International Journal of Pharmaceutical Science Invention (IJPSI) is an international journal intended for professionals and researchers in all fields of Pahrmaceutical Science. IJPSI publishes research articles and reviews within the whole field Pharmacy and Pharmaceutical Science, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
The document summarizes the design and statistical optimization of a pulsatile delivery system containing pantoprazole sodium. Key points include:
- The aim is to develop a pulsatile drug release tablet for pantoprazole sodium using MCC, CCS, and SSG to achieve a lag time of 5 hours followed by immediate drug release.
- A 32 factorial design is used to optimize the formulation. Preliminary studies evaluate formulations with varying levels of MCC, CCS, and SSG.
- Tablets are evaluated for pre-compression parameters, drug content, disintegration time, and dissolution profile in pH 6.8 buffer.
- The best formulation from preliminary studies will be selected for
Formulation and Evaluation of Pantoprazole Sodium Enteric Coated TabletsSriramNagarajan18
The document summarizes the formulation and evaluation of pantoprazole sodium enteric coated tablets. Pantoprazole is an acid-labile drug that requires enteric coating to protect it from degradation in the stomach. Various enteric coated tablet formulations were prepared using different concentrations of superdisintegrants and enteric coating polymers. Tablets were evaluated for hardness, thickness, weight variation, friability, drug content and in vitro drug release. Formulation EC8, coated with 6% Eudragit RS100, showed the best results with a thickness of 2.2mm, hardness of 3.52kg/cm2, drug release of 100.16% within 2 hours and 45 minutes, and acid resistance
Synthesis and Pharmacological evaluation of new Benzoxozole DerivativesSriramNagarajan15
Benzoxazoles1 are usually prepared by heating 2-Aminophenol with formic acids in the presence of Boric acid under reflux. Condensation of these two substances under milder conditions. Being a heterocyclic compound, benzoxazole finds use in research as a starting material for the synthesis of larger, usually bioactive structures. It is found within the chemical structures of pharmaceutical drugs such as flunoxaprofen. Benzoxazole derivatives are provided a protection against noxious UV radiation.Benzoxazole derivatives are also used in cosmotic compositions, such as for examples mainly cinnamic acid, 4-aminobenzoic acid.Benzoxazole derivatives are also used in the optical brighteners.These derivatives are used as Anticonvulsant and Neurotoxicity2 , Anti-inflammatory agents3, “Antibacterial activity”4, Cholesteryl ester transfer Protein inhibitors5, Antimicrobial activity6,7, Antifungal activity’8, Cyclooxygenase inhibitors9, hair treatment products and also used as a skin protectants.
Synthesis and Pharmacological evaluation of new Benzoxozole Derivativespharmaindexing
This document describes the synthesis and pharmacological evaluation of new benzoxazole derivatives. It first introduces benzoxazoles and their various pharmaceutical and cosmetic uses. It then details the synthesis of a benzoxazole derivative (Compound IV) in a multi-step reaction and provides its structural formula and properties. The document evaluates the acute oral toxicity and analgesic activity of Compound IV in mice based on OECD guidelines. It found that Compound IV had an oral LD50 greater than 2000 mg/kg and showed analgesic effects in the tail immersion test at doses of 50 and 100 mg/kg, suggesting it has potential as a new analgesic drug.
Development and Evaluation of Enteric Coated Herbal Drug Delivery System for ...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).
Biopharmaceutics and Pharmacokinetics Practical ManualReshma Fathima .K
The document describes an experiment to determine the partition coefficient and dissociation constant of ibuprofen. It provides background on how these properties influence drug absorption. The pH-partition hypothesis states that passive drug diffusion is governed by the drug's pKa, lipid solubility of the un-ionized form (partition coefficient), and gastrointestinal pH. The experiment involves measuring the extraction of ibuprofen into an organic phase at different buffer pH levels to calculate the apparent and true partition coefficients and dissociation constant. Plotting the results allows determining these pharmacokinetic parameters.
Kinetic Spectrophotometric Determination of Drugs Based On Oxidation by Alkal...IOSR Journals
Simple, accurate and precise spectrophotometic methods for quantitative determination of four drugs viz., Levofloxacin (LEV), Moxifloxacin (MOX), Pseudo Ephidrine (PSE), Torsemide (TOR) have been developed based on oxidation of the drugs by alk.KMnO4. Kinetics of the oxidation reaction is followed spectrophotometrically, as one of the reaction product, Mn(VI), absorbed at 610 nm. Initial rate and fixed time method are used for the construction of calibration curves Beer’s law is obeyed in the range 6.25-37.5 μg ml-1 for LEV; 5-30 μg ml-1 for MOX; 6.25-37.5 μg ml-1 for PSE and 2.5-15 μg ml-1 for TOR. Recovery studies using pure samples and pharmulations in the Beer’s Law limits have been carried out. Excellent recoveries indicate the methods are accurate and precise. The methods have been validated in terms of ICH guidelines. Statistical analysis in terms of student’s t- test and variance F- tests demonstrate high accuracy and precision and suggest the methods can be applied in bulk drug and pharmaceutical industries.
International Journal of Pharmaceutical Science Invention (IJPSI) is an international journal intended for professionals and researchers in all fields of Pahrmaceutical Science. IJPSI publishes research articles and reviews within the whole field Pharmacy and Pharmaceutical Science, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
The document summarizes the design and statistical optimization of a pulsatile delivery system containing pantoprazole sodium. Key points include:
- The aim is to develop a pulsatile drug release tablet for pantoprazole sodium using MCC, CCS, and SSG to achieve a lag time of 5 hours followed by immediate drug release.
- A 32 factorial design is used to optimize the formulation. Preliminary studies evaluate formulations with varying levels of MCC, CCS, and SSG.
- Tablets are evaluated for pre-compression parameters, drug content, disintegration time, and dissolution profile in pH 6.8 buffer.
- The best formulation from preliminary studies will be selected for
Formulation and Evaluation of Pantoprazole Sodium Enteric Coated TabletsSriramNagarajan18
The document summarizes the formulation and evaluation of pantoprazole sodium enteric coated tablets. Pantoprazole is an acid-labile drug that requires enteric coating to protect it from degradation in the stomach. Various enteric coated tablet formulations were prepared using different concentrations of superdisintegrants and enteric coating polymers. Tablets were evaluated for hardness, thickness, weight variation, friability, drug content and in vitro drug release. Formulation EC8, coated with 6% Eudragit RS100, showed the best results with a thickness of 2.2mm, hardness of 3.52kg/cm2, drug release of 100.16% within 2 hours and 45 minutes, and acid resistance
Synthesis and Pharmacological evaluation of new Benzoxozole DerivativesSriramNagarajan15
Benzoxazoles1 are usually prepared by heating 2-Aminophenol with formic acids in the presence of Boric acid under reflux. Condensation of these two substances under milder conditions. Being a heterocyclic compound, benzoxazole finds use in research as a starting material for the synthesis of larger, usually bioactive structures. It is found within the chemical structures of pharmaceutical drugs such as flunoxaprofen. Benzoxazole derivatives are provided a protection against noxious UV radiation.Benzoxazole derivatives are also used in cosmotic compositions, such as for examples mainly cinnamic acid, 4-aminobenzoic acid.Benzoxazole derivatives are also used in the optical brighteners.These derivatives are used as Anticonvulsant and Neurotoxicity2 , Anti-inflammatory agents3, “Antibacterial activity”4, Cholesteryl ester transfer Protein inhibitors5, Antimicrobial activity6,7, Antifungal activity’8, Cyclooxygenase inhibitors9, hair treatment products and also used as a skin protectants.
Synthesis and Pharmacological evaluation of new Benzoxozole Derivativespharmaindexing
This document describes the synthesis and pharmacological evaluation of new benzoxazole derivatives. It first introduces benzoxazoles and their various pharmaceutical and cosmetic uses. It then details the synthesis of a benzoxazole derivative (Compound IV) in a multi-step reaction and provides its structural formula and properties. The document evaluates the acute oral toxicity and analgesic activity of Compound IV in mice based on OECD guidelines. It found that Compound IV had an oral LD50 greater than 2000 mg/kg and showed analgesic effects in the tail immersion test at doses of 50 and 100 mg/kg, suggesting it has potential as a new analgesic drug.
