Abstract:
The purpose of present research work was to
optimize the formulation of fast dissolving tablet
of carbamazepine. Carbamazepine is one the most
prescribed antiepileptic drug. Fast dissolving
tablets of carbamazepine were prepared by using
different types of superdisintegrants like
croscarmellose sodium and sodium starch
glycolate. Fast dissolving tablet is prepared by
direct compression method. The formulations
were evaluated for wetting time, hardness,
friability, content uniformity, invitro
disintegration time, release profile. The result
revealed that the formulation F5 which containing
the 5% croscarmellose sodium as a
superdisintegrant have good dissolution profile
with shortest Disintegration time. It can be
concluded that the tablet of carbamazepine with
better pharmaceutical properties than conventional
tablets could be obtained using formulation F5.
FORMULATION AND EVALUATION OF OCUSERTS OF CIPROFLOXACIN HClMohammad Adil
Conventional ocular drug delivery system i.e., eye drops, ointments, gels etc., had become less popular pertaining to their disadvantages like evaporation by tears, pre-corneal loss, drug metabolism, drug-protein interaction, drainage, sticking of eye lids, induced lacrimation, poor patient compliance, systemic side effect and blurred vision etc. That’s why fundamentals of controlled release by means of ocular inserts were utilized to increase problem pre-corneal drug residence time.
This project title “Formulation and Evaluation of Ocuserts of Ciprofloxacin HCl” revealed following results:
Compatibility study using FTIR was performed to check the compatibility of drug with various excipient. Characteristics peaks obtained with pure drug were compared with that produced with different excipients that confirmed the compatibility of drug with excipients.
Ocusert of Ciprofloxacin HCl was prepared using different material i.e., PVP K-30, PVA, PEG 400 and glycerin.
Prepared ocuserts were evaluated for various parameters viz., percentage moisture loss, percentage moisture absorbs, thickness, weight variation, drug content and In-vitro diffusion.
The percentage (%) moisture absorption and loss of ocular insert were found to be 26% and 27% respectively.
The thickness of ocular insert was found to be uniformed and its mean while measuring at different points was found to be 0.124mm.
The weight of ocular inserts was found to be in the range of 12.2 - 12.6mg which indicated decent distribution of the drug, polymer and plasticizer.
The drug content of ocular insert was found to be 99.89%.
Percentage drug release from Ciprofloxacin HCl Ocusert was found to be 41.969% in 8 hr.
It was concluded that prepared Ocusert of Ciprofloxacin HCl could be a better alternative to conventional ocular formulations that retained on ocular surface for longer duration and released drug in controlled manner.
The release of the drug substance from the drug product leading to the bioavailability of the drug substance. The assessment of drug product performance is imp. Since bioavailability is related both to the pharmacodynamic responses and the adverse events. The performance tests relate the quality of a drug product to clinical safety and efficacy.
Bioavailability studies are drug product performance studies used to define
the effect of changes in the physicochemical properties of the drug substance, the formulation of the drug, and the manufacturing process of the drug product.
FORMULATION AND EVALUATION OF OCUSERTS OF CIPROFLOXACIN HClMohammad Adil
Conventional ocular drug delivery system i.e., eye drops, ointments, gels etc., had become less popular pertaining to their disadvantages like evaporation by tears, pre-corneal loss, drug metabolism, drug-protein interaction, drainage, sticking of eye lids, induced lacrimation, poor patient compliance, systemic side effect and blurred vision etc. That’s why fundamentals of controlled release by means of ocular inserts were utilized to increase problem pre-corneal drug residence time.
This project title “Formulation and Evaluation of Ocuserts of Ciprofloxacin HCl” revealed following results:
Compatibility study using FTIR was performed to check the compatibility of drug with various excipient. Characteristics peaks obtained with pure drug were compared with that produced with different excipients that confirmed the compatibility of drug with excipients.
Ocusert of Ciprofloxacin HCl was prepared using different material i.e., PVP K-30, PVA, PEG 400 and glycerin.
Prepared ocuserts were evaluated for various parameters viz., percentage moisture loss, percentage moisture absorbs, thickness, weight variation, drug content and In-vitro diffusion.
The percentage (%) moisture absorption and loss of ocular insert were found to be 26% and 27% respectively.
The thickness of ocular insert was found to be uniformed and its mean while measuring at different points was found to be 0.124mm.
The weight of ocular inserts was found to be in the range of 12.2 - 12.6mg which indicated decent distribution of the drug, polymer and plasticizer.
The drug content of ocular insert was found to be 99.89%.
Percentage drug release from Ciprofloxacin HCl Ocusert was found to be 41.969% in 8 hr.
It was concluded that prepared Ocusert of Ciprofloxacin HCl could be a better alternative to conventional ocular formulations that retained on ocular surface for longer duration and released drug in controlled manner.
The release of the drug substance from the drug product leading to the bioavailability of the drug substance. The assessment of drug product performance is imp. Since bioavailability is related both to the pharmacodynamic responses and the adverse events. The performance tests relate the quality of a drug product to clinical safety and efficacy.
Bioavailability studies are drug product performance studies used to define
the effect of changes in the physicochemical properties of the drug substance, the formulation of the drug, and the manufacturing process of the drug product.
DISSOLUTION
Dissolution is a process in which solid substance solubilizes in a given solvent
DISSOLUTION TESTING
A dissolution test uses an apparatus with specific test conditions in combination with acceptance criteria to evaluate the performance of the product. In-vitro test must predict the in-vivo behaviour
Factors in design of dissolution tests:
Factors relating to dissolution apparatus
Factors relation to dissolution fluid
Process parameters
Need of Dissolution Testing:
Development and optimisation of dosage forms
Batch to batch drug release uniformity
Quality, safety, efficacy and stability of the product
IVIV Correlation
Bioequivalence
Assessing pre and post approval changes
DISSOLUTION APPARATUS
Dissolution apparatus evolved to prepare a sample under controlled conditions thereby making the test repeatable.
Principle types of dissolution apparatus-
Close-compartment apparatus
Open-compartment apparatus
Dialysis systems
Ideal features of Dissolution Apparatus:
The fabrication, dimensions, and positioning of all components must be precisely specified and reproducible
Simple in design, easy to operate and useable
Sensitive
Nearly perfect sink conditions
Provide an easy means of introducing the dosage form into the dissolution medium
Provide minimum mechanical abrasion
Easy withdrawal of samples
Elimination of evaporation of solvent medium
DISSOLUTION METHODS
The Standard Dissolution Methods Database has been prepared by the Division of Bioequivalence, Office of Generic Drugs (OGD), Center for Drug Evaluation and Research (CDER), Food and Drug Administration (FDA).
Official methods:
Rotating Basket
Rotating Paddle
Reciprocating Cylinder
Flow-Through Cell
Paddle Over Disc
Rotating Cylinder
Reciprocating Disc
Non-official methods:
Static Disc Method
Beaker Method
Flask Stirrer Method
Peristalsis Method
Rotating Bottle Method
Dialysis Method
Diffusion Cell Method
Dissolution Apparatus Types and their Applications
Problems associated with dissolution apparatus
USP Performance Verification Test (PVT):
The USP Performance Verification Test (PVT) assesses the suitable performance of apparatus used in dissolution testing.
Responsible for detecting problems associated with the dissolution apparatus that are found to be within mechanical tolerances.
REFERENCES
Biopharmaceutic considerations in drug product design and In Vitro Drug Produ...PRAJAKTASAWANT33
Introduction, biopharmaceutic factors affecting drug bioavailability, rate–limiting steps in drug absorption, physicochemical nature of the drug formulation factors affecting drug product performance
Optimization technique is a rational approach for selecting the excipients, their concentrations and process conditions for obtaining the best possible product satisfying the quality characteristics.
Optimization is an act, process or methodology of making design, system or decisions as fully perfect, functional or as effective as possible.
