scholarly journals Inclusion Complexation in Sulfobutyl Ether Beta Cyclodextrin and Dispersion in Gelucire for Sustained Release of Nifedipine Employing Almond Gum

2019 ◽  
Vol 9 (6) ◽  
pp. 70-78
Author(s):  
Kanteti Venkata Ramesh ◽  
Meena Achamma ◽  
Hemant Kumar Yadav ◽  
Tamer Salama Elmarsafawy ◽  
Quamrul Islam
Keyword(s):  
Sustained Release ◽  
Solid Dispersion ◽  
Inclusion Complexation ◽  
Matrix Tablets ◽  
Scanning Calorimetry ◽  
Enhanced Dissolution ◽  
Beta Cyclodextrin ◽  
Novel Approach ◽  
Poorly Soluble ◽  
Sulfobutyl Ether

In the present research investigation, the utility of employing high dissolving forms of nifedipine for sustained release from matrix tablets with almond gum as major release retardant is explored. A poorly soluble BCS class II drug nifedipine is chosen as a model drug. Efforts were made to alter the dissolution characteristics of the drug before it is entrapped in the polymer matrix of almond gum. Inclusion complexation in sulfobutyl ether beta cyclodextrin or solid dispersion in gelucire (50/13) resulted in enhanced dissolution of nifedipine. The high dissolving forms are characterized by x-ray diffraction, differential scanning calorimetry and infra-red spectroscopy. The matrix tablets prepared employing the high dissolving forms exhibited satisfactory characteristics such as hardness, friability, swelling index. The drug release is found to be slow and spread over a period of 12 hours and the release could be modified with changes in nature of high dissolving form and the proportion of almond gum as the major release retardant. Employing high dissolving forms in matrix tablets of almond gum is found to be a novel approach in obtaining slow and complete release of poorly soluble drug such as nifedipine. Keywords:  sulfobutyl ether beta cyclodextrin, solid dispersion, nifedipine

scholarly journals A REVIEW ON DISINTEGRATION CONTROL MATRIX TABLETS

2018 ◽  
Vol 8 (5) ◽  
pp. 19-22
Author(s):  
Pralhad K. Kanke ◽  
Pankaj Sawant ◽  
Ajit Jadhav ◽  
Md. Rageeb Md. Usman
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Solid Dispersion ◽  
Gastrointestinal Transit ◽  
Matrix Tablets ◽  
Surface Erosion ◽  
Matrix Tablet ◽  
Control Matrix ◽  
Dispersion Technique ◽  
Wax Coating

A number of sustained release formulations are available in the market which successfully sustained the drug release over a prolonged period of time by different mechanisms. The new approach for sustaining the drug release is disintegration control matrix tablet which sustained the drug release up to 24hrs by controlling the disintegration rate of tablet. Disintegration control matrix tablet (DCMT) mainly forms the granules containing drug and disintegrating agent such as low substituted hydroxyl propyl cellulose by various methods such as solid dispersion technique. The sustained release of drug is maintained by increasing the wax coating or decreasing the amount of disintegrants. The release of drug from tablet is uniform throughout till all the drug releases from tablet as it involves drug release by diffusion, dissolution and surface erosion mechanism. DCMT increases the solubility of drug and improves the bioavailability without disturbing gastrointestinal transit. BCS Class II, III, IV drugs are the best candidate for DCMT formulations. Keywords: Disintegration control matrix tablet (DCMT), Wax, Disintegrating agent, Solid dispersion.

scholarly journals Solubility and Dissolution Enhancement of Atorvastatin Calcium using Solid Dispersion Adsorbate Technique

2019 ◽  
Vol 28 (2) ◽  
pp. 105-114
Author(s):  
Samer K. Ali ◽  
Eman B. H. Al-Khedairy
Keyword(s):  
Polyethylene Glycol ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Poloxamer 407 ◽  
Dissolution Enhancement ◽  
Drug Solubility ◽  
Scanning Calorimetry ◽  
Poorly Soluble

            Atorvastatin (ATR) is poorly soluble anti-hyperlipidemic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs.           The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxamer 407were used as hydrophilic carriers and Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents.            All solid dispersion adsorbate (SDA) formulas  were prepared in ratios of 1:1:1  (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content,  , dissolution, crystal structure using  X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC)  studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction.                The prepared (SDA) showed significant improvement of drug solubility in all prepared formula. Best result was obtained with formula SDA12(ATR :Poloxamer407 : MAS 1:1:1) that showed 8.07 and 5.38  fold increase in solubility compared to  solubility of pure ATR and  solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improve drug solubility  and  dissolution .

scholarly journals Preparation and evaluation of azithromycin binary solid dispersions using various polyethylene glycols for the improvement of the drug solubility and dissolution rate