Development and Evaluation of Enteric Coated Herbal Drug Delivery System for ...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).
Biopharmaceutics and Pharmacokinetics Practical ManualReshma Fathima .K
The document describes an experiment to determine the partition coefficient and dissociation constant of ibuprofen. It provides background on how these properties influence drug absorption. The pH-partition hypothesis states that passive drug diffusion is governed by the drug's pKa, lipid solubility of the un-ionized form (partition coefficient), and gastrointestinal pH. The experiment involves measuring the extraction of ibuprofen into an organic phase at different buffer pH levels to calculate the apparent and true partition coefficients and dissociation constant. Plotting the results allows determining these pharmacokinetic parameters.
Kinetic Spectrophotometric Determination of Drugs Based On Oxidation by Alkal...IOSR Journals
Simple, accurate and precise spectrophotometic methods for quantitative determination of four drugs viz., Levofloxacin (LEV), Moxifloxacin (MOX), Pseudo Ephidrine (PSE), Torsemide (TOR) have been developed based on oxidation of the drugs by alk.KMnO4. Kinetics of the oxidation reaction is followed spectrophotometrically, as one of the reaction product, Mn(VI), absorbed at 610 nm. Initial rate and fixed time method are used for the construction of calibration curves Beer’s law is obeyed in the range 6.25-37.5 μg ml-1 for LEV; 5-30 μg ml-1 for MOX; 6.25-37.5 μg ml-1 for PSE and 2.5-15 μg ml-1 for TOR. Recovery studies using pure samples and pharmulations in the Beer’s Law limits have been carried out. Excellent recoveries indicate the methods are accurate and precise. The methods have been validated in terms of ICH guidelines. Statistical analysis in terms of student’s t- test and variance F- tests demonstrate high accuracy and precision and suggest the methods can be applied in bulk drug and pharmaceutical industries.
International Journal of Pharmaceutical Science Invention (IJPSI) is an international journal intended for professionals and researchers in all fields of Pahrmaceutical Science. IJPSI publishes research articles and reviews within the whole field Pharmacy and Pharmaceutical Science, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
Fabrication and evaluation of a stable flurbiprofen hydrogelpharmaindexing
This study aimed to fabricate and evaluate a stable 6% flurbiprofen hydrogel for topical delivery. Flurbiprofen hydrogel was prepared using carbopol 940 as the thickening agent. Stability studies were conducted over 28 days at different temperatures (2-40°C, 25°C, 40°C) by assessing parameters like liquefaction, color, phase separation, centrifugation and pH. The hydrogel showed no changes in these parameters, and pH values remained stable. Drug content of the hydrogel was 76.3% flurbiprofen. In vitro drug release studies found 79.46% of drug was released after 8 hours, indicating the formulation was stable for topical use.
The effect of conjugation on different polymers in bioadhesive films of losartanSriramNagarajan18
The document summarizes a study that investigated the effect of conjugating different polymers on the properties of buccal films containing the drug losartan potassium. Sodium alginate and chitosan were conjugated with cysteine and thioglycolic acid respectively, and films containing plain or conjugated polymers were prepared and evaluated. The conjugation was confirmed using FTIR and the polymers were found to contain thiol groups. Films were evaluated for properties like thickness, drug content, swelling, bioadhesion and drug permeation. Formulations containing conjugated polymers showed higher bioadhesion, swelling and longer drug permeation compared to films with plain polymers. The optimized formulations were found to be stable.
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
Pharmaceutics is the science of dosage form design and drug delivery. It draws from many disciplines to understand how drugs interact inside and outside the body. The goal is to design safe and effective dosage forms for drugs' intended uses. Dosage form design considers the drug's physicochemical properties, biopharmaceutical factors like absorption site, and logistical factors like storage stability. It is important to deliver drugs via dosage forms that provide accurate dosing, protect unstable drugs, and facilitate optimal drug action based on route of administration. Proper dosage form design allows drugs to be delivered safely and effectively.
The document discusses the Biopharmaceutical Classification System (BCS), which classifies drug substances based on their aqueous solubility and intestinal permeability. The BCS has four classes based on whether a drug is highly soluble/permeable or low soluble/permeable. It provides a framework to determine if in vitro dissolution tests can replace bioequivalence studies for certain drugs. The BCS considers factors like dose/solubility ratios, dissolution rates, and permeability to classify drugs and determine regulatory applications like biowaivers for bioequivalence studies.
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 fast-disintegrating tablets of FlupirtineijperSS
ABSTRACT
Recent developments in fast-dissolving or disintegrating tablets have brought convenience in dosing to elderly and children who have trouble in swallowing tablets. The main objective of the present study was to prepare the orally disintegrating tablets of Flupirtine, a non-steroidal anti-inflammatory drug (NSAID) using different superdisintegrants by direct compression method. Different concentrations (4%, 8%, and 10%) of super disintegrants such as Primogel, Kollidon Cl, Lycoat were used in the formulation. Mannitol was used as a bulking agent and to enhance the mouth feel and taste. The formulated tablets were evaluated for pre-formulation and post-formulation parameters and they were found to be satisfactory and within the official limits. All the tablets shown hardness 3-4.5kg/cm2, friability of all the formulations was less than 1%, weight variation and drug content were found to be within official limits. Amongst all formulations, the optimized formulation F9 was prepared with Lycoat as a super disintegrant showed least disintegration time and faster dissolution.
Key words: Flupirtine, fast-disintegrating tablet, direct compression method, superdisintegrants.
This document provides an overview of parenteral dosage forms, including definitions, advantages and disadvantages, preformulation considerations, and types of small and large volume parenterals. Parenterals refer to routes of administration other than the gastrointestinal tract, such as intravenous, intramuscular, and subcutaneous. Preformulation studies examine the drug's physicochemical properties, solubility, stability, and compatibility with excipients. Small volume parenterals are formulated with water for injection, buffers, antimicrobial preservatives, antioxidants, tonicity agents, and surfactants. Large volume parenterals provide intravenous nutrition through protein, energy, electrolyte, and vitamin substrates. Finished products are tested for content uniformity, leakage,
Studies on development of famotidine floating tablets using three grades of M...SriramNagarajan17
This document summarizes a study on the development of floating tablets of the drug famotidine using three grades of hydroxypropyl methylcellulose (HPMC; K4M, K15M, K100M) as release-retarding polymers. Tablets were prepared using different drug-polymer ratios via wet granulation. The formulations were characterized for drug-polymer compatibility, floating behavior, swelling properties, in vitro drug release, and stability. Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction studies indicated no drug-polymer interactions. In vitro tests showed that the type and concentration of polymer affected drug release rate and floating properties. The optimized formulation containing famotidine and HPMC K
This document presents the development of nizatidine mucoadhesive microballoons for the treatment of peptic ulcers. Peptic ulcers occur in the stomach and duodenum due to an imbalance between aggressive and defensive factors. Nizatidine is an H2 receptor antagonist used to treat peptic ulcers. The objective is to develop microballoons to increase gastric residence time and bioavailability of nizatidine. Preformulation studies including solubility, compatibility and analytical method development were conducted. Microballoons will be formulated using different polymer combinations and evaluated for properties like mucoadhesion, drug release and stability. The formulation aims to localize nizatidine delivery and maintain therapeutic drug
Application of biopharmaceutics classification system in formulation developm...Surang Judistprasert
The document discusses the application of the Biopharmaceutics Classification System (BCS) in formulation development. It describes the four BCS classes based on a drug's solubility and permeability properties and how these properties impact bioequivalence studies and regulatory requirements. It also discusses factors that influence the predictability of in vivo performance based on the BCS class, such as first-pass metabolism and excipient effects. Recommendations are provided for designing successful bioequivalence studies using BCS principles.
Biopharmaceutical classification system & drug delivery system associated wit...PratikShinde120
Biopharmaceutical classification system & drug delivery system based on BCS.
