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Formulation and Evaluation of Floating Microspheres for an Antihypertensive drug Telmisartan 降压药替米沙坦漂浮微球的研制及评价
Pub Date : 2022-11-12 DOI: 10.52711/0975-4377.2022.00046
Shikha Baghel Chauhan, Sakshi Nainwani
Telmisartan is one of the best options either in combination or alone, to treat hypertension. telmisartan belongs to class II antagonist angiotensin converting enzyme inhibitor. One of the main causes of hypertension is vasoconstriction of blood vessels hence increasing blood pressure which can be controlled by drugs that have vasoconstriction property and telmisartan is one of them, and it also relaxes the blood vessels. The dosage form opted here is floating microspheres as it can provide sustain release of drug over long period of time. Floating microspheres have a tendency to float over gastric fluid hence increasing gastric retention time. These are preferred over conventional form as they provide advantage of reducing gastric irritation, lesser dosing frequency will be required as it provide slow continuous release for prolong period of time. The present research aims to formulate telmisartan floating microspheres and its evaluation. The technique used is solvent evaporation method by using magnetic stirrer. Already formulated telmisartan microspheres have lower bioavailability, drug entrapment and lower release kinetics so our main aim is to formulate such a preparation which have greater bioavailability, drug entrapment and greater kinetic release, and to formulate such a formulation we have opted using variant ratios of polymer Eudragit RS 100, Ethyl Cellulose with constant dose of drug. After formulation, various characterization is done that include micromeritics properties, floating efficiency, solubility, drug entrapment efficiency along with yield and release kinetics. The study revealed that, using a more than one polymer in a different ratio have an impact on every parameter of microspheres.
替米沙坦是治疗高血压的最佳选择之一,无论是联合用药还是单独用药。替米沙坦属于II类拮抗剂血管紧张素转换酶抑制剂。高血压的主要原因之一是血管收缩,因此血压升高可以通过具有血管收缩特性的药物来控制替米沙坦就是其中之一,它还可以放松血管。这里选择的剂型是漂浮微球,因为它可以在很长一段时间内持续释放药物。漂浮微球有漂浮在胃液上的倾向,因此增加了胃潴留时间。这些是优于传统形式,因为它们提供减少胃刺激的优势,较少的给药频率将需要,因为它提供缓慢的持续释放延长的时间。本研究旨在制备替米沙坦漂浮微球并对其进行评价。所采用的工艺是磁力搅拌器溶剂蒸发法。已经配制的替米沙坦微球具有较低的生物利用度、药物夹带和较低的释放动力学,因此我们的主要目标是配制这样一种具有更高生物利用度、药物夹带和更大动力学释放的制剂,为了配制这样的制剂,我们选择使用不同比例的聚合物Eudragit RS 100、乙基纤维素和恒定剂量的药物。配制后,进行各种表征,包括微量物学性质、漂浮效率、溶解度、药物包封效率以及产率和释放动力学。研究表明,以不同比例使用一种以上的聚合物对微球的各个参数都有影响。
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引用次数: 0
Method Development and Validation for the estimation of Amlodipine and Perindopril in Bulk and Pharmaceutical Dosage Form 氨氯地平和培哚普利原料药剂型质量评价方法的建立与验证
Pub Date : 2022-11-12 DOI: 10.52711/0975-4377.2022.00047
M. V. Ramana, V. Sowmya, K. Sangeetha, K. Nagapreethi, M. Mounika, S. Divya, A. Kanakalaxmi
Literature survey reveals that few spectrophotometric, high performance liquid chromatographic (HPLC)and High performance thin layer chromatographic (HPTLC)methods were reported for the estimation of Amlodipine and perindopril in bulk and combined pharmaceutical dosage forms. But there is no any stability indicating high performance liquid chromatography study is reported for amlodipine. So the present study was aimed to development of simple, accurate, rapid and economical HPLC stability indicating assay method were established for the determination of Amlodipine and Peridopril in bulk and tablet dosage form. A High-performance liquid chromatograph WATERS, software: Empower 2,2695 separation module, 996 PDA detector, using Phenomenex Luna C18 (4.6mm×250mm) 5µm or equivalent column, with mobile phase composition of Methanol: Phosphate Buffer pH3.0 (70:30v/v) was used. The flow rate of 1.0ml min-1 and effluent was detected at 230nm. The retention time of Amlodipine and Perindopril was found to be 1.870min and 2.499minutes respectively. Linearity was observed over concentration range of 10-50µg ml-1 for Amlodipine and 16-80µg ml-1 for Perindopril respectively. The accuracy of the proposed method was determined by recovery studies and the Amlodipine was found to be 99.1% and Perindopril was found to be 98.8% respectively. The proposed method is applicable to routine analysis of Amlodipine and Perindopril in bulk and pharmaceutical formulations. The proposed method was validated for various ICH parameters like linearity, limit of detection, limits of quantification, accuracy, precision, range and specificity.
