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 Dissolution Enhancement of Rosuvastatin Calcium by Liquisolid Compact Technique

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
V. J. Kapure ◽  
V. V. Pande ◽  
P. K. Deshmukh
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Content Uniformity ◽  
Scanning Calorimetry ◽  
Weight Variation ◽  
Liquisolid Compacts ◽  
Rosuvastatin Calcium

In present investigation liquisolid compact technique is investigated as a tool for enhanced dissolution of poorly water-soluble drug Rosuvastatin calcium (RVT). The model drug RVT, a HMG-Co A reductase inhibitor was formulated in form of directly compressed tablets and liquisolid compacts; and studied for in-vitro release characteristics at different dissolution conditions. In this technique, liquid medications of water insoluble drugs in non-volatile liquid vehicles can be converted into acceptably flowing and compressible powders. Formulated systems were assessed for precompression parameters like flow properties of liquisolid system, Fourior transform infra red spectra (FTIR) analysis, X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and post compression parameters like content uniformity, weight variation, hardness and friability, disintegration test, wetting time, in vitro dissolution studies, effect of dissolution volume on drug release rate, and estimation of fraction of molecularly dispersed drug in liquid medication. As liquisolid compacts demonstrated significantly higher drug release rates, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.

scholarly journals IMPROVEMENT OF DISSOLUTION RATE OF VALSARTAN BY SOLID DISPERSION SYSTEM USING D(−) MANNITOL

2017 ◽  
Vol 10 (3) ◽  
pp. 288 ◽  
Author(s):  
Erizal Zaini ◽  
Salman Umar ◽  
Nurhidayah Nurhidayah
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
In Vitro Dissolution ◽  
Type I ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Dispersion System ◽  
Grinding Technique

ABSTRACTObjective: To improve dissolution rate of valsartan from solid dispersion system of valsartan and D(−) mannitol using co-grinding approach.Methods: Valsartan solid dispersion with different ratio of D(−) mannitol (1:1; 1:3 and 1: 5) were prepared by co-grinding method. Solid statecharacterization of the solid dispersion system was evaluated in term of crystallographic properties (powder X-ray diffraction), thermal behavior(differential scanning calorimetry [DSC]) and morphology (scanning electron microscope). The profile of dissolution rate was examined using USPdissolution apparatus type I at a temperature of 37±0.5°C.Results: Based on thermal analysis DSC and powder X-ray diffraction analysis, valsartan was transformed from semicrystalline phase to amorphousstate as indicated by the disappearance of its melting endothermic peaks and the characteristic diffraction peaks. The in vitro dissolution rate studyrevealed that all solid dispersion system showed significant increase in dissolution rate compared with the intact valsartan.Conclusion: Solid dispersion of valsartan with D(−) mannitol prepared by co-grinding technique has successfully improved the dissolution ratecompared with intact valsartan.Keywords: Valsartan, D(−) mannitol, Solid dispersion, Co-grinding, Dissolution rate.

DEVELOPMENT OF SOLID DISPERSION TABLET OF CARVEDILOL TO IMPROVE SOLUBILITY

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (01) ◽  
pp. 54-59
Author(s):  
S. S Shelake ◽  
◽  
R. G Gaikwad ◽  
S Patil ◽  
F. I. Mevekari ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Media ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Water Soluble Drugs ◽  
Ft Ir

Crystalline state compounds are typically dissolution rate limited and dissolution rate is directly proportional to the solubility for BCS class II or class IV compounds. Solid dispersions are one of the most promising strategies to improve the oral bioavailability poorly water soluble drugs. The purpose of this study was to increase solubility of carvedilol by solid dispersion (SDs) technique with Poloxamer (PXM) 407 in aqueous media. The carvedilol- PXM 407 solid dispersion was prepared by solvent evaporation, kneading and melting method. It was characterized by differential scanning calorimetry (DSC), X-ray powder diffraction (XRD), Fourier transformation infra-red spectroscopy (FT-IR), scanning electron microscopy (SEM) and in vitro dissolution studies. The prepared solid dispersion were found to have higher dissolution rates as compared to intact carvedilol. During formulation of solid dispersion crystalline to amorphous transition has been observed.