Approaches Of Gastro-Retentive Drug Delivery System or GRDDSAkshayPatane
Approaches Of Gastro-Retentive Drug Delivery System
Includes:
Floating and Non-Floating drug delivery system with their subtypes
Like Non-effervescent system, Effervescent system, Raft forming system,
High Density system, Expandable system, Muco-adhesive system,
Super porous hydrogel system and Magnetic Systems, etc.
This PPT includes what role does Dosage form impart on absorption. Why it is important in absorption. what should be its nature and type of dosage form.
Formulation and evaluation ofmetformin HCl micro beads by ionotropic gelation...Sagar Savale
The Metformin HCL Micro Beads is formulated by the Ionotropic Gelation Method. The CMC is a Swellable
polymer is responsible for the Sustained release action or activity. A combination of CMC (Carboxy Methyl
Cellulose) and Sodium Alginate shows better sustained release activity. The PreparedSustained released Micro
Beadsis Evaluated In terms of bulk density, tapped density, angle of repose, Carr’s Index, Swelling Index, Drug
Content, % Encapsulation Efficiency and vitro study. The result associated in Optimized batch is good to
Satisfactory and having a good free flowing property. The Drug Content and % Encapsulation Efficiency values are
within the pharmacopeia limit. The in vitro Dissolution studies shows Maximum percentage of release of drug
(71.15) with in end of 4 Hours.
DISSOLUTION
Dissolution is a process in which solid substance solubilizes in a given solvent
DISSOLUTION TESTING
A dissolution test uses an apparatus with specific test conditions in combination with acceptance criteria to evaluate the performance of the product. In-vitro test must predict the in-vivo behaviour
Factors in design of dissolution tests:
Factors relating to dissolution apparatus
Factors relation to dissolution fluid
Process parameters
Need of Dissolution Testing:
Development and optimisation of dosage forms
Batch to batch drug release uniformity
Quality, safety, efficacy and stability of the product
IVIV Correlation
Bioequivalence
Assessing pre and post approval changes
DISSOLUTION APPARATUS
Dissolution apparatus evolved to prepare a sample under controlled conditions thereby making the test repeatable.
Principle types of dissolution apparatus-
Close-compartment apparatus
Open-compartment apparatus
Dialysis systems
Ideal features of Dissolution Apparatus:
The fabrication, dimensions, and positioning of all components must be precisely specified and reproducible
Simple in design, easy to operate and useable
Sensitive
Nearly perfect sink conditions
Provide an easy means of introducing the dosage form into the dissolution medium
Provide minimum mechanical abrasion
Easy withdrawal of samples
Elimination of evaporation of solvent medium
DISSOLUTION METHODS
The Standard Dissolution Methods Database has been prepared by the Division of Bioequivalence, Office of Generic Drugs (OGD), Center for Drug Evaluation and Research (CDER), Food and Drug Administration (FDA).
Official methods:
Rotating Basket
Rotating Paddle
Reciprocating Cylinder
Flow-Through Cell
Paddle Over Disc
Rotating Cylinder
Reciprocating Disc
Non-official methods:
Static Disc Method
Beaker Method
Flask Stirrer Method
Peristalsis Method
Rotating Bottle Method
Dialysis Method
Diffusion Cell Method
Dissolution Apparatus Types and their Applications
Problems associated with dissolution apparatus
USP Performance Verification Test (PVT):
The USP Performance Verification Test (PVT) assesses the suitable performance of apparatus used in dissolution testing.
Responsible for detecting problems associated with the dissolution apparatus that are found to be within mechanical tolerances.
REFERENCES
Biopharmaceutic considerations in drug product design and In Vitro Drug Produ...PRAJAKTASAWANT33
Introduction, biopharmaceutic factors affecting drug bioavailability, rate–limiting steps in drug absorption, physicochemical nature of the drug formulation factors affecting drug product performance
Optimization technique is a rational approach for selecting the excipients, their concentrations and process conditions for obtaining the best possible product satisfying the quality characteristics.
Optimization is an act, process or methodology of making design, system or decisions as fully perfect, functional or as effective as possible.
Approaches Of Gastro-Retentive Drug Delivery System or GRDDSAkshayPatane
Approaches Of Gastro-Retentive Drug Delivery System
Includes:
Floating and Non-Floating drug delivery system with their subtypes
Like Non-effervescent system, Effervescent system, Raft forming system,
High Density system, Expandable system, Muco-adhesive system,
Super porous hydrogel system and Magnetic Systems, etc.
This PPT includes what role does Dosage form impart on absorption. Why it is important in absorption. what should be its nature and type of dosage form.
Formulation and evaluation ofmetformin HCl micro beads by ionotropic gelation...Sagar Savale
The Metformin HCL Micro Beads is formulated by the Ionotropic Gelation Method. The CMC is a Swellable
polymer is responsible for the Sustained release action or activity. A combination of CMC (Carboxy Methyl
Cellulose) and Sodium Alginate shows better sustained release activity. The PreparedSustained released Micro
Beadsis Evaluated In terms of bulk density, tapped density, angle of repose, Carr’s Index, Swelling Index, Drug
Content, % Encapsulation Efficiency and vitro study. The result associated in Optimized batch is good to
Satisfactory and having a good free flowing property. The Drug Content and % Encapsulation Efficiency values are
within the pharmacopeia limit. The in vitro Dissolution studies shows Maximum percentage of release of drug
(71.15) with in end of 4 Hours.
Formulation development and invitro evaluation of lamotrigine fast dissolving...SriramNagarajan19
The present study was to formulate and evaluate oral fast dissolving Oral tablet containing Lamotrigine. Present study reveals that all the nine formulated tablet showed satisfactory tablet parameters. It can be concluded that, Oral fast dissolving tablet -containing Lamotrigine can be prepared by direct compression method. 10% CCS (FV) tablet exhibited required disintegration time and dissolution time. The drug release was about 98.7 % in 15min. The accelerated stability studies of the optimized F5 formulation indicates that the formulated oral fast dissolving tablet were unaffected after 3 months storage under accelerated conditions as there were no signs of visually distinguishable changes in appearance, disintegration time and cumulative percentage of drug release. From the present investigation it can be concluded that oral fast dissolving tablet formulation can be a potential novel drug dosage form for pediatric, geriatric and also for general population.
Formulation and Evaluation of Fast Dissolving Tablets of Paracetamol Using Oa...inventionjournals
Paracetamol is a slightly water soluble drug belongs to BCS Class IV, used in various pain managements & in management of fever. The drug solubility was increased by solid dispersion method, in which two techniques namely physical mixing and co-grinding were tried at the ratios of 1:0.25, 1:0.5 & 1:0.75 for paracetamol to oats powder. Various parameters like pre & post compressional parameters were tested and final formula was selected based on disintegration time and in-vitro dissolution profile. Where, all the formulations were dispersed bellow 92 seconds and F6 formulation was showing 100% release at 20th minute and faster compared to the marketed formulation. F6 was prepared by co-grinding technique, at 1:0.75 paracetamol to oats powder ratio. F6 is showing zero-order drug release and mechanism of release is Super case – II transport (n = 0.9738). All the formulations were prepared using direct compression method, a conventional method of preparation
Formulation and Evaluation of Fast Dissolving Tablets of Paracetamol Using Oa...inventionjournals
Paracetamol is a slightly water soluble drug belongs to BCS Class IV, used in various pain managements & in management of fever. The drug solubility was increased by solid dispersion method, in which two techniques namely physical mixing and co-grinding were tried at the ratios of 1:0.25, 1:0.5 & 1:0.75 for paracetamol to oats powder. Various parameters like pre & post compressional parameters were tested and final formula was selected based on disintegration time and in-vitro dissolution profile. Where, all the formulations were dispersed bellow 92 seconds and F6 formulation was showing 100% release at 20th minute and faster compared to the marketed formulation. F6 was prepared by co-grinding technique, at 1:0.75 paracetamol to oats powder ratio. F6 is showing zero-order drug release and mechanism of release is Super case – II transport (n = 0.9738). All the formulations were prepared using direct compression method, a conventional method of preparation
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
All manuscripts are subject to rapid peer review. Those of high quality (not previously published and not under consideration for publication in another journal) will be published without delay.
