BCS is a scientific framework for classifying drug substances based on their aqueous solubility and intestinal permeability.
It is a drug development tool that allows estimation of solubility, dissolution and intestinal permeability affect that oral drug absorption.
Kashikar V S
PES Modern College of Pharmacy ( for ladies), Moshi Pune
“ Bioavailability-
means the rate and extent to which the active ingredient or active moiety is absorbed from a drug product and becomes available at the site of action."
Biopharmaceutic considerations in drug product design and In Vitro Drug Produ...PRAJAKTASAWANT33
Introduction, biopharmaceutic factors affecting drug bioavailability, rate–limiting steps in drug absorption, physicochemical nature of the drug formulation factors affecting drug product performance
“ Bioavailability-
means the rate and extent to which the active ingredient or active moiety is absorbed from a drug product and becomes available at the site of action."
Biopharmaceutic considerations in drug product design and In Vitro Drug Produ...PRAJAKTASAWANT33
Introduction, biopharmaceutic factors affecting drug bioavailability, rate–limiting steps in drug absorption, physicochemical nature of the drug formulation factors affecting drug product performance
A brief presentation on the factors affecting bioavailability of drugs along with a quick overview on what is bioequivalence, clinical equivalence, therapeutic equivalence, chemical equivalence and pharmaceutical equivalence.
Bio pharmaceutical classification System [BCS]Sagar Savale
The Biopharmaceutical Classification System was first developed by in 1995, by Amidon et al & his colleagues.
Definition:
“The Biopharmaceutical Classification System is a scientific framework for classifying a drug substance based on its aqueous solubility & intestinal permeability & dissolution rate”.
To saved time fast screening is required so drug substances are classified on basis of solubility and permeability. This classification is called Biopharmaceutical Classification System
Biopharmaceutic considerations in Drug Product DesignRiaz Islam
Drug product Design remain one of the most challenging aspects in formulation development. But nowadays formulation strategies have been far more successful in improving the bioavailability of the compounds with poor solubility, poor dissolution rate, and poor chemical stability in acidic environment. This article begins with a brief discussion on Physical and Chemical Properties of the Drug Impacting Oral Absorption. This article also reviews the Factors Contributing to Poor Aqueous Solubility. and a brief relationship between Physicochemical Properties and Drug Delivery System.
A review on waiving in vivo bioequivalence tests or Biovaiwer, with a case review on the biowaiver monograph on Ibuprofen by H. POTTHAST, J.B. DRESSMAN, H.E. JUNGINGER, K.K. MIDHA, H. OESER, V.P. SHAH,
H. VOGELPOEL, D.M. BARENDS
in J Pharm Sci 94:2121–2131, 2005
Explaining different approaches to waive different BCS class medicines based on their solubility and permeability, as is described by FDA and WHO
Methods For Assesment Of Bioavailability Anindya Jana
Bioavailability means the rate and extent to which the active ingredient or active moiety is absorbed from a drug product and becomes available at the site of action. For drug products that are not intended to be absorbed into the bloodstream, bioavailability may be assessed by measurements intended to reflect the rate and extent to which the active ingredient or active moiety becomes available at the site of action.
Bioavailability studies are important in the Primary stages of development of a suitable dosage form for a new drug entity, determination of influence of excipients, patient related factors & possible interaction with other drugs on the efficiency of absorption, development of new formulations of the existing drugs, control of quality of a drug product during the early stages of marketing in order to determine the influence of processing factors, storage & stability on drug absorption
It contain the Per oral administration of drug ,
movement of drug through the GI Tract ; and according to that BCS Classification with BIOWAIVER Application.
A brief presentation on the factors affecting bioavailability of drugs along with a quick overview on what is bioequivalence, clinical equivalence, therapeutic equivalence, chemical equivalence and pharmaceutical equivalence.
Bio pharmaceutical classification System [BCS]Sagar Savale
The Biopharmaceutical Classification System was first developed by in 1995, by Amidon et al & his colleagues.
Definition:
“The Biopharmaceutical Classification System is a scientific framework for classifying a drug substance based on its aqueous solubility & intestinal permeability & dissolution rate”.
