protocol proposal to university on ''Design and in-vitro evaluation of floating tablets of gabapentin.''

1. “FORMULATION AND IN-VITRO EVALUATION OF FLOATING
TABLETS OF GABAPENTIN”
A Protocol/ Research Proposal of dissertation submitted to
Solapur University, Solapur.
In partial fulfillment of the requirements for the award of the degree of
Master of Pharmacy
In
Pharmaceutics
By
Mr. Shinde Shivaji Vasudeo. B. Pharm.
Under the Guidance of
Mr. Bathe Ritesh S. M. Pharm.
Assistant Professor
Department of Pharmaceutics,
Sahyadri College of Pharmacy, Methwade- 413307
2015-2016
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2. CONTENTS
1. Introduction
2. Need for the study
3. Aim and objective of the study
4. Plan of work
5. Materials and methods
6. Evaluation of tablets
7. Sources of the data
8. References
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3. 1.INTRODUCTION
 The oral route is the most preferred route of administration of drugs
because of low cost of therapy, ease of administration, patient
compliance and flexibility in formulation etc.
 It is evident from the recent scientific and patent literature that an
increased interest in novel dosage forms that are retained in the stomach
for a prolonged and predictable period of time exists today in academic
and industrial research groups and development of novel drug delivery
systems by overcoming physiological troubles such as short gastric
residence times and unpredictable gastric emptying times.1-2
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4. 4
Floating Drug Delivery Systems (FDDS) is one amongst the GRDFs
(Gastro- Retentive Dosage forms) used to achieve prolonged gastric
residence time, providing opportunity for both local and systemic drug
action.
A floating dosage form is useful for those drugs that act locally in the
proximal gastrointestinal tract (GIT) are unstable in lower parts of GIT, or
are poorly absorbed in the intestine.
In the present investigation, gabapentin, an anticonvulsant, was selected
for design of GRDDS in the form of effervescent floating drug delivery
system i.e. floating tablets. Gabapentin is well known drug widely used for
the treatment of seizures and neuropathic pain 3, 4.
However, due to its short half-life (5-7h) and low bioavailability (60%),
traditional immediate-release gabapentin solid dosage forms need to be
administrated three times a day.

5. 1.2 TYPES OF GASTRO RETENTIVE DOSAGE FORMS:6
 1. High density systems.
 2. Floating systems.
a. Effervescent floating dosage forms.
b. Non effervescent dosage forms.
c. Raft forming systems.
d. Low density systems.
 3. Expandable systems.
 4. Super porous hydrogels.
 5. Mucoadhesive/ bioadhesive systems.
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6. 1.3 SUITABLE DRUG CANDIDATES FOR GASTRO RETENTION:7
 The drug having any of the following properties:
 1. Narrow absorption window in gastrointestinal time (GIT), E.g.
Gabapentin, Metformin and Levodopa.
 2. Primarily absorbed from stomach and upper part of gastrointestinal tract
(GIT), Example: Calcium supplements, Chlordizepoxide and Cinnarazine.
 3. Drugs that act locally in the stomach, Example. Antacids and
Misoprostol.
 4. Drugs that degrade in the colon, Example. Ranitidine HCl and
Metronidazole.
 5. Drugs that disturbs normal colonic bacteria, Example. Amoxicillin
trihydrate.
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7. 1.4 ADVANTAGES OF FLOATING DRUG DELIVERY SYSTEM 7
 These systems are particularly advantageous for drugs that are
specifically absorbed from stomach or the proximal part of the small
intestine, e.g., riboflavin and furosemide.
 The fluctuations in plasma drug concentration are minimized, and
concentration‐dependent adverse effects that are associated with peak
concentrations can be prevented. This feature is of special importance
for drugs with a narrow therapeutic index.
 The efficacy of the medicaments administered utilizing the sustained
release principle of floating formulation has been found to be
independent of the site of particular medicaments.
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8. 1.5LIMITATIONS OF FLOATING DRUG DELIVERY SYSTEMS. 7, 8
1. A high level of fluid in the stomach is required for drug delivery to
float and work efficiently.
2.Drugs which have stability and solubility problems in gastrointestinal
tract (GIT) are not suitable candidates for these types of systems.
3. Drugs which irritant to Gastric mucosa are also not desirable.
4. The drug substances that are unstable in the acidic environment of
the stomach are not suitable candidates to be incorporated in the
systems.
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9. 2. NEED FOR THE STUDY:
 Thus as per the discussion a drug i.e. Gabapentin would be an ideal
candidate for the floating drug delivery system.
 In the current formulation development an attempt was made to
design, development and evaluate Gastro retentive floating drug
delivery system of Gabapentin.
 Our aim behind this formulation development of delivery that release the
drug for longer period of time and at controlled rate and floating
of the same for more than eight hours.
 Therefore, an attempt has been made to develop Floating Drug Delivery
System of Gabapentin to achieve local action of drug in the stomach by
increasing its gastric residence time and also releasing it at a controlled
rate to ensure ‘once a day’ administration and optimum bioavailability,
thereby, minimizing its side effects and hence enhanced patient
compliance.11
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10. 3. AIM & OBJECTIVE OF THE STUDY
Aim
 To design and in-vitro evaluate the floating tablets of Gabapentin.
Objectives
The present research investigation is planned with following objectives:
 To design floating tablets using polymers that retains the dosage form in the
stomach.
 To investigate the effect of amount of citric acid and hydroxyl propyl methyl
cellulose on the formulation to monitor the sustained release effect
respectively.
 To evaluate and characterize the formulation with respect to the various
physical parameter.
 In-vitro buoyancy study.
 Swelling index
 In-vitro dissolution study.
 The release data will fit in to different kinetic.
 Stability study
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11. 4. PLAN OF WORK
 Literature survey.
 Selection of Drug and Polymers.
 Pre-formulation studies of drug.
 Compatibility study of drug and polymers.
 Pre-compression evaluations of drug.
 Preparation of floating tablets of selected drug.
 Post compression Evaluations of floating tablets.
 Thickness
 Hardness
 Weight variation
 Friability
 Swelling index
 In-vitro buoyancy study
 In-vitro drug release studies
 Drug release kinetic study.
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12. 5. MATERIALS & METHODS
Materials
 Following chemicals will be procured from the reliable sources and from it
suitable combination will be selected and formulation will be designed and
optimized.
 Drug: Anticonvulsant(e.g. Gabapentin)
 Polymers: - Hydroxy propyl methyl cellulose k100M, K15M.
 Excipients:-Sodium bicarbonate, Lactose, Magnesium Stearate, Aerosol etc.
Method of Preparation of Floating tablets 6,10,12
 The Floating tablet of drug will be formulated by direct compression
method or wet granulation method by using different polymers.
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13. 13
Sr. No. Instruments Name of company
1. Tablet compression machine Karnavati Rimek
Mini Press-I
2. Electronic Weighing Balance Citizen
3. Dissolution Test Apparatus Electro Lab 8
Vessels
4. UV double beam
Spectrophotometer
Shimadzu 1800
Japan
5.3 LIST OF EQUIPMENTS:
Following equipment will be used for the formulation and evaluation of
floating tablets

