JournalTOCs

Journal of Drug Delivery and Therapeutics JDDT
Number of Followers: 1

This is an Open Access Journal

Open Access journal
ISSN (Online) 2250-1177
Published by Society of Pharmaceutical Technocrats

[1 journal]

Unifying Mechanism Involving Physiological Activity of Spices: Electron
Transfer, Reactive Oxygen Species, Oxidative Stress, Antioxidants, Redox
Chemistry, and Foods
- Authors: Peter Kovacic
  Abstract: This review deals with mode of action of spices. Those studied, involving principal ones and parent substances, together are the following; capsaicin (pepper, tabasco, jalapeño), curcumin (tumeric, ginger, curry), anethole (anise, fennel), myresticin (nutmeg, parseley, dill), sesamin (sesame) and piperine (pepper). These are in the phenolic and phenolic ether class, whereas allicin alone is in the disulfide category. Evidence supports the unfying mechanism of electron transfer, reactive oxygen species and oxidative stress for the seven. The disulfide is closely related via redox reaction without electron transfer. This review is an extension in relation to the unifying mode of action. Physiological and medical effects are treated
  PubDate: 2018-03-15
  Issue No: Vol. 8 (2018)
A REVIEW ON LEARNING AND MEMORY
- Authors: Avneet Gupta, Manish Pal Singh, S. Siddhraj Sisodia
  Abstract: Learning is defined as the acquisition of information and skills and subsequent retention of the information is called memory. Dementia is one of the ages related mental problems and characteristic symptom of various neurodegenerative disorders including Alzheimer’s disease which is age related. It is a progressive and neurodegenerative disorder. The analysis of the anatomical and physical bases of learning and memory is one of the great successes of modern neuroscience. The action of drugs on memory is more or less specific and serious depending on the memory system affected. So the present study is therefore focused on the various types of learning and memory. Key Words: Learning, Memory, Dementia.
  PubDate: 2018-03-15
  Issue No: Vol. 8 (2018)
THE PREVALENCE OF INDIAN COMMON KRAIT ENVENOMATION AND ITS CLINICAL
COMPLICATIONS AMONG THE RURAL POPULATIONS OF INDIA
- Authors: Malathi Ramaswamy, Sivakumar Duraikannu, Chandrasekar Solaimuthu
  Abstract: Snake envenomations have been a serious yet often overlooked public health threat especially in tropical and subtropical countries, including Southeast Asia. The medically important venomous land snakes in Southeast Asia include snakes from the Elapidae and Crotalidae families. Among the elapids, there are only 12 species that are considered of medical importance, represented by the kraits (Bungarus caeruleus, B. candidus, B. fasciatus, B. flaviceps and B. multicinctus). The incidence of snakebite is high in India. Apart from mortality, the morbidity is due to various complications. The common krait (Bungarus caeruleus) is the most toxic snake found commonly in the plains of throughout the India and the number of snakebites in the rural areas of India was recorded by this snake. The present article highlights the prevalence and the clinical complications of Indian common krait envenomation among the rural populations of India. Keywords: snake bite, common krait, clinical complications and rural area
  PubDate: 2018-03-15
  Issue No: Vol. 8 (2018)
TECHNICAL CONSIDERATIONS OF FORCED DEGRADATION STUDIES OF NEW DRUG
SUBSTANCES AND PRODUCT: REGULATORY PERSPECTIVES
- Authors: Asheesh Singh, Parul Singh
  Abstract: Forced degradation studies of new drug substances and drug product are important to help develop and demonstrate specificity of stability indicating methods and provide knowledge about possible degradation pathways and degradation products of the active ingredients and help elucidate the structure of the degradants. They were also useful in the investigation of chemical and physical stability of crystal forms. It is better to start degradation studies earlier in the drug development process to have sufficient time to gain more information about the stability of the molecule. This information will in turn help improve the formulation manufacturing process and determine the storage conditions. As no specific set of conditions is applicable to all drug products and drug substances and the regulatory guidance does not specify the conditions to be used, this study requires the experimenter to use common sense. The aim of any strategy used for forced degradation is to produce the desired amount of degradation i.e., 5–20%. Adequate degradation required to understand the probable degradants for the evaluation of stability indicating method. It has become mandatory to perform stability studies of new drug moiety before filing in registration dossier. The stability studies include long-term studies (12 months) and accelerated stability studies (6 months).Key Words: Force Degradation, Stability Indicating, ICH, Drug substances, Drug product.
