hypromellose

羟丙甲纤维素
  • 文章类型: Journal Article
    干眼症(DED)是一种高度流行的疾病,导致生活质量下降,社会生活参与率下降,工作效率下降。羟丙基甲基纤维素(HPMC)是基于纤维素的粘度增强剂,并且是人工泪液中最受欢迎的治疗成分之一。本文旨在评估有关HPMC用于治疗DED的疗效和安全性的文献。文献检索在PubMed和CochraneCENTRAL进行。本综述共包括26种出版物中的28项临床试验,包括21项临床干预研究,评估HPMC治疗随时间推移的效果,以及7项单一滴注研究,评估滴注后HPMC的短期身体和症状影响。临床干预研究的持续时间为2周至5.5个月。DED严重程度从轻度到重度不等。滴落频率范围为每天2至16滴。人工泪液中的HPMC浓度范围为0.2%至0.5%。未报告重大并发症或不良事件。含有HPMC的人工泪液可有效改善DED的症状和一些体征。然而,与HPMC加其他治疗成分的组合滴剂似乎比单独使用HPMC更有效.HPMC似乎同样有效或劣于透明质酸(HA)。没有证据表明羧甲基纤维素(CMC)或聚乙二醇400/丙二醇(PEG/PG)的优势或劣势。没有一项研究解释了滴落频率或HPMC浓度的选择。需要更多精心设计的研究来确定HPMC治疗的循证标准,包括下降频率,不同DED严重程度和亚组的浓度和分子量。
    Dry eye disease (DED) is a highly prevalent condition, resulting in reduced quality of life, lower participation in social life and impaired work efficiency. Hydroxypropyl methylcellulose (HPMC) is a cellulose-based viscosity-enhancing agent and is one of the most popular therapeutic ingredients in artificial tears. This review aims to evaluate the literature on the efficacy and safety of HPMC used in the treatment of DED. Literature searches were conducted in PubMed and Cochrane CENTRAL. A total of 28 clinical trials from 26 publications are included in this review, including 21 clinical intervention studies evaluating the effect of HPMC treatment over time and seven single instillation studies evaluating the short-term physical and symptomatic effects of HPMC after drop-instillation. The duration of clinical intervention studies ranged from 2 weeks to 5.5 months. DED severity ranged from mild to severe. Drop frequency ranged from two to up to 16 drops per day. HPMC concentration in artificial tears ranged from 0.2% to 0.5%. No major complications or adverse events were reported. Artificial tears containing HPMC were effective at improving symptoms and some signs of DED. However, combination drops with HPMC plus other therapeutic ingredients seem more effective than HPMC alone. HPMC appears to be equally effective or inferior to hyaluronic acid (HA). There is no evidence of superiority or inferiority to either carboxymethylcellulose (CMC) or polyethylene glycol 400/propylene glycol (PEG/PG). No single study explained the choice of drop frequency or HPMC concentration. More well-designed studies are needed to determine an evidence-based standard for HPMC treatment, including drop frequency, concentration and molecular weight for different DED severity and subgroups.
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  • 文章类型: Journal Article
    所进行的研究的目的是设计具有理想药物特性的儿科剂量的氢化可的松(0.5mg;1.0mg)的2mm口腔分散小片,并使用球磨机制备固体分散体消除苦味的感觉。选择氢化可的松作为模型物质,因为它在儿科人群中被广泛使用。ODMT是通过在传统的单冲片机中压制(制粒之前)制备的,并使用药典测试进行评估。DSC,和FTIR分析。用于评估掩味效果的方法包括健康志愿者的体内参与,“电子舌”分析装置的体外药物溶解和利用。该研究采用临床前动物模型来初步研究设计的药物剂型与参考产品的生物等效性。研究证实,由于在片剂中掺入了固体分散体,因此可以制造具有掩味作用的优质氢化可的松ODMT。
    The objective of the conducted research was to design 2 mm orodispersible minitablets of pediatric doses of hydrocortisone (0.5 mg; 1.0 mg) with desirable pharmaceutical properties and eliminate the sensation of a bitter taste using preparation of solid dispersion by ball mill. Hydrocortisone was selected as the model substance, as it is widely utilized in the pediatric population. ODMTs were prepared by compression (preceded by granulation) in a traditional single-punch tablet machine and evaluated using pharmacopoeial tests, DSC, and FTIR analysis. The methods used to evaluate the effectiveness of the taste-masking effect included in vivo participation of healthy volunteers, in vitro drug dissolution and utilization of an analytical device-\"electronic tongue\". The research employed a preclinical animal model to preliminary investigate the bioequivalence of the designed drug dosage form in comparison to reference products. The study confirmed the possibility of manufacturing good-quality hydrocortisone ODMTs with a taste-masking effect owing to the incorporation of a solid dispersion in the tablet mass.
