Isomalt
(Synonyms: 异麦芽酮糖醇; Palatinitol) 目录号 : GC39392
Isomalt (Palatinitol) is a sugar alcohol used as an excipient in commercially available solid oral dosage forms. Isomalt stabilizes lactate dehydrogenase (LDH) moderately during freeze-drying.
Cas No.:64519-82-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Isomalt (Palatinitol) is a sugar alcohol used as an excipient in commercially available solid oral dosage forms. Isomalt stabilizes lactate dehydrogenase (LDH) moderately during freeze-drying.
[1] Anna-Kaisa Tuderman, et al. Int J Pharm. 2018 Mar 1;538(1-2):287-295. [2] Anna-Kaisa Koskinen, et al. Pharm Res. 2016 Jul;33(7):1752-68.
| Cas No. | 64519-82-0 | SDF | |
| 别名 | 异麦芽酮糖醇; Palatinitol | ||
| Canonical SMILES | O[C@H]([C@@H]([C@H]([C@@H](CO[C@@H]1[C@H](O)[C@H]([C@@H]([C@H](O1)CO)O)O)O)O)O)CO.O[C@H]([C@@H](CO[C@H]([C@@H]([C@@H](O)[C@@H]2O)O)O[C@@H]2CO)O)[C@H](O)[C@@H](CO)O | ||
| 分子式 | C12H24O11 | 分子量 | 344.31 |
| 溶解度 | Water: 250 mg/mL (726.09 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9044 mL | 14.5218 mL | 29.0436 mL |
| 5 mM | 0.5809 mL | 2.9044 mL | 5.8087 mL |
| 10 mM | 0.2904 mL | 1.4522 mL | 2.9044 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Design and Development of Agglomerated Isomalt
Int J Pharm Compd 2023 Jan-Feb;27(1):78-87.PMID:36720065doi
The objective of this study was to prepare agglomerated Isomalt by using the melt granulation process. This method involved the use of 99.5% of Isomalt with the meltable binder glyceryl monostearate in a concentration of 0.5%. Glyceryl monostearate has a melting point of 50°C to 55°C, therefore, glyceryl monostearate was melted at its melting point and Isomalt powder was blended with it to break the mass into agglomerates. The agglomerates were cooled to room temperature and were then screened to obtain granules of the desired size. The Fourier Transform Infrared Spectroscopy studies confirmed that the chemical structure of Isomalt was not changed before and after the melt granulation process. A differential scanning calorimetry study showed that there was no appearance of more new peaks or disappearance of one or more peaks corresponding to those of the Isomalt powder and agglomerated Isomalt, which showed no changes in the structure of the Isomalt powder before and after the agglomeration process. The agglomerated Isomalt and galenIQ 721 showed almost identical solubility profiles for g of solute per 100 g of solution at different temperatures. The scanning electron microscopy analysis of agglomerated Isomalt showed promising results for the preparation of agglomerates of Isomalt with glyceryl monostearate. The flow properties of the agglomerated Isomalt compared with the galenIQ 721 and pure Isomalt powder and melt granulation process showed promising results for agglomerated Isomalt. The melt granulation process showed promising results to prepare agglomerates of the Isomalt with the meltable binder glyceryl monostearate.
Isomalt and its diastereomer mixtures as stabilizing excipients with freeze-dried lactate dehydrogenase
Int J Pharm 2018 Mar 1;538(1-2):287-295.PMID:29341910DOI:10.1016/j.ijpharm.2018.01.015.
The purpose of this research was to study Isomalt as a protein-stabilizing excipient with lactate dehydrogenase (LDH) during freeze-drying and subsequent storage and compare it to sucrose, a standard freeze-drying excipient. Four different diastereomer mixtures of Isomalt were studied. The stability of the protein was studied with a spectrophotometric enzyme activity test and circular dichroism after freeze-drying and after 21 days of storage at 16% RH. Physical stability was analyzed with differential scanning calorimetry and Karl Fischer titration. Statistical analysis was utilized in result analysis. LDH activity was almost completely retained after freeze-drying with sucrose; whereas samples stabilized with Isomalt diastereomer mixtures had a considerably lower protein activity. During storage the sucrose-containing samples lost most of their enzymatic activity, while the Isomalt mixtures retained the protein activity better. In all cases changes to protein secondary structure were observed. Isomalt diastereomer mixtures have some potential as protein-stabilizing excipients during freeze-drying and subsequent storage. Isomalt stabilized LDH moderately during freeze-drying; however it performed better during storage. Future studies with other proteins are required to evaluate more generally whether Isomalt would be a suitable excipient for pharmaceutical freeze-dried protein formulations.
