The document is a thesis submitted to Biju Patnaik University of Technology for the award of Master of Pharmacy degree in Pharmaceutics. It discusses the formulation and evaluation of capecitabine loaded sodium alginate microbeads for colon targeting. The objectives of the research were to reduce side effects, provide controlled drug release and enhance bioavailability in the colonic site. The plan of work included preformulation studies, formulation of sodium alginate microspheres using ionic gelation method, and evaluation of drug release profile, particle size, drug entrapment efficiency and mucoadhesive properties of the formulations.
This document discusses different types of rate controlled drug delivery systems. It begins by introducing controlled release drug delivery and distinguishing it from sustained release. It then classifies controlled release systems into three main categories: rate programmed, activation modulated, and feedback regulated systems. Within each category it describes several examples of systems, identifying how drug release is controlled in each case. Key factors that can affect controlled release are also listed. The document aims to provide an overview of controlled drug delivery technologies with classifications and examples.
This document discusses targeted drug delivery to the colon. It begins with an introduction to colon targeted drug delivery and describes the anatomy and physiology of the colon. Key criteria for drug selection include drugs used to treat gastrointestinal diseases, those poorly absorbed in the upper GI tract, and drugs that degrade in the stomach and small intestine. Approaches for colon targeting include pH sensitive systems, microbially triggered systems using prodrugs and polysaccharides, timed release systems, and osmotically controlled drug delivery systems. The colon offers advantages for drug delivery including treatment of colonic diseases and absorption of proteins and peptides.
This document summarizes different types of diffusion controlled drug delivery systems. It describes reservoir and matrix devices. Reservoir devices consist of a drug core surrounded by a polymeric membrane, and drug release follows Fick's law of diffusion. Matrix devices involve drug dispersed throughout a polymer matrix, with drug on the surface dissolving first before diffusing out. The document provides the Higuchi equation that describes drug release from a matrix. It notes advantages like zero-order release for reservoir devices and lower risk of leakage for matrix devices, as well as disadvantages like need for removal after drug release. Methods for fabricating these devices like spray drying and coacervation are also summarized.
This document discusses in vitro dissolution testing methods. It defines dissolution as the process by which a solid substance solubilizes in a solvent, and dissolution rate as the amount of drug substance that goes into solution per unit time under standardized conditions. It then describes 7 common apparatus used for in vitro dissolution testing according to pharmacopeial standards, including the rotating basket, paddle, reciprocating cylinder, flow through cell, paddle over disk, rotating cylinder, and reciprocating disk methods. Each apparatus has distinct advantages and disadvantages for testing different drug products and dosage forms.
The document discusses diffusion parameters and their importance in understanding drug permeation and distribution. It defines diffusion as the mass transfer of molecules from an area of higher concentration to lower concentration. Studying diffusion parameters helps understand controlled release systems and how factors like solvent penetration rate and swelling layers influence drug release. Fick's laws of diffusion describe diffusion mathematically and diffusion coefficients are affected by concentration, temperature, and solvent properties. Techniques for studying diffusion include measuring diffusion front rates and concentration profiles using methods like microscopy, NMR, and video image processing. Variables that influence diffusion include surface area, thickness of the diffusion boundary layer, diffusion coefficient, and drug solubility. Diffusion is key to rate controlled drug delivery systems where it governs release from
This document summarizes a seminar on microsphere drug delivery systems. It discusses the classification, preparation methods, drug release mechanisms, and characterization of microspheres. The main preparation techniques covered are single and double emulsion methods, polymerization, and phase separation. Microspheres can provide controlled release and targeting of drugs. They have applications in taste masking, converting liquids to solids, and protecting drugs. Some marketed microsphere products are listed.
Controlled Release Oral Drug Delivery System
Controlled drug delivery is one which delivers the drug at a predetermined rate, for locally or systemically, for a specified period of time.
This document discusses different types of rate controlled drug delivery systems. It begins by introducing controlled release drug delivery and distinguishing it from sustained release. It then classifies controlled release systems into three main categories: rate programmed, activation modulated, and feedback regulated systems. Within each category it describes several examples of systems, identifying how drug release is controlled in each case. Key factors that can affect controlled release are also listed. The document aims to provide an overview of controlled drug delivery technologies with classifications and examples.
This document discusses targeted drug delivery to the colon. It begins with an introduction to colon targeted drug delivery and describes the anatomy and physiology of the colon. Key criteria for drug selection include drugs used to treat gastrointestinal diseases, those poorly absorbed in the upper GI tract, and drugs that degrade in the stomach and small intestine. Approaches for colon targeting include pH sensitive systems, microbially triggered systems using prodrugs and polysaccharides, timed release systems, and osmotically controlled drug delivery systems. The colon offers advantages for drug delivery including treatment of colonic diseases and absorption of proteins and peptides.
This document summarizes different types of diffusion controlled drug delivery systems. It describes reservoir and matrix devices. Reservoir devices consist of a drug core surrounded by a polymeric membrane, and drug release follows Fick's law of diffusion. Matrix devices involve drug dispersed throughout a polymer matrix, with drug on the surface dissolving first before diffusing out. The document provides the Higuchi equation that describes drug release from a matrix. It notes advantages like zero-order release for reservoir devices and lower risk of leakage for matrix devices, as well as disadvantages like need for removal after drug release. Methods for fabricating these devices like spray drying and coacervation are also summarized.
This document discusses in vitro dissolution testing methods. It defines dissolution as the process by which a solid substance solubilizes in a solvent, and dissolution rate as the amount of drug substance that goes into solution per unit time under standardized conditions. It then describes 7 common apparatus used for in vitro dissolution testing according to pharmacopeial standards, including the rotating basket, paddle, reciprocating cylinder, flow through cell, paddle over disk, rotating cylinder, and reciprocating disk methods. Each apparatus has distinct advantages and disadvantages for testing different drug products and dosage forms.
The document discusses diffusion parameters and their importance in understanding drug permeation and distribution. It defines diffusion as the mass transfer of molecules from an area of higher concentration to lower concentration. Studying diffusion parameters helps understand controlled release systems and how factors like solvent penetration rate and swelling layers influence drug release. Fick's laws of diffusion describe diffusion mathematically and diffusion coefficients are affected by concentration, temperature, and solvent properties. Techniques for studying diffusion include measuring diffusion front rates and concentration profiles using methods like microscopy, NMR, and video image processing. Variables that influence diffusion include surface area, thickness of the diffusion boundary layer, diffusion coefficient, and drug solubility. Diffusion is key to rate controlled drug delivery systems where it governs release from
This document summarizes a seminar on microsphere drug delivery systems. It discusses the classification, preparation methods, drug release mechanisms, and characterization of microspheres. The main preparation techniques covered are single and double emulsion methods, polymerization, and phase separation. Microspheres can provide controlled release and targeting of drugs. They have applications in taste masking, converting liquids to solids, and protecting drugs. Some marketed microsphere products are listed.
Controlled Release Oral Drug Delivery System
Controlled drug delivery is one which delivers the drug at a predetermined rate, for locally or systemically, for a specified period of time.
This document discusses drug diffusion, which is the movement of drug molecules into and within the biological environment. It involves drug transport across cell membranes through various passive and active processes. The main mechanisms of drug permeation and diffusion include passive diffusion via lipid or aqueous pathways, as well as carrier-mediated transport like facilitated diffusion. Factors that influence drug diffusion through the gastrointestinal tract include drug solubility, formulation properties, concentration gradient, blood flow, surface area for absorption, route of administration, gastric emptying rate, food effects, intestinal motility, and gastrointestinal drug metabolism.
