FORMULATION AND EVALUATION OF
MUCOADHESIVE BUCCAL PATCHES OF H1-ANTI HISTAMINE

BY

MOHAMEDAJMAL AHMED
M.PHARM 1ST YEAR
DEPARTMENT OF PHARMACEUTICS
M.M.U. COLLEGE OF PHARMACY

RAMANAGARAM-562159, KARNATAKA

DISSERTATION PROTOCOL

SUBMITTED TO THE

RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES

BANGALORE- 560041

KARNATAKA.

UNDER THE GUIDENCE OF

Mr.VAZIR ASHFAQ AHMED

ASST.PROFESSOR

DEPARTMENT OF PHARMACEUTICS

M.M.U. COLLEGE OF PHARMACY

RAMANAGARAM-562159

KARNATAKA

RAJIV GANDHI UNIVESITY OF HEALTH SCIENCES,

BANGALORE- 560041 KARNATAKA.

ANNEXURE-II

PROFORMA FOR REGISTRATION OF SUBJECTS FOR DISSERTATION

1. / NAME OF THE CANDIDATEAND
ADDRESS (IN BLOCK LETTERS) / MOHAMED AJMALAHMED
NO,2878 1ST CROSS MOTI NAGAR
RAMANAGARAM 562159.
2. / NAME OF THE INSTITUTION / M.M.U. COLLEGE OF PHARMACY
K.K DODDI, RAMADEVERA BETTA ROADRAMANAGARAM-562159
KARNATAKA
3. /

COURSE OF STUDY AND SUBJECT

/ M. PHARMACY
PHARMACEUTICS.
4. / DATE OF ADMISSION OF COURSE / 01-10-2010
5. /

TITLE OF TOPIC

/ FORMULATION AND EVALUATION OF
MUCOADHESIVE BUCCAL PATCHES OF H1- ANTI HISTAMINE DRUG.
6. / BRIEF RESUME OF THE
INTENDED WORK
6.1 Need for the study
6.2 Review of the literature
6.3 Objectives of the study / ENCLOSURE-I
ENCLOSURE-II
ENCLOSURE-III
7. /

