Top PDF “PREPARATION OF SOLID DISPERSION OF POORLY WATER SOLUBLE DRUG FORMULATION AND CONSIDERATION”

“PREPARATION OF SOLID DISPERSION OF POORLY WATER SOLUBLE DRUG FORMULATION AND CONSIDERATION”

“PREPARATION OF SOLID DISPERSION OF POORLY WATER SOLUBLE DRUG FORMULATION AND CONSIDERATION”

This article investigates enhancement of the dissolution profile of furosemide using solid dispersion (SD) with eudragit(RLPO & RSPO) & also control it’s by using solvent evaporation technique. 1: 0.5(w/w) 1:1(w/w) ,1:1.5 solid dispersions were prepared by solvent evaporation technique using solvent water and methanol in 1:1 ratio. Dissolution studies using the USP paddle method were performed for solid dispersions of furosemide at 37 ± 0.5 C and 55 rpm in simulated gastric fluid (SGF) of pH 1.2. Fourier transformer infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and x-ray diffractometry (XRD) were performed to identify the physicochemical interaction between drug and carrier, hence its effect on dissolution. Tablets were formulated containing solid dispersion products and compared with pure drug . IR spectroscopy, XRD, and DSC showed change in the crystal structure towards amorphous one of furosemide (FRMD). Dissolution of furosemide improved and release is controlled significantly in solid dispersion with the ratio 1:1.5 of eudragit RLPO & RSPO . Tablets containing solid dispersion exhibited better dissolution profile than pure drug. Thus, the solid dispersion technique can be successfully used for improvement of dissolution of furosemide as well as control it’s release.
Mostrar mais

7 Ler mais

Studies on Dissolution Enhancement of Prednisolone, a Poorly Water-Soluble Drug by Solid Dispersion Technique

Studies on Dissolution Enhancement of Prednisolone, a Poorly Water-Soluble Drug by Solid Dispersion Technique

some representative peak heights in diffraction patterns of the solid dispersions with those of physical mixtures. Our findings revealed that prednisolone was in its crystalline forms in the physical mixtures and solid dispersions prepared with lactose without any change compared to the corresponding treated physical mixtures and physical mixtures of the drug. On the contrary solid dispersions prepared with dextrin were characterized by the complete absence of any diffraction peaks, suggesting a complete amorphization in the amorphous carrier. In the case of solid dispersions prepared with PEG 6000, prednisolone was still detectable in crystalline form. Therefore no complete amorphization occurred.
Mostrar mais

6 Ler mais

FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF CYCLODEXTRIN INCLUSION COMPLEXED WATER INSOLUBLE DRUG: GLIMIPIRIDE

FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF CYCLODEXTRIN INCLUSION COMPLEXED WATER INSOLUBLE DRUG: GLIMIPIRIDE

Drug release is a crucial and limiting step for oral drug bioavailability, particularly for drugs with low gastrointestinal solubility and high permeability. By improving the drug release profile of these drugs, it is possible to enhance their bioavailability and reduce their side effects. Solid dispersions are one of the most successful strategies to improve the drug release of poorly soluble drugs 1 . Presenting the compound as the molecular dispersion combining the benefits of a local increase in the solubility (within the solid solution) and maximizing the surface area of the compound that comes in contact with the dissolution medium as the carrier dissolves 2 . The large surface area of the resulting suspension should result in an enhanced dissolution rate and thereby improved bioavailability 3 . The advantage of solid dispersions over other approaches is that many of the carriers that can be applied are already extensively used in the pharmaceutical industry as excipients, so additional toxicity studies above and beyond what is required for the drug itself should not be required. The possibility of combining several carriers to produce an optimized product further extends the range of possibilities for formulation 4 .
Mostrar mais

6 Ler mais

Evaluation of the parameters of a bead milling process to produce a non-aqueous nanosuspension

Evaluation of the parameters of a bead milling process to produce a non-aqueous nanosuspension

