Types Of Excipients Research Articles

"The More, the Better?": The Impact of Sugar-to-Protein Molar Ratio in Freeze-Dried Monoclonal Antibody Formulations on Protein Stability.

Lyophilization is widely used to ensure the stability of protein drugs by minimizing chemical and physical degradation in the dry solid state. To this end, proteins are typically formulated with sugars that form an amorphous immobilizing matrix and stabilize hydrogen bonds replacing water molecules. The optimal amount of sugar required and protein stability at low excipient-to-protein molar ratios are not well understood. We investigated this by focusing on the physical stability of formulations, reflecting highly concentrated monoclonal antibody (mAb) lyophilizates at low sucrose to mAb ratios between 25:1 and 360:1. Additionally, the impact of different excipient types, buffer concentrations, and polysorbates was studied. The mAb stability was evaluated over up to three months at 25 and 40 °C. We investigated the "the more, the better" approach regarding excipient usage in protein formulation and the existence of a potential stabilizing threshold. Our findings show efficient monomeric content preservation even at low molar ratios, which could be explained based on the water replacement theory. We identified an exponential correlation between the sucrose to protein molar ratio and aggregate formation and found that there is no molar ratio threshold to achieve minimum stabilization. Sucrose demonstrated the best stabilization effect. Both mannitol, used as a cryoprotectant at low concentrations, and arginine reduced aggregation compared to the pure mAb formulation. The higher ionic strength of 5 mM histidine buffer enhanced protein stability compared to that of 0.1 mM histidine buffer, which was more pronounced at lower molar ratios. The addition of polysorbate 20 contributed an additional interfacial stabilizing effect, complementing the cryoprotective and lyoprotective properties of sucrose. Overall, a model could be developed to optimize the quantity of sugar required for protein stabilization and facilitate a more rational design of protein lyophilizates. The molar ratio of sugar to protein for high-concentration mAb products is limited by the acceptable tonicity, but we showed that sufficient stabilization can be achieved even at low molar ratios.

DSC reveals the excipient impact on aggregation propensity of pharmaceutical peptides during freezing

Pharmaceutical peptides are susceptible to aggregation in solution, making stabilization by addition of suitable excipients essential. To investigate this stabilization, lengthy and cost-intensive experiments are often necessary. In this work, a differential scanning calorimetry (DSC) based method was developed that allows a rapid assessment of the stabilization properties of excipients regarding the aggregation of pharmaceutical peptides. The stabilization properties of investigated excipients are derived from the thermal behavior around Tg', the glass-transition temperature of the excipient-rich phase after freezing, as a function of repeated freeze-thaw cycles.The pharmaceutical peptide glucagon was investigated in combination with the excipients trehalose and lactose. In addition to the type of excipient, the concentration ratio of peptide/excipient was also varied. Lactose proved to better stabilize glucagon solutions compared to trehalose. On the one hand, the onset of aggregation could be delayed and after aggregation started the aggregation kinetics were slowed down. In addition, it was shown that a high excipient to peptide ratio, regardless of the type of excipient tested, reduces the aggregation tendency of glucagon.

Investigation into the swelling and dissolution behaviour of Polymer-Excipient blends of PEO Utilising dissolution imaging