MATERIALS AND METHODS

7.1 Source of data
7.2 Method of collection of data
7.3 Does study require any Investigations or interventions to be conducted on patients or Other human or animal? If so, Please describe briefly.
7.4 Has ethical clearance been obtained from your institution in case of 7.3 / ENCLOSURE-IV
ENCLOSURE-V
ENCLOSURE-VI
ENCLOSURE-VII
8. / LIST OF REFERENCES / ENCLOSURE-VIII
9. / SIGNATURE OF CANDIDATE
10. / REMARKS OF GUIDE / Recommended for approval
11. / NAME AND DESIGNATION OF
11.1 Guide
11.2 Signature
11.3 Co guide (if any)
11.4 Signature
11.5 Head of Department
11.6 Signature / Mr. VAZIR ASHFAQ AHMED
ASST.PROFESSOR
M.M.U COLLEGE OF PHARMACY
K.K DODDI, RAMADEVERA BETTA ROAD RAMANAGARAM-562159
KARNATAKA
Not applicable
Not applicable
VAZIR ASHFAQ AHAMED
ASST.PROFESSOR
DEPARTMENT OF PHARMACEUTICS,
M.M.U COLLEGE OF PHARMACY
K.K DODDI, RAMADEVERA BETTA ROAD RAMANAGARAM-562159
KARNATAKA
12. / 12.1 Remarks of the
Chairman and principal
12.2 Signature / SUBMITTED FOR APPROVAL
6. / BRIEF RESUME OF THE INTENDED WORK
ENCLOSURE-I
6.1 Need for the study
Buccal drug delivery circumvent some of the problem of oral drug delivery, such as extensive first - pass metabolism and drug degradation in the harsh gastrointestinal environment. Among the various transmucosal route, buccal mucosa has excellent accessibility, an expanse of smooth muscles and relatively immobile mucosa, hence suitable for administration of retentive dosage form. The oral cavity has rich blood supply that drains directly into the jugular vein and bypassing the liver.
Buccal patches are highly flexible and ensure more accurate dosing of the drug.Buccal patches provide systemic delivery of drug as well as for local targeting of drug, easy administration, thereby increasing patient compliance. Buccal drug absorption can be promptly terminated in case of toxicity by removing the patch from the buccal cavity.
H1-receptor antagonist is used in the treatment of of allegric rhinitis and urticaria.
The strategy for designing buccoadhesives is based principally on the utilization ofpolymers with suitable physicochemical properties, such as polyacrylic acid carbomer and cellulose derivatives hydroxypropylmethylcellulose [HPMC], many H1- antihistamine, which selectively antagonizes peripheral histamine H1- receptorundergoes extensive first-pass hepatic metabolism on oral administration and has relatively lessbioavailability.
Therefore, a buccal patches of H1- antihistamine will beformulated to prevent first-pass metabolismand to improve therapeutic efficacy.
The main aim of designing and evaluating buccal patches of H1- anti histamine drug is to provide immediate release of drug.
ENCLOSURE II
6.2Review of literature
  1. Borgaonkar PA, Virsen TG, Hariprasanna RC and Najmuddin M:Has prepared buccal tablets of Loratadine using natural polymers to control the drug release and alsoto avoid the first pass metabolism. The formulationcontaining the leastHPMC ratio showed better in-vitro drug release.the prepared tablets were evalvated for tablet thickness,weight variation,friability,drug content swelling index, surface pH and established good bioadhesion strength.
  1. Deshmane SV, Channawar MA, Chandewar AV, Joshi UM, Biyani KR: A sustained release buccal patch of verapamil-HCL were prepared by using chitosan with PVP K-30.Each formulation were subjected to various evaluation parameter. So chitosan can be choosen as bio adhesion polymer for the preparation of patches.
  1. Manasa B, Gudas GK, Sravanthi N, Madhuri RA, Lavanya Y, Pranitha C: Resperidone patches were prepared using HPMC (15 & 47 cps), chitoson, poly vinyl alcohol, poly vinyl pyrilodine. So, patches with HPMC (15 & 47 cps) was dissolution controlled, where as rest of the formulation followed diffusion controlled. The models used were zero and first-order equations, Hixon-crowell, Higuchi and Korsmeyer-peppas models. The results indicate that the mucoadhesive buccal patchesof resperidone may be good choice to bypass the extensive hepatic first pass metabolism with an improvement in the bioavialability of resperidone through buccal mucosa.
  1. Anjankumar PB: Mucoadhesive bi-layered buccal device of valsartonwere prepared containing mucoadhesive layer and a drug free backing membrane, film were fabricated by solvent casting technique and wereevaluated for various parameters,like surface texture, thickness weight uniformity,swelling index,folding endurance,bio-adhesion. The optimized film exhibited an in vitro drug release of approximately 90% in 5hr along with satisfactory bio-adhesive strength.
  1. Dharani S, Shayeda: Mucoadhesive buccal patches of Ondansetron Hydrochloride (OND) were prepared using Hydroxy Propyl Methyl Cellulose(HPMC E15) by solvent-casting technique. In vitro release studies demonstrate the suitability of developed formulations for the release of Ondensetron Hydrochloride. Buccal patches developed for Ondensetron Hydrochloride possess reasonable bioadhesion measured in terms of in vitro residence time and elongation at break values.
  1. Patel RS, Poddar SS: The study was concerned with the preparation and evaluation of mucoadhesive buccal patches for the controlled systemic delivery of Salbutamol sulphate to avoid first pass hepatic metabolism. The developed patches were evaluated for the physicochemical, mechanical and drug release characteristics, the patches showed desired mechanical and physicochemical properties to withstand environment of oral cavity. Where, also evaluated for accelareted stability studies under various accelerated condition and they also followed non- Fickian release pattern.
  1. Satyabrata B, Ellaiah P, Choudhury R, Murthy KVR, Bibhutibhusan P, Kumar MS: In this study a bilaminated patches composed of mixture of methotrexate and sodium alginate alone or in combination with sodium carboxy methyl cellulose, polyvinyl pyrollidine and carbopol 934 and backing membrane of ethyl cellulose were prepared by solvent casting technique. The result showed that the drug release of 70.78% in 8 hours was achieved with formulation not containing PVP/PCA through buccal mucosa followed zero order kinetics. The ex-vivo data fitted to korsmeyer-peppas equation which characterized the release mechanism as non-Fickian.