  PubDate: 2018-03-15
  Issue No: Vol. 8 (2018)
STABILITY TESTING GUIDELINES OF PHARMACEUTICAL PRODUCTS
- Authors: Megha Pokharana, Rajat Vaishnav, Anju Goyal, Aseem Shrivastava
  Abstract: Stability studies of pharmaceutical products ensuring the maintenance of product quality, safety and efficacy throughout the shelf life are considered as pre-requisite for the acceptance and approval of any pharmaceutical product. Stability of a pharmaceutical product may be defined as the capability of a particular formulation in a specific container/closure system to remain within its physical, chemical, microbiological, toxicological, protective and informational specifications. Stability studies are required to be conducted in a planned way following the guidelines issued by ICH, who and or other agencies. Importance of various methods followed for stability testing of pharmaceutical products, guidelines issued for stability testing and other aspects related to stability of pharmaceutical products have been included in the present review Keywords: stability testing, stability studies, stability, pharmaceutical products, international council for harmonisation
  PubDate: 2018-03-15
  Issue No: Vol. 8 (2018)
CONTRACEPTIVE USE AND FAMILY SIZE PREFERENCES AMONG RURAL WOMEN IN SOKOTO
STATE, NIGERIA
- Authors: Karima Abubakar Tunau, Kehinde Joseph Awosan
  Abstract: Background: The interplay of high fertility, low contraceptive use and high maternal mortality continues to decimate populations across sub-Saharan Africa. This study aimed to determine contraceptive use and family size preferences among rural women in Sokoto State, Nigeria. Methods: It was a cross-sectional study conducted in rural communities of Sokoto State, Nigeria, using both quantitative and qualitative methods of data collection. It involved interviews to a random sample of 202 women of child bearing age using semi-structured interviewer- administered questionnaires, and focus group discussions among women and men. The quantitative data were analyzed using the IBM SPSS version 17 computer statistical package; while the qualitative data were transcribed, sorted, categorized and analyzed thematically. Results: The mean age of the women was 27.9 + 8.0 years, most of them had no formal education (85.6%) and were aged 14-19 years when they had their first pregnancy (84.2%). Of the 202 respondents only 10 (5.0%) were using modern contraceptives, most commonly pills 4 (40.0%), and injectable contraceptives 4 (40.0%). The main barriers to use of modern contraceptives were religious beliefs, desire for more pregnancies, poor understanding of FP concept/ disapproval by husbands; and lack of communication between couples. Almost all the respondents 197 (97.5%) preferred large family sizes and most of them 149 (73.8%) were willing to have as many children as possible. Conclusion: These findings underscore the need for governments and other stakeholders to make female education the central focus of FP promotion programs, in addition to involving men and religious leaders. Keywords: Contraceptive use, modern contraceptives, family size preferences, rural women, Sokoto
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
DESIGN AND EVALUATION OF COLON TARGETED DELIVERY OF TEGASEROD MALEATE FOR
IRRITABLE BOWEL SYNDROME
- Authors: Aditya Tiwari, Mithun Bhowmick, Jagdish Rathi
  Abstract: The colon is being extensively investigated as a drug delivery site. Colonic drug delivery is a relatively recent approach for the treatment of diseases like ulcerative colitis, Crohn’s disease, and irritable bowel syndrome. To achieve successful colon targeted drug delivery, a drug needs to be protected from degradation, release and /or absorption in upper portion of GI tract and then ensure abrupt or controlled release in proximal colon. The purpose of this research is to develop and evaluate the polysaccharide based compression coated tablets of Tegaserod maleate for the treatment of irritable bowel syndrome. Core tablets of Tegaserod maleate were compression coated with various proportions of Galactosol, xanthan gum and chitosan. This work aimed to prepare compression coated tablets by direct compression method using single polymer and combination of polymers. And to evaluate prepared tablets parameters like hardness, friability, thickness, diameter, weight variation, drug content, swelling index, in vitro drug release. Keywords: Colon, Tegaserod maleate, Galactosol, xanthan gum and chitosan
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
ISOLATION AND CHARACTERIZATION OF CHEMICAL COMPOUNDS FROM FRUIT PULP OF
CASSIA FISTULA AND THEIR ANTIMICROBIAL ACTIVITY
- Authors: Deepa Hada, Kanika Sharma
  Abstract: In the present study effect of chloroform fraction of Cassia fistula fruit pulp on cyto-morphological parameters like mycelium width and conidial size of Alternaria solani has been studied. Column chromatography of chloroform extract and TLC fingerprinting of column fractions were also done. Column fractions were screened for antifungal activity and fraction showing best activity was further subjected to GC MS analysis for the purification and identification of the structure of active compound. Result suggested that mycelium width of Alternaria solani increased up to 77.89% and conidia size of the was reduced up to 97.61% at 1.25 mg/ml (Sub MIC) concentration of the chloroform extract. Eight fractions obtained from column chromatography and fraction no. 2 (FPF-2) showed maximum inhibition i.e. 98.25% against Alternaria solani. Rf values of TLC bands of column fractions were found between the range from 0.60 to 0.97cm. GC-MS analysis reveals the presence of butanoic acid, 2-methyl-, Penthiophane (2H-Thiopyran, tetrahydro) and Isopropyl acetate (Acetic acid, 1-methyl ethyl ester). These three compounds are responsible for the antimicrobial activity of Cassia fistula fruit pulp. Keywords: Column chromatography, cytomorphology, Gas chromatography/mass spectrometry, Alternaria solani, Cassia fistula