By Pratik shinde, Mpharm, University department of pharmaceutical sciences, Nagpur
Design, synthesis, characterization and biological evaluation of 3- (4-(7-chl...iosrjce
Novel thiazolidinone derivatives TQ-VI(1-10) were designed, synthesized and screened for
antimicrobial activity. Synthesis of 3-(4-(7-chloro-2-(4-chlorophenyl) 4-oxo-quinazolin-3(4H)-yl) phenyl) -
2-arylthiazolidin-4-one TQ-VI(1-10) have been achieved from the starting material 2-amino-4-chlorobenzoic
acid TQ-I on cyclization with p-chlorobenzoyl chloride TQ-II to yield 7-chloro-2-(4-chlorophenyl)-4H-3,1-
benzoxazin-4-one,TQ-III, which on treatment with p-phenylindiamine gave 3-(4-aminophenyl)-7-chloro-2-(4-
chlorophenyl)quinazolin-4(3H)-one, TQ-IV in good yield. Then, TQ-IV on reaction with substituted aromatic
aldehydes converted to TQ-V(1-10), which on cyclization with thioglycolic acid gave TQ-VI (1-10). All the
synthesized compounds have been characterized on the basis of IR,
1
H-NMR and mass spectral data. The
compounds containing 4-OH, 4-OCH3 and 3,4,5-(OCH3)3 showed good activity. The title compounds were
screened for qualitative (zone of inhibition) and quantitative antimicrobial activity (MIC) by agar cup plate
method and serial dilution technique, respectively. Among the synthesized compounds in the series, the
compound TQVI4 and TQVI5 were found to exhibit significant antifungal activity at lower concentration of
31.25 µg/ml, against A.niger. The compound TQVI5 and TQVI4 showed zone of inhibition of 17mm and 15mm
against A.niger and C.albicans respectively which is comparable to that of standard drug. The rest of the
analogues in the series displayed weak to moderate antimicrobial activity when compared to the standard
positive controls Ampicillin and Amphotericin B.
The document provides an introduction to dosage form design. It discusses key principles such as how drugs are formulated using excipients to create various dosage forms like solutions, suspensions, and tablets. It also covers important considerations for dosage form design like routes of administration, drug properties, factors that influence absorption, and therapeutic factors. The goals of dosage design are to deliver drugs in a suitable form for the administration route and provide desired release properties and stability.
The document discusses parenteral drug delivery. It defines parenteral products and other related terms. Parenteral preparations are those administered outside the digestive tract, usually via injections. They are preferred when rapid drug action is needed, the oral route cannot be used, or the drug would be inactivated in the gastrointestinal tract. The major routes of parenteral administration include subcutaneous, intramuscular, intravenous, and others. Proper formulation, sterilization, and packaging are required to ensure the safety of parenteral products.
The World Health Organization (WHO) provides guidelines for herbal drugs and formulations. Herbal drugs include crude plant materials, finished products containing plant parts, and herbal formulations made by extracting or processing plants. Standardization of herbal drugs involves identification, quality control, and determining purity using morphological, microscopic, physical, chemical and biological methods. Key steps include macroscopic and microscopic examination of plant materials, measurement of ash values, extractive values, water content, volatile oils, bitterness, and other chemical analyses.
This document describes the design of a bilayer tablet containing atorvastatin and aspirin for the treatment of cardiovascular diseases. The bilayer tablet contains an immediate release layer of atorvastatin and an enteric-coated pulsatile release layer of aspirin. Four formulations of each layer were developed with different concentrations of excipients. The pulsatile aspirin layers were coated with Eudragit S100 to protect the drug from the acidic environment of the stomach. Evaluation of the bilayer tablets showed acceptable physicochemical properties and drug release profiles. Formulation F3 was found to be the best with one layer providing immediate release of atorvastatin to lower cholesterol and the other layer delivering aspirin at the
BCS classification system : Applications in pharmaceutics Hemant Khandoliya
The document provides an overview of the Biopharmaceutics Classification System (BCS). The BCS is a scientific framework that classifies drug substances based on their aqueous solubility and intestinal permeability. It includes four key classes based on whether a drug is highly soluble/permeable, low soluble/high permeable, etc. The BCS aims to predict a drug's absorption and bioavailability based on these characteristics, and provides guidance to drug regulators on biowaiver requests for in vivo bioequivalence studies.
This document describes an inter-laboratory evaluation study conducted to validate the use of the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay as a standard method for evaluating the antioxidant capacity of food additives. Fourteen laboratories participated in the study. Five analytical samples - four existing food additives (tea extract, grape seed extract, enju extract, and d-α-tocopherol) and Trolox - were evaluated using the DPPH assay. The results showed good repeatability for measuring antioxidant capacity within laboratories, but greater variability between laboratories. However, expressing the results as Trolox equivalent antioxidant capacity reduced inter-laboratory variability, suggesting the DPPH assay could be
The document describes the synthesis and characterization of 20 new 1,3,5-trisubstituted pyrazole derivatives and their evaluation for antifungal activity. The derivatives were synthesized by reacting chalcone derivatives with succinic hydrazide in pyridine. The derivatives were characterized using IR, 1H NMR, and mass spectroscopy. The compounds were evaluated for antifungal activity against four fungal strains at two concentrations using an agar diffusion method. Several of the compounds showed mild to good antifungal activity, with the BR series (BR-1 to BR-4) being the most active. The presence of electronegative groups like Br and Cl at the third and fifth positions of the py
Synthesis, Characterization, and Antifungal Evaluation of Some New 1,3,5-Tris...BRNSS Publication Hub
Objective: The objective of the paper was to design, synthesis, and characterization of new 1,3,5-trisubstituted-2-pyrazolines derivative and evaluate for antifungal activity. Materials and Methods: The 1,3,5-tri-substituted-2-pyrazolines derivatives have been synthesized by the reaction of chalcone derivatives with succinic hydrazide in the environment of pyridine. Total 20 compounds have been synthesized and characterized by the IR, 1H NMR, and mass spectral analysis. Antifungal activity of the compounds carried out on four fungal strains, that is, Saccharomyces cerevisiae, Aspergillus niger, Candida albicans, and Rhizopus oryzae in two different concentrations, that is, 50 and 100 μg/ml by agar-diffusion method using cup-plate method and Ketoconazole was used as standard antifungal drug. Results and Discussion: In accordance with the data from antifungal activity, all the synthesized 1,3,5-trisubstituted pyrazole derivatives (ME1-ME8, CL1-CL8, and BR1-BR4) have shown mild to best activity against tested organisms. The data of antifungal activity against the fungal strains (S. cerevisiae, A. niger, C. albicans, and R. oryzae) suggested the order of activity of compounds: BR-3 > BR-2 > BR-1 > CL-4 > BR-4 > CL-3 > CL-2 > ME-3> ME-2 > CL-5 > CL-6 > ME-4 > ME-5 > ME-6 > ME-7 > CL-7 > CL-8 > ME-8 > CL-1 > ME-1. The presence of electronegative group (Br, Cl, F, and NO2) either at third and fifth position of 1,3,5-pyrazoline ring is required for the potent antifungal activity. The presence of electronegative group (Br, Cl) at third and fifth position may necessary for the best activity against bacterial and fungal strains but the addition of F, NO2 has shown the moderate activity but in case of -CH3 and -OCH3 substitution may diminish the activity. The series BR-1 to BR-4 is most active compound of the synthesized compounds. Conclusion: The 1,3,5-trisubstituted pyrazole derivatives has been successfully synthesized and antifungal activity of the compounds denotes that the series BR-1 to BR-4 is most active compound of the all twenty synthesized compounds. The addition of electronegative group (Br, Cl) at third and fifth position in pyrazole ring may necessary for the activity against fungal strains.
Fabrication and evaluation of a stable flurbiprofen hydrogelpharmaindexing
This study aimed to fabricate and evaluate a stable 6% flurbiprofen hydrogel for topical delivery. Flurbiprofen hydrogel was prepared using carbopol 940 as the thickening agent. Stability studies were conducted over 28 days at different temperatures (2-40°C, 25°C, 40°C) by assessing parameters like liquefaction, color, phase separation, centrifugation and pH. The hydrogel showed no changes in these parameters, and pH values remained stable. Drug content of the hydrogel was 76.3% flurbiprofen. In vitro drug release studies found 79.46% of drug was released after 8 hours, indicating the formulation was stable for topical use.
The effect of conjugation on different polymers in bioadhesive films of losartanSriramNagarajan18
The document summarizes a study that investigated the effect of conjugating different polymers on the properties of buccal films containing the drug losartan potassium. Sodium alginate and chitosan were conjugated with cysteine and thioglycolic acid respectively, and films containing plain or conjugated polymers were prepared and evaluated. The conjugation was confirmed using FTIR and the polymers were found to contain thiol groups. Films were evaluated for properties like thickness, drug content, swelling, bioadhesion and drug permeation. Formulations containing conjugated polymers showed higher bioadhesion, swelling and longer drug permeation compared to films with plain polymers. The optimized formulations were found to be stable.
