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A spectrofluorimetric method using fluorescent carbon dots (CDs) was developed for the selective detection of azelnidipine (AZEL) pharmaceutical in the presence of other drugs. In this study, N‐doped CDs (N‐CDs) were synthesized through a single‐step hydrothermal process, using citric acid and urea as precursor materials. The prepared N‐CDs showed a highly intense blue fluorescence emission at 447 nm, with a photoluminescence quantum yield of ~21.15% and a fluorescence lifetime of 0.47 ns. The N‐CDs showed selective fluorescence quenching in the presence of all three antihypertensive drugs, which was used as a successful detection platform for the analysis of AZEL. The photophysical properties, UV–vis light absorbance, fluorescence emission, and lifetime measurements support the interaction between N‐CDs and AZEL, leading to fluorescence quenching of N‐CDs as a result of ground‐state complex formation followed by a static fluorescence quenching phenomenon. The detection platform showed linearity in the range 10–200 μg/ml (R2 = 0.9837). The developed method was effectively utilized for the quantitative analysis of AZEL in commercially available pharmaceutical tablets, yielding results that closely align with those obtained from the standard method (UV spectroscopy). With a score of 0.76 on the 'Analytical GREEnness (AGREE)' scale, the developed analytical method, incorporating 12 distinct green analytical chemistry components, stands out as an important technique for estimating AZEL. [ABSTRACT FROM AUTHOR]

A specific, accurate and reproducible stability-indicating high performance thin layer chromatography (HPTLC) method was developed for the estimation of flurbiprofen and chloramphenicol in the presence of their degradation products. Degradation studies of both the drugs were carried out in acidic, alkaline, neutral, oxidative, photolytic and thermal stress conditions. Separation was performed on thin layer chromatography plate precoated with silica gel 60 F254 using ethyl acetate : n-hexane : methanol : tri-ethyl amine (5 : 4 : 2 : 0.5, v/v/v/v). Spots at retention factor 0.29 and 0.62 were recognized as flurbiprofen and chloramphenicol, respectively, and were quantified through densitometric measurements at wavelength 267 nm. Method was found to be linear over the concentration range 12-60 ng/spot with correlation coefficient of 0.9997 for flurbiprofen and 200-1,000 ng/spot with correlation coefficient of 0.9977 for chloramphenicol. The proposedmethod was applied to the estimation of flurbiprofen and chloramphenicol in commercial ophthalmic formulation. The developed HPTLCmethod can be applied for routine analysis of flurbiprofen and chloramphenicol in the presence of their degradation products in their individual as well as combined pharmaceutical formulations. [ABSTRACT FROM AUTHOR]

Ondansetron Hydrochloride is a potent antiemetic drug indicated for the treatment and/or prophylaxis of postoperative or chemotherapy- or radiotherapy-induced emesis. It is extremely bitter in taste. The purpose of this research was to mask the bitter taste of Ondansetron Hydrochloride with carbopol by neutralization method. The effect of variables like type of alkali, concentration of alkali, grades of carbopol and concentration of carbopol on bitterness level was studied. Results showed that neutralization of drug with equimolar sodium hydroxide and subsequent complexation with 0.6% carbopol 971G gave effective taste masking. The drug polymer complex was used to formulate orodispersible tablets by direct compression method using three different superdisintegrants like croscarmellose sodium, crospovidone and Kyron T- 314. The prepared tablets were evaluated for the parameters like general appearance, thickness, hardness, weight variation, friability, wetting time, water absorption ratio, in vitro and in vivo disintegration time. The disintegration tests showed rapid disintegration within 25-42 seconds. In vitro dissolution studies showed 100% drug release in 10 minutes. The formulations were subjected to stability testing for three months at 25°C/60%RH and 40°C/75%RH. Results revealed no appreciable change in any of the formulations. It is concluded that the method attempted here for formulation of orodispersible tablets of taste masked Ondansetron Hydrochloride being simple and cost effective. [ABSTRACT FROM AUTHOR]

A simple, accurate, sensitive and reproducible spectroflourometric method was developed and validated for the analysis of Sitagliptin in bulk and pharmaceutical dosage forms. Sitagliptin showed fluorescence in double distilled water having excitation wavelength at 265 nm and emission wavelength at 580 nm. The calibration graph was prepared in the concentration range of 10-50μg/ml and was found to be linear. The correlation co efficient was found to be 0.998. The proposed method was validated and successfully applied for analysis of tablet dosage forms. [ABSTRACT FROM AUTHOR]