2016 ◽  
Vol 52 (1) ◽  
pp. 1-13 ◽  
Author(s):  
Ehsan Adeli
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Polyethylene Glycols ◽  
X Ray Diffraction ◽  
Drug Release Profile ◽  
Scanning Calorimetry ◽  
Peg 4000 ◽  
Poorly Soluble

ABSTRACT Azithromycin is a water-insoluble drug, with a very low bioavailability. In order to increase the solubility and dissolution rate, and consequently increase the bioavailability of poorly-soluble drugs (such as azithromycin), various techniques can be applied. One of such techniques is "solid dispersion". This technique is frequently used to improve the dissolution rate of poorly water-soluble compounds. Owing to its low solubility and dissolution rate, azithromycin does not have a suitable bioavailability. Therefore, the main purpose of this investigation was to increase the solubility and dissolution rate of azithromycin by preparing its solid dispersion, using different Polyethylene glycols (PEG). Preparations of solid dispersions and physical mixtures of azithromycin were made using PEG 4000, 6000, 8000, 12000 and 20000 in various ratios, based on the solvent evaporation method. From the studied drug release profile, it was discovered that the dissolution rate of the physical mixture, as the well as the solid dispersions, were higher than those of the drug alone. There was no chemical incompatibility between the drug and polymer from the observed Infrared (IR) spectra. Drug-polymer interactions were also investigated using Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD) and Scanning Election Microscopy (SEM). In conclusion, the dissolution rate and solubility of azithromycin were found to improve significantly, using hydrophilic carriers, especially PEG 6000.

scholarly journals Optimization of amorphous solid dispersion techniques to enhance solubility of febuxostat

Folia Medica ◽  
2021 ◽  
Vol 63 (4) ◽  
pp. 557-568
Author(s):  
Vaishali P. Patel ◽  
Anita P. Patel ◽  
Ashish Shah
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Amorphous Solid ◽  
Amorphous Powder ◽  
Amorphous Solid Dispersion ◽  
Scanning Calorimetry ◽  
Residual Solvent ◽  
Percentage Yield ◽  
Poorly Soluble ◽  
Powder Characteristics

Febuxostat is a selective inhibitor of xanthine oxidase and belongs to BCS class II drugs having low solubility and high permeability. Solubility is the most important parameter which directly affects dissolution, absorption and bioavailability of the drugs. There are different techniques by which we can improve solubility and dissolution rate of poorly soluble drug. Amorphous solid dispersion is one of the methods which can improve solubility as well as powder characteristics. The aim of the present study was to formulate and optimize various methods of formulating solid dispersion by using various drug-to-polymer ratios and identifying the batch which gives higher solubility as well as amorphous powder of the drug febuxostat. Different techniques like hot melt method, solvent evaporation method and spray drying techniques were selected for optimization. Attempts were made to improve solubility of febuxostat by employing Kolliphor P 188, Kolliphor P 237, Eudragit RLPO in different drug-to-polymer ratios (1:1, 1:1.5, 1:2) as carrier. The prepared solid dispersion was characterized for the saturation solubility, percentage yield, using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), powdered X-ray diffraction studies (PXRD), and residual solvent determination. Solid state characterization indicated that febuxostat was present in the amorphous form after mixing with polymeric carrier. In contrast to the pure form of drug, solid dispersion of the drug showed better solubility and amorphous characteristics which can be attributed to decreased crystallinity due to hydrotrophy. Thus, amorphous solid dispersion approach can be used successfully to enhance solubility, dissolution rate and bioavailability of febuxostat.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF CONTROLLED RELEASE TABLETS OF CANDESARTAN CILEXETIL/Β-CYCLODEXTRIN INCLUSION COMPLEX

2019 ◽  
pp. 198-209
Author(s):  
OMAR SAEB SALIH ◽  
ZAHRAA M. HAMODDI ◽  
SALAM S. TAHER
Keyword(s):  
Sustained Release ◽  
Candesartan Cilexetil ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
Matrix Tablet ◽  
Scanning Calorimetry ◽  
Weight Variation

