C K Ashok Kumar

sree vidyanikethan college of pharmacy, Tirumalai, Andhra Pradesh, India

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Publications (18)22.69 Total impact

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    ABSTRACT: Context: Rauvolfia serpentina (L). Benth. ex Kurz. (Apocynaceae) possessing antibacterial properties are widely used in modern herbal medicines. Curcuma longa L. (Zingiberaceae), a readily available antiseptic, possess antioxidant, antibacterial, blood purifying and antiinflammatory properties and used in various skin creams. Azadirachta indica A. Juss. (Meliaceae) possess astringent, antiviral, discutient, stimulant and antibacterial properties and works excellently well against acne and keeps the skin healthy. Objective: Acne is the common skin problem that 85% of the teenagers face today. In this study, poly herbal anti-acne face wash gels were prepared using two polymers Carbopol and hydroxy propyl methyl cellulose (HPMC) along with the extracts of plants Rawvolfia serpentina, Curcuma longa, and Azadiracta indica. Materials and methods: The gel formulations were prepared in four different concentrations of 50, 100, 200 mg/ml as Gel-CRB 100, Gel-HPMC 50, Gel-HPMC 100, Gel-HPMC 200, respectively. The formulations were tested for the anti-acne activity by turbidimetric method. Results: Results showed that the gels were non-irritant, stable and posses anti-acne activity. The efficacy when tested with a standard was almost same to that of Clindamycin gel. Discussion and conclusion: From this study, Gel-HPMC 100 was proved to be stable and considered as an effective herbal formulation for acne treatment.
    Pharmaceutical Biology 08/2011; 49(8):771-4. · 1.21 Impact Factor
  • Arun Rasheed, C K Ashok Kumar, Ashutosh Mishra
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    ABSTRACT: The present investigation deals with the synthesis of novel prodrugs of dexibuprofen with amino acids with an aim to achieve potent anti-inflammatory activity and less gastrointestinal toxicity. Structures of synthesized compounds were confirmed by spectral and elemental analyses. In vitro hydrolytic studies in simulated intestinal fluid, 80% plasma and rat faecal matter showed satisfactory release of dexibuprofen due to enzymatic cleavage. The synthesized prodrugs were evaluated for anti-inflammatory activity, analgesia, ulcerogenicity and histopathology. The anti-inflammatory activity of dexibuprofen was 43.3% whereas an improved value of 73.4, 77.3, 72.8 and 64.5% was observed for the synthesized prodrugs. The percentage analgesia of the prodrugs increased, whereas a decrease in the mean ulcer index values than dexibuprofen was observed. The histopathological studies revealed less ulceration in the gastric region when treated with prodrugs. Thus, the prodrugs were proved to be better in action as compared with the parent drug.
    Journal of Enzyme Inhibition and Medicinal Chemistry 01/2011; 26(5):688-95. · 1.50 Impact Factor
  • Arun Rasheed, C K Ashok Kumar
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    ABSTRACT: This study deals with the synthesis, pharmacological activity, and kinetic studies of mefenamic acid (MA) prodrugs of tyrosine and glycine. The synthesis involved a series of protection and deprotection reactions. The hydrolysis of these prodrugs in the intestine was confirmed by hydrolysis kinetics studies in simulated gastric fluid, simulated intestinal fluid, and 80% plasma. The prodrugs were also evaluated for analgesic, anti-inflammatory, and ulcerogenic activities. The glycine prodrug showed maximum analgesic activity of 86%, and both tyrosine and glycine prodrugs showed better anti-inflammatory activity of 74% and 81%, respectively, when compared to the 40% of MA. Further, the prodrugs showed fewer gastric ulcers compared to MA; tyrosine and glycine prodrugs had an average ulcer index of 9.1 and 4.5, respectively, while an average ulcer index of 24.2 was observed with MA. These findings suggest that both prodrugs are better in action as compared to MA, and are advantageous in having fewer gastrointestinal side effects.
