This document discusses using hot melt extrusion (HME) technology to improve the dissolution and bioavailability of the poorly water soluble drug efavirenz (Efv) through the formation of solid dispersions with hydrophilic polymers and surfactants. Efv solid dispersions were prepared by HME using Kollidon VA64 polymer and various surfactants at 10% weight. Dissolution and permeability studies showed improved results for formulations containing PEG 4000 and sorbiton monolaurate surfactants. Pharmacokinetic studies in rats found the PEG 4000 formulation increased the extent of Efv absorption by 106.98% compared to non-HME controls. The study demonstrates HME can enhance the
Dissolution enhancement of glimepiride by solid dispersion technique.Santosh Adhikari
Dissolution Enhancement of Glimepiride by Solid Dispersion Technique.
Priyanka Shrestha1*, Shiva Kumar Bhandari1, SM Ashraful Islam1, and Santosh Adhikari2.
1Department of Pharmacy, University of Asia Pacific, Dhanmondi, Dhaka-1209, Bangladesh.
2Department of Pharmacy, Rajiv Gandhi University of Health Science, Banglore-560 041.
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
All manuscripts are subject to rapid peer review. Those of high quality (not previously published and not under consideration for publication in another journal) will be published without delay.
Solubilisation of Quinazoline drugs by using Beta cyclodextrin complex formationRavindra Zirmire
Solubility of the Quinazoline related drugs was enhanced by usind complex formation method,and the Physico chemical characterisation of these drugs was carried out by simplest methods as UV spectroscopy,TLC,FTIR Spectroscopy.
Dissolution enhancement of glimepiride by solid dispersion technique.Santosh Adhikari
Dissolution Enhancement of Glimepiride by Solid Dispersion Technique.
Priyanka Shrestha1*, Shiva Kumar Bhandari1, SM Ashraful Islam1, and Santosh Adhikari2.
1Department of Pharmacy, University of Asia Pacific, Dhanmondi, Dhaka-1209, Bangladesh.
2Department of Pharmacy, Rajiv Gandhi University of Health Science, Banglore-560 041.
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
All manuscripts are subject to rapid peer review. Those of high quality (not previously published and not under consideration for publication in another journal) will be published without delay.
Solubilisation of Quinazoline drugs by using Beta cyclodextrin complex formationRavindra Zirmire
Solubility of the Quinazoline related drugs was enhanced by usind complex formation method,and the Physico chemical characterisation of these drugs was carried out by simplest methods as UV spectroscopy,TLC,FTIR Spectroscopy.
Formulation and evaluation of microspheres with aceclofenacSagar Savale
Aceclofenac is an analgesic and anti-inflammatory drug that reduces fever, pain, and inflammation in rheumatoid
arthritis, osteoarthritis and ankylosing spondylitis. Aceclofenac has higher anti-inflammatory action than
conventional NSAIDs. Development of microspheres is a promising technology for controlled release and drug
targeting. Various types of microspheres such as bio-adhesive, magnetic, floating, radioactive and polymeric
microspheres are developed for various purposes. Microspheres occupied a central place in novel drug delivery, it
can targeted and localized drug delivery system. This Aceclofenac Microsphere is Prepared by using Spray drying
Technique in which release rate of drug is mainly depends on formulation composition (Eudragit RS 30 D and
Ethyl Cellulose (1:2 ratio)). Formulated microspheres were characterized for particle size, encapsulation efficiency
and In vitro studies. The optimum drug-to-polymer ratio and feed flow rate is responsible for higher percent yield,
smaller particle size and maximum encapsulation efficiency.
This slide share includes the introduction about smedds, difference between emulsion and smedd and sedds and smedds, composition and its formulation aspects.
Formulation and evaluation of Gastroretentive Bosentan monohydrate tablets us...mamatha jirra
The presentation is about the preparation and evaluation of Bosentan monohydrate tablets using raft technology, which is used to treat Pulmonary Arterial Hypertension (PAH). Raft technology is a novel approach to formulate Gastroretentive tablets. Raft is formed on the surface of gastric contents when the tablet comes in contact with the gastric fluid. The drug is released from the raft slowly and continuously resulting in controlled drug release.
Formulation and Evaluation of Controlled Release Tablet of LamotrigineBRNSS Publication Hub
Controlled drug delivery [16] can be defined as delivery of the drug at a predetermined rate and/or to a
location according to the needs of the body and disease states for a definite time period. Controlled
release drug administration means not only the prolongation of the duration of drug delivery, similar to
the objective in sustained release and prolonged release, but the term also implies the predictability and
reproducibility of drug release kinetics. Oral controlled release drug delivery system is one that provides
continuous oral delivery of drugs at predictable and reproducible kinetics for a pre-determined period
throughout the course of GI transit.
Self Nano-emulsifying drug delivery system (SNEDDS)Sagar Savale
The Self Nano-emulsifying Drug Delivery System (SNEDDS) is a Novel Drug Delivery System for Enhancement of water solubility of poorly water soluble drugs. It is isotropic mixture of oil, surfactant, co-surfactant molecules and it also containing co-solvent molecule.
This PPT includes what role does Dosage form impart on absorption. Why it is important in absorption. what should be its nature and type of dosage form.
Bioavailability and bioequivalence studyMcpl Moshi
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
Formulation and evaluation of microspheres with aceclofenacSagar Savale
Aceclofenac is an analgesic and anti-inflammatory drug that reduces fever, pain, and inflammation in rheumatoid
arthritis, osteoarthritis and ankylosing spondylitis. Aceclofenac has higher anti-inflammatory action than
conventional NSAIDs. Development of microspheres is a promising technology for controlled release and drug
targeting. Various types of microspheres such as bio-adhesive, magnetic, floating, radioactive and polymeric
microspheres are developed for various purposes. Microspheres occupied a central place in novel drug delivery, it
can targeted and localized drug delivery system. This Aceclofenac Microsphere is Prepared by using Spray drying
Technique in which release rate of drug is mainly depends on formulation composition (Eudragit RS 30 D and
Ethyl Cellulose (1:2 ratio)). Formulated microspheres were characterized for particle size, encapsulation efficiency
and In vitro studies. The optimum drug-to-polymer ratio and feed flow rate is responsible for higher percent yield,
smaller particle size and maximum encapsulation efficiency.