The use of dissolution imaging in analysing the behaviourof hydrophilic matrices and various types of excipients is examined in this study.The main aim was to investigate how different ratios of excipients with different solubility properties, such as lactose, microcrystalline cellulose, and dicalcium phosphate impact on the swelling properties and propranolol hydrochloride (PPN) release characteristics of polyethylene oxide matrix compacts. The surface properties of the compacts were investigated using a focus variation microscope after which dissolution studies were conducted to determine compact swelling and drug release properties. Smr2, a surface parameter representing the percentage of deeper valley structures on the surface, was used to calculate the proportion of the compact surface available for retaining lubrication (dissolution media in this case). Smr2 values of 83 and 84 were measured for the 1:1 and 1:3 PEO lactose compacts, respectively. This parameter utilised in this experiment gives an indication of the compact surface available for the initial hydration process and suggests a higher rate of hydration for the 1:1 and 1:3 PEO lactose compacts. The swelling studies revealed that a higher PEO ratio (3:1) resulted in more extensive gel layer formation as compared to the 1:3 compacts. All PEO:excipient compacts exhibited faster drug release than the compacts comprising PEO as the sole excipient. The quantity of PEO present was thus crucial in influencing the capacity of the matrix to control the release of PPN. This study underscores the potential for modifying drug release by altering the quantity of the matrix gel-former (PEO in this case) as well as the type or ratio of excipient used. The study also highlights the novelty of using UV dissolution imaging to image and quantify swelling and drug dissolution processes as well as providing qualitative observations such as channel formation which can support formulation optimisation and mechanistic understanding.

Excipient effects on supersaturation, particle size dynamics, and thermodynamic activity of multidrug amorphous formulations

Multidrug formulations enhance patient compliance and extend the life cycle of pharmaceutical products. To overcome solubility challenges for multidrug combinations, amorphous formulations are commonly used. However, the excipients for creating amorphous formulations are often selected without an understanding of their effects on the bioavailability of the drugs. In this context, we investigated the impact of three types of excipients (polymers, surfactants and amino acids) on the supersaturation and thermodynamic activity of multidrug amorphous formulations. Additionally, we studied the particle size dynamics of the colloidal phase formed as a result of liquid–liquid phase separation. The amorphous solubility of two drugs, atazanavir and ritonavir, was determined in solutions containing predissolved excipients and the particle size dynamics of the colloidal particles was measured by dynamic light scattering. Dissolution experiments of atazanavir and ritonavir were conducted in predissolved sodium dodecyl sulfate (SDS), an anionic surfactant, and alanine solutions under non-sink conditions. Membrane transport of the drugs was evaluated using a MicroFLUX setup. The polymers had only minor effects on the amorphous solubility, but SDS significantly increased the solubilities of both drugs. In contrast, the other non-ionic surfactants and amino acids reduced the solubility of atazanavir but had no negative effect on ritonavir. Polymers were effective in maintaining supersaturation and preventing the coarsening of the colloidal particles. Conversely, alanine was neither able to inhibit the solution crystallization nor increase the flux of either drug. Despite the increase in the amorphous solubility of both drugs in SDS, flux was reduced. These results highlight the importance of properly selecting excipients for supersaturating amorphous formulations. The choice of excipient impacts the thermodynamic activity, the phase behaviour of the drugs and hence, the resulting absorption after oral intake.

Understanding Excipient-Induced Crystallization of Spray-Dried Amorphous Solid Dispersion

This study investigates the compatibility of excipients with the model system SDI-X and their role in the induced crystallization of the amorphous compound-X in tablet formulations. We aimed to establish a straightforward and practical screening approach for evaluating excipient-induced crystallization of SDI in tablet matrices. Three methodologies—binary powder mixture, binary compact, and bilayer tablets—were employed to qualitatively and quantitatively evaluate the recrystallization of SDI-X with various excipients under accelerated storage conditions. The results demonstrated that binary compacts, providing direct physical contact between SDI-X and excipients, are superior in reflecting realistic drug-excipient contact within pharmaceutical tablets, enabling a more accurate assessment of excipient-induced crystallization for SDI-X. In contrast, the broadly used conventional binary blends can significantly underestimate this risk due to insufficient proximity. In addition, the bilayer tablets further confirmed that crystallization initiates at the contact surface between SDI-X and the excipients. The study highlighted that not only hygroscopicity but also the type of excipient and its physical contact with SDI-X significantly influence the recrystallization extent and rate of SDI-X. Interestingly, less hygroscopic diluents such as mannitol and lactose induced much higher levels of crystallization of SDIs, contrary to expectations based on moisture content alone. This suggests that the excipient type and contact surface are more critical in inducing recrystallization than just the level of moisture. The findings emphasize the need for careful excipient selection, study design, and sample preparation to enable appropriate assessments of SDI-excipient compatibility.

