ARUN RASHEED - Academia.edu (original) (raw)

Papers by ARUN RASHEED

Archiv der Pharmazie, 2017

Oxaprozin is a popular non-steroidal anti-inflammatory drug (NSAID) and its chronic oral use is c... more Oxaprozin is a popular non-steroidal anti-inflammatory drug (NSAID) and its chronic oral use is clinically restricted due to its gastrointestinal (GI) complications. In order to circumvent the GI complications, oxaprozin was amended as a prodrug in a one-pot reaction using N,N-carbonyldiimidazole as an activating agent. Dextran of average molecular weight (60,000-90,000 Da) was exploited as a carrier in the process of oxaprozin prodrug production by esterification. The structural profiles of the synthesized oxaprozin prodrug were characterized by FT-IR and NMR spectroscopy. The oxaprozin prodrug possessed optimal molecular weight, lipophilicity, partition coefficient, protein binding, and degree of substitution of 52.4%. The release of oxaprozin upon hydrolysis of the prodrug in both simulated gastric fluid and simulated intestinal fluid followed first-order kinetics with 55.2 min of half-life. Varied ADME properties of the prodrug resulted upon Schrodinger's QikProp tool application. Oxaprozin prodrug displayed significant analgesic, antipyretic, and anti-inflammatory activities, with a remarkable decrease in the ulcer index and being devoid of antigenicity in experimental animals. Thus, it is evident that oxaprozin prodrug is a safer oral NSAID without causing any ulcerations.

公益社団法人日本放射線技術学会, Jan 20, 1997

Pakistan Journal of Pharmaceutical Sciences, 2012

The moisture content present in human skin makes it look young and the use of moisturizer results... more The moisture content present in human skin makes it look young and the use of moisturizer results in fastening the moisture with a surface film of oil. Acne vulgaris is one of the most commonly seen diseases among the youth. The present study is focused on the use of herbs as moisturizer for acne treatment. The anti-acne moisturizer was formulated from herbal crude extracts and investigated the physico-chemical parameters as well as antibacterial activity of the formulation. The study revealed that ethanol extract of Andrographis paniculata, Glycyrrhiza glabra, Ocimum sanctum, Azadiracta indica and Green tea possessed the potential for inhibiting acne. It was observed that the optimal formula of anti-acne moisturizer was satisfactorily effective to control acne inducing bacteria i.e., Staphylococcus epidermis and Propionibacterium. The physico-chemical parameters of the formulation were also optimal with no signs of irritation.

Pakistan Journal of Pharmaceutical Sciences, 2014

Ayurvedic preparations achieved paramount importance in contemporary life owing to the safety and... more Ayurvedic preparations achieved paramount importance in contemporary life owing to the safety and efficacy when compared with those of synthetic drugs. But due to lack of proper standardization at each stage from starting to culmination results in inferior quality and less demand. Saraswataristam, a fermented ayurvedic preparation, has been employed for treating central nervous system disorders and dermatological problems. Saraswataristam, containing Centella asiatica (L) urban (Umbelliferae) as the major ingredient is prepared as per the Ayurvedic Pharmacopoeial specifications, characterized and standardized for determining the quality, safety and efficacy of herbs used in it. Saraswataristam was prepared and subjected to phytochemical screening by FTIR analysis and HPTLC fingerprinting, heavy metal determination by AAS, determination of alcohol content, test for E. coli, S. aureus, aerobic bacteria, yeasts and mould, oral toxicity studies and anti-epileptic activity by MES method....

The present investigation developed the ester prodrugs of Non-steroidal anti-inflammatory drugs (... more The present investigation developed the ester prodrugs of Non-steroidal anti-inflammatory drugs (NSAIDs), Mefenamic acid(MA) and Flurbiprofen(FBN) by conjugating with the natural antioxidant, 4-methyl umbelliferone that resulted in the formation of Mefenamic acid-umbelliferone ester prodrug (MU) and Flurbiprofen-umbelliferone ester prodrug(FU) .The principal objective of this study is the synthesis of the ester prodrugs of NSAIDs with the enhanced therapeutic activity and minimized side effects. Prodrugs were synthesized by coupling method using N,Ndicyclohexylcarbodiimide/4-dimethylaminopyrimidine, and the resulted prodrugs were subjected to physical, chemical characterization, spectral characterization (IR, H NMR, C NMR and Mass spectra), hydrolysis-kinetic study and pharmacological evaluation such as anti-inflammatory, ulcerogenecity as well as the effect of the NSAIDs in the central nervous system against degenerative mechanisms. The current study revealed that the umbelliferone...

