Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 19 de 19
Filtrar
Mais filtros










Intervalo de ano de publicação
1.
ACS Appl Mater Interfaces ; 14(36): 40698-40710, 2022 Sep 14.
Artigo em Inglês | MEDLINE | ID: mdl-36054111

RESUMO

Preventing crystallization is a primary concern when developing amorphous drug formulations. Recently, atomic layer coatings (ALCs) of aluminum oxide demonstrated crystallization inhibition of high drug loading amorphous solid dispersions (ASDs) for over 2 years. The goal of the current study was to probe the breadth and mechanisms of this exciting finding through multiple drug/polymer model systems, as well as particle and coating attributes. The model ASD systems selected provide for a range of hygroscopicity and chemical functional groups, which may contribute to the crystallization inhibition effect of the ALC coatings. Atomic layer coating was performed to apply a 5-25 nm layer of aluminum oxide or zinc oxide onto ASD particles, which imparted enhanced micromeritic properties, namely, reduced agglomeration and improved powder flowability. ASD particles were stored at 40 °C and a selected relative humidity level between 31 and 75%. Crystallization was monitored by X-ray powder diffraction and scanning electron microscopy (SEM) up to 48 weeks. Crystallization was observable by SEM within 1-2 weeks for all uncoated samples. After ALC, crystallization was effectively delayed or completely inhibited in some systems up to 48 weeks. The delay achieved was demonstrated regardless of polymer hygroscopicity, presence or absence of hydroxyl functional groups in drugs and/or polymers, particle size, or coating properties. The crystallization inhibition effect is attributed primarily to decreased surface molecular mobility. ALC has the potential to be a scalable strategy to enhance the physical stability of ASD systems to enable high drug loading and enhanced robustness to temperature or relative humidity excursions.


Assuntos
Óxido de Alumínio , Polímeros , Cristalização , Estabilidade de Medicamentos , Polímeros/química , Pós/química , Solubilidade
2.
PeerJ ; 10: e13482, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35642201

RESUMO

The objective of the present study was to improve the dissolution rate and aphrodisiac activity of tadalafil by using hydrophilic polymers. Solid dispersions were prepared by solvent evaporation-Rota evaporator using Koliphore 188, Kollidon® VA64, and Kollidon® 30 polymers in a 1:1 ratio. Prepared tadalafil-solid dispersions (SDs) evaluated for yield, drug content, micromeritics properties, physicochemical characterizations, and aphrodisiac activity assessment. The optimized SDs TK188 showed size (2.175 ± 0.24 µm), percentage of content (98.89 ± 1.23%), yield (87.27 ± 3.13%), bulk density (0.496 ± 0.005 g/cm3), true density (0.646 ± 0.003 g/cm3), Carr's index (23.25 ± 0.81), Hausner ratio (1.303 ± 0.003) and angle of repose (<25°). FTIR spectrums revealed tadalafil doesn't chemically interact with used polymers. XRD and DSC analysis represents TK188 SDs were in the amorphous state. Drug release was 97.17 ± 2.43% for TK188, whereas it was 32.76 ± 2.65% for pure drug at the end of 2 h with 2.96-fold increase in dissolution and followed release kinetics of Korsmeyer Peppa's model. MDT and DE were noted to be 17.48 minutes and 84.53%, respectively. Furthermore, TK188 SDs showed relative improvement in the sexual behavior of the male rats. Thus the developed SDs TK188 could be potential tadalafil carriers for the treatment of erectile dysfunction.


Assuntos
Afrodisíacos , Disfunção Erétil , Ratos , Masculino , Animais , Humanos , Polímeros/química , Povidona/química , Tadalafila/química , Disfunção Erétil/tratamento farmacológico , Solubilidade
3.
AAPS PharmSciTech ; 23(5): 133, 2022 May 09.
Artigo em Inglês | MEDLINE | ID: mdl-35534652

