This document describes the development and optimization of a herbal film coating for losartan potassium tablets using Moringa oleifera gum. Moringa oleifera gum was extracted from the plant using a water-based extraction procedure. The gum was used with hydroxypropyl methylcellulose to form coating formulations at different ratios. Losartan potassium tablets were prepared by wet granulation and coated with the formulations. The coated tablets were evaluated for properties like disintegration, drug content and release kinetics. The best formulation was selected based on the evaluation and subjected to stability studies.
Phytotherapeutics and Endodontics - A ReviewQUESTJOURNAL
ABSTRACT : Over the years, Phytomedicine has been gaining attention worldwide. It has been used in dentistry as anti-inflammatory, antibiotic, analgesic, sedative and also as endodontic irrigant. The herbal alternatives for endodontic usage might prove to be advantageous. This review focuses on various natural drugs and products as well as their therapeutic applications when used as phytomedicine in endodontics.
Phytotherapeutics and Endodontics - A ReviewQUESTJOURNAL
ABSTRACT : Over the years, Phytomedicine has been gaining attention worldwide. It has been used in dentistry as anti-inflammatory, antibiotic, analgesic, sedative and also as endodontic irrigant. The herbal alternatives for endodontic usage might prove to be advantageous. This review focuses on various natural drugs and products as well as their therapeutic applications when used as phytomedicine in endodontics.
Formulation and evaluation ofmetformin HCl micro beads by ionotropic gelation...Sagar Savale
The Metformin HCL Micro Beads is formulated by the Ionotropic Gelation Method. The CMC is a Swellable
polymer is responsible for the Sustained release action or activity. A combination of CMC (Carboxy Methyl
Cellulose) and Sodium Alginate shows better sustained release activity. The PreparedSustained released Micro
Beadsis Evaluated In terms of bulk density, tapped density, angle of repose, Carr’s Index, Swelling Index, Drug
Content, % Encapsulation Efficiency and vitro study. The result associated in Optimized batch is good to
Satisfactory and having a good free flowing property. The Drug Content and % Encapsulation Efficiency values are
within the pharmacopeia limit. The in vitro Dissolution studies shows Maximum percentage of release of drug
(71.15) with in end of 4 Hours.
The word “banana” is a general term comprising a number of species or hybrids in the genus Musa of family Musaceae. Many studies reported that banana is a good source of phenolic compounds, which are having potential health benefits in human beings. The phytochemical composition of eight banana varieties was investigated. Quantitative estimation of phytochemicals revealed that highest alkaloid and tannin content was noticed in variety Nendran (3.76% and 4.40 mg/100g respectively). Whereas, variety Rasakadali exhibited highest flavonoid content (9.49 mg/100). Total phenol and saponin content was found higher in variety Kadali (0.82% and 11.6 mg/100g respectively).
PREPARATION AND IN-VITRO EVALUATION OF ITRACONAZOLE LOADED NANOSPONGES FOR T...Mahewash Sana Pathan
Itraconazole is an imidazole derivative and used for the treatment of local and systemic fungal infections. It is a BCS Class II drug having very low solubility in water i.e. 1-4ng/ml. The oral use of Itraconazole is not much recommended as it has many side effects. The present research has been undertaken with the aim to develop a topical hydrogel formulation of Itraconazole loaded nanosponges to increase the solubility, permeability and stability of itraconazole. Itraconazole loaded nanosponge was prepared by emulsion solvent diffusion method by using different concentrations of ethyl cellulose as a polymer, Polyvinyl alcohol as surfactant and dichloromethane as cross linking agent. Physical characteristics of the nanosponges as well as the drug entrapment efficiency, percentage drug content, Percent yield, drug polymer compatibility, solubility studies of the nanosponges were investigated. Particle size analysis and surface morphology of nanosponges were performed. The scanning electron microscopy of nanosponges showed that they were spherical in shape and spongy in nature. Drug entrapment efficiency was found to be in the range of 42.75 % to 73.10 %. The optimized nanosponge formulation was loaded into hydrogel using carbopol 940 and studied for pH, viscosity, in vitro drug release. Of the nanosponge formulations prepared, F4 was found to show drug release of 70.62%. It was concluded that Itraconazole nanosponge hydrogel may have increased solubility and drug release
formulation and evaluation of microbeadsgurleen kaur
Microencapsulation has been employed to sustain the drug release, reduce or eliminate drug related adverse effects, dose intake and improve the bioavailability inspite drug undergo extensive first pass metabolism ultimately improve the compliance in pharmacotherapy of inflammation and pain.
Microencapsulation by ionotropic gelation technique is one of the widely used method for preparation of calcium alginate beads which has ability to form gels reaction with calcium salts .
Microencapsulation has been employed to sustain the drug release, reduce or eliminate drug related adverse effects, dose intake and improve the bioavailability inspite drug undergo extensive first pass metabolism ultimately improve the compliance in pharmacotherapy of inflammation and pain.
Microencapsulation by ionotropic gelation technique is one of the widely used method for preparation of calcium alginate beads which has ability to form gels reaction with calcium salts .
In vitro antioxidant, antimicrobial and cytotoxic activities of the various e...Akhil Gupta
The present study was designed to investigate antioxidant, antimicrobial and cytotoxic potential of pet ether, chloroform and methanol extracts of Ganoderma lucidum available in Bangladesh.
Monoherbal formulation development for laxative activitypharmaindexing
The Ayurvedic Pharmacopoeia specifically approves flaxseed as a poultice for boils externally and demulcent or laxative internally. In this study monoherbal formulation development for laxative activity of flaxseed was undertaken. The plantLinumusitatissimumhasshowed higher percentage of total ash as well as alcohol soluble extractive values. The aqueous extract of Linumusitatissimumwas prepared by using pilot scale extraction plant and spray drying unit. The qualitative phytochemical studies reveal the presence of amino acids, carbohydrates, vitamins and proteins. From the available literatures it was found that Linumusitatissimum contains more number of amino acids. The formulated tablets showed acceptable pharmacopoeial limits and complies with specifications for thickness, hardness, friability and weight variation. The formulation has showed better laxative activity indicating additive property of the combined phytoconstituents of the plant.
