Formulation and in vitro Evaluation of Sustained Release Matrix Tablets of Levetiracetam for Better Epileptic Treatment

The objective of the present study was to develop sustained release oral matrix tablets of anti epileptic drug levetiracetam. The sustained release matrix tablets of levetiracetam were prepared using hydrophilic matrix hydroxypropyl methylcellulose (HPMC) as a release retarding polymer by wet granulation method. Prior to compression, FTIR studies were performed to understand the compatibility between the drug and excipients. The study revealed that there was no chemical interaction between drug and excipients used in the study. The tablets were characterized by physical and chemical parameters and results were found in acceptable limits. In vitro release study was carried out for the tablets using 0.1 N HCl for 2 hours and in phosphate buffer pH 7.4 for remaining time up to 12 hours. The effect of polymer concentration was studied. Different dissolution models were applied to drug release data in order to evaluate release mechanisms and kinetics. The drug release data fit well to zero order kinetics. Drug release mechanism was found as a complex mixture of diffusion, swelling and erosion.

Antiangiogenic Potential of Phellodendron amurense Bark Extract Observed on Chorioallantoic Membrane

Angiogenesis, a formation of new blood vessels from a pre-existing vasculature, plays an important role in pathologic processes such as the growth and metastasis of tumours. Tumours cannot grow beyond a few millimetres without blood supply from the newly formed blood vessels from the host tissue, a process called tumour-induced angiogenesis. The successful research of antiangiogenic treatment of cancer has focused on nutraceuticals with angiogenesis-modulating properties. Berberine, as a major active component of the bark of Phellodendron amurense Rupr., has shown antitumour activity by intervening into different steps of carcinogenesis. The influence of ethanolic extract of Phellodendron amurese bark on the angiogenesis was tested in vivo on chick chorioallantoic membrane (CAM). The irritancy of the CAM after the application of the crude bark extract dissolved in normal saline (10 mg/mL) was investigated on embryonic day 7. No significant signs of the irritancy, such as vasoconstriction, hyperaemia, haemorrhage or coagulation were observed which indicates the harmless character of the extract. A significant reduction in vessel sprouting and higher percentage of avascular zone was observed in the case of CAM treated with the extract in comparison with non-treated CAM (control), which is a proof of the antiangiogenic potential of the extract. These results could contribute to the development of novel drugs for the treatment of cancer or other diseases, in which angiogenesis plays a significant role.

Solid Dispersions of Cefixime Using β-Cyclodextrin: Characterization and in vitro Evaluation

Cefixime, a BCS class II drug, is insoluble in water but freely soluble in acetone and in alcohol. The aqueous solubility of cefixime in water is poor and exhibits exceptionally slow and intrinsic dissolution rate. In the present study, cefixime and β-Cyclodextrin (β-CD) solid dispersions were prepared with a view to study the effect and influence of β-CD on the solubility and dissolution rate of this poorly aqueous soluble drug. Phase solubility profile revealed that the solubility of cefixime was increased in the presence of β-CD and was classified as AL-type. Effect of variable, such as drug:carrier ratio, was studied. Physical characterization of the solid dispersion was characterized by Fourier transform infrared spectroscopy (FT-IR) and Differential scanning calorimetry (DSC). These studies revealed that a distinct loss of drug crystallinity in the solid molecular dispersions is ostensibly accounting for enhancement of dissolution rate in distilled water. The drug release from the prepared solid dispersion exhibited a first order kinetics. Solid dispersions of cefixime showed a 6.77 times fold increase in dissolution rate over the pure drug.