To saved time fast screening is required so drug substances are classified on basis of solubility and permeability. This classification is called Biopharmaceutical Classification System
Biopharmaceutic considerations in Drug Product DesignRiaz Islam
Drug product Design remain one of the most challenging aspects in formulation development. But nowadays formulation strategies have been far more successful in improving the bioavailability of the compounds with poor solubility, poor dissolution rate, and poor chemical stability in acidic environment. This article begins with a brief discussion on Physical and Chemical Properties of the Drug Impacting Oral Absorption. This article also reviews the Factors Contributing to Poor Aqueous Solubility. and a brief relationship between Physicochemical Properties and Drug Delivery System.
A review on waiving in vivo bioequivalence tests or Biovaiwer, with a case review on the biowaiver monograph on Ibuprofen by H. POTTHAST, J.B. DRESSMAN, H.E. JUNGINGER, K.K. MIDHA, H. OESER, V.P. SHAH,
H. VOGELPOEL, D.M. BARENDS
in J Pharm Sci 94:2121–2131, 2005
Explaining different approaches to waive different BCS class medicines based on their solubility and permeability, as is described by FDA and WHO
Methods For Assesment Of Bioavailability Anindya Jana
Bioavailability means the rate and extent to which the active ingredient or active moiety is absorbed from a drug product and becomes available at the site of action. For drug products that are not intended to be absorbed into the bloodstream, bioavailability may be assessed by measurements intended to reflect the rate and extent to which the active ingredient or active moiety becomes available at the site of action.
Bioavailability studies are important in the Primary stages of development of a suitable dosage form for a new drug entity, determination of influence of excipients, patient related factors & possible interaction with other drugs on the efficiency of absorption, development of new formulations of the existing drugs, control of quality of a drug product during the early stages of marketing in order to determine the influence of processing factors, storage & stability on drug absorption
It contain the Per oral administration of drug ,
movement of drug through the GI Tract ; and according to that BCS Classification with BIOWAIVER Application.
biopharmaceuticals classification system and biowaiverRavish Yadav
The all the content in this profile is completed by the teachers, students as well as other health care peoples.
thank you, all the respected peoples, for giving the information to complete this presentation.
this information is free to use by anyone.
Pharmacy presentation about BCS classification its criteria.Biowaiever and its conditions .permeability studies in vivo,invitro,in situ.mpharmacy b pharmacy pharmaceutics
Biopharmaceutical classification system & drug delivery system associated wit...PratikShinde120
Biopharmaceutical classification system & drug delivery system based on BCS.
By Pratik shinde, Mpharm, University department of pharmaceutical sciences, Nagpur
BCS Guideline for solubility and Dissolution.pptxImdad H. Mukeri
Briefly explanation of The Biopharmaceutics Classification System (BCS) of drug substance
and its solubility in the pH range of 1–7.5, absorption or intestinal membrane permeability
In this presentation I have mentioned whatever the possible relevant content/guidelines require for biowaiver application.
Citation Is done at the end of slide.
Content is up to date & true to my belief.
Thanks & Best Regards.
Anurag Pandey
B.Pharm (FACULTY OF PHARMACY, INVERTIS UNIVERSITY)
M.Pharm (INSTITUTE OF PHARMACY, NIRMA UNIVERSITY)
Email :- anurag.dmk05@gmail.com
Biopharmaceutics classification system class 1Aloysiatreslyn
Biopharmaceutics classification system class
defination,bcs,class1 drugs,physiochemical parameters,advantages,disadvantages,list of drugs,formulaton consideration,solubility,permability,disssolution etc .The Biopharmaceutics Classification System is a system to differentiate the drugs on the basis of their solubility and permeability. This system restricts the prediction using the parameters solubility and intestinal permeability.
Methods of enhancing Dissolution and bioavailability of poorly soluble drugsRam Kanth
Greetings!
Good Day to all...
Topic: Methods of Enhancing Bioavailability
Several approaches discussed are
1. Micrnoization
2. Use of Surrfactants
3. Use of Salt forms
4. Alteration of pH of microenvironment
5. Use of metastable polymorphs
6. Solute-Solvent Complexation
7. Solvent Deposition
8. Selective Adsorption on Insoluble Carriers
9. Solid Solutions
10. Eutectic Mixtures
11. Solid Dispersions
12. Molecular Encapsulation with Cyclodextrins
Please do clarify for doubts if any....
Thank you all for watching this presentation.
Compression : It is reduction in bulk volume of the material as a result of displacement of gaseous phase (entrapped air). When external force is applied to powder mass there is reduction in bulk volume. The onset of loading is associated with closed repacking of a powder mass followed by deformation.
