scholarly journals SOLID DISPERSIONS: A METHOD TO IMPROVE BIOAVAILABILITY OF ORAL DRUG DOSAGE FORM

2019 ◽  
Vol 8 (3) ◽  
Author(s):  
Ritika Puri ◽  
Manisha Bhatti
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Systemic Circulation ◽  
Drug Dosage ◽  
Oral Drug ◽  
Surface Active Agents ◽  
Drug Dosage Form ◽  
Surface Active ◽  
Biopharmaceutical Classification System

Presently only few percent of drugs having high aqueous solubility, Number of drugs are belonging to biopharmaceutical classification system class II that means possessing  poor aqueous solubility  eventually  results in low level of drug in systemic circulation. To overcome this problem, various strategies have been come out into notion such as self emulsifying drug delivery system solid dispersions, use of surface active agents, complex formation. Solid dispersions is found to be promising approach to increase bioavailability by use of various polymers. This review focuses on the mechanism of drug release from solid dispersion with its method of preparation and applications. Key words: dissolution, particle size, solid dispersion

scholarly journals Nanosuspension: A Modern Approach In Drug Delivery System- A Review

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 1526-1530
Author(s):  
Ashish B. Budhrani ◽  
Kirti G. Sahu ◽  
Sukeshini B. Lote ◽  
Manish P. Deshmukh ◽  
Sagar B. Wankhede ◽  
...  
Keyword(s):  
Aqueous Solubility ◽  
Colloidal Dispersions ◽  
Modern Approach ◽  
System A ◽  
Surface Active Agents ◽  
Scale Range ◽  
Surface Active ◽  
The Stability ◽  
Evaluation Parameters ◽  
Biopharmaceutical Classification System

The drugs moiety included in Biopharmaceutical Classification System Class II and Class IV has low aqueous solubility and remedy for the solubility problem is nanotechnology techniques. Nanotechnology techniques play an important role at the molecular level and nano length scale size. To increase the dissolution rate of drug moiety which directly lead to increase bioavailability of drug depends on decrease drug particles into nano-scale range. Nanotechnology techniques in the pharmaceutical field include nanosuspension. Nanosuspension is biphasic dosage forms contain colloidal dispersions of nanosized drug particles which are stabilized by surface-active agents. Nanosuspension dosage form increases the stability and bioavailability of low aqueous soluble drugs. Solubility plays a crucial role in the effectiveness of drugs irrespective of the route of administration. Most of the presently investigated drug moieties having lower aqueous solubility and therefore has low bioavailability of drugs. The study is focused on formulation consideration, various methods of preparation along with evaluation parameters of nanosuspension.

scholarly journals Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion

2021 ◽  
Vol 9 (2) ◽  
pp. 127-135
Author(s):  
Anil Raosaheb Pawar ◽  
Pralhad Vitthalrao Mundhe ◽  
Vinayak Kashinath Deshmukh ◽  
Ramdas Bhanudas Pandhare ◽  
Tanaji Dilip Nandgude
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Peg 4000

The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.

scholarly journals Application of Solid Dispersion Technique to Improve Solubility and Sustain Release of Emamectin Benzoate

Molecules ◽  
2019 ◽  
Vol 24 (23) ◽  
pp. 4315
Author(s):  
Bin Bin Huang ◽  
Dong Xu Liu ◽  
De Kun Liu ◽  
Gang Wu
Keyword(s):  
Solid Dispersion ◽  
Rotational Speed ◽  
Mixing Time ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Feed Ratio ◽  
Emamectin Benzoate ◽  
Wettable Powder ◽  
Dispersion Technique ◽  
Pvp K30

