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

Synthesis and characterization of Polyindole and its catalytic performance study as a heterogeneous catalyst

The catalytic performance study of polyindole as a heterogeneous catalyst is reported for the synthesis of 3,3'-arylmethylene-bis-1H-Indole derivatives using various substituted aldehydes and indole under reflux reaction condition with good to excellent yield. Polyindole was synthesized by chemical oxidative polymerization using citric acid as a dopant. The synthesized polymer was well characterized by various spectroscopic techniques like FT-IR, XRD, FESEM, etc. The XRD pattern confirms the partially crystalline nature of polyindole. The FESEM images of polyindole revealed the formation of irregularly shaped particulate nature with size in the range of 0.2 to 6 micron. In FT-IR spectrum, the major peak at similar to 3400 cm(-1) indicates N-H stretching and at 1564-1624 cm(-1) indicates C-C stretching of benzenoid ring of indole. The presence of peak at similar to 3400 cm(-1) indicates that the polymerization does not occur at nitrogen. The present protocol has certain advantages like recyclability, low loading of the catalyst, low-cost and efficient use of polyindole as a heterogeneous catalyst

Electrochemical determination of the serotonin reuptake inhibitor, dapoxetine, using cesium-gold nanoparticles

© 2017 American Chemical Society. Cesium-gold (Cs-Au) nanoparticles are shown to be analytically advantageous for the electroanalytical sensing of dapoxetine (DPX), a serotonin reuptake inhibitor used for the treatment of premature ejaculation. The Cs-Au nanoparticles are electrically wired and supported upon mass producible, economical screen-printed electrochemical sensing platforms and are characterized electrochemically (cyclic voltammetry and electrochemical impedance spectroscopy) and physiochemically (field emission scanning electron microscopy and energy dispersive X-ray analysis). The face-centered design was applied to optimize the significant experimental factors by using square wave voltammetry. The Cs-Au-based sensor is found to exhibit a large linear range (10 -7 to 10 -4 M) with a good analytical linearity with the limits of detection and quantification corresponding to 2.50 - 10 -10 and 8.33 - 10 -8 M, respectively. The developed sensor was successfully applied in the quantification of DPX in the presence of sildenafil, both of which are commonly found within combined dose tablet pharmaceutical formulations. The proposed DPX electrochemical Cs-Au-based sensor has the advantages of being single-shot and disposable and is shown to be successful in determining DPX in pharmaceutical formulations, human urine, and serum samples with acceptable recoveries

Heterogeneous catalysis for sustainable biodiesel production via esterification and transesterification

Concern over the economics of accessing fossil fuel reserves, and widespread acceptance of the anthropogenic origin of rising CO2 emissions and associated climate change from combusting such carbon sources, is driving academic and commercial research into new routes to sustainable fuels to meet the demands of a rapidly rising global population. Here we discuss catalytic esterification and transesterification solutions to the clean synthesis of biodiesel, the most readily implemented and low cost, alternative source of transportation fuels to meet future societal demands

Rooting and hardening of<i style=""> in vitro</i> plantlets of <i style="">Garcinia</i> <i style="">indica</i> Chois

409-413In the present paper, a procedure for rooting and acclimatization of in vitro plantlets raised from immature seed cultures of Garcinia indica is described. Pulse treatment of 9800µM IBA was preferred for rooting of in vitro shoots. Nearly 100% rooting (in vitro) was obtained with half strength MS with 2% sucrose and 0.6 % agar. Rooted plantlets of about 2-4 cm height (2-3 nodes) were subsequently transferred to different media for acclimatization: 1. Cocopeat + Sand + Soil (1:2:1); 2. Cocopeat + Sand (1:1); 3. Cocopeat. Plants grown in cocopeat showed 76% of survival followed by cocopeat and sand (1:1) with 75% of survival. The in vitro elongated shoots could also be rooted ex vitro by treating with synthetic hormones like Keradix, Rootex-1, and Rootex-3. However, the success of rooting was low (20 to 55 %). The hardened plantlets were successfully acclimatized in the greenhouse and transferred to open field conditions

Analytical Method Development and Validation for the Test Related Substances of Pomalidomide in Pomalidomide Capsules