RESUMO

Sediment delivery model (SeDeM) system is innovative tool to correlate micromeritic properties of powders with compressibility. It involves computation of indices which facilitate direct compressibility of solids and enable corrective measures through particle engineering. Study had multiple objectives, viz, (i) to enhance solubility of BCS class II, nevirapine using solid dispersions; (ii) SeDeM analyses of excipients and solid dispersions to analyze direct compressibility; and (iii) prepare orodispersible tablets (ODT). Solid dispersions were prepared by solvent evaporation. Superdisintegrants and solid dispersions were analyzed for primary indices of dimension, compressibility, flowability, stability, and disgregability derived from micromeritic properties. Radar diagrams were constructed to provide visual clues to deficient properties for direct compressibility. ODTs were prepared using excipients which passed criteria for direct compressibility and evaluated for tablet properties. Solid dispersions with Eudragit S100 revealed 6 to 10 fold increase in solubility in various dissolution media including biorelevant media in comparison with plain drug. Solubility was found to be pH dependent. SeDeM analyses facilitated identification of superdisintegrants and excipients with unfavorable compressibility. Radar diagrams provided a clear pictorial evidence of lacunae in powder properties. Based on SeDeM results, tablets were formulated by direct compression using crosspovidone, croscarmellose sodium, and mannitol. All batches showed 40% release in first minute in simulated salivary fluid.


Assuntos
Excipientes , Sistemas Inteligentes , Composição de Medicamentos/métodos , Excipientes/química , Pós/química , Solubilidade , Comprimidos/química
4.
Chem Pharm Bull (Tokyo) ; 69(8): 747-759, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34334518

RESUMO

The particles of phenytoin (Phe), a poorly water-soluble model drug, were bead-milled alone or co-milled with a hydrophilic waxy additive using an ultra cryo-milling technique in liquid nitrogen (LN2) to improve its dissolution properties. However, the micronized drug particles adhered and aggregated, resulting in poor handling in manufacturing processes such as blending or tableting. To improve the dissolution profile and powder properties of the drug simultaneously, the milled products were secondarily processed together with larger spherical particles by mechanical powder processing. These secondary products were composite particles with a core-shell structure, with fine drug particles adhered and deposited on the core, based on order mixing theory. As a core, three types/sizes of spherical pharmaceutical excipient particles were applied. The resultant composite particles produced much faster release profiles than just milled or co-milled mixtures. In addition, the composite particles showed good micromeritic properties depending on the size of the core particles. These results indicate that the ultra cryo-milling and subsequent dry composite mixing is a potential approach for developing drug particles with improved dissolution.


Assuntos
Anticonvulsivantes/química , Fenitoína/química , Química Farmacêutica , Composição de Medicamentos , Tamanho da Partícula , Pós , Solubilidade
5.
Acta Pharm ; 69(3): 381-398, 2019 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-31259736

RESUMO

Reduced bioavailability of azelnidipine is related to its poor aqueous solubility and extensive first-pass metabolism, which hinder its efficacy. These problems were addressed by implementing (1) a liquisol technique for promoting the dissolution rate in a controlled-release manner and (2) a core-in-cup bucco-adhesive drug delivery system as an alternative to the oral route. A 33 factorial design was used to study the effects of polymer type (sodium carboxymethyl cellulose (CMC Na), chitosan, or Carbomer P940) concentration (5, 10 or 15 %) and preparation technique (simple mix, liquisol or wet granulation) on the dissolution and mucoadhesion of core-in-cup azelnidipine buccoadhesive tablets. Tablet micromeritics, swelling index, mucoadhesive strength and in vitro release were characterized. Statistical analyses of these factors show ed significant effects on the studied responses, where F#16 prepared by the liquisol technique and containing 15 % CMC Na was chosen with an overall desirability of 0.953.


Assuntos
Adesivos/química , Ácido Azetidinocarboxílico/análogos & derivados , Di-Hidropiridinas/química , Mucosa Bucal/metabolismo , Comprimidos/química , Resinas Acrílicas/química , Adesivos/metabolismo , Administração Bucal , Ácido Azetidinocarboxílico/química , Ácido Azetidinocarboxílico/metabolismo , Disponibilidade Biológica , Carboximetilcelulose Sódica/química , Celulose/química , Quitosana/química , Preparações de Ação Retardada/química , Preparações de Ação Retardada/metabolismo , Di-Hidropiridinas/metabolismo , Sistemas de Liberação de Medicamentos/métodos , Polímeros/química , Solubilidade/efeitos dos fármacos , Comprimidos/metabolismo
6.
Zhongguo Zhong Yao Za Zhi ; 44(8): 1558-1563, 2019 Apr.
Artigo em Chinês | MEDLINE | ID: mdl-31090319