文献调查显示,分光光度法、高效液相色谱法和高效薄层色谱法用于氨氯地平和培哚普利原料药和复方药的含量测定的文献很少。但目前尚无高效液相色谱法研究氨氯地平的稳定性。因此,本研究旨在建立一种简便、准确、快速、经济的高效液相色谱法测定氨氯地平和培立多普利原料药和片剂含量的稳定性指示法。高效液相色谱仪WATERS,软件:Empower 2,2695分离模块,996 PDA检测器,色谱柱为Phenomenex Luna C18 (4.6mm×250mm) 5µm或同等柱,流动相为甲醇:磷酸缓冲液pH3.0 (70:30v/v)。流速1.0ml min-1,在230nm处检测流出物。氨氯地平和培哚普利的滞留时间分别为1.870min和2.499min。氨氯地平和培哚普利分别在10 ~ 50µg ml-1和16 ~ 80µg ml-1浓度范围内呈线性关系。结果表明,氨氯地平的回收率为99.1%,培哚普利的回收率为98.8%。本方法适用于原料药和制剂中氨氯地平和培哚普利的常规分析。该方法对ICH的线性、检出限、定量限、准确度、精密度、范围和特异性等参数进行了验证。
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引用次数: 1
Floating Drug Delivery System: A Novel apporach for Delivery of Drug on Targated Organ 漂浮给药系统:一种靶向器官给药的新方法
Pub Date : 2022-11-12 DOI: 10.52711/0975-4377.2022.00054
Pankaj. P. Sathe, Kedar Bavaskar, Ashish Jain
The goal of this review on floating drug delivery systems (FDDS) was to compile latest data with a particular focus on the main mechanism of flotation for stomach retention. Drug delivery systems that float instantly when they come into contact with gastric fluids are promising approaches for increasing the bioavailability of drugs within absorption window in the stomach or upper small intestine. They are unstable in the intestinal or colonic environment and have low solubility at high pH values. The Current pharmaceutical scenario focuses on the development of sustained drug delivery systems to achieve required therapeutic concentration with less amount of dose. Oral delivery of the drug is the preferable drug delivery system. Because of the ease of administration, patient compliance and formulation flexibility. The ability to delay and control the emptying period of a dosage form in the stomach is an extremely variable process. For dosage forms that stay in the stomach for longer periods of time than standard dosage forms so the gastric transit time is a valuable asset for this system. The goal of this review article is to provide detailed information on the pharmaceutical basis of their design, classification, advantages, in vitro and in vivo evaluation parameters, and applications of floating systems. These systems can help with a variety of issues that arise during the development of a pharmaceutical dosage form, as well as the potential of FDDS in the future. This review article makes an attempt to introduce readers to current developments in floating drug delivery systems.
