Evaluation Of Solid Dispersions Research Articles

Comprehensive Characterization and Comparative Assessment of Carvedilol Solid Dispersions: Insights into Enhanced Bioavailability and Stability Profiles

Carvedilol, a non-selective beta-adrenergic antagonist, poses a challenge in achieving optimal bioavailability due to its poor aqueous solubility. This study aimed to enhance the solubility and dissolution rate of carvedilol through the formulation and evaluation of solid dispersions. Various solid dispersion formulations were prepared using different carriers and methods, including solvent evaporation, fusion, and spray-drying techniques. The prepared formulations were systematically characterized using Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM) to investigate drug-carrier interactions, solid-state changes, and morphological characteristics. Evaluation of the formulated solid dispersions involved in vitro dissolution studies, solubility enhancement assays, and stability assessments. Dissolution profiles revealed significantly improved drug release rates for the solid dispersion formulations compared to the pure drug. The solubility of carvedilol was notably enhanced in the solid dispersion systems, indicating improved drug dissolution behavior. Stability studies demonstrated the robustness of selected formulations against environmental factors over an extended period. Moreover, pharmacokinetic studies conducted in animal models showcased enhanced bioavailability of carvedilol from the optimized solid dispersion formulation compared to the conventional drug formulation. This comprehensive investigation provides valuable insights into the development of carvedilol solid dispersions, elucidating the influence of formulation variables on drug solubility, dissolution, stability, and ultimately, bioavailability enhancement. The findings underscore the potential of solid dispersion technology as a promising strategy to overcome the solubility challenges associated with carvedilol, paving the way for improved therapeutic efficacy and patient compliance.

Formulation and Evaluation of Solid Dispersion of Tinidazol by using Solvent Evaporation Method

Formulation and Evaluation of Solid Dispersion of Tinidazol by using Solvent Evaporation Method

STUDIES ON SOLID DISPERSIONS OF LEFLUNOMIDE

Objective: Leflunomide is Non steroidal Anti-Inflammatory drug, which is poorly water soluble. In present study attempt has been made to prepare and characterize solid dispersions of leflunomide to increase solubility of drug.Method:  In Preparation of solid dispersion of leflunomide different polymer like PEG 4000, PEG 6000, Poloxamer 188 and Poloxamer 407 were used.  Effects of several variables such as type of carrier used, drug: carrier ratios, method of preparation were studied. The evaluation of solid dispersions was done by solubility study, dissolution study and X-ray diffractometry. Result: Improvement in dissolution of drug was observed in all solid dispersions as compared to pure drug alone. Solid dispersions prepared using Poloxamer 188 showed fastest in vitro drug release. Solid dispersions prepared using solvent evaporation method showed relatively faster drug release than melt evaporation method. XRD patterns indicated reduced crystallinity of drug particles, which suggests mechanism of enhanced solubility and dissolution of drug in solid dispersion systems.Conclusion:  A significant result obtained with the study indicated that solid dispersion by solvent evaporation can successfully be further explored and employed to improve solubility and dissolution characteristics of poorly soluble drugs.Keywords: Leflunomide, Solid dispersion, Carrier

Peningkatan Kadar Ketoprofen Terdisolusi melalui Pembentukan Dispersi Padat menggunakan Polivinil Alkohol (PVA)

Ketoprofen is included in the Class II of Biopharmaceutical Classification System (BCS) which has low solubility. Low solubility will affect the dissolution rate and the dissolved concentration, so the absorption and bioavailability are low as well. Several studies have been conducted to improve the solubility and the dissolution of drugs from these group, such as by solid dispersion system. This study aims to determine the effect of polyvinyl alcohol (PVA) on the dissolved concentration of ketoprofen in solid dispersion and in physical mixture, and to decidethe optimum formula.Solid dispersion and physical mixture of ketoprofen - PVA were formulated with the ratio of 1:1, 1:2 and 1:4, and then compared with the standard ketoprofen. Evaluation of solid dispersion was performed by the intervention test of PVA as a matrix on the maximum wavelength of standard ketoprofen using a UV-Vis spectrophotometer and the dissolution test in artificial gastric fluid media without pepsin using a basket stirrer at pH ± 1,2, the temperature of 37 ± 0.5ºC, and device speed of 50 rpm. The sample was collected at 10, 20, 30, 45, and 60 minutes. The amount of dissolved ketoprofen was determined by a UV-Vis spectrophotometer at a wavelength of 260 nm. The results showed that there was no shifting on maximum wavelength point in both solid dispersions and physical mixtures. The dissolved ketoprofen concentration that was represented in solid dispersion was greater than in physical mixture and standard ketoprofen. The highest dissolved ketoprofen concentration was indicated in solid dispersion formula with the ratio of 1:1.