This slide share includes the introduction about smedds, difference between emulsion and smedd and sedds and smedds, composition and its formulation aspects.
Formulation and evaluation of Gastroretentive Bosentan monohydrate tablets us...mamatha jirra
The presentation is about the preparation and evaluation of Bosentan monohydrate tablets using raft technology, which is used to treat Pulmonary Arterial Hypertension (PAH). Raft technology is a novel approach to formulate Gastroretentive tablets. Raft is formed on the surface of gastric contents when the tablet comes in contact with the gastric fluid. The drug is released from the raft slowly and continuously resulting in controlled drug release.
Formulation and Evaluation of Controlled Release Tablet of LamotrigineBRNSS Publication Hub
Controlled drug delivery [16] can be defined as delivery of the drug at a predetermined rate and/or to a
location according to the needs of the body and disease states for a definite time period. Controlled
release drug administration means not only the prolongation of the duration of drug delivery, similar to
the objective in sustained release and prolonged release, but the term also implies the predictability and
reproducibility of drug release kinetics. Oral controlled release drug delivery system is one that provides
continuous oral delivery of drugs at predictable and reproducible kinetics for a pre-determined period
throughout the course of GI transit.
Self Nano-emulsifying drug delivery system (SNEDDS)Sagar Savale
The Self Nano-emulsifying Drug Delivery System (SNEDDS) is a Novel Drug Delivery System for Enhancement of water solubility of poorly water soluble drugs. It is isotropic mixture of oil, surfactant, co-surfactant molecules and it also containing co-solvent molecule.
This PPT includes what role does Dosage form impart on absorption. Why it is important in absorption. what should be its nature and type of dosage form.
Bioavailability and bioequivalence studyMcpl Moshi
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 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.
Formulation and Evaluation of Solid dispersion for Dissolution Enhancement of...Jing Zang
Nifedipine, a calcium channel blocker antihypertensive drug, is a poorly water soluble drug and belongs to BCS class II. The objective of the research work was to formulate and optimize solid dispersions (SDs) of a poorly water soluble drug, nifedipine, with sodium starch glycollate, croscarmellose sodium, eudragit E-100. Solid dispersions were prepared by solvent evaporation techniques in different weight ratios of polymers. The results indicated that homogeneous or heterogeneous conditions during the preparation methods employed governed the internal structures of the polymer matrices while retaining the drug in an amorphous form. The physical mixtures and solid dispersions were subjected to drug content and dissolution test. The best formulation, nifedipine with croscarmellose sodium in 1:7 ratio, among all was further adsorbed on neusilin US2 to form ternary mixture. The increased dissolution was achieved by more than 70percent and 30percent comparatively to the nifedipine API and marketed product respectively. The tablet dosage form prepared from ternary mixture was stable at stressed conditions 40±2°C and 75±5% RH. The release kinetics of drug from formulation and marketed product follows peppas model. The similar factor f2 was within limit for the product at stressed conditions with the product at room temperature at the same time.
Solubility enhancement technique of BCS Class II drug by Solvent EvaporatiomKaustav Dey
I am very happy to share with you my B.Pharm Final semester Presentation. The topic of the presentation was “SOLUBILITY ENHANCEMENT TECHNIQUE OF BCS CLASS II DRUG BY SOLVENT EVAPORATION TECHNIQUE – FORMULATION & EVALUATION" which i have done under the esteemed guidance of Dr. Goutam Kumar Jena. It was a great experience to deliver this topic infront of the expert jury. I would also like thank all my teammates especially Agniv Masanta for his efforts. I hope everyone of you will like presentation and the research and efforts behind it.Thank you for giving your precious time. #research #science #thankyou #experience #share
Formulation and evaluation of Muco adhesive Buccal Tablets of Ramprildoddaapurupa
The buccal mucosa lines the inner cheek and Buccal formulations are placed in the mouth between upper gingiva(gums) and cheek to treat local and systemic conditions.
Drugs which undergoes Extensive first pass metabolism and drug degradation in acidic media, GI tract can be administered through buccal route.
The oral cavity has been used as a site for local and systemic drug delivery.
Healing Effects of Hydroalcoholic Extract of Guava (Psidium guajava) Leaf on ...Dr. Anuj S Parihar
Oral mucositis (OM) is a common inflammatory complication among cancerous patients as an adverse effect of chemotherapy and radiotherapy. The aim of this study is to evaluate the healing effects of hydroalcoholic extract of Psidium
Guajava leaf on oral induced mucositis induced by 5-fluorouracil using histopathologic and tissue antioxidative markers assessment in male dark brown rats. In a prospective randomized double blind animal study, OM was induced in 64 male dark brown rats that allocated in 4 groups by 5-FU (60 mg/kg) on days 0, 5, and 10 of the study. The cheek pouch was scratched with a sterile needle on once daily on days 3 and 4. Starting from day 12, gel base, topical form and 600 mg/kg dietry form of hydroalcoholic extract of Psidium Guajava leaf were administered per day. Pouch histopathology score, superoxide dismutase, glutathione peroxidase, total antioxidant capacity were evaluated on day 14 and 18. DPPH scavenging activity and total phenolic content also were measured. Histopathology scores of mucositis were lower in the systemic and topical treatment groups than the gel base and control groups (P<0.05). Higher activities of SOD, GPX and TAC were detected in the topical and systemic treatment groups in comparison to the others (P<0.05). The extract was rich in total phenolic content as antioxidant. The use of extract of Psidium Guajava leave may be associated with reduced intensity of OM, increased concentration of SOD, GPX and TAC on induced
OM in dark brown rats undergoing 5-FU consumption.
