FLOATING MULTIPLE UNIT MINITABLETS OF METOPROLOL SUCCINATE: FORMULATION, IN VITRO AND IN VIVO CHARACTERIZATION

Objective: In this present research, formulation of floating multiple unit minitablets of metoprolol succinate without using gas generating agent was attempted with an objective of increased residence time, sustained release, and improved oral bioavailability. Methods: Solid dispersions were prepared with lipophilic carriers such as compritol ATO888, Gelucire 43/01, Gelucire 39/01, and precirol ATO 05 was formulated using fusion technique. Neusillin US2 was used as an adsorbent. The solid dispersions were compressed into minitablets, weighing 20 mg, and then filled into ‘0’ size capsule. Results: Formulation F9, F10, F14, and F15 showed instantaneous floating lag time, i.e., 0 min, floating time more than 12 h, and sustained release up to 12 h. Pharmacokinetic study of the optimized formulation (F9) showed 2.46 times increase in area under the curve with increased residence time. Conclusion: Hence gelucire 43/01 based floating multiple unit minitablets of metoprolol succinate can be considered a promising approach

Priprava i in vitro vrednovanje bukoadhezivnih tableta karvedilola

Buccoadhesive tablets of carvedilol were prepared using HPMC K4M, HPMC K15M and Carbopol 934 as mucoadhesive polymers. Fifteen formulations were developed with varying concentrations of polymers. Formulations of the BC or BD series were composed of HPMC K4M or HPMC K15M in ratios of 1:1 to 1:5 whereas in the BE series Carbopol 934 was used (1:0.25 to 1:1.50). The formulations were tested for in vitro drug release, in vitro bioadhesion, moisture absorption and in vitro drug permeation through porcine buccal mucosa. Formulation BC3 showed maximum release of the drug (88.7 ± 0.4%) with the Higuchi model release profile and permeated 21.5 ± 2.9% of the drug (flux 8.35 ± 0.291 µg h1cm2) permeation coefficient 1.34 ± 0.05 cm h1) through porcine buccal membrane. BC3 formulation showed 1.62 ± 0.15 N of peak detachment force and 0.24 ± 0.11 mJ of work of adhesion. FTIR results showed no evidence of interaction between the drug and polymers. XRD study revealed that the drug is in crystalline form in the polymer matrix. The results indicate that suitable bioadhesive buccal tablets with desired permeability could be prepared.Varirajući koncentracije bukoadhezivnih polimera HPMC K4M, HPMC K15M i Carbopol 934 pripravljeno je 15 tableta karvedilola. Pripravci iz serije BC ili BD izrađeni su iz karvedilola i HPMC K4 M ili HPMC K 15M u omjerima 1:1, 1:2, 1:3, 1:4 i 1:5, a pripravci iz BE serije iz karvedilola i Carbopol 934 u omjerima 1:0.25, 1:0.50, 1:0.75, 1:1.00 i 1:1.50. In vitro je ispitivana brzina oslobađanja ljekovite tvari, bioadhezija, apsorpcija vlage i permeacija kroz bukalnu membranu svinje. Iz pripravka BC3 postignuto je maksimalno oslobađanje (88,7 + 0,4 %) koje je slijedilo Higuchijev model i maksimalna permeacija 21,5 + 2,9 % (fluks 8,35 ± 0,291 µg h-1 cm-2; permeacijski koeficijent 1,34 ± 0,05 cm h-1). Sila odvajanja za taj pripravak bila je 1,62 ± 0,15 N, a adhezija 0,24 ± 0,11 mJ. FTIR ispitivanja su pokazala da nije bilo interakcija između ljekovite tvari i polimera, a XRD ispitivanja da je ljekovita tvar u kristaliničnoj formi u polimernom matriksu. Pripravljene bukalne tablete su dovoljno bioadhezivne, a permeacija iz njih je zadovoljavajuća

Influence of Momordica charantia on oxidative stress-induced perturbations in brain monoamines and plasma corticosterone in albino rats

Objectives: The objective of this study was to evaluate the antistress activity of Momordica charantia (MC) fruit extract on stress-induced changes in albino rats and also to explore attenuating effects of MC on in vitro lipid peroxidation in rat brain. Materials and Methods: In this study, Wistar albino rats (180-200 g) were used. Plasma corticosterone and monoamines-5-hydroxy tryptamine (5-HT), norepinephrine (NE), epinephrine (E) and dopamine (DA) in cortex, hypothalamus and hippocampus regions of brain were determined in animals under different stressful conditions. Ethanolic fruit extract of MC, at doses of 200 and 400 mg/kg, was used. The oxidative stress paradigms used in in vivo models were acute stress (AS) and chronic unpredictable stress (CUS). Panax quinquefolium (PQ) was used as a standard in in vivo models and ascorbic acid was used as a reference standard in the in vitro method. Results: Subjecting the animals to AS (immobilization for 150 min once only) resulted in significant elevation of plasma corticosterone levels and brain monoamine levels. Pretreatment with MC at doses of 200 and 400 mg/kg p.o. significantly countered AS-induced changes and a similar effect was exhibited by PQ at 100 mg/kg p.o. In the CUS regimen (different stressors for 7 days), plasma corticosterone levels were significantly elevated whereas the levels of 5-HT, NE, E, and DA were depleted significantly. Pretreatment with MC (200 and 400 mg/kg) attenuated the CUS-induced changes in the levels of above monoamines in cortex, hypothalamus, and hippocampus regions of brain and plasma corticosterone in a dose-dependent manner. Furthermore, MC extract (1000-5000 μg/mL) exhibited a significant quenching effect on in vitro lipid peroxidation indicating its strong antioxidant activity which was compared with ascorbic acid. Conclusions: This study reveals the antistress activity of MC as it significantly reverted the stress-induced changes, and the activity might be attributed to its antioxidant activity since stress is known to involve several oxidative mechanisms