Adverse Drug Reactions Monitoring in the Northern Region of Zambia

The Copperbelt University Health Services (CBUHS) was designated by the Zambia Medicines Regulatory Authority (ZAMRA), formally the Pharmaceutical Regulatory Authority (PRA) as a regional pharmacovigilance centre to carryout activities of drug safety monitoring in four provinces in Zambia. CBUHS’s mandate included stimulating the reporting of adverse drug reactions (ADRs), as well as collecting and collating ADR reports from health institutions in the four provinces. This report covers the researchers’ experiences from May 2008 to September, 2016. The main objectives are 1) to monitor ADRs in the Zambian population, 2) to disseminate information to all health professionals in the region advising that the CBU health was a centre for reporting ADRs in the region, 3) to monitor polypharmacy as well as the benefit-risk profile of medicines, 4) to generate independent, evidence based recommendations on the safety of medicines, 5) to support ZAMRA in formulating safety related regulatory decisions for medicines, and 6) to communicate findings with all key stakeholders. The methodology involved monthly visits, beginning in early May 2008 to September, 2016, by the CBUHS to health institutions in the programme areas. Activities included holding discussions with health workers, distribution of ADR forms and collection of ADRs reports. These reports, once collected, were documented and assessed at the CBUHS. A report was then prepared for ZAMRA on quarterly basis. At ZAMRA, serious ADRs were noted and recommendations made to the Ministry of Health of the Republic of Zambia. The results show that 2,600 ADRs reports were received at the pharmacovigilance regional centre. Most of the ADRs reports that received were due to antiretroviral drugs, as well as a few from anti-malarial drugs like Artemether/Lumefantrine – Coartem®. Three hundred and twelve ADRs were entered in the Uppsala Monitoring Centre WHO Vigiflow for further analysis. It was concluded that in general, 2008-16 were exciting years for the pharmacovigilance group at CBUHS. From a very tentative beginning, a lot of strides were made and contacts established with healthcare facilities in the region. The researchers were encouraged by the support received from the Copperbelt University management, the motivation provided by ZAMRA and most importantly the enthusiasm of health workers in all the health care facilities visited. As a centre for drug safety in Zambia, the results show it achieves its objectives for monitoring ADRs, Pharmacovigilance (drug safety monitoring), and activities of monitoring ADRs as well as preventing them. However, the centre faces critical challenges caused by erratic funding that prevents the smooth running of the programme.

In vivo Therapeutic Potential of Biologically Synthesized Silver Nanoparticles

Nowadays, nanoparticles are being used in pharmacological studies for their exclusive properties such as small size, more surface area, biocompatibility and enhanced solubility. In view of this, the present study aimed to evaluate the antihyperglycemic potential of biologically synthesized silver nanoparticles (BSSNPs) and Gymnema sylvestre (GS) extract. The SEM and SEM analysis divulges that the BSSNPs were spherical in shape. EDAX spectrum exhibits peaks for the presence of silver, carbon, and oxygen atoms in the range of 1.0-3.1 keV. FT-IR reveals the binding properties of active bio-constituents responsible for capping and stabilizing BSSNPs. The results showed increased blood glucose, huge loss in body weight and downturn in plasma insulin. The GS extract (200 mg/kg, 400 mg/kg), BSSNPs (100 mg/kg, 200 mg/kg) and metformin 50 mg/kg were administered to the diabetic rats. BSSNPs at a dose level of 200 mg/kg (b.wt.p.o.) showed significant inhibition of (p

Adverse Reactions from Contrast Media in Patients Undergone Computed Tomography at the Department of Radiology, Srinagarind Hospital

Background: The incidence of adverse reactions to iodinated contrast media has risen. The dearth of reports on reactions to the administration of iso- and low-osmolar contrast media should be addressed. We, therefore, studied the profile of adverse reactions to iodinated contrast media; viz., (a) the body systems affected (b) causality, (c) severity, and (d) preventability. Objective: To study adverse reactions (causes and severity) to iodinated contrast media at Srinagarind Hospital. Method: Between March and July, 2015, 1,101 patients from the Department of Radiology were observed and interviewed for the occurrence of adverse reactions. The patients were classified per Naranjo’s algorithm and through use of an adverse reactions questionnaire. Results: A total of 105 cases (9.5%) reported adverse reactions (57% male; 43% female); among whom 2% were iso-osmolar vs. 98% low-osmolar. Diagnoses included hepatoma and cholangiocarcinoma (24.8%), colorectal cancer (9.5%), breast cancer (5.7%), cervical cancer (3.8%), lung cancer (2.9%), bone cancer (1.9%), and others (51.5%). Underlying diseases included hypertension and diabetes mellitus type 2. Mild, moderate, and severe adverse reactions accounted for 92, 5 and 3%, respectively. The respective groups of escalating symptoms included (a) mild urticaria, itching, rash, nausea, vomiting, dizziness, and headache; (b) moderate hypertension, hypotension, dyspnea, tachycardia and bronchospasm; and (c) severe laryngeal edema, profound hypotension, and convulsions. All reactions could be anticipated per Naranjo’s algorithm. Conclusion: Mild to moderate adverse reactions to low-osmolar contrast media were most common and these occurred immediately after administration. For patient safety and better outcomes, improving the identification of patients likely to have an adverse reaction is essential.