Congenital Agenesis Of The Corpus Callosum With Intracerebral Lipoma And Fron...iosrphr_editor
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
“Hemodynamic and recovery profile with Dexmedetomidine and Fentanyl in intrac...iosrphr_editor
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
Correlation of Estrogen and Progesterone Receptor expression in Breast Canceriosrphr_editor
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
Analytical Study of Urine Samples for Epidemiology of Urinary Tract Infection...iosrphr_editor
The current study was carried out in District Abbottabad aimed to determine the common urinary
tract infections in local community to determine the epidemiology of significant diseases in asymptomatic patients
of renal disorder. In this study a total of 1000 urine samples were examined during 3rd February to 1st April 2015
from patients attending Ayub Teaching Hospital Abbottabad by using dipstick and microscopic analysis of urine.
There were 638 females and 362 males patients examined during this period. The range of age groups is between
1.5 years to 80 years. Results of this study was reported as Pyuria 11%, Proteinuria 21.1%, Hematuria 10.4%,
Epithelial Cells 8.2%, pH 7.8 %, Granular casts 7.3%, Triple phosphate 6.6%, Calcium oxalate 6.4%, Glycosuria
6.3%, Bacteria 6.2% and mucous 4.1%. This study concludes that routing urinalysis should be performed for all
individuals to diagnose the asymptomatic diseases that will help in simple therapeutic measurements as urinalysis
is a simple step to determine the root of Urinary tract disorders.
Chest sonography images in neonatal r.d.s. And proposed gradingiosrphr_editor
BACKGROUND : Lung sonography has been used to monitor the patients of R.D.S. in
N.I.C.U. in recent times.
AIMS : To Describe and Grade the changes of R.D.S. by lung sonography.
SETTING & DESIGN : Tertiary care institutional set up in a rural medical college.
STUDY DURATION : September 2014 to May 2015. Follow-up variable, upto 2 weeks.
PROSPECTIVE, ANALYTICAL STUDY.
MATERIALS AND METHODS -This was a single institute study approved by the institutional ethics
committee. Prior informed consent was obtained from the parents. 100 consecutive patients admitted in
N.I.C.U. WITH gestational age < 36 weeks with respiratory complaints were enrolled. Chest x-ray was
obtained within few hours of admission and lung sonography was performed within 24 hours. Follow – up
sonography was performed as and when necessary. Sonography image was graded and correlated with chest
xray and clinical picture
The Comprehensive Review on Fat Soluble Vitaminsiosrphr_editor
This review article deals with brief description of fat soluble vitamins with figures and tables
showing statistical analytical data duly quoting the references wherever necessary. The word “soluble” actually
means “able to be dissolved.” Whether a vitamin is classified as 'fat-soluble' or 'water-soluble' has to do with
how the vitamin is absorbed, stored and removed from the body. Vitamins are tiny organic compounds with a
huge impact on the health and well-being of the body. The body needs a small amount of fat soluble vitamins in
order to stay in optimal health. Fat soluble vitamins play an important role in keeping the body healthy and
functioning from immune system and muscle and heart function, easy flow and clotting of blood as well as eye
health. They are critical to health and wellness–particularly reproductive health and wellness. Low-fat, no-fat
and vegan diets are woefully lacking in fat soluble vitamins. However a diet based on traditional foods can
naturally provide these vitamins. Science is still learning about many of the functions of vitamins. "Too much
vitamin A, D, or K can lead to increased levels that are unhealthy and can cause serious health consequences.
Diseased conditions leading to decreased fat absorption leads to decreased absorption of vitamins. The fatsoluble
vitamins work most safely and effectively when obtained them from natural foods within the context of a
diet rich in all their synergistic partners. If fat soluble vitamins are stored for lengthy time they generate threat
for toxicity than water soluble vitamins and such situation even aggravated, provided they are consumed in
excess. Vitamin products, above the legal limits are not considered food supplements and must be registered as
prescription or non-prescription (over-the-counter drugs) due to their potential side effects. Vitamin A and E
supplements do not provide health benefits for healthy individuals, instead they may enhance mortality, and it is
held proved that beta-carotene supplements can be harmful to smokers
Sulphasalazine Induced Toxic Epidermal Necrolysis A Case Reportiosrphr_editor
Toxic Epidermal Necrolysis (TEN) is a rare and life threatening mucocutaneous reaction
characterized by extensive necrosis and detachment of epidermis. The Worldwide incidence of TEN is 0.9 to 1.4
per million populations per year [1]. Here we have discussed a case of Toxic Epidermal Necrolysis secondary
to Sulfasalazine managed with fluid replacement, analgesics, anti-infective therapy aggressive nutritional
support and intravenous high dose steroid therapy.
Keywords- Toxic Epidermal Necrolysis, Sulfasalazine
Evaluation the efficacy of IVIgG in treatment of Hemolytic Disease of Newborniosrphr_editor
Hemolytic disease of newborn (HDN) is an important cause of hyperbilirubinemia in the
neonatal period,and delayed diagnosis and treatment may lead to permanent brain damage. Traditional
neonatal treatment of HDN is intensive phototherapy and exchange transfusion.Intravenous
immunoglobulin(IVIgG) has been introduced as an alternative therapy to exchange transfusion. This study was
conducted to assess the effect of IVIG in HDN .
FIBROLIPOMATOUS HAMARTOMA OF ULNAR NERVE: A RARE CASE REPORT.iosrphr_editor
Nervous fibrolipomatous hamartoma is said to be a rare tumor-like condition involving the peripheral
nerves,in which the epineurium and perineurium are enlarged and distorted by excess of fatty and fibrous tissue
s that infiltrate between and around nerve boundaries. The median nerve is more likely to develop a hamartoma
than other nerves with a predilection for the carpal tunnel.
A fibrolipomatous hamartoma – is a rare, benign, congenital lesion most commonly found in the median nerve,
usually at the level of the wrist or hand.
We report a case of this rare condition in ulnar nerve.