RESUMO

Commonly used dosage forms of fermented Cordyceps powder products are capsules and tablets. The hygroscopicity of the powder,as one of the important parameters in the tableting process,has important effects on the tabletting process of the tablets. How to improve the hygroscopicity of powder is of great significance for the development of new composite particles. Therefore,particle design technology was used in this study to prepare composite particle powder,and its hygroscopicity was compared with fermented Cordyceps powder and physically mixed powder. By preparing three different types of powders,the equilibrium moisture absorption,particle size,scanning electron micrograph,angle of repose,contact angle and compression degree were compared to observe the effect of traditional Chinese medicine particle design technology on improving the hygroscopicity of the fermented Cordyceps powder. The results showed that the equilibrium moisture absorption was 21. 2%,19. 6%,14. 5% respectively for the fermented Cordyceps powder,physically mixed powder and composite particle powder; the median diameter was(49. 751± 0. 280),(59. 183± 0. 170),(12. 842±0. 080) µm,respectively; the mode diameter was(185. 479±1. 372),(173. 964± 1. 104),(61. 671± 0. 979) µm,respectively. In the scanning electron micrograph of the composite particle powder,it can be clearly seen that the fermented Cordyceps powder had hydrophobic gas phase nano-silica with a fixed shape and uniform size. The angle of repose was(50. 63 ± 0. 75) °,(49. 25 ± 0. 43) °,(48. 33±0. 84) ° respectively; the contact angle was(7. 4±0. 2) °,(8. 2±0. 3) °,(15. 0±2. 6) ° respectively; and the compression degree was(38. 2±1. 3) %,(35. 8±0. 2) %,(32. 5±2. 6) % respectively. This study showed that after treatment by the vibrating ultrafine pulverizer,the fermented Cordyceps powder particles had obvious and uniform small particle hydrophobic gas phase nano-silica adhered to form a partially wrapped coating structure,which reduced the contact surface of fermented Cordyceps powder with the outside world,thereby reducing the hygroscopicity of the composite particle powder. It further demonstrated that the hygroscopicity of fermented Cordyceps powder can be improved by particle design.


Assuntos
Cordyceps , Fermentação , Medicina Tradicional Chinesa , Molhabilidade , Tamanho da Partícula , Pós
7.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-774521

RESUMO

Commonly used dosage forms of fermented Cordyceps powder products are capsules and tablets. The hygroscopicity of the powder,as one of the important parameters in the tableting process,has important effects on the tabletting process of the tablets. How to improve the hygroscopicity of powder is of great significance for the development of new composite particles. Therefore,particle design technology was used in this study to prepare composite particle powder,and its hygroscopicity was compared with fermented Cordyceps powder and physically mixed powder. By preparing three different types of powders,the equilibrium moisture absorption,particle size,scanning electron micrograph,angle of repose,contact angle and compression degree were compared to observe the effect of traditional Chinese medicine particle design technology on improving the hygroscopicity of the fermented Cordyceps powder. The results showed that the equilibrium moisture absorption was 21. 2%,19. 6%,14. 5% respectively for the fermented Cordyceps powder,physically mixed powder and composite particle powder; the median diameter was(49. 751± 0. 280),(59. 183± 0. 170),(12. 842±0. 080) μm,respectively; the mode diameter was(185. 479±1. 372),(173. 964± 1. 104),(61. 671± 0. 979) μm,respectively. In the scanning electron micrograph of the composite particle powder,it can be clearly seen that the fermented Cordyceps powder had hydrophobic gas phase nano-silica with a fixed shape and uniform size. The angle of repose was(50. 63 ± 0. 75) °,(49. 25 ± 0. 43) °,(48. 33±0. 84) ° respectively; the contact angle was(7. 4±0. 2) °,(8. 2±0. 3) °,(15. 0±2. 6) ° respectively; and the compression degree was(38. 2±1. 3) %,(35. 8±0. 2) %,(32. 5±2. 6) % respectively. This study showed that after treatment by the vibrating ultrafine pulverizer,the fermented Cordyceps powder particles had obvious and uniform small particle hydrophobic gas phase nano-silica adhered to form a partially wrapped coating structure,which reduced the contact surface of fermented Cordyceps powder with the outside world,thereby reducing the hygroscopicity of the composite particle powder. It further demonstrated that the hygroscopicity of fermented Cordyceps powder can be improved by particle design.