Sustained Released Ophthalmic FormulationMcpl Moshi
Dr. V. S. Kashikar
Ophthalmic drug delivery is one of the most challenging endeavor facing the pharmaceutical scientists. The anatomy, physiology and biochemistry of the eye render this organ highly impervious to foreign substance.
Rapid and efficient drainage by the nasolacrimal apparatus, noncorneal absorption and the relative impermeability of the cornea to both hydrophilic and hydrophobic molecules, all account for such poor ocular bioavailability. Thus to increase the ocular bioavailability of drug, we need to increase the ocular residence time of the drug.
Quality audit is defined as a systematic and independent examination to determine whether activities and related results comply with planned arrangements and whether these arrangements are implemented effectively and are suitable to achieve objectives Quality audit means a systematic examination of a quality system
Quality audits are typically performed at defined intervals
.Definition
Objectives
Difference between Quality audit and Periodic evaluation
Self inspection
Types of Quality Audit
Role OF GMP Audit in QA and QC programmes
Elements of a Systemic Audit program
Dr. V. S. Kashikar
QUALITY CONTROL OF TABLETS IPQC stands for in process quality control. These are checks that are carried out before the manufacturing process is completed.
Career Guidance to First Year B. Pharm studentsMcpl Moshi
Career Guidance to First Year B. Pharm students
Induction Program
More recently, pharmacists have been faced with increasing health demands which change their direction and focus to PATIENTS instead of the Product.
Bioavailability and Bioequivalence studyMcpl Moshi
Bioavailability and Bioequivalence study, BCS is a scientific framework for classifying drug substances based on their aqueous solubility and intestinal permeability.
It is a drug development tool that allows estimation of solubility, dissolution and intestinal permeability affect that oral drug absorption.
Antibiotic Stewardship by Anushri Srivastava.pptxAnushriSrivastav
Stewardship is the act of taking good care of something.
Antimicrobial stewardship is a coordinated program that promotes the appropriate use of antimicrobials (including antibiotics), improves patient outcomes, reduces microbial resistance, and decreases the spread of infections caused by multidrug-resistant organisms.
WHO launched the Global Antimicrobial Resistance and Use Surveillance System (GLASS) in 2015 to fill knowledge gaps and inform strategies at all levels.
ACCORDING TO apic.org,
Antimicrobial stewardship is a coordinated program that promotes the appropriate use of antimicrobials (including antibiotics), improves patient outcomes, reduces microbial resistance, and decreases the spread of infections caused by multidrug-resistant organisms.
ACCORDING TO pewtrusts.org,
Antibiotic stewardship refers to efforts in doctors’ offices, hospitals, long term care facilities, and other health care settings to ensure that antibiotics are used only when necessary and appropriate
According to WHO,
Antimicrobial stewardship is a systematic approach to educate and support health care professionals to follow evidence-based guidelines for prescribing and administering antimicrobials
In 1996, John McGowan and Dale Gerding first applied the term antimicrobial stewardship, where they suggested a causal association between antimicrobial agent use and resistance. They also focused on the urgency of large-scale controlled trials of antimicrobial-use regulation employing sophisticated epidemiologic methods, molecular typing, and precise resistance mechanism analysis.
Antimicrobial Stewardship(AMS) refers to the optimal selection, dosing, and duration of antimicrobial treatment resulting in the best clinical outcome with minimal side effects to the patients and minimal impact on subsequent resistance.
According to the 2019 report, in the US, more than 2.8 million antibiotic-resistant infections occur each year, and more than 35000 people die. In addition to this, it also mentioned that 223,900 cases of Clostridoides difficile occurred in 2017, of which 12800 people died. The report did not include viruses or parasites
VISION
Being proactive
Supporting optimal animal and human health
Exploring ways to reduce overall use of antimicrobials
Using the drugs that prevent and treat disease by killing microscopic organisms in a responsible way
GOAL
to prevent the generation and spread of antimicrobial resistance (AMR). Doing so will preserve the effectiveness of these drugs in animals and humans for years to come.
being to preserve human and animal health and the effectiveness of antimicrobial medications.
to implement a multidisciplinary approach in assembling a stewardship team to include an infectious disease physician, a clinical pharmacist with infectious diseases training, infection preventionist, and a close collaboration with the staff in the clinical microbiology laboratory
to prevent antimicrobial overuse, misuse and abuse.
to minimize the developme
R3 Stem Cells and Kidney Repair A New Horizon in Nephrology.pptxR3 Stem Cell
R3 Stem Cells and Kidney Repair: A New Horizon in Nephrology" explores groundbreaking advancements in the use of R3 stem cells for kidney disease treatment. This insightful piece delves into the potential of these cells to regenerate damaged kidney tissue, offering new hope for patients and reshaping the future of nephrology.