Oral controlled drug delivery systems - Various Approaches SIVASWAROOP YARASI
these are the drug delivery systems which are given orally and the drug release is such that it releases at a controlled way at a predetermined rate for a particular period of time.
TUMOUR TARGETING DRUG DELIVERY SYSTEM.pptxSAURABH PUNIA
The document discusses tumor targeting drug delivery systems. It describes barriers to tumor targeting like heterogeneous blood flow and overexpression of efflux transporters in tumors. It also outlines three main approaches to tumor targeting - passive targeting using nanoparticles and the EPR effect, active targeting using ligands like folate and transferrin to target receptors overexpressed on tumors, and physical targeting using stimuli like pH, temperature, or external forces like magnetism and ultrasound to concentrate drugs in tumors.
This document summarizes a seminar on gastro-retentive drug delivery systems. It introduces the topic and discusses the principles and advantages of gastro-retentive drug delivery. It outlines different drug candidates that can benefit from this system and describes approaches like high density systems, floating systems, and bioadhesive systems. The document concludes that gastro-retentive drug delivery can help control drug release and enhance bioavailability for certain drugs.
This presentation includes introduction, physiology of GIT, factors affecting GRDDS, Advantages and disadvantages, approaches to GRDDS and their mechanism, some of the marketed products using GRDDS mechanism.
In this ppt include sustain drug delivery system. And that advantage,disadvantage,approaches,application.
This project is my first project.
This ppt is not made for brilent student,is use only normal student(passing student).
Thanx everyone.
-your friend DDV
Telepharmacy is delivery of pharmaceutical care via telecommunications to patients in locations where they may not have direct contact with pharmacist. It is an instance of wider phenomenon of telemedicine, as implemented in the field of pharmacy.
Telepharmacy services include drug therapy monitoring, patient counseling, monitoring of formulary compliance with the aid of teleconferencing or videoconferencing.
Telepharmacy services can be delivered at retail pharmacy sites or through hospitals, nursing homes or other medical care facilities.
Rural residents and communities lack easy access to healthcare services often due to geographical and demographical factors.
Telepharmacy holds significant promise as a technology to improve access to pharmaceutical care for people living in rural and remote communities.
Telepharmacy is quickly becoming an integral part of modern pharmacy practice that has the potential to provide quality pharmaceutical services, such as medication management, dispensing, patient counseling, and drug information.
Inherent to the adoption of these practices are legal challenges and pitfalls that need to be addressed. A well-developed system, however, can change the practice of pharmacy that is beneficial to both the rural communities and the hospital or retail pharmacies that deliver these services.
This document provides an introduction to sustained release and controlled release drug formulations. It defines sustained release as slowly releasing a drug over 8-12 hours, while controlled release delivers a drug at a predetermined rate for a specified time period. Some key advantages of these formulations are improved patient compliance, better drug utilization, and decreased side effects. Physicochemical drug properties like solubility, permeability and stability can impact whether a drug is suitable for these delivery systems. The document discusses various approaches for sustained and controlled release based on these physicochemical factors.
This document provides an overview of floating drug delivery systems. It begins with an introduction that describes how floating drug delivery systems can help modify gastric retention time and control drug release. It then discusses various factors that affect floating drug delivery systems and different mechanisms for achieving floatation. The document goes on to describe several types of non-effervescent and effervescent floating drug delivery systems that have been developed, including hydrodynamically balanced systems, hollow microspheres, alginate beads, and single-unit or multi-unit effervescent systems. It concludes by noting some applications and recent advances in floating drug delivery systems.
Controlled release drug delivery system2Bansari Patel
This document provides an overview of controlled release drug delivery systems (CRDDS). It defines CRDDS as systems that provide some control over the temporal or spatial release of drugs. The key advantages of CRDDS are maintaining effective drug levels, decreasing dosing frequency and side effects, and improving patient compliance. Factors like drug properties, pharmacokinetics, and pharmacodynamics can affect CRDDS. Various approaches to designing CRDDS are discussed.
‘Targeted drug delivery system is a special form of drug delivery system where the medicament is selectively targeted or delivered only to its site of action or absorption and not to the non-target organs or tissues or cells.’
This document discusses colon-specific drug delivery systems. It begins with an introduction to colon targeting and why it is important for treating colonic disorders. It then covers factors to consider in design such as colon anatomy, pH, transit time and microflora. Approaches discussed include pH dependent, time dependent and bacteria dependent systems. It evaluates both in vitro and in vivo methods for testing colon delivery systems.
This document discusses the differences between sustained release and controlled release drug formulations and their mechanisms of drug delivery. Sustained release aims to slowly release drug over 8-12 hours, while controlled release delivers drug at a predetermined rate according to bodily needs. Mechanisms include dissolution control using matrix or encapsulation methods, diffusion control using reservoir or matrix devices, and combinations of dissolution and diffusion. Common polymers used for coatings include ethyl cellulose and acrylic resins to control drug release rate.
Factors affecting sustained release drug delivery system.Kavya S
contented and precise , Drug delivery system , sustained release preparation.factors like absorption, distribution ,metabolism , therapeutic window , absorption window.
3D printing is a powerful manufacturing technique that can be used to create individually tailored drug formulations and dosage forms in a layer-by-layer process. It allows rapid production of complex dosage forms with multiple active ingredients and controlled release properties. 3D printing offers advantages for personalized medicine by enabling precise adjustments to dosage form size, shape, composition and drug delivery profiles. Various 3D printing methods use liquid or powder feedstocks and binding technologies like photopolymerization or thermal sintering to build up final dosage forms. This provides opportunities for sophisticated drug delivery systems with improved patient outcomes.
Microspheres are solid spherical particles ranging in size from 1-1000μm that can be used for drug delivery. They provide advantages like constant drug release, reduced dosing, and protection of drugs from degradation. Microspheres are made of polymers and exist as microcapsules or micromatrices. Various preparation methods include solvent evaporation, single/double emulsion, and polymerization. Microspheres find applications in oral, nasal, ocular, and other localized drug deliveries due to their ability to target tissues and control drug release kinetics.
This document discusses sustained release formulations (SRDFs), which are designed to release medication over an extended period of time after a single dose. It defines various types of modified release dosage forms and outlines techniques used in SRDF development, including drug and dosage form modification. Drug candidates suited for SRDFs include those with desirable solubility and a high therapeutic index. The document also examines factors that govern SRDF design such as a drug's physicochemical properties and stability.
The document discusses microspheres as a drug delivery system. It defines microspheres as small spherical particles ranging from 1μm to 1000μm that can be used to deliver drugs in a sustained, controlled release fashion. Various methods for producing microspheres are described, including single emulsion, double emulsion, phase separation, spray drying, and ionotropic gelation. The properties, mechanisms, types, and applications of microspheres are summarized. Evaluation methods for microspheres such as particle size, drug loading, and in vitro release are also outlined.
ABSTRACT- The objective of our present study was to develop multiparticulate gastro retentive drug delivery system
of Curcumin. The gastro retentive drug delivery system can be formulated to improve the absorption and bio-availability
of curcumin by retaining the system into the stomach for prolonged period of time. The floating drug delivery system of
curcumin was prepared by emulsion solvent diffusion method by using ethyl cellulose, Eudragit L100, HPMC, Phyllium
husk polymers in varying concentration. Formulations were evaluated for percent yield, particle size, entrapment
efficiency, in vitro buoyancy as well as in vitro release studies. The optimized formulations show good buoyancy and in
vitro controlled release of Curcumin.