Formulation and evaluation ofmetformin HCl micro beads by ionotropic gelation...Sagar Savale
The Metformin HCL Micro Beads is formulated by the Ionotropic Gelation Method. The CMC is a Swellable
polymer is responsible for the Sustained release action or activity. A combination of CMC (Carboxy Methyl
Cellulose) and Sodium Alginate shows better sustained release activity. The PreparedSustained released Micro
Beadsis Evaluated In terms of bulk density, tapped density, angle of repose, Carr’s Index, Swelling Index, Drug
Content, % Encapsulation Efficiency and vitro study. The result associated in Optimized batch is good to
Satisfactory and having a good free flowing property. The Drug Content and % Encapsulation Efficiency values are
within the pharmacopeia limit. The in vitro Dissolution studies shows Maximum percentage of release of drug
(71.15) with in end of 4 Hours.
The word “banana” is a general term comprising a number of species or hybrids in the genus Musa of family Musaceae. Many studies reported that banana is a good source of phenolic compounds, which are having potential health benefits in human beings. The phytochemical composition of eight banana varieties was investigated. Quantitative estimation of phytochemicals revealed that highest alkaloid and tannin content was noticed in variety Nendran (3.76% and 4.40 mg/100g respectively). Whereas, variety Rasakadali exhibited highest flavonoid content (9.49 mg/100). Total phenol and saponin content was found higher in variety Kadali (0.82% and 11.6 mg/100g respectively).
PREPARATION AND IN-VITRO EVALUATION OF ITRACONAZOLE LOADED NANOSPONGES FOR T...Mahewash Sana Pathan
Itraconazole is an imidazole derivative and used for the treatment of local and systemic fungal infections. It is a BCS Class II drug having very low solubility in water i.e. 1-4ng/ml. The oral use of Itraconazole is not much recommended as it has many side effects. The present research has been undertaken with the aim to develop a topical hydrogel formulation of Itraconazole loaded nanosponges to increase the solubility, permeability and stability of itraconazole. Itraconazole loaded nanosponge was prepared by emulsion solvent diffusion method by using different concentrations of ethyl cellulose as a polymer, Polyvinyl alcohol as surfactant and dichloromethane as cross linking agent. Physical characteristics of the nanosponges as well as the drug entrapment efficiency, percentage drug content, Percent yield, drug polymer compatibility, solubility studies of the nanosponges were investigated. Particle size analysis and surface morphology of nanosponges were performed. The scanning electron microscopy of nanosponges showed that they were spherical in shape and spongy in nature. Drug entrapment efficiency was found to be in the range of 42.75 % to 73.10 %. The optimized nanosponge formulation was loaded into hydrogel using carbopol 940 and studied for pH, viscosity, in vitro drug release. Of the nanosponge formulations prepared, F4 was found to show drug release of 70.62%. It was concluded that Itraconazole nanosponge hydrogel may have increased solubility and drug release
formulation and evaluation of microbeadsgurleen kaur
Microencapsulation has been employed to sustain the drug release, reduce or eliminate drug related adverse effects, dose intake and improve the bioavailability inspite drug undergo extensive first pass metabolism ultimately improve the compliance in pharmacotherapy of inflammation and pain.
Microencapsulation by ionotropic gelation technique is one of the widely used method for preparation of calcium alginate beads which has ability to form gels reaction with calcium salts .
Microencapsulation has been employed to sustain the drug release, reduce or eliminate drug related adverse effects, dose intake and improve the bioavailability inspite drug undergo extensive first pass metabolism ultimately improve the compliance in pharmacotherapy of inflammation and pain.
Microencapsulation by ionotropic gelation technique is one of the widely used method for preparation of calcium alginate beads which has ability to form gels reaction with calcium salts .
In vitro antioxidant, antimicrobial and cytotoxic activities of the various e...Akhil Gupta
The present study was designed to investigate antioxidant, antimicrobial and cytotoxic potential of pet ether, chloroform and methanol extracts of Ganoderma lucidum available in Bangladesh.
Monoherbal formulation development for laxative activitypharmaindexing
The Ayurvedic Pharmacopoeia specifically approves flaxseed as a poultice for boils externally and demulcent or laxative internally. In this study monoherbal formulation development for laxative activity of flaxseed was undertaken. The plantLinumusitatissimumhasshowed higher percentage of total ash as well as alcohol soluble extractive values. The aqueous extract of Linumusitatissimumwas prepared by using pilot scale extraction plant and spray drying unit. The qualitative phytochemical studies reveal the presence of amino acids, carbohydrates, vitamins and proteins. From the available literatures it was found that Linumusitatissimum contains more number of amino acids. The formulated tablets showed acceptable pharmacopoeial limits and complies with specifications for thickness, hardness, friability and weight variation. The formulation has showed better laxative activity indicating additive property of the combined phytoconstituents of the plant.
Monoherbal formulation development for laxative activitypharmaindexing
The Ayurvedic Pharmacopoeia specifically approves flaxseed as a poultice for boils externally and demulcent or laxative internally. In this study monoherbal formulation development for laxative activity of flaxseed was undertaken. The plantLinumusitatissimumhasshowed higher percentage of total ash as well as alcohol soluble extractive values. The aqueous extract of Linumusitatissimumwas prepared by using pilot scale extraction plant and spray drying unit. The qualitative phytochemical studies reveal the presence of amino acids, carbohydrates, vitamins and proteins. From the available literatures it was found that Linumusitatissimum contains more number of amino acids. The formulated tablets showed acceptable pharmacopoeial limits and complies with specifications for thickness, hardness, friability and weight variation. The formulation has showed better laxative activity indicating additive property of the combined phytoconstituents of the plant.
