“FORMULATION AND EVALUATION OF floating MICROSPHERES

of lansoprazole”

DISSERTATION PROTOCOL

Submitted to the

RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES,

BANGALORE, KARNATAKA

BY

PATHAK NARESH SHRIRAM.

M.Pharm, PART- I

DEPARTMENT OF PHARMACEUTICS

UNDER THE GUIDANCE OF

K.SENTHIL KUMAR, M.Pharm.

ASST.PROFESSOR

DEPARTMENT OF PHARMACEUTICS

Dr.H.L.T College of Pharmacy,

Kengal, Chennapatna-571502

2009

RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES, KARNATAKA, BANGALORE

Annexure – II

PROFORMA FOR REGISTRATION OF SUBJECT FOR DISSERTATION

1. / Name of the candidate and address /

mr. Pathak Naresh Shriram

DEPARTMENT OF pharmaceutics,
Dr.H.L.T. COLLEGE OF PHARMACY, KENGAL, CHaNNAPATANA – 571 502. Ramanagara dist., KARNATAKA.
2. /

Name of the institution

/ Dr.H.L.T. COLLEGE OF PHARMACY, KENGAL, CHANNAPATANA – 571 502 Ramanagara dist., KARNATAKA.
3. /

Course of study & subject

/ MASTER OF PHARMACY IN pharmaceutics.
4. /

Date of admission to course

/ 30th april 2009
5. /

Title of the topic

“formulation AND EVALUATION OF floating MICROSPHERES OF LANSOPRAZOLE”


6. Brief resume of the intended work:

6.1 Need for the study:

The floating drug delivery system or hydrodynamically balanced systems are among the several approaches that have been made developed in order to increase the gastric transit time of drug. The microspheres are characteristically free flowing powders consisting of natural or synthetic polymers and ideally having a particle size less than 200mm. Microspheres incorporating a drug dispersed or dissolved throughout particle matrix have the potential for the controlled release of drug1

Microspheres are one of the multiparticulate delivery system and are prepared to obtain controlled the drug release from the dosage form to improve bioavailability, reduces the adverse action and prolong the action of drug, reduce absorption difference in patients, reduce the dosing frequency and adverse effects during prolong treatment. It is needed to formulate in long acting dosage form, reaching to effective biological site rapidly.2,3

Lansoprazole is usually administered as conventional tablet form with the dose 15 mg, Lansoprazole is proton pump inhibitor which prevents stomach from producing gastric acid. The biological half life of Lansoprazole is 1.5 hr.4

Microspheres are one of the multiple unit dosage forms. Solvent evaporation method is the preparation technique that is widely preferred for the preparation of controlled release microspheres. To prepare emulsion by adding the dispersed phase consisting of drug, polymer and appropriate dispersion agent in organic solvent to dispersion medium which is immiscible with the dispersed phase and minimatrix forms are obtained by removing the solvent used at the dispersed phase from the droplets which are formed in the emulsion5, 6.

Advantages of microspheres: -

1.  Taste and odour masking of drug.

2.  Protection of drug against the environment (moisture, light, heat and oxidation.)

3.  To improve the bioavailability.

4.  To decrease the side effects.

5.  To reduce the dose frequency.

6.  To relative stability.

7.  To increase the patient compliance.

8.  To have better therapeutic efficacy.

9.  To reduce the fluctuation in plasma drug concentration.

10.  Safe handling of toxic substances.

11.  Production of sustained release and controlled release medication, 7. .

Among the micro particulate systems, microspheres have a special importance since it is possible to target drug and provide controlled release.8

In this present study is aimed to prepare Floating microspheres containing Lansoprazole to achieve a controlled drug release profile as well as to increase the gastric transit time.