Formulation, Characterization and Stability Aspects of Mesoporous Silica Nanoparticles

Mesoporous silica nanoparticles are a type of inorganic nanoparticles having mesopores of 2 to 50 nm in size. The nanosized mesoporous particles of silica facilitate endocytosis in drug targeting without any side effects. Mesoporous silica nanoparticle (MSN) can be used to deliver a variety of therapeutic agents or gene delivery through active or chemical adsorption. MSNs can be used in the field of biomedical for the detection and treatment of various diseases like cancers, infection, inflammation, diabetes, bone-related disorders, cardiac diseases, neurodegenerative diseases, etc. The unique characteristics of MSNs in the form of easily adjustable pore size, surface area, particle size, pore volume, and surface morphology are advantageous not only in the biomedical field but also in the fields of biosensors, imaging, agriculture, thermal energy, and catalysis, etc. MSNs provide high surface area, easy surface functionalization, and controlled drug release. MSNs are formulated after condensation of silica in the presence of molecular templates like surfactants and polymers. This review article focused on giving in-depth knowledge about formulation techniques. Various types of excipients, such as catalysts, silica, solvents and surfactants utilized for the formulation of silica-based nanoparticles, have been summarized. The characterization of MSNs using suitable techniques was also reviewed. The stability of MSNs and factors affecting their stability is a crucial part of formulation development that is discussed here

Determination of fatty acid composition after saponification of common oil pharmaceutical excipients by supercritical fluid-evaporative light scattering method and its application in oil identification

Oils and fats are commonly used in the pharmaceutical industry as solvents, emulsifiers, wetting agents, and dispersants, and are an important category of pharmaceutical excipients. Fatty acids with unique compositions are important components of oil pharmaceutical excipients. The Chinese Pharmacopoeia provides clear descriptions of the fatty acid types and limits suitable for individual oil pharmaceutical excipient. An unqualified fatty acid composition or content may indicate adulteration or deterioration. The fatty acid composition, as a key indicator for the identification and adulteration evaluation of oil pharmaceutical excipients, can directly affect the quality and safety of oil pharmaceutical excipients and preparations. Gas chromatography is the most widely used technique for fatty acid analysis, but it generally requires derivatization, which affects quantitative accuracy. Supercritical fluid chromatography (SFC), an environmentally friendly technique with excellent separation capability, offers an efficient method for detecting fatty acids without derivatization. Unlike other chromatographic methods, SFC does not use nonvolatile solvents (e. g., water) as the mobile phase, rendering it compatible with an evaporative light-scattering detector (ELSD) for enhanced detection sensitivity. However, the fatty acids in oil pharmaceutical excipients exist in the free and bound forms, and the low content of free fatty acids in these oil pharmaceutical excipients not only poses challenges for their detection but also complicates the determination of characteristic fatty acid compositions and contents. Moreover, the compositions and ratios of fatty acids are influenced by environmental factors, leading to interconversion between their two forms. In this context, saponification provides a simpler and faster alternative to derivatization. Saponification degrades oils and fats by utilizing the reaction between esters and an alkaline solution, ultimately releasing the corresponding fatty acids. Because this method is more cost effective than derivatization, it is a suitable pretreatment method for the detection of fatty acids in oil pharmaceutical excipients using the SFC-ELSD approach. In this study, we employed SFC-ELSD to simultaneously determine six fatty acids, namely, myristic acid, palmitic acid, stearic acid, arachidic acid, docosanoic acid, and lignoceric acid, in oil pharmaceutical excipients. Saponification of the oil pharmaceutical excipients using sodium hydroxide methanol solution effectively avoided the bias in the determination of fatty acid species and contents caused by the interconversion of fatty acids and esters. The separation of the six fatty acids was achieved within 12 min, with good linearity within their respective mass concentration ranges. The limits of detection and quantification were 5-10 mg/L and 10-25 mg/L, respectively, and the spiked recoveries were 80.93%-111.66%. The method proved to be sensitive, reproducible, and stable, adequately meeting requirements for the analysis of fatty acids in oil pharmaceutical excipients. Finally, the analytical method was successfully applied to the determination of six fatty acids in five types of oil pharmaceutical excipients, namely, corn oil, soybean oil, coconut oil, olive oil, and peanut oil. It can be combined with principal component analysis to accurately differentiate different types of oil pharmaceutical excipients, providing technical support for the rapid identification and quality control of oil pharmaceutical excipients. Thus, the proposed method may potentially be applied to the analysis of complex systems adulterated with oil pharmaceutical excipients.

