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Formulation and characterization of palm oil esters based nano- cream for topical delivery of piroxicam 局部递送吡罗西康用棕榈油酯基纳米乳膏的配方及表征
Pub Date : 2010-12-03 DOI: 10.5138/IJDD.2010.0975.0215.02040
M. Abdulkarim, G. Z. Abdullah, Mallikarjun Chitneni, E. S. Mahdi, M. Yam, A. Faisal, I. M. Salman, O. Ameer, M. Sahib, Munavvar Zubaid Abdulsattar, M. Basri, A. M. Noor
Palm oil esters are high molecular weight esters oil that has been newly synthesized by University Putra Malaysia researchers. It has received a lot of attention for its pharmaceutical and chemical application. Piroxicam is a nonsteroidal anti-inflammatory drug with analgesic and antipyretic activity. It has low solubility in water as well as in oil with Log P value of 1.8. Generally, drugs with Log P value of more than 0.5 are needed to be formulated into a modified dosage form. One of these formulations is nano sized cream. Hence, the ability of formulating of these tricky drugs into dispersed system is questionable. The aim of this study is to investigate the ability of palm oil esters to be the oil phase for formulation of piroxicam into O/W nano-cream. Three points were selected from prepared pseudoternary diagram of palm oil esters and different Tween and Span mixtures. Piroxicam solubility and partition coefficient in oil and external phase was detected. Rheological properties, droplet size, structural properties and zeta potential of the dispersion system containing piroxicam were measured. O/W cream was formed with droplet size measurement by TEM of less than 100 nm. It could be concluded that palm oil esters is suitable oil for the formulation of suitable nano-cream containing piroxicam. Keywords: Palm oil esters; Piroxicam Solubility; partition coefficient; Rheology; Surface activity.
棕榈油酯是马来西亚博特拉大学研究人员新合成的高分子量酯油。它在制药和化工方面的应用受到了广泛的关注。吡罗昔康是一种非甾体抗炎药,具有镇痛和解热作用。在水和油中的溶解度较低,logp值为1.8。一般情况下,Log P值大于0.5的药物需要配制成改性剂型。其中一种配方是纳米级乳霜。因此,将这些棘手的药物配制成分散系统的能力是值得怀疑的。本研究的目的是研究棕榈油酯作为吡罗西康O/W纳米乳膏的油相的能力。从制备的棕榈油酯和不同的Tween和Span混合物的伪三元图中选取了三个点。测定吡罗昔康在油和外相中的溶解度和分配系数。测定了吡罗昔康分散体系的流变性能、液滴大小、结构性质和zeta电位。用透射电镜测定的液滴尺寸小于100 nm,形成了O/W乳膏。结果表明,棕榈油酯是制备吡罗昔康纳米乳膏的理想油脂。关键词:棕榈油酯类;吡罗昔康溶解度;分配系数;流变学;表面活性。
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引用次数: 12
Film forming gel for treatment of oral mucositis: In vitro studies 成膜凝胶治疗口腔黏膜炎:体外研究
Pub Date : 2010-12-03 DOI: 10.5138/IJDD.2010.0975.0215.02043
M. A. Attia, Heba Y. El Badawy
Oral mucositis is one of the main complications of non-surgical cancer treatments. The present work focuses on the treatment or reduction of oral mucositis by using combined mechanism by formation of physical barrier by forming a film to cover the oral ulcer and use of therapeutic agents, such as diclofenac sodium and ofloxacin separately or in combination. The selected polymers for film forming gel formulations are Hydroxypropylcellulose (HPC), hydroxypropyl methylcellulose (HPMC), sodium carboxymethylcellulose (Na CMC) and carbopol 940 (CP). The residence time in simulated buccal saliva was between 5.5 to 6 hours for all formulations. The in-vitro release data of the investigated drugs from the prepared formulations followed zero-order and diffusion mechanism. The permeability studies data revealed that diclofenac sodium showed higher permeability from Na CMC/CP (2:0.3%) than from HPMC 4%, while in case of ofloxacin higher permeability was shown from Na CMC/CP (2:0.3%) than from HPMC/HPC (2:3%). The permeation parameters for diclofenac sodium and ofloxacin in their combination do not depend on either viscosity or pH, they depend on the type of polymers used. Keywords: Mucositis; Film-forming gel; Rheology; In vitro studies.