The oral route is the most favorable route for administration of drugs because of accurate dosage, low cost of therapy, self medication, non-invasive method, and ease of administration leading to a high level of patient compliance. Of the oral Dosage forms, solid dosage form is the preferred class of product as tablet represents a unit dosage form in which one dose of drug is placed accurately.
Effervescent technique in development of floating tablets for antiviral drugsSriramNagarajan19
The purpose of this investigation was to prepare a regiospesific drug delivery system of Stavudine. Floating tablets of Stavudine were prepared by direct compression method employing different concentration of HPMC K15M by effervescent technique. Sodium bicarbonate was incorporated as a gas-generating agent. The floating tablets were evaluated for uniformity of weight, hardness, friability, drug content, swelling studies, in vitro buoyancy and dissolution studies. The effect of different concentration of HPMC K15M on drug release profile and floating properties was investigated. The prepared tablets exhibited satisfactory physico-chemical characteristics. All the prepared batches showed good in vitro buoyancy. The tablet swelled radially and axially during in vitro buoyancy studies. It was observed that the tablet remained buoyant for more than 12 hours. Increased in the HPMC K15M level, decreased the floating lag time but tablets floated for longer duration. The formulation with 1:1 drug: Polymer ratios were found to float for longer duration as compared with other formulations containing HPMC K15M. The drug release from the tablets was sufficiently sustained and non-Fickian transport of the drug from tablets was confirmed.
The Metformin HCL Gastroretentive Floating Sustained released Tablet is formulated by the Wet Granulation technique. This Tablet is containing both Effervescent as well as Non Effervescent system. The HPMC K 100 Swellable polymer is responsible for the Floating. (Non Effervescent system) and The Sodium Bicarbonate is responsible for
the effervescent system. A combination of HPMC K 100 and Xanthum Gum shows better sustained release activity. The Prepared Gastroretentive Floating Sustained released Tablet is Evaluated In terms of bulk density, tapped density, angle of repose, Carr’s Index and, weight variation test, friability test and in vitro study, Total Floating Time. The result associated in Optimized batch is good to Satisfactory and having a good free flowing property. The weight variation and friability these values are within the pharmacopeia limit. The in vitro Dissolution studies shows Maximum percentage of release of drug (99.25) with in end of 8 Hours.
ABSTRACT The purpose of this study was to prepare and evaluate immediate release itraconazole pellets and comprehensive studies of the same. The itraconazole pellets is prepared using fluid bed processer with different concentration of HPMC (Hydroxy Propyl Methyl Cellulose). The physicochemical compatibility of the drug and the excipient studied by differential scanning calorimetry. The prepared pellets were physically evaluated with size, shape, bulk density, tapped density, compressibility index, hausners ratio, angle of repose, sieve analysis, surface roughness, density, moisture content, assay and drug release etc. The in vitro drug release profile from pellets shows that all the formulation release more than 75% drug within 90min. Optimized formulations were found to have HPMC concentration 2-5% of total weight of pellets to maximize high-quality surface, desired release, and size distribution within the range. These results indicate that pellets containing 10 % HPMC of total weight of pellets give better quality of itraconazole pellets for immediate release. Key Words: Itraconazole, Hydroxyl propyl methyl cellulose and Immediate release.
CO–PROCESSED EXCIPIENTS FOR TABLETS.pdfYamini Shah
Purpose of the present review is to provide an in depth knowledge on recent developments in excipients preparation, technology and approaches involved in their formation and development. Excipients play an important role in dosage form development. In conventional formulation of dosage forms, each excipient is used to provide its required function/performance. Presently, excipient manufacturers have focused their attention on producing a multifunctional excipients with improvement in their performance and quality of dosage form. Manipulation in the functionality of excipient is provided by the co-processing of two or more existing excipients.
Formulation and evaluation of mucoadhesive tablets of carvedilol using natura...Nausheen Fatima
Present work describes formulation and evaluation mucoadhesive tablets of Carvedilol using natural binders such as Chitosan and Guar Gum to reduce the first pass metabolism and frequency of administration.
Abstract:
The present study was done with the aim to evaluate anthelmintic activity of ethanolic extract of Cassia occidentalis Linn using adult earthworm Pheritima posthuma. Various concentrations (25, 50, 75 mg/ml) of all extracts were tested and results were expressed in terms of time for paralysis and time for death of worms. Albendazole was used as a reference standard and gum acacia in saline as a control group. Dose dependent activity was observed in all extracts Cassia occidentalis Linn.
Abstract
A total ten strains of Pseudomonas spp. were isolated frompaddy soil. Among isolated strains three Pseudomonasisolates P1, P2 and P3were shown siderophore production on succinic acid medium and chromo azural S agarplate medium.The ability of Pseudomonas to grow and to produce siderophores is dependent on the iron content and the type of carbon sources in the medium. Four basal media, supplemented with different concentration of iron, were employed to study the effectof iron and different organic carbon sources on siderophore production in Pseudomonas isolates.Cell growth reached a maximal value with150µ/ml Fe3+ siderophore production was maximum at this iron concentration. The optimal iron concentration for high siderophore production was in the succinate medium.The cultures under study, growth of cultures increasing with the increased concentration of iron up to 60µM, where as siderophore production repressed at high concentration of iron. Maximum siderophore production was 94, 88, 83 units for P1, P2 and P3 isolates respectively. All three isolates have shown both type of siderophore production i.e. wine red color formation in supernatant indicated production of hydroxamate type (pyoverdine) while yellow color formation in supernatant showed presence of catecholate or phenolate type (pyochelin) siderophore.
Abstract
A rapid advance of nanotechnology has the potential approach for significant improvements in disease prevention, diagnosis and treatment. In this article, we report a simple and eco-friendly biosynthesis of silver nanoparticles (Ag-NPs) using silver nitrate as metal precursor in Curcuma longa. These Ag-NPs were characterized by UV–vis spectroscopy, and Transmission electron microscopy (TEM). These nanoparticles exhibited maximum absorbance in specific nano meter range in UV–vis spectroscopy. TEM micrographs revealed the formation of well-dispersed Ag-NPs with its size and morphology. Microbiology assay founds that Ag-NPs are effective against V.cholera bacteria. These developments raise exciting opportunities to diagnose and treat pathogenic mode of infection based on the various profiles to target diseases.
Abstract:
Hyperlipidemia is a major risk factor in the
initiation and progression of atherosclerotic lesions,
conditions such as coronary heart disease, ischemic
cerebrovascular disease and peripheral vascular
disease. This leads to high mortality and morbidity
rate in developed countries. This is mainly due to
altered lipoprotein metabolism. Standard treatments
for Hyperlipidemia & dyslipidemia with statins and
with the other available agents have adverse effects.
Thus, there is more need for development of newer
pharmacological agents which are more efficient in
lowering LDL Cholesterol and Triglycerides. The
hypolipidemic activity of Nathaichoori Chooranam
was studied on high fat diet induced
hyperlipidemic rats. Hyperlipidemia in experimental
rats was evidenced by an enhancement in the levels
of Cholesterols, Triglycerides, LDL and VLDL.
The trial drug showed significant hypolipidemic
effect by lowering the serum levels of biochemical
parameters, such as significant reduction in the level
of serum Cholesterol, TGL, LDL, VLDL and
increase in HDL level which was similar to the
standard drug atorvastatin. So, it is concluded that
the Nathaichoori chooranam can be used in the
treatment of Hyperlipidemia and Obesity.
