TABLE OF CONTENTS
Title page
Abstract
Table of contents
List of Abbreviations
CHAPTER ONE
1.0 INTRODUCTION
1.1 Pharmaceutical Tablets
1.1.1 Properties of a Good Tablet
1.1.2 Advantages and Disadvantages of Tablet as a Solid Dosage Form
1.1.3 Advantages
1.1.4 Disadvantages
1.2 MANUFACTURE OF TABLETS
1.2.1 Dry Granulation
1.2.2 Wet Granulation
1.2.3 Direct Compression
1.3 TABLET PRESSES
1.3.1 Single Punch Press
1.3.2 Rotary Press
1.4 TABLETING EXCIPIENTS
1.4.1 Diluents (Fillers)
1.4.2 Binders
1.4.3 Disintegrants
1.4.4 Lubricants
1.4.5 Sweeteners, Flavours and Colouring Agents
1.5 NEED FOR DEVELOPMENT OF NEW EXCIPIENTS
1.5.1 New Excipients Sources
1.6 MODIFICATION OF STARCH
1.6.1 Physical Modification
1.6.2 Chemical Modification
1.6.3 Enzymatic Modification
1.6.4 Genetic Modification
1.7 POWDER COMPACTION AND PARTICLE BONDING
1.7.1 Powder Consolidation Models
1.7.2 Factors that affect the Mechanical Properties of Powders
1.7.3 Brittle Fracture Index
1.7.4 Tableting Behaviour of Pharmaceutical Materials
1.8 STATEMENT OF THE RESEARCH PROBLEM
1.8.1 Justification for the Study
1.8.2 Aim
1.8.3 Objectives
1.8.4 Scope of Work
CHAPTER TWO
2.0 LITERATURE REVIEW
2.1 TABLET MANUFACTURING
2.1.1 Direct Compression
2.1.2 An Ideal Direct compression Excipient
2.2 CO-PROCESSING
2.3 EXAMPLES OF DIRECTLY COMPRESSIBLE EXCIPIENTS
2.3.1 Soluble Fillers
2.3.2 Cellulose Derivatives
2.3.3 Sugars
2.3.4 Starch Rx1500
2.3.5 Dicalcium Phosphate Dihydrate
2.4 EXAMPLES OF CO-PROCESSED DIRECTLY COMPRESSIBLE EXCIPIENTS
2.5 Starch
2.5.1 Structure of Starch
2.6 MODIFICATION OF STARCH
2.6.1 Properties of Starch granules
2.6.2 Aim of Modification
2.6.3 Methods of Modification
2.6.4 Studies on Modified Starches
CHAPTER THREE
3.0 MATERIALS AND METHODS
3.1 MATERIALS
3.1.1 Chemicals and Reagents
3.2 METHODS
3.2.1 Collection and Identification of Cassava Tubers
3.2.2 Extraction of Cassava Starch
3.2.3 Preparation of Acid Modified Starch
3.3 PHYSICOCHEMICAL TESTS CARRIED OUT ON STARCH
3.4 EVALUATION OF BASIC POWDER PROPERTIES OF MODIFIED STARCH
3.4.1 Particle Size Analysis
3.4.2 Determination of True Density
3.4.3 Flow Rate
3.4.4 Angle of Repose
3.4.5 Bulk/Tapped densities
3.4.6 Powder Porosity
3.4.7 Hydration Capacity
3.4.8 Swelling Capacity
3.4.9 Moisture Sorption Capacity
3.4.10 Loss on Drying/ Moisture content
3.5 PREPARATION OF CO-PROCESSED EXCIPIENTS CONSISTING OF ACID HYDROLYZED STARCH, GELATIN AND LACTOSE
3.6 EVALUATION OF THE POWDER PROPERTIES OF THE CO-PROCESSED EXCIPIENTS
3.6.1 Basic Powder Properties
3.6.2 FTIR Studies
3.6.3 DSC Studies
3.6.4 Dilution Potential
3.6.5 Compaction Studies
3.6.6 Determination of Tensile Strength
3.6.7 Determination of Brittle Fracture Index (BFI)
3.7 FORMULATION STUDIES
3.8 EVALUATION OF TABLET PROPERTIES
3.9 STATISTICAL ANALYSIS
CHAPTER FOUR
4.0 RESULTS
4.1 PRELIMINARY INVESTIGATION OF NATIVE CASSAVA STARCH AND ACID MODIFIED CASSAVA STARCH
4.1.1 Organoleptic properties
4.1.2 Physico-chemical properties of Native Cassava Starch and various Batches of Acid hydrolyzed Cassava Starch (AHS)
4.1.3 Comparison of the Physicochemical Properties of Native Cassava Starch with Acid Hydrolyzed Cassava Starch, (after 24h of hydrolysis)
4.2 INVESTIGATION OF TABLETS PROPERTIES OF VARIOUS BATCHES OF ACID HYDROLYZED CASSAVA STARCH
