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Design and characterization of controlled release formulation of Mesna by using different polymers 使用不同聚合物设计和表征 Mesna 的控释制剂
Pub Date : 2024-07-26 DOI: 10.26452/fjphs.v4i3.643
Padhy Aniket, Gopi G, P. Pk
The current study created a controlled-release formulation of Mesna to keep the drug at therapeutic levels for longer than ten hours. Eudragit L 100, Chitosan, HPMC K4M. The dose of mesna was set at 100 mg. The tablet's total weight was calculated to be 100 mg. Polymers were employed in concentrations of 50 mg, 100 mg, and 150 mg. Every formulation passed several physicochemical evaluation criteria and was determined to be within tolerances. However, it was clear from the dissolving trials that the formulation (F6) had a better and more desirable drug release pattern, achieving 96.47% in 10 hours. As a controlled release substance, it contains the naturally occurring polymer Mesna. The release kinetics mechanism was in zero order. The optimal formulation was used again for reproducibility, and conformance was tested in all quality control procedures. It was discovered that the outcomes were very impossible for one another. The optimized formula will be used for formulation development and other studies, such as bio-equivalency research, to ensure a successful product launch.
目前的研究创建了一种 Mesna 的控释制剂,可将药物保持在治疗水平长达十多个小时。Eudragit L 100、壳聚糖、HPMC K4M。美司那的剂量设定为 100 毫克。计算得出片剂的总重量为 100 毫克。聚合物的浓度分别为 50 毫克、100 毫克和 150 毫克。每个制剂都通过了多项理化评估标准,并被确定在容许范围内。不过,从溶解试验中可以明显看出,配方(F6)的药物释放模式更好、更理想,在 10 小时内达到 96.47%。作为一种控释物质,它含有天然聚合物 Mesna。释放动力学机制为零阶。再次使用最佳配方进行重现性试验,并对所有质量控制程序的一致性进行测试。结果发现,两者之间的结果很不可能一致。优化配方将用于配方开发和其他研究,如生物等效性研究,以确保产品成功上市。
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引用次数: 0
Formulation and evaluation of Metoprolol succinate buccal tablets in hypertension treatment 琥珀酸美托洛尔口腔片在高血压治疗中的配制和评估
Pub Date : 2024-07-22 DOI: 10.26452/fjphs.v4i3.636
Kishore Bandarapalle, Rajasekhar Kk, Teja Sri Kamasani, Sangeetha Mohanrao, Neeraja Boyalapalli, Likhitha Chejarla, Bhargavi Cy, Chaitanya Krishna
The research aims to formulate and evaluate the Metoprolol succinate buccal tablets in hypertension treatment. The Fourier transform infrared (FTIR) results depict no incompatibility between the drug and excipients. The study results of pre-compression parameters have excellent flow qualities and compressibility. The post-compression parameters show that the results are within the specified standard deviations. The swelling index reveals that the formulation F6 shows that the complete drug was released and the tablet integrity was maintained during the expected duration. Formulation F6 chitosan and Carbopol 934 were used in a ratio of 1:1, resulting in the release of the drug up to the 10th hour and completely. Therefore, formulation F6 was optimized and compared with the marketed product. Formulation F6 exhibited better drug release performance than the marketed product.