Assuntos
Cordyceps , Fermentação , Medicina Tradicional Chinesa , Tamanho da Partícula , Pós , Molhabilidade
8.
J Pharm Sci ; 105(10): 3105-3114, 2016 10.
Artigo em Inglês | MEDLINE | ID: mdl-27492963

RESUMO

Control and optimization of the physical properties of a drug substance (DS) are critical to the development of robust drug product manufacturing processes and performance. A lack of isolatable, for example, crystalline, DS solid forms can present challenges to achieving this control. In this study, an isolation scheme for an amorphous DS was developed and integrated into the synthetic route producing DS with optimized properties. An inert absorbent excipient (Neusilin® US2) was used to isolate the DS via a novel antisolvent scheme as the final step of the route. Isolation was executed at kilogram scale utilizing conventional equipment. The resulting 50 wt% DS:Neusilin complex had improved physical stability and exceptional micromeritic and tableting properties. Improved dissolution was observed and attributed to enhanced dispersion and increased surface area. Characterization data suggest a high degree of penetration of the DS into the Neusilin, with DS occupying 70% of mesopore and 12% of macropore volume. This approach has application in the isolation and particle engineering of difficult to isolate DS without additional unit operation, such as spray drying, and has the potential for a high degree of optimization and control of physical properties over the course of DS development.


Assuntos
Compostos de Alumínio/química , Compostos de Alumínio/isolamento & purificação , Compostos de Magnésio/química , Compostos de Magnésio/isolamento & purificação , Silicatos/química , Silicatos/isolamento & purificação , Silicatos de Alumínio/química , Silicatos de Alumínio/isolamento & purificação , Força Compressiva , Magnésio/química , Magnésio/isolamento & purificação , Tamanho da Partícula , Propriedades de Superfície , Difração de Raios X/métodos
9.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-477035

RESUMO

Objective To compare the micromeritics properties and external dissolution rates of Sanhuang Powder in different particle sizes;To provide references for its direct use and application as raw materials for TCM preparation.Methods Particle size, bulk density, tap density, angle of repose, and hygroscopicity ofSanhuang micro-powder and common powder were investigated and evaluated. External dissolution rates ofSanhuang micro-powder and common powder were detected by ultraviolet spectrophotometry.Results The flowability of bothSanhuang micro-powder and common powder were not very well. With the sizes decreasing, the hygroscopicity of micro-powder became stronger. The external dissolution ofSanhuang micro-powder was more sufficient and much more quickly than common powder.Conclusion Properties ofSanhuang micro-powder and common powder are obviously different.Sanhuang micro-powder has stronger hygroscopicity and worse flowability compared with common powder. However, external dissolution ofSanhuang micro-powder is more sufficient and much more quickly than common powder. WhenSanhuang micro-powder is used directly and used as raw materials for TCM preparation, much more discretion should be considered.