Key-words- Floating microsphere, Ethyl cellulose, Hydroxypropyl Methyl cellulose (HPMC), Eudragit L 100, Phyllium
Husk
This document discusses drug diffusion, which is the movement of drug molecules into and within the biological environment. It involves drug transport across cell membranes through various passive and active processes. The main mechanisms of drug permeation and diffusion include passive diffusion via lipid or aqueous pathways, as well as carrier-mediated transport like facilitated diffusion. Factors that influence drug diffusion through the gastrointestinal tract include drug solubility, formulation properties, concentration gradient, blood flow, surface area for absorption, route of administration, gastric emptying rate, food effects, intestinal motility, and gastrointestinal drug metabolism.
Oral controlled drug delivery systems - Various Approaches SIVASWAROOP YARASI
these are the drug delivery systems which are given orally and the drug release is such that it releases at a controlled way at a predetermined rate for a particular period of time.
TUMOUR TARGETING DRUG DELIVERY SYSTEM.pptxSAURABH PUNIA
The document discusses tumor targeting drug delivery systems. It describes barriers to tumor targeting like heterogeneous blood flow and overexpression of efflux transporters in tumors. It also outlines three main approaches to tumor targeting - passive targeting using nanoparticles and the EPR effect, active targeting using ligands like folate and transferrin to target receptors overexpressed on tumors, and physical targeting using stimuli like pH, temperature, or external forces like magnetism and ultrasound to concentrate drugs in tumors.
This document summarizes a seminar on gastro-retentive drug delivery systems. It introduces the topic and discusses the principles and advantages of gastro-retentive drug delivery. It outlines different drug candidates that can benefit from this system and describes approaches like high density systems, floating systems, and bioadhesive systems. The document concludes that gastro-retentive drug delivery can help control drug release and enhance bioavailability for certain drugs.
This presentation includes introduction, physiology of GIT, factors affecting GRDDS, Advantages and disadvantages, approaches to GRDDS and their mechanism, some of the marketed products using GRDDS mechanism.
In this ppt include sustain drug delivery system. And that advantage,disadvantage,approaches,application.
This project is my first project.
This ppt is not made for brilent student,is use only normal student(passing student).
Thanx everyone.
-your friend DDV
Telepharmacy is delivery of pharmaceutical care via telecommunications to patients in locations where they may not have direct contact with pharmacist. It is an instance of wider phenomenon of telemedicine, as implemented in the field of pharmacy.
Telepharmacy services include drug therapy monitoring, patient counseling, monitoring of formulary compliance with the aid of teleconferencing or videoconferencing.
Telepharmacy services can be delivered at retail pharmacy sites or through hospitals, nursing homes or other medical care facilities.
Rural residents and communities lack easy access to healthcare services often due to geographical and demographical factors.
Telepharmacy holds significant promise as a technology to improve access to pharmaceutical care for people living in rural and remote communities.
Telepharmacy is quickly becoming an integral part of modern pharmacy practice that has the potential to provide quality pharmaceutical services, such as medication management, dispensing, patient counseling, and drug information.
Inherent to the adoption of these practices are legal challenges and pitfalls that need to be addressed. A well-developed system, however, can change the practice of pharmacy that is beneficial to both the rural communities and the hospital or retail pharmacies that deliver these services.
This document provides an introduction to sustained release and controlled release drug formulations. It defines sustained release as slowly releasing a drug over 8-12 hours, while controlled release delivers a drug at a predetermined rate for a specified time period. Some key advantages of these formulations are improved patient compliance, better drug utilization, and decreased side effects. Physicochemical drug properties like solubility, permeability and stability can impact whether a drug is suitable for these delivery systems. The document discusses various approaches for sustained and controlled release based on these physicochemical factors.
This document provides an overview of floating drug delivery systems. It begins with an introduction that describes how floating drug delivery systems can help modify gastric retention time and control drug release. It then discusses various factors that affect floating drug delivery systems and different mechanisms for achieving floatation. The document goes on to describe several types of non-effervescent and effervescent floating drug delivery systems that have been developed, including hydrodynamically balanced systems, hollow microspheres, alginate beads, and single-unit or multi-unit effervescent systems. It concludes by noting some applications and recent advances in floating drug delivery systems.
Controlled release drug delivery system2Bansari Patel
This document provides an overview of controlled release drug delivery systems (CRDDS). It defines CRDDS as systems that provide some control over the temporal or spatial release of drugs. The key advantages of CRDDS are maintaining effective drug levels, decreasing dosing frequency and side effects, and improving patient compliance. Factors like drug properties, pharmacokinetics, and pharmacodynamics can affect CRDDS. Various approaches to designing CRDDS are discussed.
‘Targeted drug delivery system is a special form of drug delivery system where the medicament is selectively targeted or delivered only to its site of action or absorption and not to the non-target organs or tissues or cells.’
This document discusses colon-specific drug delivery systems. It begins with an introduction to colon targeting and why it is important for treating colonic disorders. It then covers factors to consider in design such as colon anatomy, pH, transit time and microflora. Approaches discussed include pH dependent, time dependent and bacteria dependent systems. It evaluates both in vitro and in vivo methods for testing colon delivery systems.
This document discusses the differences between sustained release and controlled release drug formulations and their mechanisms of drug delivery. Sustained release aims to slowly release drug over 8-12 hours, while controlled release delivers drug at a predetermined rate according to bodily needs. Mechanisms include dissolution control using matrix or encapsulation methods, diffusion control using reservoir or matrix devices, and combinations of dissolution and diffusion. Common polymers used for coatings include ethyl cellulose and acrylic resins to control drug release rate.
Factors affecting sustained release drug delivery system.Kavya S
contented and precise , Drug delivery system , sustained release preparation.factors like absorption, distribution ,metabolism , therapeutic window , absorption window.
3D printing is a powerful manufacturing technique that can be used to create individually tailored drug formulations and dosage forms in a layer-by-layer process. It allows rapid production of complex dosage forms with multiple active ingredients and controlled release properties. 3D printing offers advantages for personalized medicine by enabling precise adjustments to dosage form size, shape, composition and drug delivery profiles. Various 3D printing methods use liquid or powder feedstocks and binding technologies like photopolymerization or thermal sintering to build up final dosage forms. This provides opportunities for sophisticated drug delivery systems with improved patient outcomes.
Microspheres are solid spherical particles ranging in size from 1-1000μm that can be used for drug delivery. They provide advantages like constant drug release, reduced dosing, and protection of drugs from degradation. Microspheres are made of polymers and exist as microcapsules or micromatrices. Various preparation methods include solvent evaporation, single/double emulsion, and polymerization. Microspheres find applications in oral, nasal, ocular, and other localized drug deliveries due to their ability to target tissues and control drug release kinetics.
This document discusses sustained release formulations (SRDFs), which are designed to release medication over an extended period of time after a single dose. It defines various types of modified release dosage forms and outlines techniques used in SRDF development, including drug and dosage form modification. Drug candidates suited for SRDFs include those with desirable solubility and a high therapeutic index. The document also examines factors that govern SRDF design such as a drug's physicochemical properties and stability.
The document discusses microspheres as a drug delivery system. It defines microspheres as small spherical particles ranging from 1μm to 1000μm that can be used to deliver drugs in a sustained, controlled release fashion. Various methods for producing microspheres are described, including single emulsion, double emulsion, phase separation, spray drying, and ionotropic gelation. The properties, mechanisms, types, and applications of microspheres are summarized. Evaluation methods for microspheres such as particle size, drug loading, and in vitro release are also outlined.