Hepatoprotective activity and sub acute toxicity study of whole part of the p...Cây thuốc Việt
Objective: The present investigation aimed at phytochemical screening of the whole plant of Anoectochilus formosanus Hayata (Orchidaceae) after successive extraction followed by hepatoprotective activity of its aqueous extract. The research work also focused on the sub acute toxicity study of
aqueous extract of the same plant. Methods: Successive extraction was carried out with petroleum ether, chloroform, methanol and water respectively. Hepatoprotective activity of its aqueous extract was investigated in carbon tetrachloride, ethanol and paracetamol induced hepatotoxic rat models and compared with silymarin (20 mg/kg) as reference standard. Sub acute toxicity study was elicited by studying the effect of Anoectochilus formosanus on the lipid profile, biochemical parameters and hematological parameters in rats and compared with standard silymarin (20 mg/kg). Results: Phytochemical screening revealed the presence of anthraquinone glycosides, cardiac glycosides, reducing sugars, carbohydrates, phenolic compounds, tannins, flavonoids and saponins in the aqueous extract of the plant under investigation. Two way analysis of variance study of the
estimated biochemical parameters for instance, aspartate aminotransferase, alanine amino transferase and alkaline phosphatase were revealed that there is significant difference (p-value < 0.0001) exists between the different treatment groups supported by least significant difference test of various biochemical parameters, which was also evident from the histopathological study of liver sections. Sub acute toxicity study revealed no significant toxic effects. Conclusion: Aqueous extract of Anoectochilus formosanus (200 mg/kg) had shown significant hepatoprotective activity as compared to standard silymarin. Sub acute toxicity studies had concluded that it might be considered safe for a longer duration of time
Protective Effect of Leaves of Ficus carica Against Carbon Tetrachloride-Indu...UKJPB Journal
The outcomes of histological study revealed that there was significant reversal of histological functional of liver. In conclusion, the findings of this study validated that the Ficus carica can improve CCl4-induced hepatotoxicity.
Preliminary phytochemical studies and evaluation of Antipyretic property of t...researchplantsciences
Purpose-The root of Ritchiea longipedicellata was claimed to have anti pyretic, analgesic and antimicrobial properties. The people of Idemili area in Anambra State of Nigeria use the decoction of it to treat wounds, running stomach, aches and pains as well as fever. It is to this backdrop that this investigation was carried out to ascertain the veracity of the claim.
Methodology-The root of Ritchiea longipedicellata was collected and dried at ambient temperature. It was pulverized into powder. 500 gm of the powdered drug was placed into a two litre beaker containing one litre of methanol. It was allowed to stand with occasional shaking for 48 h. The content was filtered and the filtrate was concentrated using rotary evaporator. The extract contains the following secondary metabolites-alkaloids, flavonoids, terpenoids, saponins and glycosides. The antipyretic activity was investigated using brewer’s yeast to induce pyrexia.
Result -The root of Ritchiea longipedicellata exhibited significant (p<0.05) antipyretic effect at 600 mg/kg from 1 h to 4 h and at 3 h to 4 h at 300 mg/kg compared with the control.
Conclusion-The claim of Idemili people of Anambra State Nigeria on the use of Ritchiea longipedicellata appears to be obvious in line with the results of the investigation.
Article Citation:
Chinedu Fred Anowi, Ezugwu CO, Ilodigwe EE, Ajaghaku DL.
Preliminary Phytochemical Studies and Evaluation of Antipyretic Property of the Methanol Extract of the Rootbark of Ritchiea longipedicellata Gilg (capparidaceae)
Journal of Research in Plant Sciences (2013) 2(2): 192-195.
Full Text:
http://plantsciences.co.in/documents/PS0048.pdf
Formulation, Development and Evaluation of Fast Disintegrating Tablet of Piro...ijtsrd
The solubility behavior of drugs remains one of the most exigent aspects in formulation development. With the advent of combinatorial chemistry and high throughput screening, the number of poorly water soluble compounds has dramatically increased. Among all the newly discovered chemical entities, about 40 45 drugs fail to reach market due to their poor water solubility. Because of solubility problem, bioavailability of drugs gets affected and hence solubility enhancement becomes necessary. In present study the attempts have been made to increase the dissolution of BCS class 2 drug Piroxicam using hydrophilic polymers namely polyethylene glycol PEG 6000 and sodium lauryl sulphate as a surfactant by using solid dispersion technique. In solid dispersion microwave induced solid dispersion and conventional fusion method is compared. Drug polymer complex was prepared using batch method. Maximum dissolution rate was obtained of the complex prepared from Piroxicam PEG6000 SLS . A successful solubility enhancement of drug complex was confirmed by taking drug release in phosphate buffer pH 6.8. The drug was characterized according to different compendial methods, on the basis of identification by UV spectroscopy, organoleptic properties and other tests. After that among the all formulation batches, solid dispersion F16 was selected for further tablet formulation batches, nine formulations were developed and studied. The values of pre compression parameters was evaluated, results were within prescribed limits and indicated good free flowing properties. The data obtained of post compression parameters such as weight variation, hardness, friability, wetting time, water absorption ratio, content uniformity, disintegration time and dissolution was found to superior over conventional formulation. The F9 batch with disintegrating time 10 ± 0.52 second and dissolution 93.20 ± 0.61 was selected as optimized formulation and was found superior over other formulation. Batch F9 was also subjected to stability studies for three months and was tested for its disintegrating time, drug contents and dissolution behavior monthly. F9 formulation after stability study was found to be stable. Mr. Yennuwar Dhiresh Pramod | Mr. Sujit Kakade | Mrs. Trusha Shangrapawar | Dr. Ashok Bhosale "Formulation, Development and Evaluation of Fast Disintegrating Tablet of Piroxicam using Solid Dispersion Technique" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-6 | Issue-5 , August 2022, URL: https://www.ijtsrd.com/papers/ijtsrd50422.pdf Paper URL: https://www.ijtsrd.com/pharmacy/pharmaceutics/50422/formulation-development-and-evaluation-of-fast-disintegrating-tablet-of-piroxicam-using-solid-dispersion-technique/mr-yennuwar-dhiresh-pramod
In Ayurveda, the leaf juice of Adhatoda vasica, a shrub native to Asia is incorporated in
many traditional herbal formulations. However, suitable solvent and a suitable extraction
method for phytochemical profiling are not well established, and there is no published mass
spectra structural interpretation of the identified compounds. This has caused a few
problems in herbal formulation research due to the bias derived from different extraction
methods. Therefore, this study used polar and non polar extraction for phytochemical
analysis on Adhatoda vasica, aiming to assess the potential impact of different solvents. This
study included extractive value, total phenol and alkaloid content of the leaves in different
preparations. Gas Chromatography coupled with Mass Spectrometry (GC-MS) was used to
study the phytochemical profile of different solvents. Significant differences were observed in
all the parameters such as extract yield, total phenol, total alkaloid and phytochemical
composition. The ethanol extract stood out most for effective extraction of phytochemicals,
especially for the alkaloids. The results highlight the necessity for comparative analyses of
chemical composition in different solvent extractions and careful choice and validation of
analytical methodology in herbal formulation research.