Global launch of the Healthy Ageing and Prevention Index 2nd wave – alongside...ILC- UK
The Healthy Ageing and Prevention Index is an online tool created by ILC that ranks countries on six metrics including, life span, health span, work span, income, environmental performance, and happiness. The Index helps us understand how well countries have adapted to longevity and inform decision makers on what must be done to maximise the economic benefits that comes with living well for longer.
Alongside the 77th World Health Assembly in Geneva on 28 May 2024, we launched the second version of our Index, allowing us to track progress and give new insights into what needs to be done to keep populations healthier for longer.
The speakers included:
Professor Orazio Schillaci, Minister of Health, Italy
Dr Hans Groth, Chairman of the Board, World Demographic & Ageing Forum
Professor Ilona Kickbusch, Founder and Chair, Global Health Centre, Geneva Graduate Institute and co-chair, World Health Summit Council
Dr Natasha Azzopardi Muscat, Director, Country Health Policies and Systems Division, World Health Organisation EURO
Dr Marta Lomazzi, Executive Manager, World Federation of Public Health Associations
Dr Shyam Bishen, Head, Centre for Health and Healthcare and Member of the Executive Committee, World Economic Forum
Dr Karin Tegmark Wisell, Director General, Public Health Agency of Sweden
CHAPTER 1 SEMESTER V PREVENTIVE-PEDIATRICS.pdfSachin Sharma
This content provides an overview of preventive pediatrics. It defines preventive pediatrics as preventing disease and promoting children's physical, mental, and social well-being to achieve positive health. It discusses antenatal, postnatal, and social preventive pediatrics. It also covers various child health programs like immunization, breastfeeding, ICDS, and the roles of organizations like WHO, UNICEF, and nurses in preventive pediatrics.
ICH Guidelines for Pharmacovigilance.pdfNEHA GUPTA
The "ICH Guidelines for Pharmacovigilance" PDF provides a comprehensive overview of the International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use (ICH) guidelines related to pharmacovigilance. These guidelines aim to ensure that drugs are safe and effective for patients by monitoring and assessing adverse effects, ensuring proper reporting systems, and improving risk management practices. The document is essential for professionals in the pharmaceutical industry, regulatory authorities, and healthcare providers, offering detailed procedures and standards for pharmacovigilance activities to enhance drug safety and protect public health.
India Clinical Trials Market: Industry Size and Growth Trends [2030] Analyzed...Kumar Satyam
According to TechSci Research report, "India Clinical Trials Market- By Region, Competition, Forecast & Opportunities, 2030F," the India Clinical Trials Market was valued at USD 2.05 billion in 2024 and is projected to grow at a compound annual growth rate (CAGR) of 8.64% through 2030. The market is driven by a variety of factors, making India an attractive destination for pharmaceutical companies and researchers. India's vast and diverse patient population, cost-effective operational environment, and a large pool of skilled medical professionals contribute significantly to the market's growth. Additionally, increasing government support in streamlining regulations and the growing prevalence of lifestyle diseases further propel the clinical trials market.
Growing Prevalence of Lifestyle Diseases
The rising incidence of lifestyle diseases such as diabetes, cardiovascular diseases, and cancer is a major trend driving the clinical trials market in India. These conditions necessitate the development and testing of new treatment methods, creating a robust demand for clinical trials. The increasing burden of these diseases highlights the need for innovative therapies and underscores the importance of India as a key player in global clinical research.
One of the most developed cities of India, the city of Chennai is the capital of Tamilnadu and many people from different parts of India come here to earn their bread and butter. Being a metropolitan, the city is filled with towering building and beaches but the sad part as with almost every Indian city
Telehealth Psychology Building Trust with Clients.pptxThe Harvest Clinic
Telehealth psychology is a digital approach that offers psychological services and mental health care to clients remotely, using technologies like video conferencing, phone calls, text messaging, and mobile apps for communication.
