Dosage Form For Oral Administration Research Articles

Lipid-based oral formulation in capsules to improve the delivery of poorly water-soluble drugs

Poorly water-soluble drugs demonstrate significant challenge in pharmaceutical development, which is linked to their limited oral bioavailability and therapeutic efficacy. To overcome these limitations, lipid-based formulations have emerged as a promising approach to enhance the delivery of such drugs. Moreover, encapsulation within capsules to provide a convenient dosage form for oral administration. The encapsulation techniques are optimized to ensure uniform drug content and efficient encapsulation efficiency. Several investigations demonstrated that the lipid-based formulations in capsules significantly improved the solubility and dissolution rate of poorly water-soluble drugs compared to non-lipid formulations. Additionally, the encapsulation of lipid-based formulations protected the drug against degradation and improved its stability. Overall, incorporating lipid-based formulations in capsules represents a promising strategy for enhancing the delivery of poorly water-soluble drugs with improvement in solubility, dissolution, stability, and bioavailability, overcoming the challenges associated with these challenging drug molecules. The review focussed a brief on utilization of lipids in capsule form to improve therapeutic efficacy of poorly soluble, dissolution and bioavailability of drugs.

3D-printed dosage forms for oral administration: a review.

Oral administration is the most commonly used form of treatment due to its advantages, including high patient compliance, convenient administration, and minimal preparation required. However, the traditional preparation process of oral solid preparation has many defects. Although continuous manufacturing line that combined all the unit operations has been developed and preliminarily applied in the pharmaceutical industry, most of the currently used manufacturing processes are still complicated and discontinuous. As a result, these complex production steps will lead to low production efficiency and high quality control risk of the final product. Additionally, the large-scale production mode is inappropriate for the personalized medicines, which commonly is customized with small amount. Several attractive techniques, such as hot-melt extrusion, fluidized bed pelletizing and spray drying, could effectively shorten the process flow, but still, they have inherent limitations that are challenging to address. As a novel manufacturing technique, 3D printing could greatly reduce or eliminate these disadvantages mentioned above, and could realize a desirable continuous production for small-scale personalized manufacturing. In recent years, due to the participation of 3D printing, the development of printed drugs has progressed by leaps and bounds, especially in the design of oral drug dosage forms. This review attempts to summarize the new development of 3D printing technology in oral preparation and also discusses their advantages and disadvantages as well as potential applications.

Solidification and oral delivery of biologics to the colon- A review

The oral delivery of biologics such as therapeutic proteins, peptides and oligonucleotides for the treatment of colon related diseases has been the focus of increasing attention over the last years. However, the major disadvantage of these macromolecules is their degradation propensity in liquid state which can lead to the undesirable and complete loss of function. Therefore, to increase the stability of the biologic and reduce their degradation propensity, formulation techniques such as solidification can be performed to obtain a stable solid dosage form for oral administration. Due to their fragility, stress exerted on the biologic during solidification has to be reduced with the incorporation of stabilizing excipients into the formulation. This review focuses on the state-of-the-art solidification techniques required to obtain a solid dosage form for the oral delivery of biologics to the colon and the use of suitable excipients for adequate stabilization upon solidification. The solidifying processes discussed within this review are spray drying, freeze drying, bead coating and also other techniques such as spray freeze drying, electro spraying, vacuum- and supercritical fluid drying. Further, the colon as site of absorption in both healthy and diseased state is critically reviewed and possible oral delivery systems for biologics are discussed.

Absolute bioavailability of a substance with cardioprotective activity (ALM-802) in rats

The pharmacokinetics of a new potential cardioprotective agent ALM-802 was studied in rats after single intravenous and intragastric administration at doses of 10 and 100 mg/kg, respectively. The absolute bioavailability was 4.45 %, which indicates the potential for the development of a dosage form for oral administration

REVIEW STUDY ON ANALYSIS OF THE SOLUBILITY OF BIOPHARMACEUTICAL CLASSIFICATION SYSTEM CLASS II DRUGS IN A SELF-EMULSIFYING DRUG DELIVERY SYSTEM