这篇关于漂浮给药系统(FDDS)的综述的目的是汇编最新的数据,特别关注胃潴留的漂浮主要机制。在胃或上小肠的吸收窗口内提高药物的生物利用度,在与胃液接触时立即漂浮的药物输送系统是很有前途的方法。它们在肠道或结肠环境中不稳定,在高pH值下溶解度低。当前的制药方案侧重于开发持续的药物输送系统,以较少的剂量达到所需的治疗浓度。口服给药是较好的给药系统。因为易于管理,患者的依从性和配方的灵活性。延缓和控制一种剂型在胃中的排空期的能力是一个极其多变的过程。因为剂型在胃中停留的时间比标准剂型长所以胃的传递时间是这个系统的宝贵资产。本文就其设计、分类、优点、体外和体内评价参数及应用等方面的药学基础进行综述。这些系统可以帮助解决药物剂型开发过程中出现的各种问题,以及FDDS在未来的潜力。这篇综述文章试图向读者介绍漂浮给药系统的最新发展。
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引用次数: 0
Formulation and Evaluation of Microcapsules of Aspirin by Coacervation Phase Separation Method 凝聚相分离法制备阿司匹林微胶囊及评价
Pub Date : 2022-11-12 DOI: 10.52711/0975-4377.2022.00042
Priti B. Savant, Shrikrushna A. Shinde, Jayamala S. Barge
Microencapsulation is a process in which tiny particles or droplets are surrounded by a coating to give small capsules, with useful properties. Microcapsule is a small sphere with uniform wall around it. The material inside the microcapsule is referred to as the core, internal phase or fill, whereas the wall sometimes called as shell, coating or membrane. Microencapsulation is a rapidly expanding technology in which very tiny droplets or particles of liquid or solid material are surrounded or coated with a continuous film of polymeric material. Aspirin (Acetylsalicylic acid) is a Non steroidal anti-inflammatory drug. It inhibits platelets aggregation and prolong bleeding time. This research article will emphasize formulation and evaluation of microcapsules of aspirin by coacervation phase separation method. coacervation phase separation techanique have been widely used to incorporate drugs into polymeric microcapsules.
微胶囊化是一种将微小的颗粒或液滴包裹在一层涂层中形成具有有用性能的小胶囊的过程。微胶囊是一种周围有均匀壁的小球体。微胶囊内部的物质被称为核心、内相或填充物,而壁有时被称为外壳、涂层或膜。微胶囊化是一种迅速发展的技术,其中液体或固体材料的非常微小的液滴或颗粒被聚合材料的连续膜包围或包裹。阿司匹林(乙酰水杨酸)是非甾体类抗炎药。它能抑制血小板聚集,延长出血时间。本文将重点研究阿司匹林微胶囊凝聚相分离法的制备及评价。聚敛相分离技术已被广泛应用于将药物整合到聚合物微胶囊中。
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引用次数: 1
Methods for Improving the Solubility of Water-Insoluble Drugs: A Comprehensive Review 提高水不溶性药物溶解度的方法综述
Pub Date : 2022-11-12 DOI: 10.52711/0975-4377.2022.00051
Wajid Ahmad, Rihan Sheikh, Razia Ahmad, Suhana Khan
Orally directed medications totally ingest just when they show reasonable dissolvability in gastric medium and such medications shows great bioavailability. The solvency and disintegration properties of medications assume a significant part during the formulation development. Greater part of the disappointments in the new medication improvement have been credited to poor water dissolvability of medication. It is widely accepted that poor water dissolvability is quite possibly the most every now and again experienced troubles in the field of pharmaceutics. Low solvency and ensuing unacceptable disintegration rate regularly bargain oral bioavailability. There are most remedial specialists used to create fundamental impacts by oral course that are the favored method of organization inferable from its few benefits and high quiet consistence contrasted with different courses. Thusly the current methodologies being utilized for BCS class II medications, along with retention enhancers, can be applied to detail class IV compound. Effervescent Assisted Fusion Technique, Solvent Evaporation method, Microemulsion, Liposomes are some imperative methodologies regularly utilized to improve the dissolvability of ineffectively water dissolvable medications. Determination of technique for solvency upgrade relies on drug qualities like dissolvability, substance nature, melting point, retention site, actual nature, pharmacokinetic conduct, etc, measurement structure necessity like tablet or capsule formulation, strength, quick or modified release. This review features the novel strategies accessible for improving solvency, disintegration and bioavailability of medications with poor fluid dissolvability.