Patient Support Program in Pharmacovigilance: Foster Patient Confidence and Compliance

The pharmaceutical companies are getting more inclined towards patient support programs (PSPs) which assist patients and/or healthcare professionals (HCPs) in more desirable disease management and cost-effective treatment. The utmost objective of these programs is patient care. The PSPs may include financial assistance to patients, medicine compliance programs, access to HCPs via phone or online chat centers, etc. The PSP has a crucial role in terms of customer acquisition and retention strategies. During the conduct of these programs, Marketing Authorisation Holder (MAH) may receive information related to concerned medicinal products, which is usually reported by patients or involved HCPs. This information may include suspected adverse reaction(s) during/after administration of medicinal products. Hence, the MAH should design PSP to comply with regulatory reporting requirements and avoid non-compliance during PV inspection. The emergence of wireless health devices is lowering the burden on patients to manually incorporate safety data, and building a significant option for patients to observe major swings in reference to drug safety. Therefore, to enhance the adoption of these programs, MAH not only needs to aware patients about advantages of the program, but also recognizes the importance of time of patients and commitments made in a constructive manner. It is indispensable that strengthening the public health is considered as the topmost priority in such programs, and the MAH is compliant to Pharmacovigilance (PV) requirements along with regulatory obligations.

Screening for Larvicidal Activity of Aqueous and Ethanolic Extracts of Fourteen Selected Plants and Formulation of a Larvicide against Aedes aegypti (Linn.) and Aedes albopictus (Skuse) Larvae

This study aims to: a) obtain ethanolic (95% EtOH) and aqueous extracts of Selaginella elmeri, Christella dentata, Elatostema sinnatum, Curculigo capitulata, Euphorbia hirta, Murraya koenigii, Alpinia speciosa, Cymbopogon citratus, Eucalyptus globulus, Jatropha curcas, Psidium guajava, Gliricidia sepium, Ixora coccinea and Capsicum frutescens and screen them for larvicidal activities against Aedes aegypti (Linn.) and Aedes albopictus (Skuse) larvae; b) to fractionate the most active extract and determine the most active fraction; c) to determine the larvicidal properties of the most active extract and fraction against by computing their percentage mortality, LC50, and LC90 after 24 and 48 hours of exposure; and d) to determine the nature of the components of the active extracts and fractions using phytochemical screening. Ethanolic (95% EtOH) and aqueous extracts of the selected plants will be screened for potential larvicidal activity against Ae. aegypti and Ae. albopictus using standard procedures and 1% malathion and a Piper nigrum based ovicide-larvicide by the Department of Science and Technology as positive controls. The results were analyzed using One-Way ANOVA with Tukey’s and Dunnett’s test. The most active extract will be subjected to partial fractionation using normal-phase column chromatography, and the fractions subsequently screened to determine the most active fraction. The most active extract and fraction were subjected to dose-response assay and probit analysis to determine the LC50 and LC90 after 24 and 48 hours of exposure. The active extracts and fractions will be screened for phytochemical content. The ethanolic extracts of C. citratus, E. hirta, I. coccinea, G. sepium, M. koenigii, E globulus, J. curcas and C. frutescens exhibited significant larvicidal activity, with C. frutescens being the most active. After fractionation, the ethyl acetate fraction was found to be the most active. Phytochemical screening of the extracts revealed the presence of alkaloids, tannins, indoles and steroids. A formulation using talcum powder–300 mg fraction per 1 g talcum powder–was made and again tested for larvicidal activity. At 2 g/L, the formulation proved effective in killing all of the test larvae after 24 hours.

Effect of Natural Binder on Pang-Rum Hardness

The aim of this study is to improve Pang-Rum (PR) hardness by adding natural binders. PR is one of Thai tradition aroma products. In the past, it was used for aesthetic propose on face and body with good odor. Nowadays, PR is not popular and going to be disappeared. Five natural materials, i.e. agar, rice flour, glutinous flour, corn starch, and tapioca starch were selected to use as binders. Binders were dissolved with boiled water into concentration 5% and 10% w/w except agar that was prepared 0.5% and 1% w/w. PR with and without binder were formulated. Physical properties, i.e. weight, shape, color, and hardness were evaluated. PR with 10% of corn starch solution had suitable hardness (14.2±0.9 kg) and the best appearance. In the future, it would be planned to study about odor and physical stability for decorated product development.

