Application of micro-nano laser particle size analysis technology in drug preparation research and industrialization

Application of micro-nano laser particle size analysis technology in drug preparation research and industrialization
The pharmaceutical dosage form is the form in which the drug is present and administered to the body. The pros and cons of pharmaceutical preparation technology mark the level of a country's medical and medical science. The research and application of this technology plays an extremely important role in medical practice and industrial practice, and plays a role in promoting the advancement of medical and pharmaceutical science. In recent years, as new pharmaceutical preparations have become the growth point of the pharmaceutical industry, the sales of new drug delivery systems worldwide have steadily increased, accounting for more than 10% of the entire pharmaceutical market. The new concept of treatment has promoted the development of new drug delivery systems, and new technologies have promoted the launch of new formulation products. The laser particle size analyzer plays an increasingly important role in the research and production of pharmaceutical preparations, and is valued by engineers and technicians and drug inspectors who are quality control in the research and production process of pharmaceutical preparations. The following is a discussion of the application of particle laser detection technology in the research and production of new formulations.

First, the microcapsule:
Microencapsulation technology is a technology that is developing rapidly, versatile and mature in the world today. The process of preparing microcapsules is called microencapsulation, which encapsulates a solid, liquid or gas in a tiny capsule. The particle size of the microcapsules varies depending on the preparation process and the use. Theoretically, microcapsules of 0.1 to 1000 nm can be prepared, thereby having micron microcapsules and nanometer nanocapsules. There are three types of preparation of microcapsules: physical and chemical methods, physical and mechanical methods, and chemical methods. Among them, the phase separation process in physical and chemical methods has become one of the main processes of microencapsulation of drugs. The process still involves some quantitative problems that cannot be quantitatively studied and is difficult to accurately evaluate, such as the ubiquitous microcapsule adhesion and aggregation problems. Products obtained by similar processes vary widely in particle size range and release data. With the LS laser particle measurement method, the particle size and distribution of the sample can be observed relatively intuitively, and the more concentrated the distribution, the more uniform the representation (Fig.). This test reveals whether the process is reasonable and rigorous. Whether the sensitivity of the microencapsulation reaction is appropriate, and small changes in conditions can cause controllability in the case of significant effects. For example, a process in which gelatin is used as a capsule.
Capsule material\/
↓
Suspension (or emulsion)
↓
Coagulation sac laser particle detection point → ↓Diluent ↓ Settling sputum -→→ ↓
Curing capsule
The concentration of the diluent used in the microcapsules→formulation is too high or too low to cause the coacervate to adhere to agglomerates or dissolve.
2. Microspheres Microspheres refer to microparticle dispersions in which a drug is dispersed or adsorbed in a polymer matrix. The drug can be dissolved or dispersed in the base layer of the polymer material to form a solid skeleton of the base layer type microspherical entity. The particle size is generally from 1 to 300 μm, or even larger. In addition, a solid drug or a liquid drug is encapsulated into a capsule-type microcapsule, which is called a microcapsule. There is no strict distinction between the two. The size of the microspheres varies from 0.01 to 700 μm. The detection method is laser granulometry and Coulter counter method in addition to microscopy and electron microscopy. Laser particle size analysis is more extensive than the first two methods. The microscope is limited to the field of view, and the range observed by the electron microscope is smaller, and the morphology of the particles can only be observed more finely. From the perspective of formulation research and production, laser particle size analysis and Coulter calculation method can better guide the process and reflect the quality.

Third, powder (powderinhalation)
A powder spray is a drug delivery system that delivers systemic or local effects in a dry powder form after being administered by a special drug delivery device. It has a targeted, high-efficiency, quick-acting, toxic side effect. Small and other characteristics. According to the different parts of the medication, it can be divided into nasal powder and oral (pulmonary inhalation) powder. The characteristics of the powder are: 1 no gastrointestinal degradation; 2 no liver first pass effect; 3 rapid drug absorption, rapid onset after administration; 4 bioavailability of macromolecular drugs can be through absorption enhancers or other methods Application: 5 small molecule drugs are especially suitable for direct inhalation or injecting into the respiratory tract; 6 drugs directly into the circulation after absorption, to achieve the purpose of systemic treatment; 7 can be used for water-soluble drugs that are difficult to absorb in the gastrointestinal tract; 8 patients with good compliance, especially suitable for patients who need to be treated with long-term injection; 9 drugs with local effects, the dosage is significantly reduced, and the side effects are less. Different dosing sites have different requirements on the particle size. For example, the lung inhalation powder requires the main drug particle size to be less than 5 μm, and the nasal powder particle size should be 30 to 150 μm. The quality study of powder is a particle quality check. The main inspection of particle size distribution, particle morphology, and determination of these items, is more suitable with the LS laser particle size analyzer.
Fourth, the size and distribution of liposomes Liposomes particle size and distribution uniformity is related to its encapsulation efficiency and stability, directly affecting the behavior and disposal of liposomes in the body tissues. The particle size of the liposome is less than 100 nm, and the blood circulation time is longer. If the particle size of the liposome is more than 200 nm, the liposome is easily phagocytized by the macrophages as foreign foreign matter, and the circulation time of the liposome in the body. very short. There are many factors affecting the size and distribution of liposomes. It can be said that all factors affecting the stability of liposome aggregation are related to the particle size and distribution of liposomes. The liposome test can quickly and easily display the particle size of the liposome by laser particle size analysis. The average particle size and the median particle size can be measured. The distribution map can determine whether the particles are uniform and stable.

5. Liposomal ophthalmic drug system Liposomes are used as ocular drug delivery systems. The constituent materials are phospholipid bilayer membranes, similar to biofilms, which are easy to fuse with organisms and promote the penetration of drugs into biofilms. The trans-corneal transport efficiency of the external eye drops is relatively high; by selecting different preparation methods, the liposome has a particle size of 0.02 to 5 μm, and there is no foreign body sensation in the eye, which does not affect the normal physiological function of the eye.
The preparation of liposome ophthalmic administration systems is similar to that of general liposomes. Quality Control—Using a laser particle size analyzer should be sampled and analyzed after homogenization.
6. New emulsion stability emulsions are two immiscible liquids which are emulsified by a surfactant to disperse one liquid in another to form a non-uniform micro or nano dispersion system. Microscopic examination of the emulsion is carried out in this range, and the size and distribution of the emulsion microparticles can be determined by using a laser particle size analyzer. The size and number of particles in each particle diameter interval can be analyzed through 116 analysis channels; the particle distribution and uniformity can be observed through the particle distribution map; commonly used technical parameters can also be collected by using the distribution chart statistics table.
7. Nanoparticles Generally, the particle size of nanoparticles is defined in the range of 1 to 1000 nm. Nanoparticles that have been studied include polymer nano and nanospheres, drug bodies, lipid nanoparticles, nanoemulsions, and polymer capsules.
For example, the oil phase can be obtained by using liquid paraffin to obtain an average particle diameter of 820 nm.
The cotton seed oil has an average particle diameter of 560 nm.
Summary: With the rapid development of pharmaceutical preparation technology, new preparations are gradually transferred from laboratories to pharmaceutical production enterprises. The application of laser particle size analysis in process control and drug quality control is also becoming more and more important. Understanding and mastering laser particle size analysis methods will welcome us in the new era of pharmaceutical preparations.
This article is taken from the official website of Jinan Weiner Jinan Micro-Nano Particles Instrument Co., Ltd.

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