Objective: Matrix tablet approach is one of the delivery systems intended for poorly water-soluble drugs like candesartan cilexetil. Candesartan cilexetil is a class II drug used for the treatment of hypertension. Methods: Matrix tablets from (F1x to F18z) were prepared in the presence of β-cyclodextrin. Matrix tablet formulation ensures control release of the drug and higher dissolution by β-cyclodextrin. Fourier transform infrared spectroscopy and differential scanning calorimetry were used to study compatibility. Results:The angle of repose determination showed good flow for most of the formulas besides having good compressibility. Weight variation test for all formulas showed accepted value. Drug content measurement showed accepted values. Friability and hardness of tablets were within the allowed values. Higher tablet swelling was obtained for the formulas containing hydroxy propyl methyl cellulose (HPMC) K100M (F3x and F15z) in which the ratio of the polymer was (1:1) and (1:3) respectively. In vitro release showed that F1x to F13z were studied depends on the type and amount of polymer i.e. (1:1), (1:2) and (1:3) respectively. F1x release after 8h was 95% which contain (1:1) polymer ratio in compare to F3x, which showed 85% after 8h, Which include 1:3 (drug: HPMC K100). Kinetic studies showed a zero-order model. Conclusion: The use of β-cyclodextrin modify the release profile of the drug, and control the sustained release formulas. The lower the time of the release but in a range that a sustained release of the drug was observed in compare with the formulas prepared without β-cyclodextrin.

Beta-Cyclodextrin and Maltodextrin Based Solid Dispersion of Meloxicam to Enhance the Solubility of Meloxicam; Formulation and In-vitro Evaluation

2019 ◽  
Vol 41 (1) ◽  
pp. 133-133
Author(s):  
Muhammad Zaman Muhammad Zaman ◽  
Muhammad Hanif Muhammad Hanif ◽  
Syed Saeed Ul Hassan Syed Saeed Ul Hassan ◽  
Javed Iqbal and Muhammad Ahmad Shehzad Javed Iqbal and Muhammad Ahmad Shehzad
Keyword(s):  
Solid Dispersion ◽  
X Ray Diffraction ◽  
Flow Properties ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
X Ray ◽  
Beta Cyclodextrin ◽  
Release Studies ◽  
Pure Drug

The purpose of the current study was to enhance the solubility of the meloxicam (MLX) by preparing complex with β-Cyclodextrin (CD) and maltodextrin (MD). Dextrins have the ability to capture the drug inside their cavities without forming any chemical bonding. Three (3) formulations, each of solid dispersion (SD) and physical mixture (PM) were prepared by using different drug to polymer ratios (1:4, 1:6 and 1:8) followed by evaluation for micromeritic properties, drug contents, and in vitro drug release studies, scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and x-ray diffraction (XRD) studies. Chemical compatibility of the ingredients was evaluated by using Fourier transform infrared spectroscopy (FTIR). Results of conducted studies exposed excellent flow properties of SDs as well as prepared PMs, with reasonable amount of loaded drug, i.e. andgt;90%. SEM showed a bit irregular surface while XRD suggested crystalline behavior of pure drug, which was masked after its conversion into SDs and PMs based on dextrins. Solubility of the MLX was increased significantly form its initial extent of solubility i.e. 12.5 and#181;g/ml in pure form to 786.72 and#181;g/ml in the form of SD (pandlt;0.05), advocating suitability of materials and methods for solubility enhancement of MLX.

scholarly journals Development and Characterization of Controlled Release Tablets of Candesartan Cilexetil/ β‑Cyclodextrin Inclusion Complex

2020 ◽  
Vol 10 (02) ◽  
pp. 273-283
Author(s):  
Omar Saeb Salih ◽  
Zahraa M. Hamoddi ◽  
Salam S. Taher
Keyword(s):  
Sustained Release ◽  
Candesartan Cilexetil ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
Matrix Tablet ◽  
Scanning Calorimetry ◽  
Weight Variation

Objective: Matrix tablet approach is one of the delivery systems intended for poorly water-soluble drugs, like candesartan cilexetil (CC). CC is a class II drug used for the treatment of hypertension. Methods: Matrix tablets from (F1x to F18z) were prepared in the presence of β‑cyclodextrin. Matrix tablet formulation ensures control release of the drug and higher dissolution by β‑cyclodextrin. Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) were used to study compatibility. Results: The angle of repose determination showed good flow for most of the formulas, besides having good compressibility. Weight variation test for all formulas showed accepted value. Drug content measurement showed accepted values. Friability and hardness of tablets were within the allowed values. Higher tablet swelling was obtained for the formulas containing hydroxypropyl methylcellulose (HPMC) K100M (F3x and F15z), in which the ratio of the polymer was 1:1 and 1:3, respectively. In vitro release showed that F1x to F13z were studied depends on the type and amount of polymer, i.e., 1:1, 1:2, and 1:3, respectively. F1x release after 8 hours was 95%, which contains 1:1 polymer ratio in comparison to F3x, which showed 85% after 8 hours, which includes 1:3 (drug: HPMC K100). Kinetic studies showed a zero-order model. Conclusion: The use of β‑cyclodextrin modifies the release profile of the drug, and some control the more sustained-release formulas. The lower the time of the release but in a range that a sustained release of the drug was observed in comparison with the formulas prepared without β‑cyclodextrin.

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