ABSTRACT- The objective of our present study was to develop multiparticulate gastro retentive drug delivery system
of Curcumin. The gastro retentive drug delivery system can be formulated to improve the absorption and bio-availability
of curcumin by retaining the system into the stomach for prolonged period of time. The floating drug delivery system of
curcumin was prepared by emulsion solvent diffusion method by using ethyl cellulose, Eudragit L100, HPMC, Phyllium
husk polymers in varying concentration. Formulations were evaluated for percent yield, particle size, entrapment
efficiency, in vitro buoyancy as well as in vitro release studies. The optimized formulations show good buoyancy and in
vitro controlled release of Curcumin.
Key-words- Floating microsphere, Ethyl cellulose, Hydroxypropyl Methyl cellulose (HPMC), Eudragit L 100, Phyllium
Husk
Design, optimization and in vitro evaluation of gastroretentive hollow micros...SURYAKANTVERMA2
To modify the GIT time is one of the main challenge in the development of oral controlled drug delivery system.
Gastric emptying of pharmaceutical dosage form is highly variable and dependent on the dosage form and the fed/fasted state of the stomach.
Normal gastric residence time usually ranges between 5 minutes to 2 hours.
This document presents a research study on the development of bilayered buccal tablets of chlorpheneramine maleate (CPM) for the treatment of allergic conditions. Various polymers including Carbopol 934, sodium alginate, guar gum, HPMC K4M, and HPMC K15M were used to prepare the tablets by direct compression method. The tablets were then evaluated for characteristics like hardness, thickness, drug content, swelling index, and in vitro drug release. Literature on buccal drug delivery and CPM was also reviewed to support the study. The aim was to increase the bioavailability of CPM using suitable formulation approaches for the buccal route of administration.
1) The document outlines the plan and experimental work for developing a buccal mucoadhesive drug delivery system of the drug Simvastatin using polymers like sodium alginate and guar gum.
2) Preformulation studies like drug-polymer compatibility using FTIR and characterization of polymers were carried out. Mucoadhesive tablets were prepared by direct compression method using different drug-polymer ratios.
3) The tablets were evaluated for hardness, weight variation, surface pH, swelling index and ex-vivo bioadhesion. F3 formulation with drug:polymer ratio of 1:5 showed maximum swelling and bioadhesion.
4) The study concluded that sodium alginate and guar gum
Formulation and Evaluation of Floating microspheres of L-CarnitineDarshanChhajedD
This document summarizes a research project on formulating and evaluating floating microspheres containing L-carnitine. L-carnitine was chosen as the model drug due to its low bioavailability when administered orally. Floating drug delivery systems were developed to increase gastric retention time and improve absorption. Ethyl cellulose was used as the polymer to prepare microspheres using solvent evaporation method. Microspheres were characterized for percentage yield, particle size, micromeritic properties, in-vitro floating ability, and shape. The objectives were to enhance bioavailability, increase absorption window, and gastric residence time of L-carnitine through a floating microsphere delivery system.
In this ppt ,i have covered the introduction of microspheres,various preparation methods of microspheres, advantages and disadvantage of microspheres,types and evaluation parameters of the microspheres.
This document describes the formulation development and evaluation of clobetasol propionate transferosomal gel. It begins with an introduction that discusses topical drug delivery and the benefits of transferosomes. The aim is then stated to develop a clobetasol propionate transferosomal gel and evaluate it. The plan of work, materials, instruments, and experimental work are outlined. Formulations are prepared varying phospholipid, surfactant concentrations and polymer concentration in the gel. Results include preformulation studies like solubility and compatibility. Characterization involves determining vesicle size, entrapment efficiency and in vitro drug release from formulations.
The document discusses various in vitro, in vivo, and in situ methods for determining drug absorption. In vitro methods include physicochemical techniques like measuring partition coefficients as well as more complex methods like using everted intestinal sacs or cell culture models. In vivo methods directly measure drug levels in blood/urine over time or indirectly via pharmacological response. In situ techniques simulate in vivo conditions by perfusing drug solutions through an intestinal segment while keeping the blood supply intact. The document provides detailed descriptions of techniques like the everted sac method, Caco-2 cell cultures, and Doluisio intestinal perfusion method.
Design, Development, Evaluation and Optimization of Microballoons of TelmisartanSnehal Patel
Abstract: In present study an attempt was made to prepare microballoons of
Telmisartan by emulsion solvent diffusion technique for sustained delivery by
using polymers like Ethyl cellulose to extend the drug release for about 12 hours in
the upper GIT, which may result in enhanced absorption and there by improved
bioavailability. Formulation optimization of Telmisartan loaded microballoons was
carried out by using different concentration of Polyvinyl alcohol (PVA) and Ethyl
cellulose. Total 9 batches were formulated. All 9 batches were evaluated for
entrapment efficiency (EE) and buoyancy. Among all batches DP4 shows
maximum entrapment efficiency (EE) and buoyancy and was considered as
optimized formulation. DP4 batch was further used for process optimization. The
process optimization was carried out at three different stirring speeds i.e. 1300,
1500 and 1700 rpm for three different stirring time period i.e. 1hr, 2hr and 3 hr and
another 9 batches were formulated. Out of all the batches DP13 showed the
spherical shape of microballoons without formation of flakes. Optimized batch
DP13 was evaluated for Zeta Potential, Particle Size Distribution which show -
41.8mV and 1.344 μm particle size, SEM, XRD Analysis. Batch DP13 was
charged for stability and were placed in glass vials container and stored at ICH
storage condition (2°C - 4°C Refrigeration condition , 30 ± 2°C / 60% ± 5% RH ,
40 ± 2°C / 75% ± 5% RH ) for a period of 30 days. The samples were analyzed for
physical appearance, buoyancy and for the drug release after 30 days. After 1
months samples were withdrawn and microballoons showed no change in physical
appearances, buoyancy and drug release, which indicate that the microballoons
were stable.
Keywords: Telmisartan, Microballoons, Emulsion solvent diffusion technique,
Buoyancy, Entrapment Efficiency.
MICROBALLOONS: A NOVEL APPROACH IN GASTRO-RETENTION FLOATING DRUG DELIVERY SY...Snehal Patel
ABSTRACT
Oral controlled release dosage forms face several physiological restriction like inability to retain
and position the controlled drug delivery system within the targeted region of the gastrointestinal
tract (GIT) due to fluctuation in gastric emptying. This results in non uniform absorption
pattern, inadequate medication release and shorter residence time of the dosage form in the
stomach. As the fallout of this episode there is inadequate absorption of the drug having
absorption window predominantly, in the upper area of GIT. These contemplations have
provoked to the development of oral controlled release dosage forms with gastroretentive
properties. Microballoons (Hollow microspheres) hold certification as one of the potential
approaches for gastric retention. Microballoons are spherical empty particles without core and
can remain in the gastric region for delayed periods. They significantly increase the gastric
residence time of medication, thereby enhance bioavailability, improves patient compliance by
reducing dosing frequency, lessen the medication waste, enhance retention of medication which
solubilize only in stomach, enhance solubility for medications that are less soluble at a higher pH
environment. The present review preparation methods, characterization, advantages,
disadvantages, mechanism of drug release from microballoons, applications and list of the drugs
formulated as microballoons are discussed.
KEYWORDS: Microballoons, Gastro-retention, Floating drug delivery system (FDDS).
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/
Formulation of Rutin trihydrate Liposomes for Topical Deliveryprescottasia
1. Rutin trihydrate liposomes were formulated using the thin film hydration method to enhance topical delivery of the antioxidant rutin trihydrate.