该研究旨在配制和评估用于治疗高血压的琥珀酸美托洛尔口含片。傅立叶变换红外光谱(FTIR)结果表明,药物与辅料之间没有不相容性。压缩前参数的研究结果表明,片剂具有良好的流动性和可压缩性。压缩后参数显示结果在规定的标准偏差范围内。膨胀指数显示,配方 F6 在预期的时间内释放了全部药物并保持了片剂的完整性。配方 F6 中壳聚糖和 Carbopol 934 的使用比例为 1:1,结果表明药物在第 10 小时内完全释放。因此,对配方 F6 进行了优化,并与市售产品进行了比较。配方 F6 的药物释放性能优于市售产品。
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引用次数: 0
Deciphering the role and impact of India's pharmaceutical industries and its regulatory compliance 解读印度制药业的作用和影响及其合规性
Pub Date : 2024-07-22 DOI: 10.26452/fjphs.v4i3.634
Harika Sirivella, Lavanya Agamudi, Sarah Sujitha Y
The pharmaceutical industry faces exceptionally high R&D costs, with the US research-based sector investing about 17% of sales into R&D. The cost of bringing a new compound to market was estimated at $802 million in 2001, up from $138 million in the 1970s and $318 million in the 1990s, necessitating stringent regulations. This study aims to determine the role and impact of India's pharmaceutical industry and its regulatory compliance. Personnel from organizations established between 1884 and 2004, with turnovers ranging from Rs. 25 crore (US $5.3 million) to Rs. 5500 crore (US $1.2 billion), were surveyed. Out of 150 companies approached, 73 responded, with 70 complete responses analyzed. Ongoing interactions with regulatory agencies helped companies better understand the regulatory system. Three key areas emerged as priorities: awareness of intellectual property rights (IPR) and patents, fostering a suitable environment for research and development, and implementing Good Manufacturing Practices (GMP), considered more critical than price control. The findings underscore the importance of regulatory compliance in promoting innovation and maintaining quality within the pharmaceutical industry, ensuring its competitiveness and ability to meet global standards.
制药业面临着极高的研发成本,美国以研究为基础的部门将销售额的 17% 投入研发。2001 年,将一种新化合物推向市场的成本估计为 8.02 亿美元,高于 20 世纪 70 年代的 1.38 亿美元和 20 世纪 90 年代的 3.18 亿美元,因此有必要制定严格的法规。本研究旨在确定印度制药业的作用和影响及其监管合规情况。对成立于 1884 年至 2004 年、营业额从 25 亿卢比(530 万美元)到 5500 亿卢比(12 亿美元)不等的企业人员进行了调查。在接触的 150 家公司中,有 73 家做出了答复,其中 70 份完整答复得到了分析。与监管机构的持续互动帮助企业更好地了解监管体系。三个关键领域被列为优先事项:知识产权 (IPR) 和专利意识、营造适宜的研发环境以及实施良好生产规范 (GMP),这被认为比价格控制更为重要。调查结果表明,在促进制药业创新和保持质量、确保其竞争力和达到全球标准的能力方面,遵守法规非常重要。
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引用次数: 0
Formulation and evaluation of amoxapine mucoadhesive buccal films 阿莫沙平粘合剂口腔胶片的配制与评估
Pub Date : 2024-07-08 DOI: 10.26452/fjphs.v4i3.629
Mahaboob Ali Sk., S. Kv, Gautham Chakra R
Among innovative drug delivery methods, buccal mucoadhesive systems have been attracting much interest recently because of their capacity to stick to the oral mucosa, stay there, and gradually release their drug content. By improving medication absorption through the oral mucosa and reducing the hepatic first-pass impact, buccal mucoadhesive films can increase the drug's bioavailability and enhance its therapeutic effect. The current study aimed to synthesize the medicine as a buccal bioadhesive film, which reduces the frequency of dosage form administration by releasing the drug at a sufficient concentration over time. Because this formulation is simple to administer and requires no water to swallow, improved patient compliance is one of its benefits. Dissolving profile as investigated in USP dissolving apparatus type 1 using saliva at pH 6.8. The impact of factors such as polymer type, concentration, and release profile of Amoxapine was investigated. The formulation was optimized Based on several evaluation criteria, including drug content and in-vitro drug release. Formulation F6 successfully releases the drug in 7 hours. The stability studies followed ICH recommendations, and the results showed that the optimized formulation was stable. The IR spectra demonstrated the stable qualities of Amoxapine in a mixture of polymers utilized and revealed the absence of interaction between the drug and the selected polymer.