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  • 文章类型: Journal Article
    药物的水溶性差是其生物利用度和药理活性的限制因素。许多方法是已知的,以提高药物的溶解度,其中,物理方法,固体分散体(SD),是应用的。SDs是药物和载体的物理混合物,有时添加表面活性剂,可以通过铣削获得,冷冻研磨,喷雾干燥,或冻干过程。在这项研究中,使用不同的载体通过研磨方法制备含依托度酸的固体分散体(ETD-SD),比如羟丙甲纤维素,聚乙烯吡咯烷酮,共聚维酮,尿素,还有甘露醇.溶解度研究,溶出度试验,形态学评估,热分析,和FTIR成像用于评价SD性能。结果表明,球磨工艺可用于获得具有ETD的SD。与未加工的ETD相比,所有设计的ETD-SD的特征在于更高的水溶性和更快的溶解速率。具有无定形载流子的SDs(HPMC,PVP,和PVP/VA)提供了比具有结晶特征的分散体(尿素和甘露醇)更大的ETD溶解度。FTIR光谱证实了ETD与测试载体的相容性。
    Poor water solubility of drugs is a limiting factor for their bioavailability and pharmacological activity. Many approaches are known to improve drug solubility, and among them, the physical method, solid dispersions (SDs), is applied. SDs are physical mixtures of a drug and a carrier, sometimes with the addition of a surfactant, which can be obtained by milling, cryomilling, spray-drying, or lyophilization processes. In this study, solid dispersions with etodolac (ETD-SDs) were prepared by the milling method using different carriers, such as hypromellose, polyvinylpyrrolidone, copovidone, urea, and mannitol. Solubility studies, dissolution tests, morphological assessment, thermal analysis, and FTIR imaging were applied to evaluate the SD properties. It was shown that the ball-milling process can be applied to obtain SDs with ETD. All designed ETD-SDs were characterized by higher water solubility and a faster dissolution rate compared to unprocessed ETD. SDs with amorphous carriers (HPMC, PVP, and PVP/VA) provided greater ETD solubility than dispersions with crystalline features (urea and mannitol). FTIR spectra confirmed the compatibility of ETD with tested carriers.
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  • 文章类型: Journal Article
    微粒作为多室药物递送系统对于难溶性药物是有益的。在微粒技术中应用的粘膜粘附聚合物延长了药物与粘膜表面的接触,增强了药物的生物利用度并延长了药物活性。海藻酸钠(ALG)和羟丙基甲基纤维素(羟丙甲纤维素,HPMC)是天然或半合成来源的聚合物,分别。它们的特征在于粘膜粘附特性,并应用于微粒技术。喷雾干燥是一种用于微粒制备的技术,由液体在气流中的雾化组成。在这项研究中,将具有泊沙康唑的喷雾干燥的ALG/HPMC微粒的药物特性与具有相同定性和定量组成的粉末的物理混合物的特性进行了比较。泊沙康唑(POS)作为一种相对新颖的抗真菌药被用作水溶性差的模型药物,和硬明胶胶囊作为设计制剂的储库。在0.1MHCl中的释放研究显示,与粉末混合物相比,从微粒的POS释放显著延长。在模拟阴道液(SVF)中没有遵循这种关系。微粒的特征还在于更强的粘膜粘附特性,增加的溶胀率,与粉末的物理混合物相比,停留时间延长。获得的结果表明,填充有微粒的硬明胶胶囊的药物性能与具有粉末混合物的硬明胶胶囊明显不同。
    Microparticles as a multicompartment drug delivery system are beneficial for poorly soluble drugs. Mucoadhesive polymers applied in microparticle technology prolong the contact of the drug with the mucosa surface enhancing drug bioavailability and extending drug activity. Sodium alginate (ALG) and hydroxypropyl methylcellulose (hypromellose, HPMC) are polymers of a natural or semi-synthetic origin, respectively. They are characterized by mucoadhesive properties and are applied in microparticle technology. Spray drying is a technology employed in microparticle preparation, consisting of the atomization of liquid in a stream of gas. In this study, the pharmaceutical properties of spray-dried ALG/HPMC microparticles with posaconazole were compared with the properties of physical mixtures of powders with equal qualitative and quantitative compositions. Posaconazole (POS) as a relatively novel antifungal was utilized as a model poorly water-soluble drug, and hard gelatin capsules were applied as a reservoir for designed formulations. A release study in 0.1 M HCl showed significantly prolonged POS release from microparticles compared to a mixture of powders. Such a relationship was not followed in simulated vaginal fluid (SVF). Microparticles were also characterized by stronger mucoadhesive properties, an increased swelling ratio, and prolonged residence time compared to physical mixtures of powders. The obtained results indicated that the pharmaceutical properties of hard gelatin capsules filled with microparticles were significantly different from hard gelatin capsules with mixtures of powders.
