Why is mannitol becoming more and more popular as a pharmaceutical excipient in solid dosage forms?

被引:125
作者
Ohrem, H. Leonhard [1 ]
Schornick, Eva [1 ]
Kalivoda, Adela [1 ]
Ognibene, Roberto [1 ]
机构
[1] Merck KgaA, D-64293 Darmstadt, Germany
关键词
binder; direct compression; excipients; filler; incompatibility; mannitol; solid oral dosage forms; stability; tablet; LACTOSE; INTOLERANCE; COMPACTION; MALABSORPTION; ADSORPTION; BEHAVIOR; TABLETS; SUGAR; DRUGS;
D O I
10.3109/10837450.2013.775154
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Various fillers/binders which are applied for the formulation of solid oral dosage forms are assessed for their benefits and drawbacks, including lactose, sorbitol, mannitol, microcrystalline cellulose and calcium hydrogen phosphate dihydrate. A focus of this work was to evaluate the application of mannitol in comparison to other common fillers/binders as it was observed that this excipient is gaining more and more attention in pharmaceutical formulation development and production. While one of the main advantages of conventional fillers/binders such as lactose, microcrystalline cellulose and calcium hydrogen phosphate dihydrate is their low price level, mannitol excels regarding its physicochemical characteristics such as a low hygroscopicity, a strong inertness towards both the API and the patient's body, its good compactibility and the ability to produce extremely robust tablets. Additionally, the suitability of mannitol for the emerging formulation technology of orally disintegrating tablets is pointed out. In summary, it is emphasized that the selection of the filler/binder is highly individual, depending, for example, on the preferred characteristics of the final solid dosage form, the applied API and the available budget. However, mannitol exhibits many strong advantages which can be expected to result in a more widespread application in the near future.
引用
收藏
页码:257 / 262
页数:6
相关论文
共 42 条
[1]   Adsorption of ketotifen onto some pharmaceutical excipients [J].
AlNimry, SS ;
Assaf, SM ;
Jalal, IM ;
Najib, NM .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1997, 149 (01) :115-121
[2]  
[Anonymous], HDB DIABETES MED NUT
[3]  
[Anonymous], 2003, Stability testing of New Drug Substances and Products
[4]   Effect of spray-dried mannitol on the performance of microcrystalline cellulose-based wet granulated tablet formulation [J].
Badawy, Sherif I. F. ;
Shah, Keyur R. ;
Surapaneni, Madhu S. ;
Szemraj, Marta M. ;
Hussain, Munir .
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY, 2010, 15 (04) :339-345
[5]  
BEDINE MS, 1973, GASTROENTEROLOGY, V65, P735
[6]  
Bharate S., 2010, Journal of Excipients and Food Chemicals, V1, P3, DOI DOI 10.1016/J.INDCROP.2015.11.088
[7]   Excipients for direct compaction - an update [J].
Bolhuis, GK ;
Armstrong, NA .
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY, 2006, 11 (01) :111-124
[8]   Carbohydrate malabsorption in patients with non-specific abdominal complaints [J].
Born, Peter .
WORLD JOURNAL OF GASTROENTEROLOGY, 2007, 13 (43) :5687-5691
[9]  
BRANDSTETTER RD, 1986, NEW ENGL J MED, V315, P1613
[10]   PHYSICAL AND CHEMICAL-PROPERTIES OF CALCIUM PHOSPHATES FOR SOLID-STATE PHARMACEUTICAL FORMULATIONS [J].
CARSTENSEN, JT ;
ERTELL, C .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1990, 16 (07) :1121-1133