Compaction properties of Isomalt
Eur J Pharm Biopharm 2009 Aug;72(3):621-5.PMID:19327398DOI:10.1016/j.ejpb.2009.03.005.
Although other polyols have been described extensively as filler-binders in direct compaction of tablets, the polyol Isomalt is rather unknown as pharmaceutical excipient, in spite of its description in all the main pharmacopoeias. In this paper the compaction properties of different types of ispomalt were studied. The types used were the standard product sieved Isomalt, milled Isomalt and two types of agglomerated Isomalt with a different ratio between 6-O-alpha-d-glucopyranosyl-d-sorbitol (GPS) and 1-O-alpha-d-glucopyranosyl-d-mannitol dihydrate (GPM). Powder flow properties, specific surface area and densities of the different types were investigated. Compactibility was investigated by compression of the tablets on a compaction simulator, simulating the compression on high-speed tabletting machines. Lubricant sensitivity was measured by compressing unlubricated tablets and tablets lubricated with 1% magnesium stearate on an instrumented hydraulic press. Sieved Isomalt had excellent flow properties but the compactibility was found to be poor whereas the lubricant sensitivity was high. Milling resulted in both a strong increase in compactibility as an effect of the higher surface area for bonding and a decrease in lubricant sensitivity as an effect of the higher surface area to be coated with magnesium stearate. However, the flow properties of milled Isomalt were too bad for use as filler-binder in direct compaction. Just as could be expected, agglomeration of milled Isomalt by fluid bed agglomeration improved flowability. The good compaction properties and the low lubricant sensitivity were maintained. This effect is caused by an early fragmentation of the agglomerated material during the compaction process, producing clean, lubricant-free particles and a high surface for bonding. The different GPS/GPM ratios of the agglomerated Isomalt types studied had no significant effect on the compaction properties.
Physical Stability of Freeze-Dried Isomalt Diastereomer Mixtures
Pharm Res 2016 Jul;33(7):1752-68.PMID:27059921DOI:10.1007/s11095-016-1915-3.
Purpose: Isomalt is a sugar alcohol used as an excipient in commercially available solid oral dosage forms. The potential of Isomalt as a novel freeze-drying excipient was studied in order to increase knowledge of the behavior of Isomalt when it is freeze-dried. Methods: Isomalt was freeze-dried in four different diastereomer compositions and its physical stability was investigated with differential scanning calorimetry, Fourier-transform infrared and Raman spectroscopy, X-ray powder diffraction, Karl-Fischer titration and thermogravimetric analysis in order to verify the solid state form of Isomalt after freeze-drying and observe any changes occurring during storage in three different relative humidity conditions. Results: Isomalt was successfully transformed into the amorphous form with freeze-drying and three diastereomer combinations remained stable as amorphous during storage; one of the diastereomer compositions showed signs of physical instability when stored in the highest relative humidity condition. The four different crystalline diastereomer mixtures showed specific identifiable solid state properties. Conclusions: Isomalt was shown to be a suitable excipient for freeze-drying. Preferably a mixture of the diastereomers should be used, as the mixture containing only one of the isomers showed physical instability. A mixture containing a 1:1 ratio of the two diastereomers showed the best physical stability in the amorphous form.
Spray-dried amorphous Isomalt and melibiose, two potential protein-stabilizing excipients
Int J Pharm 2016 Aug 20;510(1):311-22.PMID:27321131DOI:10.1016/j.ijpharm.2016.06.038.
The possibility of producing amorphous Isomalt and melibiose by spray drying was studied. The impact of process parameters on yield and solid-state stability was compared to sucrose and trehalose. All powders remained amorphous during 2-3 weeks. Processing was challenging due to powder stickiness. Low-temperature and low-humidity drying processes generally performed best. Most Isomalt and sucrose powder was retrieved when using 60°C inlet temperature, 800L/h atomizing rate, 1.4ml/min feed rate, 15% concentration and 100% aspirator rate, giving 42-43°C outlet temperature. Isomalt was the most problematic, because it had the lowest Tg and became sticky very easily, therefore process parameters needed to be precisely balanced. There was more freedom in designing processes for melibiose but best yields were obtained with low-temperature (50°C inlet temperature, 800L/h atomizing rate, 4.9ml/min feed rate, 10% concentration and 100% aspirator, 39°C outlet temperature). Trehalose was different in that higher temperatures resulted in better yields. Yet, trehalose generally contained the highest moisture contents. The possibility to produce amorphous Isomalt and melibiose at low-temperature process conditions makes them promising considering spray drying applications for heat-sensitive proteins. Melibiose is a better candidate than Isomalt because of easier processability and superior solid-state stability.