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  • 文章类型: Journal Article
    DDSolver中可用的数学模型应用于通过分析基于羟丙甲纤维素(HPMC)的基质片剂的卡维地洛释放而获得的实验溶出数据。通过改变制剂中填料和卡维地洛释放改性剂的综合选择来产生不同的卡维地洛释放曲线。对全部相关溶出度数据进行模型拟合,通过使用配对t检验确定,和独立的溶出数据高达约60%的卡维地洛释放。根据残差平方和(RSS)结果选择最佳模型,用作拟合优度的一般度量,以及利用各种标准对模型拟合进行视觉评估,并确定估计模型参数的可接受性,这些参数表明有关实验溶解结果和先前研究的爆发释放或滞后时间。此外,对卡维地洛释放机制进行了模型依赖性分析.
    The mathematical models available in DDSolver were applied to experimental dissolution data obtained by analysing carvedilol release from hypromellose (HPMC)-based matrix tablets. Different carvedilol release profiles were generated by varying a comprehensive selection of fillers and carvedilol release modifiers in the formulation. Model fitting was conducted for the entire relevant dissolution data, as determined by using a paired t-test, and independently for dissolution data up to approximately 60% of carvedilol released. The best models were selected based on the residual sum of squares (RSS) results used as a general measure of goodness of fit, along with the utilization of various criteria for visual assessment of model fit and determination of the acceptability of estimated model parameters indicating burst release or lag time concerning experimental dissolution results and previous research. In addition, a model-dependent analysis of carvedilol release mechanisms was carried out.
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  • 文章类型: Journal Article
    口腔不断地暴露于与外部环境接触。病原体可以很容易地进入和定殖它,导致许多通常伴有炎症的医疗状况,这反过来需要医疗干预,并导致健康恶化。这项研究的目的是获得可以作为氯己定载体的聚合物薄膜,一种用于治疗口腔炎症的活性物质,同时充当粘膜上的敷料。使用三种生物相容性和生物可降解聚合物的组合来制备膜。通过评估干燥后的失水来表征获得的样品,溶胀能力,吸湿性和拉伸强度。研究表明,HPMC和结冷胶或明胶的混合物可用于制备透明的,柔性聚合物膜与氯己定。所有测试的膜均显示出高吸湿性和溶胀能力。然而,观察到含有结冷胶的组合物更适合于获得在给药部位长时间停留的薄膜,这使它容易成为当地敷料的作用。
    The oral cavity is constantly exposed to contact with an external environment. Pathogens can easily access and colonize it, causing a number of medical conditions that are usually accompanied by inflammation, which in turn require medical intervention and cause the deterioration of wellbeing. The aim of this study was to obtain polymer films that could be a carrier for chlorhexidine, an active substance used in the treatment of inflammation in the oral cavity, and at the same time act as a dressing for the application on the mucous membrane. Combinations of three biocompatible and biodegradable polymers were used to prepare the films. The obtained samples were characterized by assessing their water loss after drying, swelling ability, hygroscopicity and tensile strength. It was shown that the mixture of HPMC and gellan gum or gelatin could be used to prepare transparent, flexible polymer films with chlorhexidine. All tested films showed high hygroscopicity and swelling ability. However, it was observed that the composition containing gellan gum was more suitable for obtaining films with prolonged stay at the site of administration, which predisposes it to the role of a local dressing.
