This document summarizes a research study that formulated and evaluated a unidirectional bucco-adhesive tablet of sumatriptan succinate for the treatment of migraines. The tablet was designed to bypass first-pass hepatic metabolism by delivering the drug through the buccal mucosa. Various polymers including PEO WSR 301 and Carbopol 934p were evaluated as excipients. A 32 full factorial design was used to optimize the tablet formulation based on responses like mucoadhesive strength and drug release profile. Characterization of the optimized formulation showed it provided controlled drug release over 6 hours and had suitable mucoadhesive and swelling properties for buccal delivery.
Aim: This diploma thesis focused on the study of the influence of two types of high-shear
mixers as well as the effect of poly(meth)acrylate concentrations on the properties of
prepared granules and consequently matrix tablets.
Methods: Caffeine was employed as the model drug and matrix tablets were prepared via
the wet granulation process using two different high-shear mixers either Stephan UMC5 or
Rotolab mixer. Eudragit® NM 30D was used in various concentrations as a wet granulation
agent for time controlled drug release with low permeability and pH independent swelling.
In addition, lactose monohydrate was added as indifferent soluble filler, magnesium
stearate served as the antiadhesive excipient and colloidal silica was added for flowability
improvement. Matrix tablets were evaluated for mass, content and dosage uniformity,
uniformity of dosage units, friability, hardness and dissolution according to Ph. Eur.
Results - Conclusions: All prepared tablets exhibited sustained drug release. The
employment of different mixers for sustained matrix tablets preparation did not
significantly influence the release profile of caffeine (Eudragit® NM concentrations 9-
14%), except when the lower Eudragit® NM concentration (7%) was used for granulation.
Furthermore, Eudragit® NM concentrations (7 – 14% per tablet) did not significantly affect
the release profile of caffeine from matrix tablets, neither in the Stephan UMC5 nor the
Rotolab mixer.
Formulation and Evaluation of Mouth Dissolving Tablets in MirtazapineSriramNagarajan15
The present study was undertaken with an aim to development of formulation and evaluation of mouth dissolving tablets in mirtazapine. Mirtazapine, Gelatin, Cross Caramellose Sodium, Mannitol, aerosil, magnesium stearate, aspartame, mango flavor and microcrystalline cellulose were used for the preparation of tablets. The tablets were prepared by wet granulation method and evaluated for tablets thickness, weight variation, tablet hardness, friability, and in vitro drug release. Formulation F6 can be considered as an ideal or optimized formulation for mouth dissolving tablets of mirtazapine. It can be concluded that mouth dissolving tablet of mirtazapine. Can be successfully formulated and improving its bio availability.
Aim: This diploma thesis focused on the study of the influence of two types of high-shear
mixers as well as the effect of poly(meth)acrylate concentrations on the properties of
prepared granules and consequently matrix tablets.
Methods: Caffeine was employed as the model drug and matrix tablets were prepared via
the wet granulation process using two different high-shear mixers either Stephan UMC5 or
Rotolab mixer. Eudragit® NM 30D was used in various concentrations as a wet granulation
agent for time controlled drug release with low permeability and pH independent swelling.
In addition, lactose monohydrate was added as indifferent soluble filler, magnesium
stearate served as the antiadhesive excipient and colloidal silica was added for flowability
improvement. Matrix tablets were evaluated for mass, content and dosage uniformity,
uniformity of dosage units, friability, hardness and dissolution according to Ph. Eur.
Results - Conclusions: All prepared tablets exhibited sustained drug release. The
employment of different mixers for sustained matrix tablets preparation did not
significantly influence the release profile of caffeine (Eudragit® NM concentrations 9-
14%), except when the lower Eudragit® NM concentration (7%) was used for granulation.
Furthermore, Eudragit® NM concentrations (7 – 14% per tablet) did not significantly affect
the release profile of caffeine from matrix tablets, neither in the Stephan UMC5 nor the
Rotolab mixer.
Formulation and Evaluation of Mouth Dissolving Tablets in MirtazapineSriramNagarajan15
The present study was undertaken with an aim to development of formulation and evaluation of mouth dissolving tablets in mirtazapine. Mirtazapine, Gelatin, Cross Caramellose Sodium, Mannitol, aerosil, magnesium stearate, aspartame, mango flavor and microcrystalline cellulose were used for the preparation of tablets. The tablets were prepared by wet granulation method and evaluated for tablets thickness, weight variation, tablet hardness, friability, and in vitro drug release. Formulation F6 can be considered as an ideal or optimized formulation for mouth dissolving tablets of mirtazapine. It can be concluded that mouth dissolving tablet of mirtazapine. Can be successfully formulated and improving its bio availability.
Formulation and evaluation of oral biphasic drug delivery system of Metronida...inventionjournals
In the present study, a newly innovative drug delivery system of biphasic Metronidazole (MTZ) tablet has been studied. An attempt was made to improve the patient’s adherence and the potential clinical outcomes by reducing the dosing frequency by formulating bilayer tablets containing Metrodinazole. Each bilayer tablet is composed of a sustained release (SR) layer and an immediate release (IR) layer for rapid drug release. Five different formulations of bilayer tablets were formulated using HPMC as hydrophilic polymer to retarded the drug release and the effect of Starch and MCC on the release profile were evaluated. Wet granulation method was used to prepare granules of the immediate and sustained release layers. The tablets were evaluated for their physical parameters and all valuesobtained found to be within the acceptable limits. The dissolution test has been carried out using the USP type II rotating paddle. Collected samples were analyzed using the high performance liquid chromatography. The mechanisms of Metrodinazole release from the sustained release layer were fitted into zero-order, first order, Higuchi, Hixon- Crowell model and Korsmeyer-Peppas release model. The results of the dissolution profiles showed that the drug release from the sustained release layer varied depending on the amount of HPMC and the presence of Starch or MCC. The kinetics of the release of MTZ from the different formulations showed good fitting with Higuchi model with correlation coefficients (R2) of 0.9965 - 0.9985. From values obtained for the diffusional exponent, n, Korsmeyer-Peppas equation observed that for all the formulations n value ranged from 0.4662 to 0.5370, and this demonstrates that the release mechanism followed non-Fickian type of release ( anomalous transport).