Мultivariate analysis for rapid screening and prediction of solid-state compatibility in pharmaceutical preformulation studies-paving the road for machine learning

Multivariate analysis models were developed to evaluate the results obtained from a compatibility study designed for ibuprofen with a large group of different types of excipients, as a possible approach for rapid screening of the incompatibility between the active pharmaceutical ingredient (API) and excipients. The solid-state characterization of the binary mixtures was performed by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). Principal component analysis (PCA) and partial least squares-discriminant analysis (PLS-DA) using SIMCA® software were applied for evaluation of the experimentally obtained results. The optimal PCA model for the FTIR spectra explains 96.2 % of the variations in the dataset with good statistical indicators (R2X = 0.960, Q2 = 0.900), which was also the case for the PCA model for the DSC curves (R2X = 0.981, Q2 = 0.866). The applied PLS-DA models have shown similar behaviour to the PCA. Moreover, the main spectral variations in the FTIR spectra and the thermal events in the DSC data were attributed the highest variable importance for the projection (VIP) scores in the corresponding VIP plots, confirming the model capability for predicting ibuprofen interactions. Furthermore, the prediction power of the optimal models for FTIR and DSC experimental data was evaluated by the root mean square error of prediction (RMSEP) of 0.10 and 0.16, respectively. The obtained results demonstrated the potential of multivariate statistical analysis as a machine learning-based technique for screening and prediction of ibuprofen-excipients solid-state compatibility in the preformulation phase of the pharmaceutical development of dosage forms.

Computational Procedure for Predicting Excipient Effects on Protein-Protein Affinities.

Protein-protein interactions lie at the center of many biological processes and are a challenge in formulating biological drugs, such as antibodies. A key to mitigating protein association is to use small-molecule additives, i.e., excipients that can weaken protein-protein interactions. Here, we develop a computationally efficient model for predicting the viscosity-reducing effect of different excipient molecules by combining atomic-resolution MD simulations, binding polynomials, and a thermodynamic perturbation theory. In a proof of principle, this method successfully ranks the order of four types of excipients known to reduce the viscosity of solutions of a particular monoclonal antibody. This approach appears useful for predicting the effects of excipients on protein association and phase separation, as well as the effects of buffers on protein solutions.

Natural Excipients: Role in Nano Drug Delivery System

Background:: Excipients are increasingly employed in novel dosage forms to accomplish specialized roles, and they also directly or indirectly alter the extent and rate of drug release and absorption. The trend toward using plant-based and natural goods has raised demand and, in some ways, replaced synthetic additives with natural ones. Natural and semisynthetic materials offer various advantages over synthetic materials since they are chemically inert, less toxic, less expensive, biodegradable, increase product shelf life, and are widely accessible. Objectives:: This review aims to cover the natural excipients’ role in nanoformulations and associated prospects. Methods:: More than 500 manuscripts were collected from ScienceDirect, PubMed, google, and other sources; however the manuscripts were excluded based on their relevance to the subject and finally 80 manuscripts were analyzed for the data. Results:: The substation of synthetic lipids with natural and semisynthetic for developing lipid-based nano drug delivery, and the use of gelatin and chitosan in developing encapsulated and nano particulates are a few examples to understand the above-mentioned transition. Conclusion:: This review provides an overview of the types of excipients used in the formulation of novel drug delivery systems with special emphasis on their characteristics, safety aspects, benefits associated, and common methods through, which they are employed in nanoformulations.