INTRODUCTION Standardization of herbal formulations is essential in order to assess of quality dr... more INTRODUCTION Standardization of herbal formulations is essential in order to assess of quality drugs, based on the concentration of their active principles, physical, chemical, phyto-chemical, standardization, and In-vitro, In-vivo parameters. The quality assessment of herbal formulations is of paramount importance in order to justify their acceptability in modern system of medicine [1]. One of the major problems faced by the herbal industry is the unavailability of rigid quality control profiles for herbal materials and their formulations. In India, the department of Ayush, Government of India, launched a central scheme to develop a standard operating procedures for the manufacturing process to develop pharmacopeial standards for ayurvedic preparations. The subject of herbal drug standardization is massively wide and deep. There is so much to know and so many seemingly contradictory theories on the subject of herbal medicines and their relationship with human physiology and mental ...

Standardization of a crude drug is an important aspect in discussion today. The standardization p... more Standardization of a crude drug is an important aspect in discussion today. The standardization parameters of any crude drug will be resolved primarily by estimating the microscopical features, chemical constituents and physicochemical characters. It was found interesting Lannea coromandelica, a widely distributed plant in India and in Africa, leaves having claimed for many traditional uses and medicinal properties like aphrodisiac, ailment for tooth aches; ulcers etc. many activities have been investigated like wound healing activity, anti inflammatory activity, hypotensive activity etc. In the present work the microscopical, phytochemical and physicochemical evaluation of the leaf powder of the plant has been done and the reports showed all the distinctive microscopic features of the plant and physico chemical constants like ash values, loss on drying, extractive values, flourescent analysis showed all the values are under limits. The Priliminary phytochemical screening, TLC and T...

In this work, we evaluate the structural differences of transmembrane helix 3 in rhodopsin and th... more In this work, we evaluate the structural differences of transmembrane helix 3 in rhodopsin and the 5-hydroxytryptamine 1A (5-HT 1A) receptor caused by their different amino acid sequence. Molecular dynamics simulations of helix 3 in the 5-HT 1A receptor tends to bend toward helix 5, in sharp contrast to helix 3 in rhodopsin, which is properly located within the position observed in the crystal structure. The relocation of the central helix 3 in the helical bundle facilitates the experimentally derived interactions between the neurotransmitters and the Asp residue in helix 3 and the Ser/Thr residues in helix 5. The different amino acid sequence that forms helix 3 in rhodopsin (basically the conserved Gly 3.36 Glu 3.37 motif in the opsin family) and the 5-HT 1A receptor (the conserved Cys 3.36 Thr 3.37 motif in the neurotransmitter family) produces these structural diver-This work was supported in part by grants from Dirección General de Investigación Científica y Tecnológica (PB97-0282), Comisión Interministerial de Ciencia y Tecnologica (SAF98-0064-C02 and SAF99-0073), Comunidad de Madrid (08.5/0079/2000), Universidad del Pais Vasco (G15/98), and Fundació La Marató TV3 (0014/97).

Dexibuprofen and aceclofenac are well‐known NSAID molecules, their oral use leads to gastrointest... more Dexibuprofen and aceclofenac are well‐known NSAID molecules, their oral use leads to gastrointestinal (GI) toxicity. To circumvent that GI toxicity, the prodrug approach is a better alternative. Hence, this research was undertaken to synthesize prodrugs of dexibuprofen and aceclofenac using acrylic polymers with degradable ester bonds. Dexibuprofen was linked to 2‐hydroxypropyl methacrylate by an activated ester technique. The resulting material was copolymerized with 2‐hydroxyethyl methacrylate and methyl methacrylate (in 1:3 mole ratios) by the free radical polymerization method, utilizing azoisobutyronitrile at 65–70°C. Similarly aceclofenac was also processed. The resulting prodrugs were characterized by IR, NMR, and elemental analysis. The synthesized prodrugs possess optimal physicochemical characteristics such as the intended molecular weight, lipophilicity, partition coefficient, and protein binding. The drug release on hydrolysis was studied in various fluids such as SGF (p...

The gastrointestinal toxicity associated with aceclofenac (AC) can be reduced by synthesis of its... more The gastrointestinal toxicity associated with aceclofenac (AC) can be reduced by synthesis of its prodrugs. It involves condensing the carboxylic acid group of AC with methyl esters of amino acids like tyrosine and glycine to give tyrosine conjugated aceclofenac (3a) and glycine conjugated aceclofenac (3b), respectively. Physicochemical characterization of the prodrugs by various analytical and spectral methods was carried out. In vitro hydrolysis in simulated gastric fluid (SGF), simulated intestinal fluid (SIF) and human plasma showed an encouraging hydrolysis rate in SIF and human plasma than in SGF. This indicated that the prodrugs do not break in stomach but release aceclofenac in SIF and human plasma. The pharmacological evaluations showed a comparable increase in anti-inflammatory activity and marked reduction of ulcer index for the prodrugs. Normal histological findings revealed that the prodrugs are not producing any ulceration in the gastric region. The prodrugs thus posse...