The increasing number of poorly soluble drugs requires innovative formulation approaches to reach drugs high bioavailability. There are many conventional methods for increasing the solubility of poorly soluble drugs, which include micronisation, solubilisation using co‐solvents, salt form, surfactant dispersion and lipophilic solution (1). Other techniques like liposomes (2), emulsions (3), microemulsions (1), solid dispersions (4) and cyclodextrins (5) show sensible achiever, but they lack universal applicability to all drugs (6). All these approaches are mostly limited by the physicochemical properties of the drug, such as solubility in oil, the need for a certain molecular size to fit into the cyclodextrin ring or the toxicity associated with some organic solvents. Micronisation of drug powders to sizes between 1 and 10 µm to increase the drug surface area, and thus improve overall dissolution profile, is used for Biopharmaceutical Classification System (BCS) class II drugs, i.e. drugs having a good permeability and poor solubility. Nowadays, many of the new drugs exhibit such a low solubility that micronisation does not lead to a sufficiently high bioavailability (7). Consequently, the next step was to move from micronisation to nanonisation, producing drug nanocrystals, which are nanoparticles (NP) being composed of 100% drug without any matrix material (7).
Mostrar mais

56 Ler mais

Preparation and physicochemical characterization of meloxicam orally fast disintegration tablet using its solid dispersion

Preparation and physicochemical characterization of meloxicam orally fast disintegration tablet using its solid dispersion

Figure 5 represents the dissolution profiles of the prepared MLX ODTs. According to the United States Pharmacopeia (USP), an MLX tablet should release 70 percent of its drug content after 30 min. F4 and F8 showed the highest percentage of MLX release after 30 min; 80.4±1.6 and 82.66±5.1 respectively. This high amount of release could be due to the high amount of water-soluble mannitol and low amount of low water- soluble avicel in their formulations. The use of a high amount of mannitol in tablet formulation could help the dissolution of poorly water-soluble drugs (Myers, Battist, Fuisz, 1995). Moreover, F4 and F8 released about 50% of their drug content only after 2 min. This burst release of MLX might be due to the effect of water-soluble mannitol, which could increase the degree of cracking and bursting (Shirai et al., 1994). An ANOVA analysis showed only one factor, namely, mannitol–avicel ratio (p < 0.0001) had a significant effect on the percentage of dissolved MLX (after 30 min) from the prepared MLX ODTs (Figure 6). The results also showed that the percentage of MLX dissolved after 30 min increased as the mannitol–avicel ratio become greater. The compression force and percentage of super disintegrant did not show any significant effects on the percent of MLX released after 30 min. The resulting equation for responses, Y3 (percent of MLX that dissolved after 30 min), is presented below:
Mostrar mais

9 Ler mais

Braz. J. Pharm. Sci.  vol.52 número1

Braz. J. Pharm. Sci. vol.52 número1

The solid dispersion technique has been used for a wide variety of poorly water-soluble drugs such as irbesartan (Adeli, 2015), nimesulide (Babu et al., 2003) and ursodeoxycholic acid (Okonogi et al., 1997). One major problem associated with azithromycin is its very poor solubility (belongs to BCS class II) in biological luids which accounts for the poor bioavailability, upon its oral administration. In this study, the solid dispersion method was utilized in order to increase the dissolution rate and solubility of azithromycin. Although there have been previous studies on this technology for over half-a-century, its application in drug development has attained greater importance since early 1990s owing to the widespread application of combinatorial chemistry and high-throughput screening in drug discovery, which favors the selection of poorly water-soluble new chemical entities (NCEs) (Vasanthavada et al., 2008; Pudipeddi et al., 2006).
Mostrar mais