Objective: Present investigation was undertaken to study the effectiveness of hydroalcoholic extract of roots of Boerhaavia diffusa in experimental benign prostatic hyperplasia (BPH) in rats using various animal models. Materials and Methods: BPH in rats was induced by subcutaneous injection of testosterone (5 mg/kg) daily for 28 days. Rats were divided in to five groups (six rats each). A negative control group received arachis oil (1 ml/kg s.c.) and four groups were injected testosterone. These four groups were further divided into reference group (finasteride 1 mg/kg), model group (testosterone), study group A (B. diffusa 100 mg/kg), and study group B (B. diffusa 250 mg/kg). On the 29th day, rats were sacrificed and body weight, prostate weight, bladder weight, and serum testosterone level were measured and histological studies were carried out. Further in vitro analysis of B. diffusa extract on contractility of isolated rat vas deferens and prostate gland, produced by exogenously administered agonists were carried out. All results were expressed as mean ± SEM. Data were analyzed by one-way analysis of variance followed by Tukey's test. Results: B. diffusa (100 mg/kg) treatment for 28 days resulted in significant inhibition of prostate growth (P < 0.05). Drug extract did not have significant change on serum testosterone level. Histopathological analysis of prostate gland supported above results. Results of in vitro experiment suggest that extracts had attenuated the contractile responses of isolated vas deferens and prostate gland to exogenously applied agonists. Conclusion: The results suggested that treatment with B. diffusa may improve symptoms of disease and inhibit the increased prostate size. In vitro study implies that herbal extracts has the machinery to produce beneficial effect on prostatic smooth muscle, which would relieve the urinary symptoms of disease. B. diffusa could be a potential source of new treatment of prostatic hyperplasia. [ABSTRACT FROM AUTHOR]

Objective: Aqueous root extract of Oroxylum indicum was evaluated in rats against dinitrobenzene sulfonic acid (DNBS) induced colitis. Materials and Methods: Rats were pre-treated orally for seven days and continued for four days after the induction of colitis with OIaq (100, 200, and 400 mg/kg) or vehicle. Colitis was induced by intracolonic instillation of 25 mg of DNBS per rat dissolved in 50% alcohol and 4 days later, the colonic mucosal damage was analyzed along with food intake, body weight, colon weight, spleen weight, histological damage, myeloperoxidase (MPO) activity, malondialdehyde (MDA) levels, reduced glutathione (GSH), and nitric oxide levels in colonic tissue homogenate. Results: Significant reduction in gross damage area, weight loss and increase in colonic and spleen weight were evident in test substance-pretreated animals' dose dependently as compared to vehicle treated control. These effects were confirmed biochemically by a reduction in colonic myeloperoxidase activity, malondialdehyde levels, nitric oxide levels, and increase in reduced glutathione (GSH) levels. Furthermore, microscopic examination revealed diminution of inflammatory cell infiltration and submucosal edema in colon segments of rats treated with OIaq. Conclusion: The results demonstrate the protective effect of OIaq in the animal model of acute colitis possibly through an antioxidant, anti-lipoperoxidative or due to reduction in nitric oxide generation. [ABSTRACT FROM AUTHOR]

Abstract: Ethnopharmacological relevance: A well-known traditional herb Solanum xanthocarpum is widely used in India for the management of different ailments including urolithiasis. This study was designed to rationalize the use of Solanum xanthocarpum in kidney stone and to investigate its mechanism of action. Materials and methods: The saponin rich fraction prepared from fruits of Solanum xanthocarpum (SXS) was evaluated for antiurolithiatic activity by in vitro and in vivo studies. In ethylene glycol (EG, 0.75% in drinking water for 28 days) induced urolithiasis model, two different experimental doses (20mg/kg and 40mg/kg, p.o., for 28 days) of saponin rich fraction were selected by dose fixation study. After 28 days, various biochemical parameters were measured in urine, serum and kidney homogenate. Kidneys were also subjected to histopathological analysis. Results: In vitro calcium oxalate crystal (CaOx) nucleation as well as aggregation was inhibited in artificial urine solution by SXS. The lithogenic treatment caused polyuria, damage renal function and oxidative stress, manifested as increased malondialdehyde, depleted reduced glutathione and decreased antioxidant enzyme catalase activities of the kidneys, which were prevented by simultaneous administration with SXS. Lithogenic treatment also caused crystalluria, hyperoxaluria, hypercalciuria, hypocitrauria, and hypomagnesaemia. Deposition of CaOx in renal tissue and cellular injury were seen in histopathology. Co-administration of SXS had potential to prevent these pathological changes due to lithogenic treatment. Moreover, SXS raised level of glycosaminoglycan, a stone inhibitor macromolecule found in urine which decreased. Conclusion: The antiurolithiatic activity in Solanum xanthocarpum is mediated possibly through the inhibition of CaOx crystal formation and its effect on the urinary concentration of stone-forming constituents and nephrolithiasis inducing factors and this study rationalizes its medicinal use in urolithiasis. [ABSTRACT FROM AUTHOR]