2. The liposomes were characterized for parameters like entrapment efficiency, vesicle size, and zeta potential. The optimized formulation showed 88% entrapment efficiency.
3. In vitro and ex vivo release studies showed that the rutin trihydrate liposomal gel provided prolonged drug release over 12 hours and exhibited anti-elastase activity, demonstrating its potential for topical delivery applications.
This document summarizes colon targeted drug delivery systems. It discusses pH dependent systems, time dependent systems, and microbially triggered systems as primary approaches. It also discusses newer approaches like pressure controlled colon delivery capsules and complex delivery systems (CODES). Advantages of colon targeted delivery include protection of drugs from degradation in the stomach and small intestine and targeting delivery to the colon for local treatment of diseases like IBD or systemic delivery of proteins and peptides. Novel drug delivery systems discussed include nano systems for targeted delivery to the colon to treat diseases like IBD and colon cancer.
In the present study, a gastro retentive micro particulate system was formulated with different Polymers by using
solvent evaporation technique. A series of 8 formulations was prepared based on 23 Design of experiments. The
formulated microspheres were evaluated flow characteristics, Practical yield (up to 80 %) and Encapsulation
efficiency (up to 94%). Scanning electron Microscopy confirmed their porous and spherical structure and the
particles were of the Size range of (65-525 μm). The release of drug at 1 hour and 8 hours’ time points were
taken as the measurable parameters for running the DOE experiments. According to design space Hollow
Microspheres formulated with Drug in the range of 50 to 70 mg/unit, Ethyl cellulose 7 cps in the range of 145 to
150 mg/unit and HPMC 5 cps in the range of 0.4 to 2 mg/unit were observed to have the best floating
characteristics and in vitro dissolution profile as per the preset target product profile. Stability studies showed no
significant change in the drug content in the formulations at 3 months accelerated condition. In this study
concluded that a micro particulate floating dosage form of an anti-infective drug can be successfully designed to
give controlled release and improved oral bioavailability.
KEYWORDS
Gastro retentive system, Ciprofloxacin Hcl, Ethyl Cellulose 7 cps, HPMC 5cps, Hollow microspheres.
microspheres,types, advantages and disadvantages,methods of preparation, evaluation or characterization of microspheres and applications of microspheres in various pharmaceutical fields.
The document discusses the formulation and evaluation of an artemether sustained release floating bilayer tablet. It aims to develop a floating drug delivery system for artemether to increase its gastric residence time and provide sustained release to ensure optimal drug levels in the blood and minimize side effects. The document provides background on floating drug delivery systems and reviews previous literature on developing such systems for other drugs. It then gives information on the drug artemether and outlines the objectives and methodology that will be used in the study.
Metformine power point presentation .. .slide sharesriram kota
The document describes the formulation and characterization of metformin HCl microspheres for controlled drug delivery. Various methods of microsphere preparation are discussed. The aim is to develop microspheres using sodium alginate polymer at different ratios to provide sustained release of metformin. Metformin HCl is characterized and microspheres are prepared using ionotropic gelation. The microspheres are evaluated for particle size, drug content, swelling, in vitro drug release and stability studies. The optimized formulation shows no degradation over 1 month and provides controlled release of metformin over an extended period.
FORMULATION AND INVITRO EVALUATION OF COLON SPECIFIC DRUG DELIVERY SYSTEM BY ...alok prakash kar
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FORMULATION AND EVALUATION OF CAPECITABINE IN COLON TARGETING
1. ENHANCEMENT 0F SOLUBILITY OF SELECTED MODEL DRUGBY LIQUID-SOLID
COMPACTIONTECHNIQUE
FORMULATION AND EVALUATION OF CAPECITABINE
LOADED SODIUM ALGINATE MICROBEADS FOR
COLON TARGETING
THESIS SUBMITTED TO BIJU PATNAIK UNIVERSITY OF TECHNOLOGY FOR
THE AWARD OF THE DEGREE OF
MASTER OF PHARMACY
IN
PHARMACEUTICS
SUBMITTED BY
RAKESH CHANDRA PARIDA, B.Pharm.
Regd. No- 1508267030
UNDER THE ESTEEMED GUIDANCE OF
Mr. GOUTAM KUMAR JENA
M. Pharm. , Asst. Professor
DEPARTMENT OF PHARMACEUTICS
ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES, BERHAMPUR, ODISHA (2017) 1
4. 4
1.INTRODUCTION
DEFINITION- Colon drug delivery system refers to targeted
delivery of drug in to the lower parts of GI tract , mainly large
intestine.
The major goal of any drug delivery system is to supply a
therapeutic amount of drug to a target site in a body.
A targeted drug delivery system is preferred in drugs having
instability, low solubility and short half life
Targeted delivery of drugs to the colon is usually to achieve one
or more of four objectives.
To reduce dosing frequency .
To delay delivery to the colon to achieve high local concentrations
in the treatment of diseases of the distal gut.
To delay delivery to a time appropriate to treat acute phases of
disease.(chrono therapy).
To deliver to a region that is less hostile metabolically, e.g., to
facilitate absorption of acid and enzymatically labile materials,
especially peptides.
5. 5
ANATOMY OF COLON :-
The GIT consists of parts from mouth to anus. It mainly consists of two
parts namely stomach, intestine. The intestine includes small intestine
and large intestine.The GIT measures about 5 meters long. The different
parts of GIT are divided into upper and lower gastrointestinal tract. The
upper GIT includes oesophagus, stomach, and duodenum. The lower GIT
includes small intestine and large intestine. The small intestine measures
an average of about 6.9 meters to 7.1 meters. It include duodenum,
jejunum and ileum. The main function of small intestine is the absorption
of nutrients and minerals from food. The retention time of small intestine
is 3-5 hr. The large intestine measures about 1.5metres long. It includes
caecum, colon and rectum. The main function of large intestine is to
remove the water and minerals from the food and it sends the
indigestible matter to the rectum.The retention time of large intestine is
3-10hr.
6. 6
The colon consists of four parts: ascending colon, transverse colon,
descending colon and sigmoid colon. It extracts water and salts from solid
wastes before they are eliminated from the body. The parts of colon are
located either in the abdominal cavity or behind it in retro peritoneum. The
ascending and descending colon and rectum are retroperitoneal, while
transverse colon is intra peritoneal. The pH of colon varies from 5.5 to 7.
Transit time of different parts of GIT pH in different parts of Colon
Part Of GIT Transist
Time
Fasted state 10min – 2hr
Fed state >2hr
Small intestine
transit
3-4hr
Colon transit 20-35hr
Part of GIT pH
Stomach
Fasted state
1.5-2
Fed state 2-6
Small Intestine 6.0- 6.8
Colon
Ascending colon
Transverse colon
Descending colon
7.0
7.2
7.4
7. 7
MICROPARTICLES :-
These are the particles with size more than ‘1’m, containing the polymer.
At present, there is no universally accepted size range that particles must
have in order to be classified as microparticles. However, many workers
classify the particles smaller than ‘1’m, as nonparticles and those more than
1000 m as macroparticles.
CLASSIFICATION :
Micro particles are classified into two groups:
MICROCAPSULES
Microcapsules have an either spherical geometry with a continuous core
region surrounded by a continuous shell or have an irregular geometry and
contain a number of small droplets
MICROSPHERES:-
Microspheres are solid, spherical particles containing dispersed drug
molecules, either in solution or crystalline form, among the polymer
molecules.
