This document provides an overview of intrauterine and intravaginal drug delivery systems. It discusses the anatomy and physiology of the female reproductive system and factors that affect vaginal drug absorption. Various types of intravaginal drug delivery systems are classified and described, including suppositories, bioadhesive semisolids, elastomeric rings, and solid polymeric carriers. Advantages include avoiding first-pass metabolism and providing controlled drug release over extended periods. Intrauterine systems can deliver drugs locally via non-hormonal or hormonal IUDs. Animal models for studying vaginal drug absorption are also mentioned.
This document provides an overview of gastric retention drug delivery systems (GRDDS). It discusses the need for and advantages of GRDDS. The key approaches covered for achieving gastric retention include floating drug delivery systems, mucoadhesive systems, swellable systems, and high density systems. The document reviews gastrointestinal physiology and factors affecting gastric emptying. It also evaluates different GRDDS approaches and provides examples of commercial gastroretentive formulations. In conclusion, the document states that GRDDS are preferable for delivering drugs that need to be released in the gastric region.
Mucoadhesive drug delivery systems aim to increase drug bioavailability by keeping formulations in close contact with mucus membranes. There are three main stages of mucoadhesion: wetting and swelling, interpenetration of polymer chains with the mucus layer, and formation of chemical bonds. Several theories explain mucoadhesion, including electronic, adsorption, wetting, diffusion, and fracture theories. Key factors affecting mucoadhesion are related to the polymer properties, such as molecular weight, concentration, flexibility, and spatial conformation, as well as environmental and physiological factors. Mucoadhesive systems can provide benefits like prolonged drug residence at the site of action and increased drug absorption.
ocular barriers and methods to overcome barriersTarun Gollapudi
This document summarizes barriers to ocular drug delivery and methods to overcome them. The major barriers include ocular surface barriers like the cornea, ocular wall barriers like the sclera, retinal barriers, the vitreous body, lachrymal fluid, and properties of the drug itself like solubility and molecular weight. Methods to enhance delivery include microneedles, ultrasound, iontophoresis, periocular routes, and intravitreal injections. Various ophthalmic formulations are also discussed like eye drops, gels, ointments, and inserts that utilize approaches like prodrugs, penetration enhancers, and nanoparticle carriers to improve ocular bioavailability.
Intrauterine & Intravaginal Drug Delivery SystemPRASHANT DEORE
This document discusses intrauterine and intravaginal drug delivery systems. It begins with an introduction and overview of anatomy and physiology of the female reproductive system. It then describes various types of intravaginal drug delivery systems including suppositories, bioadhesive semisolids, elastomeric rings, and solid polymeric carriers. Factors affecting vaginal drug absorption are also discussed. The document concludes by describing intrauterine drug delivery systems including non-hormonal and hormonal IUDs, and discussing advantages and disadvantages of both intravaginal and intrauterine systems.
Application Of Polymer In Controlled Release FormulationAnindya Jana
Polymers are becoming increasingly important in the field of drug delivery. The pharmaceutical applications of polymers range from their use as binders in tablets to viscosity and flow controlling agents in liquids, suspensions and emulsions. Polymers can be used as film coatings to disguise the unpleasant taste of a drug, to enhance drug stability and to modify drug release characteristics.
As a consequence, increasing attention has been focused on methods of giving drugs continually for a prolonged time periods and in a controlled fashion.
This technology now spans many fields and includes pharmaceutical, food and agricultural applications, pesticides, cosmetics, and household products.
Barriers and routes of occular drug delivery systemShresthaPandey1
The document discusses various barriers to ocular drug delivery and routes to overcome these barriers. The key barriers include anatomical barriers like the cornea and conjunctiva, physiological barriers like tear turnover and drainage, and blood-ocular barriers. Methods to improve bioavailability and provide controlled drug delivery include adjusting viscosity, using prodrugs, penetration enhancers, and ocular inserts. Inserts can be non-erodible like Ocusert or erodible like Lacriserts, SODI, and Mindisc to continuously deliver drugs to the eye.
This document provides an overview of gastric retention drug delivery systems (GRDDS). It discusses the need for and advantages of GRDDS. The key approaches covered for achieving gastric retention include floating drug delivery systems, mucoadhesive systems, swellable systems, and high density systems. The document reviews gastrointestinal physiology and factors affecting gastric emptying. It also evaluates different GRDDS approaches and provides examples of commercial gastroretentive formulations. In conclusion, the document states that GRDDS are preferable for delivering drugs that need to be released in the gastric region.
Mucoadhesive drug delivery systems aim to increase drug bioavailability by keeping formulations in close contact with mucus membranes. There are three main stages of mucoadhesion: wetting and swelling, interpenetration of polymer chains with the mucus layer, and formation of chemical bonds. Several theories explain mucoadhesion, including electronic, adsorption, wetting, diffusion, and fracture theories. Key factors affecting mucoadhesion are related to the polymer properties, such as molecular weight, concentration, flexibility, and spatial conformation, as well as environmental and physiological factors. Mucoadhesive systems can provide benefits like prolonged drug residence at the site of action and increased drug absorption.
ocular barriers and methods to overcome barriersTarun Gollapudi
This document summarizes barriers to ocular drug delivery and methods to overcome them. The major barriers include ocular surface barriers like the cornea, ocular wall barriers like the sclera, retinal barriers, the vitreous body, lachrymal fluid, and properties of the drug itself like solubility and molecular weight. Methods to enhance delivery include microneedles, ultrasound, iontophoresis, periocular routes, and intravitreal injections. Various ophthalmic formulations are also discussed like eye drops, gels, ointments, and inserts that utilize approaches like prodrugs, penetration enhancers, and nanoparticle carriers to improve ocular bioavailability.
