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ABSTRACT

Floating Drug delivery system is used to target the drug release in the stomach or to the upper parts of the intestine. The eradication of Helicobacter pylori requires the administration of various medicaments several times a day, which often results in poor patient compliance. More reliable therapy can be achieved by using FDDS which can be expected that the topical delivery of antibiotic through a FDDS may result in complete removal of the organisms in the fundal area due to bactericidal drug levels being reached in this area, and might lead to better treatment of peptic ulcer. Since gatifloxacin is a potential drug for eradication of H. Pylori infection responsible for gastric and duodenal ulcers, the oral delivery of antibiotic gatifloxacin was facilated by preparing a non-disintegrating floating dosage form which can increase its local availability in the stomach by increasing the drug’s gastric residence time. The tablets were prepared in six batches F1 to F6 by the direct compression technique using polymers such as hydroxyl propylmethylcellulose (HPMC K4M, HPMCK 15M M, and HPMC K100M, along with sodium bicarbonate as the gas –generating agents. The prepared tablets were evaluated for their physicochemical properties and drug release. In-vitro release studies indicated that the gatifloxacin release form the floating dosage form was uniform F2 and F6 and followed Higuchi drug release.  Sodium bicarbonate was used as the gas-generating agents which cause the tablets to float on the G.I fluids. Formulation showed a floating lag time less than 60 seconds and floating time above 12 hrs.  

Keywords:- Floating drug delivery system, Gatifloxacin, HPMC, Direct compression technique.

ABSTRACT

The behavior of different technological variants of extended release tablets of divalproex Sodium (960mg) obtained by direct compression technique. The extended time and the percentage of the dissolved drug showed a significant dependence of the polymers ratios present in formulae. The physical and chemical properties of tablets were assessed during Three months (accelerated stability), respectively. From the formulae selected it was possible to obtain granulates and tablets with organoleptic, physiochemical and technological properties, demonstrating the feasibility of the process of fabrication of this product. Results showed the good stability in the extended release divalproex Sodium tablets selected. The in vitro dissolution hasn\'t significant differences, thus, neither the time elapsed nor the composition of formula influenced on the percentages of dissolved drug. The assessment demonstrated significant differences, however, assessed formulae fulfilled with official pharmaceutical specifications during 3 months.

Keywords:-Divalproex sodium, Hydroxyl Propyl Methyl Cellulose, Extended release, Direct compression technique,

     Stability studies.

ABSTRACT

The high molecular weight water soluble  homopolymer type of acrylamide was  reported to obtain very high viscosity in low concentration, transparency, film forming properties and useful in formation of transdermal gel. The piroxicam gels were prepared by using different concentration of polyacrylamide for topical drug delivery with an aim to gradually increase transparency and spreadability. These preparations were further compared with marketed known Dolonex gel. Spreadability and consistency of polyacrylamide gel containing piroxicam gel (S9) were 6.5g.cm/sec and 5mm as compared to 5.5g.cm/sec and 10mm respectively of known marketed gel, indicating good spreadability nature and consistency of the prepared gel (S9). The transparency nature of prepared batch (S9) was good as compared to the known marketed gel. The percent drug release was 97.85% and 98.84% from S9 and known marketed gel respectively. No irritation was felt in the skin irritation test. Stability studies’ conducting under accelerated condition was shown satisfactory results. It can be concluded that polyacrylamide gel containing piroxicam gel showed good consistency, spreadability, homogeneity and stability and had wider prospect for topical preparations.

Keywords:- Topical drug delivery, Water soluble polymer, Piroxicam gel, Transdermal gel, Polyacrylamide.

ABSTRACT

A number of drugs are in the clinical use, search for new NSAIDS is still relevant because the existing molecules suffer from the drawback of adverse effects such as gastric ulceration, inhibition of platelet function, alterations in the renal function, hypersensitivity reactions. The present research work focuses on the diazotization, alkylation with conventional stirring and refluxation methods to form some novel benzotriazole derivatives containing pyrazolidine dione moieties. The characterisation of n=8 derivatives was carried out using I.R, ¹H NMR and mass spectral analysis. The percentage yield of final compounds was found to be 71.43 % to 88.06%. Purity of the compounds was checked by using TLC and elemental analysis. These compounds showed a considerable anti-inflammatory activity and analgesic activity using In vivo methods compared to Indomethacin and Tramadol respectively.