10.
Int J Pharm ; 462(1-2): 83-102, 2014 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-24378327

RESUMO

Ibuprofen was recrystallized in the presence of aqueous solution of cationic dextran derivative, Diethylaminoethyl Dextran (Ddex) using the melt-in situ granulation-crystallization technique in order to produce a stable amorphous ibuprofen-Ddex conjugates with improved morphological, micromeritic and thermo-analytical characteristics without the use of organic solvent. Ddex was used in this study because of its ability to form conjugates with various drug molecules and enhance their physicochemical characteristics and therapeutic activities. Cationic dextrans are also biocompatible and biodegradable. Mechanism of conjugation as well as the impact of conjugation on the ibuprofen crystal habit was investigated. Gaussian type normal particle size distribution was obtained and the size of the crystals in the crystanule conjugates decreased steadily, with increasing concentration of Ddex, to a minimum of 480 nm (440-folds reduction, p<0.05, n=20) at Ddex molar concentration of 0.01 mM. FT-IR spectra showed electrostatic interaction and hydrogen bonding between ibuprofen and Ddex which was confirmed with the (1)H NMR and (13)C NMR spectra. DSC curves exhibited single peaks from the binary ibuprofen-Ddex conjugate crystanules suggesting compatibility and formation of an eutectic product. The conjugate crystanules showed broad and diffuse endothermic peaks with a glass transition temperature (T(g)) of 58.3 and 59.14°C at Ddex molar concentrations of 1.56 × 10(-4) and 3.125 × 10(-4)mM respectively confirming the existence of ibuprofen-Ddex crystanule conjugates in amorphous state. Higher concentrations of Ddex decreased T(g) steadily. TGA curves showed first order degradation at low molar concentrations of Ddex up to 3.125 × 10(-4)mM which coincides with the critical granular concentration of the crystanules while higher concentrations exhibited second order degradation profile. This study provides the basis for the development of stable amorphous drug-polymer conjugates with potential practical application in controlled and extended drug release formulations.


Assuntos
Anti-Inflamatórios não Esteroides/química , DEAE-Dextrano/química , Portadores de Fármacos/química , Ibuprofeno/química , Varredura Diferencial de Calorimetria , Química Farmacêutica/métodos , Cristalização , Preparações de Ação Retardada , Composição de Medicamentos/métodos , Estabilidade de Medicamentos , Ligação de Hidrogênio , Tamanho da Partícula , Espectroscopia de Infravermelho com Transformada de Fourier , Eletricidade Estática , Temperatura , Temperatura de Transição
11.
Chinese Pharmaceutical Journal ; (24): 1625-1630, 2014.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-860003

RESUMO

OBJECTIVE: To evaluate the micromeritic properties of Parteck® ODT to provide preliminary theoretical basis for the direct compression technology of orally disintegrating tablets (ODTs).

12.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-440121

RESUMO

Objective To optimize the forming process of Wuzibushen Capsules. Methods Category and ratio of accessories were investigated by taking moisture absorption percentage as index. The inspected angle of repose, bulk density and critical relative humidity were also investigated. Results Starch was used as the excipien. Remedium cardinale and starch in the ratio of 1.15∶1.25 was more appropriate, 60% alcohol was added, dried at 60 ℃. Granules had a good fluidity, critical relative humidity was about 62%. Conclusion The forming technology was reasonable and provide reliable basis for production.

13.
Indian J Pharm Sci ; 75(3): 302-9, 2013 May.
Artigo em Inglês | MEDLINE | ID: mdl-24082346

RESUMO

The objective of our work was to study the micromeritic properties of lyophilized diclofenac potassium-loaded lipospheres and to evaluate in vivo, the analgesic properties of diclofenac potassium in the lipospheres in addition to other in vitro properties. Solidified reverse micellar solutions were prepared by fusion using 1:1, 2:1, and 1:2% w/w of Phospholipon(®) 90H and Softisan(®) 154. Diclofenac potassium (1, 3, and 5% w/w) was incorporated into the solidified reverse micellar solutions. Solidified reverse micellar solutions-based lipospheres were formulated by melt homogenization techniques using Ultra-Turrax homogenizer, and thereafter lyophilized to obtain water-free lipospheres. The lipospheres were characterized in terms of particle size and morphology, stability, thermal analysis, drug content, encapsulation efficiency, and loading capacity. The flow properties of the lipospheres were studied using both direct and indirect methods of assessing flow. The analgesic properties of the lipospheres were studied using the hot plate method. Results obtained showed that the yield of diclofenac potassium-loaded lipospheres was high and the particle size ranged from 0.61±0.07 to 2.55±0.04 µm. The lipospheres had high encapsulation efficiency of 95%, which was affected by the amount of drug loaded, while the loading capacity increased with the increase in drug loading. Diclofenac potassium-loaded lipospheres exhibited poor flow. The formulations exhibited good analgesic effect compared with the reference and had 84 to 86% drug release at 13 h. The lipospheres based on solidified reverse micellar solutions could be used for oral delivery of diclofenac potassium.