14. 6. EVALUATION OF TABLETS 5
Physical Evaluation
 Preformulation studies
 Drug Excipient Compatibility studies
Flow properties of blend
 Angle of repose.
 Carr’s index,
 Hausner’s ratios,
 Bulk Density,
 Tapped Density.
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Evaluation of tablets
o Weight variation
o Thickness
o Hardness
o Friability
o Drug content uniformity
o In-Vitro Drug Release studies
o In-Vitro buoyancy studies
o Swelling index
o Stability studies

15. 7. SOURCES OF THE DATA
 The preliminary data required for the experimental study was obtained
fromLibrary of Sahyadri College of Pharmacy, Methwade, Sangola.
 Journals and e-journals.
 Internet sources.
7.1 Method of collection of data
 Internet browsing.
 Referring books and Referring National and International journals.
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16. 8. REFERENCES
1. Arora Shweta, Ali Javed , Ahuja Alka, Kha rRoop K. and Baboota Sanjula,
Floating Drug Delivery Systems: Review. American Association of
Pharmaceutical Scientist (AAPS) Pharm Sci Tec, 2005; 06(03): 372-390.
2. Prescott LC, Nimma WS., “In rate control In Drug Therapy”, 1985; 59.
3. Tripathi, K.D., Essentials of Medical Pharmacology, 5thEdn, New Jaypee
Brothers, Delhi 2003.
4. Goodman and Gilman. The Pharmacological Basis of Therapeutics. 11thEdn.
McGraw-Hill, New York 2006.
5.CH.Swarna Kamala Chinthala*, K.Srinivas Reddy Kota, M. Hadassah,
E.HepsibhaMetilda, S.SrideviFormulation and evaluation of gastroretentive
floating tablets of gabapentin using effervescent technology., Int J Pharm
Biomed Res 2012, 3(4), 202-208.
6. Zaware SR, Gaikwad PD, Bankar VH, Pawar SP,A Review on Floating Drug
Delivery System, Int J Pharma Sci, 2010; 2(3): 834–847. 16

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7. Punitha S, Sabitha G, A Review Article On Floating Drug Delivery System
Chronotherapeutic Approach, Int Res J Pharm, 2011;2(4):38-45.
8. Bardonnt pl, a review article on gastroretentive dosage form: overview and
special case of helicobacter pylori, J contr rel, 2006:1-18.
9. Sharma HL, Sharma KK, Principles of pharmacology. 1st edition. Paras
medical publisher, Hyderabad, new delhi; 2007.392
10. Kaza Rajesh, Usharani E, Nagaraju R, Haribabu R, Siva Reddy P.V. Design
and evaluation of sustained release floating tablets for the treatment of gastric
ulcers, J Pharma Sci & Res, 2009;1(4):81-7.
11. The official compendia of standards. USP/NF,2007,Pharmacopeal Forum;
32(6):1689.
12. Www.Medicinenet.Com [updated on 2009 sep 24]. Available at:
http://www.Medicinenet.Com/gastroesophageal_reflux_disease_gerd/article.Html

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