SELF MEDICATION PRACTICES FOR ORAL HEALTH PROBLEMS AMONG DENTAL PATIENTS IN B...iosrphr_editor
Introduction: Self‑ medication is commonly practiced all over the world. Self-medication is defined as the use
of medication by a patient on his own initiative or on the advice of a pharmacist or a lay person instead of
consulting a medical practitioner. The present study was aimed to estimate the prevalence of self-medication for
oral health problems among dental patients in Bengaluru city; to identify triggering factors that could influence
self-medication practices; to identify sources of medications used; to identify sources of information about
medications used; and to identify reasons for self-medication.Study Design: A Cross sectional Study.Methods:A
survey was conducted among 175 subjects among dental patients in Bengaluru city. Data were collected
through a specially designed proforma using a closed‑ ended, self‑ administered questionnaire containing 15
questions, in five sections.
Results: The prevalence of
Clinico-haematological Profile of Falciparum Malaria in a Rural Hospital of T...iosrphr_editor
Aim: To study the clinico-haematological profile malaria in a rural hospital of Tripura.
Material and methods: A cross-sectional hospital-based study was done from at Kulai District
Hospital,Tripura. This hospital based cross sectional study was done on 60 confirmed cases of falciparum
malaria (either by peripheral smear or rapid diagnostic test) admitted in Kulai District Hospital. A case sheet
proforma was prepared and data (demographic profile,clinical feature, investigation, treatment, and
complication) from all indoor patients was collected and analyzed.
Result: Out of 60 patients, 40(66.6%) were males and 20 (33.4%) were females. Most of the patients were
between the age group 21-40 years with the highest prevalence between the age group of 21-30. Fever was the
most common symptom. Anemia was present in 42(70%) patients, out of which 6(10%) patients had severe
anemia. Thrombocytopenia was present in 36(60%) patients.Abnormal liver function tests were observed in
26(43.3%) subjects while abnormal kidney function tests were observed in16(26.6%) patients. All the 60
patients received Artemisinin based antimalarial drugs.
Conclusion: Early detection, prompt management, and adequate supportive therapy may reduce mortality due
to falciparum cerebral malaria.
Indonesian Wild Ginger (Zingiber sp) Extract: Antibacterial Activity against ...iosrphr_editor
Lempuyang gajah (Zingiber zerumbet (L.) Smith), lempuyang pahit (Zingiber amaricans BL.), and
lempuyang wangi (Zingiber aromaticum Vahl.) are used as traditional medicine (jamu) in Indonesia. It is also
used for treatment of microbial infections, helps to increase appetite and stimulate digestion in chickens.
Information on their uses are available, but only limited in the scientific data on their bioactivity. The study was
conducted on the antibacterial effect of organic extracts of these plants with Mycoplasma gallisepticum as the
agent of chronic respiratory disease in chickens. Juice and extracts of fresh and dried rhizome are evaluated
through the disc diffusion assay and minimum inhibitory concentration. Oxytetracyclin (30 µg) are used as
standards. All extracts are individually exhibited as antibacterial activity against Mycoplasma gallisepticum (7
± 0.11 mm to 21 ± 0.86 mm). The minimum inhibitory concentration (MIC) determination of plants extracts are
ranged from 7.8 mg/ml to 31.2 mg/ml. The preliminary results suggested promising antibacterial properties of
wild ginger from Indonesia, and probably could be used in management of chronic respiratory disease in
chickens.
A case of allergy and food sensitivity: the nasunin, natural color of eggplantiosrphr_editor
Abstract: Allergies and food sensitivities can both be considered as "adverse reactions individualistic" to food.
Are pathological and individual forms because they affect a few individuals in way rather serious; immediate
or delayed reactions occur instead with simple effects histamine, or, in severe cases with respiratory and
anaphylactic shock
The eggplant (Solanum melongena L.) is known to cause food allergies in some Asian countries, but detailed
studies on allergies caused by eggplant are lacking, however, it was highlighted the presence of allergens in
edible parts of eggplant with preponderance in the peel .
The purpose of this study was to propose an extraction method rapid, efficient and cost of natural dye from
waste products from the food industry, such as the peels of eggplant, from which it was extracted, isolated and
purified the nasunin,a colored molecule in red-fuchsia.
Nasusin was tested on 58 patients to evaluate the potential sensitizing effect on the skin. The results demonstrate
that allergenic effects are negligible and therefore the nasunin can be used as a colorant in various industrial
sectors with a certain safety margin
Complete NMR Assignment of MogrosidesII A2, II E andIII A1Isolated from Luo H...iosrphr_editor
NMR analysis allowed complete assignments of three known mogrol glycosides, Mogroside IIA2 (1),
II E (2)and IIIA1 (3), isolated from the extracts of Luo Han Guo. Herein, complete 1H and 13C NMR
assignmentsof all threemogrosidesare described based on NMR experiments (1H NMR, 13C NMR, COSY,
HSQC-DEPT, HMBC, NOESY and 1DTOCSY) and mass spectral data.
Nanoemulsion and Nanoemulgel as a Topical Formulationiosrphr_editor
: Nanoemulsion is referred type of emulsion with uniform and extremely small droplet size in the range
of 20-200 nm. Nanoemulsion provides numerous advantages over other carrier such as polymeric nanoparticle
and liposomes, including low cost preparation procedure, high hydrophilic and lipophilic drug loading system
to enhance the longer shelf live upon preserving the therapeutic agents. Incorporating the preparation of
nanoemulsion with hydrogel matrix to produce nanoemulgel exhibited by the two separate systems that forming
it. Nanoemulgel possesses the properties of thixotropic, non-greasy, effortlessly spreadable, easily be removed,
emollient, not staining, soluble in water, longer shelf life, bio-friendly, translucent and agreeable appearance.
Pharmacokinetics of High-Dose Methotrexate in Egyptian Children with Acute Ly...iosrphr_editor
Aim:Since several factors have been shown to influence the clearance of methotrexate, the purpose of this study
was to identify potential relationships between patient covariates and the methotrexate clearance estimates and
deduce a pharmacokinetic model for the estimation of methotrexate clearance in Egyptian pediatric ALL
patients that may help dosage adjustment and achieve target steady-state plasma concentrations in a similar
sittings.