14.
J Pharm Sci ; 102(11): 4087-99, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24018750

RESUMO

Gas pycnometry is applied to determine the density of solid materials. The analysis of lyophilisates is particularly challenging because of their porous structure. In this study, the density of raw materials and freeze-dried products was determined using different pycnometric methodologies and gases [helium (He), nitrogen (N2 ), sulfur hexafluoride]. The number of purges was set to 60 independent of the gas used. Intact and ground lyophilisates were examined, and major differences were found between use of He and N2 . For example, the density of sucrose lyophilisates measured using He remained almost constant before (1.51 g/cm(3) ) and after (1.52 g/cm(3) ) grinding. In contrast, the density of a sucrose lyophilisate before grinding determined with N2 was 1.33 g/cm(3) . On the basis of µCT and scanning electron microscopy pictures, it appears likely that the majority of pores are interconnected, with only a small fraction of closed pores. Helium is able to penetrate deep into the freeze-dried matrix and is supposedly absorbed by the material. The N2 molecules were not able to penetrate closed pores; therefore, the skeletal density of an intact lyophilisate was determined. Reproducibility of the established method was verified, and freeze-dried orally disintegrating tablets of different compositions were analyzed.


Assuntos
Excipientes/química , Liofilização , Sacarose/química , Tecnologia Farmacêutica , Liofilização/métodos , Gases/química , Hélio/química , Nitrogênio/química , Porosidade , Gravidade Específica , Comprimidos/química , Tecnologia Farmacêutica/métodos
15.
Chinese Pharmaceutical Journal ; (24): 358-361, 2012.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-860804

RESUMO

OBJECTIVE: To study influence of humidity on granule flowability, explore relationship between flowability and quality of guaifenesin sustained tablet, give a basis for industrialization. METHODS: By hygroscopicity study, CRH was measured. After 10 days in RH 33%, 60%, 75%, 84%, 92.5%, flowability of granule and quality index of tablet, such as appearance, extremum of weighty friability was measured and compared with result of 0 d. Functional relationship between micromeritics parameter and quality index of tablet was fitted. RESULTS: CRH of granule is between RH 67%-68%. When relative humidity is above RH 60%, flow-ability and quality of tablet is changed obviously. Used compressbiliity as X1, repose angle as X2, extremum of tablet weight as Y1, friability as Y2, linear relationship of them is Y1 = 0.192X1+ 0.092X2- 7.398 (r = 0.9921), Y2= 0.069X1 + 0.087X2 - 3.505 (r = 0.9881), when P < 0.001, the equations had statistical significance in the range of observation. CONCLUSION: Relative humidity of production and storage of granule should less than RH 60%. Functional relationship between micromeritics parameter of granule (compressbiliity and repose angle) and quality index of tablet (extremum of weighty friability) had statistical significance in the range of observation. Copyright 2012 by the Chinese Pharmaceutical Association.

16.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-855743

RESUMO

Objective: To study the micromeritics of common powder and superfine powder of Chuan-xiong Rhizoma. Methods: Particle size and particle size distribution were detected by laser particle analyzer; Microscopic characteristics of the two sorts of powder of Chuanxiong Rhizoma were surveyed by biological microscope; The angle of repose and the bulk density were measured; The moisture absorption of common powder and superfine powder were determined on condition of 25°C and relative humidity of 75%. Results: D50 of common powder and superfine powder were 14.58 and 58.54 μm, and the superfine powder was more uniformly distributed. There were many differences between superfine powder and common powder in microscopic characteristics, including greatly smaller oil droplets in superfine powder. There was no significant change in flow ability, bulk density, and moisture absorption. Conclusion After being superfinely comminuted, the powder of Chuanxiong Rhizoma is more uniformly distributed with greatly increased broken cell wall. The oil droplets are much smaller in surperfine powder, which provides a preliminary basis for "emulsification structure". There is no significant change in flow ability, bulk density, and moisture absorption because of rich volatile oil in Chuanxiong Rhizoma.