口腔黏膜炎是非手术治疗癌症的主要并发症之一。本研究的重点是通过在口腔溃疡处形成一层物理屏障,并单独或联合使用双氯芬酸钠和氧氟沙星等治疗剂,利用联合机制治疗或减轻口腔粘膜炎。成膜凝胶配方选用的聚合物有羟丙基纤维素(HPC)、羟丙基甲基纤维素(HPMC)、羧甲基纤维素钠(Na CMC)和卡波波尔940 (CP)。所有制剂在模拟口腔唾液中的停留时间在5.5至6小时之间。在所制备的制剂中,所研究药物的体外释放数据符合零级扩散机制。渗透性研究结果表明,双氯芬酸钠对Na CMC/CP的渗透性(2:0.3%)高于HPMC/ CP(2:3%),而氧氟沙星对Na CMC/CP的渗透性(2:0.3%)高于HPMC/HPC(2:3%)。双氯芬酸钠和氧氟沙星组合的渗透参数不取决于粘度或pH值,而是取决于所使用的聚合物类型。关键词:粘膜炎;成膜凝胶;流变学;体外研究。
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引用次数: 10
Multiple unite sustained released floating of sodium diclofenac: Formulation and evaluation using factorial design 双氯芬酸钠多单位缓释浮剂:配方及因子设计评价
Pub Date : 2010-12-03 DOI: 10.5138/IJDD.2010.0975.0215.02047
B. Zadeh, Taybeh Jamei, F. Rahim, Mohammd Reza Abbaspur
The aim of this study was prepare and evaluate floating granules of sodium diclofenac with lipid excipient for prolonged gastric residence and reduced dose regimen. Floating granules prepared by extruder-spheronization technique. Compritol and gelucire as lipid excipient, HPMC as retardant and tween 80 as emulsifier were used. The effect of drug/lipid, drug/HPMC, drug amount, percentage of tween and type of lipid on floating ability, morphology and dissolution parameters were evaluated by factorial design. Results showed floating ability of granules was influenced by proportion of drug/lipid, drug/HPMC and percentage of tween. Floating property of Compritol was more than gelucire and provided good floating particles. Compritol granules provided suitable sustained release pattern in the manner that increase in D/L reduced D8 and MDT and increase in %T increased MDT. Higuchi model was the best fitted for dissolution data of granules prepared by Compritol and gelucire. In conclusion, Compritol provided more suitable floating ability and sustained release property. Keywords: Sodium diclofenac; Floating granules; Gastric residence time; Extruder-spheronization
本研究的目的是制备双氯芬酸钠脂质赋形剂漂浮颗粒,并对其减给药和延长胃停留时间的效果进行评价。用挤出滚圆技术制备漂浮颗粒。以合成醇和甘油为脂质赋形剂,HPMC为阻燃剂,吐温80为乳化剂。采用因子设计评价药物/脂质、药物/HPMC、药量、间质百分比和脂质类型对漂浮能力、形态和溶出参数的影响。结果表明,药物/脂质比、药物/HPMC和间质比例影响颗粒的漂浮能力。舒普利醇的漂浮性能优于凝胶,提供了良好的悬浮颗粒。舒普利醇颗粒剂具有较好的缓释模式,D/L增加可降低D8和MDT, %T增加可增加MDT。通口模型最适合于孔普醇和凝胶制备颗粒的溶出度数据。综上所述,康普利醇具有较好的漂浮性和缓释性。关键词:双氯芬酸钠;漂浮的颗粒;胃停留时间;Extruder-spheronization
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引用次数: 1
Stability studies of nano-cream containing piroxicam 吡罗昔康纳米乳膏的稳定性研究
Pub Date : 2010-12-03 DOI: 10.5138/IJDD.2010.0975.0215.02045
M. Abdulkarim, G. Z. Abdullah, Mallikarjun Chitneni, E. S. Mahdi, M. Yam, A. Faisal, I. M. Salman, O. Ameer, M. Sahib, Munavvar Zubaid Abdulsattar, M. Basri, A. M. Noor
The aim of this study is to study the stability of the nano-cream formula containing the newly synthesized palm oil esters when stored for reasonable storage duration. The prepared 0.5% piroxicam nano-cream formula contained phosphate buffer as external phase, palm oil esters as the oil phase and a combination of (80:20) of Tween 80 and Span 20 as emulsifier at a ratio of 37:25:38, respectively. Piroxicam is a hydro-lipophobic drug. Stability on storage is an important aspect which ensures the dosage form can exert the effects it is supposed to exert for the duration of storage. Droplets size, electrical conductivity, drug content, pH and rheological parameters are the parameters that have been assessed under different temperature to evaluate the stability of nano-cream preparation. Thus, experiments which measure the above parameters were conducted at storage temperatures of 4, 25 and 40οC.The data obtained from the stability study conducted on nano-cream formula showed that this formulation was stable for the whole 3 months period of the study when stored at tested several temperatures. Keywords: Palm oil esters; Nonionic surfactant; Piroxicam; Nano-cream