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
ANTIHYPERGLYCEMIC ACTIVITY OF PITHECELLOBIUM DULES PLANT EXTRACTS ON BLOOD
GLUCOSE LEVELS OF STREPTOZOCIN-INDUCED DIABETIC RATS
- Authors: Ashutosh Upadhayay, Sadhana Kumari, Shalini Shalini, Jayabalan Govindaswami
  Abstract: Background: The prevalence of diabetes mellitus continues to rise worldwide and treatment with oral hypoglycemic drugs leads to numerous side effects and huge monetary expenditure. Therefore active research on identification of new antidiabetic drugs with minimal side effects from medicinal plants is a challenge according to WHO recommendations. In this aspect, the present study was undertaken to evaluate the antihyperglycemic potential of Pithecellobium dules plant in streptozotocin (STZ) induced diabetic rats. Methods: Diabetes was induced in male wister rats by intraperitoneal administration of STZ (45 mg/kg.b.w).Fasting blood glucose (FBG) levels were measured by glucose-oxidase & peroxidase method. The statistical analysis of results was carried out using and one-way analysis (ANOVA) followed by Student t-test. Results and Discussion: Antihyperglycemic potentials of plant of Pithecellobium dules extract has been investigated at the doses of 150, 300 and 600 mg/kg body weight orally administered to streptozocin-induced diabetes male wistar rats. Treatment of streptozocin diabetic male wistar rats with the extracts caused a significant (P<0.01) reduction in the blood glucose levels. The highest activity resides at the dose of 600 mg/kg body weight with mean percentage blood glucose level change of 55.32% after 6 hours of extract administration while the other two doses 150 and 300 mg/kg have blood glucose level change of 40.45% and 47.14% respectively after 6 hours of extract administration. This result suggests that the Pithecellobium dules plant extracts possess antihyperglycemic effect on streptozocin-induced diabetic male wistar rats. Conclusions: The plant extract is capable of managing antihyperglycemia and complications of diabetes in STZ induced diabetic rats. Hence, this plant may be considered as one of the potential sources for the isolation of new oral anti hypoglycemic agent(s) Keywords: Antihyperglycemic activity, Streptozocin, Pithecellobium dules, Diabetes mellitus
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
EVALUATION OF ANTIDIABETIC ACTIVITY OF FRUITS OF WITHAHNIA COAGULANS IN
STREPTOZOCIN INDUCED DIABETIC RATS
- Authors: Ashutosh Upadhayay, Shalini Shalini, Sadhana Kumari, Mujeeb Ur Rahman
  Abstract: In past there have been many medicinal plants, which have been used in traditional medicines for their antihyperglycemic properties without any scientific support and pharmacological evidence. The aqueous extract of Withania coagulans dunal fruit has been taken to evaluate the antihyperglycemic activity in normal and streptozotocin-induced diabetic rats. The plant is known as ‘the cheese maker’ or ‘vegetable rennet’ because fruits and leaves of the plant are used as a coagulant. The milk coagulating property of the fruit is attributed to the pulp and husk berries which posses an enzyme which has milk coagulating activity an antihyperglycemic activity of aqueous extract has not been yet done, as no such reports are available in the literature through the activity is reported. The scientific evaluation of its antihyperglycemic activity was, therefore, explored and also compared with the effect of a standard hypoglycemic drug, glibenclamide. A single oral administration of variable dose levels (100, 200 and 300 mg/kg b.wt) of aqueous extract led to lowering of blood glucose level in normal as well as in diabetic rats. In acute treatment maximum % reduction in glucose level (57.02%) was seen with 300mg/kg b.wt WCD at 6 hr while with standard drug maximum % reduction (62.25%) at 6 hr was found. In subacute study the maximum % reduction in blood glucose level was found (57.22%) with WCD aq. extract in dose 300 mg/kg b.wt which is slightly lesser then the % reduction seen with standard drug (64.52%) respectively. Both the doses 100 & 200 mg/kg b.wt of WCD showed significant effect (p<.05) at 4 hr and highly significant (p<0.01) at 6 hr while in chronic treatment both the doses showed significant reduction in blood glucose from 14th day to 28th days. The findings from this study suggest that the aqueous extract of these fruits may be prescribed as adjunct to dietary therapy and drug treatment for controlling diabetes mellitus. Keywords: Withania coagulans, Antihyperglycemic activity, Diabetes mellitus; Streptozotocin
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
EVALUATION OF PHYSICOCHEMICAL STANDARDIZATION PARAMETERS OF SOLENA
AMPLEXICAULIS LEAF
- Authors: Kshitij Agarwal, Anurekha Jain
  Abstract: Solena amplexicaulis, commonly called as the creeping cucumber, belongs to the family Cucurbitaceae. Traditional it is used as astringent, appetizer, carminative, cardiotonic, digestive, diuretic, expectorant, invigorating, purgative and stimulant. Plant also having antioxidant antidiabetic and antibacterial action. The leaves showed potent anti-inflammatory activity.The present study was carried out to establish physico-chemical parameters along with preliminary phytochemical screening of petroleum ether, chloroform, methanolic and aqueous extracts of Solena amplexicaulis leaf. Preliminary phytochemical screening of various extracts revealed the presence of carbohydrate, alkaloids, flavonoids, sterols, phenolic & tannins compounds. The physico-chemical parameters such as total, water soluble, acid insoluble and sulphated ash (2.2, 1.9, 1.17 and 1.3%w/w respectively) and loss on drying (10.0 %w/w), extractive values foaming and swelling index were studied. These studies will be helpful in developing standards for quality, purity and sample identification of this plant. Keyword: Standardization, Solena amplexicaulis, physicochemical and phytochemical.