Compatibility Study of Ketoprofen With Selected Excipients Used in Solid Dosage Forms: Experimental Design Approach

A good understanding of the physico-chemical characteristics of a drug substance and excipients is necessary to obtain a safe and effective drug dosage form. Based on the current recommendations of the regulatory agencies (EMA, FDA) regarding the implementation of the Quality by Design concept at the drug product development stage, this article is focused on the application of the experimental design approach at the preformulation studies. The purpose of this work was the implementation of experimental design methodology in a compatibility study between ketoprofen (non-steroidal anti-inflammatory drug) and selected solid dosage forms excipients. The fractional factorial design was used to generate a matrix of multi-component mixtures of ketoprofen and selected excipients. In order to accelerate any chemical incompatibilities, the received mixtures were exposed to elevated temperature and humidity (60°C/75% RH) in a climate chamber for 3 weeks. The ketoprofen-excipients compatibility was studied by means of the RP-HPLC method. It was confirmed that the type of disintegrant had a strong impact on ketoprofen degradation. The incompatibility in mixtures of ketoprofen with sodium starch glycolate was indicated. According to literature data, it may be the result of a decrease in crystallinity and thus a decrease in the stability of ketoprofen in the presence of sodium starch glycolate. The effects of the other types of excipients were statistically insignificant (p > 0.05). The applied experimental design methodology allowed for a rational selection of optimal excipients and thus, this approach may support significantly decision-making in the pharmaceutical industry.

FLOWABILITY PROPERTIES OF BINARY POWDER MIXTURES CONTAINING DATES POWDER (PHEONIX DACTYLIFERA) MIXED WITH LACTOSE MONOHYDRATE AND MICROCRYSTALLINE CELLULOSE BASED EXCIPIENTS

Powder flow is important in powder processing industries to obtain a quality by design product and efficient manufacturing process. Poor powder flowability can cause problems especially during high speed tableting and capsule filling processes. In this study, dates powder (DP), lactose monohydrate powder, and two types of microcrystalline-based powder excipients evaluated for their flow properties as a binary mixture. Angle of repose (AoR), Hausner ratio (HR) and Carr index (CI) were used to characterize the extent of the powder cohesion. The results show that generally, as particle size increases, values of AoR generally decreases, depicting lower flowability characteristics with decreasing binary mixture particle size. However, HR and CI flowability indicators give contrasting flowability characteristics for the binary mixture containing lactose monohydrate and dates powder.

The Influence of the Intergranular Superdisintegrant Performance on New Drotaverine Orodispersible Tablet Formulations.

The main objective of this study consists in establishing the influence of the intergranular superdisintegrant on the specific properties of drotaverine hydrochloride fast-dissolving granules (DROT-FDGs) and orodispersible tablets (DROT-ODTs). The orodispersible tablets were obtained by the compression of the FDGs and excipient mixture with an eccentric tableting machine. To develop DROT-ODTs, two types of superdisintegrant excipients in different concentrations (water-soluble soy polysaccharides (SSP) (1%, 5%) and water-insoluble soy polysaccharides-Emcosoy® STS IP (EMCS) (1%, 3%, 5%)) were used, resulting in five formulations (D1-D5). The DROT-FDGs and the DROT-ODTs were subjected to pharmacotechnical and analytical evaluation. All the orodispersible tablets obtained respect the quality requirements in terms of friability (less than 1%), crushing strength (ranging between 52 N for D2 and 125.5 N for D3), and disintegration time (<180 s). The in vitro release of drotaverine from ODTs showed that all formulations presented amounts of active substance released greater than 85% at 10 min. The main objective, developing 30 mg DROT-ODTs for children aged between 6 and 12 years by incorporating the API in FDGs, was successfully achieved.