6.2 Review of Literature:

An explicit literature review was done by exploring through various national & international journals, official standard reference books and by surfing through various websites on the internet.9

1.  Varaporn et.al. Studied the floating property and release characteristic of hallow microspheres of Acyclovir. The microspheres were prepared by solvent evaporation technique. The present study shows that the hallow microspheres improve the bioavailability and patients compliance by prolonging the residence time in gastrointestinal tract.10

2.  E.Dini et.al, Synthesis and characterization of cross linked chitosan microspheres containing an hydrophilic drug, Hydroquinone. The microspheres were prepared by suspension cross linking method using glutaraldehyde. It was found that slower drug release rate was obtained from microspheres prepared by using a high concentration of chitosan.11

3.  Anandkumar Shrivastava et.al. Preparation of characterization of floating microsphere of cemitidine. The cemitidine microsphere were prepared by solvent evaporation method, thus this study shows that floating microspheres will increase the gastric residence time.12

4.  T. Comoglue et.al. Prepared the microspheres of Pantaprazole by solvent evaporation method and characterize. The pantaprazole is the proton pump inhibitor used in treatment of gastric ulcer and gastroesophagal disease. So purpose of this study was to developed the microspheres that absorb through gastrointestinal tract.13

5.  Hui Yun Zhou et.al. Prepared the Cellulose acetate (CA) /Chitosan multimicrospheres of Ranitidine. He prepared microsphere by w/o/w emulsion technique. The concentration of CA and the ratio of CA: Chitosan influence the drug release. It prolongs the release of Ranitidine.14

6.  Jain A.K. et.al. prepared the Buyont microsphere of Famotidine. The microspheres were prepared by solvent evaporation method. The presen study conlude that Buyont microspheres prolongs the gastric residence time of Famotidine15

6.3 Objectives of the Study:

The objectives of proposed study are:

1. Preparation of Floating Microspheres containing Lansoprazole

2. Evaluation of Microspheres

1.  Incorporation efficiency of microspheres,

2.  Surface morphology of microspheres,

3.  Particle size analysis,

4.  Buoyancy Percentage,

5.  In vitro release.

7. Materials and Methods:

Materials:-

1)  Drug: Lansoprazole.

2)  Polymers: Hydroxypropyl methylcellulose (HPMC), Ethyl cellulose (EC).

Method:-

Preparation of microspheres by solvent evaporation method.

Evaluation: as in section 7.2

7.1 Source of Data:

The preliminary data required for the experimental study was obtained from:

CD-Rom search available at National Center for Scientific Information (NCSI). “Indian Institute of Science, Bangalore”; Dr.H.L.T.College of pharmacy library; scientific abstracts; Journals; Internet sources; relevant books.

The data will be collected by laboratory investigation at Pharmaceutics Department Laboratory of Dr. HLTCP and recording observation. Microspheres shall prepare by using suitable methods.

7.2Method of collection of data: (Including sampling procedure, if any)

Microspheres shall prepare by using solvent evaporation methods.

·  The evaluation of microspheres shall be carried out by using following instruments.

1.  Compatibility studies: - Compatibility of drug with various polymers will be investigated using UV, IR.

2.  Surface Morphology: SEM, Optical microscopy,

3.  Particle size determination,;

4.  Estimation of drug content by using UV-Spectroscopic method

5.  Sieve analysis.

·  In vitro dissolution study: USP Dissolution Apparatus (DISSO 2000, LAB INDIA)

·  Obtained data will be subjected to statistical analysis.

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.

Not applicable.

7.4 Has ethical clearance been obtained from your institution in case of 7.3?

Not applicable.

8. List of References:

1)  Vyas Khar, Roop K khar. Microspheres. Chap 11, Targeted and controlled drug delivery. Published by CBS prakashan, I st edn, 2002; P-418

2)  A. A. Deshpande, C. T. Rhodes, N. H. Shah and A. W. Malick, Controlled-release drug delivery systems for prolonged gastric residence: an overview, Drug Dev. Ind. Pharm. 22 (1996) 531–539.

3)  Raymond et.al, Handbook of Pharmaceutical Excipients. Published by Pharmaceutical Press, sixth edition, 2006, P-262-267(EC),333-337(HPMC)

4)  Muge klicarslan, Tamer Baykara. The effect of the drug/ polymer ratio on the properties of the verapamil HCl loaded microspheres. Int.J.Pharmaceutics 252:2003; 99-109.

5)  James Swarbrick, James C.Boylan. Encyclopedia of Pharmaceutical technology, Volume 12, New York (NY), Marcel Dekker, Inc; 1995.

6)  L. Whitehead, J. T. Fell, J. H. Collett, H. L. Sharma and A. M. Smith, Floating dosage forms: an in vivo study demonstrating prolonged gastric retention, J. Control. Rel. 55 (1998) 3–12.