By dissolving drug molecules in these solutions, a unit dosage form for oral administration can be generated for oral administration. Self-emulsifying drug delivery system (SEDDS) is utilized to address the inadequate bioavailability of poorly soluble and highly permeable drugs, according to the literature. These methods can disseminate and deliver hydrophobic medications as a unit dose form for oral administration in this fashion. SEDDS formulations self-emulsify (micro/nano) after being discharged into the intestinal lumen and coming into contact with the gastrointestinal (GI) fluid. Several factors must be considered to make the oral drug administration difficult, including poor water solubility and limited permeability. Self-emulsifying drug delivery can increase the solubility of biopharmaceutical classification system (BCS) II medicines. The SEDDS is a drug delivery system that enhances the solubility of lipophilic medications. It has risen in popularity over time. Under moderate agitation and subsequent dilution, GI fluids are categorized as hydrophilic liquid mixes that are isotropic. This research looks at a variety of uses as well as recent advancements in SEDDS composition, evaluation, dosage forms, and novel techniques to convert liquid SEDDS to solids. Final Thoughts Determining whether or not it is feasible to construct a BCS Category 2 medication formulation based on SEDDS represents a significant contribution of this effort. Medicines with solubility issues and low and variable bioavailability will benefit from the connected technologies.

DEVELOPMENT OF OPTIMAL COMPOSITION FORMULATION OF RESVERATROL AND SOLUBILISERS

Introduction. Increasing of poorly soluble pharmaceutical substances bioavailability is one of important problems of pharmaceutical technology. Resveratrol is a plant origin polyphenol with a broad spectrum of biological effects. However, due to poor solubility and, as a result, low bioavailability, it is not promising for the development of oral drugs. Thus, today resveratrol is presented only as a biologically active substance that is component of biologically active food supplements.The objective of the research is selection of the optimal solubilizer to increase the solubility of resveratrol by determining the solubilization parameters.Materials and methods. The spectrophotometric characteristics of resveratrol were studied using three groups of solubilizers: poloxamers, polysorbates and cyclodextrins. Studies were carried out in 50 mM hydrochloric acid buffer(pH 1.2) and 50 mM phosphate buffer(pH 6.8). Spectrophotometric measurements were carried out on a spectrophotometer UV/VIS-3600 Shimadzu (Japan) in the wavelength range of 220–380 nm. The effect of solubilizers on the spectrophotometric characteristics of resveratrol was determined in buffer solutions containing the solubilizer and resveratrol in significantly less concentration of its own solubility in water. The used multiple excess of the solubilizer ensured the finding of all resveratrol in a solubilized form. During the determining parameters of solubilization, buffer solutions containing from 2 to 10 mM solubilizers were added to the obviously excess of resveratrol. The indicated amount of resveratrol ensured the presence of its precipitate in all experimentsto determine the completeness of solubilization of the studied polyphenol.Results. Based on the obtained spectrophotometric characteristics of solubilizers solutions with resveratrol, the most effective for the further development of solid dosage forms for oral administration are poloxamer 407, polysorbate 80 and modified methyl-beta-cyclodextrin, which ensure complete dissolution of resveratrol when its content in the composition with a solubilizer is about 10 %.Conclusion. Based on the data obtained on the spectrophotometric characteristics of resveratrol using solubilizers, it can be argued that it is possible to create drugs with improved solubility of the studied polyphenol. On the basis of its compositions with poloxamer 407, polysorbate 80 and modified methyl-beta-cyclodextrin, with the selection of appropriate excipients, solid dosage forms for oral intake can be developed.