4.3 PHYSICOCHEMICAL PROPERTIES OF VARIOUS BATCHES OF CO-PROCESSED EXCIPIENTS
4.4 PRELIMINARY INVESTIGATION OF THE TABLETING PROPERTIES OF VARIOUS BATCHES OF STARGELAC
4.5 CHARACTERIZATION OF STARGELAC (SGL4)
4.6 DILUTION POTENTIAL STUDY
4.7 COMPACT ANALYSIS OF CO-PROCESSED EXCIPIENTS
4.7.1 Heckel Analysis
4.7.2 Kawakita Analysis
4.8 MECHANICAL PROPERTIES OF STARGELAC AND SOME COMMERCIAL DC EXCIPIENTS
4.9 ANALYSIS OF TABLETS FORMULATED WITH CO-PROCESSED EXCIPIENTS AND MODEL DRUGS
4.10 DISSOLUTION STUDIES
CHAPTER FIVE
5.0 DISCUSSION
5.1 PRELIMINARY INVESTIGATION
5.1.1 ORGANOLEPTIC AND PHYSICOCHEMICAL PROPERTIES OF NATIVE CASSAVA STARCH AND ACID MODIFIED CASSAVA STARCH
5.1.2 PHYSICOCHEMICAL PROPERTIES OF NATIVE CASSAVA STARCH AND VARIOUS BATCHES OF ACID HYDROLYZED STARCH
5.2 INVESTIGATION OF TABLETS PROPERTIES OF NATIVE CASSAVA STARCH AND VARIOUS BATCHES OF ACID HYDROLZED STARCH
5.3 PRELIMINARY INVESTIGATION OF THE PHYSIO-CHEMICAL PROPERTIES OF VARIOUS BATCHES OF CO-PROCESSED EXCIPIENTS
5.4 PRELIMINARY INVESTIGATION OF THE TABLETS PROPERTIES OF VARIOUS BATCHES OF CO-PROCESSED EXCIPIENT
5.5 CHARACTERIZATION OF CO-PROCESSED EXCIPIENT STARGELAC (SGL IV)
5.6 FTIR STUDY
5.7 DSC
5.8 DILUTION POTENTIAL STUDY
5.9 COMPACT ANALYSIS OF CO-PROCESSED EXCIPIENT
5.9.1 Heckel Analysis
5.9.2 Kawakita Analysis
5.10 MECHANICAL PROPERTIES OF STARGELAC AND SOME COMMERCIAL DIRECT COMPRESSION EXCIPIENTS
5.11 ANALYSIS OF TABLETS FORMULATED WITH CO-PROCESSED EXCIPIENT AND MODEL DRUGS
5.12 DISSOLUTION STUDIES
CHAPTER SIX
6.0 SUMMARY, CONCLUSION AND RECOMMENDATION
6.1 SUMMARY
6.2 CONCLUSION
6.3 RECOMMENDATIONS
REFERENCES
APPENDICES
ABSTRACT
Co-processed excipients are a mixture of two or more existing excipients at subparticle level. These multipurpose excipients have significantly reduced the number of incorporating excipients in the tablet. The aim of this work is to design and prepare a co-processed excipient from acid hydrolyzed cassava starch, gelatin and lactose and evaluate its functionality in tablet formulations. Native cassava starch (NCS) extracted from cassava tubers ( Mannihot esculenta crantz ) was modified chemically by acid hydrolysis using the
process described by the World Intellectual Property Organization, to obtain acid
hydrolyzed cassava starch. The flow, compression and tableting properties of acid hydrolyzed cassava starch were evaluated using flow rate, angle of repose, bulk and tapped densities, Hausner‟s ratio, Carr‟s (compressibility) index, friability, crushing strength and disintegration time. Acid hydrolyzed starch (AHS-24) was co-processed with gelatin and lactose in ratios of 52.5:5:42.5; 42.5:5:52.5; 32.5:5:62.5; 22.5:5:72.5 and 12.5:5:82.5 using the co-drying method. These initial batches of co-excipients that were developed were evaluated for their physicochemical and tableting properties. Further characterization utilized: hydration capacity, Fourier Transfor Infrared Spectroscopy (FTIR) study, Differential Scanning calorimetry (DSC), compaction indices from Heckel and Kawakita analyses, dilution potential and mechanical strength properties such as tensile strength and brittle fracture indices as indicators. Paracetamol and ascorbic acid tablets were prepared by