Evaluation of Thrombolytic Activity of Zingiber cassumunar Roxb. and Thai Herbal Prasaplai Formula

The propose of this study was to investigate in vitro thrombolytic activity of Zingiber cassumunar Roxb. and Prasaplai, a Thai herbal formulation of Z. cassumunar Roxb. Herbs were extracted with boiling water and concentrated by lyophilization. To observe their thrombolytic potential, an in vitro clot lysis method was applied where streptokinase and sterile distilled water were used as positive and negative controls, respectively. Crude aqueous extracts from Z. cassumunar Roxb. and Prasaplai formula showed significant thrombolytic activity by clot lysis of 17.90% and 25.21%, respectively, compared to the negative control water (5.16%) while the standard streptokinase revealed 64.78% clot lysis. These findings suggest that Z. cassumunar Roxb. exhibits moderate thrombolytic activity and cloud play an important role in the thrombolytic properties of Prasaplai formula. However, further study should be done to observe in vivo clot dissolving potential and to isolate active component(s) of these extracts.

Preparation of Polymer-Stabilized Magnetic Iron Oxide as Selective Drug Nanocarriers to Human Acute Myeloid Leukemia

Drug delivery to target human acute myeloid leukemia (AML) using a nanoparticulate chemotherapeutic formulation that can deliver drugs selectively to AML cancer is hugely needed. In this work, we report the development of a nanoformulation made of polymeric-stabilized multifunctional magnetic iron oxide nanoparticles (PMNP) loaded with the anticancer drug Doxorubicin (Dox) as a promising drug carrier to treat AML. Dox@PMNP conjugates simultaneously exhibited high drug content, maximized fluorescence, and excellent release properties. Nanoparticulate uptake and cell death following addition of Dox@PMNPs were then evaluated in different types of human AML target cells, as well as on normal human cells. While the unloaded MNPs were not toxic to any of the cells, Dox@PMNPs were found to be highly toxic to the different AML cell lines, albeit at different inhibitory concentrations (IC50 values), but showed very little toxicity towards the normal cells. In comparison, free Dox showed significant potency concurrently to all the cell lines, suggesting huge potentials for the use of Dox@PMNPs as selective AML anticancer cargos. Live confocal imaging, fluorescence and electron microscopy confirmed that Dox is indeed delivered to the nucleus in relatively short periods of time, causing apoptotic cell death. Importantly, this targeted payload may potentially enhance the effectiveness of the drug in AML patients and may further allow physicians to image leukemic cells exposed to Dox@PMNPs using MRI.

Antibacterial Effect of Silver Diamine Fluoride Incorporated in Fissure Sealants

Introduction: The application of fissure sealants is considered to be an important primary prevention method used in dental medicine. However, the formation of microleakage gaps between tooth enamel and the fissure sealant applied is one of the most common reasons of dental caries development in teeth with fissure sealants. The association between various dental biomaterials may limit the major disadvantages and limitations of biomaterials functioning in a complementary manner. The present study consists in the incorporation of a cariostatic agent – silver diamine fluoride (SDF) – in a resin-based fissure sealant followed by the study of release kinetics by spectrophotometry analysis of the association between both biomaterials and assessment of the inhibitory effect on the growth of the reference bacterial strain Streptococcus mutans (S. mutans) in an in vitro study. Materials and Methods: An experimental in vitro study was designed consisting in the entrapment of SDF (Cariestop® 12% and 30%) into a commercially available fissure sealant (Fissurit®), by photopolymerization and photocrosslinking. The same sealant, without SDF was used as a negative control. The effect of the sealants on the growth of S. mutans was determined by the presence of bacterial inhibitory halos in the cultures at the end of the incubation period. In order to confirm the absence of bacteria in the surface of the materials, Scanning Electron Microscopy (SEM) characterization was performed. Also, to analyze the release profile of SDF along time, spectrophotometry technique was applied. Results: The obtained results indicate that the association of SDF to a resin-based fissure sealant may be able to increase the inhibition of S. mutans growth. However, no SDF release was noticed during the in vitro release studies and no statistical significant difference was verified when comparing the inhibitory halo sizes obtained for test and control group.  Conclusions: In this study, the entrapment of SDF in the resin-based fissure sealant did not potentiate the antibacterial effect of the fissure sealant or avoid the immediate development of dental caries. The development of more laboratorial research and, afterwards, long-term clinical data are necessary in order to verify if this association between these biomaterials is effective and can be considered for being used in oral health management. Also, other methodologies for associating cariostatic agents and sealant should be addressed.