Student information management system project report ii.pdfKamal Acharya
Our project explains about the student management. This project mainly explains the various actions related to student details. This project shows some ease in adding, editing and deleting the student details. It also provides a less time consuming process for viewing, adding, editing and deleting the marks of the students.
Final project report on grocery store management system..pdfKamal Acharya
In today’s fast-changing business environment, it’s extremely important to be able to respond to client needs in the most effective and timely manner. If your customers wish to see your business online and have instant access to your products or services.
Online Grocery Store is an e-commerce website, which retails various grocery products. This project allows viewing various products available enables registered users to purchase desired products instantly using Paytm, UPI payment processor (Instant Pay) and also can place order by using Cash on Delivery (Pay Later) option. This project provides an easy access to Administrators and Managers to view orders placed using Pay Later and Instant Pay options.
In order to develop an e-commerce website, a number of Technologies must be studied and understood. These include multi-tiered architecture, server and client-side scripting techniques, implementation technologies, programming language (such as PHP, HTML, CSS, JavaScript) and MySQL relational databases. This is a project with the objective to develop a basic website where a consumer is provided with a shopping cart website and also to know about the technologies used to develop such a website.
This document will discuss each of the underlying technologies to create and implement an e- commerce website.
Hybrid optimization of pumped hydro system and solar- Engr. Abdul-Azeez.pdffxintegritypublishin
Advancements in technology unveil a myriad of electrical and electronic breakthroughs geared towards efficiently harnessing limited resources to meet human energy demands. The optimization of hybrid solar PV panels and pumped hydro energy supply systems plays a pivotal role in utilizing natural resources effectively. This initiative not only benefits humanity but also fosters environmental sustainability. The study investigated the design optimization of these hybrid systems, focusing on understanding solar radiation patterns, identifying geographical influences on solar radiation, formulating a mathematical model for system optimization, and determining the optimal configuration of PV panels and pumped hydro storage. Through a comparative analysis approach and eight weeks of data collection, the study addressed key research questions related to solar radiation patterns and optimal system design. The findings highlighted regions with heightened solar radiation levels, showcasing substantial potential for power generation and emphasizing the system's efficiency. Optimizing system design significantly boosted power generation, promoted renewable energy utilization, and enhanced energy storage capacity. The study underscored the benefits of optimizing hybrid solar PV panels and pumped hydro energy supply systems for sustainable energy usage. Optimizing the design of solar PV panels and pumped hydro energy supply systems as examined across diverse climatic conditions in a developing country, not only enhances power generation but also improves the integration of renewable energy sources and boosts energy storage capacities, particularly beneficial for less economically prosperous regions. Additionally, the study provides valuable insights for advancing energy research in economically viable areas. Recommendations included conducting site-specific assessments, utilizing advanced modeling tools, implementing regular maintenance protocols, and enhancing communication among system components.
1. International Journal of Research in Advent Technology, Vol.7, No.1, January 2019
E-ISSN: 2321-9637
Available online at www.ijrat.org
440
Screening, Development and Optimization of an herbal
film former for the purpose of film coating of losartan
potassium tablets
Mr. Ayan Kumar Kar1
, Miss Banhishikha Kar2
, Dr. Amitava Roy3
, Mr. Hiranmoy Parya5
, Dr. Jyotirmoy
Dev4
1,2,5
Department of Pharmaceutics, Calcutta Institute of Pharmaceutical Technology & AHS, Banitabla, Uluberia-
721636, Howrah, West Bengal, India.
3
Department of Pharmaceutics, Himalayan Pharmacy Institute, Majitar, Rangpo, East Sikkim, West Bengal, India.
4
Department of Pharmacy, HUDA Group of Institutions, Nagaon, Assam.
Email : ayancipt@gmail.com1
Abstract: Film coated Losartan potassium tablet was prepared by the wet granulation method with a coat consisting
of different proportion of the respective synthetic polymer hydroxypropyl methyl cellulose and the natural herbal
polymer Moringa Oleifera which is the main objective of my project work for its gum, exudates and adhesive
yielding properties. Moringa Oleifera belongs to a monogeneric family, the Moringaceae. Water based extraction
procedure was used to extract the gum that is used for the purpose of film coating on a model drug, namely losartan
potassium tablets to retard its release. Primary development of the coating formulation has done on the basis of
optimization of different in-process physical parameters. Hence, there is no interaction between drug and polymers
used in the study. After coating with different proportion of synthetic and extracted natural polymer, primarily visual
observation was done to show the normal defect during the preliminary coating procedure like chipping, cracking
etc. Simultaneous evaluation of the uncoated and coated tablets for its physical performances like disintegration,
hardness etc was satisfactory. The release data was analyzed according to different kinetic equations where it is
normally said to follow non-fickian anomalous release. The stability study was carried based on the best
formulation.
Keywords: Moringa Oleifera1; Losartan Potassium2; Hydroxypropyl methyl cellulose3; Wet granulation method4.
1. INTRODUCTION
The oral route of drug administration is the most
important method of administering the drugs to the
systemic effects. Solid dosage forms represent the
preferred class of the product. Among the drugs
administered orally, solid dosage forms represent the
preferred choice of class of product. Most common
solid oral dosage forms are tablets and capsules.