Keywords: Benzotriazole, Pyrazolidine 3, 5-dione, Anti -inflammatory activity, Analgesic activity.

ABSTRACT

Annona Squamosa, a multipurpose, drought resistant evergreen tree commonly known as “Custard apple” belonging to family Annonaceae, is gaining lot of importance for its therapeutic potentials. Various part of tree has been used in traditional folkloric medicine. The crushed leaves are sniffed to overcome hysteria and fainting spells; they are also applied on ulcer and wounds and a leaf decoction is taken in case of dysentery. Before exploiting any plant for medicinal purpose it is imperative to have complete information about its biology, chemistry, and all other applications so that the potential of plant could be utilized maximally. The taxonomy, botanical description of the plant, its distribution and ecological requirement are discussed in this paper. The possibilities of potential of plant for various pharmacological activities have been summarized. Overall, this paper gives an overview on covering the biology, chemistry, and various commercial and therapeutic applications

Keywords: Annona squamosa, Ecological requirement, Pharmacological, Commercial, Therapeutic applications.

ABSTRACT

The objective of the present study was to develop a thermo sensitive in situ gel system based on chitosan (CS) and poly vinyl alcohol (PVA) for nasal delivery of Levodopa. The hydrogel was prepared by mixing the chitosan and poly vinyl alcohol. The concentration of the components was optimized during formulation development. The prepared hydrogel was characterized for gelation temperature, gelation time, viscosity changes, degree of swelling, in vitro release and in vivo activity. The prepared hydrogel was liquid at room temperature while underwent thermal transition from solution below or at room temperature to non-flowing hydrogel when incubated at 37^oc within 12-15 minutes with increased viscosity. The in vitro release of Levodopa from gel network was observed, the release of levodopa through gel network decreases upon increasing the chitosan concentration from 1 to 5%. Furthermore, the formulation when evaluated for their in vivo activity results indicates that the proposed thermo sensitive in situ gelling system has substantial potential as nasal delivery system for Levodopa.

Key words: In situ gel system, Nasal delivery, Levodopa, Chitosan, PVA.

ABSTRACT

The coconut, Cocos nucifera L., has been described as \"the tree of life\" or the tree of plenty and nature’s greatest gift to man. Coconut is a large palm (30 mts tall) and member of Arecaceae family with binomial nomenclature as Cocos nucifera. Coconut is known as Naarikela in ayurveda. The fruit, flower and root of this plant are used as ingredients for many ayurvedic preparations and it is also used in Malay traditional medicine to treat ailments such as fever, headaches, stomach upset and diarrhea. Coconut products provide food, shelter and energy to farm households and can be made into various commercial and industrial products. The husk fiber of Cocos nucifera has antibacterial and antiviral, antitumoral alternative for oral rehydration and intravenous hydration of patients particularly in remote regions. It may also offer protection against myocardial infarction and control of hypertension. It is also effective in the treatment of kidney and urethral stones, urinary infections and mineral poisonings. This study is an attempt to compile an up-to-date data and comprehensive review of Cocos nucifera that covers its overview of traditional and medicinal uses, phytochemistry and pharmacology profile.

Keywords: Cocos nucifera, Arecaceae, Naarikela, Phytochemistry.

ABSTRACT

Cucurbitaceae family is major source of medicinal agents since ancient time. Various plants parts including fruits of this family have been established for their pharmacological potential. In the series of Cucurbitaceae plants, Praecitrullus fistulosus is one of the excellent plants, gifted by the nature having composition of all the essential constituents that are required for normal and good human health. Genus Praecitrullus fistulosus is very similar to Citrullus in its morphological characters, but differs in the stratification of pollen grains, haploid chromosome number and to some extent in leaf morphology. . This study is an attempt to compile an up-to-date and comprehensive review of Praecitrullus fistulosus that covers its traditional and folk medicinal uses, phytochemistry and pharmacology profile.

