EVALUATING THE BEST POLYETHYLENE GLYCOL AS SOLID DISPERSION CARRIER BY TAKING ETORICOXIB AS A MODEL DRUG

Objective: The main objective of the current research is focused in discovering the best polyethylene glycol (PEG) as solid dispersion carrier using etoricoxib (ECB) as a model drug. Methods: Varieties of PEG, namely PEG - 3350, PEG - 4000, PEG - 6000, PEG - 8000, and PEG - 20000, were evaluated as a carrier for making ECB solid dispersions. ECB:PEG was taken in the ratios of 1:1, 1:2, 1:4, and 1:6. The solid dispersions were prepared by microwave fusion method and compressed using 8 station tablet compression machine. The fabricated solid dispersion tablets were tested for physicochemical characteristics and drug release rates. The release of ECB from the prepared solid dispersions was further analyzed kinetically using the first order and Hixson-Crowell’s plots. Results: All the solid dispersion batches were shown satisfactory physicochemical characteristics. ECB solid dispersion batches with PEG - 6000 showed good solubility in distilled water (up to 2.29±0.01 μg/ml) and in 0.1 N HCl (up to 2.18±0.01 μg/ml) when compared with ECB alone (0.21±0.01 μg/ml and 0.32±0.01 μg/ml). The prepared solid dispersions with PEG 6000 are shown good ECB release. Conclusion: Among PEG carriers, PEG - 6000 was found to be the best carrier for increasing the solubility and release rate of ECB form the solid dispersions compared to PEG - 3350, PEG - 4000, PEG - 8000, and PEG - 20000

Impact of Azadirachta indica Fruit Mucilage on particle size and swelling index in Central Composite Designed Acyclovir mucoadhesive microspheres

الهدف من الدراسة هو التحقيق في أصول اللصق المخاطي لصمغ الفاكهة A. indica (Azadirachta indica) من خلال دمجه في مجهرية مخاطية مع Acyclovir (AVR) كدواء نموذجي. أجريت الدراسة للتحقق من تأثير نسبة الصمغ على حجم الحبيبات ومؤشر الانتفاخ. تم عمل تسع دفعات من كريات اللصق المخاطي AVR بنسب متفاوتة من حمض البولي أكريليك 934P وصمغ الفاكهة A. إنديكا (AIFM). وتم تصميم مركب مركزي مع برنامج خبير التصميم للتحقق من تأثير المتغيرات التابعة (الصمغ الإنديكا ومستويات حمض بولي أكريليك 934 ف) على حجم الجسيمات ومؤشر الانتفاخ كاستجابة. كجزء من دراسات التوافق ، تم فحص الدفعات لمعرفة القيود المادية ومحتويات AVR والتحرير. تم العثور على حجم الجسيمات لتكون 35.2 ± 0.3-48.1 ± 0.6 ميكرومتر. في الدفعة B-1 ، كان حجم الجسيم أقل مقارنة بالحجم الأكبر في B-5. ووجدت الدراسة أن حجم الجسيمات ومؤشر الانتفاخ يعتمدان على نسب AIFM وحمض بولي أكريليك. اكتشف البحث أن AVR تم إطلاقه بشكل منهجي بطريقة خاضعة للرقابة ، وأن فعالية الالتحام المخاطي ومحتوى الدواء  والقيود الأخرى كانت جيدة. كما اتضح ان الأسيكلوفير قادر على توصيل دواء جيد للمعدة عن طريق حمض بولي أكريليك 934P ومعزز بصمغ فاكهة A. إنديكا عند تحضيره ككرات مخاطية مجهرية. يكشف الفحص المجهري الإلكتروني أن الكرات المجهرية كانت كروية ذات سطح أملس إلى حد ما.The drive of this exploration is to investigate the mucoadhesive assets of A. indica (Azadirachta indica) fruit mucilage by incorporating it into mucoadhesive microspheres with Acyclovir (AVR) as a model drug. The study was performed to check the impact of the mucilage proportion on particle size and swelling index. Nine batches of AVR mucoadhesive microspheres were made with varying proportions of Polyacrylic acid 934P and A. indica fruit mucilage (AIFM). A central composite design with design expert software to check the impact of dependent variables (A. indica mucilage and Polyacrylic acid 934 P levels) on particle size and swelling index as a response. As part of congeniality studies, the batches were examined for their physical constraints, AVR contents, and liberation. The particle size was found to be 35.2±0.3-48.1±0.6μm. In batch B-1, the particle was least sized compared to the larger size in B-5. The investigation found that the particle size and the swelling index depended on AIFM and Polyacrylic acid proportions. The research discovered that AVR was systematically released in a controlled manner and that the entrapment efficacy, mucoadhesion, drug content, and other constraints were found to be good. Acyclovir is capable of good stomach-specific drug delivery by Polyacrylic acid 934P and enhanced by A. indica fruit mucilage when prepared as mucoadhesive microspheres. Scanning electron microscopy reveals that the microspheres were spherical with a fairly smooth surface