本研究的目的是研究新合成的棕榈油酯纳米乳膏配方在合理的贮存时间内的稳定性。制备的0.5%吡罗昔康纳米乳膏配方以磷酸缓冲液为外相,棕榈油酯为油相,Tween 80和Span 20以(80:20)的比例(37:25:38)为乳化剂。吡罗昔康是一种疏水脂药。贮存稳定性是保证制剂在贮存期间能发挥其应有作用的一个重要方面。以液滴大小、电导率、药物含量、pH值和流变性参数作为不同温度下评价纳米乳膏制备稳定性的参数。因此,测量上述参数的实验是在4、25和40οC的储存温度下进行的。对纳米霜配方进行的稳定性研究数据表明,该配方在测试的几种温度下储存,在整个3个月的研究期间都是稳定的。关键词:棕榈油酯类;非离子表面活性剂;吡罗昔康;Nano-cream
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引用次数: 12
Novel thermosensitive poly (N-isopropylacrylamide-co-vinylpyrrolidone-co-methacrylic acid) nanosystems for delivery of natural products 新型热敏聚(n -异丙基丙烯酰胺-共乙烯基吡咯烷酮-共甲基丙烯酸)纳米体系用于天然产物的递送
Pub Date : 2010-12-03 DOI: 10.5138/IJDD.2010.0975.0215.02039
O. Mashinchian, R. Salehi, G. Dehghan, Ayoub Aganejad, S. Davaran, Y. Omidi
The purpose of this research was to synthesize polymer based smart nanosystems for delivery of important bioactive natural products such as sesquiterpene coumarin derivatives of ferula szowitsiana, farnesiferol C as a potent anticancer. To this aim, polymeric micelles were prepared using Nisopropylacrylamide (NIPAAM), vinyl pyrrolidone (VP) and methacrylate (MAA) as monomers which were cross-linked with N, N-methylene bisacrylamide (MBA). The molar ratio of the PNIPAAm: VP: MAA group was 75.7:9.5:14.8. These micelles were further characterized upon their physicochemical properties using particle size analyzer, FT-IR, H-/C-NMR, HPLC. Particle size analyzer resulted in ~500 nm micelles with ~95% drug entrapments. Drug release from the polymeric micelles after 300 hours at 37°C and 40°C were 60 and 98 %, respectively. Upon these findings, it is proposed that the P (N-isopropylacrylamide-co-Methacrylic acid-coVinylpyrrolidone) micelles may be considered as thermosensitive delivery nanosystem.
本研究的目的是合成基于聚合物的智能纳米系统,用于递送重要的生物活性天然产物,如阿魏的倍半萜香豆素衍生物,作为一种有效的抗癌药物。为此,以异丙基丙烯酰胺(NIPAAM)、乙烯基吡啶酮(VP)和甲基丙烯酸酯(MAA)为单体,与N, N-亚甲基双丙烯酰胺(MBA)交联制备了聚合物胶束。PNIPAAm: VP: MAA的摩尔比为75.7:9.5:14.8。采用粒度分析仪、FT-IR、H-/C-NMR、HPLC等对胶束进行了理化性质表征。粒径分析仪测定的胶束为~500 nm,药物包封率为~95%。37℃和40℃作用300小时后,聚合物胶束的药物释放率分别为60%和98%。在此基础上,提出了P (n -异丙基丙烯酰胺-共甲基丙烯酸-聚乙烯基吡咯烷酮)胶束可以被认为是热敏递送纳米体系。
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引用次数: 16
Effect of two different superdisintegrants on combinaion dispersible tablets of isoniazid and rifampicin for oral treatment of tuberculosis 两种超崩解剂对异烟肼与利福平联合分散片口服治疗肺结核的影响
Pub Date : 2010-12-03 DOI: 10.5138/IJDD.2010.0975.0215.02044
V. Shukla, F. Manvi
Oral route of administration have wide acceptance up to 50-60% to total drug forms. Fast disintegrating drug delivery system has number of advantage such as faster onset of action, attractive elegance, ease of administration. In this study, an attempt has been made to study direct compression method, for formulation of fast disintegrating tablets of Isoniazid and Rifampicin, an anti-tubercular drug in view of enhancing bioavailability. These formulations have sufficient hardness and can be manufactured by commonly used equipment. Prior to formulation the pre-compression parameters were characterized for flow properties and prepared formulations were evaluated for physico-chemical parameters, X-ray powder crystallography, SEM and in-vivo bioavailability. All four formulations possessed good disintegration properties with total disintegration time of 25 to 40 seconds. The effects of different superdisintegrants and process variables on drug release profile and disintegration property were evaluated and results revealed the better drug release with different superdisintegrants such as Ac-di sol and Polyplastadone XL. All formulations are rapidly disintegrated in oral cavity as well as all formulations possess good anti-tubercular properties. SEM Showed the mechanical strength of the formulations affected the morphological changes after compression. Hence, it is evident from this study that fast dispersible tablets could be a promising delivery system for Isoniazid, Rifampicin and their combination with good mouth feel and improved drug availability with better patient compliance. Keywords: Isoniazid; Rifampicin; Superdisintegrants; Direct compression method; Bioavailability.