Keywords: Praecitrullus fistulosus, Cucurbitaceae, Citrullus.

ABSTRACT

Site specific drug delivery has gained a lot of interest in the last decade. Colon targeting has potential opportunities and challenges in the area of research. Colon was considered as “BLACK BOX” as, most of drugs are absorbed from upper part of GIT tract. Colon-specific drug delivery has gained increased importance as it has large amounts of lymphoma tissue, lack of digestive enzymes and long transit time. Colon specific drug delivery is not only used for the delivery of the drugs for the local treatment of diseases associated with colon but also for the systemic delivery. Colon is the potential site for the delivery of the proteins and peptides. This article reviews the surge of focus on the colon targeting multiparticulate systems as they are having less inter and intra subject variability. Reports suggest that drug carrier systems larger than 200 µm possess very low gastric transit time due to physiological condition of the bowel in colitis. Thus considering the selective uptake of micron or sub-micron particles by cancerous and inflamed cells or tissues a multiparticulate approach based on pellets, granules, and microsphere or nanoparticle type formulation is expected to have better pharmacological effect in the colon.

Key words: Transit time, Multiparticulate systems, Lymphoma tissue, Inter and intra subject variability.

ABSTRACT

India is one of the world’s twelveth leading biodiversity centers with the presence of over 45000 different plant species. Herbs and its active constituents are being used to treat the infectious organisms, which no longer responsive to conventional medicine. The herbal drugs been used throughout the world  have received greater attention in recent times, because of its diversity of curing diseases and well tolerated remedies compared to the conventional medicines. The aim of this study was to evaluate the anti-diabetic activity, anti-microbial activity and pharmacological activity of leaves extracts of Prosopis chilensis. All the extract was subjected to phytochemical analysis. It shows the presence of Saponins, Carbohydrates, Cardiac glycosides, The percentage yield of solvent extracts method and yield from leaves of Prosopis chilensis of petroleum ether (6.5%), chloroform (6.9%), ethanol (14.6%) and water extracted (27.14%)  and Solvent Extraction method and yield from leaves of Prosopis chilensis of petroleum ether (6.1%), chloroform (5.9%), ethanol (12.6%) and water extracted (21.11%). The present study concluded that the anti-microbial activity and anti-diabetic activity of various extracts of leaves of Prosopis chilensis extracts showed significant therapeutic activity, but in specific ethanolic extract exhibit maximum activity may be due to presence of steroids, triterpenes.

Key Words:-Prosopis chilensis, Anti-diabetic activity and Anti-microbial Activity.

ABSTRACT

Microwave assisted organic synthesis is an enabling technology for accelerating drug discovery and development processes. A series of novel 4-(substituted amino) phenyl)-N-phenylpiperazine-1-amine as potential biological active compounds were derived from microwave irradiation with bromoaniline and different aromatic aldehydes. All the compounds were characterized by melting point, TLC and their chemical structures were confirmed by elemental analysis, spectrometry (IR, ¹H NMR). The synthesized compounds were subjected for antibacterial and antioxidant activity. The synthesized compound was shown to exhibit good antibacterial activity comparable to that of standard. The antioxidant properties were evaluated by following methods: Phosphomolybdate method and reducing power assay. The compound 3a₁ showed good antioxidant activity compared to that of standard.

Key Words:- Microwave, Piperazine, Antioxidant, Antibacterial.

ABSTRACT

The present study deals with the pharmacognostical evaluation of the leaves of the plant Vigna radiata (L.) R. wilczek. Vigna radiata belonging to the family Fabaceae is an annual herb. It grows up to one meter high, bears small, yellow-colored flowers, and produces small, light yellowish-orange, edible fruit sometimes referred to as Cape gooseberry or cut leaf ground cherry. Even though this plant has gained scientific importance recently, there is a need for the pharmacognostic standardization. Hence, in the present work the leaf a part of the plant were subjected to various microscopical and physical evaluations. In the microscopical studies, the different cell structures and arrangements were studied and in physical evaluation the ash values and extractive values were studied. The various pharmacognostical constants were obtained which could help in the development of a suitable monograph for the plant. Morphological and anatomical aspects as well as microscopical characteristics have been worked out to identify the diagnostic features of the plant. Physical constant values involving moisture content, ash and extractives as well as qualitative and quantitative estimation of various phytochemical have been studied. The study confirms that the evaluation showing presence of Saponins, Tannins, Terpenoids, Steroid, Flavonoids and some other chemical constituents.