Intrauterine & Intravaginal Drug Delivery SystemPRASHANT DEORE
This document discusses intrauterine and intravaginal drug delivery systems. It begins with an introduction and overview of anatomy and physiology of the female reproductive system. It then describes various types of intravaginal drug delivery systems including suppositories, bioadhesive semisolids, elastomeric rings, and solid polymeric carriers. Factors affecting vaginal drug absorption are also discussed. The document concludes by describing intrauterine drug delivery systems including non-hormonal and hormonal IUDs, and discussing advantages and disadvantages of both intravaginal and intrauterine systems.
Application Of Polymer In Controlled Release FormulationAnindya Jana
Polymers are becoming increasingly important in the field of drug delivery. The pharmaceutical applications of polymers range from their use as binders in tablets to viscosity and flow controlling agents in liquids, suspensions and emulsions. Polymers can be used as film coatings to disguise the unpleasant taste of a drug, to enhance drug stability and to modify drug release characteristics.
As a consequence, increasing attention has been focused on methods of giving drugs continually for a prolonged time periods and in a controlled fashion.
This technology now spans many fields and includes pharmaceutical, food and agricultural applications, pesticides, cosmetics, and household products.
Barriers and routes of occular drug delivery systemShresthaPandey1
The document discusses various barriers to ocular drug delivery and routes to overcome these barriers. The key barriers include anatomical barriers like the cornea and conjunctiva, physiological barriers like tear turnover and drainage, and blood-ocular barriers. Methods to improve bioavailability and provide controlled drug delivery include adjusting viscosity, using prodrugs, penetration enhancers, and ocular inserts. Inserts can be non-erodible like Ocusert or erodible like Lacriserts, SODI, and Mindisc to continuously deliver drugs to the eye.
This document discusses various approaches to developing implantable drug delivery systems, including controlled drug delivery via diffusion, activation processes, and feedback regulation. It describes systems that use polymer membranes, matrices, microreservoirs, and hybrid designs to control drug release rates. Activation methods include osmotic pressure, vapor pressure, magnetism, hydration, and hydrolysis. Feedback systems can be regulated by bioerosion and bioresponses to biochemical factors. The document provides examples of implantable systems and discusses how drug and system properties influence release kinetics.
The document discusses ocular drug delivery and barriers to drug permeation in the eye. It describes the anatomy of the eye and mechanisms of drug absorption through corneal and non-corneal routes. The major barriers to ocular drug delivery are precorneal drainage, blinking, lacrimation, and barriers posed by the cornea, conjunctiva, sclera, blood-ocular barriers, and physiological factors. Methods to overcome these barriers include alternative delivery routes like intravitreal injections and novel drug delivery systems providing controlled release and improved permeability. Conventional systems like solutions, suspensions, and ointments have limitations like poor bioavailability and frequent dosing that novel particulate and vesicular systems aim to address.
The document discusses the physics of tablet compression. It describes the processes of compaction, consolidation and compression that tablets undergo in their production. It outlines the main stages of compression including particle rearrangement, deformation, fragmentation and bonding. It also discusses the forces involved and common compaction profiles and equations used to describe the process, including the Heckel and Kawakita equations. The document provides an overview of the key concepts and stages in understanding the physics behind tablet production through compression.
History of computers in pharmaceutical research and developmentZahid1392
Computers have been used in pharmaceutical research since the 1940s, starting with early machines like the IBM 650. Over subsequent decades, computational approaches like quantum chemistry, molecular mechanics, molecular simulations, and QSAR grew alongside increasing computer power. The 1980s saw many of these approaches combine into modern computational chemistry. By the 1990s, computer-based drug discovery was yielding new drugs, as workstations and supercomputers assisted research. Computational chemistry experts now play an important role in pharmaceutical research and development.
This document discusses rheological additives used in cosmetics. It begins with an introduction to rheology and how it relates to cosmetics performance. It then classifies rheological additives into aqueous-phase and non-aqueous phase additives. The main types of aqueous additives discussed are associative thickeners, hectorite, and bentone hydrophilic clays. For non-aqueous additives, it covers bentone organophilic clays, bentone gel, and thixcin r additive. It concludes by listing some applications of these additives and citing references.
The document provides an overview of optimization techniques used in pharmaceutical formulation and processing. It begins by defining optimization and its importance in developing drug products that meet bioavailability and mass production requirements. The key parameters of optimization discussed are problem type (constrained vs unconstrained), variables (independent vs dependent), and application areas (formulation vs processing). Several optimization techniques are then outlined, including evolutionary operations, simplex method, Lagrangian method, search method, and canonical analysis. Examples of each technique are provided, such as using simplex to optimize an analytical method or the Lagrangian method to optimize tablet formulation based on two variables.
Factors affecting design of Controlled Release Drug Delivery Systems (write-up)Suraj Choudhary
This document discusses factors affecting the design of controlled release drug delivery systems (CRDDS). It outlines several key considerations including selection of the drug candidate based on properties like solubility and half-life. It also discusses medical rationales like dosing frequency and patient compliance. Biological factors that influence absorption, distribution, and elimination are examined. Physicochemical properties of the drug like solubility, molecular size, and ionization must also be considered. The document provides an in-depth overview of factors involved in developing an effective CRDDS formulation.