口服给药途径被广泛接受,占总药物形式的50-60%。快速崩解给药系统具有起效快、美观大方、给药方便等优点。为了提高抗结核药物异烟肼利福平快速崩解片的生物利用度,本研究尝试采用直接压缩法制备异烟肼利福平快速崩解片。这些配方具有足够的硬度,可以用常用的设备制造。在配方前,对预压缩参数进行流动特性表征,并对制备的配方进行理化参数、x射线粉末晶体学、扫描电镜和体内生物利用度评估。4种配方均具有良好的崩解性能,总崩解时间为25 ~ 40秒。考察了不同的超崩解剂和工艺参数对药物释放曲线和崩解性能的影响,结果表明不同的超崩解剂如Ac-di sol和Polyplastadone XL对药物释放效果更好。所有制剂在口腔内迅速崩解,并具有良好的抗结核性能。扫描电镜显示,配方的机械强度影响压缩后的形态变化。因此,从本研究中可以明显看出,快速分散片可能是异烟肼、利福平的一种很有前途的给药系统,它们的联合使用具有良好的口腔感觉和改善的药物可用性,并且患者的依从性更好。关键词:异烟肼;利福平;Superdisintegrants;直接压缩法;生物利用度。
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引用次数: 7
Development and characterization of gastroretentive mucoadhesive tablets of venlafaxine hydrochloride 盐酸文拉法辛胃保留黏粘片的研制与表征
Pub Date : 2010-12-03 DOI: 10.5138/IJDD.2010.0975.0215.02041
S. U. Zate, P. Kothawade, Mohan N. Rathi, Mohan H. Shitole, Chetan Yewale, Vinayak S. Gawande
The present study was undertaken with an aim to formulation development and evaluation of gastroretentive mucoadhesive sustained release tablet of Venlafaxine hydrochloride which releases the drug in a sustained manner over a period of 12 hours, by using Carbopol 971P in combination with eudragit RS-PO and ethyl cellulose as a mucoadhesive and release retardant respectively. Preformulation study was done initially and results directed for the further course of formulation. Based on Preformulation studies different batches of Venlafaxine hydrochloride were prepared using Carbopol 971P, Eudragit RS-PO and ethyl cellulose chosen for their different hydrophilic properties to calculate the sustained release properties. Sustained release tablets were prepared by direct compression and were evaluated for bioadhesion time, swelling index and matrix erosion, and in vitro drug release. The tablets of batch F3 and F6 had high swelling behaviors but release of drug is very less. And batch F2 having considerable swelling index and in vitro drug release (99.85%). Batch F2 can be taken as an ideal or optimized formulation of sustained release tablets for 12 hour release as it fulfills all the requirements for sustained release tablet. From the discussion it is concluded that use of carbopol as a release retardant and adhesive polymer is very effective; and also it act as strong release retardant in combination with hydrophobic polymers. Keywords: Gastroretentive; Mucoadhesive; Venlafaxine hydrochloride; Tablet.
