scholarly journals DESIGN, FORMULATION, AND EVALUATION OF SOLID DISPERSION TABLETS OF POORLY WATER-SOLUBLE ANTIDIABETIC DRUG USING NATURAL POLYMER

2019 ◽  
pp. 195-197 ◽  
Author(s):  
SUDIPTA DAS ◽  
PRIYANKA MANDAL
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
In Vitro Release ◽  
Gellan Gum ◽  
Water Soluble ◽  
Angle Of Repose ◽  
Wet Granulation ◽  
Natural Polymer ◽  
Poorly Water Soluble ◽  
Release Study

Objective: The objective of the present study was to formulate the solid dispersion (SD) of poorly water-soluble drug glimepiride and the development of the tablets of prepared SD of glimepiride using natural and synthetic polymers. Methods: The SD of glimepiride was to prepare using fusion method. The tablets were prepared by wet granulation method using synthetic polymer such as HPMC and natural polymer gellan gum. Results: The granules were evaluated by determining the angle of repose (23.70±0.761 to 29.21±0.127º), bulk density, tapped density, Hausner ratio, and Carr’s index. It shows satisfactory results. The tablets were subjected to the measurement of hardness (3.9±0.08 to 4.6±0.04kg/cm2), friability (0.22±0.004 to 0.40±0.005%), and in vitro release studied. Release study of pure drug was performed. In the release study, SD of glimepiride tablets with gellan gum gives considerably good result compared to HPMC. Conclusion: From the results, it was shown that dissolution rate of pure glimepiride was very slow. When the glimepiride was prepared in SD form, then the dissolution rate was very fast. The tablets of the SD of glimepiride were prepared and release study was shown depending on various quantities of HPMC and gellan gum used. Therefore, the long term stability study is required for future development of this formulation.

scholarly journals Formulation and Evaluation of Ciprofloxacin Solid Dispersion Controlled Release Floating Capsules for Solubility Improvement

2017 ◽  
Vol 5 (03) ◽  
pp. 07-16
Author(s):  
Gaurav Subhash Katore ◽  
S. J. Bidkar ◽  
G. Y. Dama
Keyword(s):  
Controlled Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Evaluation Studies ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Angle Of Repose ◽  
Drug Dissolution ◽  
Wet Granulation ◽  
Weight Variation

Solid dispersions in water soluble carriers have attracted considerable interests as a mean of improving the dissolution rate and hence possibly bioavailability range of hydrophobic drugs. The poor solubility of ciprofloxacin leads to poor dissolution and hence variation in bioavailability. The purpose of present investigation was formulation and evaluation of controlled release floating capsule of ciprofloxacin with improved solubility and dissolution rate. In present study solid dispersion using various carriers like mannitol and lactose in different ratios were prepared by solvent evaporation method. The prepared solid dispersions were characterized for drug content, solubility and dissolution rate. The dissolution rate substantially improved for ciprofloxacin from its solid dispersions compared with pure drug. Dissolution rate increased with increase in carrier content. The dissolution rate was increased 3 folds with solid dispersions containing 1:4 of drug: lactose. The granules of ciprofloxacin solid dispersion containing 1:4 of drug: lactose ratio was prepared by wet granulation method using polymer such as ethyl cellulose and HPMC. The prepared granules were evaluated to preformulation studies such as angle of repose (18.41-24.22), bulk density, tapped density, compressibility index (11.31-12.75) and hausner’s ratio. All the parameters shows that the granules having good flow properties. These granules had converted into the capsule forms. Then the formulated capsules were taken to the evaluation studies such as weight variation, release study, buoyancy and floating duration (more than 6 hrs.). We can conclude that all the parameters were within the acceptable limits.

scholarly journals Preparation and Characterization of PEG4000 Palmitate/PEG8000 Palmitate-Solid Dispersion Containing the Poorly Water-Soluble Drug Andrographolide