14 Ler mais

Braz. J. Pharm. Sci.  vol.49 número3

Braz. J. Pharm. Sci. vol.49 número3

The objective of the present work was to enhance the solubility and dissolution rate of the drug raloxifene HCl (RLX), which is poorly soluble in water. The solubility of RLX was observed to increase with increasing concentration of hydroxypropyl methylcellulose (HPMC E5 LV). The optimized ratio for preparing a solid dispersion (SD) of RLX with HPMC E5 LV using the microwave-induced fusion method was 1:5 w/w. Microwave energy was used to prepare SDs. HPMC E5 LV was used as a hydrophilic carrier to enhance the solubility and dissolution rate of RLX. After microwave treatment, the drug and hydrophilic polymer are fused together, and the drug is converted from the crystalline form into an amorphous form. This was conirmed through scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) studies. These results suggested that the microwave method is a simple and eficient method of preparing SDs. The solubility and dissolution rate of the SDs were increased signiicantly compared with pure RLX due to the surfactant and wetting properties of HPMC E5 LV and the formation of molecular dispersions of the drug in HPMC E5 LV. It was concluded that the solubility and dissolution rate of RLX are increased signiicantly when an SD of the drug is prepared using the microwave-induced fusion method.
Mostrar mais

8 Ler mais

FORMULATION AND EVALUATION OF SOLID LIPID NANOPARTICLES OF  A POORLY WATER SOLUBLE MODEL DRUG, IBUPROFEN

FORMULATION AND EVALUATION OF SOLID LIPID NANOPARTICLES OF A POORLY WATER SOLUBLE MODEL DRUG, IBUPROFEN

Oral ingestion is the most convenient and commonly employed route of drug delivery due to its ease of administration, high patient compliance, cost-effectiveness, least sterility constraints and flexibility in the design of dosage form. As a result, many of the generic drug companies are inclined more to produce bioequivalent oral drug products. The high costs and time involved in new drug development, expiry of patents for a significant number of drug molecules, ease of manufacturing and ready availability of technology for the production of oral drug products are also driving the generic pharmaceutical companies towards the development of bioequivalent oral dosage forms. However, the major challenge with the design of oral dosage forms lies with their poor bioavailability. The oral bioavailability depends on several factors including aqueous solubility, drug permeability, dissolution rate, first-pass metabolism, pre-systemic metabolism and susceptibility to efflux mechanisms 1, 2, 3 . The most frequent causes of low oral bioavailability are attributed to poor solubility and low permeability 4 . In recent years it has become more and more evident that the development of new drugs alone was not sufficient to ensure progress in drug therapy. Exciting experimental data obtained in vitro were very often followed by disappointing results in vivo because of the insufficient drug concentration due to poor absorption, rapid metabolism and elimination, poor water solubility and high fluctuation of plasma levels due to unpredictable bioavailability after per oral administration. A promising strategy to overcome these problems involves the development of suitable drug carrier systems 5 . The size of the carrier depends on the desired route
Mostrar mais

6 Ler mais

The Impact of E-Commerce Securi ty, and National Environment  on Consumer adoption of Intern et Banking in Malaysia and  Singapore

The Impact of E-Commerce Securi ty, and National Environment on Consumer adoption of Intern et Banking in Malaysia and Singapore

The research model is designed to examine the impact of customers’ perception of e- commerce security, and national environmental factors on their acceptance of Internet banking in Malaysia and Singapore. Several models have been used to explain factors determining consumer acceptance of Internet banking (Straub et. al., 1997; Liao et. al., 1999; Sathye, 1999; Tan & Teo, 2000; Pavlou, 2003; Suh & Han, 2003; Brown et. al., 2003; Venkatesh et. al., 2003). For example: technology acceptance model (TAM) devices by Davis (1986) was used by Suh and Han (2003). According to Suh and Han (2003), one of the most widely used models for explaining the factors that affects user acceptance of information systems or information technology is TAM. Another model is Fishbein and Ajzen’s (1989) theory of reasoned action (TRA), which is based on Davis’s (1986) technology acceptance model (TAM). TRA model asserts that attitude towards a behavior is determined by relevant beliefs (Davis et. al., 1989). Other theories are the theory of planned behavior (TPB), the decomposed theory of planned behavior (DTPB) by Taylor and Todd (1995) and the diffusion of innovation theory, Rogers (1983). The decomposed TPB model, according to Tan and Teo (2000), uses constructs from the innovation literature such as relative advantage, compatibility, subjective norms, and perceived behavioral control by decomposing them into more specific dimensions. While, Venkatesh et. al.’s (2003) unified theory of acceptance and use of technology (UTAUT) on the other hand posits four core determinants (performance expectancy, effort expectancy, social influence and facilitating condition) and four moderators (gender, age, experience and voluntariness of use) of the key relationships of intention and usage of information technology.
Mostrar mais

