Posted by admin on Dec 31, 2019 in |
Objectives: In the present study, an effort was made to develop a novel pulsatile dosage form for the treatment of hypertension using Propranolol hydrochloride as a model drug. A time-delayed capsule was prepared by sealing the pellets inside the insoluble hard gelatin capsule body with an erodible hydrogel plug. Methods: The pellets were prepared by the Fluidized Bed Wurster (bottom spray) technique. The entire device was enteric coated so that the variability in gastric emptying time can be overcome and a colon-specific release can be achieved. Hydrogel plug (HPMCK4 and lactose in 1:1 ratio) having 4.5 kg/cm2 hardness and 100 mg weight was placed in the capsule opening and found suitable to avoid the drug release in small intestinal fluid and eject the plugin colonic fluid, releasing the pellets into colonic fluid after a lag time criterion of 5 h. Three dissolution media with pH 1.2, 7.4 and 6.8 were consecutively used to simulate the pH changes along the GI tract. Results: FTIR study confirmed that there was no...
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Posted by admin on Dec 31, 2019 in |
A series of some quinolino-benzimidazole/thiazole derivatives (3a-3h) have been synthesized from2-hydroxyquinoline-3-formaldehyde derivatives (1a-1d) and 1, 2-phenylenediamines/2-aminothiophenols (2a-2c). The synthesized compounds were characterized by FTIR, 1H-NMR and Mass Spectrometry. All the compounds were screened in-vitro for their antibacterial activity against Mycobacterium tuberculosis (H37 RV strain) ATCC No-27294. Among the compounds tested, compounds 3e showed potent antitubercular activity against M. tuberculosis at MIC 6.25 µg/mL. We extended our study to explore the inhibition mechanism by conducting molecular docking analysis by using...
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Posted by admin on Dec 31, 2019 in |
A simple and sensitive Ultra Performance Liquid Chromatography-Tandem Mass Spectrometry method was developed to perform a stability study of diltiazem and its metabolites in human plasma using various buffer reagents at a different strength. The method was applied for the quantification of diltiazem and its two major metabolites N-desmethyl diltiazem and desacetyl diltiazem in human plasma. The analytes were separated using a binary solvent delivery mode on a reversed-phase column and analyzed by Mass Spectrometry in the multiple reaction monitoring mode using the respective (M+H)+ ions, m/z 415.05/178.03 for diltiazem, m/z 401.09/150.04 for N-desmethyl diltiazem m/z 373.21/108.85 for desacetyl diltiazem, m/z 419.22/314.0 for diltiazem-D4 (internal standard). The linearity was 0.93 to 250.10 ng/mL for diltiazem, 0.24 to 64.00 ng/mL for N-desmethyl diltiazem and 0.15 to 40.69 ng/mL for desacetyl diltiazem in human plasma. The lower limit of quantification was 0.93 ng/mL, 0.24 ng/mL and 0.15 ng/mL for diltiazem, N-desmethyl diltiazem, and desacetyl diltiazem, respectively. The plasma samples buffered with 1% of 0.1 M NaF solution was able to limit...
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Posted by admin on Dec 31, 2019 in |
Background: Herbal extracts have been used in dental products for many years owing to their anti-adherence effect on Streptococcus mutans (S. mutans) in the biofilm formation. Dental caries are developed by the colonization of oral bacteria on the surface of teeth and adherence is the first step in the colonization process. Objective: The objective of the present study was to explore the anti-biofilm effect of the various combinations of herbal extracts and essential oils against S. mutans which play a central role in causing dental caries. Methods: Hydroalcoholic extracts of Terminalia chebula (T. chebula), Psidium guajava (P. guajava), Azadirachta indica (A. indica) and Pongamia pinnata (P. pinnata) were prepared separately and dried. Various combinations of herbal extracts, as well as essential oils Syzygium aromaticum (clove) and Mentha piperita (Peppermint oil), were tested for anti-biofilm potential on the glass surface. The number of adhering bacteria (CFU/ml) was determined by the plate count method. Results: It was found that all extract combinations and essential oils have shown anti-biofilm activity. The 2:2:1:1...
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Posted by admin on Dec 31, 2019 in |
Protocatechuic acid (PCA) is a type of widely distributed naturally occurring phenolic acid, commonly found in bran, grain, brown rice, fruits such as plums, gooseberries, grapes and also in onion peels. A new, simple, precise, accurate and sensitive stability-indicating HPTLC method for Protocatechuic acid was successfully developed. This method is based on HPTLC separation followed by UV detection at 258 nm. The HPTLC method is used to determine the presence and quantify the protocatechuic acid in onion peel extract. The separation was carried out on Merck TLC aluminum sheets precoated with silica gel 60F254 using Toluene: Ethyl Acetate: Formic acid (6:6:1.2 v/v/v) as a mobile phase and scanning was done by using TLC Scanner III. Protocatechuic acid gave well defined and sharp peak at Rf 0.52 ± 0.03 at 258 nm. The calibration curve was linear in range 100-500 ng/band. Protocatechuic acid was subjected to stress conditions like hydrolysis under acidic, basic and neutral conditions, oxidation, heat, and...
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