The use of antihypertensive drugs with different sustained and controlled release dosage forms in nasal feeding
-
摘要: 抗高血压药物的口服固体制剂在鼻饲患者中存在许多不合理用药现象。许多固体制剂因其特殊的制药技术，不能掰开、研磨后鼻饲。本文通过查阅相关文献，阐述口服药物体内的释药过程，归纳总结了几类抗高血压药物缓控释制剂的类型和结构特点，并尝试探讨药物不同缓控释类型在鼻饲使用中的特点，为全科医生在临床工作中提供合理用药参考。缓控释制剂主要有骨架型缓控释制剂、膜控型缓控释制剂、渗透泵型缓控释制剂、肠溶型控释制剂、微丸控释制剂几大类。目前常用的硝苯地平缓控释制剂主要为拜耳公司的进口原研药渗透泵型硝苯地平控释剂(拜新同，Adalet)，国产硝苯地平缓释剂为亲水凝胶型骨架型缓释剂，控释片为渗透泵型控释剂。常用的美托洛尔为阿斯利康公司的进口原研药酒石酸美托洛尔片(倍他乐克)和琥珀酸美托洛尔缓释片(倍他乐克缓释片)，分别为普通片剂和骨架微丸型控释剂，国产酒石酸美托洛尔主要为基于渗透压释药原理的以羟丙甲纤维素(hydroxypropyl methyl cellulose，HPMC)或乙基纤维素(ethyl cellulose ethoce，EC)为骨架的缓释制剂或胶囊剂。缓控释制剂因其研磨后，不同程度破坏其缓控释结构，药物快速入血，加之单片剂量为普通片剂数倍，带来极大副反应，禁止研磨鼻饲使用，尤其是渗透泵型控释片。有刻痕的骨架型缓释片可掰服，禁止研磨。Abstract: The oral solid preparation of antihypertensive drugs has many unreasonable uses in patients with nasal feeding. Most solid preparations cannot be broken and ground after nasal feeding due to their special pharmaceutical technology. In this paper, referring to relevant literature, we summarized the types and structural characteristics of several types of antihypertensive drugs slow and controlled release preparation. To explore the characteristics of different controlled release types of drugs in the use of nasal feeding, and to provide a reference for general practitioners to use the drugs rationally in clinical work. The main types of sustained-release formulations are skeletal sustained-release formulations, membrane controlled-release formulations, osmotic pump sustained-release formulations, enteric-release controlled-release formulations and pellet controlled-release formulations. The commonly used nifedipine controlled release preparations mainly include Bayer company's imported original research drug osmotic pump nifedipine controlled release agent (Adalet), domestic nifedipine sustained release agent for hydrophilic gel matrix type sustained release agent, controlled release tablets for osmotic pump type-controlled release agent. Commonly used metoprolol for imported drugs which Swiss astrazeneca company tartrate metoprolol and succinic acid metoprolol (Betaloc) are ordinary tablets and skeleton type micro pill respectively controlled release agent. And the domestic tartrate metoprolol is mainly based on osmotic pressure release principle with hydroxypropyl methyl cellulose (HPMC)/ethyl cellulose ethoce (EC) as the skeleton of sustained release preparation or capsule preparation. Delayed and controlled release preparation is prohibited to be used for grinding nasal feeding, especially osmotic pump controlled release tablets, because the delayed and controlled release structure is damaged to varying degrees after grinding, the drug enters the blood quickly, and the single dose is several times that of ordinary tablets, which brings great side effects. The frame type sustained-release tablets with scratches can be snapped off and do not grind.
