BUDESONIDE COMPATIBILITY STUDY WITH EXCIPIENTS FOR PREPARATION OF NANOPARTICLE

Objective: As a condition of acceptance and approval of any pharmaceutical product, stability studies ensuring the durability of the consistency, stability and efficacy of the product during the shelf life are taken into consideration. These studies should be conducted according to the guidelines provided by ICH, WHO and other agencies as intended. Methods: The aim of this research was to evaluate the stability of the budesonide solution in some solutions and excipients and to further study the production of budesonide nanoparticles. In order to study the Budesonide stability mixture of solvent and polymers were used. To study the effect of temperature and relative humidity on the stability of budesonide preparations, prepared mixtures were stored under Accelerated (40 °C±2 °C/75 percent RH±5 percent RH), Intermediate (30 °C±2 °C/65 percent RH±5 percent RH), Long-term (25 °C±2 °C/60 percent RH±5 percent RH) and at 2-8 °C. Results: Budesonide showed good compatibility at defined stability conditions in one month. Such type of preformulation compatibility study is necessary in preparation of nanoparticles. Conclusion: It would be helpful in screening and identifying a suitable solvent, polymer and mixture at a desired concentration

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 a Reliable Method for the Spectrophotometric Determination of Palladium(II) with o-Methoxyphenyl Thiourea: Separation of Palladium from Associated Metal Ions

A simple and sensitive method is described for the solvent extraction and spectrophotometric  determination of palladium(II) using low concentrations of o-methoxyphenyl thiourea (OMePT). Trace concentrations of palladium(II) were quantitatively extracted when equilibrated withOMePTin chloroformat 1.0 mol  L–1hydrochloric acid media for 10 s. The absorbance of a yellow coloured palladium(II)-OMePT complex was measured at 325 nm. The palladium(II)-OMePT complex was stable for more than 72 h. The composition of extracting species was 1:1, determined by mole ratio, Job’s continuous variation method and it was confirmed by a log–log plot. Beer’s law was obeyed up to 15.0 μg mL–1. The molar absorptivity and Sandell’s sensitivity were 3.38 × 103 L mol–1 cm–1 and 0.031 μg cm–2, respectively. The method was free from a large number of interferences from cations and anions. The method was applied for separation of palladium(II) from multi-component mixtures and synthetic mixtures corresponding to alloy.KEYWORDS: Solvent extraction, spectrophotometric determination, o-methoxyphenyl thiourea, palladium

APPLICATION OF A VALIDATED STABILITY-INDICATING HPTLC METHOD FOR SIMULTANEOUS QUANTITATIVE DETERMINATION OF CANDESARTAN CILEXETIL AND HYDROCHLOROTHIAZIDE IN PHARMACEUTICAL DOSAGE FORM

Objective: To develop and validate stability indicating HPTLC method for simultaneous quantitative determination of candesartan cilexetil (CDT) and hydrochlorothiazide (HCT) in pharmaceutical dosage form.Methods: The present study deals with development and validation of stability indicating HPTLC method for simultaneous estimation of CDT and HCT. Chromatographic separation was performed on aluminum plate precoated with Silica Gel 60 F254 using toluene: chloroform: ethanol: glacial acetic acid (2:7:1:0.1 v/v) as mobile phase. The wavelength selected for densitometry scanning was 270 nm. Regression plots revealed linear relationships in the concentration range of 500-5000 and 400-2000 ng/band for CDT and HCT respectively. The correlation coefficient of calibration curves was found to be more than 0.99 for both analytes.Results: The chromatographic conditions gave compact spots at Rf value (±SD) 0.12 (±0.01) and 0.70 (±0.02) for HCT and CDT respectively. The method was validated as per International Conference on Harmonization (ICH) guidelines, demonstrating to be accurate and precise within the corresponding linearity range of titled analytes. Inherent stability of these drugs was studied by exposing drug substances to various stress conditions as per ICH guidelines namely oxidative, photolysis and hydrolytic conditions under different pH. Relevant degradation was found to take place under these conditions.Conclusion: A new simple, accurate, precise, sensitive and economic stability-indicating HPTLC method has been developed and validated for the simultaneous determination of CDT and HCT in pharmaceutical dosage form. The proposed method can be used for the routine estimation of CDT and HCT in bulk and formulation and can be employed for stability-indicating analysis.Keywords: Candesartan cilexetil, Hydrochlorothiazide, HPTLC, Stability indicating method, Forced degradation, Stress studies, Validatio

