Sustained and Controlled Release Technology Research
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Sustained and Controlled Release Technology Research

Although common drug preparations are widely used, they have many shortcomings such as large fluctuations in blood drug concentration, strong drug toxicity and side effects, many times of administration, and inconvenient drug use. As the third generation preparation, sustained and controlled release preparations promote the rapid development of the preparation industry as a whole, and can achieve constant or non-constant drug release according to specific requirements, effectively maintain stable blood drug concentration, and avoid the phenomenon of "peak and valley". Improve drug safety and patient adaptability. BOC Sciences is committed to providing advanced drug sustained-release technology research and development services to help drug developers take the lead in a highly competitive market.

What is sustained and controlled release technology?

Sustained release (SR) technology: The drug can be continuously released for a long time to achieve a long-term effect, and the drug release is mainly a first-order rate process. By releasing the drug slowly and steadily, SR formulations reduce the need for frequent medication, improve patient compliance, and maintain the therapeutic level of the drug.

Controlled release (CR) technology: The drug can be automatically released at a predetermined speed within a predetermined time, so that the blood concentration is maintained within the effective concentration range for a long time, and the drug release is mainly at zero or near zero rate within a predetermined time.

Our sustained and controlled release techniques research

Skeleton sustained and controlled release preparation

A skeleton sustained release preparation is made by combining a drug with one or more inert solid skeleton materials through a specific process such as pressing or fusion. The skeleton type of controlled release preparation is a type of diffusion controlled release system, which releases the drug according to the first order process. According to different skeleton materials, it can be divided into hydrophilic gel skeleton preparation, insoluble skeleton preparation and dissolved skeleton preparation.

Hydrophilic gel skeleton: Hydrophilic gel skeleton sustained and controlled release preparation uses hydrophilic polymer as the skeleton material, which expands after contact with water or digestive fluid, etc., to produce a solid gel layer on the surface of the tablet. Controlled release of the drug is achieved through diffusion in the gel layer and dissolution of the gel layer.

Insoluble skeleton: When the skeleton pores of insoluble skeleton tablets permeate the digestive fluid, the drug dissolves and slowly diffuses, and the drug release characteristics of this type of preparation meet the "rate-limited release" drug release characteristics. There are many methods for the preparation of insoluble skeleton tablets, usually the drug and insoluble skeleton materials are first made into particles, and then pressed into tablets. Preparation methods include:

  • Organic solvents (such as acetone, ethanol, isopropyl alcohol and dichloromethane) are used as wetting agents for granulation.
  • The use of organic solvent soluble skeleton material solution (such as ethyl cellulose ethanol solution) or part of the polymer material dissolved in organic solvent as a binder granulation.
  • The organic solution of the skeleton material is supplemented with other polymers (such as polyethylpyrrolidone) as wetting agents for granulation.
  • The drug is dissolved in the organic solvent for the wetting agent granulation.
  • Dissolve the drug in the solution containing the skeleton material, the solid dispersion of the drug in the skeleton material is obtained after the solvent is evaporated, and the tablet is crushed and granulated.
  • Add a certain amount of skeleton material powder to the drug particles, mix evenly and press directly.

Corrosion type skeleton: After being dissolved, wax substances or inert fats are generated, which achieve drug release through corrosion or related pore diffusion, and the drug can be released from the skeleton, and the skeleton is dissolved, and the preparation of such slow release preparations can be directly combined with the drug and the polymer through chemical bonding, or the expansion type controlled release skeleton can be used. Preparation methods include:

  • Water dispersion method adopts solvent evaporation technology, adding the solution or dispersion of the drug and excipients into the molten waxy phase, then evaporating away the solvent, drying and mixing into a lump and then granulosa. The drug release rate of all kinds of biodissolved matrix tablets prepared with water dispersible tablets is faster, which may be related to the water contained on the surface of drug particles and inside the skeleton.
  • The solidification method adopts the melting technology, the drug and auxiliary materials are directly added to the molten wax, the temperature is controlled slightly higher than the melting point of wax about 90℃, the molten material is spread condensation, solidification, crushing, or poured into a rotating dish to make flakes, and then ground and sifted to form particles. In the absence of an additive, drug release is prolonged and non-linear, with apparent zero-order release when PVP or polyethylene lauryl ether is added.
  • The drug was mixed with hexadecyl alcohol at a temperature of 60℃ by hot mixing method, and the clumps were granulated with zein alcohol solution. The release performance of the tablets obtained by this method was stable.

Osmotic pump system technology

The osmotic pump controlled release preparation is made by using the principle of osmotic pump and laser technology to release the drug at zero order kinetic uniform constant speed. It is free from the influence of physiological variables such as gastrointestinal movement and medium environment pH, maintains stable drug plasma concentration, provides a consistent release curve independent of gastrointestinal conditions, effectively reduces drug side effects and administration frequency, and improves drug safety and effectiveness.

