scholarly journals Understanding the Role of Sodium Lauryl Sulfate on the Biorelevant Solubility of a Combination of Poorly Water-Soluble Drugs Using High Throughput Experimentation and Mechanistic Absorption Modeling

2019 ◽  
Vol 22 ◽  
pp. 221-246 ◽  
Author(s):  
Matthew Nathan Bahr ◽  
Dimple Modi ◽  
Sarsvatkumar Patel ◽  
Gossett Campbell ◽  
Gregory Stockdale
Keyword(s):  
High Throughput ◽  
Dosage Form ◽  
Water Soluble ◽  
Lauryl Sulfate ◽  
Solid Dosage Form ◽  
Solid Dosage ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Free Energy Of Micellization

This study investigates the influence of surfactant sodium lauryl sulfate (SLS) on the solubility of poorly-water soluble drug substances, model Compound X and Compound Y, used in a fixed dose combination oral solid dosage form. To determine the impact of SLS concentration on the solubility of compounds X and Y, we experimentally determined the critical micelle concentration (CMC) of SLS in water, simulated gastric fluid (SGF), and fed state simulated intestinal fluid (FeSSIF) in the presence of Compound X and Compound Y using UV/Visible spectrophotometry at 25°C. The aggregation of SLS was characterized by calculating the standard Gibbs free energy of micellization in all the media investigated.  To enhance the understanding of SLS aggregation, high throughput experiments and in-vivo mechanistic modelling were used to determine the effect of increasing levels of SLS on the solubility of compounds X and Y as both single agent and combination products to be formulated into a suitable oral solid dosage form. Micellar formation of SLS is a spontaneous process as shown by the negative values of the standard free energy of micellization. The CMC of SLS in the various media investigated in the presence of compounds X and Y decreases in the following order: water> FeSSIF> SGF. However, the aggregation of SLS in the various media is overall more spontaneous in the following order: SGF>FeSSIF>water. Using high throughput experimentation and in-vivo mechanistic modelling, it was determined that a combination oral solid product of compounds X and Y will have optimum solubility and in-vivo absorption if 2 mg of SLS was used in the oral solid dosage form.  The results obtained from this study will help broaden the understanding of the micellization process involving SLS and poorly-water soluble drugs used in combination oral solid dosage forms.

Encapsulation of lipid-based formulations in porous carriers for controlled drug delivery

2021 ◽  
Vol 28 ◽  
Author(s):  
Phuong H.L. Tran ◽  
Thao T.D. Tran
Keyword(s):  
Porous Materials ◽  
Controlled Drug Release ◽  
Water Soluble ◽  
Solid Dosage Forms ◽  
Pharmaceutical Ingredients ◽  
Solid Dosage ◽  
Water Soluble Drugs ◽  
Porous Carriers ◽  
Poorly Water Soluble ◽  
And Control

: Lipid-based formulations have recently been investigated as a promising approach to enhance the bioavailability of drugs, especially poorly water-soluble drugs. The encapsulation of lipid-based formulations in porous materials can result in a transformation of liquids or semisolid forms to solid dosage forms. Moreover, the specific structure of porous carriers could offer an enhanced ability to load and control active pharmaceutical ingredients. Although there have been prominent reports on lipid-based formulations and porous materials as promising technologies for controlled drug release, the overall methods of encapsulating lipid-based formulations need to be discussed for further formulation investigations. This review aims to present the key strategies used for producing porous carriers containing lipid-based formulations. We also discuss methods that enhance the encapsulation efficiency of loaded drugs within porous structures (instead of lipid-based formulations). Moreover, the critical factors that affect tablet formation are outlined. This overview of lipid-based formulations encapsulated within porous materials provides a summary of the technical methods used in the development of these formulations and their clinical translation.

In-Vitro Functionality of Clozapine Biphasic Release Minitablet Using Advanced Statistical Tools

2021 ◽  
Vol 11 ◽  
Author(s):  
Hardik Rana ◽  
Rushikesh Chaudhari ◽  
Vaishali Thakkar ◽  
Tejal Gandhi
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Ethyl Cellulose ◽  
Dosage Form ◽  
Immediate Release ◽  
Solid Dosage Form ◽  
Solid Dosage ◽  
Precipitation Inhibitor

