CURCUMIN-ZN-ARTEMETHER COMBINATION THERAPY FOR PLASMODIUM BERGHEI INFECTED MICE

Objective: Studies have shown that a new combination therapy with artemisinin derivatives and curcumin is unique, with potential advantages over known Artemisinin Combination Therapy (ACT). The problems of poor solubility, stability and bioavailability of curcumin can be overcome by preparing curcumin metal complex. In present study curcumin-Zn complex was prepared and evaluated for antimalarial activity in combination with artemether.Methods: Curcumin Zn complex was prepared using zinc sulfate. The mice survival and % parasitemia were studied in Plasmodium berghei (P. berghei) infected albino mice treated with curcumin, curcumin-Zn complex and combination of curcumin-Zn with artemether.Results: The mean survival time in mice infected with P. berghei was compared after treatment with curcumin, curcumin-Zn, artemether and combination of curcumin-Zn-artemether. Oral administration of curcumin-Zn-artemether prolonged the survival of P. berghei infected mice. All the mice were treated with Curcumin-Zn (5 mg/day) artemether (1000 µg) survived for more than 40 days and recovered with no detectable parasitemia. Administration of curcumin-Zn artemether combination reduced the parasitemia in mice more effectively compared to that in mice treated with a single drug.Conclusion: In vivo antimalarial activity of curcumin-Zn complex was found superior to curcumin. A single dose of 1000 µg of artemether in combination with curcumin-Zn gives complete protection in P. berghei infected mice. Such suppressive action was superior to that of administration of the single drug at the same dose. This may reduce the chances of drug resistance.Â

DEVELOPMENT OF MUCOADHESIVE DELIVERY OF CHLORZOXAZONE POLYETHYLENE GLYCOL SOLID DISPERSION

ABSTRACTObjective: Chlorzoxazone (CLZ) is centrally acting skeletal muscle relaxant. It is insoluble in water, so employed for the formation of solid dispersions(SD) as a means to enhance the dissolution rate, and carrier selected was polyethylene glycol 6000 (PEG 6000).Methods: The SDs were prepared by different methods and characterized by in vitro drug release, drug content, fourier transform infraredspectroscopy (FTIR), differential scanning calorimetry, powder X-ray diffraction. All the SD showed dissolution improvement compare to pure drug.These techniques revealed distinct loss of drug crystallinity in the formulation accounting for enhancement in dissolution rate. The SD methodsshowing best in vitro drug release profile were selected in the further development of mucoadhesive buccal patches. A buccal patch has been developedusing two mucoadhesive polymers, i.e. hydroxyl propyl methyl cellulose K4M and carbopol 974. The patches were evaluated for the physicochemical,mechanical and drug release characteristics. The optimized patches showed good mechanical and physicochemical properties to withstand theenvironment of the oral cavity. The in-vitro permeation study showed that patches could deliver drug to the oral mucosa for a period of 8 hrs.Results: The results indicate that suitable bioadhesive buccal patches with good permeability could be prepared. The batches FH4 and FC4 showed81.95% and 79.97% permeated through goat mucosa membrane in 8 hrs. The physicochemical interactions were investigated by FTIR, showed noany evidence of interactions and were present in an unchanged state. The stability study for SD and buccal patch carried out revealed that were stablefor a period of 3-month.Conclusion: Phase-solubility studies indicate significantly increase in solubility. The optimized buccal patches showed good mechanical andphysicochemical properties to withstand environment of the oral cavity.Keywords: Solid dispersions, Chlorzoxazone, Dissolution studies, Buccal patch, In vitro permeation studies

Studies on in-vitro transcutaneous delivery of losartan potassium, influence of penetration enhancers and barrier membrane