Drug Development and Industrial Pharmacy, 2017

Bosentan is a poorly soluble drug and pose challenges in design delivery systems. To enhance the ... more Bosentan is a poorly soluble drug and pose challenges in design delivery systems. To enhance the solubility, dissolution and shelf-life of bosentan by formulating it as S-SMEDDS capsules. Solubility of bosentan was tested in various liquid vehicles such as oils (rice bran and sunflower), surfactants (span 20 and tween 80) and co-surfactants (PEG 400 and propylene glycol) and microemulsions were developed. Bosentan was incorporated into appropriate microemulsion systems which were previously identified from pseudo ternary phase diagrams. Bosentan loaded SMEDDS were evaluated for drug content, drug release, zeta potential and droplet size. The selected liquid SMEDDS were converted into solid SMEDDS by employing adsorption and melt granulation. Solid SMEDDS were characterized for micromeritics and evaluated for drug content, drug release and shelf-life. Isotropic systems R5, R13, S5 and S13 with submicron droplet size had exhibited 85.45, 94.12, 81.67 and 96.64% drug release respectively. Solid SMEDDS of MR13 and AS13 formulations with rapid reconstitution ability, they exhibited 84.85 and 86.74% of on par drug release. The formulations were physicochemically intact for 1.02 and 1.56 years. Liquid SMEDDS composed with PEG400 had displayed optimal characters. Solid SMEDDS had high dissolution profiles than bosentan due to modification in the crystalline structure of drug upon microemulsification. Thus, solid SMEDDS addressed the solubility, dissolution and stability issues of bosentan and becomes an alternate for clinical convenience.

Journal of Acute Disease, 2016

Inflammation mediators, prostaglandins are causing inflammation, pain and pyrexia in the body. Sy... more Inflammation mediators, prostaglandins are causing inflammation, pain and pyrexia in the body. Synthesis of these mediators can be effectively blocked by administering the nonsteroidal anti-inflammatory drugs (NSAIDs). The NSAIDs had age-old history in medicine due to their therapeutic potentials and thus they occupy the major share in clinical practice as well as in commercial market. Mostly the NSAID moieties are chemically composed of carboxylic functional groups and this could be a potential reason for the damage of mucosal lining. Moderate and chronic oral use of these NSAIDs leads to ulcerogenicity, abdominal cramps, intestinal bleeding, mucosal haemorrhage and gastritis. Therapeutic handling of above side-effects is becoming ever challenge for the researchers. In research of surmounting side-effects caused by NSAID, prodrug approach was proven to be effective and successful. Over the time, prodrug concept becomes big boom in the arena of inflammation and its clinical treatment. In last few decades, many researchers have been attempted to synthesize the NSAID prodrugs successively. With this background of information, this article was composed and aimed to provide needful information on NSAID prodrugs such as background history, rationale, mechanism of action, principles involved and their therapeutic outcomes. The successful prodrugs were listed and their molecular structures were also demonstrated here.

Pharmaceutical Chemistry Journal

Dexibuprofen (DI) is a non-narcotic analgesic and anti-inflammatory drug. A biodegradable polymer... more Dexibuprofen (DI) is a non-narcotic analgesic and anti-inflammatory drug. A biodegradable polymer dextran has been utilized as a carrier for synthesis of dexibuprofen-dextran prodrugs to improve aqueous solubility, to increase therapeutic efficiency and to reduce its gastrointestinal side effects. The synthesis involves the condensation of acyl imidazole derivatives of dexibuprofen with dextran of different molecular weights (10000 and 20000) to obtain dexibrofen-dextran prodrugs DD10 and DD20 respectively. The structure of synthesized prodrugs was confirmed by IR and NMR spectroscopy. The molecular weight was determined by Mark-Howink Sakurada viscosity equation and the degree of substitution was obtained as 15.6 % and 16.5 % for the prodrugs. A hydrolysis study was performed in buffer solutions at different pH and in simulated colonic fluid (SCF). The hydrolysis followed first order kinetics. Much faster hydrolysis was observed at pH 9.0 than in pH 7.4 buffer solution and pH 7.4 S...

Pakistan journal of pharmaceutical sciences

Oriental Pharmacy and Experimental Medicine

Asian Pacific Journal of Reproduction, 2014

Pakistan journal of pharmaceutical sciences, 2014

Bhasmas are unique Ayurvedic-metallic preparations with herbal juices/fruits, widely recommended ... more Bhasmas are unique Ayurvedic-metallic preparations with herbal juices/fruits, widely recommended to treat variety of chronic ailments. Trivanga bhasma, a calcinated preparation, is used to treat Diabetes mellitus and as Diuretic. In the present research an attempt has been made to carry out a comparative standardization of formulated Trivanga bhasma (TB1) prepared as per Ayurvedic formulary and marketed Trivanga bhasma (TB2) integrating conventional and modern analytical tools. The formulations were evaluated for physical properties, chemical characterization using FTIR, AAS, SEM, TGA, XRD and AFM along with anti-diabetic, diuretic and toxicology studies. The X-ray Diffraction analysis of both formulations exhibited crystalline nature and nano-sized particles by…