    Journal of Enzyme Inhibition and Medicinal Chemistry 12/2010; 25(6):804-11. · 1.50 Impact Factor
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    Arun Rasheed, C K Ashok Kumar
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    ABSTRACT: The gastrointestinal toxicity associated with aceclofenac can be reduced by condensing its carboxylic acid group with methyl esters of amino acids like histidine and alanine to give amide linkage by the Schotten-Baumann method. Physicochemical characterization of the conjugates was carried out by various analytical and spectral methods. The synthesized conjugates were also subjected to in vitro hydrolysis in simulated gastric fluid (SGF) at pH 1.2, simulated intestinal fluid (SIF) at pH 7.4 and SIF+ 80% human plasma at pH 7.4. The release of free aceclofenac from histidine and alanine conjugated aceclofenac showed negligible hydrolysis in SGF compared to SIF. This indicated that the conjugates do not break in stomach, but release aceclofenac in SIF. Both synthesized conjugates showed excellent pharmacological response and encouraging hydrolysis rate in SIF and SIF + 80% human plasma. Marked reduction of the ulcer index and comparable increase in analgesic and anti-inflammatory activities were obtained in both cases compared to aceclofenac alone. These findings suggest that the conjugates are better in action compared to the parent drug and have fewer gastrointestinal side-effects.
    Acta Pharmaceutica 03/2010; 60(1):99-109. · 1.16 Impact Factor
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    Rasheed1 Arun, Theja1 I, Silparani1 G, C.K. Ashok Kumar
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    ABSTRACT: Drugs used in the treatment of diseases affecting the brain would be delivered directly to the site of action. However, drugs generally do not readily enter the brain from the circulating blood. The major obstacle in the development of centrally acting therapeutics is the lipoidal Blood Brain Barrier (BBB). The main challenge is to develop drug delivery strategies that will allow the passage of drug molecules through the BBB in a safe and effective manner.This paper focuses on the review of various drug delivery strategies developed to enhance drug delivery across the blood brain barrier.
    Journal of Innovative Trends in Pharmaceutical Sciences. 01/2010;
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    Arun Rasheed, C. K. Ashok Kumar
    Acta Pharmaceutica - ACTA PHARMACEUT. 01/2010; 60(1):99-109.
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    ABSTRACT: CS) is a naturally occurring polymer which finds a wide array of pharmaceutical applications due to its low production costs, biodegradability, biocompatibility, nontoxic nature and mucoadhesion. As a result of its cationic character, CS is able to react with polyanions giving rise to polyelectrolyte complexes. CS has found pronounced application in multiparticulate drug delivery and it enhances the dissolution of drugs having poor solubility. CS microspheres can be prepared by chemical denaturation process, ion induced coagulation and spray drying methods. This review aims to compile the various application of CS in microspheres based drug delivery. This review also aims to include the process variables factors that affect the release of drugs from the microspheres. Chitosan (CS) [a (1→4) 2-amino-2-deoxy-β--glucan] (Figure1). is derived by the alkaline deacetylation of chitin[1]. The primary amine groups render special properties that make CS very useful in pharmaceutical applications [2]. Chitin is an amino polysaccharide (combination of sugar and protein) [3]. Most CS in practical and commercial use comes from the production of deacetylated chitin with the shells of crab, shrimp, and krill (the major waste by-product of the shellfish -processing industry) being the most available source of CS [4]. CS is a polysaccharide polymer containing more than 5,000 glucosamine units, respectively, and their molecular weights are over one million Daltons.CS comprises of copolymers of glucosamine
    Journal of Pharmaceutical Sciences 12/2009; 17:1-12. · 3.13 Impact Factor
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    A. Rasheed, C. K. A. Kumar
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    ABSTRACT: Prodrug design is really not different from the general drug discovery process, in which a unique substance is observed to have desirable pharmacological effects, and studies of its properties lead to the design of better drugs. It is a very fruitful way of research, and its introduction in human therapy has given successful results in improving the clinical and therapeutic effectiveness of drugs suffering from some undesirable properties that otherwise hinder their clinical usefulness. The present article reviews various prodrugs and their applications and presents the developments in this field during the last few decades. This review also highlights developing strategies in targeted prodrug design, including antibody-directed enzyme prodrug therapy, gene-directed enzyme prodrug therapy and peptide transporter-associated prodrug therapy.