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
Pharmaceutics is the science of dosage form design and drug delivery. It draws from many disciplines to understand how drugs interact inside and outside the body. The goal is to design safe and effective dosage forms for drugs' intended uses. Dosage form design considers the drug's physicochemical properties, biopharmaceutical factors like absorption site, and logistical factors like storage stability. It is important to deliver drugs via dosage forms that provide accurate dosing, protect unstable drugs, and facilitate optimal drug action based on route of administration. Proper dosage form design allows drugs to be delivered safely and effectively.
The document discusses the Biopharmaceutical Classification System (BCS), which classifies drug substances based on their aqueous solubility and intestinal permeability. The BCS has four classes based on whether a drug is highly soluble/permeable or low soluble/permeable. It provides a framework to determine if in vitro dissolution tests can replace bioequivalence studies for certain drugs. The BCS considers factors like dose/solubility ratios, dissolution rates, and permeability to classify drugs and determine regulatory applications like biowaivers for bioequivalence studies.
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 fast-disintegrating tablets of FlupirtineijperSS
ABSTRACT
Recent developments in fast-dissolving or disintegrating tablets have brought convenience in dosing to elderly and children who have trouble in swallowing tablets. The main objective of the present study was to prepare the orally disintegrating tablets of Flupirtine, a non-steroidal anti-inflammatory drug (NSAID) using different superdisintegrants by direct compression method. Different concentrations (4%, 8%, and 10%) of super disintegrants such as Primogel, Kollidon Cl, Lycoat were used in the formulation. Mannitol was used as a bulking agent and to enhance the mouth feel and taste. The formulated tablets were evaluated for pre-formulation and post-formulation parameters and they were found to be satisfactory and within the official limits. All the tablets shown hardness 3-4.5kg/cm2, friability of all the formulations was less than 1%, weight variation and drug content were found to be within official limits. Amongst all formulations, the optimized formulation F9 was prepared with Lycoat as a super disintegrant showed least disintegration time and faster dissolution.
Key words: Flupirtine, fast-disintegrating tablet, direct compression method, superdisintegrants.
This document provides an overview of parenteral dosage forms, including definitions, advantages and disadvantages, preformulation considerations, and types of small and large volume parenterals. Parenterals refer to routes of administration other than the gastrointestinal tract, such as intravenous, intramuscular, and subcutaneous. Preformulation studies examine the drug's physicochemical properties, solubility, stability, and compatibility with excipients. Small volume parenterals are formulated with water for injection, buffers, antimicrobial preservatives, antioxidants, tonicity agents, and surfactants. Large volume parenterals provide intravenous nutrition through protein, energy, electrolyte, and vitamin substrates. Finished products are tested for content uniformity, leakage,
Studies on development of famotidine floating tablets using three grades of M...SriramNagarajan17
This document summarizes a study on the development of floating tablets of the drug famotidine using three grades of hydroxypropyl methylcellulose (HPMC; K4M, K15M, K100M) as release-retarding polymers. Tablets were prepared using different drug-polymer ratios via wet granulation. The formulations were characterized for drug-polymer compatibility, floating behavior, swelling properties, in vitro drug release, and stability. Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction studies indicated no drug-polymer interactions. In vitro tests showed that the type and concentration of polymer affected drug release rate and floating properties. The optimized formulation containing famotidine and HPMC K
This document presents the development of nizatidine mucoadhesive microballoons for the treatment of peptic ulcers. Peptic ulcers occur in the stomach and duodenum due to an imbalance between aggressive and defensive factors. Nizatidine is an H2 receptor antagonist used to treat peptic ulcers. The objective is to develop microballoons to increase gastric residence time and bioavailability of nizatidine. Preformulation studies including solubility, compatibility and analytical method development were conducted. Microballoons will be formulated using different polymer combinations and evaluated for properties like mucoadhesion, drug release and stability. The formulation aims to localize nizatidine delivery and maintain therapeutic drug
Application of biopharmaceutics classification system in formulation developm...Surang Judistprasert
The document discusses the application of the Biopharmaceutics Classification System (BCS) in formulation development. It describes the four BCS classes based on a drug's solubility and permeability properties and how these properties impact bioequivalence studies and regulatory requirements. It also discusses factors that influence the predictability of in vivo performance based on the BCS class, such as first-pass metabolism and excipient effects. Recommendations are provided for designing successful bioequivalence studies using BCS principles.
Biopharmaceutical classification system & drug delivery system associated wit...PratikShinde120
Biopharmaceutical classification system & drug delivery system based on BCS.
By Pratik shinde, Mpharm, University department of pharmaceutical sciences, Nagpur
Design, synthesis, characterization and biological evaluation of 3- (4-(7-chl...iosrjce
Novel thiazolidinone derivatives TQ-VI(1-10) were designed, synthesized and screened for
antimicrobial activity. Synthesis of 3-(4-(7-chloro-2-(4-chlorophenyl) 4-oxo-quinazolin-3(4H)-yl) phenyl) -
2-arylthiazolidin-4-one TQ-VI(1-10) have been achieved from the starting material 2-amino-4-chlorobenzoic
acid TQ-I on cyclization with p-chlorobenzoyl chloride TQ-II to yield 7-chloro-2-(4-chlorophenyl)-4H-3,1-
benzoxazin-4-one,TQ-III, which on treatment with p-phenylindiamine gave 3-(4-aminophenyl)-7-chloro-2-(4-
chlorophenyl)quinazolin-4(3H)-one, TQ-IV in good yield. Then, TQ-IV on reaction with substituted aromatic
aldehydes converted to TQ-V(1-10), which on cyclization with thioglycolic acid gave TQ-VI (1-10). All the
synthesized compounds have been characterized on the basis of IR,
1
H-NMR and mass spectral data. The
compounds containing 4-OH, 4-OCH3 and 3,4,5-(OCH3)3 showed good activity. The title compounds were
screened for qualitative (zone of inhibition) and quantitative antimicrobial activity (MIC) by agar cup plate
method and serial dilution technique, respectively. Among the synthesized compounds in the series, the
compound TQVI4 and TQVI5 were found to exhibit significant antifungal activity at lower concentration of
31.25 µg/ml, against A.niger. The compound TQVI5 and TQVI4 showed zone of inhibition of 17mm and 15mm
against A.niger and C.albicans respectively which is comparable to that of standard drug. The rest of the
analogues in the series displayed weak to moderate antimicrobial activity when compared to the standard
positive controls Ampicillin and Amphotericin B.
The document provides an introduction to dosage form design. It discusses key principles such as how drugs are formulated using excipients to create various dosage forms like solutions, suspensions, and tablets. It also covers important considerations for dosage form design like routes of administration, drug properties, factors that influence absorption, and therapeutic factors. The goals of dosage design are to deliver drugs in a suitable form for the administration route and provide desired release properties and stability.
The document discusses parenteral drug delivery. It defines parenteral products and other related terms. Parenteral preparations are those administered outside the digestive tract, usually via injections. They are preferred when rapid drug action is needed, the oral route cannot be used, or the drug would be inactivated in the gastrointestinal tract. The major routes of parenteral administration include subcutaneous, intramuscular, intravenous, and others. Proper formulation, sterilization, and packaging are required to ensure the safety of parenteral products.
The World Health Organization (WHO) provides guidelines for herbal drugs and formulations. Herbal drugs include crude plant materials, finished products containing plant parts, and herbal formulations made by extracting or processing plants. Standardization of herbal drugs involves identification, quality control, and determining purity using morphological, microscopic, physical, chemical and biological methods. Key steps include macroscopic and microscopic examination of plant materials, measurement of ash values, extractive values, water content, volatile oils, bitterness, and other chemical analyses.