  1. Vishnu YV, Chandrasekhar K, Ramesh G, Rao YM: A buccal patch for systemic administration of carvedilol in the oral cavity has was developed by using HPMC, HPC. The results indicate that suitable bioadhesive buccal patches with desired permeability could be prepared. Bioavailability studies in healthy pigs reveal that carvedilol has got good buccal absorption. The bioavailability of carvedilol from buccal patches has increased 2.29 folds when compared to that of oral solution.The devolpment of bioadhesive buccal formulation for one dose carvedilol has decreased side effect when formulated with HPMC E-15.
  1. Cuvillo AD, Mullol J, Bartra J, Dávila I, Jáuregui I, Montoro J,Sastre J, Valeroet.al: Has studied the comparative absorption of H-1 antihistamine.Most anti histamine shows better absorption when administered through oral route shows better effective plasma concentration within 3 hours after the drug has been administred, good liposolubility of this anti histamines allows to pass cell membrane with no difficulties by facilitating their bioavailability.
  1. K Kathiresan, Vijin P, Moorthi C, Manavalan R:Formulated loratidine chewable tablets by using Avicel CE 15 (Microcrystalline cellulose 70% and guar gum 30%) and starch paste showed better physical character of chewable tablets and better dissolution profile. Stability study showed no significant changes in physical parameters like weight variation, hardness, friability, their drug content and dissolution profile. Hence, the chewable tablet formulations of Loratadine may be an advantageous alternative to oral conventional Loratadine formulation and improve the compliance in children.The use of Avicel CE 15 and starch can show better charectistics of chewable tablets.
ENCLOSURE-III
6.3Objectives of the study
1. To select suitable polymer for Mucoadhesive buccal patches.
2. To formulate mucoadhesive buccal patches of H-1 antihistamine drug to ensure
Immediate release of the drug.
3. Evaluation of different formulations with varying polymer concentration.
4. To evaluate physicochemical properties for the prepared formulation.
5. To carry out in vitro permeation study of mucoadhesive buccal patches.
6. To carry out measurement of in vitro residence time.
ENCLOSURE-IV
MATERIALS AND METHODS:
7. Materials:
Drug : H-1 antihistamine drug.
Polymer: Hydroxypropylmethylcellulose, Polyvinyl alcohol, Polyvinyl pyrollidine,
Sodium carboxy methyl cellulose, Ethyl cellulose, Sodium alginate.
Solvents: Water, Alcohol.
Equipments: Magnetic stirrer, Vacuum oven, Desiccator,Digitalbalance, PH meter,
Dissolution apparatus, UV-spectrophotometer, FTIR etc.
Methods: Mucoadhesive buccal patches prepared by solvent casting method.
7.1. Source of Data
1) Review of literature from :
a. Journals : such as
- Indian journal of pharmaceutical sciences.
- International journal of comprehensive pharmacy.
- International journal of pharmaceutical research.
- European journal of pharmaceutical sciences.
- International journal of pharmaceutical sciences and Nanotechnology.
b. Internet browsing.
2) Library: M.M.U. College of Pharmacy.
3) Laboratory based studies.
ENCLOSURE-V
7.2. Method of Collection of Data
Data on drugs will be collected through literature survey andfrom
physiochemical database. The steps that will be followed are:
  1. Mucoadhesive buccal patches of H-1 antihistamine drug will be prepareusing different concentration of polymer.
  1. The patches will be evaluated for –
  • Physical appearance.
  • Weight variation.
  • Thickness variation test.
  • Surface pH of Films.
  • Folding endurance.
  • Swelling.
  • Moisture Absorption Studies.
  • Measurement of Mechanical Properties.
  • Mucoadhesion and Tensile strength.
  • Drug content.
  • In vitro Release Studies.
  • Measurement of in vitro Residence Time.
ENCLOSURE-VI
7.3. Does the study require any investigation or intervention to be conducted on patients or other humans or animals? If so, please mention briefly.
-NO-
ENCLOSURE-VII
7.4. Has ethical clearance been obtained from your institution in case of 7.3?
-NOT APPLICABLE-
ENCLOSURE-VIII
LIST OF REFERENCES
1.Borgaonkar PA, Virsen TG, Hariprasanna RC and Najmuddin M. Formulation and in vitro evaluation of buccal tablet of loratidine for effective treatment of allergy.Int. J. Resch. Pharm. Chem. 2011; 1(3): 2231-2281.
2.Deshmane SV, Channawar MA, Chandewar AV, Joshi UM, Biyani KR. Chitosan based sustained release mucoadhesive buccal patches containing verapamil Hcl. Int J. Pharm. and Pharm. Sci. Nov.-Dec. 2009; 1(1): 216-219.
3.Manasa B, Gudas GK, Sravanthi N, Madhuri RA, Lavanya Y, Pranitha C. Formulation and Evaluation of Mucoadhesive Buccal Patches of Resperidone. J. Chem. Pharm. Res. 2010; 2(4): 866-872.
4.Anjankumar PB.Design and evaluation of buccal patches of valsartan.J. Pharma. and Cos. 2011; 1(2): 123-129.
5.Dharani S, Shayeda. Formulation and In vitro Evaluation of Mucoadhesive Buccal Patches of Ondansetron Hydrochloride. Int J. Pharma Sci and Nanotech. April – June 2010; 3(1): 860-866.
6.Patel RS, Poddar SS.Development and Characterization of Mucoadhesive Buccal Patches of Salbutamol Sulphate. Current Drug Delivery. 2009; 6(1): 140-144.
7.Satyabrata B, Ellaiah P, Choudhury R, Murthy KVR, Bibhutibhusan P, Kumar MS.Design and evaluation of methotrexate buccal mucoadhesive patches. Int J Pharm Biomed Sci.2010; 1(2): 31-36.
8.Vishnu YV, Chandrasekhar K, Ramesh G, Rao YM.Development of Mucoadhesive Patches for Buccal Administration of Carvedilol. Current Drug Delivery.2007; 4(1): 27-39.
9.Cuvillo AD, Mullol J, Bartra J, Dávila I, Jáuregui I, Montoro J, Sastre J.Comparative pharmacology of the H1 antihistamines. J Investig Allergol Clin Immunol. 2006; 16(1): 3-12.
10.Kathiresan K, Vijin P, Moorthi C, Manavalan R.Formulation and evaluation of loratadine chewable tablets.Ind.Res. J. Pharm. Bio. & Chem. Sci.Oct. – Dec. 2010; 1(4): 763.