口服药物只要在胃介质中表现出合理的可溶性,就完全被摄入,这类药物具有很高的生物利用度。药物的溶解性和崩解性在制剂开发过程中起着重要的作用。在新的药物改进中,令人失望的主要原因是药物的水溶性较差。人们普遍认为,水溶性差很可能是制药领域中最常遇到的问题。低偿付能力和随之而来的不可接受的分解率经常降低口服生物利用度。有大多数补救专家使用口头课程来创造基本影响,这是最受欢迎的组织方法,从它的少数好处和与其他课程相比的高安静一致性可以推断出来。因此,目前用于BCS II类药物的方法,以及保留增强剂,可以应用于详细的IV类化合物。泡腾辅助融合技术、溶剂蒸发法、微乳法、脂质体法是提高水溶性无效药物溶解性的常用方法。溶出度提升技术的确定依赖于溶出度、物质性质、熔点、保留部位、实际性质、药动学行为等药物质量,以及片剂或胶囊配方、强度、快速或缓释等计量结构必要性。本文综述了改善液体溶解性差的药物的溶解性、崩解性和生物利用度的新策略。
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引用次数: 0
Preparation and Evaluation of Sustained Release Tablet of Rifaximin by using Cross linked Sodium Alginate 交联海藻酸钠制备利福昔明缓释片及评价
Pub Date : 2022-11-12 DOI: 10.52711/0975-4377.2022.00043
Wajid Ahmad, Rihan Sheikh, Razia Ahmad, Suhana Khan
Rifaximin treats traveler's diarrhea and irritable bowel syndrome by stopping the growth of the bacteria that cause diarrhea. Rifaximin treats hepatic encephalopathy by stopping the growth of bacteria that produce toxins and that may worsen liver disease. The short half life and high frequency of administration of drug makes it a suitable candidate for designing sustained drug delivery system. The aim of the present investigation was to develop a sustained release matrix tablet of Rifaximin using sodium alginate and cross linked sodium alginate and to evaluate the drug release kinetics. In order to achieve the required sustained release profile, the tablets were prepared by a wet granulation method. The formulated tablets were characterized for pre-compression and post-compression parameters and they were in the acceptable limits. The drug release data obtained after an in vitro dissolution study was fitted to various release kinetic models in order to evaluate the release mechanism and kinetics. The criterion for selecting the best fit model was linearity (coefficient of correlation). Drug release mechanism was found to follow a complex mixture of diffusion, swelling and erosion. The dosage form holds the potential to control the release rate of drug and extend the duration of action of a drug.
利福昔明通过阻止引起腹泻的细菌的生长来治疗旅行者腹泻和肠易激综合征。利福昔明治疗肝性脑病的方法是阻止产生毒素并可能使肝病恶化的细菌的生长。药物的半衰期短,给药频率高,是设计持续给药系统的合适人选。以海藻酸钠和交联海藻酸钠为原料制备利福昔明缓释基质片,并对其释放动力学进行评价。为了达到所需的缓释特性,采用湿造粒法制备了该片剂。对制剂的压缩前后参数进行了表征,均在可接受范围内。通过体外溶出试验获得药物释放数据,拟合各种释放动力学模型,以评价其释放机制和动力学。选择最佳拟合模型的标准是线性(相关系数)。发现药物释放机制遵循扩散,肿胀和侵蚀的复杂混合。该剂型具有控制药物释放速度和延长药物作用时间的潜力。
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引用次数: 0
A Review that on Emphasizes the Traditional uses and Clinical Potential Calendula officinalis 金盏菊的传统用途及临床潜力综述
Pub Date : 2022-11-12 DOI: 10.52711/0975-4377.2022.00056
Wajid Ahmad, Jaza Quazi
This review assesses the use of Calendula officinalis extract in antihyperlipidemic activities, cardiovascular activities, antidiabetic, hepatoprotective activities; anthelmintic activities; antioxidant activities; anti-inflammatory activities; wound healing activities; anticancer activities; hepatoprotective activities, antibacterial activities; and anti-HIV activities. C. officinalis extract has been shown to have some remedial effects and has been used in herbal remedies, according to this review. To examine the effect of calendula officinalis, larger as well as well-designed random control trials are needed. Calendula officinalis is a flowering plant that comes under the Asteraceae family. This herb is used as curative in Europe, China, and India. It's been the subject of a number of chemical and pharmacological research, and it's also known as "African marigold." It's commonly utilized in indigenous medicine to treat jaundice, wound recovery, plasma cleansing, and spasmolytic treatment. A vast range of chemicals, including amino acids, triterpenoids, coumarines, quinones, flavonoids, volatile oils, and carotenoids, have been found through chemical analysis.
