Oral Fast-Dissolving Technology Development

With the increasing demand for instant drug delivery system and the continuous improvement of drug safety and effectiveness, many new instant technology has appeared and developed continuously. 3D printing technology, freeze-drying technology, hot melt extrusion technology, electrospinning technology and other instant technology are used in the preparation of oral disintegrating tablets, oral instant dissolving film agent, instant dissolving granules and other dosage forms, which are favored by the majority of patients and show a good application prospect. BOC Sciences is committed to providing research and development services of oral medicine instant solution technology, aiming to bring more efficient, convenient and personalized drug solutions to the global pharmaceutical industry.

Advantages of oral fast-dissolving technology

The instant drug delivery system has the following advantages: without water and swallowing action, it can solve the problem of swallowing difficulty for children, the elderly and people with difficulty in accessing water; rapid release of drugs, rapid onset of action, providing a new dosage form for clinical emergencies; drug absorption through oral mucosa can avoid liver first-pass effect and improve oral bioavailability of drugs; improve patient compliance.

Fast-dissolving technology in oral disintegrating tablets

Oral disintegrating tablet is a new type of tablet with the advantages of rapid disintegrating, easy swallowing, good taste and no irritation to oral mucosa. The current preparation methods include tablet pressing, sublimation, molding, phase transformation, freeze drying, 3D printing and so on. The research of these techniques focuses on two important parameters that affect oral disintegrating tablets: disintegration time and mechanical strength. In recent years, the emergence of new disintegrating agents has promoted the application of tablet compression method in the study of oral disintegrating tablets. This kind of disintegrant has strong water absorption, swelling, fluidity, etc. It can eliminate the binding force caused by adhesives or high compression, improve the disintegration and mechanical strength of oral collapse tablets, and can be one of the research directions of disintegrating tablets in the future.

Freeze-dried technology

Freeze-drying technology is a drying method in which the water in the drug solution is removed by sublimation at low temperatures while the active ingredient is retained in a solid substrate. The preparation process is to mix gelatin, sucrose or other sugars, drugs and other ingredients (such as colorants) in liquid or semi-solid state, foam into the molded plate, after freeze-drying, solvent sublimation, tablets left in the film hole, directly sealed packaging. Freeze-drying is essentially a fluffy porous structure formed by chemicals and hydrophilic excipients, and the pill melts on the tip of the tongue in just a few seconds. The main characteristics of freeze-dried tablets are short disintegration time and good taste. This is due to the porous amorphous structure formed by the freeze-drying process and the selection of water-soluble auxiliary materials, which is conducive to the rapid disintegration of the tablet into fine particles, speeding up the dissolution of the drug while reducing the sense of gravel. In addition, freeze-drying technology gives freeze-dried tablets the characteristics of rapid disintegration and dissolution, which is conducive to the mucosal absorption of some fat-soluble drugs, so as to achieve the purpose of rapid onset of effect, while avoiding the liver first-pass effect and improving bioavailability. The low temperature and low pressure operating environment of freeze-drying technology can protect the physical and chemical properties of heat-sensitive substances from changing to a certain extent. Therefore, freeze-drying technology makes it possible to make proteins and biomacromolecules into oral preparations.

3D printing technology

3D printing is a rapid prototyping technology based on the principle of "layer-by-layer printing, layer-by-layer superposition", based on computer-aided design, and controlled by computer to directly prepare objects with special shapes or complex internal structures. The mouth collapse tablets prepared by 3D printing are formed by powder accumulation and curing, without compression process, so the tablets have high porosity, high internal surface area and fast disintegration. The unique manufacturing properties of 3D printing technology better balance the disintegration and mechanical properties of oral disintegrating tablets, increasing the hardness without affecting the disintegration. The technology can also produce geometric structures that cannot be obtained by traditional formulation technology, such as pyramid, cylinder, cube, sphere and ring, etc., to meet the drug needs of different populations. In addition, the special loading method of 3D printing dissolution spraying can flexibly and accurately control the position of the drug in the tablet; High accuracy of drug loading, can achieve personalized drug delivery.

Direct compression - co-processed disintegrants

The pressing method is to directly press the raw materials after mixing or press the tablets after pelleting. In order to achieve the purpose of rapid disintegration, it is necessary to add a certain amount of disintegrant. These disintegrants break the internal binding force of the tablet through capillary action, swelling action and wetting, and cause the tablet to disintegrate in water. By polyols, disintegrators or adhesives and other auxiliary materials according to a specific proportion, in a special preparation process such as spray drying, fluidized bed granulation, grinding, solvent volatilization, physical or chemical modification, etc., pre-mixed to form a new disintegrant with specific functions and uniform performance. Such disintegrators can maintain the chemical properties of each single excipient, aggregate the functions of each single excipient, and show better characteristics than physical mixtures, such as disintegration, fluidity, compressibility, etc. Therefore, premixed disintegrating agent has obvious advantages in promoting the disintegrating of oral disintegrating tablets and improving the mechanical strength, which has a certain promoting effect on the development of oral disintegrating tablets.

