Formulation Design of a Highly Hygroscopic Drug (Pyridostigmine Bromide) for its Hygroscopic Character Improvement and Investigation of In Vitro/In Vivo Dissolution Properties

Huang, Yuh-Tyng; Tsai, Tsung-Yu; Cheng, Chun-Jen; Cham, Thau-Ming; Lai, Tsun-Fwu; Chuo, Wen-Ho

doi:10.1080/03639040601031890

Cited by 14 publications

(7 citation statements)

References 29 publications

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“…Another modified release dosage forms of PB are Eudragit RS microparticles (Hegazy et al 2002), sustained released pellets (Huang et al 2007b), HPMC-based SR tablet (Huang et al 2007c), and prolonged release matrix tablet (Bolourchian et al 2012). Release rate of PB from these formulations was relatively high and 100 % of PB is released in less than 1 day (Huang et al 2007a, c;Hegazy et al 2002;Bolourchian et al 2012). Another modified release dosage of PB is poly (lactic acid) nanoparticles (NPs) (Tan et al 2012a), which releases most of the drug in the initial burst (50 % of PB was released in less than 1 h) followed by a very slow release over an extended period of time (72 h) (Tan et al 2012a).…”

Section: Introductionmentioning

confidence: 96%

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Eudragit RS PO nanoparticles for sustained release of pyridostigmine bromide

et al. 2013

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Pyridostigmine bromide (PB) is an inhibitor of cholinesterase, which is used in the treatment of myasthenia gravis and administered for protection against exposure to toxic nerve agents. Tests were done to investigate prolonging the half-life of PB and improving its release behavior. PB was loaded in nanoparticles (NPs) of Eudragit RS PO (Eu-RS) prepared using the technique of quasi emulsion solvent diffusion. Variables of output power of the sonicator, bath temperature and mixing time, were chosen as the optimization factors to obtain the minimum sized NPs. In addition, emulsions were tested at different ratios of drug-to-polymer by dynamic light scattering to determine size and zeta potential of NPs. UV-spectroscopy was used to determine PB content of the NPs. Drug-loaded NPs were characterized by scanning electron microscopy, X-ray diffraction, and Fourier transform infrared spectra. Results determined that mixing time had a significant impact on the size of Eu-RS NPs, but power output of sonicator and bath temperature had no significant effect. The particle size obtained at the optimum condition (power output of 70 W, bath temperature of 33°C, and mixing time of 7 min) was less than 200 nm (optimum sizes were 138.9 and 179.5 nm for Eu-RS and PB-loaded Eu-RS NPs, respectively). The optimum PB-loaded Eu-RS NPs at the PB to Eu-RS weight ratio of 1-4 and 20 % of loaded PB released from the nanocarriers within 100 h.

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Section: Introductionmentioning

confidence: 96%

“…The nerve agents (NAs) used in chemical attacks cause disturbance to the synapse activity (Huang et al 2007a). Soman is one of the strongest of these NAs and treating Soman poisoning is difficult and dependent on timing (Huang et al 2007b).…”

Section: Introductionmentioning

confidence: 99%

Eudragit RS PO nanoparticles for sustained release of pyridostigmine bromide

et al. 2013

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“…Desired and reproducible results were achieved via microporous membrane coating using a soluble salt like sodium lauryl sulfate in the film coating solution (Elchidana and Deshpande, 1999). Huang et al have shown that the hygroscopic character of pyridostigmine bromide can be improved by coating process and the sustained-release pellets with specific release rate can be achieved by sustained-release coated pellets (Huang et al, 2007 Sustained-release matrix pellets Sustained-release matrix pellets are preferred to sustainedrelease coated pellets because of their ease of manufacture and in-process control. Theoretically, sustained-release matrix pellets can be formulated via the extrusion-spheronization process.…”

Section: Coated Pellets For Sustained Drug Deliverymentioning

confidence: 99%

Controlled-Release Pelletized Dosage Forms Using the Extrusion-Spheronization Process