scholarly journals Ground Calcium Carbonate as a Low Cost and Biosafety Excipient for Solubility and Dissolution Improvement of Praziquantel

Pharmaceutics ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 533 ◽  
Author(s):  
Ana Borrego-Sánchez ◽  
Rita Sánchez-Espejo ◽  
Beatrice Albertini ◽  
Nadia Passerini ◽  
Pilar Cerezo ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Calcium Carbonate ◽  
Dissolution Rate ◽  
Solid Dispersions ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Limiting Factor ◽  
Scanning Calorimetry ◽  
Interaction Product

Calcium carbonate is an abundant mineral with several advantages to be a successful carrier to improve oral bioavailability of poorly water-soluble drugs, such as praziquantel. Praziquantel is an antiparasitic drug classified in group II of the Biopharmaceutical Classification System hence characterized by high-permeability and low-solubility. Therefore, the dissolution rate is the limiting factor for the gastrointestinal absorption that contributes to the low bioavailability. Consequently, the therapeutic dose of the praziquantel must be high and big tablets and capsules are required, which are difficult to swallow, especially for pediatric and elderly patients. Mixtures of praziquantel and calcium carbonate using solid-solid physical mixtures and solid dispersions were prepared and characterized using several techniques (X-ray diffraction differential scanning calorimetry, thermogravimetric analysis, scanning electron microscopy, laser diffraction, Fourier transform infrared and Raman spectroscopies). Solubility of these formulations evidenced that the solubility of praziquantel-calcium carbonate interaction product increased in physiological media. In vitro dissolution tests showed that the interaction product increased the dissolution rate of the drug in acidic medium. Theoretical models were studied to understand this experimental behavior. Cytotoxicity and cell cycle studies were performed, showing that praziquantel-calcium carbonate physical mixture and interaction product were biocompatible with the HTC116 cells, because it did not produce a decrease in cell viability or alterations in the cell cycle.

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.

The Potential Migrated Mechanism of Water-Soluble Components in Pellets Prepared by Wet Extrusion/Spheronization: Effect of Drying Rate

2020 ◽  
Vol 17 ◽  
Author(s):  
Bingwei Wang ◽  
Jianping Liu ◽  
Zhenghua Li ◽  
Yulong Xia ◽  
Shuangshuang Zhang ◽  
...  
Keyword(s):  
Relative Humidity ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Drying Rate ◽  
Scanning Calorimetry ◽  
Drying Temperature ◽  
Wet Extrusion ◽  
Extrusion Spheronization ◽  
Soluble Components

Background: At present, there were numerous researches on the migration of components in tablets and granules, the investigation in the pharmaceutical literatrue concerning the effect of drying rate on the migration of water-soluble components of pellets was limited. Temperature and relative humidity (RH) were crucial parameters during the drying process which was an essential step in the preparation of pellets via wet extrusion/spheronization. To quantify these variables, the water loss percentage of pellets per minute was defined as drying rate. Objective: The study aimed to investigate the influence of drying rate on the migration of water-soluble components in wet pellets and the potential migrated mechanism. Methods: The pellets containing tartrazine as a water-soluble model drug and microcrystalline cellulose as a matrix former were prepared by extrusion/spheronization and dried at four different drying temperature and relative humidity. Afterward, the extent of migrated tartrazine was assessed regarding appearance, in-vitro dissolution test, Differential Scanning Calorimetry, X-Ray Powder Diffraction, Attenuated total reflectance Fourier transform infrared spectroscopy and Confocal Raman Mapping. Results: Results demonstrated that red spots of tartrazine appeared on the surface of pellets and more than 40% tartrazine were burst released within 5 minutes when pellets dried at 60℃/RH 10%. While pellets dried at 40℃/RH 80%, none of these aforementioned phenomena was observed. Conclusion: In conclusion, the faster drying rate was, the more tartrazine migrated to the exterior of pellets. Adjusting drying temperature and relative humidity appropriately could inhibit the migration of water-soluble components within wet extrusion/spheronization pellets.