2020 ◽  
Vol 2020 ◽  
pp. 1-7
Author(s):  
Qingyun Zeng ◽  
Liquan Ou ◽  
Guowei Zhao ◽  
Ping Cai ◽  
Zhenggen Liao ◽  
...  
Keyword(s):  
Thermal Stability ◽  
Molecular Weight ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Water Soluble ◽  
Carrier Material ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Solid dispersion (SD) is the effective approach to improve the dissolution rate and bioavailability of class II drugs with low water solubility and high tissue permeability in the Biopharmaceutics Classification System. This study investigated the effects of polyethylene glycol (PEG) molecular weight in carrier material PEG palmitate on the properties of andrographolide (AG)-SD. We prepared SDs containing the poorly water-soluble drug AG by the freeze-drying method. The SDs were manufactured from two different polymers, PEG4000 palmitate and PEG8000 palmitate. The physicochemical properties of the AG-SDs were characterized by Fourier transform infrared spectroscopy, thermogravimetric analysis, differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, dissolution testing, and so on. We found that AG-PEG4000 palmitate-SD and AG-PEG8000 palmitate-SD were similar in the surface morphology, specific surface area, and pore volume. Compared with the AG-PEG4000 palmitate-SD, the intermolecular interaction between PEG8000 palmitate and AG was stronger, and the thermal stability of AG-PEG8000 palmitate-SD was better. In the meanwhile, the AG relative crystallinity was lower and the AG dissolution rate was faster in AG-PEG8000 palmitate-SD. The results demonstrate that the increasing PEG molecular weight in the PEG palmitate can improve the compatibility between the poorly water-soluble drug and carrier material, which is beneficial to improve the SD thermal stability and increases the dissolution rate of poorly water-soluble drug in the SD.

scholarly journals Improving the Dissolution Rate of Poorly Water Soluble Drug by Solid Dispersion and Solid Solution—Pros and Cons

Drug Delivery ◽  
2007 ◽  
Vol 14 (1) ◽  
pp. 33-45 ◽  
Author(s):  
Rina J. Chokshi ◽  
Hossein Zia ◽  
Harpreet K. Sandhu ◽  
Navnit H. Shah ◽  
Waseem A. Malick
Keyword(s):  
Solid Solution ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Water Soluble Drug ◽  
Pros And Cons ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

scholarly journals RESEARCH AND DEVELOPMENT OF DIAZEPAM SOLID DISPERSION POWDER USING NATURAL POLYMERS

2018 ◽  
Vol 10 (5) ◽  
pp. 220
Author(s):  
Uditi Handa ◽  
Kamal Saroha
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Natural Polymers ◽  
Drug Content ◽  
Ftir Studies ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Pure Drug ◽  
Poorly Water Soluble Drug

Objective: The objective of this study was to enhance the solubility and dissolution rate of a poorly water-soluble drug by solid dispersion (SD) technique, in order to conduct an investigation of the effect of these natural hydrophilic polymers on release mechanism from SD.Methods: The SD of diazepam (DZM) were prepared by using modified sodium alginate (SA) and modified guar gum (GG) in different drug: polymer ratios (1:1 and 1:2) by using physical mixture method (PM) and fusion method (FM). Further, the formulations were characterized for calibration curve, Fourier transforms infrared spectroscopy (FTIR) studies, % age practical yield, drug content estimation, solubility studies, dissolution studies.Results: The pure drug and SD were characterized by pre and post-formulations studies. The %age practical yield ranged from 92.9±0.25 to 49±0.57%, and the drug content estimation ranged from 99.34±0.40 to 65.25±0.25 %. The FTIR studies shown that the compatibility between pure drug and natural polymers was stable. All the SD showed improved solubility as compared to the pure drug (PD). SD prepared with modified SA (1:2) by PM and FM shown the huge enhancement of solubility and dissolution rate of the DZM. This can be specific to the improvement in wettability and dispersibility, as well as enhances the drug amorphous fraction.Conclusion: On the basis of the research study, the SD technique shows the enhancement in the solubility of poorly water-soluble drug using natural polymers. SD containing natural polymers prepared with PM and FM shown the remarkable improvement in the release outline compared with PD, DZM.

scholarly journals Effect of Carrier Lipophilicity and Preparation Method on the Properties of Andrographolide–Solid Dispersion

Pharmaceutics ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 74 ◽  
Author(s):  
Guowei Zhao ◽  
Qingyun Zeng ◽  
Shoude Zhang ◽  
Youquan Zhong ◽  
Changhao Wang ◽  
...  
Keyword(s):  
Surface Morphology ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Preparation Method ◽  
Water Soluble ◽  
Vacuum Drying ◽  
Dissolution Behavior ◽  
Drying Method ◽  
Carrier Material ◽  
Poorly Water Soluble