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE OF SIMVASTATIN BY USING
SOLID DISPERSION TECHNIQUE ALONG WITH DIFFERENT COMBINATION OF POLYMERS
- Authors: Komal Komal, Taranjit Kaur, Ajeet Pal Singh, Amar Pal Singh, Prachi Sharma
  Abstract: The solubility and dissolution rate of simvastatin, a drug used for the treatment of hyperlipidaemia. Simvastatin is a selective competitive inhibitor of HMG Co A reductase. However its absolute bioavailability is 5%. To increase the solubility of drug solid dispersion was prepared. Solid dispersion preliminary solubility analysis was carried out for the selection of the carrier and solid dispersion was prepared with Hydroxy Propyl Methyl Cellulose (HPMC) and Methyl Cellulose (MC). These solid dispersions were analyzed for the solubility and in-vitro dissolution profile solid dispersion of drug with polymer has shown enhanced solubility with improved dissolution rate. Further FTIR, X-Ray studies were carried out. Solid dispersion prepared with polymer in 1:5 ratios shows the presence of amorphous form confirmed by the characterization study. The study also shows that dissolution rate of simvastatin can be enhanced to considerable extent by solid dispersion technique with Polymer. Keywords: Solubility enhancement, Solid dispersion, Low aqueous solubility
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
ESTROGEN ANCHORED NANOMICELLES FOR COMBINATIONAL DRUG DELIVERY WITH
ENHANCED THERAPEUTIC EFFICACY: A PROTEOMICS GUIDED INVESTIGATION FOR
MULTIFUNCTIONAL NANOTHERAPEUTICS
- Authors: Juan-Juan Yin, Christopher Burgess, Liping Shu, Stepan P. Shumyak, Nicholas Raymond, Li Xu, Lu-Lin Li, Shu-Ming He
  Abstract: The employment of the stable isotope labeling with amino acids in cell culture (SILAC) based proteomic analysis as a guidance tool for investigation of cellular response of a multifunctional nanodelivery system has been described for cancer therapy. The multifunctional nanodelivery system in this study was based on an estrogen anchored multimodal nanomicelle (NPG). The key components of the multifunctional nanomicelle consist: β-cyclodextrin conjugated estrone (CDE1), an escort molecule; polymeric BH3 mimetic, a proapoptotic BcL-2 inhibitor; and the mitotic catastrophe agent paclitaxel. They were assembled into the nanomicelle by multiple weak interactions including hydrophobic/hydrophilic interaction and host-guest recognition. The resulting nanomicelle exhibited unimodal morphology with average size of 170 nm with sustained release. It was found that the nanoparticle exhibits excellent anti-tumor activities for the treatment of breast adenocarcinoma with exceptional targeting efficacy both in MCF-7 tumor bearing mice. NPG as a new drug delivery system demonstrated several merits such as the increased drug uptake in breast tumor tissue, low toxicity, potent tumor growth retardation and metastasis inhibition, as well as potential clinical practicality without compromising liver, kidney and immune function and ameliorating the conventional chemotherapeutics induced phlebitis in breast tumor bearing nude mice model. The systematic SILAC based proteomics study and the subsequent validation revealed that the synergistic induction of mitotic catastrophe through enhanced G2/M phase arrest and PI3K/Akt/mTOR mediated autophagy, account for the exceedingly potent anti-tumor activity of this convergent nanomicelle. Additionally, the verification of the top upregulated gene from the proteomics profiling revealed that the overexpression of zinc finger protein 350 (ZNF350/ZBRK1) is associated with the enhanced antitumor effect induced by NPG.KEYWORDS: Drug targeting, Estrogen Receptor, Proteomics, Paclitaxel, Gossypol, Synergism
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
STUDIES ON MICROCRYSTALLINE CELLULOSE OBTAINED FROM SACCHARUM OFFICINARUM
2: FLOW AND COMPACTION PROPERTIES
- Authors: Nkemakolam Nwachukwu, Kenneth Chinedu Ugoeze
  Abstract: Microcrystalline cellulose (MCC) derived from Saccharum officinarum stem was evaluated for its powder flow and compaction properties in order to assess its suitability as a potential direct compression excipient in tablet formulations. Alpha (α) cellulose obtained from different sodium hydroxide and bleaching treatments of dried shred S. officinarum stem pulp were hydrolyzed with 2.5 N Hydrochloric acid (2.5 N HCl) to obtain MCC which was coded MCC-Sacc. This was compared with a commercial brand, Avicel PH 102. Results of some powder flow parameters were: Bulk and tapped density (0.41 ± 0.01 and 0.54 ± 0.01 g/mL) respectively, particle density (1.82 ± 0.10), porosity (81.69 ± 0.20), Carr’s index (31.47 ± 0.75 %), Hausner’s quotient (1.47), angle of repose (31.00 ± 1.00 °) and these indices indicate poor flowability. Kawakita model assessment of powder showed good densification and cohesiveness. Compacts of MCC-Sacc showed good uniformity of weight, friability, disintegration and mechanical strength. The Heckel model showed good plasticity and slippage of the material. Values obtained were comparable to Avicel PH 102 in terms of compressibility and mechanical strength, hence MCC-Sacc has a good potential for use as a pharmaceutical excipient in direct compression formulation procedure. Keywords: Microcrystalline cellulose, Saccharum officinarum, Avicel PH 102, powder, compaction.