-
表 1 常用缓控释抗高血压口服药物特点
类别 药物 商品名 通用名 制剂类型 规格 推荐剂量 特点 利尿剂 吲达帕胺 纳催离 吲达帕胺缓释片 基质缓释制剂 1.5 mg 1.5 mg, 1次/d 可完整吞服, 不能嚼碎、研磨或鼻饲。 钙离子拮抗剂 硝苯地平 伲福达 硝苯地平缓释片 胶体骨架控释制剂 20 mg 20 mg, 1~2次/d 完整吞服, 可沿片面“中心线”完整分开半片服用, 不能嚼碎或研磨鼻饲 拜新同Adalat 硝苯地平控释片Ⅱ 渗透泵控释制剂 30 mg; 60 mg 30~60 mg, 1次/d 完整吞服, 不能掰片服用, 不能嚼碎或研磨鼻饲 非洛地平 波依定 非洛地平缓释片 亲水骨架型缓控释制剂 2.5 mg; 5 mg; 10 mg 5~10 mg, 1次/d; 老人2.5 mg, 1次/d 整片吞服, 不能咬碎、咀嚼、掰开服用 尼莫地平 易夫林/抒孚 尼莫地平缓释片 基质缓释 60 mg 60~120 mg, 2次/d 整片吞服。 尼立苏 尼莫地平缓释胶囊 缓释胶囊 60 mg 60~120 mg, 2次/d 整颗吞服。 维拉帕米 盖衡 盐酸维拉帕米缓释片 骨架控释制剂 120 mg 180~240 mg, 1次/d; 老人120 mg, 1次/d 说明书未给出。整片吞服, 不推荐咀嚼、掰开、研磨鼻饲服用。 地尔硫卓 合贝爽/艾克朗 盐酸地尔硫卓缓释胶囊 缓释胶囊 90 mg; 120 mg 90 mg, 1~2次/d; 180 mg, 1次/d 整颗吞服, 不能去除胶囊溶解后鼻饲 恬尔新 盐酸地尔硫卓缓释片 基质缓释 90 mg 90~180 mg, 1次/d 整片吞服, 不能研磨鼻饲 芊克 盐酸地尔硫卓控释胶囊 缓释微丸胶囊制剂 180 mg 180 mg, 1次/d 整颗吞服, 可去除胶囊后化水鼻饲 β受体阻滞剂 普萘洛尔 海力欣 盐酸普萘洛尔缓释片 基质缓释制剂 40 mg 40 mg, 1次/d 整片吞服, 可掰片服用, 不能嚼碎或研磨鼻饲 杭达来 盐酸普萘洛尔缓释胶囊 缓释微丸胶囊制剂 40 mg 40 mg, 1次/d 整片吞服, 不能掰服, 不能嚼碎或研磨鼻饲 美托洛尔 倍他乐克 酒石酸美托洛尔片 普通片剂 25 mg; 50 mg; 100 mg 100~200 mg, 1~2次/d 整片口服、掰服、研磨吞服 倍他乐克缓释片 琥珀酸美托洛尔缓释片 膜控型包衣缓释微丸制剂 23.75 mg; 47.5 mg; 95 mg; 190 mg 47.5~95 mg, 1次/d 可整片口服, 有刻痕, 可掰开服用, 但不能研磨后鼻饲 
下载: 导出CSV
-
[1] WHELTON P K, CAREY R M, ARONOW W S, et al. 2017 ACC/AHA/AAPA/ABC/ACPM/AGS/APhA/ASH/ASPC/NMA/PCNA guideline for the prevention, detection, evaluation, and management of high blood pressure in adults: A report of the american college of cardiology/american heart association task force on clinical practice guidelines[J]. Hypertension, 2018, 71(6): e140-e144. [2] ALTREUTER D H, KIRTANE A R, GRANT T, et al. Changing the pill: Developments toward the promise of an ultra-long-acting gastroretentive dosage form[J]. Expert Opin Drug Deliv, 2018, 15(12): 1189-1198. doi: 10.1080/17425247.2018.1544615 [3] AXEL ZEITLER J, RADES T. Interdependence of dosage form microstructure and performance[J]. Pharm Res, 2017, 34(5): 887-889. doi: 10.1007/s11095-017-2137-z [4] LAU E T L, STEADMAN K J, CICHERO J A Y, et al. Dosage form modification and oral drug delivery in older people[J]. Adv Drug Deliv Rev, 2018, 135: 75-84. doi: 10.1016/j.addr.2018.04.012 [5] 杨堆进. 老年患者合理用药的研究进展[J]. 临床合理用药杂志, 2018, 11(9): 174-177. https://www.cnki.com.cn/Article/CJFDTOTAL-PLHY201809088.htm [6] 郑东鹏, 卢爱敏, 许友贤. 基于高血压病诊疗实践的上海市慢性病长处方签约服务的效果评价[J]. 中华全科医学, 2019, 17(4): 583-585, 681. https://www.cnki.com.cn/Article/CJFDTOTAL-SYQY201904019.htm [7] LI Y, ZHONG M, XIE F, et al. The effect of ph on the stabilization and digestive characteristics of soybean lipophilic protein oil-in-water emulsions with hypromellose[J]. Food Chem, 2020, 309: 125579. doi: 10.1016/j.foodchem.2019.125579 [8] 王立, 刘华石, 张文君, 等. 包衣技术在口服固体缓控释制剂中的应用[J]. 