Patients and methods: A total of 94 pediatric patients with B-cell ALL, of whom 70 were the studied population
and 24 were the test population, were treated with four courses of HDMTX doses 2.5 gm/m2
(low-risk arm) or 5
gm/m2
(standard-/high-risk arm) given every other week by intermittent intravenous infusions over 24 hours as
a part of their treatment protocol. Patients were monitored for the 24 hour MTX concentration and the systemic
methotrexate clearance was calculated for each methotrexate dose
Epidemiology of Tuberculosis (TB) in Albania 1998-2009iosrphr_editor
Abstract : In Albania, many people erroneously think that tuberculosis (TB) is a disease of the past-an illness
that no longer constitutes a public health threat. Surveillance is an integral part of tuberculosis (TB) control.
Albania has a highTB notification rate and there are doubts about underreporting. The evolution of the
incidence of tuberculosis is presented, together with more detailed figures over the period 1998-2009. These
figures were obtained by the monthly forms (called 14/Sh) compared with the individual notification data.
Objective: To examine the distribution and sources of increased tuberculosis (TB) morbidity and reporting
system deficiencies in the Albania from 1998 through 2009. Metodology: The study is descriptive one conductet
during the period 1998-2009. The statistical analysis is based on data reported from regional level (regional
epidemiological departments) to the central level (Public Health Institute). Results: The main findings were:
discordance between the collected data (individual form) and reported data (monthly form); tuberculosis
incidence rate shows little oscillations which ranges from 6.67 to 9.2 cases/100.000 population; 50% of the
regions show a lack of information on the confirmation of diagnosis and laboratory examination type used for
confirmation. Conclusion: TB disease in high-risk populations where it is difficult to detect, diagnose, and treat;
limitations of current control measures and the need for new tests and treatments, including an effective
vaccine; improving information system, regulation of individual form and personnel training.
Total Phenol and Antioxidant from Seed and Peel of Ripe and Unripe of Indones...iosrphr_editor
Study on total phenol and antioxidantactivity ofsugar apple fruits of various solvent, part of fruits, and level of ripening. Solvent extraction used were 80% (v/v) methanol, 50% (v/v) acetone, boiling water, and 50% (v/v) ethanol. Part of fruits thatbeen used for samples were seed and peel which are normally by products of sugar apple processing, level of ripening were unripe, and ripe sugar apple fruits. Total phenol was determined by Folin-ciocalteau method. Total antioxidant was quantified by 1,1-diphenyl-2-picrylhydrazyl(DPPH) method.Therewas a difference in type of solvent, part of fruits, and level of ripeningon total phenol and antioxidant concentration of sugar apple fruits. Seeds have higher total phenol concentration than peels of this fruits. Unripe sugar apple fruits have higher total phenol and antioxidant than ripe fruit. The best solvent for phenol extraction was ethanol 50%butthe best solvent for antioxidant extraction was acetone 50%.
A Review on Step-by-Step Analytical Method Validationiosrphr_editor
When analytical method is utilized to generate results about the characteristics of drug related samples it is essential that the results are trustworthy. They may be utilized as the basis for decisions relating to administering the drug to patients. Analytical method validation required during drug development and manufacturing and these analytical methods are fit for their intended purpose. To comply with the requirements of GMP pharmaceutical industries should have an overall validation policy which documents how validation will be performed. The purpose of this validation is to show that processes involved in the development and manufacture of drug, production and analytical testing can be performed in an effective and reproducible manner. This review article provides guidance on how to perform validation characteristics for the analytical method which are utilized in pharmaceutical analysis.
A Cross Sectional Study of Ethnic Differences in Occurrence and Severity of A...iosrphr_editor
Non-steroidal anti-inflammatory drugs are the most widely used "over the counter" medication all over the world despite their complications in different major organs. Present studies envisaged for knowing the occurrence and severity of adverse drug reactions from NSAIDs in different ethnic communities of Sikkim. A cross sectional study was undertaken in the medicine outpatients department of a secondary and tertiary care hospital. The patients belonging to Nepalese, Bhutias, Lepchas ethnic communities and others community (settlers from other parts of India) were included to analyzed the data based on the age and gender, ethnicity and ADRs, drugs and ADRs. Severity assessment was done using Hartwing and Siegel scale and causality assessment by Naranjo scale. Total 109 cases of ADRs, predominating in female were detected. Nepalese were the most affected and Gastrointestinal tract (GIT) being the most affected organ in them. Diclofenac showed maximum number of ADRs in all the communities. Maximum number of cases occurred on single day use (40.36%) of drugs. All the cases were belonging to the "possible category" and the maximum being the mild (72.48%) in nature. It is advisable to consider the ethnic/racial differences equally with other factors, to improve the safety and efficacy of a drug.
A Cross Sectional Study of Ethnic Differences in Occurrence and Severity of A...
H045047053
1. IOSR Journal Of Pharmacy
(e)-ISSN: 2250-3013, (p)-ISSN: 2319-4219
www.iosrphr.org Volume 4, Issue 5 (May 2014), PP. 47-53
47
Dissolution and Bioavailability Enhancement of Efavirenz by Hot
Melt Extrusion Technique
Smita Kolhe1
, Dr. P.D.Chaudhari2
, Mr. Dhananjay More3
1
Modern College of Pharmacy (For Ladies), Moshi,MS, India
2
Modern College of Pharmacy, Nigdi, MS, India
3
Emcure Pharmaceuticals Ltd.,Pune, MS, India
ABSTRACT: The aim of this study is to improve dissolution and bioavailability of poorly water soluble
Efavirenz (Efv), a potent and selective non-nucleoside inhibitor of HIV-1 reverse transcriptase. Its effectiveness
can be attributed to its long half-life (t1/2) of 52–76 h after single dose. Formulation of poorly water soluble
drug for oral delivery is one of the biggest challenges. Amongst the available approaches, the novel solid
dispersion (SD) technique known as hot melt extrusion (HME) has often proved to be the most widely used
method in improving dissolution and bioavailability of the drugs because of its various advantages. Dissolution
enhancement of Efv was done by HME technology where crystalline form of API is converted to amorphous
form using hydrophilic polymer like Kollidon VA64. Surfactants like Polyethylene glycol (PEG 4000), polyoxy
35 castor oil (Chremophor EL) and Sorbiton monolaurate (Montane 20PHA) were used as plasticizer for
process feasibility. Physical mixtures of drug, polymer and surfactant were prepared in ratio of 1:1:0.1. These
physical mixtures were subjected to melt and the resultant formulations were subjected to physical
characterization, dissolution, permeability and in vivo testing. Pharmacokinetics of Efv was studied in rats.