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
GC-MS PROFILING, CHEMICAL CHARACTERIZATION, ANTIOXIDANT, Α-AMYLASE AND
Α-GLUCOSIDASE INHIBITION OF SELECTED SEAWEEDS FROM SOUTHEAST COAST OF
INDIA: AN IN VITRO APPROACH
- Authors: Paramasivam Deepak, Rajamani Sowmiya, Chinnaperumal Kamaraj, Muthu Paulraj Diviya Josebin, Dilipkumar Aiswarya, Govindasamy Balasubramani, Vadivel Amutha, Pachiappan Perumal
  Abstract: The present study focuses on in vitro antioxidant and enzyme inhibitory activity of three different solvent extracts (Methanol, Ethyl acetate and Hexane) of 3 different seaweeds viz: Sargassum wightii, Caulerpa racemosa, and Acanthophora spicifera. The preliminary phytochemical analyses of the seaweed extracts have revealed the presence of various phytochemicals. The antioxidant activities of the seaweed extracts have shown the scavenging effect. Among the extracts, SWEA, SWME and SWHE have exerted effective antioxidant activity with the IC50 values (µg/mL) of: 32.86, 130.1 and 212.8, respectively. And similar trend of α-amylase and α-glucosidase activity/inhibitory property by seaweeds have been recorded. Hence, the ethyl acetate extract of S. wightii was subjected to gas chromatography. All the seaweed extracts were characterized through HPLC and, FTIR analyses. The GC-MS analysis of ethyl acetate extract of S. wightii showed the presence of a bioactive compound, Heptadecanoic acid that might be have been the reason for the recorded inhibitory activity. Keywords: Seaweeds, Sargassum wightii, DPPH, Column chromatography, GC-MS.
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
IMPROVED DISSOLUTION CHARACTERISTICS AND SOLUBILITY ENHANCEMENT OF POORLY
WATER SOLUBLE DRUG BY NOVEL METHOD USING NATURAL GUM AND WATER SOLUBLE
POLYMER
- Authors: Taranjit Kaur, Prachi Sharma
  Abstract: The main objective of the present study is too prepared, characterized and evaluate and surfactant used as a carrier in solid dispersions for enhancing the dissolution rate of simvastatin. The feasibility of formulating solid dispersions of pure drug with gum and surfactant combination that enhanced dissolution rate was also investigated. Solid dispersions of simvastatin in gum: surfactant different polymer ratios were prepared by kneading method and evaluated for dissolution rate and efficiency. All the solid dispersions prepared gave rapid and higher dissolution of simvastatin when compared with pure drug. The DE60 was also increased from many folds in the case of pure drug and solid dispersions. Experimental design was applied systematically and determine the influence of the individual and combined effect on independent variables (X1) ratio and (X2) concentration of surfactants on the dependent variables percent dissolution efficiency at 60 min (%DE 60) and yield percent and optimized formulation selected and characterised by its UV, Differential scanning caloriemetery, Scanning electron microscopy and X- Diffraction studies and formulated into capsule dosage form. In conclusion, the result of this work to suggest that solid dispersion is a useful technique for enhancing the solubility and dissolution study of water insoluble drug. Keywords: Solubility enhancement, Poorly water soluble drug, Simvastatin, Solid dispersions
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
DEVELOPMENT AND IN VITRO EVALUATION OF AN ORAL FLOATING TABLET OF
METRONIDAZOLE
- Authors: Harshal Soni, Chetan Ghulaxe, Surbhi Upadhyay, Sujit Pillai
  Abstract: The present study was undertaken with an aim to develop and evaluate gastroretentive floating tablets of Metronidazole that are designed to retain in the stomach for a long time and have developed as a drug delivery system for better eradication of Helicobacter Pylori in peptic ulcer diseases. The floating tablets of Metronidazole were made by direct compression method using polymer Carbopol 934 and sodium bicarbonate and citric acid as gas generating agent. The tablets were evaluated by pre and post compression parameters such as weight variation, thickness, friability, hardness, drug content, in- vitro buoyancy studies and in-vitro dissolution studies and results were within the limits. Hardness was found to be in the range of 7.6 ± 0.27 kg/ cm² to 7.9 ± 0.35 kg/cm², the percent friability was in the range of 0.48% to 0.52% w/w and the tablets showed 94% to 97% uniformity in drug content. The in-vitro dissolution studies were carried out in a USP type- II apparatus in 0.1N HCl. The formulations were able to within 2-7 minutes and showed buoyancy >12 hrs. The drug-polymer ratio, viscosity grades of Carbopol 934 and gas generating agents were found to influence the release of drug and floating characteristics from the prepared floating drug delivery system of Metronidazole. Kinetically, among the 4 assessed models the release pattern of Metronidazole from the tablets fitted best to Higuchi’s and zero order indicated that diffusion is the predominant mechanism controlling the drug release. Keywords: Metronidazole, Floating tablets, Carbopol 934, Gastroretentive, Dissolution
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
HYPOGLYCEMIC EFFECT OF POLYHERBAL FORMULATIONS IN ALLOXAN INDUCED DIABETIC
MICE
- Authors: Noopur Srivastava, Awani K. Rai