Совершенствование использования лекарственных средств в организациях здравоохранения для решения проблемы нерационального применения лекарственных средств в Республике Казахстан

The effectiveness of the provided drug therapy remains an urgent problem and is directly proportional to the rational use of drugs. According to WHO, the most common causes of improper use of drugs are polypharmacy, improper use of antibacterial agents, unjustified use of the parenteral route of administration of drugs in cases where it is preferable to use dosage forms for oral administration, non-compliance with clinical guidelines in case of prescribing drugs and inappropriate self-medication. To ensure the rationality of pharmacotherapy, appropriate assessment methods are used. The world standard for assessing the rationality of drug use and the impact on irrational options for their use are indicators for assessing good drug use management practices, which are unified objective and simple parameters for evaluating drug use and the quality of medical care. As a solution to the problems of the irrational use of drugs, policies are proposed to improve the rational use of drugs by introducing an assessment and monitoring of the use of drugs, conducting an information campaign for the population and medical workers with the aim of creating the right behaviors regarding the use of drugs and introducing mandatory continuing education for the rational use of drugs of all medical workers. The existing legislative framework of Kazakhstan, as well as the programs, plans and projects adopted in recent years for the development of the health care system, have all the necessary conditions to support the implementation of the proposed policy options, however, the main barriers to the implementation of policy options may be a lack of human resources, unethical behavior of pharmaceutical companies lobbying their interests in the promotion of drugs, the lack of support from the authorized body in the field of healthcare, and the lack of understanding by healthcare managers of the goal of implementing an assessment of the rational use of drugs.

Pharmacokinetic properties of an innovative nootropic agent based on a derivative of 3,7-diazabicyclo[3.3.1]nonane

The pharmacokinetics and bioavailability of a derivative of 3,7-diazabicyclo[3.3.1]nonane exhibiting a nootropic effect, were studied after a single dose to rats. The pharmacokinetics of the compound was studied after oral and intravenous administration to 270 male rats Sprague Dawley at doses of 2.5 mg/kg, 13 mg/kg and 25 mg/kg. Its distribution in organs and tissues (brain, thymus, heart, lungs, liver, kidneys, and spleen) was also investigated. It was found that after a single intravenous administration, the investigated substance was determined in the blood of animals for 24 h; the half-life was 4.69 h. The relative bioavailability of the 3,7-diazabicyclo[3.3.1]nonane derivative after oral administration was 42.3%, thus suggesting the prospect of creating dosage forms for oral administration. After a single oral administration, the dose dependence of AUC0-t was exponential. The substance is characterized by heterogeneous distribution in the body with preferential accumulation mainly in well-vascularized tissues.

Decoding the small size challenges of mini-tablets for enhanced dose flexibility and micro-dosing.

Mini-tablets are an age appropriate dosage form for oral administration to pediatric and geriatric patients, either as individual mini-tablets or as composite dosage units. Smaller size mini-tablets than the commonly used 2mm or larger size would offer more tailored micro-dose delivery of investigational drugs. This work demonstrated drug substance particle size, drug loading and mini-tablet size ranges to achieve acceptable quality attributes of mini-tablets. A platform formulation with 60, 80, and 100μm (particle size D6,3) ibuprofen at 3, 14, and 25% loadings were directly compressed into 1.2, 1.5, 2, and 2.5mm diameter mini-tablets. With an enhanced weight control approach, all the mini-tablet batches except the 1.2mm diameter mini-tablets with 100µm ibuprofen at 3% loading would achieve acceptable content uniformity as individual mini-tablets (USP <905> L2 criteria) and as composite dosage units of five or more mini-tablets (USP <905> L1 criteria). A dissolution method was developed and successfully utilized to evaluate the formulations herein. Small size mini-tablets, small ibuprofen particle size, and low dose (or low ibuprofen loading) enhanced the dissolution performance. In addition, hypothetical scenarios of potential dose flexibility, dose range, dose titration, and excipient burden were discussed. The results of this study provide guidance for development of smaller size mini-tablets that enable dosing as a single or composite dosage unit, reduce excipient burden and leverage dispensing technology to achieve enhanced dosing flexibility and micro-dosing.