Pushing Limits: Exploring Torsemide's Potential Through In-Vitro Mucoadhesive Buccal Delivery Characterization

This study focuses on developing and evaluating mucoadhesive buccal tablets containing Torsemide, utilizing HPMC K-100, Xanthan Gum, and chitosan polymers at varying concentrations. Physicochemical parameters were well-maintained according to Indian Pharmacopeia standards. Swelling indices ranged from 201.75% to 241.85% over 8 hours, with suitable tablet pH (6.8-6.9) for buccal administration. Mucoadhesive strengths (18.00-27.33 g) varied with polymer concentration. Batch 6 displayed sustained Torsemide release (73.73% at 8 h), supported by optimized swelling index and mucoadhesive strength. Formulation F6, combining Xanthan Gum and Chitosan, emerged as optimal. Dissolution followed zero-order kinetics, fitting the Korsmeyer-Peppas model, indicating a diffusion-based, non-Fickian mechanism. No Torsemide-excipient interactions were observed through Fourier Transform Infrared Spectroscopy. This study successfully designed controlled-release mucoadhesive buccal tablets, influenced by polymer behavior and concentration, advancing drug delivery systems

Preparation of Fluconazole β-Cyclodextrin Complex Ocuserts: In Vitro and In Vivo Evaluation

The main purpose of the present study was to develop ocuserts of Fluconazole β-CD (beta-cyclodextrin) complex and to evaluate both in vitro and in vivo. Fluconazole was made complex with β-CD, and the release rate was controlled by HPMC K4M and ethyl cellulose polymers using dibutyl Phthalate as permeability enhancer. Drug-polymer interactions were studied by Fourier transform infrared spectroscopic studies. The formulated ocuserts were tested for physicochemical parameters of in vitro release and in vivo permeation in rabbits. The optimized formulations (F-5 and F-8) were subjected to stability studies. The formulated ocuserts were found to have good physical characters, thickness, diameter, uniformity in weight, folding endurance, less moisture absorption, and controlled release of drug both in vitro and in vivo. The optimized formulations retained their characteristics even after stability studies. The study clearly showed that this technique was an effective way of formulating ocuserts for retaining the drug concentration at the intended site of action for a sufficient period of time and to elicit the desired pharmacological response

HUMAN ORGANIC SOLUTE TRANSPORTERS UTTERED IN SMALL INTESTINE, LIVER, AND KIDNEY FOR HOMEOSTASIS

The transporters participate in a significant role in drug absorption, distribution, metabolism, and elimination. Transporters are of efflux and influx type, need ATP-binding sites for their in and out movement across the cell membrane. These transporters play an important role in allowing or opposing the drugs into the cells, results in non-linearity in drug pharmacokinetics. A wide range of transporters was discovered; among them, organic solute transporters (OST) play a key role in drug absorption and disposition. Organic solute transporters is a heteromeric transporter localized to the basolateral of epithelial cells. It is the primary efflux bile acid transporter in the intestine of mammals

Rp-HPLC Method for Simultaneous Estimation of Levocetirizine Dihydrochloride and Montelukast Sodium in tablets

A simple, selective and sensitive reverse phase high performance liquid chromatography (Rp-HPLC) method has been proposed for the simultaneous quantitative determination of levocetirizine dihydrochloride (LEV) and Montelukast sodium (MON) in pure form as well as in its pharmaceutical formulation. The chromatography was carried out on Waters C18 analytical column (15cm × 4.6 mm, 5µ) using a mobile phase of methanol: water (75:25 v/v). The flow rate was 1.0 ml/min with detection at 235 nm. The retention time of LEV and MON were found to 2.88 and 3.83 min respectively. The linearity for LEV and MON were in the range of 50-150 µg/mL and 100- 300 µg/mL respectively. The recoveries of LEV and MON were found to be 100.00% and 99.00%, respectively. The proposed method was validated and successfully applied to the estimation of LEV and MON in combined tablet dosage forms

DESIGNING AND EVALUATION OF DICLOFENAC SODIUM SUSTAINED RELEASE MATRIX TABLETS USING HIBISCUS ROSA-SINENSIS LEAVES MUCILAGE

ABSTRACT The main objective of the present investigation was to design matrix tablets of Diclofenac sodium using Hibiscus rosa-sinensis leaves mucilage and to study its release retardant activity in prepared sustained release formulations. Hibiscus rosa-sinensis leaves were evaluated for physicochemical properties. Different matrix tablets of Diclofenac sodium Hibiscus rosa-sinensis leaves mucilage were formulated. The matrix tablets found to have better uniformity of weight, hardness, friability and drug content with low deviated values. The swelling behavior, release rate characteristics and the in-vitro dissolution study proved that the dried Hibiscus rosa-sinensis leaves mucilage can be used as a matrix forming material for preparing sustained release matrix tablets. The kinetics of drug release from selected DHR-5 formulation followed zero order. It was concluded that Hibiscus rosa-sinensis leaves mucilage can be used as an effective matrix forming polymer, to sustain the release of Diclofenac sodium from the formulation