  Abstract: Objective: The present work was executed to evaluate the antidiabetic potency of herbal preparation which was the combination of wheat germ oil, fresh juice of Coriander sativum and Aloe vera gel in normal and alloxan-induced diabetic mice. Methods: The serum glucose lowering activity of the herbal preparation (PH-1 in the ratio of 1:1:1of wheat germ oil, fresh juice of C.sativum and Aloe vera) was studied in normal rats after oral administration at 1.0 and 2.0ml/kg and herbal preparation (PH-1, PH-2 wheat germ oil, fresh juice of coriander sativum and Aloe vera gel in ratio of 2:2:1) and PH-3 (wheat germ oil, fresh juice of coriander sativum and Aloe vera gel in ratio of 1:2:2) on alloxan induced diabetic swiss albino mice, at doses of 1.0 and 2.0 ml/kg. Blood samples were collected and analyzed for serum glucose at 0,1/2, 1, 2, 4, 8, 12 and 24 h in normal mice and at 0, 1, 3, 7, 15 and 30 days in diabetic mice after drug administration by glucose oxidase/peroxidase method. The data were compared statistically by using one way ANOVA method followed by Dunnett multiple component test. Statical significance was set at p<0.05. Results: The herbal preparation (1.0 and 2.0 ml/kg) produced significant (p<0.05) reduction in serum glucose level of both normal and diabetic mice and comparable with that of control and standard drug Glibenclamide. Conclusion: The herbal preparation showed significant glucose lowering effect in normal and alloxan induced diabetic rats. This preparation is giving to be a promising antidiabetic preparation for masses and however, it requires further extensive studies in human beings. Keywords: Antidiabetic potency, alloxan-induced diabetic rats, Aloe vera
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
DESIGN AND CHARACTERIZATION OF SUSTAINED RELEASE MATRIX TABLETS OF
METFORMIN HYDROCHLORIDE USING COMBINATION OF HYDROPHILIC POLYMERS
- Authors: Anjita Singh, Devendra Singh Rajput, Awankar Akshay Gopalrao, Deepak Chauhaan, Rajmani Mafidar, Mithun Bhowmick, Jagdish Rathi, Rahul Mathur
  Abstract: Sustained release system is types of modified drug delivery system that can be used as an alternative to conventional system. Among different dosage forms, matrix tablets are widely accepted for oral sustained release Metformin hydrochloride has relatively short plasma half-life, low absolute bioavailability. The need for the administration two to three times a day when larger doses are required can decrease patient compliance. Sustained release formulation that would maintain plasma level for 8-12 h might be sufficient for daily dosing of metformin. Sustained release products are needed for metformin to prolong its duration of action and to improve patient compliances. They are capable of reducing the dose intake, minimize the blood level oscillation dose related adverse effect and cost thus improves the patient compliance in the therapeutic management of diabetes. The Metformin hydrochloride matrix Sustained release tablets were prepared using different hydrophilic polymers in various proportions as release retarding agent to prolong the drug release and to improve the patience compliance. The tablets were evaluated for various tests like hardness, friability, disintegration and in-vitro dissolution studies. Keywords: Matrix Tablets, Metformin hydrochloride, Hardness, Friability, Disintegration and in-vitro dissolution studies
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
FORMULATION AND DEVELOPMENT OF SUSTAINED RELEASE MATRIX TABLETS OF
LORNOXICAM
- Authors: Rahul Pagar, D M PATIL, P A PAWAR, R S GHULE, V A BAIRAGI
  Abstract: Lornoxicam is a NSAID having oxicam class mainly prescribed in the treatment of osteoarthritis and rheumatoid arthritis. NSAID have the potential to relieve the pain and inflammation without the immunosuppressive and metabolic side effects associated with corticosteroids. Generally the classification of NSAID is applied to drugs that inhibit one or more steps in the metabolism of Arachidonic Acid (AA). In general, NSAID do not inhibit lipoxygenase formation or the formation of other inflammatory mediators. Due to its more biological half-life i.e. 3-5 hrs. in India, the dosage form is available in 8-16 mg, it can be increased upto 24 mg/day if necessary. The main objectives of present investigation are to confirm the drug by various analytical techniques, to study the drug excipients compatibility, to avoid the dose as well as the frequency of the dosage form and to perform the stability. The tablet can be developed with the combination of HPMC K 100M and Ethyl Cellulose as a matrix former. Lornoxicam is NSAID that has numerous functions in the body. It can be absorbed rapidly and completely from gastrointestinal track after the oral administration. Absolute bioavailability of Lornoxicam is 90-100%. No first pass effect is observed. It is found in the plasma in the unchanged form and as its hydroxylated metabolite. The hydroxylated metabolite exhibits no pharmacological activity. CYP2C3 has been shown to be the primary enzyme responsible for the biotransformation of Lornoxicam. Approximately 2/3 part of Lornoxicam is eliminated via the liver and 1/3 via the kidneys as inactive substance. Lornoxicam inhibits the production of prostaglandins by inhibiting the action of cyclooxygenase, which regulates the conversion of Arachidonic Acid to Prostaglandins. Lornoxicam mainly prescribed in the treatment of osteoarthritis and rheumatoid arthritis, and also in the management of ankylosing spondylitis, acute sciatica and low back pain.Keywords: Lornoxicam, Sustained release, matrix.