When it is too much: Identifying butamben excess on the surface of pharmaceutical preformulation samples by Raman mapping

Butamben is a topical local anesthetic which formulation in lipid-based drug delivery systems (DDS) is challenging due to its affinity for hydrophilic excipients. This means that a medium polarity excipient is preferred for the development of a stable nanostructured lipid carrier (NLC) formulation. In turn, in NLC, the type and number of excipients will determine the active pharmaceutical ingredient (API) solubility and the maximum drug upload. To solve this dilemma and get the best formulation, a throughout screening study to evaluate API solubilization in different excipients was carried out. Subsequently, excipients with different solubilization capacities were selected for microscopic evaluation by Raman mapping, and in turn analysis of the distributional homogeneity index (DHI) and standard deviation of the histograms allowed solving the posed question. Design of experiments (DoE) was employed to understand better the interactions between the excipients; linear and higher-order models were obtained with R2 above of 0.8824. Even though DHI is a good parameter to be used as response, an API concentration higher than 30% (w/w) provided a homogeneous surface in case of good miscibility and, in this case, this parameter needs to be employed with an inspection and/or evaluation of other parameters. A curve of concentration vs. mean scores of images proved to be an alternative to identify the saturation/limit of linear range.

Modeling the Impact of Excipients Selection on Nitrosamine Formation towards Risk Mitigation.

Risk control for nitrosamine impurities in drug products is currently a major challenge in the industry. Nitrosamines can form during drug product manufacturing and storage through the reaction of nitrites with amine-containing APIs or impurities. The level of nitrites in excipients and the rate of reaction often control the build-up of nitrosamine. Although the variability in nitrite levels across excipient types and suppliers is well recognized, the impact of excipient selection on the level of nitrosamine formed has not been systematically studied. This gap of knowledge is addressed in the current work. We present theoretical case studies of formulations where microcrystalline cellulose (MCC), or lactose supplier, or superdisintegrant type are changed in pursuit of lower levels of nitrite. The impact of the average, maximum, and minimum levels of nitrites in each excipient on nitrosamine formation in the dosage form is calculated. The input data for this calculation are the formulation composition, nitrosamine molecular weight (MW), percentage of conversion, and nitrite levels per excipient. The percentage of conversion (based on the formulation and manufacturing variables) and nitrite levels were taken from the recent literature. We show that changing the supplier of a single excipient, or of the three most critical excipients, can reduce nitrosamine formation by up to -59% and -89%, respectively. We also show that high-risk formulations, e.g., high MW nitrosamines, high dosage weights, and high percentages of conversion (e.g., wet granulation), can often be de-risked below regulatory acceptable daily intake via careful excipient selection. Finally, we provide an open-access tool that enables users to calculate the theoretical formation of nitrosamines in their specific formulations. This calculation template can be used for (i) the preliminary screening of the risk of nitrosamine formation in drug products and (ii) the preliminary assessment of the impact of excipient selection for risk mitigation.

Pharmacotechnical, Physico-Chemical, and Antioxidant Evaluation of Newly Developed Capsule Formulations.

The excess of free radicals causes numerous imbalances in the body that lead to premature aging, the degradation of internal structures, and the appearance of numerous pathologies responsible for the increased risk of premature death. The present work aims to evaluate the physical, chemical, pharmacotechnical, and antioxidant activity of newly achieved capsule formulations. These two formulations were F1a.i., which contains melatonin:biotin:coenzyme Q10 (weight ratio of 1:2:60), and F2a.i., which contains quercetin:resveratrol:biotin:coenzyme Q10 (weight ratio of 10:10:1:10). The adequate selection of the excipient types and amounts for final capsule formulations (F1c.c., F2c.c.) was based on preformulation studies performed on the powders containing active ingredients. The antioxidant activity assessed using three methods (ABTS, DPPH, and FRAP) compared with acid ascorbic as a positive control demonstrated that the F2c.c. formulation possesses the strongest antioxidant capacity. The results confirmed the suitable formulation and the accurate selection of the types and amounts of active ingredients, as well as the auxiliary excipients used in newly developed capsule formulations as supplements with an excellent antioxidant effect on the human body.

