scholarly journals Enhanced Dissolution of Sildenafil Citrate Using Solid Dispersion with Hydrophilic Polymers: Physicochemical Characterization and In Vivo Sexual Behavior Studies in Male Rats

Polymers ◽  
2021 ◽  
Vol 13 (20) ◽  
pp. 3512
Author(s):  
Mohammed F. Aldawsari ◽  
Md. Khalid Anwer ◽  
Mohammed Muqtader Ahmed ◽  
Farhat Fatima ◽  
Gamal A. Soliman ◽  
...  
Keyword(s):  
Sexual Behavior ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Hydrophilic Polymers ◽  
Sildenafil Citrate ◽  
Male Rats ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Onset Of Action

Sildenafil citrate (SLC) is a frequently used medication (Viagra®) for the treatment of erectile dysfunction (ED). Due to its poor solubility, SLC suffers from a delayed onset of action and poor bioavailability. Hence, the aim of the proposed work was to prepare and evaluate solid dispersions (SDs) with hydrophilic polymers (Kolliphor® P188, Kollidon® 30, and Kollidon®-VA64), in order to enhance the dissolution and efficacy of SLC. The SLC-SDs were prepared using a solvent evaporation method (at the ratio drug/polymer, 1:1, w/w) and characterized by Differential Scanning Calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), Scanning electron microscope (SEM), drug content, yield, and in vitro release studies. Based on this evaluation, SDs (SLC-KVA64) were optimized, with a maximum release of drug (99.74%) after 2 h for all the developed formulas. The SDs (SLC-KVA64) were further tested for sexual behavior activity in male rats, and significant enhancements in copulatory efficiency (81.6%) and inter-copulatory efficiency (44.9%) were noted in comparison to the pure SLC drug, when exposed to the optimized SLC-KVA64 formulae. Therefore, SD using Kollidon®-VA64 could be regarded as a potential strategy for improving the solubility, in vitro dissolution, and therapeutic efficacy of SLC.

FORMULATION AND EVALUATION OF SOLID LIPID NANOPARTICLES CONTAINING CAFFEINE TO TREAT CLINICAL MASTITIS

2020 ◽  
pp. 72-78
Author(s):  
AMRUTHA U ◽  
SUSHMITHA B ◽  
SHAIK RUBINA ◽  
PADMINI IRIVENTI
Keyword(s):  
Sustained Release ◽  
Solid Lipid Nanoparticles ◽  
Evaluation Studies ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Clinical Mastitis ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Solid Lipid

Objective: The objective of the present study was to formulate and evaluate caffeine loaded solid lipid nanoparticles (SLNs) in the treatment of clinical mastitis. Methodology: These were prepared by homogenization technique using cholesterol, tween 80, and chloroform as excipients. Preformulation studies such as ultraviolet spectrophotometry, Fourier transform infrared (FTIR), and differential scanning calorimetry (DSC) were performed for the drug. Entrapment efficiency and in vitro dissolution studies were carried out for prepared SLN’s and the optimum formulation (F2) was taken for further studies such as FTIR, DSC, scanning electron microscopy, particle size, and zeta potential analysis. Results: Obtained results stated that prepared SLNs are roughly spherical in nature and are in nanorange. These were incorporated in Carbopol gel and further evaluation studies such as pH, spreadability, viscosity, homogeneity, and in vitro drug diffusion studies were carried out. All the results obtained state that prepared nanogel has shown sustained release of drug. The antimicrobial study was carried out using Staphylococcus aureus and it was confirmed by appearance of the zone of inhibition. Conclusion: Nanogel that contains Caffeine SLNs with 1:2 ratio drug:lipid has shown good in vitro release. Sustained release of Caffeine drug till 12 h was achieved by delivering it in the form of nanogel.

scholarly journals Formulation and Evaluation of Tablets Containing Fenugreek Extract Using Sodium Starch Glycolate as Super Disintegrant

2021 ◽  
pp. 47-53
Author(s):  
Divya Jyothi
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Antidiabetic Activity ◽  
Wet Granulation ◽  
Onset Of Action ◽  
Plant Materials ◽  
Sodium Starch Glycolate ◽  
Tablet Formulations