Design and in vitro evaluation of bilayer tablets of Tramadol hydrochloride f...ijperSS
ABSTRACT
The aim of the present work was to design bilayer tablet of Tramadol hydrochloride for biphasic release and its in vitro evaluation. Bilayer tablets comprises of two layers, i.e., immediate release and sustained release layer. The immediate release layer comprised of various superdisintegrants and the sustained release layer comprised HPMC K4M, HPMC K15M, and HPMC K100M as the release retarding polymers. The bilayer tablets were prepared by direct compression method. The seven different formulations (F1-F7) were evaluated for pre- and post-compression parameters. In vitro dissolution studies were carried out for the optimized formulation (F6). It has found that the release of drug from the sustained release layer by 99.5% in 12 h. FT-IR studies revealed that there was no interaction between the drug and polymers used in the study. The release of Tramadol hydrochloride was found to follow a pattern of Korsmeyer-Peppas, with Quasi-Fickian diffusion. Accelerated stability studies were carried out on the prepared tablets in accordance with ICH guidelines. There were no changes observed in physicochemical properties and drug release pattern of tablets. Biphasic drug release pattern was successfully achieved through the formulation of bilayer tablets in this study.
Key words: Tramadol hydrochloride, bilayer tablet, direct compression, carmellose sodium, cross povidone, HPMC K4M.
Formulation and evaluation of sitagliptan floating tabletsSriramNagarajan19
Gastro retentive dosage form using Guar gum was prepared to develop floating tablets of Sitagliptin that could retain in the stomach for longer periods of time delivering the drug to the site of action, i.e., stomach. The pre-compression parameters of all formulations showed good flow properties and these can be used for tablet manufacture. The post-compression parameters of all formulations were determined and the values were found to be satisfactory. From the drug content and in-vitro dissolution studies of the formulations, it was concluded that the formulation F9 i.e. the formulation containing guargum, Sodium bicarbonate, citric acid, micro crystalline cellulose and Magnesium stearate is the best formulation. As a result of this study it may be concluded that the floating tablets using a guar gum in optimized concentration can be used to increase the GRT of the dissolution fluid in the stomach to deliver the drug in a sustained manner. The concept of formulating floating tablets of Sitagliptin offers a suitable and practical approach in serving desired objectives of gastro retentive floating tablets.
Development and evaluation of a novel twice daily cup core metformin hydrochl...SriramNagarajan19
The study was undertaken with an aim to formulate develop and evaluation of a novel twice daily core cup of Metformin hydrochloride(Antidiabetic drug) tablets using different grades and weight of HPMC polymers as release retarding agent. Granules were evaluated for tests Bulk density, tapped density, Hausner ratio before being punched as tablets. Tablets were tested for weight variation, thickness, hardness and friability as per official procedure. F-2 was found to be 73.90. From the above results and discussion it is concluded that formulation of Cup core tablet of containing Metformin hydrochloride HPMC K 4M & 215: 230 (in mg) can be taken as an ideal or optimized formulation of sustained release tablets for 12hour release as it fulfills all the requirements for sustained release tablet and our study encourages for the further clinical trials on this formulation. The core in cup tablets of Metformin hydrochloride were prepared by wet granulation method, they were evaluated for weight variation, friability, hardness, and thickness for all batches (F1 – F9). No significant difference was observed in the weight of individual tablets from the average weight. The weight variation tests were performed according to the procedure given in the pharmacopoeia. In a weight variation test, pharmacopoeial limit of tablet for percentage deviation is 5%. The average percentage deviation of all tablet formulation was found to be within the pharmacopoeial limit and hence all formulation passed the test for uniformity of weight.
In the present study an attempt will be made to design oral disintegrating tablets of Sumatriptan succinate (anti migraine) by using treated agar and Croscarmellose sodium as a superdisintigrants with a view to provide a convenient means of administration to those patients suffering from difficulties in swallowing such as pediatric and geriatric patients and uncooperative mentally ill patients.
Formulation and evaluation of oral biphasic drug delivery system of Metronida...inventionjournals
In the present study, a newly innovative drug delivery system of biphasic Metronidazole (MTZ) tablet has been studied. An attempt was made to improve the patient’s adherence and the potential clinical outcomes by reducing the dosing frequency by formulating bilayer tablets containing Metrodinazole. Each bilayer tablet is composed of a sustained release (SR) layer and an immediate release (IR) layer for rapid drug release. Five different formulations of bilayer tablets were formulated using HPMC as hydrophilic polymer to retarded the drug release and the effect of Starch and MCC on the release profile were evaluated. Wet granulation method was used to prepare granules of the immediate and sustained release layers. The tablets were evaluated for their physical parameters and all valuesobtained found to be within the acceptable limits. The dissolution test has been carried out using the USP type II rotating paddle. Collected samples were analyzed using the high performance liquid chromatography. The mechanisms of Metrodinazole release from the sustained release layer were fitted into zero-order, first order, Higuchi, Hixon- Crowell model and Korsmeyer-Peppas release model. The results of the dissolution profiles showed that the drug release from the sustained release layer varied depending on the amount of HPMC and the presence of Starch or MCC. The kinetics of the release of MTZ from the different formulations showed good fitting with Higuchi model with correlation coefficients (R2) of 0.9965 - 0.9985. From values obtained for the diffusional exponent, n, Korsmeyer-Peppas equation observed that for all the formulations n value ranged from 0.4662 to 0.5370, and this demonstrates that the release mechanism followed non-Fickian type of release ( anomalous transport).
Design and in vitro evaluation of bilayer tablets of Tramadol hydrochloride f...ijperSS
ABSTRACT
The aim of the present work was to design bilayer tablet of Tramadol hydrochloride for biphasic release and its in vitro evaluation. Bilayer tablets comprises of two layers, i.e., immediate release and sustained release layer. The immediate release layer comprised of various superdisintegrants and the sustained release layer comprised HPMC K4M, HPMC K15M, and HPMC K100M as the release retarding polymers. The bilayer tablets were prepared by direct compression method. The seven different formulations (F1-F7) were evaluated for pre- and post-compression parameters. In vitro dissolution studies were carried out for the optimized formulation (F6). It has found that the release of drug from the sustained release layer by 99.5% in 12 h. FT-IR studies revealed that there was no interaction between the drug and polymers used in the study. The release of Tramadol hydrochloride was found to follow a pattern of Korsmeyer-Peppas, with Quasi-Fickian diffusion. Accelerated stability studies were carried out on the prepared tablets in accordance with ICH guidelines. There were no changes observed in physicochemical properties and drug release pattern of tablets. Biphasic drug release pattern was successfully achieved through the formulation of bilayer tablets in this study.
Key words: Tramadol hydrochloride, bilayer tablet, direct compression, carmellose sodium, cross povidone, HPMC K4M.