    Pharmaceutical Chemistry Journal 02/2009; 42(12):677-686. · 0.32 Impact Factor
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    ABSTRACT: CS) is a naturally occurring polymer which finds a wide array of pharmaceutical applications due to its low production costs, biodegradability, biocompatibility, nontoxic nature and mucoadhesion. As a result of its cationic character, CS is able to react with polyanions giving rise to polyelectrolyte complexes. CS has found pronounced application in multiparticulate drug delivery and it enhances the dissolution of drugs having poor solubility. CS microspheres can be prepared by chemical denaturation process, ion induced coagulation and spray drying methods. This review aims to compile the various application of CS in microspheres based drug delivery. This review also aims to include the process variables factors that affect the release of drugs from the microspheres. Chitosan (CS) [a (1→4) 2-amino-2-deoxy-β--glucan] (Figure1). is derived by the alkaline deacetylation of chitin[1]. The primary amine groups render special properties that make CS very useful in pharmaceutical applications [2]. Chitin is an amino polysaccharide (combination of sugar and protein) [3]. Most CS in practical and commercial use comes from the production of deacetylated chitin with the shells of crab, shrimp, and krill (the major waste by-product of the shellfish -processing industry) being the most available source of CS [4]. CS is a polysaccharide polymer containing more than 5,000 glucosamine units, respectively, and their molecular weights are over one million Daltons.CS comprises of copolymers of glucosamine
    Journal of Pharmaceutical Sciences and Research. 01/2009; 1:1-12.
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    ABSTRACT: The anti-inflammatory potential of methanol extract of Pavetta indica Linn. leaves (Family: Rubiaceae) was evaluated against several models of inflammation such as carragenin, histamine and dextran induced pedal inflammation in rats. The extract showed 48.41%, 41.10% and 24.22% inhibition respectively; when compared to that of control animals. The effect was comparable with that of the standard drug indomethacin, a standard non-steroidal anti-inflammatory drug. Simultaneous subplantar administration of the extract and carrageenin in a mixture helps in differentiating true anti-inflammatory action from an apparent anti-inflammatory effect due to counter-irritant activity. The methanol extract also effectively and significantly reduced cotton pellet induced granuloma. The percentage of inhibition was 62.78 at the dose 500 mg/kg, thereby suggesting its activity in the proliferative phase of the inflammatory process.
    Phytotherapy Research 09/2003; 17(7):817-20. · 2.40 Impact Factor
  • Subhash C Mandal, C K Ashok Kumar
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    ABSTRACT: Methanol extract of Ficus hispida L. showed significant inhibitory activity against castor oil-induced diarrhoea and PGE(2)-induced enteropooling in rats. It also showed a significant reduction in gastro-intestinal motility on charcoal meal test in rats. The results obtained establish the F. hispida leaf extract as an anti-diarrhoeal agent.
    Fitoterapia 01/2003; 73(7-8):663-7. · 2.23 Impact Factor
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    ABSTRACT: The antiinflammatory activity of Betula alnoides extract was evaluated in acute and subacute inflammation models. The extract was also evaluated for antiinflammatory activity in sheep RBC induced sensitivity and in membrane stabilization models. Except for the sheep RBC induced sensitivity model, the extract showed significant antiinflammatory activity.