Drug efflux pumps like P-glycoprotein (P-gp) were recognized to posses’ functional role in determining the
pharmacokinetics of drugs. Inhibition of P-gp improves intestinal absorption and tissue distribution while
reducing the substrate metabolism and its elimination. Drug release showed comparative similar release for all
the HME formulations while the permeability studies showed improved permeability of formulations containing
Sorbiton Monolaurate and PEG 4000. In comparison to the Non HME (NHME) formulation, the SD prepared
with KollidonVA64 (drug: polymer 1:1) by HME process showed a significant enhancement in permeability
with all the three surfactants. SD prepared by PEG 4000 resulted in 106.98% enhancement in extent of
absorption. In conclusion, solid dispersion prepared using certain polymer could serve as a promising
formulation approach to enhance the dissolution and bioavailability of Efv.
KEYWORDS: Efv, HME, Invivo, Kollidon VA64, Permeability.
I. INTRODUCTION
Efv is a potent and selective non-nucleoside inhibitor of HIV-1 reverse transcriptase [1, 2], but its
aqueous solubility is relatively poor (<10 μg/mL in water) [1]. For such hydrophobic compound, poor solubility
would result in a slow dissolution and hence low and erratic oral bioavailability, which may limit its further
clinical application. Majority of the drugs are administered by preoral route. Many hurdles starting from drug
dissolution in gastrointestinal fluid to first pass metabolism due to various physicochemical and
biopharmaceutical problems occur. It was recently identified that drug efflux pumps like P-gp are playing major
role in altering the pharmacokinetics of various drugs and particularly associated with poor bioavailability in co-
ordination with gut wall metabolism. Thus, a deep insight and thorough understanding of P-gp, its physiological
and biochemical role in effluxing drugs is worthwhile, in order to have an opportunity to improve the
bioavailability of drugs restricted by P-gp. [3]Improved clinical efficacy of various drugs observed by P-gp
inhibition, P-gp inhibitors are gaining recognition to improve bioavailability by inhibiting P-gp in intestine,
brain, liver and kidneys. P-gp can be inhibited (i) by blocking drug binding site either competitively, non-
competitive or allosterically; (ii) by interfering ATP hydrolysis ; and (iii) by altering integrity of cell membrane
lipids [3].
The bioavailability enhancement of poorly water soluble drugs by use of P-gp inhibitors finds to be
improving by use of various surfactants. Out of all the surfactants Chremophor EL [4] have been used as P-gp
inhibitors for this study. SD technique namely the HME technique was used for the preparation of formulations
which were further subjected to pharmacokinetic study. Plasticisers are included to the polymers to facilitate
thermal processing, to modify drug release from polymeric system and enhance mechanical properties and
surface appearance of dosage form. When plasticisers are added to the polymers the flexibility of the polymers
is increased by increasing the intermolecular separation of polymer molecules which results in reduction in glass
2. Dissolution And Bioavailability Enhancement…
48
transition temperature (Tg), polymer melt viscosity and tensile strength. [5] Various approaches are available to
improve dissolution rate of poorly water-soluble drug, including the use of surfactants, inclusion complexation,
drug micronization into an amorphous form and SD. [6] In the SD, the drug may be dispersed or solubilized
within a polymeric carrier at molecular levels or in the amorphous state, and provide a large surface which leads
to significant enhancement in the dissolution process. The improvement in dissolution is mainly attributed to the
reduction in particle size, increase in surface area and reduction in crystallinity. Furthermore, no energy is
required to breakup the crystal lattice of a drug during the dissolution process, and drug solubility and
wettability may be improved by surrounding hydrophilic polymers used in SD. In comparison with traditional
methods for preparation of SD, HME is a promising novel technology [7] for improving the bioavailability of
water insoluble drugs, and presents many advantages for pharmaceutical applications. It can be used as a
continuous process with the absence of organic solvents and subsequent drying steps, which makes scaling up
easier. In addition, intense blending and agitation during process prevent the aggregation of drug particles
suspending in the molten polymer, leading to a more homogeneous dispersion of fine particles. However, not all
the thermal plastic polymer carriers are compatible with the drugs and suitable carriers as well the drug/polymer
ratio for a specific drug need to be optimized. In the present studies, we attempted to improve dissolution and
bioavailability of Efv by preparation of SD with HME technique. Hydrophilic polymer with certain Tg and
backbones will be used to prepare SD. Further pharmacokinetics of Efv in rats was investigated to evaluate the
in vivo performance of prepared SD.
II. MATERIALS AND METHODS:
MATERIALS:
Efv was obtained as a gift sample from Emcure Pharmaceuticals ltd (Pune) and all other chemicals
were obtained from the college source.
Animals:
Wistar Rats ranging to about 230-290g body weight approximately were used in the study.
METHODS:
2.1 Optimization of Drug: Polymer Ratio [8]
Solubility of Efv and polymer was checked in different solvents such as methanol, ethanol and water.
Both the drug and polymer were soluble in ethanol, hence selected as a solvent for optimization of drug:
polymer ratio. Drug and polymer (1:1 to 1:5) were solubilised in ethanol. The obtained solution was then poured
into the petri plates and films were cast by solvent evaporation method and were observed after 24 hrs at room
temperature for their appearance.