Organoleptic excipients used in pediatric antibiotics

Taste is a crucial factor that determines the palatability of the oral dosage form and patient compliance. ObjectiveThe aim of this work was to evaluate the organoleptic excipients in oral antibiotics for pediatric use marketed in Brazil. MethodsThe information was obtained from the GuidetoPharmacy, a reference for the pharmaceutical trade. The analysis included dosage forms for oral administration and drugs and their combination with antibacterial action. After this survey, we identified the constitution of the flavoring, sweetening, and coloring agents of each medicine. The results are presented in a descriptive form. ResultsTwelve drugs or associations are distributed in 70medicines. Oral suspension was the most common pharmaceutical dosage form. Sweeteners were sucrose, sodium saccharin, and sodium cyclamate. All the coloring agents observed are synthetic and the most frequent ones were yellow twilight no. 6, yellow tartrazine no. 5, and red ponceau 4R. The presence of two or more types of flavorings per medicine was observed. ConclusionAntibacterials use coloring agents, flavorings, and sweeteners to facilitate the administration of medicines for children, using up to six different substances per formulation. No natural coloring agent was observed, demonstrating an issue to be explored in the future. It is important to note that, although necessary, these excipients are responsible for a high incidence of allergic reactions in children.

New Perspective Enteric-Coated Tablet Dosage Form for Oral Administration of Ceftriaxone: In Vitro and In Vivo Assessments

Ceftriaxone (CTX) is a widely used injectable third-generation cephalosporin that exhibits broad-spectrum antibacterial activity. Unfortunately, the oral route of this drug suffers different encumbrances, such as instability in the upper part of the GIT and enzymatic degradation, as well as poor permeability. There is no reported tablet dosage form for this drug. In this respect, the authors investigated the possibility of developing an enteric-coated oral tablet of CTX that would be helpful for better patient compliance. The tablet consists of directly compressed core of CTX, citric acid (CA), sodium chloride (NaCl), and two biopolymers-chitosan (CH), a permeation enhancer, and silicified microcrystalline cellulose (SMCC), a wicking agent. Both biopolymers are naturally occurring polysaccharides that are biodegradable in the colon and able to incorporate acid labile drugs. CA is a pH modulator to protect CTX from protease enzymes, while NaCl is a translocation enhancer that helps drug penetration. The enteric coat of the core was shellac (SH) with plasticizer glycerol tristearate (GTS) and CA that was applied by direct compression (dry coating). The solventless heat curable coat resulted in an enteric-coated tablet that complies with the USP pharmacopeia. The optimized formula was further subjected to in vitro release and stability studies, as well as ingredient compatibility. In vivo oral bioavailability of the enteric-coated tablets in rabbits gave promising results (absolute bioavailability of about 80%). Synergistically, all ingredients together augmented oral bioavailability of CTX. This developed formula could be a perspective delivery system for those drugs intended to be absorbed from the colon such as peptides and peptide-like drugs.

Formulation and Development of Rosuvastatin Fast Dissloving Tablets using Natural Super Disintegrates

Rosuvastatin is in category of the drug class. It is used to treat high cholesterol and to block cardiovascular disease. The main aim of this study is to develop oral dispersible tablets of Rosuvastatin using different types of super disintegrates to enhance the disintegration and dissolution of Rosuvastatin to improve bioavailability of the drug. Many trials were made to prepare a satisfactory rosuvastatin oral dispersible tablet using direct compression and wet granulation method. Formulate tablets were examine with different parameters such as weight variation, hardness, friability, wetting time, in vitro disintegration time, drug content, water absorption ratio and in vitro drug release. Formulas prepared by direct compression showed good flowability, while formulas were prepared by wet granulation showed with very poor flow properties. Numerous super disintegrates were used such as cross carmellose (CCS), sodium starch glycolate (SSG) and cross povidone (CP), then latter found to be the best in term of showing the fastest disintegration time. Among the two-diluents mannitol was found to be the best one in preparing rosuvastatin tablet with fastest disintegration time in mouth. The optimized selected formula (F11) was prepared by using 15% w/w cross povidone, by direct compression resulted that the shortest disintegration time in mouth (11 seconds), superior drug release profile [the time required for 80% of the drug to be released (t80%) and percent drug dissolved in 2 min (D2min) were 6 min. and 56 %respectively]. In addition to that the selected formula had shown acceptable hardness and friability, hence it is selected as the best formula. The overall results showed that cross povidone was the best super disintegrate of showing the shortest disintegration time while mannitol was the best diluent in preparing Rosuvastatin oral dispersible tablet and this suggested the possibility of utilizing the selected best formula (F11) in the preparation of Rosuvastatin oral dispersible tablet as a new dosage form for oral administration.