This document describes the design of a bilayer tablet containing atorvastatin and aspirin for the treatment of cardiovascular diseases. The bilayer tablet contains an immediate release layer of atorvastatin and an enteric-coated pulsatile release layer of aspirin. Four formulations of each layer were developed with different concentrations of excipients. The pulsatile aspirin layers were coated with Eudragit S100 to protect the drug from the acidic environment of the stomach. Evaluation of the bilayer tablets showed acceptable physicochemical properties and drug release profiles. Formulation F3 was found to be the best with one layer providing immediate release of atorvastatin to lower cholesterol and the other layer delivering aspirin at the
BCS classification system : Applications in pharmaceutics Hemant Khandoliya
The document provides an overview of the Biopharmaceutics Classification System (BCS). The BCS is a scientific framework that classifies drug substances based on their aqueous solubility and intestinal permeability. It includes four key classes based on whether a drug is highly soluble/permeable, low soluble/high permeable, etc. The BCS aims to predict a drug's absorption and bioavailability based on these characteristics, and provides guidance to drug regulators on biowaiver requests for in vivo bioequivalence studies.
This document describes an inter-laboratory evaluation study conducted to validate the use of the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay as a standard method for evaluating the antioxidant capacity of food additives. Fourteen laboratories participated in the study. Five analytical samples - four existing food additives (tea extract, grape seed extract, enju extract, and d-α-tocopherol) and Trolox - were evaluated using the DPPH assay. The results showed good repeatability for measuring antioxidant capacity within laboratories, but greater variability between laboratories. However, expressing the results as Trolox equivalent antioxidant capacity reduced inter-laboratory variability, suggesting the DPPH assay could be
The document describes the synthesis and characterization of 20 new 1,3,5-trisubstituted pyrazole derivatives and their evaluation for antifungal activity. The derivatives were synthesized by reacting chalcone derivatives with succinic hydrazide in pyridine. The derivatives were characterized using IR, 1H NMR, and mass spectroscopy. The compounds were evaluated for antifungal activity against four fungal strains at two concentrations using an agar diffusion method. Several of the compounds showed mild to good antifungal activity, with the BR series (BR-1 to BR-4) being the most active. The presence of electronegative groups like Br and Cl at the third and fifth positions of the py
Synthesis, Characterization, and Antifungal Evaluation of Some New 1,3,5-Tris...BRNSS Publication Hub
Objective: The objective of the paper was to design, synthesis, and characterization of new 1,3,5-trisubstituted-2-pyrazolines derivative and evaluate for antifungal activity. Materials and Methods: The 1,3,5-tri-substituted-2-pyrazolines derivatives have been synthesized by the reaction of chalcone derivatives with succinic hydrazide in the environment of pyridine. Total 20 compounds have been synthesized and characterized by the IR, 1H NMR, and mass spectral analysis. Antifungal activity of the compounds carried out on four fungal strains, that is, Saccharomyces cerevisiae, Aspergillus niger, Candida albicans, and Rhizopus oryzae in two different concentrations, that is, 50 and 100 μg/ml by agar-diffusion method using cup-plate method and Ketoconazole was used as standard antifungal drug. Results and Discussion: In accordance with the data from antifungal activity, all the synthesized 1,3,5-trisubstituted pyrazole derivatives (ME1-ME8, CL1-CL8, and BR1-BR4) have shown mild to best activity against tested organisms. The data of antifungal activity against the fungal strains (S. cerevisiae, A. niger, C. albicans, and R. oryzae) suggested the order of activity of compounds: BR-3 > BR-2 > BR-1 > CL-4 > BR-4 > CL-3 > CL-2 > ME-3> ME-2 > CL-5 > CL-6 > ME-4 > ME-5 > ME-6 > ME-7 > CL-7 > CL-8 > ME-8 > CL-1 > ME-1. The presence of electronegative group (Br, Cl, F, and NO2) either at third and fifth position of 1,3,5-pyrazoline ring is required for the potent antifungal activity. The presence of electronegative group (Br, Cl) at third and fifth position may necessary for the best activity against bacterial and fungal strains but the addition of F, NO2 has shown the moderate activity but in case of -CH3 and -OCH3 substitution may diminish the activity. The series BR-1 to BR-4 is most active compound of the synthesized compounds. Conclusion: The 1,3,5-trisubstituted pyrazole derivatives has been successfully synthesized and antifungal activity of the compounds denotes that the series BR-1 to BR-4 is most active compound of the all twenty synthesized compounds. The addition of electronegative group (Br, Cl) at third and fifth position in pyrazole ring may necessary for the activity against fungal strains.
This research article describes the development and evaluation of a polyherbal solid dosage formulation with antioxidant properties. Researchers developed a chewable tablet formulation containing extracts of Amla, Withania, and Tulsi, which are plants known to have antioxidant activity. The formulation was evaluated for its antioxidant effects using nitric oxide scavenging, DPPH free radical scavenging, and hydroxyl radical scavenging assays and showed significant antioxidant activity in vitro. The results indicate that the polyherbal chewable tablet exhibited pronounced antioxidant effects based on inhibition levels in the various assays compared to the standard vitamin E.
Topical Delivery of Fenoprofen Proliposomes: Preparation, Evaluation and In V...inventionjournals
International Journal of Pharmaceutical Science Invention (IJPSI) is an international journal intended for professionals and researchers in all fields of Pahrmaceutical Science. IJPSI publishes research articles and reviews within the whole field Pharmacy and Pharmaceutical Science, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
Membrane Stabilizing And Antimicrobial Activities Of Caladium Bicolor And Che...IOSR Journals
The crude methanol extracts of whole plant of Caladium bicolor (Aiton) Vent. and leaf of Chenopodium album L. as well as their pet-ether, carbon tetrachloride, chloroform and aqueous soluble fractions were evaluated for membrane stabilizing and antimicrobial activities. At concentration 1.0 mg/ml, the carbon tetrachloride soluble fraction of C. bicolor inhibited 43.92±1.63% and 38.08±0.83 % hypotonic solution and heat induced haemolysis of RBCs, respectively. Among the extractives of C. album, the aqueous soluble fraction inhibited 47.11±0.49 % and 36.73±0.76 % hypotonic solution and heat induced haemolysis of RBCs as compared to 72.79 % and 42.12 % by acetyl salicylic acid (0.10 mg/ml), respectively. C. bicolor test samples demonstrated zone of inhibition ranging from 6.0 to 20.0 mm. The chloroform soluble fraction showed the highest zone of inhibition (20.0 mm) against Staphylococcus aureus. The test samples of C. album displayed zone of inhibition ranging from 7.0 to 13.0 mm. The highest zone of inhibition (13.0 mm) was showed by the chloroform soluble fraction against Salmonella paratyphi
Formulation and Evaluation of Sublingual Tablets of Asenapine Maleate By 32 F...PRASANTAKUMARMOHAPAT3
Objectives: The aim of this work was to formulate and evaluate sublingual tablets of Asenapine
maleate for the treatment of schizophrenia and the treatment of manic episodes associated with
bipolar I disorder. Methods: In the present work, the bitter taste of Asenapine maleate was
masked by using Kyron T-114 in 1:1.5 ratio. The Drug-Resin Complex was formulated as
sublingual tablets using Cross Povidone (X1) and Avicel PH102 (X2) by direct compression
method. The sublingual tablets were evaluated such as thickness, hardness, % Friability,
Wetting time, disintegration time, Water absorption ratio and % CDR.Results: In this study, the
fast release of tablets depends on the concentration of Cross Povidone (X1) and Avicel PH102
(X2). The selected formulation showed the fastest release of the tablets in 54 s. Stability study
was performed by taking an optimized formulation and it was observed stable. The sublingual
tablets showed acceptable results in all studies.Conclusion: The results indicate that the
formulation can be used for the treatment of schizophrenia and the treatment of manic episodes
associated with bipolar I disorder. Moreover, Asenapine maleate as sublingual tablets may
overcome the first pass effect, gives better bioavailability, rapid onset of action and patient
compliance.
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.