The present work is aimed to formulate the tablets containing fenugreek extract as drug by wet granulation method. Further the effect of Sodium Starch Glycolate as super disintegrant on disintegration and drug release was studied. Fenugreek extract contains mucilage which retards the disintegration of tablets and hence shows slower drug release. Hence in order to improve disintegration and thereby in vitro drug release, Sodium Starch Glycolate was used as super disintegrant. Tablet formulations were prepared without the SSG (Conventional-F1) and also with sodium starch glycolate (F2-F4) by wet granulation method. Assessment of flow properties of granules, physicochemical characterization of tablet formulations was carried out. Fenugreek is widely used for its antidiabetic activity which is attributed to mainly to the presence of an alkaloid Trigonelline. Hence in vitro release study of trigonelline was carried out which showed that the percentage release from F1 and F2 was found to be 58.12±4.49 and 99.08±0.01 respectively after 6 hrs. This study concludes that tablet formulation of fenugreek seed extracts with super disintegrants will be more desirable, advantageous and therapeutically more beneficial than incorporating the direct plant materials for the treatment of diabetes for faster onset of action.

scholarly journals FORMULATION AND EVALUATION OF LIQUISOLID COMPACTS OF LORNOXICAM

2019 ◽  
pp. 33-37
Author(s):  
Asma Azaruddin Mokashi ◽  
SNEHALATA L. GAIKWAD
Keyword(s):  
Dissolution Rate ◽  
Drug Concentration ◽  
In Vitro Release ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Spectra Analysis ◽  
X Ray ◽  
Liquisolid Compacts

Objective: Objective of the present investigation was to enhance the solubility and dissolution rate of poorly water-soluble drug lornoxicam using liquisolid technique with comparative determination of in vitro release profile of liquisolid compacts and conventional formulation of lornoxicam. Methods: Formulation was prepared by a liquisolid technique using different drug concentration in a liquid vehicle and different carrier/coating ratio. Prepared liquisolid compact was evaluated for Fourier transform infrared (FTIR) spectra analysis, differential scanning calorimetry (DSC), X-ray diffraction (P-XRD), scanning electron microscopy (SEM) and in vitro dissolution study. Results: The result showed that liquisolid compacts of lornoxicam displayed significantly higher drug release rate as compared to pure drug and conventional tablet prepared. The results of both DSC and X-ray crystallography indicated loss of crystallinity of the drug upon formulated into the liquisolid compact. Conclusion: Dissolution rate of the drug from liquisolid compacts was affected by changing the drug concentration and excipient ratio. The liquisolid technique appeared to be a promising approach for improving the dissolution of poorly soluble drug lornoxicam.

scholarly journals Evaluation of in vitro Dissolution Profile and Physicochemical Characterization of Polymer Based Formulations of Sparingly Soluble Rosuvastatin

2021 ◽  
Vol 20 (2) ◽  
pp. 199-211
Author(s):  
KM Yasif Kayes Sikdar ◽  
Md Shahoriar Nazir ◽  
Md Mahbubul Alam ◽  
Md Raihan Sarkar ◽  
Sad Al Rezwan Rahman
Keyword(s):  
Solid Dispersion ◽  
Fourier Transforms ◽  
Promising Result ◽  
Physicochemical Characterization ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Drug Release Profile ◽  
Scanning Calorimetry ◽  
Physical Mixing

Rosuvastatin (RVT) is a BCS class II antilipidemic crystalline drug, which exhibits low bioavailability due to its very poor aqueous solubility; therefore, it is challenging to develop a proper formulation of RVT. To enhance solubility and bioavailability of this API, an attempt has been made by implementing solid dispersion technique. Solid dispersion (SD) technique is a solubility enhancing technique where one or more active entities are dispersed in an inert medium (matrix or carrier) at solid state. In this study, different ratios of Kollicoat® IR (KIR) and Kollidon® 90F (KF90) polymers were used with API to prepare various formulations by physical mixing (PM) and SD approaches; here solvent evaporation technique was used whereas methanol was used as solvent which was completely evaporated from the homogenously dispersed system by placing in a water-bath at 60-65°C and then in oven for 30 minutes at 50 °C. Among the formulations, RVT-KF90 SD formulations showed the most promising result in in-vitro study in terms of drug release profile (78.04 – 99.21%) in comparison to pure RVT (63.1%) and physical mixing of RVT with those polymers. USP dissolution apparatus type II was used at 37°C ± 0.5°C with 50 rpm to conduct the in-vitro experiment. The experiment also unraveled that the dissolution of RVT improved with increasing the amounts of polymers. Subsequently, stability of the developed formulations was conducted by Fourier transforms infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) as well as scanning electron microscopy (SEM). The results obtained from FTIR ensured no involvement of any significant drug-excipient interaction. Moreover, the DSC study signified thermal stability at high temperature. Besides, the SEM micrograph illustrated homogenous distribution of RVT in the polymer and transformation of crystal-like RVT into amorphous formulations. Dhaka Univ. J. Pharm. Sci. 20(2): 199-211, 2021 (December)