Background: The better control of the drug release with immediate effect is the major concern to achieve better therapeutic action and patient compliance. The failure of the solid dispersion complex during storage as well as in-vivo is another concern for the oral solid dosage form. Objective: The prime objective of the present study was to optimize the biphasic minitablet incorporating quality by design approach using the combination of waxy erodible and water-impermeable excipients. Exploration of Soluplus as a precipitation inhibitor and Dexolve as a solubility enhancer in oral solid dosage form was the secondary objective. Methods: The drug-Excipient compatibility study was assessed by FTIR. Clozapine was chosen as a model drug that has poor aqueous solubility. The complex was formulated using B-cyclodextrin or HP B-CD or Dexolve by kneading method. The screening of solubility enhancers and their amount were performed based on phase solubility study. The precipitation inhibitor was screened as per the parachute effect study. Immediate release minitablets were formulated using a direct compression method using different disintegrating agents. The IR minitablets were evaluated for different evaluation parameters. The sustained release minitablets was formulated by hot-melt granulation technique incorporating the Precirol ATO 5 as a waxy excipient and ethyl cellulose as water impermeable excipient. The SR minitablet was optimized using a central composite design. The amount of Precirol ATO 5 and ethyl cellulose were chosen as independent variables and % drug release at 1, 6, and 10 h was selected as responses. The designed batches were evaluated for different pre and post compressional parameters. The IR and SR minitablets were filled in a capsule as per dose requirement and evaluated for in-vitro drug release. The in-vivo plasma concentration was predicted using the Back calculation of the Wagner – Nelson approach. Results: Drug – Excipient study revealed that no significant interaction was observed. Dexolve was screened as a solubility enhancer for the improvement of the solubility of clozapine. The Soluplus was chosen as a precipitation inhibitor from the parachute effect study. The immediate-release tablet was formulated using Prosolv EASYtab SP yield less disintegration time with better flowability. The sustained release mini-tablet was formulated using Precirol ATO 5 and ethyl cellulose. Two-dimensional and three-dimensional plots were revealed the significant effect of the amount of Precirol ATO 5 and ethyl cellulose. The overlay plot locates the optimized region. The in-vitro drug release study revealed the desired drug release of the final combined formulation. The in-vivo plasma concentration-time confirms the drug release up to 12h. Conclusion: The biphasic mini-tablets were formulated successfully for better control of drug release leads to high patient compliance. The use of soluplus as a precipitation inhibitor is explored in the oral solid dosage form for a poorly aqueous drug. Prosolv EASYtab SP was incorporated in the formulation as super disintegrant. The amount of Precirol ATO 5 and ethyl cellulose had a significant effect on drug release in sustained-release minitablet. The approach can be useful in the industry.

scholarly journals Comparative Plasma Exposure of Albendazole after Administration of Rapidly Disintegrating Tablets in Dogs

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Silvina G. Castro ◽  
Alicia Dib ◽  
Gonzalo Suarez ◽  
Daniel Allemandi ◽  
Carlos Lanusse ◽  
...  
Keyword(s):  
Dosage Form ◽  
Solid Dispersions ◽  
Plasma Exposure ◽  
Solid Dosage Form ◽  
Solid Dosage ◽  
Drug Plasma ◽  
Key Factor

The main objectives of this study were (a) to evaluate thein vitroperformance of the rapid disintegration tablets as a way to improve the solid dispersions and (b) to study thein vivopharmacokinetics of the albendazole modified formulation in dogs. Rapid disintegration of tablets seems to be a key factor for efficiency of solid dispersions with regard to improvement of the albendazole bioavailability. Thein vivoassays performed on dogs showed a marked increase in drug plasma exposure when albendazole was given in solid dispersions incorporated into rapid disintegration tablets compared with conventional solid dosage form.

REVIEW ON FAST DISSOLVING TABLET BY SOLID DISPERSION APPROACH

2021 ◽  
pp. 2840-2845
Author(s):  
V. Namitha
Keyword(s):  
Solid Dispersion ◽  
Dosage Form ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
And Performance ◽  
High Level ◽  
Determining Factor ◽  
Mouth Dissolving Tablet

Tablet is found to be the most popular dosage form among all existing dosage form. However, in certain occurrences as a result of the huge size of dosage forms, and in the uncooperative, pediatric and dysphasia patients, it might make a few problems, to avoid this issues, another type of dosage form is created, which is known as fast dissolving tablet or mouth dissolving tablet. These are the high level dosage form which breaks down within seconds when placed on the toungue. Mouth dissolving tablets have become impressive consideration as a better option in contrast to others because of better convenience to patients. This review discusses the method of preparation, properties, mechanisms; capsules to be incorporated inside the mouth dissolving pill and evaluation of the drugs are emphasized. The solid dispersion is one of the established solubilization techniques for poorly water-soluble drugs. It is basically the interaction between drug and polymer, and hence it is found to be the determining factor in its design and performance. This review additionally summarizes our knowledge on solid dispersions both in the solid as well as liquid state.

Sign in / Sign up

Export Citation Format

Share Document