Abstract
The compounds of the invention are solid crystallines stable to the light and heat. They show an interesting activity in preventing the depression from reserpine at doses which do not cause any untoward side efiects of the parameters considered. The study of the examined products shows a slight calming action. The first symptoms of toxicity are observed at about 1000-12000 rug/kg. by oral route. At the tested doses, the compounds are without anticonvulsive and antitremorin activity. At higher doses they potentiate barbituric hypnosis. The following table illustrates the antidepressing activity of 4H-3-carboxamidomethyl-l,3-benzoxazine-2-one to reserpine in comparison with the antidepressing activity of imipramine. 1.4H-3-carboxamidomethyl-1,3-benzoxazine- 2-one 37.9 grams of ethyl glyciuate hydrochloride were dissolved in 400 cc. of ethanol and 33.5 g. of salicylic aldehyde were added. It is refluxed for half an hour and cooled. 38 cc. of triethylamine and g. of Raney nickel are then added whereafter hydrogenation is carried out at room temperature and under atmospheric pressure. After hydrogen adsorption was complete, the mixture was filtered and the alcohol evaporated 01f. The residue was taken up with acidified water, extracted with ether to eliminate part of the byproducts, consisting mainly of o.cresol, then made alkaline with ammonia and extracted with ethyl acetate. The solvent was removed in vacuo and the residue crystallized from ether/ petroleum ether. 36.7 g. of o-hydroxybenzyl-aminoacetic acid ethyl ester melting at 47 C. are obtained.
Abstract
A simple and accurate UV method has been developed for the simultaneous estimation of Hamycin and Ketoconazole cream formulation using SHIMADZU UV-Visible 1700 spectrophotometer by simultaneous equation method, with Acetonitrile: 0.5% w/v Ammonium acetate (80:20v/v) as a solvent. The absorbance maxima were found to be 381.5 nm for Hamycin and 243.5 nm for Ketoconazole. The percentage purity of cream formulation was found to be 99.08% for Hamycin and 98.22% for Ketoconazole. This method was also validated by checking the accuracy, precision, LOQ, LOD and Ruggedness. The %RSD shows within specification limits. The linearity profile shows coefficient of variation 0.99 for both drugs.
Abstract:
The present study was done with the aim to
evaluate anthelmintic activity of ethanolic extract of
Cassia occidentalis Linn using adult earthworm
Pheritima posthuma. Various concentrations
Abstract:
A reduction of hemoglobin concentration in blood
is termed as anemia. Especially women’s are
suffering from anemia due to loss of blood in
menstrual cycle, poor nutrition foods and in
postpartum females and different types of diseases
in humans which causes anemia. To treat this
there is no specific medicine is available except
iron tablets though they are not safe and may
cause serious health problems. That’s why in this
particular review article I will emphasis on the
naturally occurring products which may be
beneficial in anemia.
Abstract:
Aloe Vera has been used medicinally for a few
thousand years. It was sufficiently in demand that
Hannibal was known to have gone to war over it in
order to obtain control over its growing area
Abstract
Calotropis genera comprise of two species, with 90% inhabiting southern Asian country and are most endemic to the India, Indonesia, Malaysia, Thailand, and Srilanka, China. Calotropis gigantea is a weed plant commonly known as giant milk weed. The plant is belonging to Apocynaceae family which includes latex bearing plants. C. gigantea is known for various
medicinal properties in traditional medicinal system and use to cure a variety of diseases. In last few decades, C. gigantea is extensively studied for its medicinal properties by advanced scientific techniques and a variety of bioactive compounds have been isolated from the different parts of the plant and were analysed pharmacologically. The plant is reported for analgesic activity, antimicrobial activity, antioxidant activity, anti-pyretic activity, insecticidal activity, cytotoxicity activity, hepatoprotective activity, pregnancy interceptive properties, purgative properties, procoagulant activity and wound healing activity. The medicinal properties of this plant represent it as a valuable source of medicinal compound. This study is collective information concerning the ethnobotany, pharmacology, phytochemistry and biological activities of the C. gigantea.
Abstract:
Oral hygiene plays a very important role in
generalized health of body that is sadly
overlooked by most doctorsand the patients.Oral
health status profoundly impacts diseases ranging
from type 2 diabetes and cancer to rheumatoid
arthritis and atherosclerosis.Recent scientific
studies show that many of the natural nutrients
confers benefits when topically applied in the
mouth.Acting as powerful allies in the fight
against periodontal disease, these natural
compounds can help safeguard against lethal agerelated
diseases that emanate from our mouths.
A new simple, sensitive, rapid, accurate,
precise and economical Derivative
Spectrophotometric method for the
simultaneous determination of Quinapril
HCl
ABSTRACT
Aim: The aim of present work was to
formulate rapid disintegrating tablet of
Fluoxetine HCLwith pleasant taste and
better mouth feel by sublimation technique.
Materials and Methods: The fast
disintegrating tablet is formulated by
sublimation technique. The super
disintegrant used in present formulation was
crospovidone the other excipient used was
mannitol, Ammonium bicarbonate and
camphor. Result and Discussion: The
cumulative % of drug release of F7 batch of
wet granulation method was found to be
99.26% at the end of 4 min. Formulation F7
prepared by direct compression method
showed 99.71 % drug release at the end of 1
min while formulation F7 prepared by wet
Palestine last event orientationfvgnh .pptxRaedMohamed3
An EFL lesson about the current events in Palestine. It is intended to be for intermediate students who wish to increase their listening skills through a short lesson in power point.
Model Attribute Check Company Auto PropertyCeline George
In Odoo, the multi-company feature allows you to manage multiple companies within a single Odoo database instance. Each company can have its own configurations while still sharing common resources such as products, customers, and suppliers.
Operation “Blue Star” is the only event in the history of Independent India where the state went into war with its own people. Even after about 40 years it is not clear if it was culmination of states anger over people of the region, a political game of power or start of dictatorial chapter in the democratic setup.
The people of Punjab felt alienated from main stream due to denial of their just demands during a long democratic struggle since independence. As it happen all over the word, it led to militant struggle with great loss of lives of military, police and civilian personnel. Killing of Indira Gandhi and massacre of innocent Sikhs in Delhi and other India cities was also associated with this movement.
Macroeconomics- Movie Location
This will be used as part of your Personal Professional Portfolio once graded.
Objective:
Prepare a presentation or a paper using research, basic comparative analysis, data organization and application of economic information. You will make an informed assessment of an economic climate outside of the United States to accomplish an entertainment industry objective.
Acetabularia Information For Class 9 .docxvaibhavrinwa19
Acetabularia acetabulum is a single-celled green alga that in its vegetative state is morphologically differentiated into a basal rhizoid and an axially elongated stalk, which bears whorls of branching hairs. The single diploid nucleus resides in the rhizoid.
Introduction to AI for Nonprofits with Tapp NetworkTechSoup
Dive into the world of AI! Experts Jon Hill and Tareq Monaur will guide you through AI's role in enhancing nonprofit websites and basic marketing strategies, making it easy to understand and apply.
Welcome to TechSoup New Member Orientation and Q&A (May 2024).pdfTechSoup
In this webinar you will learn how your organization can access TechSoup's wide variety of product discount and donation programs. From hardware to software, we'll give you a tour of the tools available to help your nonprofit with productivity, collaboration, financial management, donor tracking, security, and more.
2024.06.01 Introducing a competency framework for languag learning materials ...Sandy Millin
http://sandymillin.wordpress.com/iateflwebinar2024
Published classroom materials form the basis of syllabuses, drive teacher professional development, and have a potentially huge influence on learners, teachers and education systems. All teachers also create their own materials, whether a few sentences on a blackboard, a highly-structured fully-realised online course, or anything in between. Despite this, the knowledge and skills needed to create effective language learning materials are rarely part of teacher training, and are mostly learnt by trial and error.