scholarly journals IMPROVEMENT AND ESTIMATION OF ORALLY DISINTEGRATING TABLETS CONTAINING PILOCARPINE 2-HYDROXY PROPYL β-CYCLODEXTRIN INCLUSION COMPLEX BY RESPONSE SURFACE METHODOLOGY

2021 ◽  
pp. 217-223
Author(s):  
JOGABRATA TRIPATHY ◽  
SUBHASHREE SAHOO ◽  
AFRASIM MOIN ◽  
SIDDARAMAIAH ◽  
D. V. GOWDA
Keyword(s):  
Inclusion Complex ◽  
In Vitro Release ◽  
Test Methods ◽  
Dry Mouth ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Weight Variation ◽  
Orally Disintegrating Tablets

Objective: The study aimed to develop and evaluate an orally disintegrating tablet that contains pilocarpine and 2-hydroxy propyl β-cyclodextrin as an inclusion complex that is prepared by lyophilization used for treatment for dry mouth. Pilocarpine is utilized to treat dry mouth disorder. The inclusion complex lowers the taste of pilocarpine through the oral mucosa by the use of 2-hydroxy propyl β-cyclodextrin. Methods: The in vitro release from the insertion complex is also been studied. The parameters like differential scanning calorimetry (DSC), Fourier transformer infrared spectroscopy (FTIR), X-ray diffraction (XRD), and morphological study have been evaluated. The design of an experiment is carried out based on the concentration of croscarmellose sodium (CCS) and microcrystalline cellulose (MCC). Evaluation of the prepared orally disintegrating tablets have been carried out by different test methods like weight variation, thickness, drug content, disintegration, and in vitro dissolution study. Results: Orally disintegrating tablets are studied by utilizing the immediate pressure technique. Pilocarpine indicates the anhydrous crystalline medication, displaying sharp endothermic top at 120.2 °C, bend of 2-HPβCD demonstrates an exceptionally wide endothermal wonder among 55-100 °C for DSC. In pilocarpine spectra, characteristic band of aromatic C-H stretch at 3277 cm-1, C=C stretching at 1608 cm-1, C-N stretching at 1445 cm-1 and methoxy (CH3-O-) stretch at 2921 cm-1 was observed. The investigation shows that tablet hardness of 4.3N, breaking downtime of 12 sec and mean disintegration time is 1.562 min. Conclusion: The different diluents and super disintegrating have been applied for the quick elevation of dry mouth that helps us for patient compliance.

Characterization, Intestinal Absorption and Pharmacokinetics of Long-Circulating Nanoparticles Loaded with Panaxnotoginseng saponins

2013 ◽  
Vol 662 ◽  
pp. 227-232
Author(s):  
Guo Wei Zhao ◽  
Xu Long Chen ◽  
Xin Li Liang ◽  
Zheng Gen Liao ◽  
Chun Liu Wang ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Oral Administration ◽  
Intestinal Absorption ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Male Rats ◽  
Scanning Calorimetry ◽  
Time Curve ◽  
Vitro Release