在创新给药方法中,颊黏膜黏附系统因其能够黏附在口腔黏膜上,并在口腔黏膜上停留和逐渐释放药物成分而受到广泛关注。颊黏膜可以提高药物通过口腔黏膜的吸收率,减少肝脏的首过效应,从而提高药物的生物利用度,增强治疗效果。本研究旨在将药物合成为一种口腔生物黏附膜,通过在一段时间内释放足够浓度的药物,减少剂型给药次数。由于这种制剂给药简单,无需用水吞服,因此能提高患者的依从性,这也是它的优点之一。在 pH 值为 6.8 的美国药典 1 型溶解器中使用唾液对溶解曲线进行了研究。研究了聚合物类型、浓度和阿莫沙平释放曲线等因素的影响。根据药物含量和体外药物释放等多项评估标准,对配方进行了优化。配方 F6 成功地在 7 小时内释放了药物。稳定性研究遵循了 ICH 建议,结果表明优化后的制剂是稳定的。红外光谱显示了阿莫沙平在聚合物混合物中的稳定性,并表明药物与所选聚合物之间不存在相互作用。
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引用次数: 0
Fabrication and characterization of hydroquinone in liposomal gel for transdermal drug delivery 用于透皮给药的脂质体凝胶中对苯二酚的制备与表征
Pub Date : 2024-07-08 DOI: 10.26452/fjphs.v4i3.628
V. Penabaka, Chandrika Jorepalli, Harika Kandala, Nichitha Lakku, Nikhil Orugunta, Thulasi Thandra, Prapurnachandra Yadala
This study aimed to formulate a gel for hydroquinone dermal therapy using liposomes to maintain the active agents' concentration in the skin's deepest layers. Cholesterol was incorporated to enhance the liposome's bilayer characteristics, increasing microviscosity, membrane stability, and blister rigidity. Various methods for liposome preparation exist, but the film hydration method, being the most common, was utilized here. Results for formulation HL6, which had lower levels of Lecithin Cholesterol and rotation speed, revealed a vesicle size of 180.4 nm, a Zeta potential of -37.5 mV, and an entrapment efficiency of 69.10±1.52%. In-vitro drug release data for formulations F1, F2, and F3 within 30 minutes showed hydroquinone release rates of 97.75±0.28%, 98.92±0.56%, and 94.45±0.36%, respectively. The order of drug release was F2 > F1 > F3, with F2 demonstrating the maximum release rate. The study concludes that liposomal gel is an effective transdermal drug delivery system for therapeutic molecules. Lipid vesicles, such as liposomes, are among the best mechanisms for delivering medications to their intended locations while minimizing their dissemination to non-target tissues. This liposomal gel-based formulation shows significant potential for effectively treating acne by maintaining high concentrations of active agents in the skin's deepest layers and ensuring a controlled and sustained drug release.
本研究旨在利用脂质体配制一种用于对苯二酚皮肤疗法的凝胶,以保持活性剂在皮肤最深层的浓度。加入胆固醇可增强脂质体的双分子层特性,提高微粘度、膜稳定性和水疱硬度。脂质体的制备方法多种多样,但这里采用的是最常见的薄膜水合法。卵磷脂胆固醇含量和旋转速度较低的配方 HL6 的结果显示,囊泡大小为 180.4 nm,Zeta 电位为 -37.5 mV,包封效率为 69.10±1.52%。制剂 F1、F2 和 F3 在 30 分钟内的体外药物释放数据显示,对苯二酚的释放率分别为 97.75±0.28%、98.92±0.56% 和 94.45±0.36%。药物释放顺序为 F2 > F1 > F3,其中 F2 的释放率最高。研究得出结论,脂质体凝胶是一种有效的治疗分子透皮给药系统。脂质体等脂质囊泡是将药物输送到预定位置的最佳机制之一,同时可最大限度地减少药物向非目标组织的扩散。这种基于脂质体凝胶的配方能在皮肤最深层保持高浓度的活性药物,并确保药物的可控和持续释放,因此在有效治疗痤疮方面显示出巨大的潜力。
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引用次数: 0
Significance of Alternative Medicines in Treatment of Chronic Diseases: A Comprehensive Review 替代药物在治疗慢性疾病中的意义:全面回顾
Pub Date : 2024-07-08 DOI: 10.26452/fjphs.v4i3.630
Afsar Shaik, Fazeen Mohamed
The treatment of chronic diseases poses significant challenges to healthcare systems worldwide. While conventional medical approaches have made substantial progress, alternative medicines have gained recognition for their potential to complement or even substitute conventional treatments. This comprehensive review examines the role of alternative medications in chronic disease management, encompassing a wide range of modalities, from herbal remedies and acupuncture to mind-body therapies and chiropractic care. We explore the efficacy and safety of alternative treatments, mechanisms of action, patient perspectives, regulatory and ethical considerations, cost-effectiveness, and the potential for integration with conventional medicine. Drawing upon clinical studies, patient testimonials, and scholarly sources, this review highlights alternative medicine's diverse and evolving landscape, its significance in improving patient outcomes, and the challenges that must be addressed. We offer recommendations for patients, healthcare providers, and policymakers on integrating and responsible use of alternative medicines in chronic disease management.