Knowledge and skills frameworks, generally called competency frameworks, for ELT teachers, trainers and managers have existed for a few years now. However, until I created one for my MA dissertation, there wasn’t one drawing together what we need to know and do to be able to effectively produce language learning materials.
This webinar will introduce you to my framework, highlighting the key competencies I identified from my research. It will also show how anybody involved in language teaching (any language, not just English!), teacher training, managing schools or developing language learning materials can benefit from using the framework.
How to Make a Field invisible in Odoo 17Celine George
It is possible to hide or invisible some fields in odoo. Commonly using “invisible” attribute in the field definition to invisible the fields. This slide will show how to make a field invisible in odoo 17.
Formulation and Evaluation of Fast Dissolving Tablets of Carbamazepine Using Solid Dispersion
1. ISSN: 2348 –0882
==========================================================================
Int. J. Pharm. Res. Sci., 2014, 02(1), 47-59.
www.ijprsonline.com
Formulation and Evaluation of Fast Dissolving Tablets of Carbamazepine
Using Solid Dispersion.
Metkari VB1,*, Kulkarni LV1, Patil PS1, Jadhav PA1, Jadhav PH1, Yadav PS1.
1
College of pharmacy Medha Satara, Maharashtra, India.
Corresponding author email: vmetkari@yahoo.com
---------------------------------------------------------------------------------------------------------------------------------Abstract:
The purpose of present research work was to
optimize the formulation of fast dissolving tablet
of carbamazepine. Carbamazepine is one the most
prescribed antiepileptic drug. Fast dissolving
tablets of carbamazepine were prepared by using
different types of superdisintegrants like
croscarmellose sodium and sodium starch
glycolate. Fast dissolving tablet is prepared by
direct compression method. The formulations
were evaluated for wetting time, hardness,
friability,
content
uniformity,
invitro
disintegration time, release profile. The result
revealed that the formulation F5 which containing
the
5%
croscarmellose
sodium
as
a
superdisintegrant have good dissolution profile
with shortest Disintegration time. It can be
concluded that the tablet of carbamazepine with
better pharmaceutical properties than conventional
tablets could be obtained using formulation F5.
Keywords: Fast dissolving tablet, Croscarmellose
sodium, sodium starch glycolate, Direct
compression.
Introduction:
Oral route has been one of the most of popular
routes of drug delivery due to its ease of
administration, patient compliance, least sterility
constraints and flexible design of dosage forms
(Brahmankar et al., 2005).Many patient of
different age group like geriatric and pediatric
complaint of some solid dosage form because of
difficulty in swallowing. So to solve this problem
and increase patient compliance fast dissolving
tablet is prepared. Fast dissolving tablets are those
when put on tongue disintegrating instantaneously
releasing the drug which dissolves or disperses in
the saliva. Fast dissolving tablets are also called as
mouth dissolving tablets, orodispersible tablets,
rapi melts, porous tablets, quick dissolving etc.
The faster the drug into solution, quicker the
absorption and onset of clinical effects. Some
drugs are absorbed from mouth, pharynx and
esophagus as the saliva passes down into the
stomach. In such cases bioavailability of drug is
significantly greater than those observed from
conventional tablets dosage form. According to
European pharmacopoeia, the ODT should
disintegrate in less than three minutes. The basic
approach in development of fast dissolving tablets
is the use of the superdisintegrants like
crosscarmellose sodium and sodium starch
glycolate.
Which
provide
instaneous
disintegration of the tablets after putting on
tounge, their by release the drug in saliva. The
bioavailability of some drug may be increased due
to absorption of drug in oral cavity and also due to
pregastric absorption of saliva containing
dispersed drugs that pass down into stomach
(
Abed et al., 2010). Fast dissolving tablets are
those when put on tongue disintegrating
instantaneously releasing the drug which dissolves
or disperses in the saliva. Fast dissolving tablets
are also called as mouth dissolving tablets,
orodispersible tablets, rapi melts, porous tablets,
quick dissolving etc.The faster the drug into
solution, quicker the absorption and onset of
clinical effects. Some drugs are absorbed from
mouth, pharynx and esophagus as the saliva
47
2. ISSN: 2348 –0882
==========================================================================
Int. J. Pharm. Res. Sci., 2014, 02(1), 47-59.
passes down into the stomach. In such cases
bioavailability of drug is significantly greater than
those observed from conventional tablets dosage
form. According to European pharmacopoeia, the
ODT should disintegrate in less than three
minutes. The basic approach in development of
fast dissolving tablets is the use of the
superdisintegrants like crosscarmellose sodium
and sodium starch glycolate. Which provide
instaneous disintegration of the tablets after
putting on tounge, their by release the drug in
saliva.The bioavailability of some drug may be
increased due to absorption of drug in oral cavity
and also due to pregastric absorption of saliva
containing dispersed drugs that pass down into
stomach (Madhusudan et al.,).
2. MATERIAL AND METHODS:
2.1 Material:
Carbamazepine is obtained as a gift sample from
Abbott pvt ltd, Mumbai. Croscarmellose sodium
is obtained from Fine chem industry Mumbai.
Sodium starch glycolate is obtained from
Chemika Biochemika Reagents. All other
chemicals used were of analytical grade.
2.2 Methods:
2.2.1 Preparation of solid dispersion of
Carbamazepine
Carbamazepine solid dispersions were prepared
by solvent evaporation, melting and kneading
methods using drug: polyethylene oxide N10 in
proportion, viz. 1:1, 1:1.25, 1:1.5, 1:2. (Drug:
Carrier). Methanol and isopropyl alcohol were
selected as common solvents for solid dispersion.
2.2.1.1 Solvent evaporation method:
The 100 mg of carbamazepine was dissolved in 20
ml of methanol in beaker and weighed amount of
polyethylene oxide N 10 was added and stirred to
dissolve both drug and carrier to get clear
solution. Solution was poured on Petri plate and
allowed to evaporate the solvent. The process of
evaporation was operated until all methanols get
evaporated. Solid dispersion prepared was then
dried at room temperature and stored in
desiccators for further study (Lewis et al., 2009).
www.ijprsonline.com
2.2.1.2 Kneading method
Accurate weighed amount of Carbamazepine and
polyethylene oxide N 10 were taken into glass
mortar and then methanol was added in small
quantity to make paste. The paste was allowed to
stand for 45 mins and then dried in oven at 400c.
The product obtained was pulverized and passed
through mesh (#) 80 and stored in desiccator for
further study (Madhavi et al., 2011).
2.2.1.3 Physical mixture:
Accurate weighed amount of Carbamazepine and
polyethylene oxide N 10 were taken into glass
mortar and then mixed for 10 minutes to get good
mixture of drug and polymer. Then product was
stored in the desiccator for further study
(Kahkeshan et al., 2012).
2.2.1 Formulation of fast dissolving tablets:
Fast dissolving tablets containing optimized
solid dispersion were prepared by direct
compression method using single punch tablet
machine to produce convex faced tablets
weighing 500 mg each with a diameter of 12
mm. A minimum of 40 tablets were prepared
for each batch (Solanki et al.,2011).
2.2.2 By direct compression technique
The direct compression technique was selected for
developing novel fast dissolving tablets. In direct
compression technique all materials accurately
weighed like solid dispersion complex,
microcrystalline cellulose, sodium saccharine,
talc, magnesium state, and mannitol passed
through a 40 mesh prior to mixing. The solid
dispersion complex was properly mixed with
superdisintegrant, and then with diluents MCC.
The mixture was mixed with talc, sodium
saccharine, magnesium state and mannitol. Then
mixture was subjected to compression using
single punch tablet machine (Solanki et al.,2011).