Fast-dissolving technology in oral instant film

As a new type of instant preparation, instant film has the advantages of large specific surface area, fast disintegration, good taste, easy to take, easy to transport, etc., and is favored by people with dysphagia.

Electrospinning technology

Electrospinning is a simple, fast and easy to industrialize micron and nano spinning technology. The instant film prepared by electrospinning technology has high specific surface area, porous and amorphous structure, and can disintegrate quickly. The wettability of the film agent and the capillary action between the internal fibers can accelerate the infiltration of water and promote the disintegration of the film. In addition, electrospinning technology can make the insoluble drug acetaminophen form a solid dispersion, and the drug dissolves 93.8% in 2 min, which significantly improves the dissolution rate

Hot melt extrusion (HME)

Hot melt extrusion is a simple, continuous production technology that does not require the addition of water or any solvent. The active ingredient is mixed with the thermoplastic film forming material and other auxiliary materials, and extruded under the condition of specific temperature and shear rate. The extruded material is extruded into film by the reverse rotating wheel.

Inkjet printing technology

Inkjet printing is the spraying of a drug-containing solution onto the surface of a blank film matrix through a nozzle. The instant film prepared by this technology can quickly melt in tens of seconds. Moreover, this special drug loading method can avoid the plasticizing or anti-plasticizing effect caused by the drug being dispersed in the matrix in a molecular state. Therefore, the mechanical properties and stability of the prepared instant film are better than that of the solvent casting method. In addition, inkjet printing can show good process reproducibility in future industrial scale-up production.

Flexible printing technology

Flexible printing is a technique in which an API is deposited on a blank polymer film by a series of rotating rollers to form an instant film. This technology can make the suspension of insoluble drugs uniformly distributed on the surface of the membrane without affecting the original characteristics of the blank film, such as disintegration and mechanical properties, so it has great advantages in preparing oral instant film of insoluble drugs. In addition, the flexible printing technology is a relatively stable process, API is almost unaffected by various stresses in the process of high-pressure shear mixing, solvent volatilization and heating, and can be used for the preparation of heat-sensitive drugs and biochemical products.

Advantages of the our oral fast-dissolving technology

• Professional team and advanced equipment
• Customized service
• Strict quality control
• Continuous technological innovation

As a new drug delivery method, oral fast-dissolving technology has broad application prospects. BOC Sciences' research and development services in this area cover a wide range of technical means, from freeze-drying technology to flexible printing technology, to meet the needs of different drugs. Through continuous technological innovation and optimization, we are committed to providing our customers with efficient, safe and personalized drug delivery solutions to promote the development of the biomedical field.

FAQ

1. How does oral fast-dissolving technology work?

Oral fast-dissolving formulations rapidly disintegrate or dissolve upon contact with saliva. The drug is then absorbed through the oral mucosa or gastrointestinal tract, leading to a swift onset of action.

2. What types of drugs can be formulated using oral fast-dissolving technology?

A wide range of drugs can be formulated, including:

• Analgesics
• Antipyretics
• Antihistamines
• Antiemetics
• Cardiovascular drugs
• CNS drugs
• Vitamins and supplements

3. What is lyophilization, and how does it contribute to fast-dissolving formulations?

Lyophilization, or freeze-drying, involves freezing the drug formulation and then sublimating the ice under vacuum. This process creates a porous matrix that dissolves rapidly in saliva, enhancing the disintegration rate of the formulation.

4. What is the process for developing oral fast-dissolving formulations at your company?

• Pre-formulation studies: Assessing the properties of the API and selecting suitable excipients and techniques.
• Formulation development: Using advanced technologies to create robust formulations.
• Analytical testing: Ensuring quality, safety, and efficacy through rigorous testing.
• Scale-up and manufacturing: Transitioning from small-scale to large-scale production while maintaining quality.
• Regulatory support: Assisting with regulatory submissions and approvals.

5. How do you ensure the quality and safety of oral fast-dissolving formulations?

We conduct thorough analytical testing, including dissolution testing, stability studies, and bioavailability assessment. Our facilities adhere to stringent good manufacturing practice (GMP) standards.

6. Can you customize oral fast-dissolving formulations for specific client needs?

Yes, we offer customized solutions tailored to the unique requirements of each drug and therapeutic application. We can develop fast-dissolving tablets, powders, or granules based on client specifications.

7. Are there any limitations to oral fast-dissolving technology?

While highly beneficial for many applications, oral fast-dissolving technology may not be suitable for drugs with high doses, those that require controlled release, or those that are highly unstable in the oral cavity.

8. How do you address the taste masking of bitter drugs in fast-dissolving formulations?

We utilize various taste-masking techniques, such as coating the drug particles, using sweeteners and flavoring agents, and employing complexation methods to enhance the palatability of the formulation.