Microencapsulation technology

By encapsulating drugs in biodegradable polymers, we create microcapsules and microspheres with sustained and controlled release capabilities. Techniques such as solvent evaporation, condensation and spray drying are used to achieve the desired release characteristics.

Nanoparticle and liposome formulations

Development of nanoparticle and liposome based delivery systems that provide targeted and sustained release. These systems improve drug bioavailability and therapeutic effectiveness while reducing systemic side effects.

In situ gel systems technology

These novel formulations gelate when administered, forming a reservoir at the injection site. The reservoir releases the drug in a controlled manner over an extended period of time, making it ideal for long-term treatment.

Our sustained and controlled release formulation development include:

  • Tablets

Skeleton tablets: Hydrophilic gel skeleton tablets, dissolve skeleton tablets, insoluble skeleton tablets, bioadhesive tablets, multilayer tablets, colon positioning tablets, etc.

Film coated tablets: Enteric-coated tablet, microporous diaphragm.

Osmotic pump tablets: Add electrolytes or organic acids to produce osmotic pressure.

Gastric hysteresis tablets: Mainly gastric floating tablets, and the prescription adds MgCO3, NaHCO3, high alcohol or wax to increase buoyancy.

Multilayer tablets: Quick-release and sustained-release or compound ingredients.

  • Capsules

It mainly refers to multi-particle preparations, which are divided into membrane control type, skeleton type, and the combination of membrane control and skeleton technology.

  • Liquid preparations

Sustained-release suspension, sustained-release emulsion, sustained-release gel.

Advanced characterization and analysis techniques

The development of sustained-release and controlled-release formulations requires rigorous characterization and analytical testing to ensure optimal performance and safety. Our advanced analytical capabilities include:

In vitro release testing: We study the release curves of our formulations using a variety of techniques, including USP dissolver, Franz diffusion cell and dialysis. These tests provided important insights into the release dynamics and mechanisms of our agents.

Stability studies: It is essential to ensure the stability of our formulations under different storage conditions. We conduct accelerated and long-term stability studies in accordance with ICH guidelines to evaluate the shelf life and performance of our products.

Pharmacokinetic (PK) and pharmacodynamic (PD) studies: Through in vivo studies, we evaluate the pharmacokinetic and pharmacodynamic profiles of our agents. These studies help us understand the absorption, distribution, metabolism, and excretion of drugs (ADME) and their therapeutic effects.

Physicochemical properties: Using advanced techniques such as scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray diffraction (XRD), we characterize the physical and chemical properties of formulations. This ensures consistency, quality and performance.

Cutting-edge technology and equipment

Hot melt extrusion: This technique is used to form a solid dispersion of the drug in a polymer matrix, thereby enhancing solubility and controlled release properties.

Supercritical fluid technology: Used in particle engineering and microencapsulation, this technology allows precise control of particle size, morphology, and encapsulation efficiency.

3D printing: This innovative technology enables the manufacture of complex, patient-specific drug delivery systems with precise control of drug release curves.

Spray drying and coating: These techniques are used to produce uniform particles and coatings that improve drug stability and release characteristics.

Advantages of our sustained and controlled release technology

Enhanced treatment: Maintain optimal drug concentrations in the blood through the development of advanced formulations to improve treatment outcomes and reduce the frequency of medication.

Improved patient compliance: Improved patient adherence to treatment regimens by reducing the frequency of dosing and minimizing side effects.

Reduced side effects: Controlled drug release minimizes the risk of peak-related side effects, ensuring a more consistent and safer treatment regimen.

Customization and flexibility: Offers a customized approach to developing formulations that meet specific treatment needs and patient requirements.

Regulatory expertise: Our comprehensive regulatory support ensures that the regulatory process runs smoothly, speeding time to market.

FAQ

1. What types of drugs can benefit from sustained-release and controlled-release technologies?

A wide range of drugs can benefit from these technologies, including:

  • Small molecules
  • Peptides and proteins
  • Nucleic acids
  • Hormones
  • Vaccines

2. What are the common methods used in sustained and controlled release formulations?

  • Polymer-based systems: Using hydrophilic or hydrophobic polymers to control drug release.
  • Osmotic pump systems: Utilizing osmotic pressure to drive drug release.
  • Microencapsulation: Encasing drugs in biodegradable polymers for controlled release.
  • Nanoparticles and liposomes: Using nanotechnology for targeted and sustained drug delivery.
  • In situ gelling systems: Formulations that gel upon administration, creating a drug depot for controlled release.

3. Can you customize sustained and controlled release formulations for specific needs?

Yes, we offer tailored solutions to meet specific therapeutic needs and patient requirements. Our approach allows us to develop customized formulations that achieve the desired release profiles and therapeutic outcomes.

4. How can I get more information or start a project with your company?

For more information or to discuss your specific needs, please contact us. We are committed to providing innovative and effective drug delivery solutions and look forward to collaborating with you on your next project.