&lt;p&gt;The percent impurities of pomalidomide in capsules of 1mg, 2mg, 3mg, and 4mg were determined using an HPLC technique. The current study provides the pomalidomide method validation for related chemicals test's procedural design and acceptance criteria. On a 1 mg capsule, the following tests were performed: force degradation, LOD, and LOQ, linearity and range, accuracy, solution stability, filter study, specificity, and robustness. On the pomalidomide capsules, precision and intermediate precision were also conducted. The study's output cleared that method is easy, quick, specific &amp; accurate, making it suitable for regular pomalidomide determination in bulk and pharmaceutical dose forms.&lt;/p&gt;&lt;p&gt;Keywords:- Pomalidomide; HPLC; Method validation; Capsules.&lt;/p&gt

Biopolymer catalysed synthesis of 6-methyl-4-phenylcarbamoyl-1, 2, 3, 4-tetrahydropyrimidine-2-ones and evaluation of their anti-bacterial and anti-tubercular activities

1ackground: An efficient one-pot biocatalysed ultrasound assisted synthesis of dihydropyrimidinones/thiones has been developed under solvent free conditions. Materials and Methods: The use of biodegradable, non toxic, agar-powder as a catalyst provide advantages like high yield, simple operation, mild reaction condition with short reaction time. 1,2,3,4-tetrahydropyrimidine-2-ones/thiones formed were characterized by mass and 1H NMR spectroscopy. Results: The dihydropyrimidinones substituted with electron donating groups like fluorine, hydroxy along with thienyl groups exhibited good antibacterial activity. The compounds exhibited favorable binding interactions with mycobacterium target protein H37Rv. Conclusion: 4-methoxy substituted dihydropyrimidinones derivative showed significant antituberculosis activity

Optimization Studies on Compression Coated Floating-Pulsatile Drug Delivery of Bisoprolol

The purpose of the present work was to design and optimize compression coated floating pulsatile drug delivery systems of bisoprolol. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. The prepared system consisted of two parts: a core tablet containing the active ingredient and an erodible outer shell with gas generating agent. The rapid release core tablet (RRCT) was prepared by using superdisintegrants with active ingredient. Press coating of optimized RRCT was done by polymer. A 32 full factorial design was used for optimization. The amount of Polyox WSR205 and Polyox WSR N12K was selected as independent variables. Lag period, drug release, and swelling index were selected as dependent variables. Floating pulsatile release formulation (FPRT) F13 at level 0 (55 mg) for Polyox WSR205 and level +1 (65 mg) for Polyox WSR N12K showed lag time of 4 h with >90% drug release. The data were statistically analyzed using ANOVA, and P<0.05 was statistically significant. Release kinetics of the optimized formulation best fitted the zero order model. In vivo study confirms burst effect at 4 h in indicating the optimization of the dosage form

Preparation and in vitro evaluation of Allopurinol-Gelucire 50/13 solid dispersions

The rate-limiting step to absorption of drugs from the gastrointestinal tract is often dissolution from the dosage form. Allopurinol is a commonly used drug in the treatment of chronic gout or hyperuricaemia associated with leukaemia, radiotherapy, anti-neoplastic agents. One of the major problems with allopurinol is that, it is practically insoluble in water, which results in poor bioavailability after oral administration. In the present study, solid dispersions of allopurinol were prepared by solvent evaporation method, kneading method, co-precipitation method, co-grinding method and closed melting method to increase its water solubility. In the present study amphiphilic carrier like gelucire 50/13 was used in the ratio of 1:1, 1:2 and 1:4. Prepared solid dispersions were characterized in the liquid state by phase solubility studies and in the solid state by Differential Scanning calorimetric analysis, Powder X-ray diffractometry and Fourier Transform Infrared spectroscopy. The aqueous solubility of allopurinol was preferential by the presence polymer with increasing concentration. Solid state characterizations indicated that allopurinol was present as an amorphous material and entrapped in polymer matrix.Mathematical modeling of in vitro dissolution data indicated the best fitting with Korsemeyer-Peppas model and the drug release kinetics primarily as Non-Fickian diffusion. Therefore, the current study showed that gelucire 50/13 has a significant solubilizing effect on allopurinol.Keywords: Allopurinol, gelucire 50/13, closed melting-method, co-grinding, dissolution study, powder X-ray diffraction analysi