本研究以卡波波尔971P与乌龙油RS-PO和乙基纤维素分别作为黏附剂和缓释剂,对盐酸文拉法辛胃保留黏附缓释片进行配方开发和评价,该缓释片的缓释时间为12小时。初步进行了制剂前研究,其结果将指导进一步的制剂过程。在预处方研究的基础上,选择亲水性不同的卡波波尔971P、乌龙木RS-PO和乙基纤维素制备不同批号的盐酸文拉法辛,计算其缓释性能。采用直接压片法制备缓释片,并对其生物黏附时间、溶胀指数、基质侵蚀、体外释放度进行评价。F3、F6批片剂具有较高的溶胀行为,但释药量极少。F2批具有较好的溶胀指数和体外释药率(99.85%)。F2批符合缓释片的各项要求,可作为12小时缓释片的理想或优化制剂。结果表明,卡波波尔是一种有效的缓粘剂;与疏水聚合物结合,也可作为强释放阻燃剂。关键词:Gastroretentive;Mucoadhesive;盐酸文拉法辛;平板电脑。
{"title":"Development and characterization of gastroretentive mucoadhesive tablets of venlafaxine hydrochloride","authors":"S. U. Zate, P. Kothawade, Mohan N. Rathi, Mohan H. Shitole, Chetan Yewale, Vinayak S. Gawande","doi":"10.5138/IJDD.2010.0975.0215.02041","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02041","url":null,"abstract":"The present study was undertaken with an aim to formulation development and evaluation of gastroretentive mucoadhesive sustained release tablet of Venlafaxine hydrochloride which releases the drug in a sustained manner over a period of 12 hours, by using Carbopol 971P in combination with eudragit RS-PO and ethyl cellulose as a mucoadhesive and release retardant respectively. Preformulation study was done initially and results directed for the further course of formulation. Based on Preformulation studies different batches of Venlafaxine hydrochloride were prepared using Carbopol 971P, Eudragit RS-PO and ethyl cellulose chosen for their different hydrophilic properties to calculate the sustained release properties. Sustained release tablets were prepared by direct compression and were evaluated for bioadhesion time, swelling index and matrix erosion, and in vitro drug release. The tablets of batch F3 and F6 had high swelling behaviors but release of drug is very less. And batch F2 having considerable swelling index and in vitro drug release (99.85%). Batch F2 can be taken as an ideal or optimized formulation of sustained release tablets for 12 hour release as it fulfills all the requirements for sustained release tablet. From the discussion it is concluded that use of carbopol as a release retardant and adhesive polymer is very effective; and also it act as strong release retardant in combination with hydrophobic polymers. Keywords: Gastroretentive; Mucoadhesive; Venlafaxine hydrochloride; Tablet.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88749633","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 8
Biochemical evaluation of low dose methyl 2-benzimidazole carbamate fungicide on male albino rats 低剂量2-苯并咪唑氨基甲酸甲酯杀菌剂对雄性白化大鼠的生化评价
Pub Date : 2010-12-03 DOI: 10.5138/IJDD.2010.0975.0215.02048
V. Muthuviveganandavel, P. Muthuraman, S. Muthu, K. Srikumar
Methyl 2-benzimidazole carbamate (carbendazim) is one of the synthetic fungicides that controlled organisms that caused plant diseases of different types. It is widely used as a preservative in leather, paint, textile, fruits and papermaking industry. It is also used as an anticancer drug in chemical medicine. In the present study low concentrations of carbendazim was administered at 5, 10, 25 and 50mM doses intradermally to male albino rats. At the end of 6 hr, 12hr and 24hr duration, blood samples were collected from the animal for the analysis of biochemical and haematological parameters. Carbendazim caused an increase of cholesterol, uric acid, glucose and creatinine while serum phosphorous content was decreased. However, mean hemoglobin, WBC, E, and platelet counts increased and total RBC, N and L counts decreased. These results indicated that low dose level carbendazim contributed to toxicological effects in the rat tissues. Keywords: Methyl 2-benzimidazole carbamate; Fungicide; Rat tissues
2-苯并咪唑氨基甲酸甲酯(carbendazim)是一种合成杀菌剂,用于防治引起不同类型植物病害的生物。广泛应用于皮革、油漆、纺织、水果、造纸等行业。在化学医学中也被用作抗癌药物。在本研究中,低浓度多菌灵分别以5、10、25和50mM的剂量皮下注射给雄性白化大鼠。实验结束后,分别于6小时、12小时和24小时采集动物血液进行生化和血液学参数分析。多菌灵引起胆固醇、尿酸、葡萄糖和肌酐升高,血清磷含量降低。然而,平均血红蛋白、白细胞、E和血小板计数增加,总红细胞、N和L计数下降。结果表明,低剂量多菌灵对大鼠组织有一定的毒理学作用。关键词:2-苯并咪唑氨基甲酸甲酯;杀菌剂;大鼠组织
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引用次数: 4
Spectrophotometric method development and validation of itopride hydrochloride in bulk and dosage form 盐酸依托必利原料药和剂型分光光度法的建立与验证
Pub Date : 2010-12-03 DOI: 10.5138/IJDD.2010.0975.0215.02046
S. U. Zate, P. Kothawade, Jitendra W Gajbe, Anantwar S. Pramod, S. Boraste
A simple, precise and economical spectrophotometric method for the estimation of Itopride hydrochloride in pharmaceutical bulk and tablet dosage form was developed and validated. Identification was carried out using a UV-visible double beam spectrophotometer detector with working wavelength at 258nm in 0.1N HCl medium. The method was validated with respect to its specificity, linearity range, accuracy, and precision in analytical media. Itopride hydrochloride show the maximum absorbance (λmax) at 258 nm, Regression analysis showed good correlation in the concentration range 5-100 mcg/ml and 96.80 to 106.84% recovery with relative standard deviation 0.293 to 3.98%. Statistical treatment of data reflects that the proposed method is precise, accurate and easily applicable for determination of Itopride hydrochloride in bulk and pharmaceutical preparation. Keywords: Spectrophotometric; Itopride hydrochloride; Validation.