Formulation and evaluation of sitagliptan floating tabletsSriramNagarajan19
Gastro retentive dosage form using Guar gum was prepared to develop floating tablets of Sitagliptin that could retain in the stomach for longer periods of time delivering the drug to the site of action, i.e., stomach. The pre-compression parameters of all formulations showed good flow properties and these can be used for tablet manufacture. The post-compression parameters of all formulations were determined and the values were found to be satisfactory. From the drug content and in-vitro dissolution studies of the formulations, it was concluded that the formulation F9 i.e. the formulation containing guargum, Sodium bicarbonate, citric acid, micro crystalline cellulose and Magnesium stearate is the best formulation. As a result of this study it may be concluded that the floating tablets using a guar gum in optimized concentration can be used to increase the GRT of the dissolution fluid in the stomach to deliver the drug in a sustained manner. The concept of formulating floating tablets of Sitagliptin offers a suitable and practical approach in serving desired objectives of gastro retentive floating tablets.
Development and evaluation of a novel twice daily cup core metformin hydrochl...SriramNagarajan19
The study was undertaken with an aim to formulate develop and evaluation of a novel twice daily core cup of Metformin hydrochloride(Antidiabetic drug) tablets using different grades and weight of HPMC polymers as release retarding agent. Granules were evaluated for tests Bulk density, tapped density, Hausner ratio before being punched as tablets. Tablets were tested for weight variation, thickness, hardness and friability as per official procedure. F-2 was found to be 73.90. From the above results and discussion it is concluded that formulation of Cup core tablet of containing Metformin hydrochloride HPMC K 4M & 215: 230 (in mg) can be taken as an ideal or optimized formulation of sustained release tablets for 12hour release as it fulfills all the requirements for sustained release tablet and our study encourages for the further clinical trials on this formulation. The core in cup tablets of Metformin hydrochloride were prepared by wet granulation method, they were evaluated for weight variation, friability, hardness, and thickness for all batches (F1 – F9). No significant difference was observed in the weight of individual tablets from the average weight. The weight variation tests were performed according to the procedure given in the pharmacopoeia. In a weight variation test, pharmacopoeial limit of tablet for percentage deviation is 5%. The average percentage deviation of all tablet formulation was found to be within the pharmacopoeial limit and hence all formulation passed the test for uniformity of weight.
In the present study an attempt will be made to design oral disintegrating tablets of Sumatriptan succinate (anti migraine) by using treated agar and Croscarmellose sodium as a superdisintigrants with a view to provide a convenient means of administration to those patients suffering from difficulties in swallowing such as pediatric and geriatric patients and uncooperative mentally ill patients.
Formulation and evaluation of omeprazole floating tabletsmedicinefda
formulation and evaluation of omeprazole floating tablets, literature review and plan of work ,methods results and discussion,conclusion sample ppt http://www.medicinefda.com/
ABSTRACT
Overactive bladder (OAB) is a prevalent condition which has an adverse effect on quality of life. The presence
of urgency incontinence confers significant morbidity above and beyond that of OAB sufferers who are
continent. The primary treatment for OAB and urgency incontinence is a combination of behavioral measures
and antimuscarinic drug therapy. The ideal antimuscarinic agent should effectively relieve the symptoms of
OAB, with the minimum of side effects; it should be available as a once-daily sustained release formulation
and in dosage strength that allows easy dose titration for the majority of sufferers. Solifenacin succinate was
launched in 2005 and has been shown in both short and long term clinical trials to fulfill these requirements.
Solifenacin is a competitive M3 receptor antagonist with a long half-life (45-68 hours). It is available in two
dosage strengths namely a 5 or 10 mg once-daily tablet. The efficacy and tolerability of solifenacin for the
treatment of all symptoms of OAB has been evaluated in a number of large, placebo controlled, randomized
trials. Long-term safety, efficacy, tolerability and persistence with treatment have been established in an open
label 40 week continuation study.
KEYWORDS
Solifenacin, Urinary incontinence, Overactive bladder and Wet granulation method.
ABSTRACT
Hyperglycemia is the technical term for high blood glucose (sugar). It
happens when the body has too little or not enough insulin or when the
body can‘t use insulin properly. The main objective of the present
research work was to develop a bilayer tablet of immediate release
Pioglitazone and controlled release Metformin Hydrochloride, which is
used as an Anti-hyperglycemic agent. Metformin Hydrochloride has
biological half-life nearly about 6 hours, so, an attempt was made in
the direction of preparation and optimization of a combination of
sustained release and immediate release in a single tablet. In controlled
release layer natural gums like xanthum gum, gum trgacanth and guar
gum were used as retarding materials and in immediate release laye
croscarmellose sodium was used as a superdisintegrent to give the faster release of
pioglitazone. The tablets were prepared by wet granulation method and by direct
compression. Granules were evaluated for precompression parameters and the tablets were
evaluated for post compression parameters.
Key Words: Bilayer tablets, Metformin Hydrochloride, pioglitazone, xanthum gum, guar
gum, gum tragacanth and crosscarmellose sodium.
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.
- Video recording of this lecture in English language: https://youtu.be/kqbnxVAZs-0
- Video recording of this lecture in Arabic language: https://youtu.be/SINlygW1Mpc
- Link to download the book free: https://nephrotube.blogspot.com/p/nephrotube-nephrology-books.html
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Muktapishti is a traditional Ayurvedic preparation made from Shoditha Mukta (Purified Pearl), is believed to help regulate thyroid function and reduce symptoms of hyperthyroidism due to its cooling and balancing properties. Clinical evidence on its efficacy remains limited, necessitating further research to validate its therapeutic benefits.
Rasamanikya is a excellent preparation in the field of Rasashastra, it is used in various Kushtha Roga, Shwasa, Vicharchika, Bhagandara, Vatarakta, and Phiranga Roga. In this article Preparation& Comparative analytical profile for both Formulationon i.e Rasamanikya prepared by Kushmanda swarasa & Churnodhaka Shodita Haratala. The study aims to provide insights into the comparative efficacy and analytical aspects of these formulations for enhanced therapeutic outcomes.
Title: Sense of Taste
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the structure and function of taste buds.
Describe the relationship between the taste threshold and taste index of common substances.
Explain the chemical basis and signal transduction of taste perception for each type of primary taste sensation.
Recognize different abnormalities of taste perception and their causes.