17.
RBCF, Rev. bras. ciênc. farm. (Impr.) ; 43(3): 435-446, jul.-set. 2007. ilus, graf, tab
Artigo em Português | LILACS | ID: lil-468150

RESUMO

O processo de granulação úmida ainda encontra larga aplicabilidade junto à moderna indústria farmacêutica para a produção de comprimidos, pois elimina alguns dos principais problemas atribuídos à compressão direta: a tendência de segregação e as baixas propriedades de fluxo dos pós durante o processo. O presente trabalho avalia e compara através de estudos micromeríticos e análise estatística as características de fluxo de granulados destinados ao desenvolvimento de comprimidos de hidroclorotiazida 50 mg. Foram testados três aglutinantes (pasta de amido e as dispersões aquosas, preparadas a frio, de amido pré-gelatinizado e povidone). Avaliou-se ainda a compatibilidade entre o fármaco e os excipientes empregados, através de estudos termoanalíticos (DSC), e a influência da adição extragranular do superdesintegrante crospovidone nos valores de eficiência de dissolução ( por centoED) dos comprimidos obtidos. Os granulados obtidos apresentaram propriedades de fluxo e compressibilidade boas a excelentes, caracterizadas por: valores de índice de compressibilidade situados entre 5 e 15; proporções de Hausner inferiores a 1,25 e ângulos de repouso entre 30 e 35º. A adição de crospovidone não incrementou os valores de por centoED das formulações desenvolvidas, nas condições experimentais empregadas, ainda que tenha reduzido, de forma pouco significativa, os tempos de desintegração das formulações.


The wet granulation process still finds large applicability close to the modern pharmaceutical industry for the production of tablets, because it eliminates some of the main attributed problems of the direct compression: the segregation tendency and the low flow properties of the powders during the process. The present work evaluates and it compares through micromeritical studies and statistical analysis the flow characteristics of granulates destined to the development of tablets of hydrochlorothiazide 50 mg. Three binders were tested (paste of starch and the aqueous dispersions, prepared to cold, of pregelatinized starch and povidone). It was still evaluated the compatibility between the drug and the employed excipients, through termoanalytical studies (DSC), and the influence of the extra granular addition of the "superdisintegrant" crospovidone in the values of dissolution efficiency ( percentDE) of the obtained tablets. The obtained granulates presented good flow and compressibility properties, characterized by: values of compressibility index between 5 and 15; Hausner ratio less than 1,25 and angle of repose between 30 and 35º. The crospovidone addition did not increase the values of percentED of the developed formulations, in the experimental conditions employed, although it has reduced, in way a low significance, the disintegration times of the formulations.


Assuntos
Anti-Hipertensivos , Hidroclorotiazida , Biofarmácia , Excipientes Farmacêuticos , Comprimidos
18.
China Pharmacy ; (12)2007.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-531477

RESUMO

OBJECTIVE:To prepare oxymatrine pellets and study the pellets' properties.METHODS:Oxymatrine pellets were prepared using an experimental low-temperature extrusion-spheronization granulator.L9(34)orthogonal design was used to obtain optimal formulation.The micromeritic properties and in vitro dissolution of the pellets at different dosage were determined.RESULTS:Oxymatrine pellets prepared by extrusion-spheronization were round and smooth and well-distributed.The optimal technical conditions were as follows:water∶MCC=0.90∶1;spheronization velocity=35 Hz;spheroniza-tion time=5 min;extrusion velocity=40 Hz.The in vitro dissolution was more than 75% within 30 minutes.CONCLUSION:The process of preparing pellets by extrusion-spheronization was simple and feasible and the quality of pellets was excellent.

19.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-681429

RESUMO

Objective: To improve the physical properties of micromeritics of the extracts of Fengshilin capsule, such as anti moisture. Methods: Critical relative humidity, absoption curve of moisture, angle of repose were used as the norms of the research. The suitable excipients and formulation process of Fengshilin capsule have been sieved. Results: It was feasible that the combined excipients of microcystalline cellulose and starch (in a ratio of 1∶1) were mixed with the extract powder. The absorption of moiture of the extract powder was improved. The humidity of mass production and store was lower than 45%. Conclusion: The research has been found to be an effective in the process of Fengshilin capsule.

SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...