  
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
FORMULATION AND EVALUATION OF SUBLINGUAL TABLET CONTAINING ANTIEMETIC DRUG
- Authors: Sheetal Sem, Avinash Sharma, Ashish Gupta, G N Darwhekar
  Abstract: The aim of the present research is to formulate a sublingual tablet of antiemetic drug. Doxylamine succinate is an antihistaminic commonly used for the prevention and treatment of nausea and vomiting. Oral bioavailability of doxylamine succinate is low and shows extensive hepatic metabolism. The Objective of the present research is to formulate doxylamine succinate sublingual tablet to avoid hepatic first-pass metabolism and to improve its bioavailability. Sublingual route not only overcome the problem of dysphagia but also giving the rapid onset of action by enhancing permeability through site of administration Keywords: Sublingual tablet, Doxylamine succinate, Antiemetic, Dysphagia, Bioavailability
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
THE EFFECT OF A NOVEL HYDROPHILIC BIOPOLYMER DERIVED FROM IPOMOEA BATATAS
TUBER AS A GRANULATING AGENT IN PARACETAMOL TABLET FORMULATION
- Authors: Kenneth Chinedu Ugoeze, Nkemakolam Nwachukwu
  Abstract: A novel hydrophilic biopolymer, I-polygel (IP) derived from the tubers of Ipomoea batatas was evaluated as a granulating agent at 2.50-5.50 % w/w in paracetamol tablets. Its compatibility with paracetamol was investigated using differential scanning calorimetry (DSC). The micromeritic properties of the granules prepared by wet granulation method were considered. They were compressed into tablets with a 12.5 mm flat-faced punch‎ fitted in a single punch tabletting machine. The weight uniformity, mechanical properties, disintegration time, dissolution profile, dissolution efficiency (DE) and the organoleptic properties of the tablets were studied. Gelatin (GT) was employed as a standard granulating agent. From the results, DSC thermograms showed that paracetamol was compatible with IP. Flowability and compressibility of the granules generally improved with increasing concentrations of the granulating agents with GT yielding better results (p > 0.05). The uniformity of weight of all the batches of tablets exhibited a variation in tablet weight ranging between 0.37 – 0.87 %. A consistent increase in the mechanical properties of the tablets along the line of increasing concentrations of IP or GT with a corresponding decrease in friability was recorded, with GT indicating better outcomes at each concentration (p<0.05). The batches of tablets containing IP disintegrated within 3.76 -7.62 min whereas those of GT disintegrated between 10.89-20.92 min. All the batches of tablets containing IP and only 2.5 % w/w GT released up to 80 % of paracetamol within 30 min. The highest values of DE of 71.32- 74.17 % was obtained within 2.50-4.0 % w/w of IP only (p<0.05). Tablets with acceptable mechanical strength were obtained with either IP or GT, but lower disintegration time (<<< 15.00 min) and highest DEs of tablets were obtainable only with IP at the concentrations of 2.50-4.00 % w/w, showing that IP was better than GT as a granulating agent. Keywords: Hydrophilic biopolymer, I-polygel, Ipomoea batatas, granulating agent, paracetamol, tablet.
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
PREPARATION, CHARACTERIZATION AND EVALUATION OF NEBIVOLOL LOADED CHITOSAN
NANOPARTICLES
- Authors: Mayank Sharma, Rajesh Sharma, Dinesh Kumar Jain
  Abstract: Nebivolol (NEB) is an antihypertensive drug with poor oral bioavailability (12%) in humans due to extensive first pass hepatic metabolism. Present work is an attempt to improve oral bioavailability of nebivolol by incorporating it with biodegradable polymer chitosan and preparing its nanoparticles. The results indicated stable nanoperticles with the value of ZP to be +36.4 mV ± 2 mV, the small particle size of 79.23 ± 45 nm and high entrapment efficiency of 72.56%. The in vitro release study revealed sustained release of drug for 72 h with 71.24% cumulative drug release. The promising results from the study revealed the applicability of chitosan in the formulation of NEB loaded CNPs.