Key Topics:
Significance of Taste Sensation:
Differentiation between pleasant and harmful food
Influence on behavior
Selection of food based on metabolic needs
Receptors of Taste:
Taste buds on the tongue
Influence of sense of smell, texture of food, and pain stimulation (e.g., by pepper)
Primary and Secondary Taste Sensations:
Primary taste sensations: Sweet, Sour, Salty, Bitter, Umami
Chemical basis and signal transduction mechanisms for each taste
Taste Threshold and Index:
Taste threshold values for Sweet (sucrose), Salty (NaCl), Sour (HCl), and Bitter (Quinine)
Taste index relationship: Inversely proportional to taste threshold
Taste Blindness:
Inability to taste certain substances, particularly thiourea compounds
Example: Phenylthiocarbamide
Structure and Function of Taste Buds:
Composition: Epithelial cells, Sustentacular/Supporting cells, Taste cells, Basal cells
Features: Taste pores, Taste hairs/microvilli, and Taste nerve fibers
Location of Taste Buds:
Found in papillae of the tongue (Fungiform, Circumvallate, Foliate)
Also present on the palate, tonsillar pillars, epiglottis, and proximal esophagus
Mechanism of Taste Stimulation:
Interaction of taste substances with receptors on microvilli
Signal transduction pathways for Umami, Sweet, Bitter, Sour, and Salty tastes
Taste Sensitivity and Adaptation:
Decrease in sensitivity with age
Rapid adaptation of taste sensation
Role of Saliva in Taste:
Dissolution of tastants to reach receptors
Washing away the stimulus
Taste Preferences and Aversions:
Mechanisms behind taste preference and aversion
Influence of receptors and neural pathways
Impact of Sensory Nerve Damage:
Degeneration of taste buds if the sensory nerve fiber is cut
Abnormalities of Taste Detection:
Conditions: Ageusia, Hypogeusia, Dysgeusia (parageusia)
Causes: Nerve damage, neurological disorders, infections, poor oral hygiene, adverse drug effects, deficiencies, aging, tobacco use, altered neurotransmitter levels
Neurotransmitters and Taste Threshold:
Effects of serotonin (5-HT) and norepinephrine (NE) on taste sensitivity
Supertasters:
25% of the population with heightened sensitivity to taste, especially bitterness
Increased number of fungiform papillae
263778731218 Abortion Clinic /Pills In Harare ,sisternakatoto
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micro teaching on communication m.sc nursing.pdfAnurag Sharma
Microteaching is a unique model of practice teaching. It is a viable instrument for the. desired change in the teaching behavior or the behavior potential which, in specified types of real. classroom situations, tends to facilitate the achievement of specified types of objectives.
Title: Sense of Smell
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the primary categories of smells and the concept of odor blindness.
Explain the structure and location of the olfactory membrane and mucosa, including the types and roles of cells involved in olfaction.
Describe the pathway and mechanisms of olfactory signal transmission from the olfactory receptors to the brain.
Illustrate the biochemical cascade triggered by odorant binding to olfactory receptors, including the role of G-proteins and second messengers in generating an action potential.
Identify different types of olfactory disorders such as anosmia, hyposmia, hyperosmia, and dysosmia, including their potential causes.
Key Topics:
Olfactory Genes:
3% of the human genome accounts for olfactory genes.
400 genes for odorant receptors.
Olfactory Membrane:
Located in the superior part of the nasal cavity.
Medially: Folds downward along the superior septum.
Laterally: Folds over the superior turbinate and upper surface of the middle turbinate.
Total surface area: 5-10 square centimeters.
Olfactory Mucosa:
Olfactory Cells: Bipolar nerve cells derived from the CNS (100 million), with 4-25 olfactory cilia per cell.
Sustentacular Cells: Produce mucus and maintain ionic and molecular environment.
Basal Cells: Replace worn-out olfactory cells with an average lifespan of 1-2 months.
Bowman’s Gland: Secretes mucus.
Stimulation of Olfactory Cells:
Odorant dissolves in mucus and attaches to receptors on olfactory cilia.
Involves a cascade effect through G-proteins and second messengers, leading to depolarization and action potential generation in the olfactory nerve.
Quality of a Good Odorant:
Small (3-20 Carbon atoms), volatile, water-soluble, and lipid-soluble.
Facilitated by odorant-binding proteins in mucus.
Membrane Potential and Action Potential:
Resting membrane potential: -55mV.
Action potential frequency in the olfactory nerve increases with odorant strength.
Adaptation Towards the Sense of Smell:
Rapid adaptation within the first second, with further slow adaptation.
Psychological adaptation greater than receptor adaptation, involving feedback inhibition from the central nervous system.
Primary Sensations of Smell:
Camphoraceous, Musky, Floral, Pepperminty, Ethereal, Pungent, Putrid.
Odor Detection Threshold:
Examples: Hydrogen sulfide (0.0005 ppm), Methyl-mercaptan (0.002 ppm).
Some toxic substances are odorless at lethal concentrations.
Characteristics of Smell:
Odor blindness for single substances due to lack of appropriate receptor protein.
Behavioral and emotional influences of smell.
Transmission of Olfactory Signals:
From olfactory cells to glomeruli in the olfactory bulb, involving lateral inhibition.
Primitive, less old, and new olfactory systems with different path
Tom Selleck Health: A Comprehensive Look at the Iconic Actor’s Wellness Journeygreendigital
Tom Selleck, an enduring figure in Hollywood. has captivated audiences for decades with his rugged charm, iconic moustache. and memorable roles in television and film. From his breakout role as Thomas Magnum in Magnum P.I. to his current portrayal of Frank Reagan in Blue Bloods. Selleck's career has spanned over 50 years. But beyond his professional achievements. fans have often been curious about Tom Selleck Health. especially as he has aged in the public eye.
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Introduction
Many have been interested in Tom Selleck health. not only because of his enduring presence on screen but also because of the challenges. and lifestyle choices he has faced and made over the years. This article delves into the various aspects of Tom Selleck health. exploring his fitness regimen, diet, mental health. and the challenges he has encountered as he ages. We'll look at how he maintains his well-being. the health issues he has faced, and his approach to ageing .
Early Life and Career
Childhood and Athletic Beginnings
Tom Selleck was born on January 29, 1945, in Detroit, Michigan, and grew up in Sherman Oaks, California. From an early age, he was involved in sports, particularly basketball. which played a significant role in his physical development. His athletic pursuits continued into college. where he attended the University of Southern California (USC) on a basketball scholarship. This early involvement in sports laid a strong foundation for his physical health and disciplined lifestyle.
Transition to Acting
Selleck's transition from an athlete to an actor came with its physical demands. His first significant role in "Magnum P.I." required him to perform various stunts and maintain a fit appearance. This role, which he played from 1980 to 1988. necessitated a rigorous fitness routine to meet the show's demands. setting the stage for his long-term commitment to health and wellness.
Fitness Regimen
Workout Routine
Tom Selleck health and fitness regimen has evolved. adapting to his changing roles and age. During his "Magnum, P.I." days. Selleck's workouts were intense and focused on building and maintaining muscle mass. His routine included weightlifting, cardiovascular exercises. and specific training for the stunts he performed on the show.