Microparticles
Microcapsules
(Micrometric
Reservoir Systems)
Microspheres
(Micrometric Matrix
Systems)
8. 8
TYPES OF MICROSPHERES:
1. Bioadhesive microspheres
These kinds of microspheres exhibit a prolonged residence time at the site
of application and causes intimate contact with the absorption site and
produces better therapeutic action.
2. Magnetic microspheres
These kind of delivery system is very much important which localises the
drug to the disease site.
3. Diagnostic microspheres
It can be used for imaging liver metastases and also can be used to
distinguish bowel loops from other abdominal structures by forming nano
size particles supramagnetic iron oxides .
4. Polymeric microspheres
The different types of polymeric microspheres can be classified as follows
and they are biodegradable polymeric microspheres and Synthetic polymeric
microspheres. Biodegradable polymeric microspheres Natural polymers such
as starch are used with the concept that they are biodegradable,
biocompatible, and also bio adhesive in nature
9. 9
5.Radioactive microspheres
Radio emobilisation therapy microspheres sized 10-30 nm. They are
injected to the arteries that lead to tumour of interest. So all these
conditions radcioactive microspheres deliver high radiation dose to the
targeted areas without damaging the normal surrounding tissues.
6. Floating microspheres
Floating types the bulk density is less than the gastric fluid and so remains
buoyant in stomach without affecting gastric emptying rate. The drug is
released slowly at the desired rate.
Various methods of preparations of Microspheres
Emulsion solvent evaporation technique
Emulsion cross linking method
Co-acervation method
Spray drying technique
Emulsion-solvent diffusion technique
Multiple emulsion method
Ionic gelation
Solvent extraction
11. 11
SL .NO DRUG WORK RESULT
1 CAPECITABINE Formulation and Evaluation of
Coated Microspheres for Colon
Targeting.
Coated microspheres of 5-
FlChitosan is used as
polymeruorouracil (FU).
Eudragit S100 coating of
chitosan microspheres was
performed by oil-in-oil solvent
evaporation method using
coat: core ratio (5:1).
2 SATRANIDAZOLE Design and Dev. of Satranidazole
Microsphere For Colon Targeted
Drug Delivery
The release rate was much
slower; however, the drug was
released quickly at pH 7.4. It is
concluded from the present
investigation that Eudragit
microspheres are promising
controlled release carriers for
colontargeted delivery of
satranidazole.
3 CAPECITABINE Formulation And Charecterisation
Of Colon Targeted pH Dependent
Microspheres Of Capecitabine For
Col.orectal Cancer
PH-sensitive polymer Eudragit
L100, S100 separately and in
combination (1:2) was used to
formulate the microspheres by
emulsion solvent diffusion
technique using varying drug –
polymer ratios (1:2 to 1:6).
2. LITERATURE REVIEW
12. 12
04
MELOXICAM
Formulation And Evaluation Of
Meloxicam Loaded Microspheres For
Colon Targeted Drug Delivery
The present investigation that
Eudragit-coated sodium
alginate microspheres are
promising controlled
release carriers for colon-
targeted delivery of Meloxicam
05 TINIDAZOLE
Formulation and development of
Tinidazole Microspheres for colon
targeted drug delivery System
The release rate was
Much slower; however, the drug
was released quickly at
pH7.4.It is concluded from the
present investigation that
Eudragit microspheres are
promising as a carrier for
colontar-geted delivery of
Tinidazole.
06 TELMISARTAN
Formulation and evaluation of
controlled-release of Telmisartan
microspheres: In vitro/in vivo study
The release mechanism was
studied by comparing the values
of correlation coefficients, and
the drug release was found to
be controlled by diffusion of
drug through the microsphere
matrix (TMRS formulation). The
Higuchi model was found to be
the best fitted for drug release
from telmisartan microspheres
of TMRS formulations.
14. 3. AIM AND OBJECTIVE
In recent years, microspheres have been proven to deliver drugs
efficiently to the target site with improved bioavailability.
The objective of present research work is to prepare microspheres
using Capecitabine.
In order to achieve the aim, the following objectives have been set:
To reduce the side effect.
To controlled the drug release .
To enhance the bioavailability in colonic site.
14
15. PLAN OF WORK
Preformulation Studies:-
Characterization of Active Pharmaceutical Ingredient by determining
organoleptic parameters and analytical evaluation.
Solubility studies of pure drug and polymer.
Formulation Studies:-
To select suitable cross linking agents such as CaCl2 & ZnSO4, Polymer such
as Sodium Alginate , Eudragit S100 & Eudragit L100.
Preparation of Sod. Alginate microspheres by Ionic Gelation method.
Determination of drug release profile of microparticles.
Determination of swelling property of formulation in different solvents.
Observation of average particle size of microspheres.
Determination of dissolution rate of microspheres prepared for
Capecitabine.
Encapsulation of microspheres using different coating materials.
Determination of drug entrapment efficiency of various microsphere
formulations.
Determination of Mucoadhesive property of formulation.
15
17. 17
4.DRUG PROFILE
CHEMICAL STRUCTURE :-
CAPECITABINE
MOLECULAR WEIGHT :- 359.350083 G/MOL
MOLECULAR FORMULA :- C15H22FN3O6
GENERIC NAME :- Capecitabine
TRADE MAN :- Xeloda
CHEMICAL NAME:- Pentyl N[1[(2R,3R,4S,5R)3,4dihydrox
5methyloxolan2yl]5fluoro2oxopyrimidin4yl] carbamate.
DESCRIPTION :- Off white or almost white crystalline powder
M.O.A:- Nucleic acid synthesis inhibitor.
THERAPEUTIC CATEGORY:- Anti cancer drug
18. 18
DOSE:- 150-500mg.
BIOLOGICAL HALF LIFE:- 45-60 minutes
M.P:- 110-1210c
BIOAVAILABILITY:- 80-90% (extensive)
SOLUBILITY :- Insoluble in water, 0.1N HCl,Glacial acetic acid and soluble
in acetone, ethanol, 0.1N NaOH, phosphate buffer pH 6.8 and solubility is
highest in phosphate buffer pH 7.6.
STORAGE:- Capecitabine should be stored in tightly closed containers at 25
0C but may be exposed to temperatures of 15-30 0C.
USES:- CapecItabine is a deoxycytidine derivative and fluorouracil Prodrug
that is used as an Antineoplastic Antimetabolite in the treatment of Colon
Cancer, Breast Cancer and Gastric Cancer.
ADVERSE EFFECTS:- Most common advese reactions are headache,
abdominal pain, constipation , Nausea , Vomiting and Diarrhoea.
20. 20
SL.NO Name of the material MANUFACTURER
1 Capecitabine Gift sample from college
2 Sodium Alginate Gift sample from college
3 Eudragit L 100 Evonik , India
4 Eudragit S 100 Evonik , India
5 CaCl2
Merck, India
6 ZnSO4
Merck, India
7 Acetone Triveni Chemicals
8 Glacial acetic acid Arihant chemicals
MATERIALS USED
21. 21
EQUIPMENT USED
SL.