CHAPTER 1 SEMESTER V - ROLE OF PEADIATRIC NURSE.pdfSachin Sharma
Pediatric nurses play a vital role in the health and well-being of children. Their responsibilities are wide-ranging, and their objectives can be categorized into several key areas:
1. Direct Patient Care:
Objective: Provide comprehensive and compassionate care to infants, children, and adolescents in various healthcare settings (hospitals, clinics, etc.).
This includes tasks like:
Monitoring vital signs and physical condition.
Administering medications and treatments.
Performing procedures as directed by doctors.
Assisting with daily living activities (bathing, feeding).
Providing emotional support and pain management.
2. Health Promotion and Education:
Objective: Promote healthy behaviors and educate children, families, and communities about preventive healthcare.
This includes tasks like:
Administering vaccinations.
Providing education on nutrition, hygiene, and development.
Offering breastfeeding and childbirth support.
Counseling families on safety and injury prevention.
3. Collaboration and Advocacy:
Objective: Collaborate effectively with doctors, social workers, therapists, and other healthcare professionals to ensure coordinated care for children.
Objective: Advocate for the rights and best interests of their patients, especially when children cannot speak for themselves.
This includes tasks like:
Communicating effectively with healthcare teams.
Identifying and addressing potential risks to child welfare.
Educating families about their child's condition and treatment options.
4. Professional Development and Research:
Objective: Stay up-to-date on the latest advancements in pediatric healthcare through continuing education and research.
Objective: Contribute to improving the quality of care for children by participating in research initiatives.
This includes tasks like:
Attending workshops and conferences on pediatric nursing.
Participating in clinical trials related to child health.
Implementing evidence-based practices into their daily routines.
By fulfilling these objectives, pediatric nurses play a crucial role in ensuring the optimal health and well-being of children throughout all stages of their development.
Medical Technology Tackles New Health Care Demand - Research Report - March 2...pchutichetpong
M Capital Group (“MCG”) predicts that with, against, despite, and even without the global pandemic, the medical technology (MedTech) industry shows signs of continuous healthy growth, driven by smaller, faster, and cheaper devices, growing demand for home-based applications, technological innovation, strategic acquisitions, investments, and SPAC listings. MCG predicts that this should reflects itself in annual growth of over 6%, well beyond 2028.
According to Chris Mouchabhani, Managing Partner at M Capital Group, “Despite all economic scenarios that one may consider, beyond overall economic shocks, medical technology should remain one of the most promising and robust sectors over the short to medium term and well beyond 2028.”
There is a movement towards home-based care for the elderly, next generation scanning and MRI devices, wearable technology, artificial intelligence incorporation, and online connectivity. Experts also see a focus on predictive, preventive, personalized, participatory, and precision medicine, with rising levels of integration of home care and technological innovation.
The average cost of treatment has been rising across the board, creating additional financial burdens to governments, healthcare providers and insurance companies. According to MCG, cost-per-inpatient-stay in the United States alone rose on average annually by over 13% between 2014 to 2021, leading MedTech to focus research efforts on optimized medical equipment at lower price points, whilst emphasizing portability and ease of use. Namely, 46% of the 1,008 medical technology companies in the 2021 MedTech Innovator (“MTI”) database are focusing on prevention, wellness, detection, or diagnosis, signaling a clear push for preventive care to also tackle costs.
In addition, there has also been a lasting impact on consumer and medical demand for home care, supported by the pandemic. Lockdowns, closure of care facilities, and healthcare systems subjected to capacity pressure, accelerated demand away from traditional inpatient care. Now, outpatient care solutions are driving industry production, with nearly 70% of recent diagnostics start-up companies producing products in areas such as ambulatory clinics, at-home care, and self-administered diagnostics.
Defecation
Normal defecation begins with movement in the left colon, moving stool toward the anus. When stool reaches the rectum, the distention causes relaxation of the internal sphincter and an awareness of the need to defecate. At the time of defecation, the external sphincter relaxes, and abdominal muscles contract, increasing intrarectal pressure and forcing the stool out
The Valsalva maneuver exerts pressure to expel faeces through a voluntary contraction of the abdominal muscles while maintaining forced expiration against a closed airway. Patients with cardiovascular disease, glaucoma, increased intracranial pressure, or a new surgical wound are at greater risk for cardiac dysrhythmias and elevated blood pressure with the Valsalva maneuver and need to avoid straining to pass the stool.