Selleck adjusted his fitness routine as he aged to suit his body's needs. Today, his workouts focus on maintaining flexibility, strength, and cardiovascular health. He incorporates low-impact exercises such as swimming, walking, and light weightlifting. This balanced approach helps him stay fit without putting undue strain on his joints and muscles.
Importance of Flexibility and Mobility
In recent years, Selleck has emphasized the importance of flexibility and mobility in his fitness regimen. Understanding the natural decline in muscle mass and joint flexibility with age. he includes stretching and yoga in his routine. These practices help prevent injuries, improve posture, and maintain mobilit
2. Austin J Anal Pharm Chem 3(2): id1063 (2016) - Page - 02
Champaneri AM Austin Publishing Group
Submit your Manuscript | www.austinpublishinggroup.com
sumatriptan succinate with the following objectives to avoid hepatic
first pass metabolism, to reduce the frequency of administration,
overcome the side effects, simplify the treatment regimen, and to
obtain greater therapeutic efficacy to improve patient compliance.
Material and Method
Material
Sumatriptan succinate raw material was received as gift sample
from Sun Pharmaceutical Limited, Ahmedabad, PEO WSR 301 from
Lubrizol, Carbopol 934 p from ACS chemical, Ahmedabad, Lactose
Monohydrate from Loba chemicals, Thane, Ethyl Cellulose from
Loba chemicals, Mumbai, Magnesium Stearate from ASES, Jodhpur
and Talc from Vikas pharma, Mumbai.
Method
Method of core tablet: The Sumatriptan succinate unidirection
Bucco-adhesive tablet were prepared by direct compression method,
the composition of various formulation was mentioned in Table 1 [3].
All the ingredient was individually passed through sieve no 60. The
required quantities of mucoadhesive polymer were mix properly with
other excipients. Prepared the core tablet in the tablet compression
machine mini press-I (Karnavati, Ahmedabad). After prepared core
tablet then using ethyl cellulose (backing layer) for the unidirectional
design. Composition of the mucoadhesive tablet was optimized
using 32
full factorial design where amount of PEO WSR 301 (X1)
and amount of Carbopol 934p (X2) were taken as independent
variables and mucoadhesive strength, Drug release at 6 hour and
% swelling index taken as response variables. The formulations of
design batches were characterized for post compression parameters
like weight variation, hardness, thickness, friability, Drug content,
swelling index, ex-vivo Mucoadhesive strength, surface pH, drug
release at 6hr., ex-vivo residence time, and curve fitting analysis. The
optimized formulation was obtained using Minitab software based
on desirability value. Characterization of optimized batch was carried
out by, ex-vivo permeation study.
Method of core-in-cup tablet: Total weight of the core tablet
was 80mg, prepared by direct compression in 8 mm punch (excipient
same as shown above). Resulted round shape flat core tablet is
recompressed in 10mm round shape flat punch after adding ethyl
cellulose (70mg) mixture at free three side around the tablet.
Identification of drug
Melting point method: Melting point of drug was determined by
Capillary Method. Fine powder of Sumatriptan succinate was filled in
glass capillary tube (previously sealed at one end), tube was placed in
melting point apparatus and the temperature at which powder melted
was noted.
IR Spectroscopy: FTIR studies were carried out to identify the
drug [4]. Fourier Transform Infrared Spectroscopy studies were
carried out by sample with dried potassium bromide and acquiring
IR spectrum in the range of 400-4000 cm-1
. The FT-IR spectrum of the
obtained sample of the drug was compared with the standard FT-IR
spectra of the pure drug.
Batch No. Bulk density (g/cm3
)
Tapped density
(g/cm3
)
Carr’s index (%) Hausner’s ratio Angle of repose
Corebland
D1 0.28±0.010 0.32±0.002 12.5±1.15 1.14±0.020 26.33±0.12
D2 0.28±0.021 0.31±0.04 9.67±1.25 1.11±0.03 24.44±0.19
D3 0.28±0.010 0.320.055 9.81±1.21 1.14±0.010 22.68±0.21
D4 0.29±0.010 0.34±0.001 14.7±1.05 1.17±0.010 23.25±0.34
D5 0.28±0.015 0.33±0.005 15.1±1.24 1.18±0.014 26.78±0.41
D6 0.3±0.015 0.34±0.001 11.7±1.35 1.13±0.005 27.63±0.38
D7 0.3±0.023 0.33±0.002 9.09±1.12 1.10±0.01 25.55±0.26
D8 0.28±0.010 0.33±0.003 15.1±1.18 1.18±0.030 26.46±0.14
D9 0.27±0.006 0.31±0.051 12.90±1.20 1.15±0.035 23.88±0.35
Table 2: Composition of tablet for Factorial design batches (“Core-in-Cup”).
Ingredients (mg) D1 D2 D3 D4 D5 D6 D7 D8 D9
Sumatriptan succinate 10 10 10 10 10 10 10 10 10
PEO WSR 301 10 20 30 10 20 30 10 20 30
CP 934p 2.5 2.5 2.5 5 5 5 7.5 7.5 7.5
Lactose 32.5 22.5 12.5 30 20 10 27.5 17.5 7.5
Ethyl cellulose 10 10 10 10 10 10 10 10 10
PEG 4000 10 10 10 10 10 10 10 10 10
Mg stearate 2.5 2.5 2.5 2.5 2.5 2.5 2.5 2.5 2.5
Talc 2.5 2.5 2.5 2.5 2.5 2.5 2.5 2.5 2.5
Total 80 80 80 80 80 80 80 80 80
Ethyl cellulose (Backing layer) 70 70 70 70 70 70 70 70 70
Total 150 150 150 150 150 150 150 150 150
Table 1: Composition table of formulations.
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DSC Study: Thermal behavior of drug was examined using
thermal analyzer [4]. All accurately weighed samples (about 1mg)
were placed in sealed aluminum pans before heating under nitrogen
flow (20mL/min) at a scanning rate of 10 °C min-1
from 50 to 300 °C.
An empty aluminum pan was used as reference.
Compatibility studies
FTIR spectroscopy: Compatibility must be established between
the active ingredients and other excipients to produce a stable,
efficacious, attractive and safe product. FTIR spectra of Sumatriptan
succinate with different polymers and other excipients were recorded
between 400 to 4000 cm–1
using FTIR spectrometer (Shimadzu).
Evaluation parameter
Pre Compression parameter of core powder blend
Bulk density: A bulk density is defined as the mass of powder
divided by the volume [5,6,7]. A bulk density largely depends on the
particle shape, as particles becomes more spherical in shape, bulk
density is increase. In addition as granules size increase, bulk density
decrease. Powder weighing 10 g was placed into 100 ml measuring
cylinder. Volume occupied by the powder was noted without
disturbing the cylinder and bulk density was calculated in gm/ml by
the following equation.