本文综述了金盏菊提取物在降血脂、心血管、抗糖尿病、保肝等方面的应用;驱虫剂活动;抗氧化活动;抗炎活动;创面愈合活动;抗癌活动;保肝活性、抗菌活性;以及抗艾滋病毒活动。根据这篇综述,officinalis提取物已被证明具有一定的治疗效果,并已被用于草药治疗。为了检验金盏菊的效果,需要更大规模和精心设计的随机对照试验。金盏菊是一种开花植物,属于菊科。这种草药在欧洲、中国和印度被用作治疗药物。它一直是许多化学和药理学研究的主题,它也被称为“非洲万寿菊”。它通常用于治疗黄疸,伤口愈合,血浆清洗和解痉治疗。通过化学分析发现了大量的化学物质,包括氨基酸、三萜、香豆酚、醌、类黄酮、挥发油和类胡萝卜素。
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引用次数: 0
Solubility Enhancement of Resveratrol by Effervescence Assisted Fusion Technique 泡沫辅助融合技术增强白藜芦醇溶解度的研究
Pub Date : 2022-11-12 DOI: 10.52711/0975-4377.2022.00048
M. Tawar, Kiran H. Raut, Reshma Chaudhary, N. Jain
The basic reason behind this study was to enhance the solubility rate of resveratrol which will finally enhance the dissolution i.e. the rate of drug release due to which the absorption of the drug will increase. The method applied here was effervescent assisted fusion technique. Various batches were prepared by employing water soluble carrier and sodium bicarbonate. The results obtained from the study revealed that the solubility of the drug can be increased up to 10 times than compared with the pure drug in various solvents i.e. phosphate buffer and distilled water. The compatibility study showed no interaction between drug and the excipient while the micromeretics property showed good flow property with good compressibility property. The percent yield of the dispersions prepared ranges between 79.20±0.28% - 89.38±0.25% while the drug release data showed a better rate of drug release than compared with the pure drug which ranges between 10.87% - 99.14%. The pure drug was having a drug release of less than 70% while the optimized batch F5 was having a drug release of more than 95% in the specific period of time. The XRD data showed that the drug’s crystalline structure was not hampered during the preparation while the SEM data revealed the surface shape of the pure drug which was tile shaped and the prepared dispersion was of flakes like formation. From the study it can be concluded that the methods employed in this study can be proven to be a excellent method for enhancing the solubility of the drug up to 10 folds.
这项研究的基本原因是为了提高白藜芦醇的溶解度,从而最终提高溶出度,即药物的释放速度,从而增加药物的吸收。这里采用的方法是泡腾辅助融合技术。采用水溶性载体和碳酸氢钠制备了不同批次的样品。研究结果表明,与纯药物相比,该药物在磷酸盐缓冲液和蒸馏水等溶剂中的溶解度可提高10倍。配伍研究表明,药物与辅料之间无相互作用,微动力学性能表现出良好的流动性能和良好的可压缩性。制备的分散体产率在79.20±0.28% ~ 89.38±0.25%之间,释药率在10.87% ~ 99.14%之间。纯药在特定时间内的释药率小于70%,而优化批F5的释药率大于95%。XRD数据表明药物的晶体结构在制备过程中没有受到阻碍,SEM数据显示纯药物的表面形状为瓦片状,制备的分散体呈片状。从研究中可以得出结论,本研究中采用的方法可以证明是一种将药物的溶解度提高10倍的极好方法。
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引用次数: 2
Natural Polymer Based Floating Matrix Tablets of Domperidone 天然聚合物基多潘立酮漂浮基质片
Pub Date : 2022-11-12 DOI: 10.52711/0975-4377.2022.00044
Sheeba Fr, Amar Sahani, Yogesh Db
Aim: This study is aimed to prepare floating matrix Domperidone Maleate tablets by using natural polymers. Materials and Methods: Domperidone maleate was formulated as floating matrix tablets to increase the gastric residence time. Natural polymers like xanthan gum, tragacanth, sodium alginate along with sodium bicarbonate, citric acid and HPMC were used to increase the buoyancy time and decrease the floating lag time. The compressed tablets were evaluated for various parameters like friability, hardness, uniformity of weight, uniformity of drug content, swelling index, bouncy time and in-vitro drug release. Results: The evaluated parameters were in compliance with the pharmacopoeial limits. The most successful formulation was F2, containing xanthan gum as polymer. The drug release was extended up to 10 h which was close to that of theoretical release profile. Mathematical modelling of in-vitro dissolution data indicated the best-fit release kinetics was achieved with Zero order model with R2 values of 0.99. Conclusion: The prepared sustained-release floating tablets of domperidone maleate could perform therapeutically better than that of conventional sustained release tablets with improved efficacy and better patient compliance.