药学研究, 2017, 36(2): 108-110. https://www.cnki.com.cn/Article/CJFDTOTAL-SDYG201702013.htm [9] 袁春平, 侯惠民, 钱明英, 等. 渗透泵片剂的新型热塑包衣技术制备工艺的开发[J]. 中国医药工业杂志, 2019, 50(1): 48-58. https://www.cnki.com.cn/Article/CJFDTOTAL-ZHOU201901005.htm [10] 安欣欣, 周洪雷, 李传厚, 等. 口服渗透泵控释制剂的研究进展[J]. 中国药房, 2018, 29(22): 3165-3168. doi: 10.6039/j.issn.1001-0408.2018.22.30 [11] 褚晓杰. 肠溶型阿司匹林与普通阿司匹林胃肠道不良反应分析[J]. 中国现代药物应用, 2018, 12(13): 162-163. https://www.cnki.com.cn/Article/CJFDTOTAL-ZWYY201813092.htm [12] 刘毓婷, 苏峰, 刘为中, 等. 缓控释微丸制剂的研究进展[J]. 广州化工, 2017, 45(24): 34-36. doi: 10.3969/j.issn.1001-9677.2017.24.013 [13] 吉顺莉, 徐安保, 吴伟. 右旋雷贝拉唑钠肠溶微丸的制备及体外释放度考察[J]. 中国药师, 2016, 19(4): 797-800. doi: 10.3969/j.issn.1008-049X.2016.04.057 [14] CHEN T, LI J, CHEN T, et al. Tablets of multi-unit pellet system for controlled drug delivery[J]. J Control Release, 2017, 262: 222-231. doi: 10.1016/j.jconrel.2017.07.043 [15] AVILA-SALAS F, RODRIGUEZ NUÑEZ Y A, Marican A, et al. Rational development of a novel hydrogel as a ph-sensitive controlled release system for nifedipine[J]. Polymers (Basel), 2018, 10(7): 806. doi: 10.3390/polym10070806 [16] El-MASRY S M, El-KHODARY N M. Pharmacokinetic and tolerability comparison of sustained and immediate release oral formulations of nifedipine tablet formulations: A single-dose, randomized, open-label, two-period, two-way crossover study in healthy, fasting egyptian male volunteers[J]. Drug Res (Stuttg), 2020, 70(2-03): 91-96.2020. [17] 2019 American Geriatrics Society Beers Criteria? Update Expert Panel. American geriatrics society 2019 updated ags beers criteria for potentially inappropriate medication use in older adults[J]. J Am Geriatr Soc, 2019, 67(4): 674-694. doi: 10.1111/jgs.15767 [18] ACOG. Committee opinion no. 767: Emergent therapy for acute-onset, severe hypertension during pregnancy and the postpartum period[J]. Obstet Gynecol, 2019, 133(2): e174-e180. [19] 蔡畅. 硝苯地平缓释片与硝苯地平控释片治疗原发性高血压患者的疗效对比[J]. 中国现代药物应用, 2019, 13(22): 149-151. https://www.cnki.com.cn/Article/CJFDTOTAL-ZWYY201922088.htm [20] 李茜娴. 硝苯地平缓释片与控释片治疗妊娠期高血压疗效对比探讨[J]. 现代诊断与治疗, 2019, 30(10): 1625-1627. https://www.cnki.com.cn/Article/CJFDTOTAL-XDZD201910020.htm [21] 刘静哲. 硝苯地平缓释片与硝苯地平控释片治疗原发性高血压的效果研究[J]. 中国医药指南, 2018, 16(27): 160-161. https://www.cnki.com.cn/Article/CJFDTOTAL-YYXK201827128.htm [22] 潘远安, 刘江红, 张志超, 等. 硝苯地平缓释片与硝苯地平控释片治疗高血压合并糖尿病的疗效比较[J]. 现代诊断与治疗, 2017, 28(7): 1225-1227. doi: 10.3969/j.issn.1001-8174.2017.07.032 [23] 孙海凤. 高血压患者选取硝苯地平缓释片与硝苯地平控释片治疗的疗效对比[J]. 临床医药文献电子杂志, 2018, 5(82): 75, 78. https://www.cnki.com.cn/Article/CJFDTOTAL-LCWX201882053.htm [24] 田凤莲, 肖忠琴. 硝苯地平缓释片与硝苯地平控释片治疗高血压的效果对比[J]. 医药前沿, 2019, 9(31): 58-59. https://www.cnki.com.cn/Article/CJFDTOTAL-ZWYY201922088.htm [25] 杨伟. 