vaibhav tb
TRANSCRIPT
FORMULATION DEVELOPMENT AND EVALUATION OF ANTI-TB TABLETS
Name of student Name of guide Mr.Vaibhav Tate Mrs.Swapnila Shinde (M. Pharm Sem – 3rd Pharmaceutics) (Dept. of Pharmaceutics)
Sinhgad Institute of Pharmacy, Narhe, Pune
CONTENTS
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INTRODUCTION
LITRATURE SURVEY
AIM & OBJECTIVE
PLAN OF WORK
EXPERIMENTAL METHODLOGY
EVALUATION
REFERENCE
INTRODUCTION
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Tuberculosis, or TB, is an infectious bacterial disease caused by Mycobacterium tuberculosis,
most commonly affects the lungs. It is transmitted from person to person via droplets from the throat and lungs of people with the active respiratory disease
gram +ve bacilliNon motile, non sporing,& noncapsulated
TRANSMISSIONTB spread from person to person by airborne
transmission. Infected person release droplet nuclei (1-5 micro meter in diameter) through, Talking Coughing Sneezing Laughing Singing
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SYMPTOMS
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SIGNIFICANT LAB TEST
Sputum examination and Cultures; Is examined under a microscope to look for tuberculosis bacteria and
used to grow the bacteria in a culture Interferon-gamma Blood test; A simple blood is mixed with synthetic proteins similar to those
produced by the tuberculosis bacteria. If people are infected with tuberculosis bacteria, their white blood
cells produce certain substances (interferon) in response to the synthetic proteins.
Imaging Consideration Chest C.T Scan Chest X Ray
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TREATMENT
• Prevent death
• Cure
• Prevent relapse
• Prevent transmission
• Prevent development of • Drug resistance
AIM
CLASSIFICATION OF DRUG
First-line drugs: good efficacy, less toxicity and being well tolerated for patients Isoniazid (INH), Rifampin, Pyrazinamide, Ethambutol, Streptomycin. Second-line drugs: usually used as alternatives to the first-line drug when drug
resistance occurs or when a particular therapy is required. Para-aminosalicylic acid, Kanamycin, Amikacin, Capreomycin, Ciprofloxacin, Ethionamide
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Trade name Active drug Manufacturer
3FD Isoniazide Novartis Pharmaceutical
Acute Z IsoniazideRifampicin Biocin Pharma
AKT 3 IsoniazideRifampicinEthambutol
Lupin Pharma
Afarcin 5IsoniazideRifampicin Assam Chemical &
Pharmaceutical Pvt Ltd
AFB 4 Isoniazide Lark Lab.
List of commercially Available AntiTB Tablets
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LITERATURE SURVEY
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LITERATURE SURVEY
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AIM AND OBJECTIVE
AIM : Formulation development and evaluation of Anti-TB tablet.
OBJECTIVE :1) To design, develop and evaluate oral tablet dosage form.2) To provide rapid disintegration ,systemic effect3) Rapid drug release4) To prepare stable formulation.
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PLAN OF WORK
• 1st – 2nd month
• Literature survey, selection of drug & excipients
• 3rd – 4th month
• Pre-formulation study & analytical method development
• 5th – 7th month
• Formulation , Development and Optimization
• 8th -10th month
• In- vitro & In-vivo Evaluation &Stability study as per ICH guidelines
• 11th -12th month
• Thesis writing & Publication
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TB Drug Selection
Bio-equivalence /Bio-availability Drug formulations (tablets, fixed-dose combination tablets
soluble tablets, powder in sachets) Marketing approval/registration Applied pharmacy-economics:
the most cost effective TB treatment = DOTS Costs of different drugs, availability, delivery times
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DRUG PROFILE
ISONIAZIDE
Appearance: White Crystalline Powder
Mol wt : 137.14
Structure:
IUPAC name: pyridine-4-carbohydrazide
Empirical formula: C6H7N3O
Melting point: 170-173 oC
Solubility : soluble In water
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Isoniazide It is the most active drug for the treatment of tuberculosis
After orally administered, well absorbed, widely distributed in body.
Most INH is metabolized in the liver
Mechanism of action
the inhibition of synthesis of mycolic acids, which are important and
characteristic components of mycobacterium cell wall.
As a result of the activity, tubercle bacilli lose their features of acid-
resistance, water-resistance and proliferating ability, leading to death.
Pharmacologic activity- It is bactericidal for actively growing tubercle bacilli. But, for resting
tubercle bacilli, it is bacteriostatic. Isoniazid is able to penetrate into phagocytic cells and thus is active
against both extracellular and intracellular organisms.
Adverse Reaction Allergic Reaction: fever, skin rash. Nausea Vomiting Weakness Dark Urine
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SELECTION OF EXCIPIENTS
Excipients are selected on the basis of compatibility and release of drug from formulation
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FORMULATION AND DEVELOPMENT OF TABLETS
EXCIPIENTS EXAMPLES
API ISONIAZIDE
Binders Maize starch.
Disintegrates Carmalose sodium
Wetting Agent Sodium Lauryl Sulphate
Lubricants Talc, Ca-stearate
solvent Purified water
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TECHNIQUES USE TO PREPARE TABLETS
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PREFORMULATION STUDY
Preformulation Parameter
Affected Properties Evaluation Technique
Color Purity Color strips
Odor Purity Inhalation
Melting point Purity Melting point apparatusDetect Physical changes
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PREFORMULATION STUDY
Preformulation Study Affected Properties Evaluation techniqueParticle Size Distribution
Flow properties during filling, reconstitution time, blend uniformity,syringeability
Sieve analysis with particle sizing equipment
Bulk density & compactability
Flow properties and compact formation in dry powders for reconstitution
Angle of repose, Carrs’ Index, Hausner ratio
Charactrization Provides additional information about drug I.R
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PREFORMULATION STUDY
Characterization of Drug
• Melting Point Determination
Apparatus- Buchi-M560
Standard M.P-170-173 oC
Observed M.P 173 oC
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PREFORMULATION STUDY
FT-IR Spectroscopy of Isoniazide:Apparatus-Perkinelmer 304082
Software-Spectraes
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EVALUATION TABLETS
• General parameters
• Hardness
• Friability
• Weight variation
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EVALUATION OF TABLETS
• Disintegration time
• Content uniformity
• Dissolution test
Stability
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Approach to understanding the mechanism of action of isoniazid, an anti-TB Drug Lingaraja Jena a, Pranita Waghmare a, Supriya Kashikar b, Satish Kumar Received 2 August 2014 Accepted 5 August 2014 Available online 2 September 2014
Quality Problem of Anti-TB FDC Combination a way to Forward Saranji Singh1, Hemant Bhutani2 and T.T. Mariappan3 (Original receive on 13.12.2005. Revised version received on 6.3.2006. Accepted on 6.6.2006)
REFERENCE
. Treatment of tuberculosis. In: Sharma SK, Mohan A (Eds). Tuberculosis, 2nd edn. New Delhi: Jaypee Brothers Medical Publishers; 2009.pp.751-75.
Centers for Disease Control and Prevention Division of Tuberculosis Elimination website http://www.cdc.gov/nchstp/tb
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REFERENCE
Handbook of Anti-Tuberculosis Agents Global Alliance for TB Drug Development 80 Broad Street Volume 88 Number 2 2008 Pages 85–170
Effect of maize starch excipient properties on drug release Rate P. Zámostný a*, J. Petrů, D. Majerová a Department of Organic Technology, Faculty of Chemical Technology, Institute of Chemical Tech Prague Technika 5, 166 28
http://www.who.int/tb/en/
http://www.drugbank.ca/drugs/DB00951