The aim of the present study was to increase bioavailability after oral administration. In this study, Panaxnotoginseng saponins (PNS) was entrapped within the long-circulating nanoparticles (LCNs) by the multiple emulsion method. The PNS-LCNs were characterized in terms of size, zeta potential, morphology, thermal properties, drug entrapment efficiency (EE), and in vitro release of the PNS. In addition, the intestinal absorption of PNS-LCNs in vitro was investigated. The pharmacokinetics of PNS-LCNs following oral administration was determined over 72 h in male rats. It was found that the mean particle size and zeta potential of the PNS-LCNs were 147±4.5nm and −44.7±1.5mV, respectively, and the entrapment efficiency (EE) was 53.93%±0.69%. differential scanning calorimetry (DSC) indicated that PNS has different states in PNS-LCNs and original PNS. The release pattern of the PNS-LCNs followed the Weibull model. The release parameters (T50, TD) were observed to be higher for PNS-LCNs compared with original PNS (p< 0.01) in vitro release. The intestinal absorption study indicated that the intestinal permeability coefficient (Papp) of PNS-LCNs was higher than original PNS’s. The pharmacokinetics of PNS-LCNs was studied after oral administration to male rats, PNS-LCNs provided greater area under the concentration-time curve (AUC), higher plasma concentration (Cmax), longer mean residence time (MRT) and median time to maximum drug concentration (Tmax). LCNs could be used for improving permeability and increased bioavailability after oral administration of PNS.

scholarly journals Enhancement of the dissolution profile of the diuretic hydrochlorothiazide by elaboration of microspheres

2018 ◽  
Vol 83 (11) ◽  
pp. 1243-1259
Author(s):  
Oum Larbi ◽  
Haouaria Merine ◽  
Youssef Ramli ◽  
Fawzia Toumi ◽  
Kaddour Guemra ◽  
...  
Keyword(s):  
Ftir Spectroscopy ◽  
Release Kinetics ◽  
Drug Loading ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Xrd Analysis ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Scanning Calorimetry

Hydrochlorothiazide (HCTZ), which was developed and introduced in the late 1950s, is still one of the most frequently employed drugs in antihypertensive treatments. Its poor aqueous solubility is one of the reasons for its limited bioavailability after oral administration. The present paper provides details of the preparation of HCTZ-loaded microspheres by the solvent evaporation technique. A total of seven formulations were prepared using ethyl cellulose, poly(?-caprolactone) (PCL), ?-cyclodextrin (?-CD) and synthesized poly-(methyl methacrylate) (PMMA) of different molecular weights in different drug-to-carrier ratios in order to investigate their effect on the encapsulation efficiency and drug release kinetics. The prepared formulations were characterized by Fourier transform-infrared (FTIR) spectroscopy, powder X-ray diffractometry, differential scanning calorimetry, yield, drug loading, optical microscopy, surface morphology by scanning electron microscopy (SEM), and in vitro release studies in simulated gastrointestinal tract fluid. The loading efficiency was found in the range from 18?0.34 to 39?0.95 %. The microspheres were spherical, and the mean Sauter diameter (d32) of the obtained microparticles ranged from 26?0.16 to 107?0.58 ?m. The presence of the drug and polymer carriers in the microparticles was confirmed by FTIR spectroscopy and XRD analysis. In vitro dissolution studies showed that the release rate was largely affected by the characteristics of the microparticles, namely the particle size and the nature of the matrix. The release data are best fitted to the Higuchi model with high correlation coefficients (r?).

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

Design, Optimization and Evaluation of Fast-Dissolving Oral Films of Ropinirole

2018 ◽  
Vol 11 (1) ◽  
pp. 3958-3967
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Srinivas A
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Good Alternative ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Peg 4000 ◽  
Oral Films

The main objective of this study was to develop fast dissolving oral films of ropinirole HCl to attain quick onset of action for the better management of Parkinson’s disease. Twenty-seven formulations (F1-F27) of ropinirole oral dissolving films by solvent-casting method using 33 response surface method by using HPMC E15, Maltodextrin PEG 4000 by using Design of experiment software. Formulations were evaluated for their physical characteristics, thickness, folding endurance, tensile strength, disintegration time, drug content uniformity and drug release characteristics and found to be within the limits. Among the prepared formulations F4 showed minimum disintegration time 11 sec, maximum drug was released i.e. 99.68 ± 1.52% of drug within 10 min when compared to the other formulations and finalized as optimized formulation. FTIR data revealed that no interactions takes place between the drug and polymers used in the optimized formulation. The in vitro dissolution profiles of marketed product and optimized formulation was compared and found to be the drug released was 92.77 ± 1.52 after 50 min. Therefore, it can be a good alternative to conventional ropinirole for immediate action. In vitro evaluation of the ropinirole fast dissolving films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of ropinirole. The oral dissolving film is considered to be potentially useful for the treatment of Parkinson’s disease where quick onset of action is desired

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