formulated orodispersible tablets are having enhanced bioavailability than conventional tablets7.
  6. Nagendrakumar D et al., carriedoutfast dissolving tablets of fexofenadine hydrochloride by effervescent method and they concluded that formulated tablets are best(t50% 4 min.) based on in vitro drug drug release charecteristics compared to conventional commercial tablet formulation(t50%is15 min)8.
  7. Gattani SG et al., developed formulation and evaluation of mouth dissolving tablets of ondensetron hydrochloride using natural superdisintegrants along with Ac-Di-Sol, primogel, polyplasdone XL and they reported that Ac-Di-Sol was found to be more effective than others due its high swelling capacity9.
  8. Shailesh Sharma et al., carried out formulation and characterization of fast dissolving tablets of promethazine thecolate by direct compression with Ac-Di-Sol, sodium starch glycolate and crospovidone in different concentrations and it has been found that tablets containing Ac-Di-Sol showed superior organoleptic properties, along with excellent in vitro and in vivo dispersion time and drug release, as compared to conventional tablets10.
  9. Nagendra kumar D et al., studied formulation design of novel fast dissolving tablets of granisetron hydrochloride using low and high compressible saccharides such as mannitol and sorbitol by direct compression. In this study the conclusion was made that the formulated tablets have showed good stability and in vitro drug release characteristics11.
  10. Na zhao et al., made comparison of three different classes of superdisintegrants primogel, polyplasdone XL, Ac-Di-Sol in promoting aspirin tablets disintegration and dissolution and they reported that Ac-Di-Sol was found to disintegrate tablets rapidly into small particles12.
6.3Objectives of the study:
  • To formulate rapid dissolving tablets by different methods.
  • To improve oral bioavailability.
  • To evaluate prepared tablets by different physical characterization tests.
  • To improve the dissolution efficiency in view to provide rapid onset of action than the oral conventional dosage forms.
  • To improve patient compliance.
7. Materials andmethods:
7.1 Materials:
Drug : Antiemetic drug like Promethazine Hydrochloride, etc ..
Superdisintegrants: Crospovidone, sodium starch glycolate, crosscaramellose etc…
Flavours : Menthol etc…
Sweetners : Sodium saccharin, aspartame, mannitol, etc…
Other ingredients : Lactose, microcrystalline cellulose, talc, magnesium
sterate, etc…
7.2 Methods: Rapid dissolving tablets of an antiemetic drug can be prepared by direct compression and other methods.
. 1 Source of data :
Library: Bharathi college of pharmacy
e-library: Bharathi college of pharmacy
Practical data’s are obtained from laboratory-based studies.
2 Method of collection of data :
The data required for the study would be collected from the laboratory based work planned as follows:
  • Prepared granules for rapid dissolving tablets will be evaluated for flow properties such as:
a)Angle of repose
b)Carr’s consolidation ratio
c)Bulk density
d)Haunser ratio
  • Prepared rapid dissolving tablets will be evaluated for
a)Hardness
b)Weight variation
c)Friability
d)in vitro dispersion time
e)in vitro dissolution time
f)Stability studies as per ICH guidelines
g)Wetting time
  • Characterization of an antiemetic drug can be done by using UV- visible spectroscopy and other methods.

7.3 Does the Study require any investigation or intervention to be conducted on patients or other human or animals? If so please describe briefly.
--- No ---

7.4 Has ethical clearance been obtained from your institution in case of 7.3?
--- No ---

8. LIST OF REFERENCES
  1. Kaushik D, Dureja H, Saini TR. Mouth dissolving tablets: a review. Indian Drugs. 2004; 41 (4):187-93.
  2. Hirani JJ, Rathod AD, Vadalia KR. Orally disintegrating tablets: A review. Trop J Pharm Res 2009; 8(2):161-72.
  3. Parmar RB, Baria AH, Tank HM, Faldu SD. Formulation and evaluation of Domperidone fast dissolving tablets. Int J Pharm Tech Res 2009;1(3):483-87.
  4. Gnanaprakash K, Mallikarjuna rao K, Chandrasekhar KB, Madhusudhanashetty C, Alagusundaram M, Ramkanth S. Formulation and evaluation of fast dissolving tablets of Valedoxib. Int J Pharm Tech Res 2009;1(4):1387-93.
  5. Singh J, Singh R. Optimization and formulation of orodispersible tablets of Meloxicam. Trop J Pharm Res 2009;8(2):153-59
  6. Bhalerao AV, Deshkar SS, Shirolkar SV, Gharge VG, Deshpande AD. Development and evaluation of Clonazepam fast dissolving tablets using Superdisintegrants and Soid dispersion technique. Research J Pharm and Tech 2009;2(2):375-77.
  7. Shahi SR, Agarwal GR, Shinde NV, Somani PB, Shamkuvar PB, Kale MA et al. Formulation and in vitro evaluation of orodispersible tablets of Etoroxib with emphasis on comparision of three classes of superdisintegrants. Rasayan J Chem 2008;1(2):292-300.
  8. Nagendrakumar D, Para MS, Raju SA, Shirsand SB, Rampure MV. Fast dissolving tablets of Fexofenadine HCL by effervescent method. Indian J Pharm Sci 2009;71(2): 116-19.
  9. Gattani SG, Shiyani BG, Kakade KN, Patil AB, Surana SJ. Formulation and evaluation of mouth dissolving tablet of Ondensetron Hydrochloride by using superdisintegrants. Indian Drugs. 2009; 46(1):44-50.
  10. Sharma S, Gupta GD. Formulation and characterization of fast dissolving tablet of Promethazine theoclate. Asian J Pharm 2008;2(1):70-72.
  11. Nagendra Kumar D, Raju SA, Shirsand SB, Para MS. Formulation design of novel fast dissolving tablets using low and high compressible saccharides. Int J Pharm Tech Res 2009;1(4):1585-88.
Na zaho, Augsburger LL. Functionality comparision of 3 classes of superdisintegrants in promoting Aspirin tablets disintegration and dissolution. AAPS Pharm Sci Tech 2005;6(4):63-9.
9. / Signature of Candidate / ARBIND KUMAR YADAV
10. / Remarks of guide / The proposed work is a simple method of Product development and evaluation of an orally disintegrating anti-emetic tablet hence recommended for registration.
11. / Name and designation:
11.1 Guide / DR. DEHGHAN MOHAMMED HUSSAN
PROFESSOR DEPARTMENT OF PHARMACEUTICS
12 / 11.2 Signature of Guide
11.3 Co-guide
11.4Signature of Co-guide
12.1 Remarks of the Chairman and Principal / We will provide all the necessary facilities required for the proposal research work. So, recommended for registration.
12.2 Signature