The solid dispersion technique, which is widely used in the medical field, was applied to prepare a pesticide dosage form of emamectin benzoate (EM). The preparation, physicochemical characterization, aqueous solubility, release dynamics, photolytic degradation, bioactivity, and sustained-release effects of the prepared EM solid dispersions were studied by a solvent method, using polymer materials as the carriers. Water-soluble polyvinyl pyrrolidone (PVP) K30 and water-insoluble polyacrylic resin (PR)III were used as the carriers. The influence of various parameters, such as different EM:PVP-K30 and EM:PRIII feed ratios, solvent and container choices, rotational speed and mixing time effects on pesticide loading, and the entrapment rate of the solid dispersions were investigated. The optimal conditions for the preparation of EM-PVP-K30 solid dispersions required the use of methanol and a feed ratio between 1:1 and 1:50, along with a rotational speed and mixing time of 600 rpm and 60 min, respectively. For the preparation of EM-PRIII solid dispersions, the use of methanol and a feed ratio between 1:4 and 1:50 were required, in addition to the use of a porcelain mortar for carrying out the process. Under optimized conditions, the prepared EM-PVP-K30 solid dispersions resembled potato-like, round, and irregular structures with a jagged surface. In contrast, the EM-PRIII solid dispersions were irregular solids with a microporous surface structure. The results of X-ray powder diffraction (XRD), differential scanning calorimetry (DSC), ultraviolet (UV) spectrometry, and infrared (IR) spectrometry showed that the solid dispersions were formed by intermolecular hydrogen bonding. The solid dispersion preparation in PVP-K30 significantly improved the solubility and dissolution rate of EM, particularly the aqueous solubility, which reached a maximum of 37.5-times the EM technical solubility, when the feed ratio of 1:10 was employed to prepare the dispersion. Importantly, the wettable powder of EM-PVP-K30 solid dispersion enhanced the insecticidal activity of EM against the Plutella xylostella larvae. Furthermore, the solid dispersion preparation in PRIII afforded a significant advantage by prolonging the EM technical release in water at a pH below 7.0, especially when the PRIII content in solid dispersions was high. While the amplified toxicity of the wettable powder of EM-PRIII solid dispersions against the P. xylostella larvae showed no significant differences from that of the EM technical, the long-term toxicity under the field condition was much better than that of the commercially available EM 1.5% emulsifiable concentrate. Notably, solid dispersions with both the PVP-K30 and PRIII carriers reduced the effect of UV photolysis.

scholarly journals Design and Characterization of Phosphatidylcholine-Based Solid Dispersions of Aprepitant for Enhanced Solubility and Dissolution

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 407
Author(s):  
Sooho Yeo ◽  
Jieun An ◽  
Changhee Park ◽  
Dohyun Kim ◽  
Jaehwi Lee
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Promising Alternative ◽  
Dispersion System ◽  
Enhanced Solubility ◽  
Water Soluble Drugs

This study aimed to improve the solubility and dissolution of aprepitant, a drug with poor aqueous solubility, using a phosphatidylcholine (PC)-based solid dispersion system. When fabricating the PC-based solid dispersion, we employed mesoporous microparticles, as an adsorbent, and disintegrants to improve the sticky nature of PC and dissolution of aprepitant, respectively. The solid dispersions were prepared by a solvent evaporation technique and characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry, and X-ray powder diffraction. The FTIR results showed that aprepitant interacted with the PC carrier by both hydrogen bonds and van der Waals forces that can also be observed in the interaction between aprepitant and polymer carriers. The solid dispersions fabricated with only PC were not sufficient to convert the crystallinity of aprepitant to an amorphous state, whereas the formulations that included adsorbent and disintegrant successfully changed that of aprepitant to an amorphous state. Both the solubility and dissolution of aprepitant were considerably enhanced in the PC-based solid dispersions containing adsorbent and disintegrant compared with those of pure aprepitant and polymer-based solid dispersions. Therefore, these results suggest that our PC-based solid dispersion system is a promising alternative to conventional formulations for poorly water-soluble drugs, such as aprepitant.

scholarly journals Review: Solid Dispersion of Fenofibrate Using Poly Ethylene Glycol 6000

2021 ◽  
Vol 6 (6) ◽  
pp. 42-51
Author(s):  
Nelvia Helsinta ◽  
Auzal Halim ◽  
Maria Dona Octavia ◽  
Harrizul Rivai
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Literature Search ◽  
Solid Dispersions ◽  
Poly Ethylene Glycol ◽  
Peg 6000 ◽  
Poly Ethylene ◽  
Low Solubility ◽  
Biopharmaceutical Classification System