Ameliorating Effect of Frankincense on Red Blood Cells of Alloxan Induced-Dia...inventionjournals
International Journal of Pharmaceutical Science Invention (IJPSI) is an international journal intended for professionals and researchers in all fields of Pahrmaceutical Science. IJPSI publishes research articles and reviews within the whole field Pharmacy and Pharmaceutical Science, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
This study investigated the phytochemical composition, antimicrobial, and alpha-glucosidase inhibition properties of Rubus ellipticus leaf extracts. Methanol extracts showed the highest levels of total phenols and flavonoids. In antimicrobial testing, the methanol extract demonstrated significant inhibitory effects against both gram-positive and gram-negative bacteria as well as fungi. The minimum inhibitory concentration values ranged from 15-62.5 μg/ml depending on the microorganism. In alpha-glucosidase inhibition assays, the methanol extract and positive control both achieved over 80% inhibition, suggesting compounds in the leaves may help manage diabetes. Overall, the results correlated antimicrobial and anti-diabetic activities with the high phenolic and
Department of Pharmaceutical Management and Regulatory Affairs, Lachoo Memorial College of Science & Technology, Pharmacy Wing, Jodhpur National University, Rajasthan – 342003
The document summarizes research evaluating the anti-inflammatory and antioxidant activities of Ficus krishnae. Total phenol and flavonoid content were measured in methanol and aqueous extracts of F. krishnae. The methanol extract showed higher phenol (0.34 mg/g) and flavonoid (0.60 mg/g) content than the aqueous extract. In vitro assays found the methanol extract inhibited protein denaturation better than the reference drug diclofenac sodium. Additional antioxidant assays, including DPPH radical scavenging, were conducted to characterize the extracts' antioxidant potentials.
The document summarizes an experiment that exposed mice susceptible to atherosclerosis to different components of ultrafine particles (UFP) to evaluate their effects on oxidative stress. Mice were exposed to either the semi-volatile or non-volatile fraction of UFP for 8 weeks. Biomarkers of oxidative stress (glutathione, malondialdehyde, protein carbonyl) were measured in mice serum to determine if one fraction induced more stress. Results suggested the semi-volatile fraction containing polycyclic aromatic hydrocarbons caused higher lipid peroxidation, supporting the hypothesis that these components influence oxidative stress more than non-volatile ones.
Design and Development of Effervescent Floating Tablet Dapagliflozinijtsrd
The objective of the present study was to formulate and evaluate Effervescent Floating Tablet of Dapagliflozin for the treatment of antidepressant agent. Tablets were prepared by direct compression using directly compressible polymers such as HPMC K4M, and Carbopol 934 were evaluated for drug excipient compatibility, density, buoyancy test, swelling study, drug content and In Vitro release profile. Sodium bicarbonate and citric acid were used producing effervescent base for buoyancy of tablets. Analysis of drug release from tablet indicates drug release by zero order, first order rate kinetics. No significant change was observed in physical appearance, drug content, floatability or in vitro dissolution pattern after storage at 450C 750C RH for three months. Samadhan Mali | Shweta Gedam | Swati Talele | Anil Jadhav "Design and Development of Effervescent Floating Tablet Dapagliflozin" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-4 | Issue-5 , August 2020, URL: https://www.ijtsrd.com/papers/ijtsrd31674.pdf Paper Url :https://www.ijtsrd.com/pharmacy/pharmaceutics/31674/design-and-development-of-effervescent-floating-tablet-dapagliflozin/samadhan-mali
folic acid chitosan conjugate nanoparticle containing azithromycin for the tr...shivamgupta1083
The document presents a research proposal for developing folic acid-chitosan conjugate nanoparticles containing azithromycin for treating colorectal diseases. The objectives are to prepare drug-loaded conjugates with desired release characteristics and assess their targeting efficacy and bio-distribution. The plan involves preformulation studies, preparing the folic acid-chitosan conjugate, loading the conjugate with azithromycin, and characterizing the nanoparticles. In vitro and in vivo studies will evaluate particle properties, drug release, cytotoxicity, and the ability to treat colorectal inflammation in a rat model.
Screening of immunomodulatory activity of Sphaeranthus indicus Linn. whole plantiosrjce
This document summarizes a study that evaluated the immunomodulatory activity of the methanolic extract of Sphaeranthus indicus Linn. (MESI) whole plant in rats. The study assessed the effects of MESI at doses of 100, 200, and 400 mg/kg on humoral immunity (antibody titers, plaque forming cells), cellular immunity (delayed type hypersensitivity, T-cell populations), and myelosuppression. MESI showed significant increases in circulating antibody titers, plaque forming cells, delayed type hypersensitivity responses, and T-cell populations compared to control, indicating immunostimulatory effects. The results suggest that Sphaeranthus indicus has potential as
The document summarizes a study that investigated the antioxidant and anti-inflammatory activities of Pterospermum acerifolium. The study found that the ethyl acetate fraction of P. acerifolium showed the highest free radical scavenging activity in various in vitro antioxidant assays. This fraction also demonstrated significant anti-inflammatory effects in both in vivo and in vitro models of inflammation. The results support the traditional use of P. acerifolium for reducing oxidative stress and inflammation.
The document summarizes a study that investigated the antioxidant and anti-inflammatory activities of Pterospermum acerifolium. The study found that the ethyl acetate fraction of P. acerifolium showed the highest free radical scavenging activity in various in vitro antioxidant assays. This fraction also demonstrated significant anti-inflammatory effects in both in vivo and in vitro models of inflammation. The results support the traditional use of P. acerifolium for reducing oxidative stress and inflammation.
The document summarizes a study that investigated the antioxidant and anti-inflammatory activities of Pterospermum acerifolium. The study found that the ethyl acetate fraction of P. acerifolium showed the highest free radical scavenging activity in various in vitro antioxidant assays. This fraction also demonstrated significant anti-inflammatory effects in both in vivo and in vitro models of inflammation. The results support the traditional use of P. acerifolium for reducing oxidative stress and inflammation.
Learnings from Successful Jobs SearchersBruce Bennett
Are you interested to know what actions help in a job search? This webinar is the summary of several individuals who discussed their job search journey for others to follow. You will learn there are common actions that helped them succeed in their quest for gainful employment.
Success is often not achievable without facing and overcoming obstacles along the way. To reach our goals and achieve success, it is important to understand and resolve the obstacles that come in our way.
In this article, we will discuss the various obstacles that hinder success, strategies to overcome them, and examples of individuals who have successfully surmounted their obstacles.
In the intricate tapestry of life, connections serve as the vibrant threads that weave together opportunities, experiences, and growth. Whether in personal or professional spheres, the ability to forge meaningful connections opens doors to a multitude of possibilities, propelling individuals toward success and fulfillment.
Eirini is an HR professional with strong passion for technology and semiconductors industry in particular. She started her career as a software recruiter in 2012, and developed an interest for business development, talent enablement and innovation which later got her setting up the concept of Software Community Management in ASML, and to Developer Relations today. She holds a bachelor degree in Lifelong Learning and an MBA specialised in Strategic Human Resources Management. She is a world citizen, having grown up in Greece, she studied and kickstarted her career in The Netherlands and can currently be found in Santa Clara, CA.
Joyce M Sullivan, Founder & CEO of SocMediaFin, Inc. shares her "Five Questions - The Story of You", "Reflections - What Matters to You?" and "The Three Circle Exercise" to guide those evaluating what their next move may be in their careers.
Leadership Ambassador club Adventist modulekakomaeric00
Aims to equip people who aspire to become leaders with good qualities,and with Christian values and morals as per Biblical teachings.The you who aspire to be leaders should first read and understand what the ambassador module for leadership says about leadership and marry that to what the bible says.Christians sh
We recently hosted the much-anticipated Community Skill Builders Workshop during our June online meeting. This event was a culmination of six months of listening to your feedback and crafting solutions to better support your PMI journey. Here’s a look back at what happened and the exciting developments that emerged from our collaborative efforts.
A Gathering of Minds
We were thrilled to see a diverse group of attendees, including local certified PMI trainers and both new and experienced members eager to contribute their perspectives. The workshop was structured into three dynamic discussion sessions, each led by our dedicated membership advocates.
Key Takeaways and Future Directions
The insights and feedback gathered from these discussions were invaluable. Here are some of the key takeaways and the steps we are taking to address them:
• Enhanced Resource Accessibility: We are working on a new, user-friendly resource page that will make it easier for members to access training materials and real-world application guides.
• Structured Mentorship Program: Plans are underway to launch a mentorship program that will connect members with experienced professionals for guidance and support.
• Increased Networking Opportunities: Expect to see more frequent and varied networking events, both virtual and in-person, to help you build connections and foster a sense of community.
Moving Forward
We are committed to turning your feedback into actionable solutions that enhance your PMI journey. This workshop was just the beginning. By actively participating and sharing your experiences, you have helped shape the future of our Chapter’s offerings.