Bulk density = Weight of powder / Bulk volume
Tapped density: Tapped density was achieved by mechanically
tapping a measuring cylinder containing 20 tablet powders. After
observing the initial volume, the cylinder was mechanically tapped
and volume reading was taken until further volume changes were
observed. The mechanical tapping was achieved by raising the cylinder
and allowing it to drop under own weight a specific distance. Device
that rotates the cylinder during tapping may be preferred to minimize
any possible separation of the mass during tapping down. Cylinder
dropping distance: 14 ± 2 mm at a normal rate of 300 drops /min. The
final volume was recorded and the tap density was calculated by the
following equation.
Tapped Density = Weight of powder / Tapped volume
Hausner’sratio:The Hausner’s ratio is a number that is correlated
to the flow ability of a powder or granular material.
Hausner’s Ratio = Tapped Density/Bulk density
Compressibility index (Carr’s index) [7]: Compressibility index
of the drug was determined using the following formula
Carr’s Index (%) = [(Tapped Density-Bulk Density) x100]/
Tapped Density
Angle of repose: Angle of repose was determined by measuring
the height, radius of the heap of the powder blend. A cut system
funnel was fixed to a stand and bottom of the funnel was fixed at a
height of 2cm from the plane. Powder blend was placed in funnel and
allowed to flow freely and measured the height and radius of the heap.
tanθ=h/r
Where, h = height of heap
r = radius of heap
Post compression parameters of core tablet
Thickness: The thickness of buccal tablet was determined using
digital micrometer screw gauge. Ten individual tablets from each
batch were used and the average thickness was calculated.
Hardness: Hardness test was done for five tablets from each batch
using hardness tester and average values was calculated. The hardness
was measured in terms of kg/cm2
.
Friability test: Friability is the measure of tablet strength. Roche
type friabilator was used for testing the friability using the following
procedure. Twenty tablets were weighed accurately and placed in
the tumbling apparatus that revolves at 25rpm dropping the tablets
through a distance of six inches with each revolution. After 4min, the
tablets were weighed and the percentage loss was determined.
% Friability loss = [Initial weight − Final weight/Initial weight]
X 100
Weight variation test: The USP-XXIX weight variation test was
carried out by weighing 20 tablets individually, calculating the average
weight, comparing the individual tablet weight to average weight. The
tablet meet USP-XXIX test if no tablet differs by more than two times
of percentage deviation USP-XXIX Standards for Weight Variation
Test.
Content uniformity: Ten tablets from each batch was taken,
crushed and mixed. From the mixture 5mg of drug equivalent of
mixture was extracted thoroughly with 100mL of pH 6.8 phosphate
buffer. The amount of drug present in each extract was determined
using UV spectrophotometer at 271 nm. This procedure was repeated
Figure 1: Assembly for mucoadhesion strength study.
Figure 2: Assembly for In-vitro drug release studies.
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thrice and this average was calculated.
Ex-vivo mucoadhesion studies: The ex-vivo mucoadhesive
strength was performed after application of the buccal tablet on
freshly cut goat buccal mucosa. The fresh goat buccal mucosa was
tied on the glass slide, and a mucoadhesive core side of each tablet was
wetted with phosphate buffer pH 6.8 and adhered to the sheep buccal
mucosa by applying a light force with a fingertip for 30 seconds. The
modified physical balance was adjusted by keeping glass beaker on
another side. Water was added by burette and weight of water needed
to detach the tablet from goat buccal mucosa was recorded for the
measure of mucoadhesive strength in grams [8,9] (Figure 1).
Force of adhesion (N) = [Mucoadhesive strength] / 1000 X 9.81
In-vitro drug release studies [10,11]: The dissolution test was
carried out using USP dissolution testing apparatus II. The test was
performed at a paddle speed of 50rpm using 500ml of phosphate
buffer, pH 6.8, as the dissolution medium at 37±0.50°C. The tablet was
stuck on the paddle from the side of backing layer using cyanoacrylate
adhesive to mimic unidirectional drug release. An aliquot of 10ml of
the sample solution was withdrawn at the interval of 15, 30, 60, 120,
180, 240, 300, 360 min and the absorbance was measured at identical
wavelength [12-14] (Figure 2).
In vitro swelling rate: After weighing the tablet (W1), it was
immersed in pH 6.8 phosphate buffer solution maintained at 37°C.
The weight at the end of 360 min was reported (W2). The swelling
index was determined from the formula:
% Swelling Index = [(W2-W1)/ W1] ×100
Where, W1 = initial weight
W2= final weight
Ex-vivo permeation studies [15,16]: Diffusion studies were
carried out to evaluate the permeability of drug across the porcine
buccal mucosal membrane using glass surface franz diffusion cell.
Porcine buccal mucosa was obtained from a local slaughter house
and was used within 2h of slaughter. The tissue was stored in 0.2
molar phosphate buffer (PBS), pH 7.4, solution upon collection.
The epithelium was separated from underlying connective tissues
with surgical scissors and clamped in between donor and receiver
chambers of the diffusion cells for permeation studies. Receptor
compartment contained 21ml of pH 7.4 phosphate buffer, while
donor compartment was filled with 3 ml simulated saliva of pH 6.8.
The tablet was placed on the mucosal surface in donor compartment,
and 2ml aliquots was removed at suitable intervals from the receptor
compartment while the solution is being stirred continuously using
magnetic stirrer, replacing it with fresh 2ml medium each time. The
experiment was carried out at 37±1°C (Figure 3).
Ex-vivo residence time [17,18]: The tablet was applied on
the porcine buccal mucosa which was fixed on the glass slide with
cyanoacrylate glue. The slide was tied to the disintegration apparatus
and suspended in the beaker filled with 800 ml simulated saliva, pH
Figure 3: Assembly for ex-vivo permeability study.
Figure 4: FTIR spectra of Sumatriptan succinate.
Figure 5: DSC thermogram of Sumatriptan succinate.
Figure 6: Comparision of FTIR study of drug and drug + polymer mixture.
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6.8. The slide was allowed to reciprocate in the medium until the tablet
got detached or eroded from the mucosa. The test was performed in
triplicate. Time for the detachment of the tablet was recorded as ex-
vivo residence time.
Short-term stability study: Stability studies were carried out for
Sumatriptan Succinate formulation as per ICH guidelines. The best
unidirection Bucco-adhesive tablet (D6) was sealed in high density
polyethylene bottles and stored at 4±1 °C/Ambient, 25±2 °C/60±5 %
RH %, 40±2 °C/75±5 % RH for 90d. The samples were periodically
evaluated for entrapment efficiency and percentage mucoadhesion
[19-23].
