RAJIV GANDHI UNIVESITY OF HEALTH SCIENCES,BANGALORE,KARNATAKA

ANNEXURE-II

PROFORMA OF REGISTRATION OF SUBJECT OF DISSERTATION

1 / NAME OF THE CANDIDATE
AND ADDRESS / RENUKA. SANGONDI. GIRIYAPPA.
#32, 7thCROSS, SHIVANAND NAGAR, MUDALPALYA, NAGARBHAVI MAIN
ROAD.
2 / NAME OF THE INSTITUTION / VISVESWARAPURA INSTITUTE OF PHARMACEUTICAL SCIENCES, BSK
2ND STAGE
BANGALORE – 70
3 / COURSE OF THE STUDY AND SUBJECT / MASTER OF PHARMACY IN PHARMACEUTICS
4 / DATE OF ADMISSION TO THE COURSE / 24-05-2008
5 / TITLE OF THE TOPIC / FORMULATION AND EVALUATION OF PATIENT FRIENDLYDOSAGE FORM FOR MODEL ANTIHISTAMINIC
DRUG.
6.
7.
8. /

BRIEF RESUME OF THE PROJECT STUDY

6.1NEED FOR THE STUDY
Antihistaminics are used to treat seasonal allergy (also known as Hay fever or pollen allergy) symptoms such as sneezing, runny nose, itchy throat, or itchy, watery eyes. It is also used to treat chronic hives and skin itching.
Hay fever is caused by breathing in pollen from trees, grasses, or weeds that cause an allergic reaction. This can results in classic allergy symptoms.
Fexofenadine is an antihistamine. It works by blocking a substance in the body called HISTAMINE this helps to decrease allergy symptoms.
Antihistaminics are used for—
Relief of seasonal allergy symptoms (hay fever).watery, or red eyes.luding:
om trees,grasses, or weeds that cause an allergic reaction.this
Treatment of chronic (long-term) hives and itching.
Used to treat hay fever symptoms, including:
-Sneezing
-Runny nose
-Itchy nose or throat
-Itchy, watery, or red eyes.
Dose of Fexofenadine is depends on factors-
  • Age of patient.
  • The severity of symptoms.
  • Other medical conditions of patients
  • Other medications patients are currently taking.1
Generally, the following points are considered for patient compliance in case of anti histaminics.
A rapid onset of action is necessary for immediate relieve the symptoms of hay fever, hives, and itching.
Patient has difficulty to swallow tablet or any another dosage form during pain.
Geriatrics has difficulty to swallow the dosage form.

Thus dispersible dosage form offers:

