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1.
Colloids Surf B Biointerfaces ; 189: 110833, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32058254

RESUMO

The implimentation of newer technologies in drug delivery system have always been the focus of pharmaceutical scientists with advancement of technologies. In this investigation, a novel controlled-release drug-resin combination device (DRC) was designed using dental resin to control the release of dextromethorphan hydrobromide (DH). The influence of different factors on in-vitro drug release were investigated. A Box-Behnken design was used to select the optimized DRC formulation. The optimized DH loaded DRC (DH-DRC) was prepared using 59.88% of PEG400, 16 mg of dental resin and 6.64 mg of sodium chloride (NaCl). The DH releases at 2 h, 4 h and 8 h of the optimized formulation were significantly close to the predicted responses. The pharmacokinetic study in rabbits showed DH-DRC had prolonged tmax and apparently reduced Cmax compared with commercial tablets and the AUC0-24h of DH-DRC was slightly higher than commercial tablets. This study confirmed the novel DRC could control the release of drug. It concluded that DRC would be a promising and alternative approach for the development of controlled release dosage form.


Assuntos
Resinas Compostas/química , Dextrometorfano/química , Animais , Dextrometorfano/sangue , Liberação Controlada de Fármacos , Tamanho da Partícula , Coelhos , Propriedades de Superfície , Comprimidos/química
2.
Eur J Pharm Sci ; 143: 105165, 2020 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-31765810

RESUMO

The objective of the present study was to develop a novel long-acting intra-oral delivery system (LIDS) to overcome the frequent administration by the nonparenteral route with Huperzine A (HupA) as a model drug. HupA-LIDS was prepared using a magnetic drug delivery with dental resin as release controlling layer for long-term release of HupA. The factors that influenced the drug release comprised of the type and amount of pore formers, the speed of shaker, resin layer weight and drug loading. These factors were evaluated and optimized. The in-vitro release studies showed that the system was able to deliver HupA in an approximately zero-order kinetic. The SEM study showed that the multiple orifices on the surface of a resin layer formed due to presence of pore formers, which contributed to the HupA release. The pharmacokinetic study in rabbits demonstrated the HupA-LIDS could be released in vivo for more than 8 days with prolonged Tmax and significantly reduced Cmax in comparison with commercial tablets. This study provided some pioneering ideas for developing intra-oral extended release drug delivery system using dental resin as release controlling materials. The optimized HupA-LIDS can make excellent sustained release and have the potential for the long-acting product in the therapy of Alzheimer's disease.


Assuntos
Alcaloides/administração & dosagem , Inibidores da Colinesterase/administração & dosagem , Fármacos Neuroprotetores/administração & dosagem , Resinas Sintéticas/administração & dosagem , Sesquiterpenos/administração & dosagem , Administração Oral , Alcaloides/química , Alcaloides/farmacocinética , Animais , Inibidores da Colinesterase/farmacocinética , Preparações de Ação Retardada/administração & dosagem , Preparações de Ação Retardada/química , Preparações de Ação Retardada/farmacocinética , Liberação Controlada de Fármacos , Mucosa Bucal/metabolismo , Fármacos Neuroprotetores/farmacocinética , Coelhos , Resinas Sintéticas/química , Resinas Sintéticas/farmacocinética , Sesquiterpenos/química , Sesquiterpenos/farmacocinética , Comprimidos
3.
Biomed Pharmacother ; 108: 1225-1236, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30372824

RESUMO

Insulin, as the most important drug for the treatment of diabetes, can effectively control the blood glucose concentration in humans. Due to its instability, short half-life, easy denaturation and side effects, the administration way of insulin are limited to subcutaneous injection accompany with poor glucose control and low patient compliance. In recent years, emerging insulin delivery systems have been developed in diabetes research. In this review, a variety of stimuli-responsive insulin delivery systems with their response mechanism and regulation principle are described. Further, the introduction of stem cell transplantation and mobile application based delivery technologies are prudent for the diabetes treatment. This article also discusses the advantages and limitations of current strategies, along with the opportunities and challenges for future insulin therapy.


Assuntos
Diabetes Mellitus/tratamento farmacológico , Sequência de Aminoácidos , Humanos , Insulina/química , Insulina/metabolismo , Internet , Smartphone , Transplante de Células-Tronco
4.
AAPS PharmSciTech ; 5(2): e34, 2004 Apr 08.
Artigo em Inglês | MEDLINE | ID: mdl-15760092

RESUMO

The purpose of this research was to prepare a gastroretentive drug delivery system of ranitidine hydrochloride. Guar gum, xanthan gum, and hydroxypropyl methylcellulose were evaluated for gel-forming properties. Sodium bicarbonate was incorporated as a gas-generating agent. The effects of citric acid and stearic acid on drug release profile and floating properties were investigated. The addition of stearic acid reduces the drug dissolution due to its hydrophobic nature. A 3(2) full factorial design was applied to systemically optimize the drug release profile. The amounts of citric acid anhydrous (X1) and stearic acid (X2) were selected as independent variables. The times required for 50% (t50) and 80% drug dissolution (t80), and the similarity factor f2 were selected as dependent variables. The results of the full factorial design indicated that a low amount of citric acid and a high amount of stearic acid favors sustained release of ranitidine hydrochloride from a gastroretentive formulation. A theoretical dissolution profile was generated using pharmacokinetic parameters of ranitidine hydrochloride. The similarity factor f2 was applied between the factorial design batches and the theoretical dissolution profile. No significant difference was observed between the desired release profile and batches F2, F3, F6, and F9. Batch F9 showed the highest f2 (f2 = 75) among all the batches, and this similarity is also reflected in t50 (approximately 214 minutes) and t80 (approximately 537 minutes) values. These studies indicate that the proper balance between a release rate enhancer and a release rate retardant can produce a drug dissolution profile similar to a theoretical dissolution profile.


Assuntos
Sistemas de Liberação de Medicamentos , Antagonistas dos Receptores H2 da Histamina/administração & dosagem , Ranitidina/administração & dosagem , Química Farmacêutica , Antagonistas dos Receptores H2 da Histamina/farmacocinética , Ranitidina/farmacocinética , Estômago
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