DISPERSIBLE TABLETS: AN OVERVIEW

DISPERSIBLE TABLETS: AN OVERVIEW Naveen Kumar*, Sonia Pahuja Swami Vivekanand College of Pharmacy, Banur, Punjab, India ABSTRACT The new drug delivery system helps to achieve better patient compliance. Rapid dispersible tablets are one of these. Dispersible Tablets has benefits such as accurate dosing, easy transportability and fabrication, good physical and chemical stability and an ideal alternative for pediatric and geriatric patients. The oral route of drug administration remains the most ideal route because of its various advantages, including ease of ingestion, pain evasion, versatility and, above all, patient compliance. The tablets and capsules are the most common solid dosage forms. On the other hand, many elderly people will have struggles to take the conventional solid dosage forms (tablets and capsules), due to dysphasia. Swallowing complications are also common in children’s because of their underdeveloped mucosal system. Other groups that may have trouble swallowing a solid dosage form are the psychologically ill, the developmentally disabled, and the non-cooperative patients. In certain circumstances, such as motion sickness, the sudden episode of an allergic attack or cough and the lack of water availability, the ingestion of tablets can be difficult. To meet these medicinal requirements, the pharmaceutical scientist has devoted significant effort to the development of a new type of dosage form for oral administration, the fast dispersible/ rapid dispersible tablets, and a tablet that disintegrates and dissolves rapidly in saliva without the requirement of water. Keywords: Dispersible tablets, orodispersible tablets, rapid dispersible tablets Full Text Article

Enhancement of Aqueous Solubility and Dissolution of Celecoxib through Phosphatidylcholine-Based Dispersion Systems Solidified with Adsorbent Carriers.

This study aimed to design phosphatidylcholine (PC)-based solid dispersion (SD) systems for enhancing the apparent aqueous solubility and dissolution of celecoxib (CLC), a selective cyclooxygenase-2 inhibitor with a highly hydrophobic property. Although PC-based dispersion formulations considerably increased solubilities of CLC, the lipidic texture of PC was not appropriate as a solid dosage form for oral administration of CLC. To mask the lipidic texture of PC-based matrices, Neusilin® US2, an adsorbent material with a porous structure and large surface area widely used in the pharmaceutical industry, was employed and thereby fully powderized PC-based dispersion formulations could be fabricated. However, PC matrices containing CLC strongly adsorbed to the pores of Neusilin® US2 was not able to be rapidly released. To address this problem, different hydrophilic materials were examined to promote the release of the CLC-dispersed PC matrices from Neusilin® US2. Among tested hydrophilic materials, croscarmellose sodium was the most suitable to facilitate fast drug dissolution from Neusilin® US2 particles, showing significantly enhanced apparent aqueous solubility and dissolution behavior of CLC. Through differential scanning calorimetry, X-ray diffraction, and Fourier transform infrared spectroscopy (FT-IR) analysis, a considerably reduced crystallinity of CLC dispersed in the PC-based dispersion formulations was demonstrated. The PC-based SD formulations developed in this study would be useful for improving the oral bioavailability of poorly soluble drugs such as CLC.

Improved Biopharmaceutical Properties of Oral Formulations of 1,2,4-Thiadiazole Derivative with Cyclodextrins: in Vitro and in Vivo Evaluation.

The synthesized 1,2,4-thiadiazole derivative displaying biological activity has low aqueous solubility and dissolution rate. Novel oral formulations of thiadiazole with β- and hydroxypropyl-β-cyclodextrins were obtained by grinding and freeze-drying methods with the purpose to improve the aqueous solubility. Complex formation of 1,2,4-thiadiazole derivative with cyclodextrins was confirmed by means of solid-state 13C MAS CP/TOSS NMR. Solubility, dissolution rate and permeability of the solid inclusion complexes were evaluated in different biorelevant media (SGF, FaSSGF, FaSSIF) simulating the conditions in the gastrointestinal tract. It was demonstrated that the content of biorelevant media affects the properties of the inclusion complexes. In particular, solubilizing effect of cyclodextrins became less pronounced when the micelles of taurocholic acid and lecithin are formed in the dissolution media. The inclusion of thiadiazole into cyclodextrin cavity is in competition with its partitioning into the micelles and this should be taken into account when the in vivo behavior is predicted. The results of in vitro and in vivo experiments were found to be in agreement and showed the highest solubility, dissolution rate and bioavailability of the freeze-dried complexes of thiadiazole with hydroxypropyl-β-cyclodextrin. These complexes can be proposed as more effective dosage forms for oral administration.