48
3. Table 1. Formulation of fast dissolving tablets using croscarmellose sodium
Ingredients in (mg)
SD complex
Croscarmellose sodium
Microcrystalline cellulose
Mannitol
Magnesium state
Sodium saccharine
talc
Total weight
F1
250
10
145
75
5
10
5
500
F2
250
20
135
75
5
10
5
500
F3
250
30
125
75
5
10
5
500
F4
250
40
115
75
5
10
5
500
F5
250
50
105
75
5
10
5
500
F6
250
75
80
75
5
10
5
500
Table 2. Formulation of fast dissolving tablets using sodium starch glycolate
Ingredients in (mg)
F1 F2 F3
SD complex
250 250 250
Sodium starch glycolate
10 20 30
Microcrystalline cellulose 145 135 125
Mannitol
75 75 75
Magnesium state
5
5
5
Sodium saccharine
10 10 10
talc
5
5
5
Total weight
500 500 500
resistant to powder flow. However, a high bulk
2.2.3 Characterization of blends:
The quality of tablet, once formulated by rule,
density does not necessarily imply a close-packed
is generally dictated by the quality of
low-porosity bed, as bulk density is directly
physicochemical properties of blends. There are
proportional to true density. Bulk density can be
many formulations and process variables
defined as the mass of powder divided by the bulk
involved in mixing step and all these can affect
volume. Bulk density of powder blends was
the characteristics of blend produced. The
determined using 25ml calibrated plastic
characterization of mixed blend done for the
measuring cylinder, in which powder blends were
flow property of powder that are bulk density,
simply poured and bulk density was measured in
tapped density, Hausner’s ratio, Compressibility
unit gm/ml. Bulk density is also known as fluff or
index, angle
of
repose.
The
various
poured bulk density. It can be calculated by
characteristics of blends tested are given below
following equation,
and results were shown in Table below (Kakde et
Bulk Density = Mass/volume
al.,2010).
ρb = M/Vb
Bulk density
Tapped density
Bulk density of powder blend is always less than
As stated above that due to interparticulate voids
the true density of its component particles because
bulk density of a powder is always less than true
the powder contains interparticulate pores or
density. This statement reveals that whereas as a
voids. The bulk density of powder is dependent on
powder can only possess a single true density, it
particle packing and changes as powder
can have many different bulk densities, depending
consolidates. A consolidated powder is likely to
on the way in which the particles are packed and
have a greater arch strength than a less
the bed porosity. For powders having comparable
consolidated one and may therefore be more
true densities, an increase in bulk density causes
49
4. decrease in porosity. This increases the number of
interparticulate contacts and contacts areas and
causes an increase in cohesion. In very coarse
particles this may still be insufficient to overcome
the gravitational influence on particles. Tapped
density is defined as the mass of a powder divided
by the tapped volume. Tapped density of powder
blends was performed for 100 taps by using
digital bulk density equipment and was measured
in unit of gm/ml. True density is also known as
equilibrium, tapped or consolidated bulk density.
It can be calculated by following equation,
Tapped Density = Mass/ Tapped
volume
ρt = M/Vt
’
Carr s Compressibility index
The simplex way of measurement of the free flow
of powder is compressibility, an indication of ease
with which a material can be induced to flow is
given by compressibility index of the granules
was determined by Carr’s compressibility index (I)
which is calculated by using the formula
(Rockville et al.,2000).
Compressibility index = Bulk volume – Tapped
volume/Bulk
volume
×
100
Table 3. Compressibility Index as an Indication of Powder Flow Properties
Carr̀,s Index (%)
>12
12-16
18-21
23-35
33-38
>40
Type of Flow
Excellent
Good
Fair to passable
Poor
Very poor
Extremely poor
funnel that can be raised vertically until a
maximum cone height (h) was obtained. Radius of
heap (r) was measured and angle of repose was
calculated using formula
-1
Ө = tan h/r
Where, Ө is angle of repose, h is height of
pile and r is radius of base pile.
Hausner ratio
Hausner ratio is an indirect index of ease of
powder flow. It is calculated by the following
formul
Hausner ratio = tapped density/ bulk density
Hausner ratio =
ρt/ ρb
Angle of repose
Angle of repose was determined using fixed
funnel method. The blend was poured through a
Table 4. Angle of Repose as an Indication of Powder Flow Properties
Angle of repose (o)
<25
25-30
30-40
>40
2.2.2.4 Characterization of fast dissolving
tablets:
After compression of powder, the tablets were
evaluated for diameter, thickness and physical
characteristics like
hardness,
friability,
Type of flow
Excellent
Good
Passable
Very poor
disintegration time, wetting time, dispersion
time and dissolution studies. The results were
shown in Table below.
Tablet Thickness
50
5. Ten tablets from each batch formulation were
from each formulation and weighed collectively
selected randomly and their thickness was
and average weight was calculated using digital
measured with a screw gauge for calculating
balance. The individual weights were compared
thickness variation (Shirsand et al.,2010).
with the average weight for obtaining weight
variation.
Uniformity of weight
As per IP twenty tablets were taken randomly
Table 5. Weight Variation Limits for Tablets as per IP.
Average of Tablets (mg) Maximum% difference allowed
130 or less
10
130-324
7.5
More than 324
5
The In vitro dispersion time of fast dissolving
Hardness
Hardness of the tablet was measured using the
tablets of carbamazepine was determined by
Monsanto hardness tester (soumya et al.,2013).
placing one tablet in a beaker containing 100 ml
of phosphate buffer and time required for
Friability
Friability of the tablets was determined using
complete dispersion was determined.
Roche friabilator. This device subjects the
Wetting time
tablets to the combined effect of abrasions and
Wetting time of fast dissolving tablets of
shock in a plastic chamber revolving at 25 rpm
carbamazepine was determined by carefully
and dropping the tablets at a height of 6 inch in
placing tablets on to a twice folded circular tissue
each revolution. Pre-weighed sample of tablets
paper placed in a Petri-dish having the internal
was placed in the friabilator and were subjected
diameter of 5 cm containing 6 ml of water. The
to 100 revolutions. Tablets were dusted using a
time required for water to reach the upper surface
soft muslin cloth and reweighed. The friability
of the tablet and to completely weight the tablet
(F %) is determined by the formula (Rangole et
was noted as wetting time(Rangole et al.,2008).
al., 2008).
Water absorption ratio
% friability = loss in weight/initial
The weight of the tablets prior to placing in Petri
weight×100
dish was noted (wb) using the digital balance. The
weighted tablet was removed and reweighed (wa).
Water absorption ratio(R) was then determined
Drug content uniformity
Drug content of fast dissolving tablets of
according to the following equation.
carbamazepine was calculated by weighing ten
R = 100× (wa-wb)
tablets of each formulation, pulverizing to a fine
Where, wb and wa were tablet weights before and
powder. A quantity of powder equivalent to 10 mg
after water absorption respectively.
of carbamazepine dissolved in methanol and
In-vitro dissolution study
solution was filtered through a 0.45 μm whatmann
In-vitro dissolution study of fast dissolving tablets
filter paper. Carbamazepine content was
of carbamazepine was performed according to
determined by measuring the absorbance at 285
USP type-II dissolution apparatus employing a
nm at UV visible spectrophotometer after
paddle stirrer at 50 rpm using 900 ml of phosphate
appropriate dilution with methanol. The drug
buffer of pH 6.8 at 37±0.5 as dissolution medium.
content was determined using calibration curve.
One tablet was used in each test. Aliquots of the
The mean percent drug content was calculated as
dissolution medium 5 ml were withdrawn at
an average of three dimensions(Masareddy et
specific time interval 5, 10, 15,20,25,30 minutes
al.,2008).
and replaced with the equal volume of fresh
medium. The samples were filtered through 0.45
μm whatman analyzed by measuring the
In Vitro dispersion time
51
6. absorbance at 285 nm. Drug concentration was
IR Spectrum of Carbamazepine
calculated from the standard calibration curve and
IR spectrophotometer was used for infrared
expressed as cumulative percent drug dissolved.
spectroscopy analysis of carbamazepine. The
The release studies were performed in triplicate
samples were prepared in KBr disk by means of a
(Arora et al.,2010).
hydrostatic press. The scanning range was 4004000 cm-1 (Wan et al., 2012).