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  • 文章类型: Randomized Controlled Trial
    背景和目的:干眼症(DED)影响全球5-50%的人口,并深刻影响日常生活活动。本研究比较了疗效,耐受性,含有脂质和羟丙甲纤维素(HPMC)的新型Respilac人工泪液与广泛使用的Nextal人工泪液的安全性,也是基于HPMC的,用于治疗隐形眼镜(CL)配戴者的中度DED。材料与方法:在前瞻性中,单中心,随机调查,30名年龄≥18岁的患者,诊断为中度DED,佩戴CL的患者被随机分配到Respilac组(n=15)或Nextal组(n=15)。患者每天三次在双眼中自我给药一滴Respilac或Nextal,共21天。终点的变化(视觉模拟评分(VAS)对眼睛耐受性的评分,干眼症状评估(SANDE)评分,非侵入性首次分手时间(NIF-BUT)结果,撕裂分析值,介体图结果,和CL耐受性结果进行了评估,比较治疗组和时间点评估。不良事件(AE)也被记录和评估。结果:两组VAS评分均随时间下降(p<0.001),它们之间没有统计学上的显著差异(p=0.13)。从筛查到治疗结束也检测到了改善,SANDE的严重程度和频率评分(p<0.001)和撕裂分析结果(p<0.001)表明了这一点,而Nextal和Respilac臂之间没有观察到差异。NIF-但是,介体图,和CL耐受性值显示受治疗和时间的影响不显著。在该研究队列中未检测到AE。结论:Respilac被证实是有效的,安全,和良好的耐受性。基于脂素的眼用溶液显示不劣于目前使用的Nextal,然而,显示DED症状的改善。在现有文献中,我们的研究是首次报道含MPC+HPMC的滴眼液是治疗隐形眼镜配戴者中度干眼病和预防干燥损害的有效选择之一.
    Background and Objectives: Dry eye disease (DED) affects 5-50% of the global population and deeply influences everyday life activities. This study compared the efficacy, tolerability, and safety of novel Respilac artificial tears containing lipidure and hypromellose (HPMC) with the widely used Nextal artificial tears, which are also HPMC-based, for the treatment of moderate DED in contact lenses (CL) wearers. Materials and Methods: In a prospective, single-center, randomized investigation, 30 patients aged ≥18 years, diagnosed with moderate DED, and wearing CL were randomly assigned to the Respilac (n = 15) or Nextal group (n = 15). Patients self-administrated one drop of Respilac or Nextal in both eyes three times daily for 21 days. Changes in the endpoint (visual analogue scale (VAS) score for ocular tolerability, symptom assessment in dry eye (SANDE) score, non-invasive first break-up time (NIF-BUT) results, tear analysis value, meibography results, and CL tolerability results were assessed, comparing treatment groups and time-point evaluations. Adverse events (AEs) were also recorded and evaluated. Results: VAS scores decreased with time (p < 0.001) in both groups, showing no statistically significant difference among them (p = 0.13). Improvements were also detected from screening to end-of-treatment, which were indicated by the SANDE scores for severity and frequency (p < 0.001) and by tear analysis results (p < 0.001) with no observed difference between the Nextal and Respilac arms. NIF-BUT, meibography, and CL tolerability values were shown to be non-significantly affected by treatment and time. There were no AEs detected in this study cohort. Conclusions: Respilac was confirmed to be effective, safe, and well-tolerated. Lipidure-based ophthalmic solution was shown not to be inferior to the currently used Nextal, however, showing improvements in DED symptoms. Within the existing literature, our study is one of the first to report that MPC plus HPMC-containing eye drops are an effective option for the treatment of moderate dry eye disease and desiccation damage prevention in contact lens wearers.
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  • 文章类型: Journal Article
    从产品品牌和假冒的角度来看,制药公司生产的片剂和胶囊的颜色很重要。根据一些研究,在储存过程中,光线可以改变平板电脑的颜色。在这项研究中,包含苯磺酸氨氯地平(AB)的片剂,一种众所周知的光敏药物,用常用的涂层材料涂覆并暴露于光。与没有暴露在光线下的药片相比,暴露在光线下的颜色会随着时间的推移而改变。事实上,在暴露于光线的片剂中观察到更快、更明显的颜色变化;然而,这些片剂中AB的量没有显著减少.改变涂层材料及其量以澄清颜色变化中涉及的材料。根据结果,二氧化钛和羟丙甲纤维素可能参与颜色变化过程。因为二氧化钛是一种光催化剂,它可以诱导或促进羟丙甲纤维素在光照下的化学变化。总的来说,在选择包衣聚合物时应该小心,因为二氧化钛可以促进包衣的光降解,同时保护片剂的活性成分不受光照。
    The color of the tablets and capsules produced by pharmaceutical companies is important from the perspectives of product branding and counterfeiting. According to some studies, light can change tablet color during storage. In this study, tablets comprising amlodipine besylate (AB), a well-known light-sensitive drug, were coated with commonly used coating materials and exposed to light. Compared to the tablets that were not exposed to light, the color of those exposed to light changed over time. In fact, a faster and more pronounced color change was observed in the tablets exposed to light; however, the amount of AB did not decrease significantly in these tablets. The coating materials and their amounts were varied to clarify the materials involved in the color change. Based on the results, titanium dioxide and hypromellose may be involved in the color change process. As titanium dioxide is a photocatalyst, it may induce or promote chemical changes in hypromellose upon light irradiation. Overall, care should be exercised during selection of the coating polymer because titanium dioxide may promote photodegradation of the coatings while protecting the tablet\'s active ingredient from light.