Comparison of Statins Dose Intensity on HbA1c Control in Outpatients with Type 2 Diabetes: A Prospective Cohort Study

The effect of statins dose intensity (SDI) on glycemic control in patients with existing diabetes is unclear. Also, there are many contradictory findings were reported in the literature; thus, it is limiting the possibility to draw conclusions. This project was designed to compare the effect of SDI on glycated hemoglobin (HbA1c%) control in outpatients with Type 2 diabetes in the endocrine clinic at Hospital Pulau Pinang, Malaysia, between July 2015 and August 2016. A prospective cohort study was conducted, where records of 345 patients with Type 2 diabetes (Moderate-SDI group 289 patients and high-SDI cohort 56 patients) were reviewed to identify demographics and laboratory tests. The target of glycemic control (HbA1c < 7% for patient < 65 years, and < 8% for patient ≥ 65 years) was estimated, and the results were presented as descriptive statistics. From 289 moderate-SDI cohorts with a mean age of 57.3 ± 12.4 years, only 86 (29.8%) cases were shown to have controlled glycemia, while there were 203 (70.2%) cases with uncontrolled glycemia with confidence interval (CI) of 95% (6.2–10.8). On the other hand, the high-SDI group of 56 patients with Type 2 diabetes with a mean age 57.7±12.4 years is distributed among 11 (19.6%) patients with controlled diabetes, and 45 (80.4%) of them had uncontrolled glycemia, CI: 95% (7.1–11.9). The study has demonstrated that the relative risk (RR) of uncontrolled glycemia in patients with Type 2 diabetes that used high-SDI is 1.15, and the excessive relative risk (ERR) is 15%. The absolute risk (AR) is 10.2%, and the number needed to harm (NNH) is 10. Outpatients with Type 2 diabetes who use high-SDI of statin have a higher risk of uncontrolled glycemia than outpatients who had been treated with a moderate-SDI.

Evaluation of South African Plants with Acaricide Activity against Ticks

Acaricides are commonly used to control ticks but are toxic, harmful to the environment and too expensive to resource-limited farmers. Traditionally, many communities in South Africa rely on a wide range of indigenous practices to keep their livestock healthy. One of these health care practices includes the use of medicinal plants and this offers an alternative to conventional medicine. An investigation was conducted at the CSIR in South Africa, and selected indigenous plants used in communities were scientifically evaluated for the management of ticks in animals. 17 plants were selected from 239 plants used traditionally in South Africa. Two different organic extracts were prepared from the 17 samples, resulting in 34 plant samples. These were tested for efficacy against two tick species, namely Rhipicephalus microplus and Rhipicephalus turanicus. The plant extracts were also screened against Vero cells and most were found to have low cytotoxicity. This study has shown that there is potential for the development of botanicals as natural acaricides against ticks that are non-toxic and environmentally benign.

Cytotoxic Effect of Crude Extract of Sea Pen Virgularia gustaviana on HeLa and MDA-MB-231 Cancer Cell Lines

Marine organisms such as soft coral, sponge, ascidians, and tunicate containing rich source of natural compound have been studied in last decades because of their special chemical compounds with anticancer properties. The aim of this study was to investigate anti-cancer property of ethyl acetate extracted from marine sea pen Virgularia gustaviana found from Persian Gulf coastal (Bandar Abbas). The extraction processes were carried out with ethyl acetate for five days. Thin layer chromatography (TLC) and high-performance liquid chromatography (HPLC) were used for qualitative identification of crude extract. The viability of HeLa and MDA-Mb-231 cancer cells was investigated using MTT assay at the concentration of 25, 50, and a 100 µl/ml of ethyl acetate is extracted. The crude extract of Virgularia gustaviana demonstrated ten fractions with different Retention factor (Rf) by TLC and Retention time (Rt) evaluated by HPLC. The crude extract dose-dependently decreased cancer cell viability compared to control group. According to the results, the ethyl acetate extracted from Virgularia gustaviana inhibits the growth of cancer cells, an effect which needs to be further investigated in the future studies.