Formulation and Evaluation of Herbal Facewash Preventing Dermatological Problem

Abstract: Facewash is one type of cosmeceuticals as well as semisolid dosage forms used for external purposes. It is applied on the skin surface to protect the skin from various microbial attacks. This type of cosmeceutical is also used to clean different types of skin problems like skin acne, skin pimples, skin rashes, dark circles, black spot, oily skin, skin discolored, etc. In this study, we have formulated one herbal face wash containing different extraction of herbal materials like fresh aloevera gel, leaves of neem, turmeric, lemon juice, Fresh leaves of Tulsi, fresh pudina leaves, Chandan, liquorice, Honey, Coffee, Multani mati, rose water as well as various types of excipients like sodium CMC, sodium lauryl sulphate, sodium benzoate, glycerol and distilled water. After formulation study we focused the evaluation cum validation of the formulated new herbal facewash like testing of pH ,Spreadability test, foam forming test, etc.

Effect of co-processed excipient type on properties of orodispersible tablets containing captopril, tramadol, and domperidone

An important feature of orodispersible tablets (ODTs) is the convenient administration of the drugs, in some cases, faster onset of action, stability maintenance, and dose precision. This work focused on the preparation of ODTs containing mannitol-based co-processed excipients Prosolv® ODT G2, Ludiflash® and Parteck® ODT in combination with tramadol, captopril, and domperidone by direct compression.Prosolv® ODT G2 showed high energy of plastic deformation due to the content of microcrystalline cellulose. Parteck® ODT provided compact tablets due to the content of granulated mannitol. All drugs decreased tensile strength, increased friability, prolonged disintegration time, and decreased the porosity of tablets. Tablets containing Prosolv® ODT G2 with captopril, domperidone, and tramadol; and Parteck® ODT with domperidone met the requirements for ODTs production, i.e., friability ≤ 1% and disintegration time ≤ 180 s, fast wetting time, high water absorption ratio, and adequate tensile strength. The disintegration time was tested using both the pharmacopeial method and the BJKSN-13 apparatus. The results indicate the significant difference between these methods, with the disintegration time being longer when tested with the BJKSN-13 instrument.

Mucoadhesive Film Forming Spray for Buccal Drug Delivery: A Review

Film-forming sprays provide a number of advantages over conventional topical treatments, including equal medication distribution and dosing, increased bioavailability (increase local drug concentration), and less irritability (Dosing frequency). Polymers and excipients that improve the characteristics of preparations and increase the stability of active substances are the building blocks of mucoadhesive film-forming sprays. Films made from diverse combinations of polymer and excipient exhibited a wide range of characteristics. This reveiw examines the many types of polymers and excipients, the different types of sprayers, the different evaluations, as well as the essential criteria that are involved in defining the sprayability and film properties. This comes to the conclusion that natural and synthetic polymers with viscoelastic properties can both be employed to optimize the administration of buccal drugs.

Investigating Variation in Compressional Behavior of a Ternary Mixture from a Plastic, Elastic and Brittle Fracture Perspective in the Context of Optimum Composition of a Pharmaceutical Blend

The choice of optimum composition of a mixture of binary and ternary excipients for optimum compressional properties was investigated in this work. Excipients were chosen based on three types of excipients: plastic, elastic, and brittle fracture. Mixture compositions were selected based on a one-factor experimental design using the response surface methodology technique. Compressive properties comprising Heckel and Kawakita parameters, work of compression, and tablet hardness were measured as the main responses of this design. The one-factor RSM analysis revealed that there exist specific mass fractions that are associated with optimum responses for binary mixtures. Furthermore, the RSM analysis of the 'mixture' design type for the three components revealed a region of optimal responses around a specific composition. The foregoing had a mass ratio of 80:15:5 for microcrystalline cellulose: starch: magnesium silicate, respectively. Upon comparison using all RSM data, ternary mixtures were found to perform better in compression and tableting properties than binary mixtures. Finally, the finding of an optimal mixture composition has proven effective in its applicability in the context of the dissolution of model drugs (metronidazole and paracetamol).