Formulation and in vitro evaluation of losartan potassium (LP) loaded transdermal delivery system (TDS) was investigated for controlled release and improved therapeutic efficacy. TDS (patches) were prepared by varying the composition of Eudragit RL 100 and Eudragit RS 100 (5:0, 4:1, 3:2, 2.5:2.5, 2:3, 1:4 and 0:5). Patches were evaluated for thickness, content uniformity, mechanical properties, moisture uptake and in vitro drug release. Technological parameters for all the formulations were found to be within the limit. In vitro studies showed relatively high permeation of LP (F1- 42.17 ± 1.13 %) from the formulation comprising 4:1 ratio of polymer. Inclusion of capsaicin (55.70 ± 1.55 %) and pluronic F-68 (70.88 ± 1.20 %) to formulation F1 resulted increased permeation of LP across human skin. In conclusion, this study demonstrated the potential of simple transdermal adhesive patch incorporating LP to deliver therapeutically useful dose in-vivo for the treatment of hypertension.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Development and Validation of UV-Visible Spectrophotometric Baseline Manipulation Method for Simultaneous Quantitation of Tenofovir Disoproxil Fumarate and Emtricitabine in Pharmaceutical Dosage Form

A simple, economical, precise, and accurate new UV-visible spectrophotometric baseline manipulation method for simultaneous determination of tenofovir disoproxil fumarate (TE) and emtricitabine (EM) in combined tablet dosage form has been developed. e method is based on baseline manipulation (difference) spectroscopy where amplitudes at 261 and 289.9 nm were selected to determine TE and EM, respectively, in combined formulation, and distilled water was used as solvent. Both drugs obey Beer's law in the concentration ranges of 4-20 g/mL for TE and 6-30 g/mL for EM. e results of analysis have been validated statistically, and recovery studies con�rmed the accuracy of the proposed method which was carried out by following the ICH guidelines

Synthesis and evaluation of analgesic, anti-asthmatic activity of (E)-1-(8-hydroxyquinolin-7-yl)-3-phenylprop-2-en-1 ones

Abstract Seventeen (E)-1-(8-hydroxyquinolin-7-yl)-3-phenylprop-2-en-1 one derivatives were synthesized via aldol condensation of substituted benzaldehydes with quinoline chalcones starting from 8-hydroxy quinoline. Molecular docking studies were performed on COX-2 protein for analgesic activity and PDE 4 enzyme for anti-asthmatic activity. Docking studies for analgesic activity reveal that the compounds 2 , 4 , 12 , 14 , and 15 showed significant interaction in terms of hydrogen bonding, hydrophobic attachment and van der Waal interaction with COX-2. The docking studies and pharmacological screening indicate that substitution of hydroxyl and conjugated ketone groups on the aldehyde ring and the quinoline ring accelerates analgesia with better binding to active site. Eddy's hot plate method was used to evaluate analgesic activity of the synthesized compounds. Compounds showed a substantial increase in reaction time when compared with standard pentazocin. Compounds 2 , 4 , 7 , 9 and 13 showed significant binding interactions with PDE 4 enzyme and hence were selected for evaluation of anti-asthmatic activity using the goat tracheal chain method. Studies reveal that substitution of the methoxy group at 4th & 5th positions for compounds 2 , 4 & 7 leads to significant percentage inhibition of histamine induced contraction. The synthesized compounds are thus found to be potent as analgesic and anti-asthmatic agents

Razvoj i optimizacija sustava za isporuku metoprolol sukcinata sa zadržavanjem u želucu