慢性疾病的治疗给全世界的医疗系统带来了巨大挑战。在传统医疗方法取得长足进步的同时,替代药物也因其补充甚至替代传统疗法的潜力而获得认可。这篇综合性综述探讨了替代药物在慢性病治疗中的作用,包括从草药疗法、针灸到身心疗法和脊椎按摩等多种方式。我们探讨了替代疗法的疗效和安全性、作用机制、患者观点、监管和伦理因素、成本效益以及与传统医学结合的潜力。通过临床研究、患者证言和学术资料,本综述强调了替代医学的多样性和不断发展的前景、其在改善患者预后方面的重要性以及必须应对的挑战。我们为患者、医疗服务提供者和政策制定者提供了关于在慢性病管理中整合并负责任地使用替代医学的建议。
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引用次数: 0
Controlled Release Lercanidipine Tablets: A Study on Formulation and Evaluation by Wet Granulation 控释乐卡地平片:湿法制粒的制剂与评估研究
Pub Date : 2024-07-05 DOI: 10.26452/fjphs.v4i3.623
Sujana A, Durga Prasad K, Sarada Mrinalini Talluri
Lercanidipine blocks the entry of extracellular calcium into vascular and cardiac muscle cells, preventing myocardial smooth muscle contraction due to decreased intracellular calcium. This results in the dilation of coronary and systemic arteries, reducing blood pressure. This study aimed to develop and evaluate lercanidipine controlled-release tablets for oral administration using polymers like HPMC K 100M, sodium alginate, and guar gum. Lercanidipine, polymers, and diluents were sieved and mixed for 10 minutes. Granules were formed using isopropyl alcohol, dried at 60°C for one hour, and sieved. The granules were lubricated with colloidal silicon dioxide (Aerosil-200) and magnesium stearate, blended for 5 minutes, and compressed using a rotary machine (average weight: 500 mg; hardness: 5-6 kg/cm²). Bulk and tapped densities were nearly identical for all formulations. Compressibility index and Hausner ratio ranged from ?18 to 1.09-1.21, indicating good flow properties. Tablet thickness ranged from 5.82 to 5.91 mm, hardness from 5.9 to 6.3 kg/cm², and friability was less than 1.0 %W/W. Drug content was between 98-102%. The controlled-release order from dissolution data was F9 > F7 > F8, showing optimal release with a combination of HPMC and two natural polymers.