Experimental study of tensile strength of pharmaceutical tablets: effect of the diluent nature and compression pressure

In the pharmaceutical field, tablets are the most common dosage form for oral administration in the world. Among different manufacturing processes, direct compression is widely used because of its economics interest and it is a process which avoids the steps of wet granulation and drying processes. Tablets are composed of at least two ingredients: an active pharmaceutical ingredient (API) which is mixed with a diluent. The nature of the powders and the processing conditions are crucial for the properties of the blend and, consequently, strongly influence the mechanical characteristics of tablets. Moreover, tablets have to present a suitable mechanical strength to avoid crumbling or breaking when handling, while ensuring an appropriate disintegration after administration. Accordingly, this mechanical property is an essential parameter to consider. Experimental results showed that proportion of the diluent, fragmentary (DCPA) or plastic (MCC), had a large influence on the tensile strength evolution with API content as well as the compression load applied during tableting process. From these results a model was developed in order to predict the tensile strength of binary tablets by knowing the compression pressure. The validity of this model was demonstrated for the two studied systems and a comparison was made with two existing models.

DESIGN ZOLMITRIPTAN LIQUISOLID ORODISPERSIBLE TABLETS AND THEIR IN VITRO EVALUATION

&lt;p&gt;&lt;strong&gt;Objective: &lt;/strong&gt;The objective of present study is to develop orodispersible tablets (ODTs) of zolmitriptan by liquisolid technique using different types of super disintegrants to enhance the disintegration and dissolution of zolmitriptan to improve the bioavailability of the drug.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;Liquisolid ODTs of zolmitriptan were prepared from; microcrystalline cellulose (Avicel PH-102) as carrier, colloidal silicon dioxide (Aerosil 200) as a coating material, croscarmellose sodium (CSS), sodium starch glycolate (SSG), and crospovidone (CP) as super disintegrants, and propylene glycol as liquid vehicle. The ratio of carrier to coating material was kept constant in all formulations at 35:1, this ratio was chosen after testing the ratios 10:1, 15:1, 20:1, 25:1,30:1, and 35:1. The ratio 35:1 give optimal results relative to other ratios. The pre-compression evaluation includes: flow properties were measured using the angle of repose and the compressibility index and FT-IR. The prepared liquid-solid system compacts were evaluated for their post-compression evaluation which includes: hardness, friability, wetting time, &lt;em&gt;in vitro&lt;/em&gt; disintegration time, drug content and &lt;em&gt;in vitro&lt;/em&gt; drug release.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;The tabletting properties of the liquid-solid ODTs were within the acceptable limits. Among the three super disintegrants, CP found to be the best in term of showing the fastest disintegration time. The optimized selected formula (F11) was prepared using 5% w/w crospovidone, by direct compression showed the shortest disintegration time (24 s), superior drug release profile [ the time required for 80% of the drug to be released (T&lt;sub&gt;80&lt;/sub&gt;%) and percent drug dissolved in 2 min (D&lt;sub&gt;2 &lt;/sub&gt;min) 1.84 min and 87.59%, respectively]. In addition to that, the selected formula had an acceptable hardness and friability, so it was selected as the best formula.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion: &lt;/strong&gt;The overall results showed that CP was the best super disintegrant of showing the shortest disintegration time while loading factor of 0.125 was the best in the preparing of zolmitriptan liquid-solid ODTs, and this suggested the possibility of utilizing the selected best formula (F11) in the preparation of zolmitriptan ODTs as a new dosage form for oral administration. &lt;/p&gt;

Can lipid nanoparticles improve intestinal absorption?