Tablets and capsules account for well over half the
total number and cost of all prescription issued. In
December 1843, a patent was granted to the
Englishman, William Brockedon, for a machine to
compress powders to form compacts. The invention
was first used to produce compacts of potassium
bicarbonate and caught the imagination of a number
of pharmaceutical companies. Later, in Britain the
first company was to use the term tablets to describe
the compressed dosage forms. Generally, tablets are
oral, solid, unit dosage form containing one or more
than one medicaments. It is normally swallowed with
water but some tablets may be chewed, dissolved or
dispersed in water before administration or some are
retained in the buccal cavity of the mouth [1]
. The
granulation process combines one or more powders
and forms a granule that will allow the tableting
process to be predictable and will produce quality
tablets within the required tablet-press speed range. A
tablet formulation contains several ingredients, and
the active ingredient is the most important among
them. The remaining ingredients are necessary
because a suitable tablet cannot be composed of
active ingredients alone. The tablet may require
variations such as additional bulk, improved flow,
better compressibility, flavoring, improved
disintegration characteristics, or enhanced appearance
[2]
. Losartan Potassium is the first of a new class of
drugs to be introduced for clinical use in
hypertension. It is an orally active, non-peptide
angiotensin II receptor (type AT1) antagonist.
Angiotensin receptor blockers (ARBs) represent an
2. International Journal of Research in Advent Technology, Vol.7, No.1, January 2019
E-ISSN: 2321-9637
Available online at www.ijrat.org
441
important therapeutic advance in the blockade of the
rennin-Angiotensin pathways. Losartan is an orally
active agent that undergoes substantial first pass
metabolism by cytochrome P450 enzymes. It is
converted, in part, to an active carboxylic acid
metabolite which is also responsible for Angiotensin-
II receptor antagonism that follows Losartan
treatment. In vitro studies indicate that cytochrome
P450, 2C9 and 3A4 are involved in the
biotransformation of Losartan to its metabolite. Oral
absorption of Losartan is not affected by food, but
bioavailability is only 33% due to first pass
metabolism. It is partially carboxylated in liver to an
active metabolite E3174 which is a 10-30 times more
potent noncompetitive AT1 antagonist [3]
.
The Miracle Tree [4]
, Moringa Oleifera is the most
widely cultivated species of a monogeneric family,
the Moringaceae that is native to the sub-Himalayan
tracts of India, Pakistan, Bangladesh and
Afghanistan. This tree has in recent times been
advocated as an outstanding indigenous source of
highly digestible protein, Ca, Fe, Vitamin C, and
carotenoids suitable for utilization in many of the so-
called “developing” regions of the world where
undernourishment is a major concern. All parts of the
tree are considered to possess medicinal properties
and used in the treatment of ascites, rheumatism,
venomous bites and as cardiac, circulatory stimulant
and others3
which is shown in Figure 1 [5]
.
2. MATERIAL AND METHODS
Losartan Potassium was obtained as a gift sample
from Orchid Pharmaceuticals Ltd, Chennai. Hydroxy
propylmethyl cellulose was obtained from Loba
Chemie Pvt. Ltd., Mumbai. Other chemicals like
lactose, PVP, starch and talc was obtained from S.D.
Fine Chem. Limited, Mumbai. The Moringa Oleifera
exudates were collected from the local areas of the
Himalayan region and PEG- 4000, Propylene Glycol,
Glycerine were purchased from S.D Fines Chemical,
Mumbai. All other chemicals were used as analytical
grade.
Preparation of Moringa Oleifera Extract [6]
:-
Collection of the exudates:-
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442
The fresh exudates were collected from the fully
grown Moringa Oleifera trees growing local areas of
the Himalayan region. The bark of the trees were
scrapped off and left undisturbed for 7-10 days. The
scrapped portions were covered with a cotton
membrane to prevent exposure to direct sunlight. The
exudates in the form of the hard lumps were collected
by using a hard knife after 10th
days.
Preparation of the Moringa oleifera powder
(polymer):-
Purified water was found to be the best solubility’s
medium for Moringa oleifera. This was done by
addition of the powder extracts with water on a glass
beaker and was heated up to 60-700
C with continuous
stirring. Once the powder gets dissolved within the
aqueous phase, the whole content was poured on a
Maslin cloth for filtration and the filtrate was
collected in another glass beaker. The filtrate was
mixed with an antioxidant, ascorbic acid to prevent
any further oxidative damages and a edible
preservative, methyl paraben to prevent the further
microbial degradation. The filtrate was sprayed on a
previously clean tray dries and subjected to dry on an
hot air oven(lab instruments, siliguri) at 400
±20
C,
After 2 days of drying the flakes obtained at the
bottom were collected and was crushed in the mill
(Shakti engineering, India). The powders were
collected and were stored in a completely air-tight
zipper pack for further use.
Determination of λmax by scanning and Preparation
of Standard Graph of losartan potassium:-
About 100mg Losartan potassium powder were
weighed out accurately and taken in respective 100
ml volumetric flask and Kept 10 min with some
amount of water for complete reaction. Finally the
volume was made up to mark with the water. The
absorbance was measured at 205.5 nm in UV visible
Spectrophotometer (UV-1700, Shimadzu, Japan)
against a blank. A graph was plotted by taking
concentration vs. absorbance. The slope and
regression value was calculated from the graph which
is given in Figure 2.
Fourier Transform Infrared Radiation
measurement (FTIR) [7]
:-
To determine any interaction between drug and
polymer, Fourier Transform Infrared (FTIR-840,
Shimadzu, Japan) study was carried out. FTIR was
recorded on FTIR-840, Shimadzu, Japan. Samples
were triturated with potassium bromide and transform
into the disk. Disk was applied to the centre of the
sample holding device and scanned between 4000-
400 cm-1
at a resolution of 2 cm-1
. The IR scans were
processed using IR solution and represented as
percentage transmittance (% T) on a common scale.
The FTIR study of pure drug, Losartan Potassium
and the extracted herbal polymer, Moringa Oleifera
was given in Figure 3 and Figure 4 and the
interaction study of drug with polymers was also
given in Figure 5 and Figure 6.
Preparation of coating solution [7],[8]
:-
In a 200 ml clean beaker about 100 ml of purified
water was measured and the weighed amount of
natural polymer Moringa Oleifera was added and
allowed to soak overnight. Next morning, it was
stirred using a magnetic stirrer (Remi motors,
Mumbai) for 10-20 minutes to get a uniform
dispersion of the polymer solution. Other ingredients
such as plasticizer, opacifier, colouring agent were
added gradually in required qualities which is given
in Table 1.
Table 1: Different ratio of the coating solution.
Formulations Moringa
Oleifera
HPMC Plasticizer
(Glycerine)
Colourants Opacifier
(T2O)
Distilled
Water
F1 (%)W/W ----- 2 2 0.6 1.5 q.s.