In-vitro Disintegration time
Disintegration of FDT was generally occurring
DSC of Carbamazepine
due to water uptake by superdisintegrant via
Differential
scanning
calorimetry
(DSC)
capillary action, which results in swelling of
measurements were performed on SDT Q600
superdisintegrants and tablet get disintegrated. It
Differential scanning calorimeter. The accurately
was also reported that increased compaction force
weighed sample was placed in an aluminium pan
may increase or decrease disintegration time. In
and an empty aluminium pan was used as a
the present study disintegration test was carried
reference (Wan et al.,2012).
out on six tablets using the apparatus specified in
XRD of carbamazepine
USP (Electrolab disintegration apparatus USP).
XRD of carbamazepine was carried out by using
0
0
The distilled water at 37 C ± 2 C was used as a
the Philips PW 1729 X-ray generator (Wan et
disintegration media and time in second taken for
al.,2012).
complete disintegration of the tablet with no
3. RESULT AND DISSCUSION:
palpable mass remaining in the apparatus was
measured in seconds (Pandit et al., 2012).
Table.6. Solubility of PM and SD in water:
Drug: Polymer ratio Solubility (mg/ml)
PM
SE KM
1:1
0.13 0.16 0.27
1:1.25
0.14 0.18 0.29
1:1.5
0.15 0.19 0.35
1:2
0.14 0.17 0.26
From table 6 it is know that Solubility of
evaporation and kneading method. Kneading
carbamazepine is increased by different methods
method is only method which gives the high
of solid dispersion like physical mixture, solvent
solubility than other method i.e. 0.35 mg/ml.
Table.7.Solubility data of SD prepared by KM in water:
Drug: Polymer ratio Solubility (mg/ml)
1:1
0.27
1:1.25
0.29
1:1.5
0.35
1:1.75
0.29
1:2
0.26
1:3
0.23
1:4
0.23
From table 7 it is clear that proportion of drug to
polymer ratio 1:1.5 give the high solubility i.e.
0.35 mg/ml that’s why 1:1.5 proportion is used for
preparing fast dissolving tablets which gives high
drug release with in 30 mins i.e. 87.5±1.5.
3.1Drug polymer interaction studies:
Drug and polymer interaction study was
carried out by doing the different analysis of pure
52
7. carbamazepine, physical mixture, solid dispersion,
Fourier Transform Infrared Spectroscopy
polymer and the formulation.
Figure 1. IR spectra of A) Pure carbamazepine, B) polyox N 10 C) Physical Mixture D) Solid
almost the same wave number with same intensity
Dispersion E) Formulation F.
IR spectrum of pure carbamazepine,
in the spectra of physical mixture solid dispersion
polyox N 10, Physical Mixture and Solid
which indicate that the absence of any potential
dispersion are shown in figure 1. The IR spectra
physical or chemical interaction between drug and
of pure carbamazepine showed peak at 3458.37,
polymer and other additives, Hence drug nad
3153.61, 3032.10, 1666.50, 1595.13, 1477.47,
polymer were found to be compatible with the
-1
1377.17 cm indicating stretching of N-H, C-H,
drug.
C-H aromatic, amide, C-N , N-H deformation
respectively. These peaks seemed to be retained at
Differential Scanning Colorimetry Analysis
53
8. Figure 2. DSC thermogram of A) Pure carbamazepine, B) polyox N 10 C) Physical Mixture D) Solid
Dispersion E) Formulation F5
One of the most classic application of DSC
physical mixture, solid dispersion and formulation
analysis is the determination of the possible
F5.Endothermic peak of caarbamazepine was not
interaction between the drug and excipients in the
observed in Physical mixture, solid dispersion and
formulation supporting evidence for compatible
formulation F 5 because carbamazepine is
between drug and excipients was obtained from
dispersed in the polyox N10 at molecular level.
DSC analysis studies. As shown in the figure 2 the
This indicate the absence of any
DSC thermogram of carbamazepine showed sharp
interaction between drug and excipients, Hence
0
endothermic peak at 193.93 c which is near to
from above DSC thermogram, it was found that
melting point of carbamazepine.DSC thermogram
there was compatibility between drug and
0
of polyox N 10 showed sharp melting at 73.44 c
excipients.
which also observed in DSC thermogram of
X- Ray Diffraction (XRD)
XRD pattern were recorded using Philips 1729 X-ray generator. Powder X-ray diffraction patterns
were recorded for drug, physical Mixture, solid dispersion and polymer.
Figure 3 . XRD pattern of A) Pure carbamazepine, B) polyox N 10 C) Physical Mixture D) Solid
Dispersion
Figure 3 shows the diffraction pattern of
peaks were observed at 2θ values of 10.32, 13.32,
pure carbamazepine which shows its crystalline
16.16, 19.76, 25.14, 27.88, and 32.33 in
nature that was demonstrated by numerous sharp,
fingerprint regions referring to its crystallinity.
highly intense and less diffused peaks. These
54
9. Peak height of pure carbamazepine was
selected to calculate the RDC of CBZ, best
physical mixture and solid dispersion. When pure
CBZ was considered as a reference sample, a
significant decrement in crystallinity of the
characterized solid dispersion was observed (˂
0.1).RDC values were 1, 0.9 and 0.6. For pure
drug, physical mixture and solid dispersion
respectively indicating the amorphousness of
drug, polymer.
3.2 Characterization of blend for fast
dissolving tablets:
The data for evaluation of powder blends of
rapidly disintegrating tablets of carbamazepine is
as shown below.
Table 7. Characterization of blends:
Formulation code Bulk density Tapped density Hausner’s̀́ ratio Carr’s index Angle of repose
(gm/cm3)
(gm/cm3)
(%)
(Ө)
0.33±0.007
0.37±0.01
1.14±0.008
12.68±0.01
29.7±0.43
F1
0.33±0.01
0.40±0.012
1.20±0.005
16.62±0.69
29.57±0.33
F2
0.31±0.01
0.36±0.010
1.12±0.005
12.93±0.34
26.33±0.39
F3
0.31±0.01
0.39±0.013
1.17±0.008
17.30±0.21
25.38±0.25
F4
0.32±0.01
0.37±0.016
1.12±0.008
11.62±0.25
24.29±0.05
F5
0.33±0.01
0.40±0.007
1.16±0.005
13.27±0.38
28.38±0.21
F6
0.34±0.01
0.40±0.008
1.17±0.008
14.22±0.34
27.46±0.57
F7
0.30±0.01
0.34±0.008
1±0.007
12.39±0.26
25.19±0.10
F8
0.29±0.01
0.35±0.01
1.18±0.03
17.57±0.27
27.45±0.17
F9
Bulk density of powder blends of different
formulation was found to be in the range of 0.29
to 0.34 gm/cm3 whereas the tapped density was
found to be in the range of 0.35 to 0.40 gm/cm3.
Angle of repose was found to be less than 300
which indicate good flow characteristics of the
powder blends. Carr’s index was found to be in
the range of 11.62 to 17.57 whereas the Hausner
ratio was found to be less than 1.25. Both this
values indicate good flow property and good
compression characteristics.
3.3 Evaluation of fast dissolving tablets
3.3.1 Evaluation of physical parameter of
tablets
The data for evaluation of physical parameters of
fast dissolving tablets of carbamazepine is as
shown below.
