Powder packaging in compatibility research of auxiliary materials
ChemPlus ® Application Report of Desktop Solid Sampling Instrument
Research Background
RESEARCH BACKGROUND
The study of compatibility between raw materials and excipients is an important stage before the development of formulations. Due to potential physical, chemical, and biological interactions between raw materials and excipients that can affect the absorption and safety of formulations in vivo, it is necessary to determine the optimal prescription composition during pre prescription research. The study of compatibility between raw materials and excipients plays four important roles in the development of formulations:
Can maximize the stability of the dosage form;
Can help researchers understand possible reactions before determining the final dosage form;
The compatibility of raw materials and excipients is essential for the application of new drug clinical trials (IND);
The final list of excipients that can be used for prescription can be determined.
research process
RESEARCH PROCESS
Various medicinal excipients to be used in prescription research should be physically mixed with active pharmaceutical substances one by one, and accelerated tests should be conducted under high temperature, high humidity, and strong light conditions. The selection of test conditions should reflect the key quality attribute indicators of the formulation. The ratio of main drug and excipient components in the test should be able to reflect the changes in the formulation ratio. For example, after pre mixing and screening based on different functional excipient ratios in the prescription, the ratio of main drug to excipient should be set to 1:5 (diluent), 3:1 (adhesive, disintegrant), 5:1 (lubricant), and 10:1 (coloring agent). Take a certain amount and lay it out under high temperature, high humidity, and light conditions to study whether new impurities are generated under the above conditions.
The experimental research methods for the compatibility between medicinal excipients and medicinal chemistry are usually as follows: in the study of raw material excipient compatibility, a large number of parallel experiments are required, and a large number of raw materials and excipients are weighed and proportioned. Repetitive weighing operations will consume a lot of time and energy for researchers. For this research and development scenario, high-throughput automated solid-state sampling technology can free up researchers, fully improve research and development efficiency, and ensure the repeatability and consistency of experimental results, avoiding manual experimental errors.
ChemPlus ® Desktop solid sampler
ChemPlus ® Desktop solid sampling device, supporting multiple solid raw materials and receiving containers, without the need for manual supervision, automatically completes repetitive and time-consuming solid weighing and sampling operations.
Its characteristics include:
High throughput: can accommodate various solid raw materials and receiving containers, comprehensively improving efficiency;
Wide applicability: The sample does not require special treatment and covers powders that are hygroscopic, agglomerated, large particles, fluffy, and have poor flowability;
Intelligent algorithm parameter adjustment: adaptive powder addition algorithm, intelligent recognition of multiple types of powders;
Piezoelectric ceramic excitation technology: smoother powder extraction for multiple types of powders;
Static electricity removal: effectively reduces static electricity effects, and adds samples more accurately;
Cost controllable: Low consumable prices, cost savings;
Small footprint: Small overall size, desktop style;
Wide compatibility: compatible with various laboratory commonly used small bottle sizes;
Data tracking: barcode or QR code sample management, supporting audit tracking;
Easy interactive software: Visual operation software, easy to use.
Automated testing results
RESULT
For the research scenario of compatibility between raw materials and auxiliary materials, multiple commonly used powder samples in auxiliary material research were selected, and each sample amount of each powder was tested 6 times. The actual test results are shown in the table below:
| Powder sample |
Target sample size (mg) |
Actual sample dosage (mg) |
standard deviation |
Average sample addition time (s) |
| Low substituted methylcellulose |
500.0 |
500.0 |
0.1 |
68 |
| Low substituted methylcellulose |
800.0 |
799.9 |
0.1 |
77 |
| Microcrystalline cellulose 102 |
500.0 |
499.9 |
0.1 |
181 |
| Microcrystalline cellulose 102 |
800.0 |
799.9 |
0.1 |
262 |
| sodium carboxymethyl starch |
500.0 |
500.0 |
0.1 |
55 |
| sodium carboxymethyl starch |
800.0 |
799.9 |
0.1 |
82 |
| Hydroxypropyl methylcellulose |
500.0 |
500.0 |
0.1 |
70 |
| Hydroxypropyl methylcellulose |
800.0 |
799.9 |
0.1 |
80 |
| Povidone K30 |
500.0 |
500.0 |
0.1 |
96 |
| Povidone K30 |
800.0 |
800.0 |
0.1 |
84 |
| maltodextrin |
500.0 |
499.8 |
0.4 |
100 |
| Calcium hydrogen phosphate dihydrate |
800.0 |
800.0 |
0.1 |
133 |
| Calcium hydrogen phosphate dihydrate |
500.0 |
499.9 |
0.1 |
77 |
| Calcium hydrogen phosphate dihydrate |
800.0 |
800.1 |
0.1 |
70 |
| Lactose 80 |
500.0 |
500.0 |
0.1 |
151 |
| Lactose 80 |
800.0 |
799.9 |
0.1 |
263 |
From the test results, it can be seen that, ChemPlus ® Suitable for automated weighing of various auxiliary powder materials, it can balance weighing efficiency and accuracy at a sample dosage of one hundred milligrams. Most samples can be weighed within 2 minutes, with a weighing error of less than ± 0.5mg, which can meet the needs of experiments.
Conclusion
IN CONCLUSION
ChemPlus ® It is a compact desktop solid sampler that can efficiently perform repetitive and time-consuming powder weighing operations in the study of raw material excipient compatibility. ChemPlus ® Capable of handling various powders, covering larger particles, fluffy, and poorly flowable powders. And ChemPlus ® Support adaptive powder addition algorithm, intelligent recognition of multiple types of powders, without the need to set or optimize sample parameters for specific powders, which can fully improve research and development efficiency in the compatibility study of raw materials and auxiliary materials.