F2 (%)W/W ----- 4 2 0.6 1.5 q.s.
F3 (%)W/W ----- 6 2 0.6 1.5 q.s.
4. International Journal of Research in Advent Technology, Vol.7, No.1, January 2019
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443
F4 (%)W/W ----- 8 2 0.6 1.5 q.s.
F5 (%)W/W 2 ---- 2 0.6 1.5 q.s.
F6 (%)W/W 4 ---- 2 0.6 1.5 q.s.
F7 (%)W/W 6 ---- 2 0.6 1.5 q.s.
F8 (%)W/W 8 ---- 2 0.6 1.5 q.s.
Table 2:-The different adjusted process variables
Process variables Adjusted specifications
Pan design/Baffling 1 feet diameter with no baffles.
Rotational speed of the pan 40 rpm
Spray pressure (operational) 60-70 pound per square inch (p.s.i.)
Bed to Gun distance 1-1.5 feet
Bed temperature 40±50
c
Spray pattern type Circular
Heating Source IR-Lamp (150 watt, 250 volt)
Preliminary coating procedure[8]
:-
Two hundred tablets of Losartan Potassium were
loaded on a lab-scale pan coater previously cleaned,
dedusted. The coating liquid was filled into the spray
gun with pneumatic pump attachment. The pan was
rotated at 40 rpm for obtaining a cascading fall of
tablets. All the parameters were previously adjusted
with dummy tablets as shown below. As the tablets
rolled, the film forming liquid was sprayed
intermittently allowing the solvent to evaporate. The
process was continued until all the coating solution
was used up. The different specification of coating
procedure was shown in Table 2.
Formulation of losartan potassium tablets[9]
:-
Granules were prepared using the conventional wet
granulation technique. According to the ratio given in
the Table 3, appropriate amounts of excipients and
drug for each batch were weighed and added into a
mortar. The drug powder was properly mixed with
PVP, Talc for 20 min. Starch paste was prepared and
added to moisten the granules. The coherent mass
was passed through a 12 mesh screen sieve and dried
in an oven (Lab instruments and Chemical works,
Siliguri.) at 60 °C for 50 min. Dried granules were
forced through a 8/12 mesh, lubricated with
magnesium stearate and purified talc and then
compressed on a single punch tablet machine (Shakti
engineering, Siliguri). The tablets were round and flat
with an average diameter 0.603± 0.065 cms.
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Table 3: Formulation ratio of Losartan potassium
tablet.
Drug 10 gm
Drug : Diluent(Lactose) 1:3
Drug : Binder(Polyvinyl
Pyrollidone)
1:0.25
Drug : Disintegrant(Starch) 1:0.5
Drug : Glidant(Talc) 1:0.25
3. EVALUATION STUDY
Evaluation of Physical parameters [10], [11]
:-
Pre formulation testing is the first step in the rational
development of dosage forms of a drug substance. It
can be defined as an investigation of physical and
chemical properties of a drug substance combined
with excipients. The overall objective of pre-
formulation testing is to generate information useful
to the formulator in developing stable and bio
available dosage forms that can be developed to an
industrial scale. Before compression process, the
prepared granules were evaluated for flow properties
such as angle of repose and bulk density and tapped
density shown in Table 4. From the data obtained,
compressibility index, Hausner ratio was calculated
shown in Table 4. After compression of prepared
tablets, the prepared tablets are further evaluated for
the physical parameters like weight variation,
thickness, hardness, moisture content and friability.
The weights and thickness of twenty tablets of
losartan potassium were measured using digital
balance and a digital screw gauge, respectively given
in Table 7. The hardness of core tablets which is
given in Table 8 was measured by Monsanto
hardness tester (Testing Instrument, Kolkata, India)
and results were expressed in kg/cm2
. Friability is a
measure of mechanical strength of tablets. Rochie
friabilator (Testing Instrument, Kolkata, India) was
used to determine the friability which is given in
Table 7. Losartan potassium loaded coated tablet
were evaluated for percentage of moisture loss which
sharing an idea about its hydrophilic nature given in
Table 8. The average values, standard deviation, and
relative standard deviation were calculated.
Drug Content[11]
:-
Prepared coated and uncoated tablet of Losartan
Potassium from a batch was taken at random and was
crushed to a fine powder. The powdered material was
transferred into a 100 ml volumetric flask and 70 ml
of distilled water was added to it. It was shaken
occasionally for about 30 minutes and the volume
was made up to 100 ml by adding distilled water.
About 10 ml of the solution from the volumetric flask
was taken and centrifuged. The supernatant solution
from the centrifuge tube was collected and again
filtered by using Millipore filter. Then the filtrate was
subsequently diluted and the absorbance was
measured at 205.5 nm by UV spectrophotometer
(Shimadzu Spect-1700, Japan). This test was repeated
three times (N=3) for each batch of tablets. The
amounts of Losartan Potassium estimated from
different batches were given in Table 8.
Disintegration Test[12]
:-
Disintegration tester (Excel enterprise, Kolkata,
India) was used to determine the resistance or
breaking time of the selected aqueous film coated
tablets. Three tablets were randomly selected from
each batch and one tablet was placed in each of the
five tubes. The basket rack was positioned in a one-
liter beaker of water at 37±50
c. Perforated auxiliary
disc were placed on the bottom. The instrument was
operated and the time taken for a tablet to disintegrate
and all the particles to pass through the No. 10 USP
mesh apertures was noted according to USP/IP. The
average time is reported. All methods of this
experiment were performed in triplicate manner and
average value is taken. The disintegration time of
Losartan Potassium tablet estimated from different
batches were given in Table 7.
In-Vitro drug release studies[11]
:-
The release measurements were performed using 8
stage USP dissolution apparatus (VDR-8DR, Veego).
The dissolution rates of manufactured film coated
Losartan Potassium tablets with HPMC (F1, F2, F3,
F4) and with herbal polymer Moringa Oleifera (F5,
F6, F7, F8) and were studied using Veego dissolution
test apparatus (USP II) rotating paddle method under
sink conditions at 37±0.50
c and 50 rpm. The tablets
were placed in the basket and tested for drug release
for 5 hours in the water. The samples each of 5ml
were taken at appropriate time intervals, filtered and
assayed using UV-1700 Shimadzu spectrophotometer
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at 205.5nm wavelength respectively. The data for
percent drug release was fitted for zero order
equation. The percent of drug release was determined
as a function of time. All methods of this experiment
were performed in triplicate manner for each batch
and average value is taken.