Results and Discussion
Melting point
The observed melting point was found to be 169-171 0
C. This
melting point resembles to melting point given in article.
FTIR Spectra of Ivabradine hydrochloride
IR spectra of drug are shown in following Figure 4. The peaks
obtained in the spectra of drug correlates with functional groups of
Sumatriptan Succinate which confirms the purity of drug.
DSC study
From the observation of thermogram of pure drug, the melting
point of the sample was found at 168.30 0
C that is nearly same with
documented melting point (167-168 0
C) proving the identity and
purity of drug (Figure 5).
Compatibility studies
Physicochemical property of “Core-in-Cup” tablet.: The
prepared tablets were smooth and white in color. Weight variation in
case of all tablets was acceptable. The weight variation in case of all the
tablets was within ±7.5% of theoretical tablet weight. This falls well
within the acceptance criteria. Friability in case of all the designed
tablets was less than 1% w/w indicating suitability of the method used
for manufacturing the tablets. The prepared tablets showed maximum
thickness of 1.65 mm. Hardness value of all the formulation was in
the range of 5-5.5 Kg/cm2
(Figure 6).
Batch no.
Hardness
(kg/cm2
)
Thickness
(mm)
Weight
variation
(mg)
Friability
(%)
Drug
Content (%)
D1 5.3±0.286 1.64±0.110 152.5±1.71 0.20±0.03 97.11±0.14
D2 5.2±0.350 1.65±0.110 150.7±1.32 0.24±0.07 98.29±0.29
D3 5.35±0.521 1.64±0.109 151.3±1.23 0.23±0.05 97.23±.51
D4 5.3±0.230 1.62±0.123 153.0±1.21 0.25±0.06 98.21±0.25
D5 5.3±0.249 1.67±0.135 150.1±1.19 0.22±0.02 98.99±0.27
D6 5.3±0.520 1.63±0.125 152.1±1.16 0.26±0.05 98.42±0.31
D7 5.3±0.430 1.64±0.130 150.7±1.78 0.24±0.02 98.20±0.77
D8 5.3±0.470 1.64±0.118 152.3±1.31 0.23±0.08 96.89±0.45
D9 5.2±0.286 1.67±0.150 151.0±1.52 0.23±0.06 98.18±0.18
Table 3: Physicochemical property of “Core-in-Cup” tablet (D1-D9).
0.2
0.25
0.3
0.35
0.4
0.45
0.5
0.55
0.6
D1 D2 D3 D4 D5 D6 D7 D8 D9
Mucoadhesive strength (N)
Figure 7: Comparision of Ex Vivo mucoadhesive strength of factorial batches.
Formulation code
Mucoadhesive strength (N)
Mean ±SD
D1 0.251±0.0025
D2 0.274±0.0026
D3 0.289±0.0015
D4 0.326±0.0015
D5 0.350±0.0050
D6 0.454±0.0030
D7 0.447±0.0021
D8 0.490±0.0020
D9 0.545±0.0042
Table 4: Comparision of Ex Vivo mucoadhesive strength of factorial batches.
Formulation code Percentage Swelling index at 6 hrs Mean ±SD
D1 43.50±1.10
D2 46.23±0.64
D3 49.17±0.58
D4 45.37±0.96
D5 47.27±0.97
D6 51.73±1.19
D7 49.50±1.35
D8 49.23±0.96
D9 53.73±0.35
Table 5: Comparision of Percentage Swelling index of factorial batches.
40
42
44
46
48
50
52
54
56
D1 D2 D3 D4 D5 D6 D7 D8 D9
% Swelling at 6hr.
Figure 8: Comparision of Percentage Swelling index of factorial batches.
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To evaluate a tablet‘s potential for efficacy the amount of drug
in the tablet need to be monitored from tablet to tablet and batch to
batch. The mean drug content was found to be in between range of
96.89% to 98.99% (Table 1, 2 & 3).
Ex Vivo mucoadhesive strength
Force of adhesion (N) = Mucoadhesive strength / 1000 × 9.81
Mucoadhesive strength is an important parameter of the
mucoadhesive buccal tablet. It shows the capability of the dosage
form for adhering to the buccal mucosa. When the concentration of
polymer is low, the number of penetrating polymeric chains per unit
volume of the mucous is low resulting in weaker interaction. Increase
in adhesion with increase the concentration of polymer used can be
attributed to higher strength of gel formed by PEO WSR 301 resulting
in stronger entanglement of polymeric chains with glycoprotein
chains of mucous. Mucoadhesive strength was found to be increased
Formulation code Surface Ph Mean ±SD
D1 6.2
D2 6.3
D3 6.8
D4 6.4
D5 6.8
D6 6.8
D7 6.7
D8 6.8
D9 6.7
Table 6: Comparision of Surface pH study of factorial batches.
5.8
6
6.2
6.4
6.6
6.8
7
D1 D2 D3 D4 D5 D6 D7 D8 D9
Surface pH
Figure 9: Comparision of Surface pH study of factorial batches.
Formulation code Residence time (hour) Mean ±SD
D1 6.03±1.10
D2 6.12±0.66
D3 6.18±0.54
D4 6.10±0.87
D5 6.21±0.85
D6 6.24±1.20
D7 6.17±1.25
D8 6.28±0.83
D9 6.25±0.41
Table 7: Comparision of Ex-vivo Residence time of factorial batches.
as PEO WSR 301 concentration increases (Figure 7, Table 4).
Percentage swelling index:
% Swelling Index = [(W2-W1)/ W1] ×100
Where, W1 = initial weight
W2= final weight
Buccal tablets were weighed individually (designated as W1) and
placed separately in Petri dishes containing 15mL of phosphate buffer
(pH 6.8) solution. At regular intervals (1, 2, 3, 4, 5 and 6 hr) the buccal
tablets were removed from the Petri dishes and excess surface water
was removed carefully using the filter paper. The swollen tablets were
then reweighed (W2) (Figure 8, Table 5).
Surface pH study
The maximum and minimum pH values of the formulations were
found to be 6.8 and 6.2 respectively. The acceptable pH of saliva is
in the range of 5-7 and the surface pH of all tablets is within limits.
Hence, the formulations may not produce any irritation to the buccal
mucosa (Figure 9, Table 6).