乐卡地平能阻止细胞外钙进入血管和心肌细胞,防止心肌平滑肌因细胞内钙减少而收缩。这将导致冠状动脉和全身动脉扩张,从而降低血压。本研究旨在利用 HPMC K 100M、海藻酸钠和瓜尔豆胶等聚合物,开发和评估用于口服的勒卡尼平控释片剂。将乐卡地平、聚合物和稀释剂过筛并混合 10 分钟。用异丙醇制成颗粒,在 60°C 下干燥一小时,然后过筛。用胶体二氧化硅(Aerosil-200)和硬脂酸镁润滑颗粒,混合 5 分钟,然后用旋转机压缩(平均重量:500 毫克;硬度:5-6 千克/平方厘米)。所有配方的体积密度和敲击密度几乎相同。可压缩指数和豪斯纳比率介于 0.18 至 1.09-1.21 之间,表明具有良好的流动性。片剂厚度为 5.82 至 5.91 毫米,硬度为 5.9 至 6.3 千克/平方厘米,易碎性小于 1.0 %W/W。药物含量在 98-102% 之间。从溶解数据来看,控释顺序为 F9 > F7 > F8,表明 HPMC 和两种天然聚合物的组合具有最佳释放效果。
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引用次数: 0
Adrenoleukodystrophy an Overview 肾上腺脑白质营养不良症概述
Pub Date : 2024-07-05 DOI: 10.26452/fjphs.v4i3.625
Achala Kp, Niharika Kj, Shashank Kr, Prajnesh J Shetty
Adrenoleukodystrophy (ALD) is a rare X-linked peroxisomal oxidation disease caused by mutations in ABCD1. It presents with various clinical manifestations, including cerebral ALD, myelopathy, and primary adrenal insufficiency. About 80% of ALD patients suffer from adrenal insufficiency, and cerebral ALD affects one-third of boys under twelve, progressing to total impairment and death without treatment. Hematopoietic stem cell transplantation (HSCT) is the only disease-modifying treatment for early-stage cerebral ALD, but it does not halt adrenal insufficiency progression and carries significant morbidity and mortality risks. A recent gene therapy clinical trial showed short-term MRI and neurological outcomes equivalent to past HSCT treatments without the adverse side effects. Additionally, over a dozen states have initiated newborn screening (NBS) for ALD, with the number expected to triple by 2020. Genetic testing of NBS-positive newborns has identified novel variations of unknown significance, raising questions about monitoring and treating preclinical or moderate adrenal insufficiency or cerebral involvement. This presents further opportunities for genetic characterization. The availability of matching donors, transplant centers, and specialists will impact prompt treatment for those diagnosed with ALD at birth. As NBS and gene therapy trials improve ALD's clinical management and prognosis, endocrine management of presymptomatic and subclinical adrenal insufficiency will become increasingly important.
肾上腺白质营养不良症(ALD)是一种罕见的 X 连锁过氧化物酶体氧化病,由 ABCD1 基因突变引起。它有多种临床表现,包括脑ALD、脊髓病和原发性肾上腺功能不全。约80%的ALD患者患有肾上腺功能不全,12岁以下的男孩中有三分之一患有脑ALD,如果不进行治疗,病情会发展到完全损伤和死亡。造血干细胞移植(HSCT)是早期脑 ALD 唯一可改变病情的治疗方法,但它并不能阻止肾上腺功能不全的发展,而且有很大的发病率和死亡率风险。最近的一项基因治疗临床试验显示,其短期磁共振成像和神经系统疗效与以往的造血干细胞移植疗法相当,且无不良副作用。此外,美国已有十几个州启动了针对 ALD 的新生儿筛查(NBS),预计到 2020 年,筛查人数将增加三倍。对 NBS 阳性新生儿的基因检测发现了一些意义不明的新变异,提出了监测和治疗临床前或中度肾上腺功能不全或脑部受累的问题。这为基因特征描述提供了更多机会。匹配供体、移植中心和专家的可用性将对出生时被诊断为 ALD 的患者的及时治疗产生影响。随着 NBS 和基因治疗试验改善 ALD 的临床管理和预后,对无症状和亚临床肾上腺功能不全的内分泌管理将变得越来越重要。
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引用次数: 0
In-Vitro antidiabetic activity of leaf juice of Mespilus Germanica L Mespilus Germanica L 叶汁的体外抗糖尿病活性
Pub Date : 2024-07-05 DOI: 10.26452/fjphs.v4i3.626
Rajeswari Guduru, Kalyani Prakashini Ingilala
Diabetes mellitus, a modern civilization disease, is marked by chronic hyperglycemia and severe complications if untreated. Type II DM, a multifactorial form, accounts for 90% of global cases. Controlling postprandial glucose is vital for preventing complications, as elevated plasma glucose is influenced by ?-amylase and ?-glucosidases. Current enzyme inhibitors like Acarbose and voglibose cause gastrointestinal side effects. This study aimed to find natural source inhibitors with fewer adverse effects using in-vitro antidiabetic assays. Mespilus germanica L. leaf juice (20-100 ?g/ml) was tested against fungal ?-amylase and ?-glucosidases from albino rat intestines. The enzymes showed dose-dependent inhibition comparable to Acarbose. LJMG and Acarbose had IC50 values of 83.35 and 52.15 ?g/ml for fungal ?-amylase, and 92.44 and 54.84 ?g/ml for ?-glucosidase, respectively. The leaf juice had a protein content of 10.6 mg/ml and increased glucose uptake by yeast similarly to Metronidazole. Results suggest that polyphenolic compounds in the leaf juice mimic insulin in glucose utilization and inhibit ?-amylase and ?-glucosidase. Further pre-clinical assessments are needed to confirm the antidiabetic potential of this herb.