To elucidate kinetics of drug release from the
prepared coated & uncoated losartan potassium
tablets, cumulative release and cumulative percentage
of drug remained was plotted as the function of time
(t) in the following equations[14]
.
Q = K0t Zero order
equation. Eq. (1)
Q = 100 (1- e-k1t
) First orders
equation. Eq. (2)
Q = KHt ½
Higuchi
equation. Eq. (3)
Log Mt/ M∞ = n Log t + log Kp Peppas &
Korsmeyer equation. Eq. (4)
Q for Eq. (1) and (3) is cumulative percent drug
release. While Q for Eq. (2) is cumulative percent
drug remaining. K is the rate constant, and Mt/ M∞ is
the fraction of drug released. Value of K and n were
calculated from the intercept and the slope of plot of
log Mt/ M∞ vs log t for Eq. (4). n-value from Eq. (4)
considered as release exponent indicating the
mechanism of drug release was chosen as a response
variable to help characterize the shape of dissolution
release curve and to determine the under lying release
mechanism governing release of drug from the
dosage form. The In-Vitro release data of different
batches to various kinetics models was given in Table
9.
Accelerated Stability Studies[11], [13]
:-
The formulation which showed good in vitro
performance was subjected to accelerated stability
studies which carried out by investigating the effect
of temperature on the physical properties of tablets
and drug release from compressed tablets containing
Losartan potassium. The formulations were stored in
room temperature at 25 ± 10
c, and in refrigeration
condition at 4 ±10
c for a period of 3 weeks. The
samples were analyzed for drug content every week
by spectrophotometer at 205.5 nm and compatibility
of drug with excipients was determined by IR
spectroscopy using shimadzu FTIR-840 model IR
spectrophotometer. Percent of potency data of the
formulation was given in Table 10.
4. RESULT AND DISCUSSION
Film coated Losartan potassium tablet was prepared
by the direct compression method with a coat
consisting of different proportion of the respective
synthetic polymer hydroxypropyl methyl cellulose
and the natural herbal polymer Moringa Oleifera
which is the main objective of my project work for its
gum, exudates and adhesive yielding properties.
Micromeritic study of pure drug powder to determine
the flow ability (angle of repose, bulk density, tapped
density etc) was done & given in the table 4.
Standard graph of losartan potassium drug powder
was also prepared and the correlation coefficient (r)
was found to be 0.999 respectively. The standard
graph of the pure drug is shown in Figure 2.
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Table 4:- Micromeritic analysis of Losartan potassium granules.
Granules Losartan Potassium granules
Colour White/ Off-white powder
Angle of Repose (θ) 27.389±0.6740
Tapped Density 0.692 ± 0.075
Bulk Density 0.593±0.053
Hausner Ratio 1.167
Car’s Index 0.130
% of Compressibility 13.00
Ph 5
Melting Point 275-2800
c
Solubility
Freely Soluble – Water & methanol. Soluble – 0.1 N HCL
Slightly Soluble – Chloroform, Toluene, Isopropyl alcohol.
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Uncoated losartan potassium tablets were coated with
different proportion of hydroxypropyl methyl
cellulose and the herbal polymer, Moringa Oleifera.
After coating, primarily visual observation was done
to show the normal defect during the preliminary
coating procedure like chipping, cracking etc. which
is shown in Table 5 and table 6. The photograph of
uncoated and coated tablet with different proportion
of synthetic polymer as well as extracted herbal
polymer was shown in Figure 7. The films formed
with 4% Hydroxypropyl methyl cellulose (F2) were
free from major defects like blistering, blooming,
cracking, chipping, orange peel, roughness, having
good gloss with very slight sticking than other
formulations and the films formed with 6% Moringa
oleifera (F7) were free from major defects with
having good gloss than other formulations.
Table 5:- Visual observation for defects in the formulations containing HPMC coat.
Defects F1 F2 F3 F4
Blistering ++ -- + +++
Blooming ++ -- + +++
Chipping + -- + +++
Cracking + -- + +++
Orange Peel + -- -- ++
Roughness ++ + + +++
Sticking ++ + ++ +++
Edge erosion + -- -- ++
Values expressed in mean± Standard Deviation (n=5). Yes- (+++), No- (--), Slight- (++), Very slight- (+)
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Table 6:- Visual observation for defects in the formulations containing Moringa Oleifera coat.
Defects F5 F6 F7 F8
Blistering ++ ++ -- +++
Blooming + + -- ++
Chipping ++ + -- +++
Cracking + -- -- ++
Orange Peel + + -- ++
Roughness ++ + + +++
Sticking ++ + + +++
Edge erosion + -- -- ++
Values expressed in mean± Standard Deviation (n=5). Yes- (+++), No- (--), Slight- (++), Very slight- (+)
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Primary evaluator parameters of Uncoated & coated
losartan potassium tablets like thickness & diameter,
weight gain, drug content etc were summarized in
Table 7 and Table 8. The thickness of the tablets
prepared with different ratio of HPMC and Moringa
Oleifera were found to be in between 3.3 to 3.9 cm. A
low standard deviation value in the coated tablets
thickness measurement confirms uniformity of films
prepared by the film coating procedure. The percent
of moisture content (% W/W) of the prepared coated
formulation with Synthetic polymers, HPMC were
found in between 0.54 to 0.58 (% W/W) and the
percent of moisture content with the herbal polymer,
Moringa Oleifera were found in between 0.65 to 0.68
(% W/W). It was observed that with increase in
hydrophilic polymer concentration the moisture
content was also increasing, for different
formulations containing the synthetic polymer,
HPMC and the herbal polymer, Moringa Oleifera.
The percent drug content of different formulations
prepared was found in between 90 to 91 %. Hardness
of the tablets was satisfactory and the weight loss in
friability test was significant in all the batches with
respect to the uncoated formulation. Overall the
prepared batches were of good quality with regard to
hardness, friability, weight uniformity and drug
content.