Ex-vivo residence time
The Ex vivo residence time is one of the important physical
parameter of buccal mucoadhesive tablets. The Ex vivo residence time
time (min)
% CPR of Experimental Batches
D1 D2 D3 D4 D5 D6 D7 D8 D9
0 0 0 0 0 0 0 0 0 0
15 11.23 10.15 9.42 9.9 8.85 9.96 11.35 10.49 10.92
30 14.77 16.71 19.92 14.73 14.53 15.02 14.74 19.61 20.05
60 24.61 32.40 33.32 23.12 24.56 24.53 22.85 30.65 30.90
120 39.02 40.01 43.58 31.31 39.07 43.14 32.48 41.76 43.50
180 48.01 50.79 56.47 44.97 52.35 51.44 47.26 51.54 58.56
240 60.78 66.71 60.01 65.01 69.74 71.24 66.02 69.40 71.43
300 71.74 70.32 65.24 76.50 78.14 82.78 76.07 81.65 84.18
360 74.13 72.15 70.35 86.16 91.92 94.44 93.20 92.33 88.15
Table 8: In-vitro drug release profile of experimental batches.
0
10
20
30
40
50
60
70
80
90
100
0 100 200 300 400
%
C
P
R
TIME (min)
batch 1
batch 2
batch 3
batch 4
batch 5
batch 6
batch 7
batch 8
batch 9
Figure 10: Dissolution data of experimental batches.
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Figure 11: Contour plot showing the effect of Carbopol 934p (X1) and PEO
WSR301 (X2) on Mucoadhesive strength (Y1).
Figure 12: Response Surface plot showing the effect of Carbopol 934p (X1)
and PEO WSR 301 (X2) on Mucoadhesive strength(N) (Y1).
Figure 13: Contour plot showing the effect of Carbopol 934P(X1) and PEO
WSR 301 (X2) on %Swelling index (Y3).
was determined by using specially designed disintegration apparatus.
As the concentration of bioadhesive polymer increased,
the residence time also increased. This examination reveals the
mucoadhesive capacity of polymers used in formulations. PEO
WSR301 had much more effect on the retention time (Table 7).
In-vitro drug release profile of experimental batches
In-vitro drug release study was carried out in 6.8 pH buffer using
IP apparatus type I at 37 ± 5º C temperature. Being a delayed release
dosage form factorial batches D1, D2 and D3 showed drug release
approximately 74.13, 72.15 & 70.35 % in 360 min. respectively. D4,
D5, D8 and D9 showed drug release approx.86.16, 91.92, 92.33 &
88.15 % in 360 min. respectively. While D6 and D7 showed drug
release at approx94.44 & 93.20 % in 360 min respectively (Figure 10,
Table 8).
32
model for Mucoadhesive strength
For Mucoadhesive strength, as seen from figure 11 of the counter
plot and response surface plot revealed that the Mucoadhesive
strength was change in case of concentration of PEO WSR 301 and
Figure 14: Response Surface plot showing the effect of Carbopol 934p (X1)
and PEO WSR 301 (X2) on %Swelling index (Y3).
Figure 15: Contour plot showing the effect of Carbopol 934P (X1) and PEO
WSR 301 (X2) on %Drug release at 6hr (Y2).
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Carbopol 934p was varies.
The Polynomial equation generated from Microsoft excels for
Mucoadhesive strength Was Mucoadhesive strength=
0.36+0.044X1+0.11X2+0.014X11-0.006X22+0.015X1X2
From polynomial equation and coefficient of X1 and X2 it was
observed that the Concentration of and PEO WSR 301 showed
positive effect on Mucoadhesive strength (Figure 11, Figure 12).
32
model for % swelling index
For % Swelling index, as seen from Figure 13 of the contour plot
and response surface plot revealed that the %Swelling index was
change in case of concentration of and PEO WSR 301 was varies.
The Polynomial equation generated from Microsoft excel for
%Swelling index was %Swelling index =
47.28+2.711X1+2.261X2+1.25X11+0.43X22-0.36X1X2
From polynomial equation and coefficient of X1 and X2 it was
observed that the concentration of carbopol 934p showed positive
effect on %Swelling index. Increase in their concentration would
increase the %Swelling index and concentration of it, was more
significant than concentration of PEO WSR 301 (Figure 13, Figure
14).
32
model for %Drug release at 6hr
For %Drug release at 6 hr. as seen from Figure 15 of the contour
plot and response surface plot revealed that the %Drug release at 6hr.
was change in case of concentration of PEO WSR 301 and Carbopol
934p was varies.
The Polynomial equation generated from Microsoft excel for
%Drug release at 6hr. was %Drug release at 6hr. = 91.54-5.95X1-
0.85X2-1.06X11-0.61X22-4.53X1X2
From polynomial equation and coefficient of X1 and X2 it was
observed that the concentration of PEO N80 showed negative effect
on %Drug release while the concentration of crospovidone showed
Figure 16: Response Surface plot showing the effect of Carbopol 934p (X1)
and PEO WSR 301 (X2) on %Drug release at 6hr. (Y2).
positive effect on %Drug release. So, optimum concentration of both
polymers required for the desired %Drug release (Figure 15, Figure
16).
Desirability approach or optimization of experimental
design
Concentration of Carbopol 934p (X1) and PEO WSR 301(X2)
have an important bearing on the formulation of mucoadhesive
buccal tablet. Dependent variables as indicators of the properties
of buccal tablet were Mucoadhesive strength (Y1), %Swelling index
(6hr). (Y2) and % drug release (6hr) (Y3).
The optimum formulation was selected based on the criteria of
attaining the minimum, target and maximum range of the dependent
variables. An overall desirability function dependent on all the
investigated formulation variables was used to predict the ranges of
variables where optimum formulation might occur. The desirable
ranges are from zero to one (least two more desirable, respectively).
The restriction value chosen (minimum, target, and maximum) put
in Minitab software to obtain optimized batch. Optimized batch was
prepared by using concentration of X1(Carbopol 934p) 30mg and
Concentration of X2(PEO WSR 301) 5mg. Optimized batch was
validated by F-test between the experimental results and calculated
Value (Figure 17).
Conclusion
The unidirection bucco-adhesive tablet devices of Sumatriptan
succinate provides good concept to bypass the extensive hepatic first-
passmetabolism.FormulatedtabletusingPEO-WSR301andCarbopol
934p showed good mucoadhesion, drug release profile (unidirection),
swelling index and permeation behavior. For the sake of getting a
better mucoadhesion and drug release both the polymers i.e Carbopol
934P and PEO WSR301 (1:4) were used in the combination. The
PEO WSR301 provided mucoadhesion whereas the Carbopol 934P
provided controlled drug release. Moreover Sumatriptan succinate is
a BCS class III drug so its permeability is low, so PEG 4000 (10mg)
was used as an effective permeation enhancer and the obtained results
also revealed the same characteristic of the permeation behavior. So
it can be concluded that Sumatriptan Succinate unidirectional bucco-
Figure 17: Profile of desirability graph.