Microencapsulation techniques involve coating small particles of core materials with thin layers of coating materials to form microcapsules. Some common microencapsulation techniques described in the document include coacervation, interfacial polymerization, in situ polymerization, and solvent evaporation. Microencapsulation can be used to increase bioavailability, alter drug release profiles, mask tastes, and enable targeted drug delivery.
Microencapsulation is a process where core materials are surrounded by a coating to form microparticles or microcapsules between 3-800 μm in size. It can be used to increase bioavailability, alter drug release, improve compliance, enable targeted delivery, and mask tastes. Various techniques like coacervation, spray drying, solvent evaporation, and pan coating can be used. Polymers are common coating materials and microencapsulation can protect core materials, control reactivity, and convert liquids to solids. The microparticles are evaluated based on morphology, drug content, particle size, and dissolution studies.
The document discusses the level of detail that should be provided about active pharmaceutical ingredients (APIs), excipients, finished products, and packaging materials when transferring technology from a source unit (SU) to a recipient unit (RU). For APIs, the SU should provide information such as the manufacturer, synthesis process, impurities, and stability studies. For excipients, the SU should detail the manufacturer, category, properties like solubility, and specifications for different dosage forms. The finished product specifications, storage conditions, and analytical test procedures should also be transferred. Finally, the SU should inform the RU about the suitable packaging, labeling, and ensure the packaging will not degrade the product.
This document discusses gastroretentive drug delivery systems (GRDDS), which are oral dosage forms designed to remain in the stomach for an extended period of time to prolong drug release. It covers the rationale for using GRDDS, factors controlling gastric residence time, and various approaches for prolonging gastric retention including floating systems, high-density systems, and bioadhesive or magnetic systems. Floating systems include non-effervescent and effervescent types that float due to low density or gas generation. High-density systems do not float but remain in the stomach through bioadhesion, magnetic forces, swelling to a large size, or raft formation on gastric fluids.
Buccal drug delivery systems provide a promising route for drug administration. They allow drugs to bypass first-pass metabolism by absorbing through the buccal mucosa into the systemic circulation via the facial veins. This presentation discusses buccal tablets, patches, films, gels and ointments as potential dosage forms. Key advantages are ease of administration, termination of therapy, and localization of drug in the oral cavity. However, drugs must not irritate oral tissues and must be stable at buccal pH levels. Evaluation parameters for these systems include residence time, permeation, swelling, release rate and toxicity studies. Some commercial buccal products are used to treat nausea, angina and oral infections.
Activation modulated drug delivery systemsSonam Gandhi
This document discusses different types of activation modulated drug delivery systems (DDS). It describes DDS that are activated by physical, chemical, or biological means. Some examples of physically activated DDS include osmotic pressure-activated, hydrodynamic pressure-activated, vapour pressure-activated, and mechanically activated systems. Magnetically activated and sonophorosis activated DDS are also mentioned. The document provides details on the mechanisms and equations for rate of drug release for some of these systems. It further discusses iontophoresis-activated and hydration-activated DDS and provides one example for each.
Optimization techniques in pharmaceutical formulation and processingReshma Fathima .K
This document discusses various optimization techniques used in pharmaceutical formulation and processing. It defines optimization as making something as perfect or effective as possible. The advantages of optimization include reducing costs, saving time, and improving safety, reproducibility, and efficacy. Key optimization parameters discussed include problem type (constrained or unconstrained), variables (independent and dependent), and applied optimization methods like evolutionary operation, simplex method, search method, Lagrangian method, and canonical analysis.
Easy & to the point Topics are clearly given in this presentation..
Thanks & Best Regard
(Anurag Pandey) B.Pharm
Contact :- anurag.dmk05@gmail.com (Facebook & Gmail both)
Controlled Release Drug Delivery Systems - Types, Methods and ApplicationsSuraj Choudhary
This document discusses factors affecting the design of controlled release drug delivery systems (CRDDS). It outlines several key considerations for CRDDS design including selection of the drug candidate, medical and biological rationale, and physicochemical properties. It also discusses important physicochemical factors such as solubility, partition coefficient, molecular size and diffusivity, dose size, complexation, ionization constant, drug stability, and protein binding that influence CRDDS design. Finally, it briefly describes dissolution-controlled and diffusion-controlled release approaches for developing CRDDS.
Building blocks of different product formulations of cosmeticsAlexa Jacob
This document provides information on building blocks for different product formulations of cosmetics. It discusses the definition, ingredients, general formulas, manufacture and evaluation of moisturizing cream, vanishing cream, cold cream, shampoo, toothpaste, soap and syndet bar. Specific formulas and preparation procedures are provided for moisturizing cream, vanishing cream and cold cream. Key ingredients for different cosmetic products are also outlined, including oils, fats, waxes, emulsifying agents and preservatives. Methods of evaluating different properties of creams such as pH, viscosity, spreadability and stability studies are also summarized.
The document discusses the Common Technical Document (CTD) and electronic CTD (eCTD) formats used for submitting registration documents to international regulatory agencies. The CTD format organizes documents into 5 modules: Module 1 contains administrative information specific to each region; Module 2 contains summaries of quality, non-clinical, and clinical information; Module 3 contains quality/manufacturing data; Module 4 contains non-clinical study reports; and Module 5 contains clinical study reports. The eCTD format is the electronic version of CTD, with documents in PDF format linked together via an XML backbone for easier navigation and review compared to the paper CTD format.