This review aimed to find information about the solubility of the fenofibrate solid dispersion system using PEG 6000. Fenofibrate is an antihyperlipidemic drug that belongs to the Biopharmaceutical Classification System Class II (BCS II) with low solubility. To find information was by conducting a literature search in national and international journals in the last ten years (2010-2020) through websites, namely Google Scholar, Science Direct, NCBI, ResearchGate, and other trusted journals. Several keywords were used as follows: fenofibrate, solid dispersion, PEG 6000, and dissolution rate. The results of several research journals showed that the solid dispersion of fenofibrate using PEG 6000 made by various methods causes a reduction in particle size to increase the solubility and dissolution rate of fenofibrate. The solid dispersions system was made using several methods, namely fusion (melting), solvent evaporation, dropping, and co-grinding, which is a technique used to increase the solubility of a drug. PEG 6000 was chosen as the carrier because it has high hydrophilicity, is non-toxic, inert, economical, has a low melting point, and is dense at melting temperature to withstand crystallization. Thus it can be concluded that the manufacture of solid dispersion of fenofibrate using PEG 6000 and several methods showed the same results, namely an increase in solubility and dissolution rate.

Formulation and Characterization of Solid Dispersion Containing Capsaicin for the Treatment of Diabetes

2020 ◽  
Vol 15 (3) ◽  
pp. 219-225
Author(s):  
Tapan Kumar Giri ◽  
Payel Roy ◽  
Subhasis Maity
Keyword(s):  
Thermal Analysis ◽  
Differential Thermal Analysis ◽  
Animal Study ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Peg 6000 ◽  
X Ray

Background: Chili peppers are widely used in many cuisines as a spice, and capsaicin is the main component. It has been reported that capsaicin acts as an antihyperglycemic agent. However, it shows poor aqueous solubility and bioavailability. Objective: The is to enhance the aqueous solubility and antihyperglycemic activity of capsaicin through solid dispersion formulation. Methods: Solid dispersions were prepared by the solvent evaporation method using polyethylene glycol 6000 (PEG 6000) as a hydrophilic carrier. Polymer-drug miscibility and drug crystallinity were characterized through the differential thermal analysis and X-ray powder patterns analysis. Solid dispersions were evaluated for solubility, in vitro drug dissolution and in vivo animal study in rats. Results: Results of x-ray powder patterns analysis showed a considerable reduction of drug crystallinity in solid dispersion. Differential thermal analysis result revealed a complete disappearance of capsaicin melting onset temperature in solid dispersion. From the phase solubility data, it was observed that the aqueous solubility of capsaicin was increased with increasing concentration of PEG 6000. Solid dispersion formulation showed considerable enhancement of in vitro release of drugs in comparison to pure capsaicin. In vivo animal study in rats shows that the solid dispersion containing capsaicin significantly reduced the blood glucose level in comparison to the free capsaicin. Conclusion: Higher anti-hyperglycemic effect of capsaicin loaded solid dispersion in comparison to the pure drug may be due to the enhancement of aqueous solubility of capsaicin. Thus, the solid dispersion of capsaicin showed a simple approach for capsaicin delivery with improved antidiabetic activity.

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

2019 ◽  
Vol 5 (1) ◽  
pp. 43-48
Author(s):  
Asriana Sultan ◽  
Nur Ida ◽  
Isriany Ismail
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Gastric Fluid ◽  
Physical Mixture ◽  
Dissolution Test ◽  
Dispersion Formula ◽  
Fluid Media ◽  
Low Solubility ◽  
Physical Mixtures ◽  
Biopharmaceutical Classification System

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.

scholarly journals Enhancement of Solubility and Dissolution Rate of Curcumin Using Porous Starch by Solid Dispersion Technique

2021 ◽  
Vol 23 (2) ◽  
Author(s):  
Indrayani D.Raut ◽  
◽  
Nikita D. Gidde D. Gidde ◽  
Priyanka V. Desai ◽  
Priyanka V. Bagade V. Bagade ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
In Vitro Dissolution ◽  
Hydrophilic Matrix ◽  
Novel Method ◽  
Improved Performance ◽  
Dispersion Technique ◽  
Low Solubility ◽  
Biopharmaceutical Classification System