A spectrofluorimetric method using fluorescent carbon dots (CDs) was developed for the selective detection of azelnidipine (AZEL) pharmaceutical in the presence of other drugs. In this study, N-doped CDs (N-CDs) were synthesized through a single-step hydrothermal process, using citric acid and urea as precursor materials. The prepared N-CDs showed a highly intense blue fluorescence emission at 447 nm, with a photoluminescence quantum yield of ~21.15% and a fluorescence lifetime of 0.47 ns. The N-CDs showed selective fluorescence quenching in the presence of all three antihypertensive drugs, which was used as a successful detection platform for the analysis of AZEL. The photophysical properties, UV-vis light absorbance, fluorescence emission, and lifetime measurements support the interaction between N-CDs and AZEL, leading to fluorescence quenching of N-CDs as a result of ground-state complex formation followed by a static fluorescence quenching phenomenon. The detection platform showed linearity in the range 10-200 μg/ml (R 2  = 0.9837). The developed method was effectively utilized for the quantitative analysis of AZEL in commercially available pharmaceutical tablets, yielding results that closely align with those obtained from the standard method (UV spectroscopy). With a score of 0.76 on the 'Analytical GREEnness (AGREE)' scale, the developed analytical method, incorporating 12 distinct green analytical chemistry components, stands out as an important technique for estimating AZEL., (© 2024 John Wiley & Sons Ltd.)

Purpose: To develop controlled release osmotic pump tablets (COPT) of glipizide (GZ) solid dispersion (SD)., Methods: In elementary osmotic pump (EOP) tablets, an osmotic core with the drug is surrounded by a semi-permeable membrane which is drilled with a delivery orifice. COPT tablets eliminate the need of drilling process as controlled release can be achieved by the presence of osmogen in the coating. Poorly water soluble drug molecule cannot give satisfactory drug release hence GZ solid dispersion was prepared in the present study. The SDs having different ratio of drug to Poloxamer (PXM) 188 were prepared by hot melt method and optimized by solubility study, drug content estimation and in vitro dissolution study. Effect of two independent variables, amount of osmogen (potassium chloride) and hydrophilic polymer (polyethylene oxide WSR 303), were investigated using 3(2) factorial design. Core and coated tablets were evaluated for pharmacotechnical parameters. In-vitro drug release profiles of COPT tablets were compared with marketed with push-pull osmotic pump tablet, Glucotrol XL., Results: Prepared core and coated tablets showed acceptable pharmacotechnical parameters. Drug release was directly proportional to initial level of hydrophilic polymer, but inversely related to the osmogen, confirming osmotic mechanism. Zero order drug release pattern was achieved which was comparable to marketed product., Conclusion: Novel oral controlled release of glipizide was successfully achieved by incorporating glipizide solid dispersion into osmotic system.

The present study focuses on the formulation of ethosomal gel of ropinirole hydrochloride (ropinirole HCl), an anti-Parkinsonian drug, for delivery as a carrier for transdermal application. The ethosomes were prepared using different concentrations of phospholipids (2-5 % w/v), ethanol (20-50 % w/v), ropinirole HCl (5 % w/v) and water. They were optimized using 3(2) full factorial designs to study the effect of independent variables, concentrations of ethanol and lecithin on dependent variables, entrapment efficiency and in-vitro drug release at 24 hrs. The drug release profile exhibited Higuchi's and zero order kinetics. From the regression analysis, it was observed that independent variables had significant effect on response variables. Formulations were optimized using contour plot and response surface plot. The optimized formulation was found to be RS10 containing 30 % w/v ethanol and 4% w/v lecithin. The optimized formulation was evaluated for assay, particle characteristics, zeta potential, skin retention and stability. Ethosomal gel was prepared by incorporation of optimized ethosomal suspension into gel base. The ethosomal gel was characterized for physical appearance, pH, content uniformity, rheological behaviour, skin-retention, in-vitro and in-vivo drug release and stability. From the results it can fairly be concluded that ethosomes are capable of delivering ropinirole hydrochloride into systemic circulation by transdermal route. The amounts thus delivered are also equitable to those delivered orally and are delivered at a rate slow enough to achieve longer blood levels.

The present study was carried out with a view to enhance dissolution rate of poorly water-soluble drug glipizide (GZ) (BCS class II) using polyethylene glycol (PEG) 6000, PEG 8000 and poloxamer (PXM) 188 as carriers. Solid dispersions (SDs) were prepared by melting method using different ratios of glipizide to carriers. Phase solubility study was conducted to evaluate the effect of carrier on aqueous solubility of glipizide. SD was optimized by drug content estimation and in vitro dissolution study and optimised SD was subjected to bulk characterization, Scanning electron microscopy (SEM), Fourier transformation infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC) and X-ray diffraction study (XRD). Preclinical study was performed in mice to study the decrease in blood glucose level from prepared SD compared with pure drug. Due to high solubility and drug release, PXM 188 in weight ratio of 1:2 was optimized. Decrease in blood glucose level in mice from SD was significantly higher (p < 0.05) compared to pure glipizide. Thus, solid dispersion technique can be successfully used for the improvement of the dissolution profile of GZ.