7)  R. Talukder and R. Fassihi, Gastro retentive delivery systems: a mini review, Drug Dev. Ind. Pharm 30(2002)1019-1028

8)  N. Rouge, J. C. Leroux, E. T. Cole, E. Doelker and P. Buri, Prevention of the sticking tendency of floating minitablets filled into hard gelatin capsules, Eur. J. Biopharm. 43 (1997) 165–171.

9)  www.CRBestBuydrug.com.

10)  Varaporn, Floating properties and release characteristics of hallow microsphere of Acyclovir, Drug delivery 15(5)2008 331-341.

11) E DINI et.at, Synthesis and Characterization of cross – linked chitosan microspheres for drug delivery application. Journal of Microencapsulation 20(3): 2003; 375-385.

12) Anand kumar shrivastava Floating microsphere formulation characterization of Cemitidine acta pharm 55(2005)277-285

13) T.Comoglue.Preparation and development and in vitro evaluation of Pentaprazole loaded microsphere,Drug delivery 15(5)2008 295-302.

14) Hui Yun Zhou Cellulose acetate/Chittosan multi microsphere of ranitidine in vitro release Drug Release 13(2006)261-267

15) A.K.Jain, Buoyant microsphere of famotidine an approach dosage form for gastric dosage form J.young pharm 1(2009)20-23

16) Jain sunil k, Floating microsphere as Drug delivery system newer approaches Current drug delivery 5(2008)220-223.

17) . A. J. Moes, Gastro retentive dosage forms, Crit. Rev. Ther. Drug Carrier Syst. 10 (1993) 143–195.

18) Parul Trivedi, Verma, N.Garuda. Preparation and characterization of Aceclofenac microspheres. Asian.J.Pharmaceutics, vol.2 issue2:2008, P.110-115.

9. /

Signature of candidate

10. /

Remark of the guides

The above given information is true and this work will be done under my guidance.

11. / Name & Designation of
(in block letters)
11.1 Guide / Mr.K.SENTHIL KUMAR M.Pharm
ASST.PROFESSOR
DEPARTMENT OF PHARMACEUTICS
Dr.H.L.T. COLLEGE OF PHARMACY
KENGAL, CHANNAPATNA-571502
KARNATAKA.
11.2 Signature
11.3 Co-guide (if any)
11.4 Signature
11.5 Head of the Department / Mr. RAVADA RAMESH M.Pharm
PROFESSOR
DEPARTMENT OF PHARMACEUTICS
Dr.H.L.T. COLLEGE OF PHARMACY
KENGAL, CHANNAPATNA-571502
KARNATAKA.
11.6 Signature
12. / 12.1  Remarks of the Chairman & Principal / The above-mentioned information is correct and I recommend the same for approval.
12.2 Signature

From

Pathak Naresh Shriram.

M.Pharm, PART I

Dept.Pharmaceutics,

Dr.H.L.T College of Pharmacy,

Kengal, Channapatna.

Ramanagara Dist.,

TO

The Registrar (Evaluation),

Rajiv Gandhi University of Health Sciences,

Karnataka Bangalore,

4th ‘‘T’’ Block, Jaynagar,

Bangalore - 560 041

(Through Proper Channel)

Sub: Submission of Synopsis of Dissertation

Respected Sir,

Here with, I am submitting synopsis of dissertation work “FORMULATION AND EVALUATION OF FLOATING MICROSPHERES OF LANSoPRAZOLE” for registration in M.Pharm (Pharmaceutics) of Rajiv Gandhi University of Health Sciences, Bangalore, Karnataka.

Kindly accept the same and acknowledge.

Thanking you,

Yours Faithfully,

(PATHAK NARESH SHRIRAM.)

Place: Channapatna

Date:

Guide:

K. SENTHIL KUMAR M.Pharm,

ASST. PROFESSOR

DEPT OF PHARMACEUTICS, PRINCIPAL

Dr. H.L.T.College of Pharmacy, Dr. H.L.T.College of Pharmacy,

Kengal, Channapatna. Kengal, Channapatna.

Ramanagara Dist.-571502 Ramanagara Dist. - 571502

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