The poor dissolution characteristics of biopharmaceutical class II drugs are a major concern for scientists in thepharmaceutical industry. Solid dispersion is introduced as a novel method for enhancement of solubility. Class IIdrugs are low solubility and high permeability according to the biopharmaceutical classification system and arepromising candidates for improving solubility and bioavailability through solid dispersion. The purpose of the present attempt is to prepare a solid dispersion of curcumin and porous starch in order to increase the solubility and dissolution of drugs that are poorlysoluble. Solid dispersions (SDs) of BCS-II drugs were prepared by ball milling in ratio of drug: polymer i.e. curcumin: porous starch (1:0.5, 1:1, 1:2 and 1:3). Further, SDs were investigated by solubility, FTIR, XRD, DSC, micromeritics, and in-vitro dissolution. . Conclusively, porous starch offers a hydrophilic matrix to deliver poorwater soluble drugs and Solid dispersion system have demonstrated an improved performance. Solid dispersionsystem have demonstrated an improved performance

scholarly journals Enhancement of solubility and dissolution rate of ebastine fast-disintegrating tablets by solid dispersion method

2020 ◽  
Vol 19 (9) ◽  
pp. 1797-1805
Author(s):  
Nayyer Islam ◽  
Muhammad Irfan ◽  
Nasir Abbas ◽  
Haroon Khalid Syed ◽  
Muhammad Shahid Iqbal ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Kneading Method ◽  
The Impact ◽  
Fast Disintegrating Tablets

Purpose: To investigate the efficiency of different solubilizing agents in improving solubility as well as dissolution rate of ebastine (a BCS class II drug) by incorporating prepared solid dispersion into fast disintegrating tablets.Method: The solubility of ebastine was determined in distilled water, lipids and solubilizing agents. Subsequently, the binary solid dispersions were prepared by kneading method using varying weight ratios of ebastine and solubilizing agents. The solid dispersions were then incorporated into fast disintegrating tablets (SD-FDT). Central composite rotatable design (CCD) was used to determine the impact of super disintegrating agents on disintegration time and friability of tablets. The solubility and dissolution rate of developed SD-FDT were compared with a marketed brand. The solid dispersion particles were characterized by Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder x-ray diffraction (P-XRD) and scanning electron microscopy (SEM).Results: The saturated solubility of pure ebastine in water was 0.002 ± 0.041 mg/ml while the aqueous solubility of EBT/poloxamer solid dispersion SET3 (P) was 0.018 ± 2.510 mg/ml; on the other hand, EBT/soluplus solid dispersion SET1(S) has an aqueous solubility of 0.242 ± 1.390 mg/ml. Within 30 min, drug release was 14.00 ± 1.77, 78.00 ± 2.31 and 98.70 ± 2.54 % from pure EBT, SET3 (P) and SET1(S), respectively.Conclusion: The solubility and dissolution rate of ebastine has been successfully enhanced by incorporating its solid dispersion in fast-disintegrating tablets (SD-FDT). Keywords: Ebastine, Solid dispersion, Poloxamer 188, Soluplus, Solubility, Dissolution

scholarly journals “ENHANCING TELMESARTAN BY USING SOLID DISPERSION TECHNIQUES”

2021 ◽  
pp. 134-138
Author(s):  
Praveen Kumar Shakya ◽  
Sanjesh Kumar ◽  
Mansi Singh ◽  
Savita Savita
Keyword(s):  
Solid Dispersion ◽  
Therapeutic Potential ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Angiotensin Ii Receptor ◽  
Covalent Interaction ◽  
Wide Range ◽  
Inert Carrier ◽  
Categorization System ◽  
Direct Acting

Telmisartan (TLM) is an angiotensin II receptor antagonist used in the treatment of hypertension. Telmesartan (TLM) is an orally active direct-acting Angiotensin1receptor antagonist and possess therapeutic potential in the pharmacotherapy of hypertension. Telmisartan is classified as a class II medicine by the BCS (biopharmaceutical categorization system), and it is nearly insoluble in water, with a low solubility profile and poor absorption. Drugs with poor aqueous solubility are still an ongoing challenge in the successful formulation of therapeutic products due to their low oral bioavailability. Solid dispersions are a dispersion mixture of one or more active ingredients in an inert carrier at the solid state prepared by melting, solvent, solvent-melting or other methods. Cyclodextrins(CDs) with their cylinder-shaped cavities are capable to form inclusion complexes with a wide range of commonly used drugs. Complexation of molecules to CDs occurs through a non-covalent interaction between the molecule and the CD cavity. This is a dynamic process whereby the guest molecule continuously associates and dissociates from the host CD. The present study is to improve the solubility of Telmisartan by solid dispersion techniques using various methods and proved to be effective for further pharmaceutical usage.

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