Thank you to everyone who attended and contributed to the success of the Community Skill Builders Workshop. Your engagement and enthusiasm are what make our Chapter strong and vibrant. Stay tuned for updates on the new initiatives and opportunities to get involved. Together, we are building a community that supports and empowers each other on our PMI journeys.
Stay connected, stay engaged, and let’s continue to grow together!
About PMI Silver Spring Chapter
We are a branch of the Project Management Institute. We offer a platform for project management professionals in Silver Spring, MD, and the DC/Baltimore metro area. Monthly meetings facilitate networking, knowledge sharing, and professional development. For more, visit pmissc.org.
1. International Journal of Pharmaceutical Science Invention
ISSN (Online): 2319 – 6718, ISSN (Print): 2319 – 670X
www.ijpsi.org Volume 3 Issue 5 ‖ May 2014 ‖ PP.07-11
www.ijpsi.org 7 | P a g e
Synthesis, Characterization and Release Studies of Mutual
Prodrugs Of Norfloxacin and Trimethoprim With Indomethacin
For Colon-Specific Drug Delivery
Arshi Hussain1
, Anil Kumar Shrivastava2
, Pradeep Parashar3
1
(Department of Pharmaceutical Chemistry, School of Pharmacy, Suresh Gyan Vihar University, Jaipur-
302001, Rajasthan, India, email ID: ra.19@rediffmail.com)
2
(Nandini Nagar Mahavidyalaya College of Pharmacy, Nawabganj, Gonda-271303, Uttar Pradesh, India)
3
(Department of Chemistry, Govt. L.B.S P.G. College, Kotputli, Jaipur, Rajasthan, India)
ABSTRACT : Prodrug approach is one of the most conventional concepts used for the treatment of several
intestinal bowel diseases (IBD) such as crohn’s disease, ulcerative colitis, and colon cancer etc. The present
study aims towards formation of mutual amide prodrugs of norfloxacin and trimethoprim with indomethacin (IN
and IT) by coupling method for targeted drug delivery to the inflamed gut tissue in IBD. Their physico-chemical
properties were determined and their structures were supported and analyzed by FTIR, 1
H NMR and Mass
spectroscopy. Release study of the synthesized derivatives was done in different simulated gastro-intestinal
fluids to identify the expected hydrolysis of these amide conjugates in gastrointestinal tract. They were found
chemically stable in simulated gastric fluid and remarkable release was observed in simulated colonic fluid,
57.46 % from IN and 62.18 % from IT, although, simulated intestinal fluid reported negligible release of drugs.
So, the purpose of colon-targeting delivery of the drugs for treating infection as well as inflammation may be
achieved.
KEYWORDS: Amide conjugates, colon-targeting, IBD, indomethacin, Norfloxacin, Trimethoprim.
I. INTRODUCTION
NSAIDs are primarily absorbed in the stomach and antibiotics / antibacterial are also absorbed in the
jejunum or distal ileum. Thus, the treatment of intestinal bowel disease (IBD) had ever been a great problem due
to non availability of NSAIDs and antibacterial in the distal intestinal region. Prodrug design is a very important
concept to solve this particular problem and as per the Lipinski rule of five, the drugs having the molecular
weight lesser than 500 can be absorbed from the gastrointestinal tract [1]. Furthermore, the drug will also be
highly hydrophobic and will come under the fourth class of Biopharmaceutical classification system (BCS) [2].
Barring sulphasalazine the other prodrugs could not be successful as colon targeted in the treatment of IBD.
However, earlier various approaches have been applied to synthesize several prodrugs [3, 4]. The problem with
all those prodrugs had been the selection of the drug candidates for their formation. Most of the time 5-
aminosalicylic acid has been generated which has lower potential as compare to other anti-inflammatory drugs
and it is not adequate to be used as such because it is absorbed extensively and rapidly through the upper
intestine before it reaches to colon [5]. To overcome this mesalazine, basalazine and olsalazine etc. have also
been synthesized which protects 5-ASA from acidic pH of stomach and prevents its absorption from upper part
of the gut [6, 7], but none of them have been reported to reach to the market and their used is limited up to the
clinical trials only due to several side effects produced by the carriers such as hepatotoxicity, severe blood
disorders etc. Dose of such prodrugs is also quite high. Their molecular weight was under 500 and therefore,
such prodrugs could not prove worth for the treatment of IBD.
Therefore, in present study we have selected indomethacin which is a highly potent analgesic with a
high molecular weight. It is also used in the form of suppositories to treat the rectal inflammation. Thus, we can
say it will be pertinent to use it with the antibacterial in the form of mutual prodrugs. We have selected
norfloxacin because of the fact that it is very much useful for the treatment of bacterial dysentery. Trimethoprim
will be good to be used as a mutual prodrug along with sulfasalazine and other recently synthesized prodrugs
such as of NSAIDs viz. ibuprofen, diclofenac, and flurbiprofen with sulfonamides like sulphamethoxazole and
sulphanilamide via amide linkage using DCC coupling reaction [8] and mutual prodrug of aceclofenac with
amino acids [9]. The present study describes the formation of mutual prodrugs of norfloxacin and trimethoprim
(antibacterial drugs) with indomethacin (NSAIDs) by masking free carboxylic acid group of the indomethacin
by norfloxacin and trimethoprim via amide linkage through simple coupling process in order to reduce local
2. Synthesis, Characterization And Release…
www.ijpsi.org 8 | P a g e
irritation as well as to reduce infection. Their physico-chemical properties were determined and spectral
characterizations were carried out. The hydrolysis behaviour of the synthesized prodrugs in different simulated
fluids over 24 h was also studied.
II. MATERIALS AND METHOD
Indomethacin was purchased from Loba Chemie, Mumbai. Norfloxacin and Trimethoprim were gifted
by Vivek Pharmachem India Ltd. Jaipur and all other reagents were procured from E. Merck (India) Ltd. and
were of analytical grade. TLC of the synthesized derivatives was carried out on precoated plates of silica gel
(Merck) with chloroform: methanol: glacial acetic acid (4:4:2) as solvent system using iodine vapours and UV
light as detecting agent for visualization. Melting points of the intermediate and the conjugates were determined
by the open capillary method and uncorrected. The λmax of the synthesized prodrugs was determined in
chloroform on a Shimadzu 1700 UV double beam spectrophotometer. The IR spectra were recorded on
Shimadzu FTIR in KBr pellet (anhydrous) at the University of Rajasthan, Jaipur. The H1
NMR spectrum of the
synthesized compounds was recorded in DMSO-d6 with TMS is used as internal standard and the chemical shifts
are recorded in δ ppm, using Bruker Avance II 400 NMR spectrometer, SAIF, Panjab University, Chandigarh.
The molecular weights of compounds were determined from their Mass spectrum recorded at Jeol SX-
102(FAB) Mass spectrometer, SAIF, Panjab University, Chandigarh.
2.1 Synthesis of conjugates of indomethacin with Norfloxacin (IN) and Trimethoprim (IT) [10, 11, 12]
2.1.1Preparation of 2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetyl chloride (acyl chloride of
indomethacin):
Indomethacin (0.01 mol, 3.57 g) was first dissolved in 100 ml of chloroform and freshly distilled
thionyl chloride (0.01 mol+20% excess, 0.9 ml) was added slowly with 1-2 drop of DMF as catalyst. The
reaction mixture was refluxed for 3 h at 70-80 º C, until the evolution of hydrogen chloride and sulphur dioxide
ceased. The excess of thionyl chloride and benzene were distilled off under reduced pressure, to give white
crystalline product, m.p. 100-102 °C, yield 79 %
2.1.2 Coupling of acyl chloride of indomethacin with norfloxacin:
The weigh amount of norflloxacin (0.01 mol, 3.19 g) was taken in about 5% ice cooled solution of
NaOH (5 ml) and 60 ml acetone was added to it and kept at magnetic stirrer for 1 hr to dissolve it completely.
The above mixture was then placed in a round bottom flask containing about 10 ml of pyridine and acyl chloride
of indomethacin (0.01 mol, 3.76 g). The mixture was refluxed for 1 h at 100º C on water bath. After cooling, it
was kept aside. After 24 h the mixture was poured into crushed ice to give precipitate, which was filtered off
and washed several times with water. The crude white to light yellow color solid was then recrystallized from
rectified alcohol to give IN.