建立了一种简便、准确、经济的分光光度法测定原料药和片剂中盐酸依托普利的含量。在0.1N HCl介质中,使用工作波长为258nm的紫外-可见双光束分光光度计进行鉴定。该方法在分析介质中的特异性、线性范围、准确度和精密度进行了验证。盐酸依托必利在258 nm处的吸光度最大(λmax),在5 ~ 100 mcg/ml浓度范围内相关性良好,回收率为96.80 ~ 106.84%,相对标准偏差为0.293 ~ 3.98%。对数据的统计处理表明,该方法精密度高,准确度高,适用于原料药和制剂中盐酸依托必利的含量测定。关键词:光谱光度测量的;Itopride盐酸盐;验证。
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引用次数: 16
Spherically agglomerated solid dispersions of valsartan to improve solubility, dissolution rate and micromeritic properties 球形凝聚的缬沙坦固体分散体,以提高溶解度,溶出率和微晶性质
Pub Date : 2010-12-03 DOI: 10.5138/IJDD.2010.0975.0215.02042
A. Tapas, P. Kawtikwar, D. Sakarkar
The objective of the present work was to enhance the solubility and dissolution rate of valsartan (VAL) a poorly water soluble antihypertensive, by spherically agglomerated solid dispersions using methanol, water and dichloromethane as good solvent, poor solvent and bridging liquid, respectively. The hydrophilic polymers like polyvinyl pyrrolidone, Hydroxypropyl β-cyclodextrin, Hydroxypropyl methylcellulose were used in agglomeration process. The pure drug (VAL) and its agglomerates with different polymers were characterize by differential scanning calorimetry (DSC), X-ray diffraction (XRD), IR spectroscopic studies and scanning electron microscopy (SEM). The DSC results indicated that decrease in melting enthalpy related to disorder in the crystalline content. XRD studies also showed changes in crystallanity, IR spectroscopy revealed that there were no chemical changes in the recrystallized agglomerates. The spherically agglomerated solid dispersions with different polymers exhibited marked increase in solubility, dissolution rate and micromeritic properties (bulk density, flow property, compactability) compared with VAL. The SEM studies showed that the agglomerates posseeses a good spherical shape. Keywords: Valsartan; Spherical agglomeration; Solid dispersion; Solubility; Dissolution rate; Micromeritic properties.
以甲醇、水、二氯甲烷为好溶剂、差溶剂和桥接液,制备球形固体分散体,提高缬沙坦(VAL)的溶解度和溶出率。聚氯乙烯吡咯烷酮、羟丙基β-环糊精、羟丙基甲基纤维素等亲水性聚合物用于团聚过程。采用差示扫描量热法(DSC)、x射线衍射(XRD)、红外光谱(IR)和扫描电镜(SEM)对纯药物(VAL)及其不同聚合物的团聚体进行了表征。DSC结果表明,熔融焓的降低与晶体含量的无序有关。XRD研究也显示了结晶度的变化,IR光谱显示再结晶团块没有化学变化。与VAL相比,不同聚合物的球形团聚体的溶解度、溶解速率和微晶性能(体积密度、流动性能、压实性)均有显著提高,SEM研究表明,团聚体具有良好的球形特征。关键词:缬沙坦;球形聚集;固体分散;溶解度;溶解率;微晶粒状属性。
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引用次数: 25
期刊
International Journal of Drug Delivery
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