Formulation and Evaluation of Benidipine Nanosuspension

2021 ◽  
pp. 4111-4116
Author(s):  
Sejal Patel ◽  
Anita P. Patel
Keyword(s):  
Particle Size ◽  
Water Solubility ◽  
Polymer Concentration ◽  
Oral Route ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
23 Factorial Design ◽  
Selection Of

In the interest of administration of dosage form oral route is most desirable and preferred method. After oral administration to get maximum therapeutic effect, major challenge is their water solubility. Water insoluble drug indicate insufficient bioavailability as well dissolution resulting in fluctuating plasma level. Benidipine (BND) is poorly water soluble antihypertensive drug has lower bioavailability. To improve bioavailability of Benidipine HCL, BND nanosuspension was formulated using media milling technique. HPMC E5 was used to stabilize nanosuspension. The effect of different important process parameters e.g. selection of polymer concentration X1(1.25 mg), stirring time X2 (800 rpm), selection of zirconium beads size X3 (0.4mm) were investigated by 23 factorial design to accomplish desired particle size and saturation solubility. The optimized batch had 408 nm particle size Y1, and showed in-vitro dissolution Y2 95±0.26 % in 30 mins and Zeta potential was -19.6. Differential scanning calorimetry (DSC) and FT-IR analysis was done to confirm there was no interaction between drug and polymer.

DEVELOPMENT AND EVALUATION OF ZIPRASIDONE LOADED SOLID SELF-MICRO EMULSIFYING DRUG DELIVERY SYSTEM

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (08) ◽  
pp. 53-60
Author(s):  
Purushottam Patil ◽  
Malik Shaikh ◽  
Paresh Mahaparale
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Physical Adsorption ◽  
Gastrointestinal Transit ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Poorly Water Soluble

Solid self-micro emulsification technique is the new approach for poorly water-soluble and poorly bioavailable drugs by allowing the drug substance to be incorporated into the oil phase and thus having the ability to permeate the GI membrane to a faster extent. Oleic acid, Tween 80, methanol and colloidal silicon dioxide were used as penetrant, surfactant, co-surfactant and adsorbent, respectively. The interaction between drug and excipients was examined by differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The results of DSC and FTIR studies did not reveal any possible drug-excipient interactions. The conversion of liquid self-microemulsifying drug delivery system (SMEDDS) into the solid SMEDDS increases the stability of the emulsion formulation achieved by physical adsorption of an adsorbent material. The release of drug from SMEDDS formulation is justified by in-vitro dissolution studies. SMEDDS increases the solubility of the drug and improves the bioavailability, without disturbing gastrointestinal transit. SMEDDS has the potential to provide a useful oral solid dosage form for the poorly water-soluble drug ziprasidone.

scholarly journals SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEM OF EFAVIRENZ: FORMULATION, IN VITRO EVALUATION AND CHARACTERIZATION

2019 ◽  
pp. 217-226
Author(s):  
PAMU SANDHYA
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Vitro Release ◽  
Visual Observation ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Tween 20

Objective: The main objective of this study was to preparation and evaluation of efavirenz (EFV) to enhance its solubility and dissolution rate by self-emulsifying drug delivery system. Methods: EFV self-emulsifying drug delivery systems (SNEDDS) were formulated using different oils, surfactant, and co-surfactant. Peceol, Tween 20, and Capmul MCM were used as oil, surfactant, and co-surfactant, respectively, followed by the evaluation by the performance of different tests such as visual observation, solubility studies, thermodynamic stability study, transmittance studies, drug content, and in-vitro release study. Results: Fourier-transform infrared studies revealed negligible drug and polymer interaction. From the phase diagram, it was observed that self-emulsifying region was enhanced with increasing surfactant and co-surfactant concentrations with oil. F13 was selected as optimized formulation on the basis of physicochemical parameters, particle size, and in-vitro dissolution studies with the release of 98.39±5.10% drug in 1 hour. The optimized formulation size was found to be 156.7 nm as mean droplet size and Z-Average of 808.6 nm with -18.3 mV as zeta potential. Conclusion: The study demonstrated that SNEDDS was a promising strategy to enhance the dissolution rate of EFV by improving solubility.

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.

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