Formulation and Evaluation of Solid Dispersion and Inclusion Complex of Poorly Aqueous Soluble Diacerein

The present study was focused on a poorly aqueous soluble drug (diacerein); basic structured anthracene molecule possesses defensive activity against osteoarthritis. The problem with the diacerein is its poor bioavailability (35%) which is due to its poor dissolution profile. The present study efforts to improve the dissolution profile using solubility enhancement techniques. The objective of the study was to improve the solubility of poorly soluble drug diacerein by solid dispersion technique and inclusion complex using the most compatible carriers and technique for the formulation. The prepared solid dispersion and inclusion complex were evaluated for physiochemical characteristics and dissolution efficacy. Thesolid dispersion and inclusion complex were formulated using kneading method with PVP K30 (screened to be the best among different carriers) and β-cyclodextrin respectively. The prepared formulations were characterized by FTIR, SEM, DSC and XRPD. The prepared solid dispersion and inclusion complex were then compressed into conventional tablets which were then coated with acid resistant polymer.

Formulation and Evaluation of Solid Dispersion of Glimepiride in to Sustained Release

Formulation and Evaluation of Solid Dispersion of Glimepiride in to Sustained Release

Formulation and evaluation of solid dispersions of nabumetone

Solid dispersions are an effective method of increasing the solubility and bioavailability of poorly soluble drugs. In the present study it is aimed at to enhance solubility of Nabumetone a poorly soluble anti-inflammatory drug by solid dispersion technique by employing solvent evaporation technique using PEG 4000 And PEG 6000 as carriers. The formulations were prepared in ratios of 1:1, 1:2 , 1:3, 1:4 and characterized by FTIR, XRD, and dissolution studies. The prepared solid dispersions showed excellent improvement of drug solubility due to mean drug particle size reduction which lead to increase drug dissolution and bioavailability

Preparation and Evaluation of Solid Dispersions of Ibuprofen Using Glucosamine HCl as a Carrier

Preparation and Evaluation of Solid Dispersions of Ibuprofen Using Glucosamine HCl as a Carrier

Evaluation of solid dispersions containing magnesium levulinate salts with selected carriers

Evaluation of solid dispersions containing magnesium levulinate salts with selected carriers

Preparation and evaluation of solid dispersions of piroxicam and Eudragit S100 by spherical crystallization technique

Objective: To improve the dissolution rate of piroxicam (PX), enteric-release microparticles having solid dispersion (SD) structure were prepared in one step. Methods: SD of PX and Eudragit S100 (Eu S100) with the aid of silicon dioxide (Aerosil® 200), as an antiadhesion agent, were prepared by spherical crystallization technique. The microparticles were characterized by differential scanning calorimetry, X-ray powder diffraction, and Fourier transform infrared spectroscopy and were evaluated for yield, encapsulation efficiency, flowability, packability, and drug release (at pH 1.2 and pH 7.4). The samples were stored at severe condition [40°C, 75% relative humidity (RH)] for 3 months to investigate their stability. The effects of the polymer–drug and polymer–Aerosil ratios on the characteristics of the microparticles were also investigated. Results: PX microparticles exhibited significantly improved micromeritic properties in comparison to the crystalline pure drug. The dissolution of drug from microparticles in phosphate buffer (pH 7.4) indicated a significant increase in dissolution of PX when dispersed in Eu S100. The results of X-ray powder diffraction and differential scanning calorimetry analysis indicated that in microparticles at 2:1 Eu S100:PX ratio the crystalline form of PX was disordered, suggesting that PX was highly dispersed in microparticles, as that in the amorphous state. Fourier transform infrared spectroscopy analysis demonstrated the presence of intermolecular hydrogen bonding between PX and Eu S100 in SD. In stability test, the release profiles of the microparticles were unchanged as compared with the freshly prepared SDs; amorphous PX in the SD particles did not crystallize under storing at 40°C, 75% RH for 3 months.

Evaluation of solid dispersions on a molecular level by the Raman mapping technique

Troglitazone containing two asymmetric carbons has four isomers. Crystalline troglitazone consists of two crystalline diastereomer-pairs, RR/SS and RS/SR, which have different melting points. Using a closed melting method, troglitazone–polyvinylpyrrolidone solid dispersions with various crystallinities were prepared. Raman spectroscopy and its mapping technique were applied to discriminate between the crystalline RR/SS, crystalline RS/SR and amorphous form of troglitazone in solid dispersions. The results of the Raman mapping of solid dispersions showed the co-existence of crystal and amorphous forms, and which diastereomer-pairs remained as crystals, in addition to the distribution of the drug. Moreover, the distribution of PVP could be illustrated from the Raman mapping data. Thus, Raman spectroscopy and its mapping technique are useful tools to evaluate crystal and amorphous states, including discrimination of crystalline diastereomer-pairs in solid dispersions. In addition, by describing the distribution of the drug and the carrier, it could be guessed how drug crystals become amorphous during preparation from the point of view of the distribution of the amorphous form of the drug substance and the carrier.