High drug loading.
Ability to provide advantages of liquid medication in the form of solid preparation
Adaptable and amenable to existing processing and packaging machinery.
Cost- effective.
Dispersible tablets are a perfect fit for pediatric & geriatric patients.
Improved patient compliance.
Rapid onset of action and may offer an improved bioavailability.
Patients having difficulty in swallowing tablet can be easily administered using this type of dosage form.
Gives accurate dosing as compared to liquids.
Good chemical stability.2
Dispersible tablets combine benefits of liquid dosage forms with a solid dosage forms and are preferred for pediatric and geriatric patients. The drug from conventional dispersible tablets has tendency to settle at the bottom or adhere to the sides of the containers upon dispersion in water, leading to incomplete dosage. The aim of present work to develop a dispersible dosagewhich upon dispersion in water, forms a homogenous dispersion with reduced sedimentation rate, thus ensuring uniformity of dosage.
6.2. REVIEW OF LITERATURE:
  1. Lansoprazole is an H+, K+-adenosine triphosphatase proton pump inhibitor (PPI) used for management of acid-related disorders. Lansoprazole has been reformulated as an oro-dispersible tablet (LODT) that quickly dissolves in the mouth without water. In healthy adults the safety and bioavailability of LODT 15–30mg, taken without water or dispersed in water, were found to be comparable with those of lansoprazole 15–30mg capsules. In conclusion, LODT is effective, bioequivalent to the capsule formulation and acceptable to patients. LODT offers an alternative dose administration method to all patients requiring a PPI, especially those who have difficulty swallowing, and may increase patient convenience and compliance.3
  1. Dispersible tablets of Ibuprofen were formulated employing potato starch, primo gel, microcrystalline cellulose (MCC) an pregelatinised starch (PGS) and the tablets were evaluated for content of active ingredient, hardness, friability, disintegration time, uniformity of dispersion and dissolution rate. Tablets formulated employing primo gel as internal and external disintegrants and tablets formulated employing potato starch as internal disintegrants and Primo gel and PGS as external disintegrants fulfilled all the official and other requirements of dispersible tablets. These tablets also gave rapid and higher dissolution rate then the formulated as well as conventional (commercial) tablets. The dissolution of ibuprofen from the tablets followed first order kinetics. The dissolution rate of ibuprofen, a poorly soluble drug could be increased by formulating it as dispersible tablets.4
  1. Aceclofenac, a non-steroidal anti-inflammatory drug, is used for post traumatic pain and rheumatoid arthritis. Aceclofenac fast-dispersible tablets have been prepared by direct compression method. Effect of superdisintegrants (such as, croscarmellose sodium, sodium starch glycolate and crospovidone) on wetting time, disintegration time, drug content, and in vitro release and stability parameters has been studied. Disintegration time and dissolution parameters (t 50% and t 80%) decreased with increase in the level of croscarmellose sodium. Where as, disintegration time and dissolution parameters increased with increase in the level of sodium starch glycolate in tablets.Stability studies indicated that tablets containing superdisintegrants were sensitive to high humidity conditions. It is concluded that fast-dispersible aceclofenac tablets could be prepared by direct compression using super disintegrants.5
  1. Formulation of ayurvedic powder preparations into tablets may increase dosage uniformity. Application of direct compression method to ayurvedic preparations can be regarded as a major advance. In the present study, dispersible tablets of panchagni lavana were prepared by direct compression method. Panchagni lavana was subjected to preformulation studies to test the suitability of direct compression method and appropriate formulations were developed. These formulations were further evaluated for hardness, friability, weight variation, uniformity of dispersion, disintegration test and stability studies. Attempts were made to get minimum possible disintegration time by varying the concentrations of sodium starch glycolate and starch. It was found that, use of mixture of both the disintegrating agents was highly useful in the formulation of dispersible tablets of panchagni lavana.6