Normal defecation is painless, resulting in passage of soft, formed stool
CONSTIPATION
Constipation is a symptom, not a disease. Improper diet, reduced fluid intake, lack of exercise, and certain medications can cause constipation. For example, patients receiving opiates for pain after surgery often require a stool softener or laxative to prevent constipation. The signs of constipation include infrequent bowel movements (less than every 3 days), difficulty passing stools, excessive straining, inability to defecate at will, and hard feaces
IMPACTION
Fecal impaction results from unrelieved constipation. It is a collection of hardened feces wedged in the rectum that a person cannot expel. In cases of severe impaction the mass extends up into the sigmoid colon.
DIARRHEA
Diarrhea is an increase in the number of stools and the passage of liquid, unformed feces. It is associated with disorders affecting digestion, absorption, and secretion in the GI tract. Intestinal contents pass through the small and large intestine too quickly to allow for the usual absorption of fluid and nutrients. Irritation within the colon results in increased mucus secretion. As a result, feces become watery, and the patient is unable to control the urge to defecate. Normally an anal bag is safe and effective in long-term treatment of patients with fecal incontinence at home, in hospice, or in the hospital. Fecal incontinence is expensive and a potentially dangerous condition in terms of contamination and risk of skin ulceration
HEMORRHOIDS
Hemorrhoids are dilated, engorged veins in the lining of the rectum. They are either external or internal.
FLATULENCE
As gas accumulates in the lumen of the intestines, the bowel wall stretches and distends (flatulence). It is a common cause of abdominal fullness, pain, and cramping. Normally intestinal gas escapes through the mouth (belching) or the anus (passing of flatus)
FECAL INCONTINENCE
Fecal incontinence is the inability to control passage of feces and gas from the anus. Incontinence harms a patient’s body image
PREPARATION AND GIVING OF LAXATIVESACCORDING TO POTTER AND PERRY,
An enema is the instillation of a solution into the rectum and sig
CRISPR-Cas9, a revolutionary gene-editing tool, holds immense potential to reshape medicine, agriculture, and our understanding of life. But like any powerful tool, it comes with ethical considerations.
Unveiling CRISPR: This naturally occurring bacterial defense system (crRNA & Cas9 protein) fights viruses. Scientists repurposed it for precise gene editing (correction, deletion, insertion) by targeting specific DNA sequences.
The Promise: CRISPR offers exciting possibilities:
Gene Therapy: Correcting genetic diseases like cystic fibrosis.
Agriculture: Engineering crops resistant to pests and harsh environments.
Research: Studying gene function to unlock new knowledge.
The Peril: Ethical concerns demand attention:
Off-target Effects: Unintended DNA edits can have unforeseen consequences.
Eugenics: Misusing CRISPR for designer babies raises social and ethical questions.
Equity: High costs could limit access to this potentially life-saving technology.
The Path Forward: Responsible development is crucial:
International Collaboration: Clear guidelines are needed for research and human trials.
Public Education: Open discussions ensure informed decisions about CRISPR.
Prioritize Safety and Ethics: Safety and ethical principles must be paramount.
CRISPR offers a powerful tool for a better future, but responsible development and addressing ethical concerns are essential. By prioritizing safety, fostering open dialogue, and ensuring equitable access, we can harness CRISPR's power for the benefit of all. (2998 characters)
2. Biopharmaceutics Classification System
BCS is a scientific framework for classifying drug
substances based on their aqueous solubility and
intestinal permeability.
It is a drug development tool that allows estimation of
solubility, dissolution and intestinal permeability affect
that oral drug absorption.
Key parameters are characterized in BCS classification
are :
1. Absorption number (An)
2. Dissociation number (Dn)
3. Dose number (Do)
2
3. Absorption No. (An) :- It is the ratio of Residence time
(Tres) to Mean absorbance time (Tabs)
An ˃ 1 → indicate Complete absorption
Dissolution No. (Dn) :- The time required for drug
dissolution which is the ratio of intestinal residence time
to the dissolution time.
Higher the Dn → Higher fraction dose absorbed.
Dose No. (Do):- It is the ratio of dose concentration to
drug solubility.
Do ≤ 1→ higher solubility.
Do ˃ 1→ low solubility.