    Phytotherapy Research 12/2002; 16(7):669-71. · 2.40 Impact Factor
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    ABSTRACT: Rodents treated with extract from Xanthium strumarium Linn. (Compositae) exhibited alterations in general behavior patterns, reduction in spontaneous motility, prolongation of pentobarbitone-induced sleep, suppression of exploratory behavior patterns, and avoidance response. The observations suggested Xanthium strumarium had significant depressant action of the central nervous system.
    Journal of Herbs Spices & Medicinal Plants 05/2001; 8(1):69-77.
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    ABSTRACT: The methanol extract of Asparagus racemosus root (200 and 400 mg/kg, p.o.) showed significant antitussive activity on sulfur dioxide-induced cough in mice, the cough inhibition (40.0 and 58.5%, respectively) being comparable to that of 10-20 mg/kg of codeine phosphate (36.0 and 55.4%, respectively).
    Fitoterapia 01/2001; 71(6):686-9. · 2.23 Impact Factor
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    ABSTRACT: The methanol extract of the leaves of Ficus hispida Linn. (Moraceae) was evaluated for hepatoprotective activity in rats by inducing acute liver damage by paracetamol (750 mg/kg, p.o.). The extract at an oral dose of 400 mg/kg exhibited a significant protective effect by lowering the serum levels of transaminase (SGOT and SGPT), bilirubin and alkaline phosphatase (ALP). These biochemical observations were supplemented by histopathological examination of liver sections. The activity of extract was also comparable to that of Liv-52 a known hepatoprotective formulation.
    Phytotherapy Research 10/2000; 14(6):457-9. · 2.40 Impact Factor
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    ABSTRACT: The methanol extract of the bark of Litsea glutinosa showed antibacterial activity, comparable to chloramphenicol, against all 16 tested microorganisms.
    Fitoterapia 09/2000; 71(4):439-41. · 2.23 Impact Factor
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    ABSTRACT: The colon specific drug delivery of non steroidal anti-inflammatory drugs involves targeting the drug to the colon, thereby lowering the required dose, reducing the systemic side effects, and thus resulting in a more effective therapy system. The gastric side effect of aceclofenac is due to the presence of free carboxylic group. The present study aimed at reducing the side effects of aceclofenac by masking the carboxylic acid group with methyl esters of amino acids through the formation of amide linkage. The amino acids like histidine, alanine, tyrosine and glycine were chosen as promoiety because they had broad spectrum of anti-inflammatory, cytoprotective and immunomodulatory properties and therefore would synergize the effect of prodrug. The structures of synthesized prodrugs were confirmed by elemental analysis, IR, 1 H NMR, 13 C NMR and mass spectroscopy. In vitro reconversion of prodrugs carried out in simulated gastric fluid (SGF), simulated intestinal fluid (SIF) and simulated colonic fluid (SCF) showed that the prodrugs remained intact in SGF and SIF, except SCF. In SCF, the rat fecal content containing colonic enzyme (amidase) hydrolyzed the amide linkage of synthesized prodrugs and free aceclofenac was released Marked reduction of ulcer index and an increase in anti-inflammatory activities were observed for the prodrugs and proved to be better in action in the colon as compared to the parent drug.
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    ABSTRACT: Most of the drugs available to treat diseases are lipophilic in nature and challenging researchers to formulate them for a better bioavailablity. Out of all the approaches available nanosuspensions makes its way forward leading all other methods like cocrystals, microemulsions, liposomes etc. considering the advantages of nanosuspensions many attempts have been made to deliver poorly water soluble drugs as nanosuspensions prepared by adopting various methods. In this review, preparation methods, advantages of such methods, characterization of nanosuspensions, considerations and their applications have been reviewed hoping to make easy the future research in this area. Apart from the advancements till now, it scopes for further investigations in terms of pharmacokinetic and pharmacological correlations, invivo bioavailability studies and integration of physical chemistry, bio-informatics and bio-chemistry to study properties of nanosuspensions in detail.