20 Ler mais

The modification process of AlSi21CuNi silumin and its effect on change of mechanical properties of the alloy

The modification process of AlSi21CuNi silumin and its effect on change of mechanical properties of the alloy

Phosphorus, which can be introduced to metal bath in free form, as a master alloy or a salt, belong to well-known modifiers of hypereutectic silumins. It has been confirmed [2] that in such case the aluminum phosphide, AlP, becomes the nucleus of the crystallization. In the studies [11-12] is presented a new view on interaction of phosphorus in process of modification of hypereutectic silumins, which is an effect of local overcooling in micro-areas caused by evaporation and expansion of bubbles of phosphorus vapours. Indispensable quantity of phosphorus in the alloy was determined as interval of 0,01 ÷ 0,05 % [1-3].
Mostrar mais

4 Ler mais

Synthesis, characterization and thermal behaviour of solid state compounds of 2-chlorobenzylidenepyruvate with trivalent aluminium, gallium, indium and scandium metals

Synthesis, characterization and thermal behaviour of solid state compounds of 2-chlorobenzylidenepyruvate with trivalent aluminium, gallium, indium and scandium metals

lium nitrates were prepared from the scandium oxide and metallic gallium by treatment with con- centrated nitric acid. The resulting solutions were transferred to a volumetric flask, and their pH values were adjusted to 5 and 3, respectively, by the use of a solution of diluted nitric acid solution. Aqueous solutions of aluminium and gallium nitrates were prepared from the dissolu- tion of the solid salts in water following by the adjustment of the pH value by using a solution of the diluted nitric acid adjusted to 3. The solid- state compounds were prepared by mixing with continuous stirring, the solution of the ligand with the respective metal nitrate solution until total precipitation of the metallic (III) pyruvates. The precipitates were washed with distilled wa- ter until elimination of the nitrate ions filtered through and dried on Whatman nº 42 filter pa- per, and kept in a desiccator over anhydrous calcium chloride.
Mostrar mais

6 Ler mais

An Analysis of Student Evaluations of Native and Non Native Korean Foreign Language Teachers

An Analysis of Student Evaluations of Native and Non Native Korean Foreign Language Teachers

The most common type of complaint from students was un- questionably related to excessive lecturing on the part of the native TA (about 70% of negative comments related to excessive lecturing, not enough time to talk.) Students often felt shorthanded when not given opportunities to discuss topics in class. (Although this contra- dicts the statements above related to difficult discussion topics, we should assume that students who requested more discussion in class are expecting discussion at an appropriate language level.) One stu- dent said of a native male TA, “I think if there were more opportuni- ties to speak instead of hearing him speak for most of the class, it would have been more beneficial.” Another complained about a na- tive female TA, “She was very enthusiastic about teaching, but activi- ties that actually involved speaking were sparse.” More than anything else, students mentioned discussion in the classroom, and the majori- ty of these complaints and requests were aimed towards native female TAs: “I did not like how little we got to speak as a class. My under- standing increased but I feel my speaking skills went down”; “More class participation would have been good”; “I wish we would have had more opportunities to have class debates and class discussions”; “mostly a lecture [with] little interaction”; “I think the only thing that could be improved is if she would have us speak more in class.” Fi- nally, one student wrote an extensive comment for a female TA that depicted her as an outstanding TA, but then ended with the sugges- tion that “more emphasis on free class discussion might help.”
Mostrar mais