3
4. Class Boundaries
HIGHLY SOLUBLE:- The highest dose strength should be soluble in <
250 ml water over a pH range of 1 to 7.5.
Acc. To BCS the highest dose strength volume in 250 ml, where the D/S
ratio <250 refer to highly soluble But it s not true for pediatric patient
HIGHLY PERMEABLE:- When the extent of absorption in humans is
determined to be > 90% of an administered dose.
Based on mass balance or compared with an iv route.
RAPIDLY DISSOLVING :- When > 85% of the labeled amount of drug
substance dissolves within 30 minutes using USP apparatus I or II in a
volume of < 900 ml buffer solutions
This study is important for biological and in vivo-in vitro
correalation.(IVIVC).
4
6. Biowaiver
The term Biowaiver is applied to a regulatory drug approval process
when the drug dossier (application) is approved based on the evidence
of equivalence other than through in vivo equivalence testing.
In 1995 the American Department of Health & Human Service US
Food & Drug Administration (HHS-FDA) instigated the
Biopharmaceutics Classification System (BCS), with the aim of
granting so-called biowaivers for SUPACs.
BCS provides biowaivers for Class I, II, III drugs with some
specification.
As the BCS is only applicable to APIs which are absorbed from the
small intestine.
6
7. A Biowaiver means that in vivo bioavailability
and/or bioequivalence studies may be waived
(i.e. not considered necessary for product approval).
Bioavailability :- It means the rate and extent to which
the active drug substance is absorbed from a
pharmaceutical dosage form and becomes available at
the site of action.
Bioequivalence :-It refers to the drug substance in two or
more identical dosage forms, reaches in systemic
circulation at the same rate and to the same relative
extent.
7
8. Biowaiver for Bioequivalence study
If two product, containing the same , have the same
concentration time profile at the intestinal membrane
surface then they will have the same rate and extent of
the absorption.
8
Generic Product Innovator Product / Std
recommended by USFDA
Ex. Paracetamol Tablet 650
mg
DOLO-650 mg
API - Paracetamol API - Paracetamol
Tablet (oral) Tablet (oral)
Bioavailability 80 % Bioavailability 80 %
9. Need & Objective for BE studies
If a new product is intended to be a substitute
for an approved medicinal product as a
pharmaceutical equivalent or alternative, the
equivalence with this product should be shown
or justified.
In order to ensure clinical performance of such
drug products, bioequivalence studies should be
performed.
9
11. In vitro BE studies
In vitro studies, i.e. dissolution studies can be used
instead of in vivo bioequivalence under certain
circumstances, called as biowaiver .
For waiver of in vivo, bioequivalence test and reference
product should exhibit similar dissolution profile under
the dissolution test condition defined for rapidly
dissolving product.
Two dissolution profile may be considered similar.
When both test and the reference products dissolve 85 %
or more of the labeled amount in less than 15 minutes in
all three dissolution media (at acidic i.e 01.N HCL, at
pH 4.5 buffer and at 6.8 buffer ). A profile comparison
is unnecessary.
11
12. Techniques For Improving Bioavailability
One approach to improve the systemic availability of the
drug is to deliver it by alternative routes of
administration such as parenteral, nasal, vaginal, rectal
or transdermal. However, improvement of the oral
bioavailability of the drug is the most realistic approach,
as it is the most preferred and convenient route of
administration.
The techniques to improve oral bioavailability of the
drugs are described as follows:
12
13. Enhancement Of Drug Solubility Or
Dissolution Rate
1. Micronization
2. Nanonization
3. Supercritical Fluid Re-crystalization
4. Spray Freezing into Liquid (SFL)
5. Evaporative Precipitation into Aqueous Solution
(EPSA)
6. Use of Surfactants
7. Use of Salt Forms
8. Use of Precipitation Inhibitors
9. Alteration of pH of the Drug Microenvironment
10. Use of Amorphous, Anhydrates, Solvates and
Metastable polymorphs
13
15. Micronization :-
The process involves reducing the size of the solid
particles to 1 to 10 microns commonly by spray drying
or by use of air attrition methods. This process is also
called as mico-milling.
Nanonisation :-
It is a process of the dry powder is converted to
nanocrystals of sizes 200-600 nm . Eg. Amphotericin B.
i. Pearl milling
ii. Homogenisation in water
iii. Homogenisation in non-aqueous media.