NO
EQUIMENTS MODEL/MANUFACTURER
1 Digital balance BS223S, Sartorius, India
2 UV-Visible Spectrophotometer UV-1800, Shimadzu, Japan
3 Mechanical shaker REMI, India
4 Ultra sonicator Enartech, India
5 Magnetic stirrer Tarsons, Multispin, India
6 Optical microscope Magnus, MLX, India
7 6-Stage USP-I Dissolution
Apparatus
Electrolab, India
8 Disintegration Apparatus Electrolab, India
23. 23
Active Pharmaceutical Ingredient (API) characterization:-
Evaluation of API:
1. Organoleptic properties:
2. Analytical properties:
UV Spectroscopic Analysis:
1. Determination of ƛmax of Capecitabine by UV Spectroscopy
method:
A Stock solution of Capecitabine (1000 µg/ml) was prepared by taking 10 mg
of drug to a small volume of solution in a 10ml volumetric flask and shaked
for few seconds and made upto the volume. From this, 1ml was pipetted out
and made upto 10ml using phosphate buffer pH 7.4 solution to obtain a
concentration of 100 µg/ml. From this, 1ml was taken and diluted to 10ml
using the same buffer solution and was scanned on UV- Visible
Spectrophotometer using a scan speed of 238nm/min, data interval 0.1nm
and slit width 1.0nm in the range of 200-400nm. The wavelength of
maximum absorbance (ƛmax) was determined.
EXPERIMENTAL WORK
24. 24
Conc. In
µg/ml
Absorbance
0 0
3 0.102
6 0.216
9 0.347
12 0.461
15 0.569
18 0.699
21 0.831
1.PREPARATION OF CALIBRATION CURVE FOR CAPECITABINE.
A. Preparation Of Phosphate Buffer Ph7.4 (1000ml).
B. Preparation of Sample Solution:
0
0.102
0.216
0.347
0.461
0.569
0.699
0.831
y = 0.039x - 0.012
R² = 0.999
-0.1
0
0.1
0.2
0.3
0.4
0.5
0.6
0.7
0.8
0.9
0 10 20 30
A
b
s
o
r
b
a
n
c
e
Concentration (µg/ml)
Series1
Linear (Series1)
25. 25
SOLUBILITY STUDIES:
Excess quantity of the pure drug was added to freshly prepared
simulated gastric fluid(0.1N HCl), water, simulated intestinal
fluid(phosphate buffer pH 6.8 and 7.4), and other organic solvents like
acetone, ethanol etc into clean vials. It was shaken in a mechanical
shaker at 25+0.5oc for 24hrs.Then it was filtered and 1ml of filtrate was
collected in 10ml volumetric flasks and diluted up to the mark
respectively. Then the absorbances of the samples were collected by
using U.V spectrophotometer at 238 nm. The polymer was found to be
completely soluble in glacial acetic acid.
Table : Solubility of Drug in Various solvents
SOLVENT ABSORBANCE CONCENTRATION
(µg/ml)
CONCENTRATION
(mg/ml)
Water 1.134 344.54 0.344
0.1NHCl 0.381 101.61 0.101
PH 6.8 1.527 471.29 0.471
PH 7.4 1.567 483.23 0.483
26. 26
FORMULATION AND OPTIMIZATION OF MICROSPHERES :
Preparation Of Sodium Alginate Microspheres By Ionotropic
Gelation Method:
First of all weighed accurately all materials required for the experiment
including the drug used Capecitabine , Sodium alginate , calcium chloride and
zinc sulphate.
The weighed different formulation quantity of Capecitabine drug was dissolved
in 5% of Glacial acetic acid aqueous solution.
Distilled water was added to the weighed different formulation quanty of
sodium alginate to make aqueous mucilage of in a beaker.
The aqueous mucilage of sodium alginate was stirred in a magnetic stirrer at a
suitable speed (rpm) for 30minutes.
The drug Capecitabine was dispersed in the glacial aqu. Solution and aqueous
mucilage of sodium alginate mix susiquently stirred at suitable speed in the
magnetic stirrer.
Distilled water was also added separate beaker to the 10% W/W quantity of
calcium chloride and Zinc Sulphate .
The microparticle were formed by dropping the bubble free dispersions
through a glass syringe with the help of needle size 18 into the gently agitated
in different solution like calcium chloride , zinc sulphate and calcium chloride &
zinc sulphate solution in 100ml.
The microsphere for 30 mins and was filtered and wash thoroughly distilled
water .
The microsphere was dried in hot air oven for 2-4 hrs at 500c and evaluated.
28. 28
Table : Formulation Of Capecitabine Loaded Sodium alginate Microsphere
For 10 % of calcium chloride aqueous solution.
Formulation code Drug (mg) Polymer (mg) Drug :
Polymer
Ratio
Cacl2 Aqu.
Solu.
(% w/v)Sodium Alginate
R1 100 400 1:4 10
R2 100 600 1:6 10
R3 100 800 1:8 10
R4 100 1000 1:10 10
R5 100 1200 1:12 10
R6 100 1400 1:14 10
These are three different formulation I was found in best formulation result
of Capecitabine Loaded Sodium alginate Microsphere For 10 % of calcium
chloride and Cacl2 & Znso4 aqueous solution.
29. 29
OPTIMIZATION PROCESS OF VARIABILITY :-
In order to explore the influence of formulation and preparative variables of
the Ionic gelation technique on the formation of microsphere and their size
, polymer ,selection of solvents and their ratio were studied in order to
control and optimized the process.
Optimization Parameters Process variables
Drug polymer ratio (constant: RPM,) 1:4
1:6
1:8
1:10
1:12
1:14
Rotational speed in RPM (constant: Drug-
polymer ratio)
300
500
700
ENCAPSULATION OF CAPECITABINE LOADED SODIUM ALGINATE MICROSPHERES:-
•Microsphers were coated with Eudragit S 100 and Eudragit L 100 ata concentration of 1:1
ratio respectively.
•Microspheres were dispersed in Eudragit S 100 and Eudragit L 100 solution prepared in
10% w/v of acetone at room temperature.
•Stirring was continued for 3hours at room temperature in order to evaporate the solvent
completely.
•Encapsulated microspheres were filtered and dried.
31. 31
RESULTS & DISCUSSION
DRUG ENTRAPMENT EFFICIENCY :
The amount of Drug Entrapment was calculated by the formula
% Drug Entrapment Efficiency= Experimental Drug Content / Theoritical
Drug Content x 100
Table : Drug Entrapment Efficiency of Formulation Of Capecitabine Loaded
Sodium alginate Microsphere For 10% of Calcium chloride and Cacl2 &
Znso4 aqueous solution.
Formulation
(Drug+polymer)
Entrapment
Efficiency (%)
Formulation
(Drug+polymer)
Entrapment
Efficiency (%)
F1 72.47 R1 67.43
F2 75.64 R2 69.21
F3 77.14 R3 72.45
F4 79.04 R4 73.12
F5 81.26 R5 75.18
F6 82.78 R6 76.63
The drug entrapment efficiency of all the formulations were determined
and it was found that the % drug entrapped were increased with
increase in drug and polymer ratio.
32. 32
The Swelling index was calculated by the formula
Swelling Ratio = Final weight – Initial weight / Initial weight x 100.
Table : Swelling Index for Formulation of (Cacl2 & Znso4 aqueous
solution).
SWELLING INDEX :
SOLVENT
% SWELLING INDEX
F1 F2 F3 F4 F5 F6
1. PH 6.8 5 7 6 9 8 10
2. 0.1N HCL 6 8 10 15 18 21
3. Water 5 8 10 13 11 15
0
5
10
15
20
25
F1 F2 F3 F4 F5 F6
%SWELLING
FORMULATION
% Swelling PH. 6.8
% Swelling 0.1N HCL
% Swelling Water
34. 34
AVERAGE PARTICLE SIZE DETERMINATION:
10 divisions of eye piece = 15 divisions of stage micrometer.
1 division of eye piece = 15/10 or 1.5 divisions of stage micrometer.