目的:利用天然聚合物制备马来酸多潘立酮漂浮基质片。材料与方法:将马来酸多潘立酮配制为漂浮基质片,增加其胃停留时间。采用黄原胶、黄原胶、海藻酸钠等天然聚合物和碳酸氢钠、柠檬酸、HPMC等天然聚合物增加了浮时间,减少了浮滞时间。对压片的脆度、硬度、重量均匀性、含量均匀性、溶胀指数、弹性时间、体外释药等参数进行评价。结果:评价参数符合药典规定。最成功的配方是F2,以黄原胶为聚合物。药物释放时间延长至10 h,与理论释放曲线接近。体外溶出度数据的数学模型表明,该药物的释放动力学符合零级模型,R2值为0.99。结论:制备的马来酸多潘立酮缓释片治疗效果优于常规缓释片,疗效更高,患者依从性更好。
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引用次数: 0
A Chewable Toothpaste Tablet: An Alternative approach to the Toothpaste 牙膏咀嚼片:替代牙膏的一种方法
Pub Date : 2022-11-12 DOI: 10.52711/0975-4377.2022.00055
Deore Nisha N., R. K. Surawase
Nowadays we have all become very aware of toothpaste and its usage. Currently in the market medicated and herbal toothpaste are available. It’s a huge competition for better results from toothpaste for the prevention of tooth problems. Recently daily use lots of dental products and after use, we throw the containers and closures straight in the trash bin without thinking like are they are reusable or not. This is the current case in our country India, comparatively, in other countries, there is a growing awareness about proper waste management and the production of eco-friendly products and reusable. According to a new report published by Allied Market Research, titled, “Toothpaste Tablet Market by Product Type, Flavour Type, Packaging Type, Distribution Channel, and Price Point: Global Opportunity Analysis and Industry Forecast, 2021–2030,” the global toothpaste tablet market size was valued at $45.6 million in 2020, and is projected to reach $90.3 million by 2030, registering a CAGR of 7.3% from 2021 to 2030. Global toothpaste tablets sales are expected to grow at a healthy Compound annual growth rate (CAGR) of over 6.1% during the study forecast period 2021-2031.The toothpaste tablets sales are expected to grow significantly in the coming years. There is a future need in our developing country, however, unfortunately, there is no proper control over this. This review article aims to explore dental problems with sparing on a modified tablet dosage form i.e., chewable tablet toothpaste which will be helpful to reduce plastic waste, will be eco-friendly, cost-effective, and improve dental health.
现在我们都非常了解牙膏和它的用法。目前市场上有药物牙膏和草药牙膏。这是牙膏在预防牙齿问题方面的巨大竞争。最近我们每天使用很多牙科产品,用完后,我们把容器和瓶盖直接扔进垃圾桶,而不去想它们是否可以重复使用。这是目前在我们国家印度的情况,相比之下,在其他国家,人们越来越意识到适当的废物管理和生产环保产品和可重复使用。根据联合市场研究公司(Allied Market Research)发布的一份题为《牙膏片剂市场按产品类型、风味类型、包装类型、分销渠道和价格点:2021 - 2030年全球机会分析和行业预测》的新报告,2020年全球牙膏片剂市场规模为4560万美元,预计到2030年将达到9030万美元,从2021年到2030年的复合年增长率为7.3%。在2021-2031年的研究预测期内,全球牙膏片销售预计将以超过6.1%的健康复合年增长率(CAGR)增长。预计未来几年,牙膏片剂的销量将大幅增长。这是我们发展中国家未来的需要,然而,不幸的是,对此没有适当的控制。本文旨在探讨一种改进的片剂剂型,即咀嚼片剂牙膏,有助于减少塑料废物,环保,经济,改善牙齿健康。
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引用次数: 0
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Research Journal of Pharmaceutical Dosage Forms and Technology
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