20 Ler mais

Synthesis of nanoparticeles in ductile iron with small additions of vanadium and niobium and its mechanical properties

Synthesis of nanoparticeles in ductile iron with small additions of vanadium and niobium and its mechanical properties

were pig iron, steel scrap, Fe-75%Si, Fe-80%V and Fe-80%Nb and Fe-80%Mn-8%N. The metal was preheated at 1500 o C and then poured into sand mould to get normalized Y-shaped castings. Spheroidizing and inoculation process was made in gating system using Fe-Si-5%Mg alloy, and Foundrysil inoculant containing 0,5 % Ce in amounts 1,0 % and 0,8 % with relation to bath weight, respectively. One of the purpose of our research is to develop a method of nanoparticles synthesis in ferritic matrix of ductile cast iron, which are supposed to increase its strength without affecting notably its ductility.
Mostrar mais

8 Ler mais

Effect Of Shape And Plan Configuration On Seismic Response Of Structure

Effect Of Shape And Plan Configuration On Seismic Response Of Structure

frequency of the structure, and its intended use, this method was refined to enable increasingly adequate designs [4]. Buildings have longer periods of vibration and periods of vibration, composed largely of orthogonal, closely spaced modes. Hence, Equivalent static analysis method was adopted in order to design buildings and overcome effect of earthquake on it. In this study I have performed static analysis as per IS 1893-2002. To study the effect of irregular plan and shape configuration I have developed 9 models in STAAD Pro V8i software. Various types of input data to model the all the 9 models were kept same to obtain the predicted behaviour. Various types of data adopted for creating the models are as under,
Mostrar mais

5 Ler mais

Braz. J. Pharm. Sci.  vol.49 número3

Braz. J. Pharm. Sci. vol.49 número3

The powder flow evaluation is one of the most important parameters in the development of a solid dosage form, because commercial production requires a continuous low of powder mixes during the manufacturing process (Yang, Venkateshi, Fassihi, 1996). Because of the narrow diameter of the compression die used to obtain minitablets (3 mm), granules with excellent flow properties are required (Brabander et al., 2000). According to the literature, excellent low properties are seen for powders with an angle of repose between 25° and 30°, compressibility index below 10% and Hausner ratio below 1.11 (USP 31, 2008). All the formulations under evaluation had an angle of repose between 26° and 29°, compressibility index less than 6% and Hausner ratio below 1.05. Their excellent flow properties were also proved by the narrow weight distribution of the minitablets and their low friability, since all formulations had coeficient of variation values less than 5% relative to their mean weight and friability less than 1%. These results demonstrated the suitability of all formulation mixtures used to produce minitablets.
Mostrar mais

8 Ler mais

Influence of vibrations during crystallization on mechanical properties and porosity of AlSi13Cu2 alloy

Influence of vibrations during crystallization on mechanical properties and porosity of AlSi13Cu2 alloy

Test bed to investigation of porosity of the alloy consisted of the NEOPHOT 32 metallographic microscope equipped with high resolution camera connected to computerized system of image analysis. Next, with use of the MULTISCAN program there were performed photos of the investigated specimens (Fig. 5). Successive stage consisted on generation, with use of the image analyzer system, an image of specimens’ photos showing areas of porosity and contraction cavities only, on base of which the software could calculate surface area of the porosities and contraction cavities.
Mostrar mais