Solid dispersion (SD) is a useful approach to improve the dissolution rate and bioavailability of poorly water-soluble drugs. This work investigated the effects of carrier material lipophilicity and preparation method on the properties of andrographolide (AG)–SD. The SDs of AG and the carrier materials, polyethylene glycol (PEG) and PEG grafted with carbon chains of different length (grafted PEG), have been prepared by spray-drying and vacuum-drying methods. In AG–SDs prepared by the different preparation methods with the same polymer as carrier material, the intermolecular interaction, 5% weight-loss temperature, the melting temperature (Tm), surface morphology, crystallinity, and dissolution behavior have significant differences. In the AG–SDs prepared by the same spray-drying method with different grafted PEG as carrier material, Tm, surface morphology, crystallinity, and dissolution behavior had little difference. In the AG–SDs prepared by the same vacuum-drying method with different grafted PEG as carrier material, the crystallinity and Tm decreased, and the dissolution rate of AG increased with the increase of grafted PEG lipophilicity. The preparation method has an important effect on the properties of SD. The increase of carrier material lipophilicity is beneficial to the thermal stability of SD, the decrease of crystallinity and the increase of dissolution rate of a poorly water-soluble drug in the SD.

Surface Solid Dispersion – A Review

2013 ◽  
Vol 6 (1) ◽  
pp. 1915-1925
Author(s):  
Sadhna Khatry ◽  
Neha Sood ◽  
Sandeep Arora
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
High Surface ◽  
High Surface Area ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Insoluble Drugs ◽  
Poorly Water Soluble

Preparation of an effective formulation of poorly water-soluble drugs is a key challenge in pharmaceutical technology. Dissolution rate and solubility are the rate- limiting steps for increasing the bioavailability of poorly water‐soluble drugs. Solid dispersion is an efficient technique for improving dissolution rate and subsequently, the bioavailability of poorly water‐soluble drugs. Surface sSolid dDispersion is a novel technique of solid dispersion for dispersing one or more active ingredients on a water insoluble carrier of high surface area in order to achieve increased dissolution rates and bioavailability of insoluble drugs. The Vvarious polymers used in this technique are Avicel, Crosspovidone, sSodium starch glycolate, pPregelatinized starch, Cab-o-sil, Ac-di-sol, KyronT-314, Primojel and pPotato sStarch. This article reviews the various methods of preparation and characterization of surface solid dispersion and compiles some of the drugs formulated as surface solid dispersions. Some of the practical aspects to be considered for preparing surface solid dispersion are selection of a suitable carrier and method of preparation of surface solid dispersion.

scholarly journals Solid Dispersion by Fluidized Bed Processing: A Platform for Enhancement of Dissolution Rate of Simvastatin Poorly Water-Soluble Drug

2021 ◽  
pp. 32-43
Author(s):  
Rajendra K. Surawase ◽  
Kamalkishor G. Baheti
Keyword(s):  
Dissolution Rate ◽  
Fluidized Bed ◽  
Solid Dispersion ◽  
Zero Order ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Aim: The aim of this study was to study the solubility and dissolution kinetics of poorly water-soluble drugs simvastatin from its solid dispersion with different carriers by using fluidized bed processing technique. Methods: The effect of different surfactants such as Gelucire® 44/14, PVP- K30 and Poloxamer- 188 on solid dispersion dissolution and solubility of simvastatin was investigated. Solid dispersion is formed using various techniques with polymeric carrier to potentially enhance the solubility and dissolution rate such as fluidized bed processing, it will extend drug absorption, therefore the objectives were to make a comparative evaluation among different solid dispersions. Results: The simvastatin solid dispersion prepared by fluidized bed processing significantly enhanced in vitro dissolution and solubility relative to that of the unprocessed form. The dissolution profiles were correlated using various mathematical models such as Zero order, first order, Higuchi and Hixon Crowell model and the Zero order kinetics model gave better correlation results than the other models. Conclusion: Dissolution profile of simvastatin was significantly improved via complexation with Gelucire 44/14 as compared with the pure drug and other carriers using FBP processing is a highly effective strategy for enhancing the solubility and dissolution of poorly water-soluble drugs.

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