糖尿病是一种现代文明病,以慢性高血糖和严重并发症(如不及时治疗)为特征。II 型糖尿病是一种多因素糖尿病,占全球病例的 90%。控制餐后血糖对预防并发症至关重要,因为血糖升高会受到淀粉酶和葡萄糖苷酶的影响。目前的酶抑制剂如阿卡波糖和伏格列波糖会引起胃肠道副作用。这项研究旨在通过体外抗糖尿病试验找到不良反应较少的天然抑制剂。研究人员利用 Mespilus germanica L. 叶汁(20-100 克/毫升)对白化大鼠肠道中的真菌淀粉酶和葡萄糖苷酶进行了测试。这些酶表现出与阿卡波糖相当的剂量依赖性抑制作用。LJMG 和阿卡波糖对真菌淀粉酶的 IC50 值分别为 83.35 和 52.15 克/毫升,对葡萄糖苷酶的 IC50 值分别为 92.44 和 54.84 克/毫升。叶汁的蛋白质含量为 10.6 毫克/毫升,与甲硝唑相似,能增加酵母对葡萄糖的吸收。结果表明,叶汁中的多酚类化合物在葡萄糖利用中模拟胰岛素,并抑制淀粉酶和葡萄糖苷酶。要确认这种草药的抗糖尿病潜力,还需要进一步的临床前评估。
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引用次数: 0
Formulation and evaluation of mouth-dissolving films of memantine 美金刚口腔溶解膜的制备与评估
Pub Date : 2024-05-19 DOI: 10.26452/fjphs.v4i2.612
S. Kv, Murali Mohan Kummari, Irfan Shaik, Sai Teja Narsipally, Karishma Thotlo, Ooha Chowdary Tellapati, Manasa Medisetty, Dastagiri Udayagiri
This present research aims to formulate and evaluate mouth dissolving films using Memantine as model drug to improve bioavailability and facilitate rapid onset of action to relieve vomiting and nausea. The thicknesses of the films were in the range of 0.234 mm to 0.271mm. The weights of the films were found to be in the range of ±10%. The folding endurance of the films was found to be in the range of 38± 1 to 57 ± 2.  The surface pHs of all the films were neutral, as there was no color change in the litmus paper.  All the films were found to be 98 to 102. The disintegration time of the prepared films ranged from 21sec to 32sec. Acceptable mechanical properties were obtained in batch F-9, and the in vitro disintegration time was below 27 sec. It has been determined that formulations F-9 were found to be satisfactory batches and were optimized for the desirable properties.
本研究旨在以美金刚为模型药物,配制和评估口腔溶解膜,以提高生物利用度,促进快速起效,缓解呕吐和恶心症状。薄膜的厚度在 0.234 毫米至 0.271 毫米之间。薄膜的重量在 ±10% 的范围内。所有薄膜的表面 pH 值均为中性,石蕊试纸上没有颜色变化。 所有薄膜的pH值均为 98 至 102。所制备薄膜的崩解时间为 21 秒至 32 秒。F-9 批次获得了可接受的机械性能,体外崩解时间低于 27 秒。经确定,F-9 批次配方是令人满意的批次,并对其理想特性进行了优化。
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引用次数: 0
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Future Journal of Pharmaceuticals and Health Sciences
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