Ethnobotanical Study on the Usage of Toxic Plants in Traditional Medicine in the City Center of Tlemcen, Algeria

Traditional medicine has been part of the Algerian culture for decades. In particular, the city of Tlemcen still retains practices based on phytotherapy to the present day, as this kind of medicine fulfills the needs of its followers among the local population. The toxic plants contain diverse natural substances which supplied a lot of medicine in the pharmaceutical industry. In order to explore new medicinal sources among toxic plants, an ethnobotanical study was carried out on the use of these plants by the population, at Emir Abdelkader Square of the city of Tlemcen, a rather busy place with a high number of traditional health practitioners and herbalists. This is a descriptive and transversal study aimed at estimating the frequency of using toxic plants among the studied population, for a period of 4 months. The information was collected, using self-anonymous questionnaires, and analyzed by the IBM SPSS Statistics software used for statistical analysis. A sample of 200 people, including 120 women and 80 men, were interviewed. The mean age was 41 ± 16 years. Among those questioned, 83.5% used plants; 8% of them used toxic plants and 35% used plants that can be toxic under certain conditions. Some improvements were observed in 88% of the cases where toxic plants were used. 80 medicinal plants, belonging to 36 botanical families, were listed, identified and classified. The most frequent indications for these plants were for respiratory diseases in 64.7% of cases, and for digestive disorders in 51.5% of cases. 11% of these plants are toxic, 26% could be toxic under certain conditions. Among toxics plants, the most common ones are Berberis vulgaris with 5.4%, indicated in the treatment of uterine fibroids and thyroid, Rhamnus alaternus with 4.8% for hepatic jaundice, Nerium oleander with 3% for hemorrhoids, Ruta chalepensis with 1.2%, indicated for digestive disorders and dysmenorrhea, and Viscum album with 1.2%, indicated for respiratory diseases. The most common plants that could be toxic are Mentha pulegium (15.6%), Eucalyptus globulus (11.4%), and Pimpinella anisum (10.2%). This study revealed interesting results on the use of toxic plants, which are likely to serve as a basis for further ethno-pharmacological investigations in order to get new drug sources.

Antifungal Activity of Medicinal Plants Used Traditionally for the Treatment of Fungal Infections and Related Ailments in South Africa

The current study investigates the antifungal properties of crude plant extracts from selected medicinal plant species. Eight plant species used by the traditional healers and local people to treat fungal infections were selected for further phytochemical analysis and biological assay. The selected plant species were extracted with solvent of various polarities such as acetone, methanol, ethanol, hexane, dichloromethane, ethyl acetate and water. Leaf, roots and bark extracts of Maerua juncea Pax, Albuca seineri (Engl & K. Krause) J.C Manning & Goldblatt, Senna italica Mill., Elephantorrhiza elephantina (Burch.) Skeels, Indigofera circinata Benth., Schinus molle L., Asparagus buchananii Bak., were screened for antifungal activity against three animal fungal pathogens (Candida albicans, Aspergillus fumigatus and Cryptococcus neoformans). All plant extracts were active against the tested microorganisms. Acetone, dichloromethane, hexane and ethanol extracts of Senna italica and Elephantorrhiza elephantine had excellent activity against Candida albicans and A. fumigatus with the lowest MIC value of 0.02 mg/ml. Bioautography assay was used to determine the number of antifungal compounds presence in the plant extracts. No active compounds were observed in plant extracts of Indigofera circinnata, Schinus molle and Pentarrhinum insipidum with good antifungal activity against C. albicans and A. fumigatus indicating possible synergism between separated metabolites.

Formulation and Evaluation of Dispersible Tablet of Furosemide for Pediatric Use

The objective of this work is to formulate a dry dispersible form of furosemide in the context of pediatric dose adjustment. To achieve this, we have produced a set of formulas that will be tested in process and after compression. The formula with the best results will be improved to optimize the final shape of the product. Furosemide is the most widely used pediatric diuretic because of its low toxicity. The manufacturing process was chosen taking into account all the data relating to the active ingredient and the excipients used and complying with the specifications and requirements of dispersible tablets. The process used to prepare these tablets was wet granulation. Different excipients were used: lactose, maize starch, magnesium stearate and two superdisintegrants. The mode of incorporation of super-disintegrant changes with each formula. The use of super-disintegrant in the formula allowed optimization of the disintegration time. Prepared tablets were evaluated for weight, content uniformity, hardness, disintegration time, friability and in vitro dissolution test. 