Rhee¹,

Lee²,

Lee³

et al. 2010

Journal of Pharmaceutical Investigation

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− Pellets, which are multiple-unit dosage systems, have the several therapeutic advantages over single-unit dosage systems in oral drug delivery. This review focuses on the current status and explores extrusion-spheronization technique with special attention to controlled-release application of pellets including coated pellets for delayed release formulations, coated pellets for colon delivery, coated pellets for sustained drug delivery, sustained-release matrix pellets, pellets compressed into tablets, bioadhesive pellets, floating pellets, and pelletization with solubilization techniques.Key words − Pellets, Multiparticulates, Modified-release, Pelletization, Solubilization Pelletization process is an agglomeration process that results in agglomerates of a narrow size distribution in the range of 0.5-1.5 mm with a low intra-agglomerate porosity (about 10%) and the higher density compared to the granules. Pellets are produced by pelletization process and these agglomerates have the relatively spherical shape, low friability and free flowing properties, which facilitate the handling of pellets in the manufacturing process. Pelletization process can prevent the segregation of co-agglomerated components, resulting in an improvement of the content uniformity. Pelletization process can also avoid the dust formation resulting in an improvement of the process safety, as fine powders can cause dust explosions and respiratory health problems. Pellets are widely used in multiparticulate systems and multiparticulate systems have the several therapeutic advantages over single-unit dosage systems in oral drug delivery. The low inter-and intra-subject variability can be achieved by multiparticulate systems because multiparticulates can pass through the pylorus immediately after administration. Moreover, less effect of food on drug absorption and rather uniform gastric emptying time than single-unit dosage systems can be attainable in multiparticulate systems. Safety concerns due to dose dumping of drugs, which have narrow therapeutic index, is minimized in multiparticulate systems, and more foreseeable drug delivery in sustained release formulation is possible because the total drug dose is divided over many units, not in a single-unit system. The small size of multiparticulates also enables them to be well dispersed along the gastrointestinal (GI) tract, enhancing drug absorption and reducing the irritant effect that single-unit systems may cause to the mucosal lining, especially if remained for an extended time at a specific site. The spherical pellets can be coated with rate-controlling polymers or compressed into tablets to achieve delayed-release, extended-release, and targeted-release profiles. Multiparticulate systems with different dose strengths can be obtained from the same batch of drug-loaded pellets without additional formulation or process modification. Pellets with different drugs or with different release profiles can be blended and formulated in a single-unit dosage form such as capsule, which promo...

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“…Further alternatives may be derived 934 from pyridostigmine bromide, which rapidly transforms from solid 935 to liquid state under ambient conditions as a result of water anneal-936ing. To address this challenge, pyridostigmine bromide was encapsulated into Avicel pH 102 -a water-insoluble excipient -by 938 extrusion-spheronization and water uptake was prevented[152].Other studies deployed porous calcium silicate for formulation of 940 very hygroscopic drugs[153].These exemplarily selected formulation strategies addressing 942 the challenge of hygroscopicity might form interesting approaches943 to meet a potential increase in hygroscopicity of ILs as compared to944 crystalline, conventional salts of the APIs; however, further studies 945 are required to prove that these approaches are a reasonable concept for ILs. Beside, lipophilic counterions reduce the propensity for 947 water annealing of the API-counterion pair, however, likely affect 948 other pharmaceutical parameters such as the dissolution rate or 949 kinetic solubility.…”

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confidence: 99%

“…In most pharmaceutical 150 applications, ILs result from proton transfer (Brønsted) which is 151 sometimes specified as protic ILs [50,56]. API-ILs are usually syn- 152 thesized by metathesis reactions [43,57]. Typically the components 153 (API and counterion) are obtained as a certain salt, dissolved in a 154 suitable solvent (e.g.…”

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confidence: 99%