This document provides information about intrauterine drug delivery systems (IUDs). It discusses the anatomy and physiology of the female reproductive system. It describes the types of IUDs including non-hormonal copper IUDs and hormonal IUDs like Progestasert that release progesterone. The advantages of IUDs include avoiding first-pass metabolism and providing localized drug delivery. Applications of IUDs include emergency contraception, treatment for heavy menstrual bleeding and menopausal hormone therapy.
This document discusses various approaches to developing implantable drug delivery systems, including controlled drug delivery via diffusion, activation processes, and feedback regulation. It describes systems that use polymer membranes, matrices, microreservoirs, and hybrid designs to control drug release rates. Activation methods include osmotic pressure, vapor pressure, magnetism, hydration, and hydrolysis. Feedback systems can be regulated by bioerosion and bioresponses to biochemical factors. The document provides examples of implantable systems and discusses how drug and system properties influence release kinetics.
The document discusses ocular drug delivery and barriers to drug permeation in the eye. It describes the anatomy of the eye and mechanisms of drug absorption through corneal and non-corneal routes. The major barriers to ocular drug delivery are precorneal drainage, blinking, lacrimation, and barriers posed by the cornea, conjunctiva, sclera, blood-ocular barriers, and physiological factors. Methods to overcome these barriers include alternative delivery routes like intravitreal injections and novel drug delivery systems providing controlled release and improved permeability. Conventional systems like solutions, suspensions, and ointments have limitations like poor bioavailability and frequent dosing that novel particulate and vesicular systems aim to address.
The document discusses the physics of tablet compression. It describes the processes of compaction, consolidation and compression that tablets undergo in their production. It outlines the main stages of compression including particle rearrangement, deformation, fragmentation and bonding. It also discusses the forces involved and common compaction profiles and equations used to describe the process, including the Heckel and Kawakita equations. The document provides an overview of the key concepts and stages in understanding the physics behind tablet production through compression.
History of computers in pharmaceutical research and developmentZahid1392
Computers have been used in pharmaceutical research since the 1940s, starting with early machines like the IBM 650. Over subsequent decades, computational approaches like quantum chemistry, molecular mechanics, molecular simulations, and QSAR grew alongside increasing computer power. The 1980s saw many of these approaches combine into modern computational chemistry. By the 1990s, computer-based drug discovery was yielding new drugs, as workstations and supercomputers assisted research. Computational chemistry experts now play an important role in pharmaceutical research and development.
This document discusses rheological additives used in cosmetics. It begins with an introduction to rheology and how it relates to cosmetics performance. It then classifies rheological additives into aqueous-phase and non-aqueous phase additives. The main types of aqueous additives discussed are associative thickeners, hectorite, and bentone hydrophilic clays. For non-aqueous additives, it covers bentone organophilic clays, bentone gel, and thixcin r additive. It concludes by listing some applications of these additives and citing references.
The document provides an overview of optimization techniques used in pharmaceutical formulation and processing. It begins by defining optimization and its importance in developing drug products that meet bioavailability and mass production requirements. The key parameters of optimization discussed are problem type (constrained vs unconstrained), variables (independent vs dependent), and application areas (formulation vs processing). Several optimization techniques are then outlined, including evolutionary operations, simplex method, Lagrangian method, search method, and canonical analysis. Examples of each technique are provided, such as using simplex to optimize an analytical method or the Lagrangian method to optimize tablet formulation based on two variables.
Factors affecting design of Controlled Release Drug Delivery Systems (write-up)Suraj Choudhary
This document discusses factors affecting the design of controlled release drug delivery systems (CRDDS). It outlines several key considerations including selection of the drug candidate based on properties like solubility and half-life. It also discusses medical rationales like dosing frequency and patient compliance. Biological factors that influence absorption, distribution, and elimination are examined. Physicochemical properties of the drug like solubility, molecular size, and ionization must also be considered. The document provides an in-depth overview of factors involved in developing an effective CRDDS formulation.
Microencapsulation techniques involve coating small particles of core materials with thin layers of coating materials to form microcapsules. Some common microencapsulation techniques described in the document include coacervation, interfacial polymerization, in situ polymerization, and solvent evaporation. Microencapsulation can be used to increase bioavailability, alter drug release profiles, mask tastes, and enable targeted drug delivery.
Microencapsulation is a process where core materials are surrounded by a coating to form microparticles or microcapsules between 3-800 μm in size. It can be used to increase bioavailability, alter drug release, improve compliance, enable targeted delivery, and mask tastes. Various techniques like coacervation, spray drying, solvent evaporation, and pan coating can be used. Polymers are common coating materials and microencapsulation can protect core materials, control reactivity, and convert liquids to solids. The microparticles are evaluated based on morphology, drug content, particle size, and dissolution studies.
The document discusses the level of detail that should be provided about active pharmaceutical ingredients (APIs), excipients, finished products, and packaging materials when transferring technology from a source unit (SU) to a recipient unit (RU). For APIs, the SU should provide information such as the manufacturer, synthesis process, impurities, and stability studies. For excipients, the SU should detail the manufacturer, category, properties like solubility, and specifications for different dosage forms. The finished product specifications, storage conditions, and analytical test procedures should also be transferred. Finally, the SU should inform the RU about the suitable packaging, labeling, and ensure the packaging will not degrade the product.