4 Ler mais

FORMULATION AND CHARACTERIZATION OF SOLID LIPID NANOPARTICLES FOR TRANSDERMAL DELIVERY OF TESTOSTERONE

FORMULATION AND CHARACTERIZATION OF SOLID LIPID NANOPARTICLES FOR TRANSDERMAL DELIVERY OF TESTOSTERONE

Viscosity of testosterone containing solid lipid nanoparticles was measured by Brookfield viscometer (DV-E viscometer, Brookfield, USA) using spindle no 63 at 30 r/m in ambient condition [29] . The averages of three determinations were given in Table no. 2. Viscosity of testosterone containing solid lipid nanoparticles was found from 2850 to 3390 cp. Handling and spreading point of view it may be consider an acceptable viscosity. The in vitro release study of solid lipid nanoparticles was performed by locally fabricated Franz diffusion type cell. The study was performed at 30±2°C temperature. Receptor compartment of diffusion cell contained 30 ml 30% v/v PEG 400 in phosphate buffer (pH-6) as diffusion medium [32] . Dialysis membrane (molecular weight cut off 12 KD, HiMedia Laboratories Pvt. Ltd., India) was employed as release barrier in between receptor and donor compartment. The study was performed for 8 hour and samples were withdrawn in one hour interval. The collected samples were suitably diluted and analyzed by HPLC (Shimadzu, Japan) at 254 nm [30] . In vitro release pattern of formulation F1 to F4 was found from 36.49 to 48.63 cumulative percentage drug releases in 8 h Figure 2. Formulation F3 found to have lowest release and formulation F1 found relatively faster release. However, all the formulation showed controlled release patter which could enough for 24 h to get controlled release once a day formulation.
Mostrar mais

6 Ler mais

	Renal Metastasis of a Malignant Myopericytoma: A Case Report and Review of Literature

Renal Metastasis of a Malignant Myopericytoma: A Case Report and Review of Literature

In July 2015, the patient was referred to the department of internal medicine by her family doctor with weight loss of 8 kg, persistent fatigue, and pain in the right hypochondriac region. There were no urinary symptoms. Clinical examination revealed tenderness in the right hypochondriac region, and ultrasonography showed a mass on the upper pole of the right kidney. A computed tomography (CT) scan of the abdomen revealed a voluminous tumour of 8.2 cm in the upper pole of the right kidney. The tumour showed irregular contrast captation and was assessed as a malignant solid renal tumour, presumably renal cell carcinoma. No pathologically enlarged retroperitoneal nodes were seen (Figure 1A and 1B). A CT image of the thorax showed no abnormalities. A radical right nephrectomy was performed with an uncomplicated postoperative course.
Mostrar mais

6 Ler mais

J. Braz. Chem. Soc.  vol.28 número1

J. Braz. Chem. Soc. vol.28 número1

normally indicates a possible destabilization of the crystal lattice of the compound. This phenomenon indicates an improvement in the drug solubility due to the crystalline conformation being changed to an “arrangement” of lower energy. Furthermore, the degradation temperature of the complex, presented in Table 2, shows that the complexation confers stability to 6CN10, since with the complex formation the initial degradation temperature was displaced from 286 to 321 ºC. In the physical mixture a physical delay of the initial degradation temperature is also shown, although less effective when compared to the inclusion complex.
Mostrar mais

10 Ler mais

The Impact of the Expansion of the Bolsa Familia Program on the Time Allocation of Youths And Their Parents Lia Chitolina Miguel Nathan Foguel Naercio Menezes-Filho

The Impact of the Expansion of the Bolsa Familia Program on the Time Allocation of Youths And Their Parents Lia Chitolina Miguel Nathan Foguel Naercio Menezes-Filho

As the multinomial model is non-linear, the marginal effect of the treatment in a DID model is not the marginal impact of the interaction between time and treatment, but the difference of the cross-differences, as described by Puhani (2012). The results of Table 7 (in terms of marginal effects) show that the BVJ has a significant effect on the probability studying and working at the same time, but not on the other outcome variables. The estimated marginal effects mean that the probability of a youngster studying and working increases by 4.2 percentage points with the BVJ, compared with a baseline of 30% in the control group in 2006. The estimated coefficients for the categories ‘studying only’ and ‘working only’ were negative but not statistically significant. It seems, therefore, that treated adolescents do not quit their jobs to study because of the program, but do both activities at the same time. This raises questions about the long run impacts of the program, since the quality of the night classes is notoriously low in Brazil.
Mostrar mais

39 Ler mais

Show all 10000 documents...

temas relacionados