Synthesis, Physicochemical Characterization and Study of the Antimicrobial Activity of Chlorobutanol

Introduction and objectives: Chlorobutanol is a raw material, mainly used as an antiseptic and antimicrobial preservative in injectable and ophthalmic preparations. The main objective of our study was the synthesis and evaluation of the antimicrobial activity of chlorobutanol hemihydrates. Material and methods: Chlorobutanol was synthesized according to the nucleophilic addition reaction of chloroform to acetone, identified by an infrared absorption using Spectrum One FTIR spectrometer, melting point, Scanning electron microscopy and colorimetric reactions. The dosage of Carvedilol active substance was carried out by assaying the degradation products of chlorobutanol in a basic solution. The chlorobutanol obtained was subjected to bacteriological tests in order to study its antimicrobial activity. The antibacterial activity was evaluated against strains such as Escherichia coli (ATCC 25 922), Staphylococcus aureus (ATCC 25 923) and Pseudomonas aeroginosa (ATCC = American type culture collection). The antifungal activity was evaluated against human pathogenic fungal strains, such as Candida albicans and Aspergillus niger provided by the parasitology laboratory of the Hospital of Tizi-Ouzou, Algeria. Results and discussion: Chlorobutanol was obtained in an acceptable yield. The characterization tests of the product obtained showed a white and crystalline appearance (confirmed by scanning electron microscopy), solubilities (in water, ethanol and glycerol), and a melting temperature in accordance with the requirements of the European pharmacopoeia. The colorimetric reactions were directed towards the presence of a trihalogenated carbon and an alcohol function. The spectral identification (IR) showed the presence of characteristic chlorobutanol peaks and confirmed the structure of the latter. The microbiological study revealed an antimicrobial effect on all strains tested (Sataphylococcus aureus (MIC = 1250 µg/ml), E. coli (MIC = 1250 µg/ml), Pseudomonas aeroginosa (MIC = 1250 µg/ml), Candida albicans (MIC =2500 µg/ml), Aspergillus niger (MIC =2500 µg/ml)) with MIC values close to literature data. Conclusion: Thus, on the whole, the synthesized chlorobutanol satisfied the requirements of the European Pharmacopoeia, and possesses antibacterial and antifungal activity; nevertheless it is necessary to insist on the purification step of the product in order to eliminate the maximum impurities.

Hepatoprotective Activity of Sharbat Deenar, against Carbon Tetrachloride-Induced Hepatotoxicity in Rats

Polyherbal formulation Sharbat Deenar is a very popular unani medicine in Bangladesh. It is usually used for different kinds of liver disorders. In absence of reliable and inadequate hepatoprotective agents in conventional medicine, the herbal preparations are preferred for liver diseases. The present study was designed to evaluate the hepatoprotective activity of Sharbat Deenar on carbon tetrachloride (CCl4) induced hepatotoxicity in male Long-Evans albino rats. Group I served as normal control and received neither formulation nor carbon tetrachloride. Group II received only CCl4 1mL/kg body weight of rat intraperitoneally for consecutive 14 days. Group III received CCl4 1mL/kg body weight of rat intraperitoneally and Silymarin, in dose 50mg/kg body weight of rat orally. Group IV received CCl4 1mL/kg body weight of rat intraperitoneally and Sharbat Deenar 1mL/kg body weight of rat for the same 14 consecutive days. At the end of the study, hepatoprotective activity was evaluated by the levels of total bilirubin, alanine aminotransferase (ALT), aspartate aminotransferase (AST) and alkaline phosphatase (ALP). Histopathological study of rat liver was also carried out. The results showed that polyherbal formulation Sharbat Deenar exhibited a significant hepatoprotective effect. Such an outcome seems to be the synergistic effect of all ingredients of tested herbal formulation. Although this study suggests that Sharbat Deenar may be used to cure or minimize various liver diseases, it needs further study to attain the clarity of mechanism and safety.