This document discusses gastroretentive drug delivery systems (GRDDS), which are oral dosage forms designed to remain in the stomach for an extended period of time to prolong drug release. It covers the rationale for using GRDDS, factors controlling gastric residence time, and various approaches for prolonging gastric retention including floating systems, high-density systems, and bioadhesive or magnetic systems. Floating systems include non-effervescent and effervescent types that float due to low density or gas generation. High-density systems do not float but remain in the stomach through bioadhesion, magnetic forces, swelling to a large size, or raft formation on gastric fluids.
Buccal drug delivery systems provide a promising route for drug administration. They allow drugs to bypass first-pass metabolism by absorbing through the buccal mucosa into the systemic circulation via the facial veins. This presentation discusses buccal tablets, patches, films, gels and ointments as potential dosage forms. Key advantages are ease of administration, termination of therapy, and localization of drug in the oral cavity. However, drugs must not irritate oral tissues and must be stable at buccal pH levels. Evaluation parameters for these systems include residence time, permeation, swelling, release rate and toxicity studies. Some commercial buccal products are used to treat nausea, angina and oral infections.
Activation modulated drug delivery systemsSonam Gandhi
This document discusses different types of activation modulated drug delivery systems (DDS). It describes DDS that are activated by physical, chemical, or biological means. Some examples of physically activated DDS include osmotic pressure-activated, hydrodynamic pressure-activated, vapour pressure-activated, and mechanically activated systems. Magnetically activated and sonophorosis activated DDS are also mentioned. The document provides details on the mechanisms and equations for rate of drug release for some of these systems. It further discusses iontophoresis-activated and hydration-activated DDS and provides one example for each.
Optimization techniques in pharmaceutical formulation and processingReshma Fathima .K
This document discusses various optimization techniques used in pharmaceutical formulation and processing. It defines optimization as making something as perfect or effective as possible. The advantages of optimization include reducing costs, saving time, and improving safety, reproducibility, and efficacy. Key optimization parameters discussed include problem type (constrained or unconstrained), variables (independent and dependent), and applied optimization methods like evolutionary operation, simplex method, search method, Lagrangian method, and canonical analysis.
Easy & to the point Topics are clearly given in this presentation..
Thanks & Best Regard
(Anurag Pandey) B.Pharm
Contact :- anurag.dmk05@gmail.com (Facebook & Gmail both)
Controlled Release Drug Delivery Systems - Types, Methods and ApplicationsSuraj Choudhary
This document discusses factors affecting the design of controlled release drug delivery systems (CRDDS). It outlines several key considerations for CRDDS design including selection of the drug candidate, medical and biological rationale, and physicochemical properties. It also discusses important physicochemical factors such as solubility, partition coefficient, molecular size and diffusivity, dose size, complexation, ionization constant, drug stability, and protein binding that influence CRDDS design. Finally, it briefly describes dissolution-controlled and diffusion-controlled release approaches for developing CRDDS.
Building blocks of different product formulations of cosmeticsAlexa Jacob
This document provides information on building blocks for different product formulations of cosmetics. It discusses the definition, ingredients, general formulas, manufacture and evaluation of moisturizing cream, vanishing cream, cold cream, shampoo, toothpaste, soap and syndet bar. Specific formulas and preparation procedures are provided for moisturizing cream, vanishing cream and cold cream. Key ingredients for different cosmetic products are also outlined, including oils, fats, waxes, emulsifying agents and preservatives. Methods of evaluating different properties of creams such as pH, viscosity, spreadability and stability studies are also summarized.
The document discusses the Common Technical Document (CTD) and electronic CTD (eCTD) formats used for submitting registration documents to international regulatory agencies. The CTD format organizes documents into 5 modules: Module 1 contains administrative information specific to each region; Module 2 contains summaries of quality, non-clinical, and clinical information; Module 3 contains quality/manufacturing data; Module 4 contains non-clinical study reports; and Module 5 contains clinical study reports. The eCTD format is the electronic version of CTD, with documents in PDF format linked together via an XML backbone for easier navigation and review compared to the paper CTD format.
This document provides information about intrauterine drug delivery systems (IUDs). It discusses the anatomy and physiology of the female reproductive system. It describes the types of IUDs including non-hormonal copper IUDs and hormonal IUDs like Progestasert that release progesterone. The advantages of IUDs include avoiding first-pass metabolism and providing localized drug delivery. Applications of IUDs include emergency contraception, treatment for heavy menstrual bleeding and menopausal hormone therapy.
The document discusses vaginal drug delivery systems. It describes the anatomy and physiology of the vagina, factors that make it a favorable site for drug administration, and challenges related to its dynamic nature. It then summarizes different types of vaginal drug delivery vehicles including ointments, creams, gels, suppositories, tablets, rings and bioadhesive systems. Key benefits of vaginal drug delivery are avoiding first-pass metabolism and gastrointestinal interference while minimizing side effects.
The document discusses implants and inserts as drug delivery systems. It defines implants as single unit drug delivery systems designed to deliver a drug over a prolonged period of time. Implants can be biodegradable or non-biodegradable and come in various shapes, sizes, and drug release mechanisms. The document then discusses the advantages and disadvantages of implants, ideal characteristics, mechanisms of drug release including diffusion controlled and activated controlled systems, approaches to development, types of devices based on route of administration, and evaluation of implants.