2.2 Preparation of HME and NHME formulation
Different concentrations of surfactants in the range of 10%w/w -30%w/w of polymer quantity were
studied. Physical mixture of drug, polymer and surfactant were subjected to melt extrusion process. The HME
process was carried out using Thermo Scientific Prism Lab Model co-rotating intermeshing twin screw extruder
with L/D of 40/1 .The screw speed was adjusted to 100 rpm resulting in residence time in the extruder of less
than 1min along with the barrel(melting zone) temperature of 140ºC as melting point of Efv is 139-141 ºC. [2]
Physical mixtures of various formulations were passed through the hot melt extruder. Melt extrudates were
cooled at room temperature and were milled using hammer mill, involving coarse milling, fine milling and
screening. Milled HME granules were than lubricated and subsequently compressed into tablets. NHME
formulation was prepared by direct compression method.
2.3 Dissolution [9]
Tablets were evaluated for dissolution testing using:
Medium: 2% sodium lauryl sulfate in water; 900 mL, degassed
Apparatus 2: 50 rpm
Time: 30 min
2.4 Permeability studies
The prepared tablets were subjected to In vitro permeability test using dialysis membrane LA401. [10]
Where the tablets were placed in the dialysis membrane along with dissolution medium. This bag was then
introduced into the vessel just above the paddle and below the upper level of dissolution medium.
Medium: 2% sodium lauryl sulfate in water; 900 mL, degassed
Apparatus 2: 50 rpm
Time: up to 7 hrs
3. Dissolution And Bioavailability Enhancement…
49
2.5 Invivo studies:
Pharmacokinetic evaluation of Efv+ Kollidon VA64+PEG4000 (1:1:0.1), Efv+ Kollidon VA64+
Chremophor EL (1:1:0.1) and Efv+ Kollidon VA64+ sorbiton monolaurate (1:1:0.1) optimised SD were used
for in vivo studies in rats weighing 230-290 gm (n=4) of either sex at a dose equivalent to 100 mg/kg of Efv in
comparison to Efv pure drug. In vivo study protocols were approved by the Institutional Animal Ethics
Committee (Regd. No RCPIPER/IAEC/07-2013-14).
Collection of blood sample: [11]
200 µL blood samples were collected (into ependroff tubes containing 20 µL of heparin solution)
through tail vein from rats under light ether anesthesia at 30 min, 1 hour, 2 hour, 5 hour, 8 hour and 12 hours
after oral administration.
Drug solution: Efv 10 mg/mL suspension in 0.5 % CMC prepared immediately before administration
Polymeric formulations were prepared as 20 mg/mL suspensions in 0.5 % CMC prepared immediately before
administration
Dose: 100 mg/kg Efv oral
Calibration curve:
Preparation of Standard solutions in plasma as in Table 1.
TABLE 1: PREPARATION OF STANDARD SOLUTION IN PLASMA
Standard drug
solution (prepared
in Methanol)
(µg/mL)
Amount of plasma
(µL)
Amount added
(µL)
Final concentration
in
Plasma
(µg/mL)
200 995 5 1
200 990 10 2
200 975 25 5
200 963.5 37.5 7.5
2000 995 05 10
2000 990 10 20
Extraction procedure for the plasma samples and calibration curve related samples was as follows
Extraction procedure:
Blood samples were centrifuged at 1500 rpm for 10 minutes for separation of serum
To 75 µL of serum sample, 10 µl of internal standard (100 ppm propyl paraben solution in methanol) and
30 µL of 1.0 N NaOH solution was added and this mixture was extracted twice with 2 mL dichloromethane.
After addition of dichloromethane, each time the samples were vortexed for 5 minutes.
The vortexed samples were centrifuged at 2000 rpm for 10 minutes.
Dichloromethane layers (lower layers) were pooled and dried at room temperature.
The dried dichloromethane extracts were reconstituted in 200 µl mobile phase, filtered through 0.2 µ and
processed for HPLC analysis as stated below.
HPLC analysis:
The HPLC system Agilent 1200 HPLC, a gradient quaternary system (having four ports/reservoirs for
mobile phase), a manual rheodyne injector of 20 µm loop with DAD detector (diode array detector system)
was used.
The HPLC column used in this study was Luna C 18 (2) stationary phase with 25 cm length, 4.6 mm
internal diameter and 5 µm particle size.
HPLC analysis of standard mixture of Efv and propyl paraben: The different methods were tried to
obtain Efv peak well resolved from the peak of internal standard propylparaben. HPLC chromatograph of
mixture of Efv and propyl paraben were well resolved by optimized chromatographic conditions and is
provided below. It is necessary that the standard mixture of Efv and propyl paraben should passes the
system suitability parameters like capacity factor, number of theoretical plates, tailing factor and resolution.
With the optimized chromatographic parameters (stationary phase, mobile phase, flow rate, detection
wavelength, volume of injection applied) the standard mixture of Efv and propyl paraben is well resolved.
4. Dissolution And Bioavailability Enhancement…
50
Initially, the sample of Efv and propylparaben were dissolved in methanol (as all the compounds are soluble
in methanol).
Then, dilution of all the samples made with mobile phase [Efv (5 ppm) + Propyl paraben (5 ppm)] was
performed.
The column was saturated with mobile phase with 1 mL/min flow rate.
Mobile Phase: Methanol: Water (80:20, v/v)
Wavelength of detection: 254 nm
The HPLC method revalidated was found suitable for the estimation of Efv in plasma samples. The mobile
phase consists of a mixture of Mobile Phase: Methanol: Water (80:20 v/v).
III. RESULTS AND DISCUSSION
Based on film casting method, 1:1 ratio of Drug: Polymer was finalized as no recrystallization of API
was observed in the film after 48 hours of storage. Recrystallization was observed in sample of pure drug only.
This indicated that 1:1 drug: polymer ratio was sufficient to hold the amorphous form of API in solid solution.