  1. Eight formulations were developed containingIbuprofen in the form of orally disintegrating tablets. To prevent bitter taste and side effects of the drug, the drug was associated with Phospholipon 80H, a saturated lecithin, by wet granulation. The granules were then coated using different film forming agents (Kollicoat SR 30, Amprac 01, Kollidon 90F, Eudragit RD 100) obtaining four lots 1–4. Coated granules were then formulated with a sweetener (Aspartame), mannitol-based diluents (Pearlitol SD 200) and Kollidon CL (1-4K) or Explotab (1-4E) were added as superdisintegrants and compacted under low compression force. The eight lots of tablets, 1-4K and 1-4E were assessed if suitable as oral disintegrating tablets by determination of a range of technological parameters. Wetting and disintegregation time matched with the requirements of EP IV Ed., for almost all these formulations. Dissolution profiles suggested that the combined action of the hydrophobic lecithin and the coating delay the release of the drug from tablets with respect to when it is free or in the form of simple granules. By an appropriate combination of excipeints it was thus possible to obtain orally disintegrating tablets and a delayed release of ibuprofen using simple and conventional techniques.7
  1. A simple and sensitive Spectrophotometric method has been developed for the determination of Fexofenadine hydrochloride in bulk and pharmaceutical dosage forms. The method is based on the chloroform-extractable pale yellow colour complex formed by the reaction of fexofenadine with bromothymol blue at pH 2.6. The chromogen can be estimated at 412 nm against a reagent blank. This method obeys Beer's law in the concentration range of 10-50 µg/ml of the drug. The optimum reaction conditions and other analytical parameters were also evaluated. The proposed method has been successfully applied to the analysis of bulk drugs and their dosage forms.8
  1. Granisetron hydrochloride fast dissolving tablets were designed using superdisintegrants by direct compression. Evaluation is done for both powder blend of tablet in respect to bulk density, tapped density angle of repose, carr’s index, hardness, friability, weight variation, thickness, wetting time, disintegration time, drug content and in-vitro dissolution studies.9
  1. A method has been described to prepare and evaluate rapidly disintegrating compressed tablets in oral cavity. They used low substituted hydroxyl propylcellulose (L-HPS), microcrystalline cellulose (MCC) in various ratios to prepare tablets and tested various parameters. This showed good correlation between the disintegration behaviors in in-vitro and in-vivo.10
  1. Formulations of Domperidone of mouth dissolving tablet using different concentration of polyethylene glycol-4000, mannitol and ammonium bicarbonate or camphor has been reported.The study indicates that increase in concentration of ammonium bicarbonate or camphor reduces disintegration time.11
  1. Meloxicam is an oral NSAID. It is reported to be selective inhibitor of cyclo-oxygense-2 and used in the management of rheumatoid arthritis, for the short-term symptomatic treatment of acute exacerbations of osteoarthritis, and for treatment of alkloysingspondilytis.The rate and extent of dissolution of the active ingredient from any dosage form often determines the rate of extent of absorption of the drug.In case of a Meloxicam that is poorly water soluble, dissolution may be the rate-limiting step in the process of drug absorption.Drug with poor water solubility have been shown to be unpredictably and slowly absorbed compared with drugs of higher solubility. Therefore, a better oral, parenteral, or topical formulation can be developed by increasing the water solubility of the drugs.12
6.3. Objective of the study:
The objectives of the proposed study are as follows:
  • To develop dispersible antihistaminic drug delivery system.
  • Compatibility study of drug with polymers.
  • Evaluation of the prepared tablets.
  1. Physical properties : Appearance, Dimensions, weight variation,Hardness and friability
  2. Organoleptic parameters: Taste, mouth feel.
  3. Drug content uniformity.
  4. Wetting time and Disintegration time.
  5. In-vitro dissolution studies.
  6. In-vitro dispersion time.
  7. Stability studies according to ICH guidelines.