Implants and transdermal patches can both be used to deliver drugs in a controlled manner. Implants are medical devices that are implanted inside the body to replace or support a biological structure. They consist of a reservoir, pump, power source and control circuitry. They provide advantages like convenience and compliance but have disadvantages like being invasive and requiring surgery. Transdermal patches adhere to the skin and deliver drugs through the skin and into the bloodstream. They have advantages like avoiding the digestive system and providing prolonged effects. Common types include single-layer, multi-layer, reservoir and matrix patches. Popular uses include nicotine, hormone and pain relieving patches. Both can effectively deliver drugs but have potential side effects and risks if
This document summarizes information about parental implants as a drug delivery system. It discusses that implants consist of a drug made by compression or molding into a solid mass for controlled release over a long period of time without repeated needle injections. The polymers used can be biodegradable or non-biodegradable. Implants are classified based on their drug release mechanisms and examples are provided of buprenorphine and naltrexone implants that are placed subcutaneously to treat opioid addiction over varying time periods. Evaluation methods for implants include weight variation, thickness measurement, in vitro drug release testing using a flow through cell.
Buccal drug delivery systems provide a promising route for drug administration. They allow drugs to bypass first-pass metabolism by absorbing through the buccal mucosa into the systemic circulation via the facial vein. This presentation discusses buccal tablets, patches, films, gels and ointments as potential dosage forms. Key advantages are ease of administration, rapid drug absorption, and reduced side effects compared to oral routes. Challenges include limited drug loading and ensuring adhesion of the dosage form to the buccal mucosa. Overall, buccal delivery is a useful alternative for delivering drugs that are unstable or poorly bioavailable through oral administration.
Protein and peptide drugs can be delivered through various routes including parenteral, oral, buccal, nasal, transdermal, pulmonary, rectal, ocular, and vaginal administration. Various drug delivery systems are used to protect proteins from degradation and control release over time. These include microencapsulation, polymeric scaffolds, liposomes, magnetic targeting, and hydrogels. Recent advances provide more effective noninvasive delivery methods for these therapeutic compounds.
Family planning involves methods of birth control to plan when to have children. It aims to ensure resources are available to raise children and improve maternal and child health. Ideal contraceptives should be safe, reliable, easy to use, cost effective, and culturally acceptable. Common family planning methods include natural methods, barrier methods like condoms and diaphragms, hormonal methods like pills and IUDs, and terminal methods like vasectomy and tubectomy. Reproductive health aims for complete well-being and involves family planning, counseling, education, and treatment of infections and conditions to prevent and solve reproductive health problems.
This document discusses various drug delivery technologies used by companies like Cipla to develop targeted therapies. It describes nanotechnology used to deliver drugs to specific cell types via engineered nanoparticles. Microsphere and microparticulate technologies are used for targeted and sustained delivery via injection or oral formulations. Liposomes, hot melt extrusion, and osmotic controlled release systems are also outlined as technologies to modify drug properties and target delivery. The aim is to improve efficacy, safety, and patient compliance through specialized delivery approaches.
RECENT ADVANCES IN COLON TARGETED DRUG DELIVERYVarun Girme
This document summarizes recent advances in colon targeted drug delivery. It discusses the anatomy and physiology of the colon, pharmaceutical approaches for targeting drugs to the colon like prodrug conjugates and coating technologies, evaluation methods for colon delivery systems including in vitro dissolution tests and gamma scintigraphy imaging. It also presents a case study on the formulation of 5-fluorouracil loaded chitosan nanoparticles with Eudragit S100 coating for colon cancer treatment, showing enhanced localized drug release at colonic pH.
This document provides information on family planning and contraceptive methods. It defines family planning as individuals and couples attaining their desired number and timing of children through contraceptive use or infertility treatment. The main contraceptive methods discussed are barrier methods, combined hormonal contraception, and progesterone-only hormonal contraception. Combined methods contain estrogen and progesterone while progesterone-only methods only contain progesterone. Barrier methods include condoms and diaphragms while combined options include oral contraceptive pills, transdermal patches, and vaginal rings. Hormonal contraception is typically more effective than barrier methods at preventing pregnancy.
There are several types of implant drug delivery systems. Implantable devices can provide controlled release of drugs over long periods of time without needing repeated injections or pills. Common examples include contraceptive implants like Nexplanon that prevent pregnancy for 3 years, histrelin implants for prostate cancer and precocious puberty, buprenorphine implants for opioid dependence treatment, and naltrexone implants to reduce cravings for opioids. Implant drug delivery offers advantages of patient convenience and targeting drug release, though some minor surgery is required for insertion and removal.
1. PRESENTED BY
DEORE PRASHANT ASHOK
Department of Pharmaceutics
M. Pharm. II Semester (2014-2015)
Intrauterine & Intravaginal
Drug Delivery System
R. C. Patel Institute of Pharmaceutical Education
and Research, Shirpur .
1
Email-prashantdeore92@gmail.com Mo.09881261646
3-Mar-15
3. Introduction
• Vagina and Uterus are the route for administration of contraceptives ,
antifungals and antimicrobials.
• These are used for local or systemic absorption.
• Because of vast network of blood vessels, vaginal wall is suitable for
dug absorption.
• The rate and extent of drug absorption may vary depends upon
1) Formulation factors
2) Physiology
3) Age of patient
4) Menstrual cycle
3-Mar-15 3
5. Vulva
Basic 5 parts involved:
• Mons pubis
• Labia majora
• Labia minora
• Clitoris
• vestibules
3-Mar-15
Vagina
• Muscular canal about 3 inches long.