Use of 10%w/w concentration of surfactants gives same solubility enhancement as compared to use of 20%w/w
and 30%w/w concentrations. So 10%w/w concentration of surfactants was finalized in formulations and only
these formulations were subjected to further study like dissolution, permeability and in vivo study.
FIGURE 1: DISSOLUTION COMPARISON HME AND NHME FORMULATIONS
Kollidon VA 64 is a hydrophilic polymer and form a gel on the surface of tablet when comes in contact with
dissolution media. These tablets shows disintegration pattern by erosion mechanism. The disintegration time
(DT) of tablets of HME formulations was about three times more than DT of NHME formulation. Higher DT
affected the complete dissolution of HME formulations in 30 min. Office of Generic Drugs (OGD) of US FDA
suggested the dissolution time points upto 180 min for Norvir tablets (Ritonavir) [12] may be due to prolong
disintegration time of the dosage form. Norvir tablets are also manufactured by using HME technology. [13]
So, it was decided to perform dissolution of Efv upto 180min to achieve complete drug release. As expected the
complete release was observed at 180 min but, the dissolution rate of HME formulations is quite slower than
NHME formulation may be due to higher DT of HME formulations. (as in fig. 1) Different types of surfactants
did not show any improvement in dissolution rate or may not be reflected by present dissolution method.
Official dissolution method of Efv was unable to discriminate the formulation changes in dissolution profile.
5. Dissolution And Bioavailability Enhancement…
51
FIGURE 2: PERMEABILITY COMPARISON HME AND NHME FORMULATIONS
Invitro permeability method using dialysis membrane was able to discriminate formulation changes.
Formulation with 10%w/w PEG 4000 and Sorbiton monolaurate shows improvement in dissolution rate may be
due to higher HLB values of 12 and 18.5 respectively than HLB [14, 15] value 8 of Chremophor EL [16].
Higher is the HLB value of surfactant higher will be the depression in Tg [17] of polymer which leads to
lowering of melt viscosity and increases intermolecular separation of polymer. Lower melt viscosity of polymer
increases the efficiency of mixing of API and polymer. Increased intermolecular separation in polymer chains
improves the molecular level dispersion of API in polymer bed. NHME tablets shows lower in vitro
permeability compared to all Efv HME formulations (fig. 2), even though have higher dissolution rate. Increase
in, in vitro solubility and permeability may increase the bioavailability which leads to reduction in some fold of
Efv dose.
FIGURE 3: ANIMAL STUDY
6. Dissolution And Bioavailability Enhancement…
52
FIGURE 4: CALIBRATION CURVE
Linearity of the method was in the concentration range 0.5- 10 μg/0.5 mL of Plasma (Fig. 4 ). Plasma
concentrations of Efv following the oral administration of API and its SD is shown in Fig. 3. Pharmacokinetic
parameters estimated are summarized in Table 2.
Efv was found to be absorbed rapidly when given orally, and a highest peak plasma concentration (Cmax) 4.1
μg/mL was observed at 2.25 hrs after administration of E3 formulation (Montane 20PHA).
All the pharmacokinetic parameters (Table 2) namely Cmax, Tmax, (AUC) ∞ indicated rapid and higher
absorption of Efv when administered as SD (E1) prepared using PEG 4000. Similar Cmax value and higher
Tmax value was observed with the SD E1 (PEG 4000) compared to those of Efv in NHME form. Higher Cmax
and lower Tmax values were observed with E3 formulation and plain API respectively. AUC0-∞ was also much
higher in case of SD prepared with PEG 4000 when compared to plain API and other HME formulations. AUC0-
∞ was increased from 43 for Efv API to 89, 52 and 52 for E1, E2, E3 formulations respectively. Extent of
absorption was increased by 106.98%, 20.93%, and 20.93% in E1, E2, and E3 formulations respectively.
Noticeable boost in AUC0-∞ of E1 formulation was observed may be due to high HLB value of PEG 4000
(HLB- 18.5). HLB values of Montane 20PHA and Chremophor EL are 12 and 8 respectively so comparatively
less improvement in absorption was observed in E2 and E3 formulations. Higher the HLB value of surfactant
higher will be the drop in Tg of polymer during HME process which reduces melt viscosity of polymer and
allows maximum and efficient mixing of drug and polymer to form ideal solid solution. Efv is not a substrate
[18] of P-gp activity so P-gp inhibitor like Chremophor EL failed to enhance its bioavailability. Montane
20PHA does not have P-gp inhibition activity and has lower HLB value, hence comparatively less improvement
in absorption was observed.
TABLE 2: PHARMACOKINETIC PARAMETERS OF EFV
PARAMETERS
SAMPLES
Tmax
(hrs)
Cmax
(μM)
AUClast
(hr*µM)
AUCinf
(hr*µM)
MRTinf
(hr)
Efv 1.25 3.9 26 43 12
E1 1.50 3.9 28 89 34
E2 1.50 3.6 30 52 14
E3 2.25 4.1 32 52 12
7. Dissolution And Bioavailability Enhancement…
53
IV. CONCLUSION
SD prepared using PEG 4000 improved the bioavailability where as other SD failed to improve almost
none of the pharmacokinetic parameters. This study reveals the solubility enhancement by HME technology and
bioavailability enhancement was mainly achieved by surfactant with higher HLB value like PEG 4000. Use of
comparatively hydrophobic surfactants like Montane 20PHA not improved the absorption due to its lower HLB
value and lack of P-gp inhibition activity. Surfactant like Chremophor EL failed to modify or enhance rate and
extent of absorption, as Efv was not a substrate of P-gp activity.
HME technology improved the physical parameters and pharmacokinetic parameters which confirmed the
versatile application of this technology in pharmaceutical development of poorly water soluble drugs.
ACKNOWLEDGEMENT
The authors are thankfull to Principal Dr. S. N. Dhole Modern College of Pharmacy (for Ladies),
Moshi for providing necessary support and facilities. I am also thankfull to Dr. C. R. Patil for providing his
support for carrying out animal study.
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