15
16. Spray Freezing into Liquid (SFL) :-
This technique involves an aqueous, organic, aqueous-
organic cosolvent solution, aqueous organic emulsion
and suspension containing drug and pharmaceutical
excipients (CO2, helium, propane, ethane).
The frozen particles are then lyophilized to obtain dry
and free-flowing micronized powders.
SFL powder containing amorphous nanostructured
aggregates with high surface area and excellent
wettability.
16
17. Solvent Deposition :-
In this method, the poorly aqueous soluble drug such as
nifedipine is dissolved in an organic solvent like alcohol
and deposited on an inert, hydrophilic, solid matrix such
as starch or MCC by evaporation of solvent.
17
18. Solid Dispersions :
These are generally prepared by Solvent or co-
precipitation method whereby both the guest solute and
the solid carrier solvent are dissolved in a common
volatile liquid solvent such as alcohol.
The liquid solvent is removed by evaporation under
reduced pressure or by freeze drying which results in
amorphous precipitation of guest in a crystalline carrier.
These method is suitable for thermolabile substances.
18
19. Enhancement Of Drug Permeability
Across Biomembrane
1. Lipid technology :
With an increase in the number of emerging
hydrophobic drugs, several lipid –based formulations
have been designed to improve their bioavailability.
2. Ion pairing :
The ion pairing approach involves co-administration of a
hydrophilic or polar with a suitable lipophilic
counterion, which consequently improves the
partitioning of the resultant ion-pair into the intestinal
membrane.
These technique use to improve the oral BA of ionisable
drugs. Eg ; Atenolol
19
20. 3. Penetration Enhancers :
Compound which facilitate the transport of drugs across
the biomembrane are called penetration / permeation
enhancer or promoters.
This method is used mainly in cases of hydrophilic
drugs which are expected to have difficulty in
penetrating the lipid structure of the biomembrane.
Eg. of Penetration enhancers :-
Citric acid, SLS, EDTA, Salicylates and fatty acids such
as oleic acid linoleic acid arachidonic acid.
20
21. Enhancement of Drug Stability
1. Enteric coating :
Enteric-coated systems utilize polymeric coatings that
are insoluble in the gastric media and therefore, prevent
or retard drug release in the stomach. Such systems
release the drug in the alkaline media in intestine.
Eg. Erythromycin, penicilin v, benzimidazole,
omeprazol can be improved by enteric coating.
2. Complexation :
It can be used to increase the stability of drug in GI
media. Generally Beta- cyclodextrins are potential
carriers for increasing the oral bioavailability of
caffeiene, sodium salicylate, sodium benzoate.
21
22. 3. Use of Metabolic inhibiters :
Co-administration of drug (with low BA) and its
metabolism, which can selectively inhibit any of the
contributing processes, would result in increased
fractional absorption and hence increases bioavailability.
22
23. Significance of Biowaiver
It can save both time and money—if the immediate -
release, orally administered drug meets specific criteria,
the FDA will grant a waiver for expensive and time-
consuming bioequivalence studies.
Valuable tool for formulation scientist for selection of
design of formulated drug substance.
When integrated with other information provide a
tremendous tool for efficient drug development.
Reduces cost and time of approving Scale- up and post
approval challenges.
Applicable in both pre-clinical and clinical drug
development process.
23
24. Reference
1. Shekhawat P, Pokharkar V, Understanding peroral
absorption: regulatory aspects and contemporary approaches
to tackling solubility and permeability hurdles, Review
Article, Acta Pharmaceutica Sinica B, 2017, Volume 7, Page
no. 260-280.
2. Dahan A, Miller J, Amidon G , Prediction of Solubility and
Permeability Class Membership: Provisional BCS
Classification of the World’s Top Oral Drugs , Review
Article , American Association of Pharmaceutical Scientists,
2009 , Volume 11, Page no.740 - 746.
3. Chavda H, Patel C, Anand I, Biopharmaceutics
Classification System, Review Article , Sys Rev Pharm,
2010, Volume 1, Page no. 62-69.
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25. 4. Valsami G, Macheras P, Computational-Regulatory Developments
in the Prediction of Oral Drug Absorption, Review Article , Wiley
VCH Verlag GmbH & Co. KGaA, Weinheim , 2011, Page no. 112-
121.
5. Murakami T, Absorption sites of orally administered drugs in the
small intestine, Review Article, Informa UK Limited, trading as
Taylor & Francis Group, 2017
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