Key Words:- Vigna radiata, Macroscopical, Microscopical, Fabaceae, Leaf Constants, Proximate Analysis, Fluorescence Analysis.

ABSTRACT

The rapid proliferation of drugs being switched from prescription (Rx) to over-the-counter (OTC) drugs. The aim of this study was to investigate the general public\'s opinion and perceptions of OTC medicines. The study was conducted in randomly selected urban and rural areas of Saurastra region of Gujarat, India, between the years 2009 and 2011. Qualified pharmacists appraised of the survey procedures and study was conducted using specially prepared questionnaires. 201 responses with bronchial asthma were recorded and analyzed. Questions were explore the social and demographic variables, detailed assessment of non-prescription use of anti asthmatic drugs and self-reported medical illnesses. During the purchase of OTC drugs, we were tried to know if the patient had any knowledge of drugs and its side effects and regularity in taking medicine. The results of present study suggested that non-prescription use of anti asthmatic drugs is relatively uncommon.

Key Words:- Over-the-counter medicines, Anti asthmatic drugs, Non-prescription use.

ABSTRACT

Crystallization, a technique that had proved to be a new era in the growth of pharmaceutical industry. Crystal’s preparation by different methods solved the problem of solubility to a large extent. Furtherly, size reduction to micron level and even lesser had accelerated the solubility of major drugs. The main objective of this study is to prepare and evaluate the micro crystals of ibuprofen (class II drug according to BCS classification) and to investigate the solubility profile of the prepared micro crystals. The micro crystals of ibuprofen are prepared by antisolvent method by taking two different polymers, poly vinyl pyrrollidine and poly ethylene glycol- 300 (PEG- 300). The prepared micro crystals are evaluated from FTIR, solubility, dissolution, microscopic studies. From the data obtained from the above research work it was observed that the  treated micro crystals has shown increased solubility and dissolution rate when compared to that of the pure drug.

Key Words:- Micro crystals, Crystallization, Ibuprofen, Size reduction, Poly vinyl pyrolidine, Poly ethylene glycol- 300.

ABSTRACT

The aim of the present work was to prepare a novel self microemulsion drug delivery system (ME) to enhance the solubility, dissolution rate and ultimately the oral bioavailability of a poorly water soluble drug, Simvastatin. The prepared self microemulsion of simvastatin was charactriesed by using techniques like FTIR analysis for investigating the drug-excipients interactions, zeta potential, viscosity determination, drug entrapment efficiency and thermodynamic stability studies. The invitro drug release profile of self microemulsion was carried in phosphate buffer Ph 7.4 for 1 hr by using USP dissolution apparatus type-II device. From the invitro dissolution data, F5 formulation was found that the drug release is best and the cumulative % of drug release was 98.62% respectively. The promising formulation F5 was found by evaluation studies were compared with Marketed product (Simvas 10mg), the F5 formulation gave 98.62% of the drug release and the Marketed product gave 45.19 % of drug release in 1 hr of dissolution study. The in-vitro intestinal permeability results exhibits the drug diffused at a faster rate from the self microemulsion system than from the tablet dosage form. After 1 hour of diffusion, 76.54% of drug was diffused from the self microemulsion system, as compared with 34.23% diffused from the tablets. Therefore the developed ME formulation improved the Solubility and in-vitro drug release of Simvastatin when compared with commercial tablet formulation.

Key Words:- Simvastatin, Self Microemulsion, Characterization, In vitro release studies, Stability studies.