PHYTOCHEMISTRY AND PHARMACOLOGY OF PTEROCARPUS SANTALINUS AND ITS ROLE IN DERMATOLOGY

The review provides an updated overview of the phytochemical and pharmacological studies on Pterocarpus santalinus. It briefs on the synergistic interactions of P. santalinus with other medicinal plants and its use in Ayurvedic formulations. Phytochemical analysis suggests the presence of triterpenoids, steroids, flavonoids, and phenolic acids. The phytoconstituents and related pharmacological activities of various parts of P. santalinus include antifungal, anticholinesterase, antidiabetic, antibacterial, antipyretic, anti-inflammatory, anticancer, and antiulcer. Literature survey highlights the dermatological applications of the phytoconstituents such as pterostilbene, savinin, and betulin as potential leads for anti-aging, ultraviolet rays (UV-B) protective, and wound healing effects. Undoubtedly, P. santalinus has wide therapeutic value. The dermatologically significant phytoconstituents, namely, pterostilbene, cedrol, savinin, lupeol, betulin, β-eudesmol, and α-bisabolol, if isolated and used in dermatological formulations, can show promising skin protective effect. The data were compiled using scientific databases, namely, Google Scholar and PubMed, the data made available specifically from 2010 to 2021

Antioxidant and hepatoprotective activity of Cordia macleodii leaves

AbstractThis investigation was undertaken to evaluate ethanolic extract of Cordia macleodii leaves for possible antioxidant and hepatoprotective potential. Antioxidant activity of the extracts was evaluated by four established, in vitro methods viz. 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical scavenging method, nitric oxide (NO) radical scavenging method, iron chelation method and reducing power method. The extract demonstrated a significant dose dependent antioxidant activity comparable with ascorbic acid. The extract was also evaluated for hepatoprotective activity by carbon tetrachloride (CCl4) induced liver damage model in rats. CCl4 produced a significant increase in levels of serum glutamate pyruvate transaminase (GPT), serum glutamate oxaloacetate transaminase (GOT), Alkaline Phosphatase (ALP) and total bilirubin. Pretreatment of the rats with ethanolic extract of C. macleodii (100, 200 and 400mg/kg po) inhibited the increase in levels of GPT, GOT, ALP and total bilirubin and the inhibition was comparable with Silymarin (100mg/kg po). The present study revealed that C. macleodii leaves have significant radical scavenging and hepatoprotective activities

Solubility enhancement, physicochemical characterization and formulation of fast-dissolving tablet of nifedipine-betacyclodextrin complexes