55
10. Table 8. Evaluation of fast dissolving tablets.
Formulation code Weight variation
(mg)
Passes
F1
Passes
F2
Passes
F3
Passes
F4
Passes
F5
Passes
F6
Passes
F7
Passes
F8
Passes
F9
Diameter
(mm)
12.00±0.007
12.02±0.007
12.024±0.005
12.024±0.005
12.036±0.011
12.054±0.018
12.054±0.015
12.042±0.017
12.064±0.023
Thickness
Hardness Friability
(mm)
(Kg/cm2)
(%)
4.326±0.019 3.14±0.054 0.65±0.11
4.4±0.035
3.22±0.10 0.63±0.11
4.368±0.024 3.04±0.11 0.54±0.14
4.472±0.035 3.02±0.10 0.59±0.07
4.362±0.019
3.1±0.1
0.63±0.06
4.338±0.039 3.24±0.26 0.74±0.07
4.342±0.04 3.04±0.11 0.62±0.08
4.342±0.052 2.94±0.15 0.72±0.10
4.332±0.016 3.12±0.17 0.59±0.09
During weight variation test none of the tablet was
while thickness was found to be in the range of
found to be deviate by permissible percentage as
4.32 to 4.4 mm. Percentage friability was found to
per Indian pharmacopoeia 5% from the mean
be in the range of 0.49 to 0.74 which is within
value of 20 tablets. Thus it was found that all the
limit <1%.
formulations complied with weight variation test.
Hardness of the tablet was found to be in the
3.3.2 Wetting time and water absorption ratio
range of 2.94 to 3.24, which was found to well
The data for wetting time and water
within the required hardness for the fast dissolving
absorption ratio of fast dissolving tablets of
2
tablets (3 to 4 kg/cm ). Diameter of the tablets
carbamazepine is as shown below.
was found to be in the range of 12 to 12.064 mm
Table 9. Data for wetting time and water absorption ratio.
Formulation code Wetting time Water absorption ratio
(sec)
(%)
F1
130.2±0.44
71.14±0.53
F2
116.4±0.89
72.50±0.47
F3
105.2±0.83
77.14±0.03
F4
106.2±0.83
83.35±0.68
F5
97±0.70
97.03±0.01
F6
101±0.70
87.34±0.38
F7
110.6±0.89
82.38±0.66
F8
102.8±0.44
86.26±0.39
F9
113.4±0.89
75.73±0.10
Wetting time was found to be in the range of 97.00 to 130.2. Water absorption ratio was found to be
in the range of 71.14 to 97.03. It may be due to the hydrophilic nature of carriers used. This thing might
result into increased capillary action which has resulted into decreasing the wetting time and increasing the
water absorption ratio.
3.3.3 Disintegration time, uniformity of content and Disintegration time:
The data for disintegration time, uniformity of content and Disintegration time of fast dissolving tablets of
carbamazepine is as shown below.
56
11. Table 10. Data for disintegration time, drug content and Disintegration time of fast dissolving tablets
of carbamazepine.
Formulation code Disintegration time Drug content Dispersion
(sec)
(%)
time (Sec)
F1
85.33±1.52
95.43±0.91
91.10±0.7
F2
80±1.0
98.23±0.96 83.20±1.20
F3
76±1.0
101.84±1.11 81.46±0.5
F4
65±2.0
99.88±0.511
71±1.5
F5
57±1.0
98.85±1.04
62.20±0.6
F6
61.66±1.52
98.39±1.20
67.16±1.2
F7
71.66±1.52
96.22±0.80
75.87±1.4
F8
61±1.0
98.46±0.61
65.57±0.4
F9
63±1.0
102.08±1.09
64±0.5
3.3.4 Disintegration time:
In vitro disintegration times of all
formulations were found to be in the range of 57
to 85.33 Sec, this was found to be well within the
acceptable limit for fast dissolving tablet (≤ 3
min). In vitro disintegration time of all the
formulations was found to decrease with
correspondent increase in the concentration of
both croscarmellose sodium and sodium starch
glycolate. It may be due to the hydrophilic nature
of sodium starch glycolate and croscarmellose
sodium which attracts water and may increase the
capillary action of the tablet matrices which result
into decreasing the disintegration time.
3.3.5 Uniformity of content:
All the formulations upon spectroscopic analysis
were found to contain carbamazepine in the range
of 95.43 to 102.08 which complies with the
standard for uniformity of content laid down for
carbamazepine in official compendia.
3.3.6 In vitro Dispersion time:
In vitro dispersion time of all formulation
was found to be in range of 62.20 to 91.10 sec,
this was found to be well within acceptable range.
3.3.7 In vitro Dissolution study:
During in vitro dissolution study, it is found that
within 30 minutes drug release was found to be
62% to 83% from F1 to F9 formulation. The F5
formulation which contain 10% of the
croscarmellose sodium which shows 83.6% of
drug release. It was also observed that as the
concentration of the croscarmellose increases drug
release increases upto 10% and then get
decreased. In case of the sodium starch glycolate
concentration used were 2, 4 and 6%. From that
4% concentration of SSG shows 80.2% and other
shows less.
This may also attribute to croscarmellose
sodium and sodium starch glycolate. With
increase in concentration of this polymer capillary
action might have increased which in turn resulted
in reducing the time required for wetting and
disintegration of tablets and finally the dissolution
of drug.
57
12. Table 11. In vitro dissolution profile of formulationF1- F9.
Time
(min)
Cumulative drug release (%)
F1
F2
F3
F4
F5
F6
F7
F8
F9
0
0
0
0
0
0
0
0
0
0
5
10
15
20
25
30
20.3±1.5
24.7±2.5
32.5±2.1
40.1±1.2
51.2±1.2
62.7±2.0
24.0±1.5
29.5±0.7
35.7±1.0
47.5±1.8
59.4±2.8
66.5±2.5
27.2±2.4
33.5±1.4
39.3±2.4
49.2±2.4
62.4±0.7
70.2±1.4
38.0±1.2
41.1±3.2
46.5±2.2
57.1±1.6
65.6±2.3
78.5±2.7
40.2±2.3
47.3±2.2
52.0±1.5
59.7±0.4
69.4±1.4
83.6±2.3
29.2±1.1
34.9±0.9
41.5±1.4
50.8±1.8
65.9±1.4
71.2±2.0
29.2±1.1
34.9±0.9
40.3±0.7
51.3±1.2
61.3±2.0
70.2±1.1
39.5±1.8
40.0±2.5
48.8±1.2
57.8±0.4
67.8±2.0
80.2±0.6
25.4±1.6
31.4±0.8
38.4±1.4
54.9±1.3
59.3±3.3
70.7±1.3
90
Cumulative % drug release
80
70
F1
60
F2
F3
50
F4
40
F5
30
F6
20
F7
10
F8
0
0
5
10
15
20
25
30
35
F9
Time (min)
Figure 4. In vitro dissolution profile of formulationF1- F9.
Conclusion:
The oral fast dissolving tablet of carbamazepine
were formulated and evaluated for various
parameters from the compatibility studies by
DSC, FTIR and XRD of drug it was found to be
compatible with other formulation excipients. All
evaluation parameter were within specification.
The release of drug from the tablet was increased
as the concentration of superdisintegrants was
increased. The croscarmellose sodium shown
faster drug release than sodium starch glycolate.
Formulation F5 release maximum drug within the
30 mins.i.e.83.6% and shown minimum
disintegration time i.e. 57 sec than other
formulation and hence considered best
formulation.
It is concluded that fast dissolving tablets of
carbamazepine could be prepared by using
croscarmellose sodium and sodium starch
glycolate. In which croscarmellose sodium shows
good result as compared to the sodium starch
glycolate.
Acknowledgement:
We wish to thank Abbott healthcare Pvt.Ltd for
providing carbamazepine as a gift sample.
We also wish to thank Yashoda technical campus
Satara for providing instruments and facilities
required for research work.
58
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