ABSTRACT

A simple, specific, accurate and precise RP HPLC method has been developed for the determination of Lamivudine from Semisolid Dosage Form by reverse phase HPLC. C₁₈ column (shimadzu C₁₈ , 250 x 4.6 mm, 5 mm). The sample was analyzed using acetate buffer and methanol in the ratio of 90:10 (v/v) and glacial acetic acid was added to adjust the pH 3.8 as a mobile phase at a flow rate of 1.0ml/min and detection at 277nm. The retention time for Lamivudine was found to be 6.37 min. The stability assay was performed and was validated for accuracy, precision, linearity, specificity and sensitivity in accordance with ICH guidelines. Validation revealed the method is specific, rapid, precise, reliable, and reproducible. Calibration plots were linear over the 25 to 100 mcg/ml of concentration ranges for drug . The method can be used for estimation of Lamivudine drug in solid dosage form.

Keywords: HPLC method, Estimation of Lamivudine, Lamivudine Tablet.

ABSTRACT

The antiulcer activity of ethanolic extract of Cassia alata leaves (ECA) was investigated in pylorus ligation and ethanol induced ulcer models in experimental rats. In both models the common parameter determined was ulcer index. Ethanolic extract of Cassia alata at a dose of 150 and 300mg/kg produced significant inhibition of the gastric lesions induced by pylorus ligation induced ulcer and ethanol induced gastric ulcer. The extract (150mg/kg and 300mg/kg) showed significant (p<0.05) reduction in gastric volume, free acidity and ulcer index as compared to control. This present study indicates that ECA have potential anti-ulcer activity in both models. These results may further suggest that the extract was found to possess anti-ulcerogenic as well as ulcer healing properties, which might be due to its anti-secretory activity.

Key Words:- Ethanolic extract, Cassia alata, Pylorus ligation, Ethanol induced ulcer model.

ABSTRACT

Modern clinical studies have confirmed the efficacy and safety of Picrorhiza kurroa for the treatment of liver disease. The roots and rhizomes are used for hepatoprotective activity. Aqueous extract of Picrorhiza kurroa hepatoprotective activity was assessed in CCl₄ induced hepatotoxicity in albino wistar rats. Six groups, each group containing of six rats. Group 1 (control) is treated with normal saline (10 ml/kg bw po). Group 2 was serving as CCl₄ treated control with (3 ml/kg bw po) on the last day. Group 3, 4 and 5 received Picrorhiza kurroa at different doses (100 mg/kg, 200 mg/kg, 400 mg/kg bw po) respectively and on the final day introduction of CCl₄ was made. As for group 6, silymarin (200 mg/kg bw po) and CCl₄ on the concluding day. On the last day, after 1 hour receiving CCl₄ animals were anaesthetized with ether and blood was collected from the retro orbital plexus to study the liver function. Histopathological study was also conducted to measure the action of Picrorhiza kurroa on parameters such as hepatic fatty degeneration and centrizonal necrosis of respective groups. Present study suggested that CCl₄ administration increased the levels of transaminase enzymes. However, the aqueous extract of Picrorhiza kurroa significantly reduced the elevated serum levels of transaminase enzymes in CCl₄ intoxicated rats. Similarly histopathological studies showed the same outcome as mentioned above and showed marked reduction in fatty degeneration and centrizonal necrosis in CCl₄ intoxicated rats. Present study suggests that aqueous extract of Picrorhiza kurroa has significant hepatoprotective activity against CCl₄ intoxicated rats.

Key Words:- Picrorhiza kurroa, CCl₄, Hepatoprotective, Transaminase enzymes, Histopathological study.

ABSTRACT

This work investigated the preparation of biodegradable beads with alginate polymer by ionotropic gelation method. Ionotropic gelation was applied to prepare beads using chitosan and calcium chloride (CaCl₂) as cationic components and alginate as anion. The concentration of sodium alginate was kept at the minimum level (3.5%w/v), required for the formation of beads and study the effect of addition of poly vinyl pyrrolidone (PVP) (2%w/v) and 0.5% chitosan to the CaCl₂ solution.  The drug loading, encapsulation efficiency and in vitro release characteristics were studied the results showed that the addition of, chitosan significantly improved drug loading and encapsulation efficiency and release characteristics but addition of PVP does  not alter the release characteristics but improves drug loading and encapsulation efficiency.

Key Words:- Rifampicin, Sodium alginate, PVP, Chitosan, Ionotropic gelation method.