硝苯地平控释片对原发性高血压的血压控制效果[J]. 中国保健营养, 2019, 29(28): 112-113. https://www.cnki.com.cn/Article/CJFDTOTAL-YXLL202019021.htm [26] GAO Z, NGO C, YE W, et al. Effects of dissolution medium ph and simulated gastrointestinal contraction on drug release from nifedipine extended-release tablets[J]. J Pharm Sci, 2019, 108(3): 1189-1194. doi: 10.1016/j.xphs.2018.10.014 [27] 张继睿, 董阳雨, 韩清, 等. 聚维酮和共聚维酮为载体的硝苯地平渗透泵片的制备[J]. 药学研究, 2018, 37(7): 397-400. https://www.cnki.com.cn/Article/CJFDTOTAL-SDYG201807008.htm [28] 陈飞, 王超, 高昊. 推拉式渗透泵药物传递系统处方设计关键要素研究[J]. 中国药学杂志, 2019, 54(10): 783-789. https://www.cnki.com.cn/Article/CJFDTOTAL-ZGYX201910006.htm [29] 黄晓. 硝苯地平缓释片、控释片如何选择[N]. 家庭医生报, 2016-05-09(006). [30] 朱映华. 琥珀酸美托洛尔缓释片与酒石酸美托洛尔片治疗慢性心力衰竭临床疗效的meta分析[J]. 中国实用医药, 2018, 13(10): 108-109. https://www.cnki.com.cn/Article/CJFDTOTAL-ZSSA201810061.htm [31] 凡春红. 琥珀酸美托洛尔缓释片与酒石酸美托洛尔片治疗老年不稳定型心绞痛的效果观察[J]. 海峡药学, 2019, 31(5): 155-156. doi: 10.3969/j.issn.1006-3765.2019.05.076 [32] VINEREANU D, SPINAR J, PATHAK A, et al. Role of metoprolol succinate in the treatment of heart failure and atrial fibrillation: A systematic review[J]. Am J Ther, 2019. DOI: 10.1097/MJT.0000000000001043 [33] 于丽丽, 杨懿群, 刘禹宏, 等. 基于渗透压释药原理的混合骨架控释片研究[J]. 中国药业, 2017, 26(19): 9-13. doi: 10.3969/j.issn.1006-4931.2017.19.003 [34] 上海卡乐康包衣技术有限公司. 乙基纤维素干粉包衣的美托洛尔缓释多颗粒的稳定性评估[J]. 中国医药工业杂志, 2018, 49(8): 后插1-后插3. [35] 于红霞, 周珏, 唐珍凤. 酒石酸美托洛尔缓释片的制备[J]. 天津化工, 2016, 30(2): 39, 45. https://www.cnki.com.cn/Article/CJFDTOTAL-TJHG201602014.htm [36] MALIPEDDI V R, AWASTHI R, DUA K. Formulation and evaluation of controlled release ethylcellulose and polyethylene glycol microspheres containing metoprolol tartrate[J]. Interv Med Appl Sci, 2016, 8(2): 60-67. doi: 10.1556/1646.8.2016.2.6 [37] 刘泽华, 肖宛璐, 邸东华, 等. 易溶性药物酒石酸美托洛尔速释联合缓释片的制备[J]. 沈阳药科大学学报, 2016, 33(8): 604-608. https://www.cnki.com.cn/Article/CJFDTOTAL-SYYD201608003.htm [38] 龚健, 徐彦, 赖鹏, 等. 高端口服固体仿制药的设计及其产品关键质量属性的控制——以FDA批准的琥珀酸美托洛尔缓释片为例[J]. 药学进展, 2018, 42(9): 644-654. https://www.cnki.com.cn/Article/CJFDTOTAL-YXJZ201809002.htm [39] HIEW T N, TIAN Y H, TAN H M, et al. A mechanistic understanding of compression damage to the dissolubility of coated pellets in tablets[J]. Eur J Pharm Biopharm, 2020, 146: 93-100. doi: 10.1016/j.ejpb.2019.11.006 [40] MOHYLYUK V, PATEL K, SCOTT N, et al. Wurster fluidised bed coating of microparticles: Towards scalable production of oral sustained-release liquid medicines for patients with swallowing difficulties[J]. AAPS Pharm Sci Tech, 2019, 21(1): 3. doi: 10.1208/s12249-019-1534-5?utm_source=trendmd -
点击查看大图
表(1)
计量
- 文章访问数: 131
- HTML全文浏览量: 119
- PDF下载量: 7
- 被引次数: 0