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  • 文章类型: Journal Article
    羟丙基甲基纤维素乙酰琥珀酸酯(HPMCAS)被广泛用作药物赋形剂,详细了解其可调结构对配方设计很重要。HPMCAS的固态13CNMR光谱中最近报道的几个峰分配已使用定量光谱中的峰积分进行了校正,光谱编辑,基于溶液核磁共振的经验化学位移预测,和类似于反卷积的全光谱模拟。与纤维素不同,84ppm处的强峰必须分配给C2和C3甲基醚,而不是常规的C4纤维素。建议将<65ppm的信号分配给OCH站点,包括纤维素的C5,无法确认。CH2光谱编辑显示两个分辨的OCH2带,在>69ppm时,来自C6的O-CH2醚的强度更大,而来自其酯和可能残留的CH2-OH基团的较小,63ppm左右。乙酰分辨信号的强烈强度,琥珀酰,和羟丙基取代基表示HPMCAS中>85%的OH基团的取代。定量三个不同等级的HPMCAS中的侧组浓度。
    Hydroxypropyl methylcellulose acetyl succinate (HPMCAS) is widely used as a pharmaceutical excipient, making a detailed understanding of its tunable structure important for formulation design. Several recently reported peak assignments in the solid-state 13 C NMR spectrum of HPMCAS have been corrected here using peak integrals in quantitative spectra, spectral editing, empirical chemical-shift predictions based on solution NMR, and full spectrum simulation analogous to deconvolution. Unlike in cellulose, the strong peak at 84 ppm must be assigned to C2 and C3 methyl ethers, instead of regular C4 of cellulose. The proposed assignment of signals at <65 ppm to OCH sites, including C5 of cellulose, could not be confirmed. CH2 spectral editing showed two resolved OCH2 bands, a more intense one from O-CH2 ethers of C6 at >69 ppm and a smaller one from its esters and possibly residual CH2 -OH groups, near 63 ppm. The strong intensities of resolved signals of acetyl, succinoyl, and oxypropyl substituents indicated the substitution of >85% of the OH groups in HPMCAS. The side-group concentrations in three different grades of HPMCAS were quantified.
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  • 文章类型: Journal Article
    羟丙甲纤维素,在制药工业中广泛使用的聚合物,有几个等级,取决于甲氧基和羟丙基的取代百分比和分子量,并以各种功能形式(例如,适用于直接压缩压片)。这些差异会影响它们的物理机械性能,因此,这项研究旨在表征来自四个不同供应商的HPMCK100M聚合物等级的粒径和机械性能。使用扫描电子显微镜(SEM)和光学显微镜自动图像分析颗粒表征分析了八种聚合物(CR和DC等级),以检查粉末的颗粒形态和粒径分布。堆积密度,振实密度,和材料的真实密度也进行了分析。使用剪切池测试仪测定流量。在五种不同的压缩力下制备平面聚合物压块,并且评价压块的机械性能以给出粉末在特定压力下形成具有期望强度的片剂的能力的指示。结果表明,与DC级HPMCK100M聚合物相比,CR级聚合物显示出更小的粒度和更好的机械性能。DC等级,然而,具有比CR同行更好的流动性能。结果还表明,尽管取代水平相似,但来自不同供应商的一些聚合物之间存在一些相似性和差异。提醒用户,当需要替代时,应该给予关注和考虑。
    Hypromellose, a widely used polymer in the pharmaceutical industry, is available in several grades, depending on the percentage of substitution of the methoxyl and hydroxypropyl groups and molecular weight, and in various functional forms (e.g., suitable for direct compression tableting). These differences can affect their physicomechanical properties, and so this study aims to characterise the particle size and mechanical properties of HPMC K100M polymer grades from four different vendors. Eight polymers (CR and DC grades) were analysed using scanning electron microscopy (SEM) and light microscopy automated image analysis particle characterisation to examine the powder\'s particle morphology and particle size distribution. Bulk density, tapped density, and true density of the materials were also analysed. Flow was determined using a shear cell tester. Flat-faced polymer compacts were made at five different compression forces and the mechanical properties of the compacts were evaluated to give an indication of the powder\'s capacity to form a tablet with desirable strength under specific pressures. The results indicated that the CR grades of the polymers displayed a smaller particle size and better mechanical properties compared to the DC grade HPMC K100M polymers. The DC grades, however, had better flow properties than their CR counterparts. The results also suggested some similarities and differences between some of the polymers from the different vendors despite the similarity in substitution level, reminding the user that care and consideration should be given when substitution is required.
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