Lipid nanoparticles and their multiple designs have been considered appealing nanocarrier systems. Bringing the benefits of these nanosystems together with conventional coating technology clearly results in product differentiation.This work aimed at developing an innovative solid dosage form for oral administration based on tableting nanostructured lipid carriers (NLC), coated with conventional polymer agents. NLC dispersions co-encapsulating olanzapine and simvastatin (Combo-NLC) were produced by high pressure homogenization, and evaluated in terms of scalability, drying procedure, tableting and performance from in vitro release, cytotoxicity and intestinal permeability stand points.Factorial design indicated that the scaling-up of the NLC production is clearly feasible. Spray-drying was the method selected to obtain dry particles, not only because it consists of a single step procedure, but also because it facilitates the coating process of NLC with different polymers. Modified NLC formulations with the polymers allowed obtaining distinct release mechanisms, comprising immediate, delayed and prolonged release. Sureteric:Combo-NLC provided a low cytotoxicity profile, along with a ca. 12-fold OL/3-fold SV higher intestinal permeability, compared to those obtained with commercial tablets. Such findings can be ascribed to drug protection and control over release promoted by NLC, supporting them as a versatile platform able to be modified according to the intended needs.

Predictive model for tensile strength of pharmaceutical tablets based on local hardness measurements

In the pharmaceutical field, tablets are the most common dosage forms for oral administration. During the manufacture of tablets, measures are taken to assure that they possess a suitable mechanical strength to avoid crumbling or breaking when handling while ensuring disintegration after administration. Accordingly, the tensile strength is an essential parameter to consider. In the present study, microscopic hardness and macroscopic tensile strength of binary tablets made from microcrystalline cellulose and caffeine in various proportions were measured. A relationship between these two mechanical properties was found for binary mixture. The proposed model was based on two physical measurements easily reachable: hardness and tablet density. Constants were determined from the two extreme compositions of this given system. This model was validated with experimental results, and a comparison was made with the one developed by Wu et al. (2005). Both models are relevant for this studied system. Nonetheless, with this model, the tablet tensile strength can be connected with a tablet characteristic at microscopic scale in which porosity is not needed.

FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF ROSUVASTATIN: RESEARCH ARTICLE

The objective of the present study was to formulate and evaluate fast dissolving tablets of Rosuvastatin (BCS Class II drug) to enhance solubility, improve bioavailability and patient compliance especially for the paediatric and geriatric patients with sufficient therapeutic benefits. Rosuvastatin exhibits poor solubility in water and low bioavailability of approximately 20%. Four solid dispersions (1:1, 1:2, 1:4 and 1:6 w/w) were prepared by melting method using PEG 4000 as a polymer. Solid dispersions were characterized for drug content uniformity, XRD, DSC and in vitro dissolution studies.  It was then further compressed into tablets by direct compression method using different superdisintegrants like sodium starch glycolate, crospovidone and croscarmellose sodium. All the fast dissolving tablets were evaluated for pre compression parameters such as angle of repose (θ), bulk and tapped density, percentage compressibility (%) and Hausner ratio. Post compression parameters like general appearance, uniformity of weight, tablet hardness, thickness, friability, estimation of drug content, in vitro disintegration time, wetting time, in vitro dispersion time and water absorption ratio were evaluated. Among the solid dispersions prepared and based on the dissolution studies performed, SD4 formulation having 1:6 ratio was selected for the preparation of fast dissolving tablets. Crospovidone as superdisintegrant was found to be ideal for rapid dispersion and for improving dissolution rate, which in turn increased the bioavailability. The drug release of tablet formulations in the presence of various superdisintegrants was in the order of crospovidone &gt; croscarmellose sodium &gt; sodium starch glycolate. This study indicated the possibility of utilizing the selected best formulation F6 in the preparation of Rosuvastatin fast dissolving tablet as a new dosage form for oral administration having increased solubility, improved bioavailability, rapid dissolution and more patient compliance. Keywords: Rosuvastatin, solid dispersion, PEG 4000, Fast dissolving tablets, crospovidone, superdisintegrants