Metoprolol succinate (MS) gastroretentive (GR) controlled release system was formulated to increase gastric residence time leading to improved drug bioavailability. Box-Behnken model was followed using novel combinations of sodium alginate (SA), sodium carboxymethylcellulose (NaCMC), magnesium alumino metasilicate (MAS) as independent variables. Floating lag time (Flag), t25, t50, t75, diffusion exponent as dependent variables revealed that the amount of SA, NaCMC and MAS have a significant effect (p < 0.05) on t25, t50, t75 and Flag. MSGR tablets were prepared and evaluated for mass, thickness, hardness, friability, drug content and floating property. Tablets were studied for dissolution for 24 h and exhibited controlled release of MS with floating for 16 h. The release profile of the optimized batch MS01 fitted first-order kinetics (R2 = 0.9868, n = 0.543), indicating non-Fickian diffusion or anomalous transport by diffusion and swelling.U radu je opisan razvoj sustava za isporuku metoprolol sukcinata (MS) s kontroliranim oslobađanjem i produljenim vremenom zadržavanja u želucu (GR), u svrhu poboljšanja bioraspoloživosti. Primijenjen je Box-Behnkenov model, a kao zavisne varijable izabrane su nove kombinacije natrijevog alginata (SA), natrijeve soli karboksimetilceluloze (NaCMC) i magnezijevog aluminometasilikata (MAS). Vrijeme plutanja (Flag), t25, t50, t75 i difuzijski eksponent kao zavisne varijable otkrili su da količina SA, NaCMC i MAS ima značajan učinak (p < 0,05) na t25, t50, t75 i Flag. Pripravljenim tabletama određena je masa, debljina, tvrdoća, lomljivost, sadržaj ljekovite tvari i sposobnost plutanja. Oslobađanje MS praćeno je 24 h. Rezultati pokazuju da je oslobađanje kontrolirano, a vrijeme plutanja 16 h. Oslobađanje iz optimiranog pripravka MS01 slijedi kinetiku prvog reda (R2 = 0,9868, n = 0,543), što ukazuje na difuziju koja ne slijedi Fickov zakon već anomalni transport difuzijom i bubrenjem

Application of Design of Experiment for Floating Drug Delivery of Tapentadol Hydrochloride

The aim of the present study was to apply design of experiment (DOE) to optimize floating drug delivery of tapentadol hydrochloride. Tapentadol hydrochloride is a synthetic opioid used as a centrally acting analgesic and effective in both experimental and clinical pain. The half-life of the drug is about 4 hours and oral dose is 50 to 250 mg twice a day. For optimization 32 full factorial design was employed for formulation of tapentadol hydrochloride tablets. Sodium bicarbonate was incorporated as a gas-generating agent. Combination of polymers Xanthan gum and Locust bean gum was used to achieve controlled release effect. The concentration of polymers was considered as the independent variables and dependent variables were floating lag time and swelling index of the tablets. From the factorial batches, it was observed that formulation containing combination of 20% sodium bicarbonate and 10% citric acid shows optimum floating ability whereas the formulation containing 20% Xanthan gum and 28% Locust bean gum shows optimum sustained drug release pattern with adequate floating

FORMULATION, IN-VITRO AND IN-VIVO X-RAY EVALUATION OF KOLLIDON ® SR MATRIX TABLETS OF DILTIAZEM HCL.

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Optimization of Thermoreversible In Situ Nasal Gel of Timolol Maleate

Nasal route had shown better systemic bioavailability due to its large surface area, porous endothelial membrane, high total blood flow, and avoidance of first-pass metabolism. Timolol maleate is a beta blocker used primarily in the treatment of hypertension. Drug undergoes extensive hepatic first-pass metabolism (80%). The drug has half-life of 4 hrs. Oral bioavailability of timolol maleate is 61%. The aim of the present study was to optimize controlled release in situ nasal delivery for timolol maleate. HPMC and Poloxamer 407 were selected as polymer in formulation of thermoreversible in situ nasal gel. Optimization was carried out using 32 factorial design. It was observed that formulations f1 and f4 revealed the highest % drug release, that is, 93.57% and 91.66%, respectively. Factorial design study indicated that the drug release and viscosity were most significant dependent factors. Ex vivo diffusion study through nasal mucosa indicated 67.26 ± 2.10% and 61.07 ± 2.49% drug release for f1 and f4 formulations. f1 was the optimized batch. This batch thus can act as a potential nasal delivery with enhanced bioavailability for the drug