Este estudo teve por objetivo principal incrementar a dissolução do nifedipino, fármaco pouco solúvel em água, por meio de sua complexação com β-ciclodextrina e estudar o efeito do método de preparação sobre o perfil de dissolução in vitro. A razão estequiométrica, determinada por ensaio de solubilidade de fase, para a complexação de nifedipino por inclusão em β-ciclodextrina foi 1:1. O complexo binário foi preparado por diferentes métodos, sendo caracterizado utilizando-se difratometria de raios X (XRD), calorimetria diferencial de varredura (DSC) e espectroscopia no infravermelho com transformada de Fourier (FT-IR). Realizou-se estudo de solubilidade de saturação para avaliar o incremento da solubilidade do nifedipino. O complexo otimizado foi formulado em comprimidos de dissolução rápida preparados por compressão direta, nos quais se utilizaram os superdesintegrantes Doshion P544, amido pré-gelatinizado, crospovidona, amidoglicolato de sódio e croscarmelose sódica. Os comprimidos, que foram avaliados quanto à friabilidade, dureza, variação de peso, desintegração e dissolução in vitro, apresentaram taxa de dissolução superior à do nifedipino pura.The main objective of the study was to enhance the dissolution of nifedipine, a poorly water soluble drug by betacyclodextrin complexation and to study the effect of the preparation method on the in vitro dissolution profile. The stoichiometric ratio determined by phase solubility analysis for inclusion complexation of nifedipine with β-cyclodextrin was 1:1. Binary complex was prepared by different methods and was further characterized using XRD, DSC and FT-IR. A saturation solubility study was carried out to evaluate the increase in solubility of nifedipine. The optimized complex was formulated into fast-dissolving tablets by using the superdisintegrants Doshion P544, pregelatinized starch, crospovidone, sodium starch glycolate and croscarmellose sodium by direct compression. Tablets were evaluated for friability, hardness, weight variation, disintegration and in vitro dissolution. Tablets showed an enhanced dissolution rate compared to pure nifedipine

Formulation and in vitro evaluation of taste-masked oro-dispersible dosage form of diltiazem hydrochloride

O cloridrato de diltiazem é bloqueador do canal de cálcio geralmente indicado para o tratamento de angina e de hipertensão e é extensamente biotransformado devido ao metabolismo hepático. A formulação do cloridrato de diltiazem em orodispersão pode prover rápida liberação com maior biodisponibilidade. O sabor amargo do fármaco deve ser mascarado para ser formulado em forma palatável. No presente trabalho tentou-se mascarar o sabor pela técnica de complexação, com uma orodispersão, usando superdesintegrantes, como Doshio P544, crospivodina (CP) e glicolato de amido sódico (SSG). Os complexos de cloridrato de diltiazem com β-CD (razão molar 1:1) foram preparados por mistura, coevaporação, comoagem, liofilização e métodos de fusão. A solubilidade de fase mostrou estabilidade constante de 819,13 M-1. Os complexos de inclusão preparados foram avaliados com relação ao mascaramento do sabor e caracterizados por IV, Difração de Raios X e DSC. Empregando-se o fármaco complexado com β-CD, prepararam-se comprimidos dispersíveis e avaliaram-se os mesmos quanto à dureza, friabilidade, variação de peso, espessura, tempo de desintegração (DT), taxa de dissolução e sabor. Formulações com 4% de Doshion, 8% de CP e 4% de SSG mostraram DT de 0,54, 0,35 e 1,23 minutos, respectivamente.Diltiazem hydrochloride is a calcium channel blocker generally indicated for the treatment of angina and hypertension, and it is extensively metabolized due to the hepatic metabolism. Formulation of diltiazem hydrochloride into an oro-dispersible dosage form can provide fast relief with higher bioavailability. The bitter taste of the drug should be masked to formulate it in a palatable form. In the present work, an attempt was made to mask the taste by complexation technique, with a formulation into an oro-dispersible dosage form, using superdisintegrants Doshion P544, crospovidone (CP) and sodium starch glycolate (SSG). The complexes of diltiazem hydrochloride with β-CD (1:1 molar ratio) were prepared by kneading, co-evaporation, co-grounding, freeze-drying and melting methods. Phase solubility showed stability constant 819.13M-1. Prepared inclusion complexes were evaluated for taste masking and characterized by I.R, XRD, DSC. Using the drug β-CD complex, oro-dispersible tablets were prepared and evaluated for hardness, friability, weight variation, thickness, disintegrating time (DT), dissolution rate and taste. Formulations with 4 % Doshion, 8 % CP and 4 % SSG showed DT of 0.54, 0.35 and 1.23 minutes, respectively