• Normal pH of vagina in premenopausal female ranges from
4.5 & rises upto 7 in postmenopausal female.
• Vaginal wall surface is covered with epithelium cells.
• Size: in premenopausal female 7.8 cm in length & 2 cm
wide, in postmenopausal female 4.5 cm in length & 1-1.5
cm in width.
5
6. Uterus
• Non pregnant uterus is around 7.5cm long,
5cm wide and 2.5cm thick.
• Endometrium is highly vascular made up of
simple columnar epithelium and highly
sensitive to hormonal secretions of ovary.
• During complete cycle endometrium goes on
thickening with hormonal impact.
3-Mar-15
Fallopian tubes
• Also called ‘Oviducts’ or ‘Uterine tubes’,
around 10 cm long.
• The end portion is opened and funnel shaped
containing finger like projection called
“Fimbriae”.
• Internal surface is of ciliated columnar
epithelium cells.
6
7. Ovary
• Two ovaries, one on either side of the
uterus.
• These are having shape and size of
unshelled almonds.
• There are ovarian follicles containing
oocytes in various stages of
development.
3-Mar-15
• Matured follicle which releases secondary oocyte is called Graafian
follicle.
• Ovaries produces hormones including progesterone and estrogen,
inhibin and relaxin.
7
8. Intravaginal Drug Delivery System
• Traditionally used system as contraceptive and to treat vaginal
infections.
• The formulations given by this route are in solid, liquid and semisolid
system.
• It may be intended for local effect or systemic action.
• Systemic absorption by dense network of blood vessels is advantage
over oral route.
• The first truly controlled drug delivery systems for used in vagina
were developed in 1970, when the first vaginal ring was used for
delivery of medroxyprogesterone acetate for contraception.
• Vaginal rings are most common long term drug delivery system
currently used.
3-Mar-15 8
9. Factors affecting vaginal drug
absorption
• It is important to design formulation as well as device used for
administration.
• Factors can be categorized as:
1) Physiological factors:-
Factors related to the vaginal physiology include:
a. pH of vagina (3.5- 4.9)
b. Effect of menstrual cycle on permeability of vaginal epithelium
c. Vaginal fluid volume
d. Viscosity of vaginal fluid
e. Pressure exerted by rectal wall on dosage form affect vaginal blood
flow.
3-Mar-15 9
10. 2) Physicochemical factors:-
• Factors related to physico-chemical properties of drug such as:
a. Viscosity (semisolids)
b. Concentration and Volume for administration
c. Type of dosage form
d. Molecular size of drug
3-Mar-15 10
11. Ideality of Intravaginal DDS
1) Component should melt at vaginal temperature i.e. at 37oC.
2) Device should be nontoxic and nonirritating.
3) Formulation should be nonsensitive on vaginal pH.
4) Formulation should have wetting and emulsifying properties.
5) It should be stable on storage.
6) Formulation should have proper viscosity to avoid leakage of drug
from vagina (for semisolid).
7) Formulation should have proper bioadhesive properties to increase
contact time between membrane and formulation.
3-Mar-15 11
12. Classification of Intravaginal DDS
A. Localized :
1) Barrier contraception
(Diaphragm, Cervical cap,
Sponge)
2) Prevention/Treatment of infection
( Gels, Cream, Ointment)
3-Mar-15 12
13. B. Systemic :
A. Suppositories or pessaries.
B. Bio(muco)adhesive semisolids.
• These are emulsion bases formulation
to deliver antifungal agents such as
imidazole. Give controlled delivery
for 3 or more hrs.
3-Mar-15 13
14. b. Elastomeric intravaginal rings( IVR):
1) Matrix (homogeneous dispersion)
2) Reservoir (core)
3) Sandwich (shell)
Elastomer exert slight tension on vaginal wall,
more suitable for hydrophobic drugs.
Normally designed to contain steroidal
hormones.
3-Mar-15
C. Solid polymeric carriers.
a. Solid hydrogels:
Having swelling property which enables the
drug to diffuse out of the macromolecular
network.
eg. Nu-gel ( Johnson & Johnson)
14
15. 1) Matrix type :-
• Drug is homogeneously dispersed through out
the polymer matrix.
• Drug release from this type follows First order.
2) Reservoir type:-
• Drug is located within the centralized core that
is surrounded by drug free silicon sheath acts as
rate controlling membrane for drug diffusion.
• It follows Zero order fashion.
3) Sandwich type:-
• Consists of narrow drug containing layer
positioned between non-medicated impervious
central core & non-medicated outer rate
controlling band.
• Small and constant release of drug.
3-Mar-15 15
16. Other novel approaches :
1) Medicated Vaginal Tampons- A medicated vaginal tampon,
approved as a medical device by the Food and Drug Administration
(FDA) .
• This bifunctional tampon contains a polymeric delivery system
(strips) that absorb menstrual fluid while gradually releasing lactic
acid and citric acid.
• eg. Brilliant pH tampons
3-Mar-15 16
17. 2) Vaginal Films-
• Vaginal films are polymeric drug delivery systems shaped as thin
sheets, usually ranging from 220 to 240 μ m in thickness.
• These systems are often square (approximately 5cm × 5cm),
colorless, and soft, presenting a homogenous surface.