Antioxidant rich flavonoids from Oreocnide integrifolia enhance glucose uptake and insulin secretion and protects pancreatic β-cells from streptozotocin insult

<p>Abstract</p> <p>Background</p> <p>Insulin deficiency is the prime basis of all diabetic manifestations and agents that can bring about insulin secretion would be of pivotal significance for cure of diabetes. To test this hypothesis, we carried out bioactivity guided fractionation of <it>Oreocnide integrifolia </it>(Urticaceae); a folklore plant consumed for ameliorating diabetic symptoms using experimental models.</p> <p>Methods</p> <p>We carried out bioassay guided fractionation using RINmF and C2C12 cell line for glucose stimulated insulin secretion (GSIS) and glucose uptake potential of fractions. Further, the bioactive fraction was challenged for its GSIS in cultured mouse islets with basal (4.5 mM) and stimulated (16.7 mM) levels of glucose concentrations. The Flavonoid rich fraction (FRF) was exposed to 2 mM streptozotocin stress and the anti-ROS/RNS potential was evaluated. Additionally, the bioactive fraction was assessed for its antidiabetic and anti-apoptotic property <it>in-vivo </it>using multidose streptozotocin induced diabetes in BALB/c mice.</p> <p>Results</p> <p>The results suggested FRF to be the most active fraction as assessed by GSIS in RINm5F cells and its ability for glucose uptake in C2C12 cells. FRF displayed significant potential in terms of increasing intracellular calcium and cAMP levels even in presence of a phosphodiesterase inhibitor, IBMX in cultured pancreatic islets. FRF depicted a dose-dependent reversal of all the cytotoxic manifestations except peroxynitrite and NO formation when subjected <it>in-vitro </it>along with STZ. Further scrutinization of FRF for its <it>in-vivo </it>antidiabetic property demonstrated improved glycemic indices and decreased pancreatic β-cell apoptosis.</p> <p>Conclusions</p> <p>Overall, the flavonoid mixture has shown to have significant insulin secretogogue, insulinomimetic and cytoprotective effects and can be evaluated for clinical trials as a therapeutant in the management of diabetic manifestations.</p

Quantification of tapentadol in rat plasma by HPLC with photo diode array detection: Development and validation of a new methodology

Objective: The aim of the present study was to develop and validate a simple HPLC–PDA based method to quantify TAP in rat plasma. Several parameters both in the extraction and detection method were evaluated. The applicability of the method was determined by administering TAP orally to six albino Wister rats. Methods: The protocol yielded the expected pharmacokinetic results and plasma collected by retro orbital vein puncture at regular intervals. The mobile phase consisted of 0.1 M Dipotassium Phosphate buffer (pH 6.8) and acetonitrile in the ratio of 50:50 v/v with a flow rate of 1.2 mL min−1. The detection wavelength was 241.0 nm. TAP was extracted from the plasma using a mixture of Ethanol: Dichloro methane (70:30 v/v), which gave a recovery of 99.0–101.8%. Results: The linearity of the method for both tapentadol and tramadol demonstrated correlation coefficients (R2) above 0.99 and linear range from 9.775 to 5024.376 ng/mL for tapentadol and 100 to 500,000 ng/mL for tramadol. The lower limits of quantitation (LLOQ) were found to be 9.775 ng/mL for tapentadol, and the upper limit of quantitation (ULOQ) was determined to be 5024.376 ng/mL. The chromatographic runs were specific with no interfering peaks at the retention times of the analyte (tapentadol) and ARE (tramadol), as confirmed by HPLC–PDA experiments. Conclusion: In conclusion, this was a simple and effective method using HPLC–PDA to detect TAP in plasma, which may be useful for future pharmacokinetic studies

A Novel Mucilage from Ficus glomerata Fruits for Transdermal Patches: Taking Indomethacin as a Model Drug: A novel mucilage from Ficus glomerata fruits

The present study was performed to explore the matrix property of Ficus glomerata fruit mucilage for making transdermal patches. The mucilage was evaluated for its physicochemical properties. Various transdermal patches of indomethacin were prepared by solvent evaporation technique using different proportions of F. glomerata fruit mucilage. The compatibility studies between indomethacin and F. glomerata fruit mucilage revealed that there were no negative interactions between indomethacin and the mucilage. The formulated patches were evaluated for physical properties, pre-formulary, post-formulary and skin irritation characteristics and they were found satisfactory. The experimental results shows that the drug release from the patches delayed in controlled manner as the proportionof F. glomerata fruit mucilage increased. The accelerated stability studies proved that the formulated patches were stable at stressed storage conditions. It was concluded that F. glomerata fruit mucilage can be used as polymer for making transdermal patches