As, 100 divisions = 1mm
1 division = 0.01mm
So, Correction factor = 1.5*0.01 =0.015nm or 15µm.
Table : Average particle size of microsphere.
Range(µm) Mean
Range(µm)(d)
Total number of
microspheres(n)
n*d
30-40 35 52 1820
40-50 45 18 810
50-60 55 11 605
70-90 80 10 800
100-110 105 9 945
∑n=100 ∑n*d=4980
The average particle size was determined by using the Edmondson’equation =
Dmean= nd/n
Where , n – Total number of microsphere observed.
d- Mean size range.
Average particle size of microsphere in µm=∑n*d/∑n
=4980/100=49.8µm.
35. 35
MUCOADHESIVE PROPERTY
The mucoadhesive property of microspheres was evaluated by an in vitro adhesion
testing method . Freshly excised piece of goat stomach mucous were mounted on to
glass slides. About 20 microspheres were spread on to each prepared glass slide and
immediately there after the slides were hung to USP II tablet disintegration test
apparatus. When the test apparatus was operated the sample is subjected to slow up
and down movement Buffer ph 7.4 at 370 C . At 8 hour the machine was stopped and
number of microspheres still adhering to mucosal surface was counted.
% Mucoadhesion = Number of microspheres adhered/Number of microspheres applied
x 100.
Table : Mucoadhesion Property for Formulation of (Cacl2 & Znso4 aqueous
solution).
Formulat
ion
No of
Microsphere
Applied
No
Microspher
e Adhered
%
Mucoadhesion
F1 20 16 80
F2 20 18 90
F3 20 18 90
F4 20 19 95
F5 20 17 85
F6 20 18 90
70
75
80
85
90
95
100
R1 R2 R3 R4 R5 R6
%MUCOADHESION
FORMULATION
%
Mucoadhes
ion
% Muco adhesion of different formulation.
36. 36
Table : Mucoadhesion Property for Formulation of (Cacl2 aqueous solution)
Formulation No of Microsphere
Applied
No Microsphere
Adhered
% Mucoadhesion
R1 20 15 75
R2 20 17 85
R3 20 18 90
R4 20 19 95
R5 20 17 85
R6 20 18 90
70
75
80
85
90
95
100
R1 R2 R3 R4 R5 R6
%
MUCOADHESION
FORMULATION
% Mucoadhesion
The drug Mucoadhesion Property of all the formulations were
determined and it was found that the % Mucoadhesion was best in F4
and R4 formulation in 95% Mucoadhesion.The Mucoadhesion were
increased with increase in drug and polymer ratio.
37. 37
IN-VITRO DRUG RELEASE STUDIES:
PROCEDURE:
The dissolution technique was used of Capecitabine from microsphere
system. The receptor media used was 0.1N HCL for 2hrs then same
formulation put into 6.8 phosphate buffer for 10hrs then same formulation
put into the pH 7.4 phosphate buffer for 12hrs medium (900ml) was studied
by using a dissolution test apparatus with a Basket type stirrer. The entire
system was kept at 370C. 50mg equivalent of the drug formulation was
added and rotated at 100 rpm. Samples (5ml) from dissolution medium were
withdrawn and filtered at different interval of time and were assayed for
capecitabine Loaded sodium alginate content at 238 nm against blank.
39. 39
0
20
40
60
80
100
120
0 5 10 15 20 25 30
%CUMULATIVEDRUGRELEASE
TIME IN HOURS
Zero Order Plot
% CU DR F1
% CU DR F2
% CU DR F3
% CU DR F4
% CU DR F5
% CU DR F6
Fig. of Zero Order Plot of Drug Release Kinetics
From the above Results, It has been Found that the Cumulative %
Drug Release is best shown by Formulation With Drug & Polymer ratio
1:10 & 1:14 in Formulation F4 and F6. It has also been found that
there is an increase in release with increase in concentration of
polymer .
40. 40
Table : R2 Values Of different Plots :
Formulations
(Cacl2 & Znso4 )
Zero order R2 First order R2 Higuchi plot
R2
Korsmeyer-
peppa’ s R2
F1 0.987 0.654 0.889 0.973
F2 0.990 0.737 0.890 0.974
F3 0.992 0.775 0.897 0.975
F4 0.994 0.792 0.917 0.983
F5 0.991 0.798 0.914 0.973
F6 0.993 0.801 0.916 0.982
Analysis of drug release data from various plots such as Zero order , First
order, Higuchi and Korsmeyer Peppa’s Plot and the R2 Value presented in the
Table . We were found in R2 Value obtained from zero order kinetics.
42. 42
0
20
40
60
80
100
120
0 5 10 15 20 25 30
%CUMULATIVEDRUGRELEASE
TIME IN HOUR
Zero Order Plot
% CU DR R1
% CU DR R2
% CU DR R3
% CU DR R4
% CU DR R5
% CU DR R6
Fig. Of Zero Order Plot of Drug Release Kinetics
From the above Results, It has been Found that the Cumulative % Drug Release is
best shown by Formulation With Drug & Polymer ratio 1:10 in Formulation R4. It has
also been found that there is an increase in release with increase in concentration of
polymer .
43. 43
Table : R2 Values Of different Plots :
Formulations
(Cacl2 aqu.
solu )
Zero order
R2
First order
R2
Higuchi plot
R2
Korsmeyer-
peppa’ s R2
R1 0.992 0.760 0.913 0.968
R2 0.989 0.777 0.893 0.970
R3 0.990 0.779 0.894 0.976
R4 0.993 0.794 0.911 0.988
R5 0.989 0.751 0.889 0.969
R6 0.990 0.778 0.897 0.974
Analysis of drug release data from various plots such as Zero order , First
order, Higuchi and Korsmeyer Peppa’s Plot and the R2 Value presented in
the Table . We were found in R2 Value obtained from zero order
kinetics.
44.
45. 45
SUMMARY & CONCLUSION
SUMMARY :-
From this experimental work, Microspheres prepared by using only
CaCl2 as Cross linking agent showed spherical shape but does not control
the better release upto 24 hr as that of combined effect as ZnSo4 & CaCl2
solution.
The Microspheres prepared by ZnSo4 alone also does not produced
Spherical spread microspheres & also not able to control the drug release
upto 24 hrs. when both ZnSo4 & CaCl2 solution were used combinedly as
cross linking agent produced microspheres which were spreaded in shape
, maximize yield & control l the drug release upto 24 hrs.
Hence cross linking effect can be enhanced when both ZnSo4 & CaCl2
were used combinedly solution.
The drug release study data from various plot such as zero order , first
order , Higuchi plot & Korsmeyer peppa’s plot. We were found in R2 value
obtained from Zero order Kinetics.
CONCLUSION :-
Microspheres can be prepared by Ionotropic gelation technique by using
both ZnSo4 & CaCl2 Solution as cross linking agent which can better
conroll drug release upto 24 hr, maximized yield, produce spherical
shape.
46.
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50. ACKNOWLEDGEMENT:
Special thanks to
Prof. (Dr.) M.E. Bhanaji Rao,
M.Pharm, Ph.D.,Principal,
Roland Institute of Pharmaceutical
Sciences
Berhampur.
Prof. (Dr.) Ch. Niranjan Patra
M. Pharm., Ph.D., Professor
Deparment of Pharmaceutics
All my dearest colleagues, seniors, teaching and non teaching staff
members of Roland Institute of Pharmaceutical Sciences.
Mr. Goutam Kumar Jena
M. Pharm., Asst. Professor
Deparment of Pharmaceutics