Taste masking of oral pregabalin liquid preparation by using ion exchange resins

The purpose of this study was to use cation exchange resins to mask Pregabalin's unpleasant taste. Dowex-50, a crosslinked polystyrene backbone, was employed. DRCs were synthesised in batches with drug-to-resin ratios of 1:1, 1:2, and 1:3. The optimal drug-to-resin ratio as well as the time required for maximum complexation were discovered. In this work, an attempt was made to develop a taste-masked Pregabalin solution using a simple, rapid, and cost-effective flavour masking approach, such as complexation among ion exchange resin, that could be acceptable to industries. To mask the flavour, researchers used a combination of ion-exchange resins such as doshion P 542, Tulsion 344, Indion 234, Indion 204, and Kyron T 114, as well as formulation into a solution. The generated suspensions were tested for taste, drug content, particle size, viscosity, sedimentation volume, drug release, and accelerated stability. Kyron T 114 has been shown to effectively disguise the drug among the various resins. The newly developed formulation also has the benefit of simplifying the manufacturing process and being cost-effective. According to drug release studies, the entire medicament was released within 20 minutes.&nbsp

Spectrophotometric Determination of Raloxifene Hydrochloride in Pharmaceutical Formulations

Three new simple, sensitive, rapid and economical spectrophotometric Methods (A, B and C) have been developed for the determination of Raloxifene Hydrochloride in pharmaceutical bulk and tablet dosage form. Method A is based on the formation of yellow colored chromogen with 0.1N Sodium hydroxide exhibiting maximum absorbance against the corresponding reagent blank. The method B is based on the reaction of Raloxifene with Ferric chloride and 1, 10-phenanthroline to form blood red colored chromogen. The method C is based on the formation of blood red colored chromogen with Ferric chloride and 2, 2' bipyridyl. The absorbencies of the chromogens were measured at their respective wavelength of maximum absorbance against the corresponding reagent blank. The proposed methods have been successfully applied to the analysis of the bulk drug and its tablet dosage form. The methods have been statistically evaluated and were found to be precise and accurate

PREPARATION AND EVALUATION OF A TASTE-MASKED ARTEMETHER ORAL SUSPENSION

Objective The antimalarial drug Artemether is bitter in taste. The purpose of this work is to construct a taste-masked Artemether resinate employing ion exchange resins.   Methodology The process for drug resin complexation was adjusted in terms of drug resin ratio and medium pH. FTIR and DSC measurements were used to characterise the taste masked complex. As an ion exchange resin, Indion 204 was used. It was combined with medication in various ratios: Indion was generated at various times and pH values and the extent of complexation was determined.   Results The result indicates that a 1:1 ratio of Indion 204 to resin resulted in the largest amount of complexation after four hours of mixing. These resinate then converted into granules and they exhibit angle of repose, bulk density, and flow characteristic values that are acceptable. The loading of drugs was greater than 99 percent. Based on drug content, suitable amount of drug-resinate was taken for formulation. Then Suspension was studied for general appearance, viscosity, sedimentation ratio, drug release, resuspendability. The release test showed that 92.46% drug release within 120 min.   Conclusion Hence we can conclude that, the Indion 204 has been proved to be useful as taste masking agent. Thus we are able to achieve our objectives of preparing taste masked suspension of Artemether with minimum excipients and simple method of manufacturing.&nbsp

Development and modification of the natural polymers by converting them into nanobiocomposite

The main target ofTthis study is to develop an  antibacterial  chitosan  nanocomposite  fabric  among  in  situ   crated   silver  nanoparticles  utilizing   Vitex  leafTextract,  which  i s amedicinal herb. The CNCFs were evaluated using scanning  electron  microscopy  (SEM), Fourier transform infrared (FT-IR) spectroscopy,Xray diffraction (XRD), and antimicrobial testing. Additionally, these CNCFs have excellent antibacterial characteristics. These CNCFs could be used  in medical  applic  ations like surgical aprons, wound cleansing, wound  dressing,  and  hospital  bed  mat erials, as they were manufactured utilising a simple and environmentally acceptable approach