2.1.3 Coupling of acyl chloride of indomethacin with trimethoprim:
Weigh amount of trimethoprim (0.01 mol, 2.90 g) was taken in round bottom flask containing about 10
ml of pyridine and acyl chloride of indomethacin (0.01 mol, 3.76 g). The mixture was refluxed for 1 h at 100º C
on water bath. After cooling, the mixture was kept aside for 24 h and then poured into crushed ice. The resultant
prodrug (IT) was obtained as a precipitate, which was filtered and then washed with water and recrystallized
from rectified alcohol.
2.2 Hydrolysis studies of the synthesized prodrugs
The drug release studies of the synthesized conjugates were carried out by diffusion method in different
simulated fluids, viz, simulated gastric fluid (SGF, pH 1.2), simulated jejunal fluid (SJF, pH 4.5), simulated
intestinal fluid (SIF, pH 7.4) and simulated colonic fluids (SCF, pH 7.0) using dissolution test apparatus (Type
1). Weigh amount (10 mg) each of the synthesized prodrugs were gently introduced over the surface of 900 ml
of SGF taken in separate baskets and were kept thermostatically controlled at 37 0.5o
C [13, 14, 15]. About 5
ml aliquots were withdrawn at various time intervals and were extracted with equal amount of ether in order to
remove the interference by free drugs. The aliquots were now estimated on UV spectrophotometer for the
amount of IN and IT remaining. Parent drugs which were supposed to be released from the synthesized
conjugates did not interfere in the absorption range of IN and IT, as is obvious from the differences in the λmax
values of indomethacin (319 nm), norfloxacin (274 nm) and trimethoprim (287 nm) with their prodrugs IN (293
nm) and IT (307 nm). The study in SGF was carried for a period of 2 hours and further release studies were
carried out in SJF, SIF and SCF similarly as described above, for two hours, two hours and 18 hours
respectively, retaining solid contents and the amount of prodrug remaining in aliquots were estimated on UV
spectrophotometer.
3. Synthesis, Characterization And Release…
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R OH
O
R Cl
O
N
O
F
N
N
O
R
HOOC
N
N
NH2
N
H
R
O
MeO
OMe
MeO
N
CH3
R
O
Cl
MeO
SOCl2 / CHCl3
reflux
reflux
reflux
Trimethoprim
+
pyridine
Norfloxacin
+
pyridine
Indomethacin
Acyl Chloride of Indomethacin
IN
IT
R =
Figure 1: Scheme of synthesis of mutual amide prodrugs IN and IT
III. RESULTS AND DISCUSSION
Mutual amides prodrugs of indomethacin with norfloxacin and trimethoprim were synthesized by the
scheme shown in Fig. 1 mentioned above. They were subjected to physico-chemical characterization, the data
are shown in Table 1, and their structures were supported and confirmed by the FTIR, H1
NMR and Mass
spectroscopy as represented by Table 2. IR spectra of IN showed the characteristic absorption band for tertiary
amide C=O stretching at 1643 cm-1
while IT showed –NH stretching at 3433 cm-1
and carboxyl stretching
vibrations at 1672 cm-1
, thus confirmed the formation of amide bond in the synthesized prodrugs. The 1
H NMR
spectra of the synthesized derivatives showed characteristic chemical shifts of the anticipated structures. The
mass spectra showed the parent peak which confirmed the molecular weight of the synthesized prodrugs.
Table I: Physico-chemical properties of synthesized prodrugs
Code Chemical Formula Molecular
Weight
Elemental Analysis (%) %
Yield
Melting
Point (°C)
Rf
value
IN C35H32ClFN4O6 659.27 Calculated: C- 63.78; H,
4.89; Cl, 5.38; F, 2.88; N,
8.50; O, 14.56.
Found: C, 63.13; H, 5.02;
Cl, 5.27; F, 2.84; N, 8.38; O,
14.34
57 235-238
(melts
with
decomposi
tion)
0.83
IT C33H32ClN5O6 630.04 Calculated: C, 62.90; H,
5.12; Cl, 5.63; N, 11.11; O,
15.24.
Found: C, 62.83; H, 5.06;
Cl, 5.59; N, 10.98; O, 15.17
62 156-158 0.69
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Table II: Spectral data of the synthesized mutual amide prodrugs
Compounds IR spectral data (cm-1
) 1
H NMR spectral data (δ) Mass spectral
data (M+H)+
IN 3274 (carboxylic O-H str.), 3014
(aromatic C-H str.),
2997 (asym. C-H str. in methyl and
methylene of ethyl and piperazine),
2842 (sym. C-H str. in methyl and
methylene of ethyl and piperazine),
1720, 1687 (C=O str.),
1643 (C=O str. tert. amide), 1625 ( C=O
str. pyridone), 1473 (quinoline ring C-C
and C-N str.),
1457 (O-CH3 deformation of indole ring),
1241 (C-F and carboxylic C-O str.),
747 (C-Cl ?)
15.11 [ S, 1H] OH- carboxylic acid,
8.22 [s, 1H] CH- pyridone,
7.32-7.66 [ m, 4H] CH- (p-
chlorobenzoyl),
7.10 [s, 1H], 5.83 [ s, 1H] CH- benzene,
6.18-6.67 [m, 3H] CH- indole, 3.72 [s,
3H] –OCH3,
3.86 [q, 2H] –N-CH2-CH3,
3.43-3.61 [m, 8H] -CH2- piperazine ring,
3.28 [s, 2H] –CH2-CO- ,
2.21 [s, 3H] -CH3 gp.,
1.28 [t, 3H] –N-CH2-CH3
660
IT 3433 (N-H str. sec. amide), 3005
(aromatic C-H str.),
2966, 2935, 2837 (aliphatic C-H str.),
1672 (C=O str. sec. amide), 1507
(aromatic ring),
1477 (CH deformation),
1461 (O-CH3 deformation of indole ring),
1239, 1138 (aromatic methoxy),
749 (C-Cl ?);
7.91 [s, 1H]-NH-CO-,
7.63-7.69 [m, 4H] CH- p-chlorobenzoyl,
7.49 [s, 1H] CH-pyrimidine,
6.56-7.10 [m, 3H] CH- indole,
6.15 [s, 2H] CH- benzene,
4.1 [b, 2H] –NH2 gp.,
δ 3.75 [s, 3H]-OCH3(C4),
3.73 [s, 6H] -OCH3(C3, C5),
3.61 [s, 5H] –CH2-, –OCH3,
3.53 [s, 2H] –CH2-CO- ,
2.21 [s, 3H] -CH3 gp.
631
The in vitro hydrolysis studies of the amide conjugates IN and IT indicates negligible release of parent drugs in
SGF (pH 1.2) and SJF (pH 4.5), confirmed their stability in upper GIT which implying that they did not undergo
hydrolysis and would be stable in the acidic pH of stomach. In simulated intestinal fluid, only 1.5 % and 4 %
release of free drugs was observed for IN and IT, respectively. Thus, the objective of bypassing the upper GIT
without any free drug release was achieved. The kinetics was further studied in SCF which indicates remarkable
release of free drugs, 57.4 % from IN and 62.7 % from IT, as represented in Fig. 2
Figure 2: % release of drugs from IN and IT in different simulated fluids over 24 hrs
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IV. CONCLUSION
The authors would like to conclude that the synthesized mutual prodrugs of indomethacin with
norfloxacin and trimethoprim, through an amide linkage leads to a delivery system which is capable of releasing
the drugs in colon without any appreciable release in upper GIT due to their higher molecular weight, however,
they start releasing from prodrugs in distal intestinal region. As unwanted absorption of drugs from GIT is
prevented, this will results in lowering of doses that will ultimately enhance the therapeutic utilization of drugs.
The field is further open for the in vivo release studies of the synthesized prodrugs.
V. ACKNOWLEDGEMENT
Authors thank the Suresh Gyan Vihar University, Jaipur for providing the facilities to carry out this
research work and to Vivek Pharmachem India Ltd., Jaipur for providing the gift samples of the required drugs;
Department of Chemistry, University of Rajasthan, Jaipur; SAIF, Panjab University, Chandigarh, for carrying
out spectral analysis.
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