• Vaginal films are produced with polymers such as polyacrylates,
polyethylene glycol, polyvinyl alcohol, and cellulose derivatives.
• eg.VCF (vaginal contraceptive films)
3-Mar-15 17
18. Advantages
• Minimal systemic side effects.
• Irritation to the stomach and small intestine associated with some
drugs can be avoided.
• An increase in bioavailability.
• First pass metabolism can be avoided.
• Contact with digestive fluid is avoided, thereby preventing enzymatic
degradation of some drugs.
• Self medication is possible.
• Drug delivery can be stopped by removing the dosage form. e.g.
vaginal rings
• Rapid drug absorption and quick onset of action can be achieved.
• The vaginal bioavailability of smaller drug molecule is good.
• The bioavailability of larger drug molecules can be improved by means
of absorption enhancer.
3-Mar-15 18
19. Disadvantages
• Patient incompliance.
• Only few drugs are administered by this route.
• Some of the drugs are sensitive at the vaginal pH.
• Local irritation because some drugs variability in drug absorption related
with menstrual cycle, menopause and pregnancy.
• Gender specificity.
• Influence with sexual intercourse.
• Some time leakage of drugs from vagina and wetting of undergarments.
3-Mar-15 19
20. Animal models
Vaginal mucosa permeability:-
1) The fundamentals of vaginal absorption of drug can be
studied on female rabbits.
2) It doesn’t exhibit an estrus cycle so its vaginal tissues
shows consistency in the histological, biochemical
and physiological properties not ordinarily seen in
other mammals.
3) But the rabbits may not be suitable for CR dosage
forms due to lack of estrus cycle.
4) Rhesus monkeys are excellent animal model for CR
dosage form as they are having estrus cycle of approx
28 days like human female.
3-Mar-15 20
21. Intrauterine DDS (IUDs)
Types of IUDs for controlled drug delivery:-
1) Non-hormonal IUDs. (Ex. copper-T, copper-7)
2) Hormonal IUDs. ( Ex. Progestasert)
1) Non-hormonal IUDs/ copper medicated IUDs.
• It is consists of polyethylene or polypropylene plastic
support of number-7 or letter-T with certain amount of
pure electrolytic copper wire wound around them.
• Copper is cytotoxic and enhance spermicidal &
spermatodepressive action of IUD.
• The exposed surface area of copper is 380 mm2
.
• T-shaped IUD is popular since shape conforms to the
uterine cavity which resists displacement & rotation
within cavity and expulsion from cavity
• Types- Cu T-200--------200 mm².
Cu T-30---------30 mm².
3-Mar-15 21
22. 2) Hormonal IUDs.
• T-shaped device made of polyethylene frame
that measures 32 mm in both vertical and
horizontal direction.
• There is silicone reservoir containing dispersed
levonogestrel or progesterone on vertical stem
and further enclosed in a sleeve of rate
controlling membrane of ethylene-vinyl
copolymer.
• It prevents pregnancy up to 5 yrs by steadily
releasing small amount of progesterone directly
in to uterus.
• It works by thickening the cervical mucous so
that sperm have more difficulty to swim through
uterus.
• For some women it may also prevent ovulation
from occurring.
3-Mar-15 22
23. Advantages
Non-hormonal:-
• Safe.
• Immediately and highly effective.
• Long term (up to 10 yrs) effect- Freedom from having to remember to
use contraceptives regularly or at the time of intercourse.
• Cost effective (no on going cost after initial insertion)
• Reversible (rapid return of fertility after removal).
3-Mar-15 23
24. Hormonal :-
• After about 5 months nearly all women will experience light periods
only.
• After 12 months about 20% of women will have no periods at all.
• Can be used to treat excessively heavy menstrual bleeding
• Reduces period pain in many women.
• May be suitable for women approching menopause as it provides
effective contraception and can continue to be used as the
progesteron component for hormone replacement therapy.
3-Mar-15 24
25. Disadvantages
Non-hormonal:-
• Requires visit to trained physician for insertion and removal.
• Some risk of expulsion within first year.
• for some women, increased menstrual bleeding and cramping.
• Lack of protection against STDs, including HIV.
Hormonal :-
• Irregular bleeding pattern in the early stages (irregular bleeding and
cramping during first few weeks or months after insertion.)
• Some women experiences backache for several days or weeks after
insertion.
• Nausea, headache.
• Weight gain.
3-Mar-15 25
26. References
• Chien Y. W. (2007), Novel Drug Delivery Systems, Revised and
Expanded, Marcel Dekker, Inc., New York, Second Indian Reprint , Vol.-
50, p. 529-629.
• Tortora G. J. & Grabowski S. R. (2003), Principles of Anatomy &
Physiology, 10th edition, p.1028-1039.
• Brahmankar D. M. & Jaiswal S. B. (2009), Biopharmaceutics and
Pharmacokinetics A Treatise, 2nd edition, Vallabh Prakashan, p. 502-508.
• Bandyopadhyay A.K. (2008), Novel drug delivery system, 1st edition,
Everest publishing house, p. 215-220.
• Keshwani Bhawana & Arora Pankaj (2014), Novel concepts in vaginal
drug delivery, Journal of Pharma research, 3 (10) 184-187.
• Chatterjee Arkendu & Kumar Lalit (2009), On overview of Intra-vaginal
Drug delivery system, Journal of Pharmacy research, 2 (4) 698-700.
3-Mar-15 26