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
MULTIDRUG RESISTANT TUBERCULOSIS IN CHILDREN IN THE DEMOCRATIC REPUBLIC OF
CONGO: FIRST EXPERIENCE WITH A SHORT TREATMENT COURSE IN A UNIVERSITY
HOSPITAL
- Authors: Aketi Loukia, Shiku Diayisu Joseph, Bakoko Brian, Anshambi Nicole, Kashongwe Zacharie
  Abstract: Background: A short treatment course for multidrug-resistant tuberculosis (MR-TB) is not yet well codified in children in the Democratic Republic of Congo (DRC). The objective of this study was to evaluate a short MR-TB treatment course in children. Methods: A prospective study was performed from April 2015 (corresponding to the inclusion) through April 2017 (and the later initiation time point was April 2016) in the University Clinics of Kinshasa. Enrolled children were aged 0 to 15 years. The treatment duration was in general for 9 months, with 4 months of intensive phase treatment with Kanamycin, Levofloxacin, Isoniazid, Pyrazinamide, Prothionamide, Clofazimine and Ethambutol, and 5 months of continuous phase treatment with Levofloxacin, Pyrazinamide, Clofazimine and Ethambutol. Frequencies were reported for significant results. Results: A total of 21 children had MDR-TB (11 males and 10 females). Fifteen (71.43%) were bacteriological confirmed cases (by Xpert/MTB), and 6 (28.57%) were clinically diagnosed (MDR-TB contact with suggestive radiologic lesions); 2 patients were coinfected with HIV, 15 cases had pulmonary TB, and 6 had extrapulmonary TB. The main radiologic findings included TB cavity (3 cases), pleural effusion (5 cases), alveolar syndrome (8 cases), adenopathy (7 cases), and interstitial infiltration, fibrosis and miliary (2 cases each). The Ziehl control was negative before 4 months of treatment in the majority of the cases. Overall, 11 patients were cured, 7 completed the treatment, 2 died and 1 was lost to follow up. Conclusions: MDR-TB remains a challenge in children. A more comfortable, short treatment course is feasible in children in the DRC. It is necessary to verify this observation with a larger cohort of MDR-TB patients in pediatrics. Keywords: Multidrug-resistant tuberculosis; children; short treatment course; Africa; Kinshasa; treatment outcomes.
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
Synthesis and antihyperlipidemic activity of Dibenz[c,e]azepine-5,7-dione
derivatives in Triton WR-1339-induced hyperlipidemic rats
- Authors: Minakshi Verma, Ashish Kumar Gupta, Ravindra Nath Thakur
  Abstract: The structural requirements for decreasing cholesterol and triglyceride levels remain largely uninvestigated. Thus a systematic investigation of certain N-substituted dibenz[c,e]azepines is necessary. Nine compounds of N-substituted derivatives of Dibenz[c,e]azepine-5,7-Dione were synthesized and they were tested for antihyperlipidemic activity. Compounds synthesized (C-1, C-3, C-4 and C-5) significantly lowered the serum total cholesterol, triglyceride and LDL (low density lipoprotein) levels and also improved the HDL (high density lipoprotein) level in Triton-WR 1339 induced hyperlipidemic rats. Keywords: antihyperlipidemic activity, lipids in plasma, high density lipoprotein
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)
PREPARATION, CHARACTERIZATION, AND OPTIMIZATION OF MICROEMULSION FOR
TOPICAL DELIVERY OF ITRACONAZOLE
- Authors: TEJAS B PATEL, Tushar R Patel, B N Suhagia
  Abstract: Microemulsions (ME) have been proved to increase the cutaneous absorption of both lipophilic and hydrophilic medicaments when compared to conventional vehicles (emulsions, pure oils, aqueous solutions). Hence the aim of present investigation is to prepare, characterize and optimize microemulsion of Itraconazole (ITZ). Itraconazole is an anti fungal agent, most widely used in the ringworm infection. It is classified as class III drug as per BCS classification. It indicates lower permeability through skin. Therefore objective of the research is to improve permeability of Itraconazole through skin. Microemulsion was prepared using eucalyptus oil, tween 20 and methanol as oil phase, surfactant and co-surfactant respectively. Pseudo ternary phase diagrams were constructed to find out optimum ratio of oil: Smix (surfactant: Co-Surfactant): water. A 32 full factorial design was applied for the optimization of prepared microemulsion. Microemulsion was evaluated for globule size, zeta potential, in-vitro diffusion study etc. Results of globule size measurements and zeta potential indicated ME7 had high stability then other formulation of microemulsion. For the optimization transdermal flux and %Q6 was selected as dependant variables. Results of optimization study also revealed ME 7 as optimized microemulsion for high permeability to the skin. Further ME7 was compared to marketed Itraconazole preparation (ITASPORE) and evaluated using similarity factor F2. Results of F2 value was not near to 100 indicated there is no similarity in diffusion profiles of ME7 and ITASPORE. Hence, indirectly it suggest there was increased in permeability of drug by preparing microemulsion.
  PubDate: 2018-03-14
  Issue No: Vol. 8 (2018)