Table 7:- Primary evaluation parameters for uncoated and coated tablets of Losartan potassium tablets.
Formulation Thickness
(mm)
Diameter
(mm)
Weight
Gain
Friability
(%)
Disintegration
Time
Uncoated 3.3 ±0.02 6.0±0 Nil 0.42±0.01 14 min 18 sec ± 3
sec
F1 3.4±0.02 6.3±0.02 0.6±0.02 0.44±0.02 15 min 21 sec ± 7
sec
F2 3.44±0.01 6.3±0.02 0.7±0.01 0.35±00.01 15 min 57 sec ± 3
sec
F3 3.53±0.02 6.4±0.01 1.00±.02 0.39±0.02 16 min 42 sec ± 5
sec
F4 3.71±0.04 6.6±0.02 1.6±0.04 0.46±0.02 18 min 54 sec ± 5
sec
F5 3.5±0.02 6.4±0.02 2.1±0.02 0.5±0.03 15 min 38 sec ± 4
sec
F6 3.62±0.02 6.5±0.01 3.2±0.01 0.47±0.01 16 min 22 sec ± 4
sec
F7 3.67±0.02 6.4±0.02 3.5±0.01 0.43±0.01 17 min 50 sec ± 3
sec
F8 3.93±0.02 6.7±0.03 5.1±0.04 0.51±0.03 19 min 56 sec ± 6
sec
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Table 8:- Primary evaluation parameters for uncoated and coated tablets of Losartan potassium tablets.
Formulation Moisture Loss (%) Drug Content (%) Hardness (kg)
Uncoated 0.54±0 90±1 5.2±0.1
F1 0.57±0.01 90±1 5.2±0.1
F2 0.56±0.01 90±1 5.2±0.1
F3 0.56±0.02 90±0.98 5.2±0
F4 0.58±0.01 90±0.98 5.2±0.1
F5 0.65±0.02 90±1 5.2±0.2
F6 0.64±0.01 90±1 5.2±0.1
F7 0.68±0.01 90±1 5.2±0.01
F8 0.68±0.01 90±0.99 5.2±0
Values expressed in mean ± Standard Deviation (n=3)
From the above in-vitro release profile of all four
formulations of HPMC (F1, F2, F3, F4), it can be
seen that F2 shows 88.173% cumulative drug release
over the period of 5 hr and that formulation gives the
better result than other formulation. Similarly, from
all four formulations of Moringa oleifera coated
losartan potassium tablets, it can be shown that F7
showed 88.873% cumulative drug release over the
period of 5 hr and that formulation gives the better
release than other formulations. To describe the
kinetic of drug release from coated Losartan
potassium tablets, release data was analyzed
according to different kinetic equations described in
text. The zero order, first order, higuchi model and
peppas-korsmeyer equation represent diffusion
exponent, in all formulation it is in between 0.45 to
0.89, so it is normally said to follow non-fickian
anamolous release shown in the Table 9.
Comparative studies were also done in-between the
uncoated and coated losartan potassium tablets with
HPMC and Moringa Oleifera which was carried out
on the Figure 8 and Figure 9.
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Table 9:- In-vitro drug release Data to Various Release Models.
Zero Order model 1st
Order Model Higuchi model Peppas- korsmeyer model
Formulation R2
K0 R2
K1 Kh R2
R2
N
Uncoated 0.888 0.306 0.984 0.003 6.347 0.970 0.860 0.644
H
P
M
C
F1 0.849 0.297 0.959 0.003 6.360 0.956 0.892 0.612
F2 0.877 0.297 0.970 0.003 6.834 0.959 0.933 0.527
F3 0.732 0.246 0.867 0.002 5.308 0.861 0.892 0.615
F4 0.927 0.321 0.956 0.003 6.448 0.949 0.794 0.491
M
O
R
I
N
G
A
F5 0.770 0.221 0.923 0.002 4.739 0.894 0.886 0.585
F6 0.848 0.296 0.944 0.003 6.220 0.947 0.892 0.892
F7 0.864 0.304 0.955 0.003 6.337 0.953 0.934 0.535
F8 0.847 0.297 0.949 0.003 6.241 0.946 0.892 0.615
The accelerated stability studies were performed
according to ICH guidelines for a period of 3 weeks
and the results met the terms of the ICH guidelines
providing a safety profile of storage of Moringa
oleifera coated losartan potassium tablets in varying
temperature shown in Table 10 respectively.
Table 10: Accelerated stability studies of Moringa oleifera coated Losartan potassium tablets.
Percent of potency of the formulation
Weeks
Atmospheric Condition.
(Temperature)
F7
Initial 25 ± 10
c 99.78
3
25 ± 10
c 99.35
45 ± 10
c 98.55
4 ± 10
c 98.37
6
25 ± 10
c 99.22
45 ± 10
c 98.67
4 ± 10
c 98.13
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In conclusion, tablet coating films made of HPMC
and Moringa Oleifera with the addition of glycerin at
50% could be considered as an elegant film forming
formulation for solving different coating problems
generally faced in an industrial scale. The film
coating formulations were entirely prepared in an
aqueous environment avoiding the environmental
unfriendly toxic hazards accompanied with organic
solvents, These optimized formulations could be
further developed in an industrial scale for the
purpose of coating immediate release formulations
for those drugs whose integrity needs to be protected
from sunlight, oxidations, moisture, thermo liability,
and the foreign microbial attack.
5. CONCLUSION
The tablets were prepared in an environment free
from organic solvent. From the above result, it can
conclude that the gum has enormous potential for use
in the preparation of the polymeric films as the drug
delivery systems. In conclusion, tablet coating films
made of HPMC and Moringa Oleifera with the
addition of glycerin at 50% could be considered as an
elegant film forming formulation for solving different
coating problems generally faced in an industrial
scale. The film coating formulations were entirely
prepared in an aqueous environment avoiding the
environmental unfriendly toxic hazards accompanied
with organic solvents, These optimized formulations
could be further developed in an industrial scale for
the purpose of coating immediate release
formulations for those drugs whose integrity needs to
be protected from sunlight, oxidations, moisture,
thermo liability, and the foreign microbial attack.
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