direct compression using StarGeLac as filler-binder-disintegrant and the tablet properties were evaluated and compared with those prepared with Starlac® and Ludipress® as reference materials. The evaluation showed that the average flow rate, angle of repose and Carr‟s index of native cassava starch were 0.9 g/sec, 38.7o and 36.84 %, respectively. The corresponding values for acid hydrolyzed cassava starch (after 24 h exposure time) were 4.6 g/sec, 16.2 o and 14.9 % , showing improved functionality. Also the average flow rate, angle of repose and Carr‟s index of StarGeLac (batch IV, component ratio of acid hydrolyzed cassava starch, gelatin, lactose 22.5:5:72.5) were 50.8 g/sec, 28.9o and 16.6 %, respectively. Tablets prepared, without model drugs, using StarGeLac IV had crushing strength of 7.9 Kgf, friability of 0.8 % and disintegrated witin 6.53 minutes. The results also show that StarGeLac IV exhibited satisfactory hydration capacity, showed no evidence of chemical changes through FTIR and DSC studies and satisfactorily compressed 40 % and 33.3% of paracetamol and ascorbic acid respectively. Heckel and Kawakita plots also showed that StarGeLac consolidates by plastic deformation but that the onset was slow (higher Py value).The study also revealed that tablets of paracetamol and ascorbic acid, used as model drugs, that were prepared using StarGeLac were comparable to those prepared with Starlac ® and Ludipress®. Paracetamol tablets prepared with StarGeLac exhibited higher mean crushing strength and mean disintegration time than the ascorbic acid counterpart but both paracetamol and ascorbic acid tablets prepared with the commercial co-processed excipients had faster disintegration times.
CHAPTER ONE
INTRODUCTION
1.1 PHARMACEUTICAL TABLETS
The oral route is the most common way of administering drugs and among the oral dosage forms, tablets of various kinds are the most common type of solid dosage form in contemporary use (Kaur et al., 2011).
Modern tablet compression was instituted in England in 1844 by William Brockedon (1787-1854) who established early procedures for making compressed pills.
Tablets contain one or more active ingredients as well as a series of other components used to formulate a complete preparation usually by compression in a confined space. They contain a single dose of one or more active substances and usually obtained by compressing uniform quantities of particles (Swarbarick and Boylan, 2002).
The European Pharmacopoeia (2002) defines tablets as “solid preparations each containing a single dose of one or more active ingredients and usually obtained by compressing uniform volumes of particles; some are swallowed whole, some after being chewed, some are dissolved or dispersed in water before being administered and some are retained in the mouth where the active ingredient is liberated”. Tablets vary in shape and differ greatly in size and weight, depending on amount of medicinal substances and the intended mode of administration.
The main reasons behind formulation of different types of tablets are to create a delivery system that is relatively simple and inexpensive to manufacture, provide the dosage form......
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