MATERIALS AND METHODS
7.1 SOURCE OF DATA:
Journals, Internet, Text books, Web resources and E journals (European Journal of Pharmaceutics and Biopharmaceutics, Indian journal of pharmaceutical science,) and experimental works which includes formulation evaluation and stability studies.
7.2 METHOD OF COLLECTION OF DATA:
The data related to physiochemical details of the drug will be collected from drug information center, various standard books, journals & other sources like research literature data bases such as science direct etc and laboratory experiments.
7.3 MATERIALS AND METHODS:
Materials and drug will be selected by industry& carried out as per the guidelines of the industry.
Materials:
Model antihihistaminic drug given by industry.
Excipients/ soluble Excipients: includes substances such as binders, disintegrants, lubricants, diluents. And sweetening agents.
Methods:
Tablets will be prepared by direct compression techniques and wet granulation techniques. Suitable formulations will be prepared by varying the compositions by keeping the API (active pharmaceutical ingredient) constant and varying the percentages of excipients that goes into the formulation at different stages of tablet preparation.
EVALUATION PARAMETERS :
Pre compression parameters :
  • Angle of repose
  • Bulk density
  • Carr’s index
Post compression parameters:
  • Weight variation
  • Friability
  • Hard ness
  • Thickness
  • Wetting time
  • Disintegration time
  • Drug content
  • In vitro drug release studies
  • Stability studies as per ICH guidelines.
7.4 Does the study require any investigations or interventions to be conducted on
Patients or other human or animals? If so please describe briefly:
------No------
7.5 Has ethical clearance been obtained from your institute in case of
------Not applicable ------
7.6 PLACE OF THE STUDY:
KARNATAKA ANTIBIOTICS & PHARMACEUTICAL LIMITED, (KAPL)
(A GOVERNMENT OF INDIAENTERPRISE)
BANGALORE-560058
LIST OF REFERENCES:
  1. WWW. Wikepidia.Com- Drug source.Date-22-11-2008
  2. Biradar SS, Bhagavati ST, Kuppasad IJ. Fast dissolving drug delivery systems. A brief overview. The internet journal of pharmacology 2006; 4.
  3. F Baldi, Fabio and Lansoprazole oro-dispersible tabled: pharmacokinetics and therapeutics use in acid-related disorders; Drugs (65),N 10, 2005; 1419-1426(8) Adis Internationl.
  4. Chowdary KPR, Hemavathi R.Formulation and dissolution rate studies on dispersible tablets of Ibuprofen. IJPS.2000; 62(3):213-216.
  5. SettyCM, PrasadDVK, GuptaVRM, SaB. Development of fast dispersible Aceclofenac tablets: Effect of functionality of superdisintegrants.IJPS 2008; 70(2):180-185.
  6. S Mutgalik, RS Shetty, J Manjunatha.Formulation and evaluation of directly compressible dispersible tablets of Panchagni lavana. IJPS.2001; 63(2):128-131.
  7. F Adamo, B Valentina, C Gian, R Celestino, Bergamante, Ceschl et al.Fast dispersible/slow releasing Ibuprofen tablets. Euro J Pharm and Bio pharm, 69(1): 2008; 335-341.
  8. KumarKS, RavichandranV, RajaMK, Thyagu R, Dharamsi A. Spectrophotometric determination of Fexofenadine hydrochloride.IJPS 2006;68(6): 841-842.
  9. Aithal K, Harish NM, Rathnanand M, Shirwaikar A and Dutta M. Once daily fast dissolving tablets of Granisetron hydrochloride formulation and in-vitro evaluation. Ind drugs 2006; 43(7): 576-580.
  10. Yunxia BI, Yorinobu Yonezawa and Hisakazu Sunada “Rapidly Disintegrating Tablets by the Wet Compression Method: Mechanism and Optimization”.Journal of Pharmaceutical Sciences, 1999; 88(10),
  11. ManeAR, Kusum Devi V and Asha AN. A novel technique for the preparation of mouth dissolving tablets of Domperidone. Ind drugs 2003; 40 (9): 544-546.
  12. Inamdar N, Bhise K, Memon S. Solubility enhancement and development of dispersible tablet of Meloxicam.Asian J of pharm 2008; 2(2):128-132.

9 /

SIGNATURE OF THE CANDIDATE:-

10 /

REGISTRATION NO:-

11 / REMARKS OF THE GUIDE:-
12 / NAME AND DESIGNATION OF :
12.1 GUIDE:- / Dr. G. Y. NARMADA
M.PHARM, PhD
Professor
Department of Pharmaceutics
VIPS, Bangalore-70
12.2 SIGNATURE:-
12.3 CO-GUIDE:- (IF ANY) / VENKATA SUBBAIAH
M.PHARM
Manager of F and D department
KAPL, Bangalore-58
12.4 SIGNATURE:-
12.5HEAD OF THE DEPARTMENT:- / Dr. B. PRAKASH RAO
M.PHARM, PhD
Professor
Department of Pharmaceutics
VIPS, Bangalore-70
12.6 SIGNATURE:-
13 / 13.1 PRINCIPAL:- / Dr. KALYANI PRAKASAM
Principal
M.PHARM, PhD
VIPS, Bangalore-70
13.2REMARKS :-
13.3 SIGNATURE WITH SEAL:-