Oral Solid Dosage Form Development

The pharmaceutical industry is constantly evolving to meet the growing demand for effective, safe, and patient-friendly medicines. Among various pharmaceutical formulations, the oral solid dosage form (OSDF) has received a lot of attention due to its stability, ease of administration, patient compliance, and cost-effectiveness. OSDF includes tablets, capsules, pills, pellets and powder pharmaceutical preparations. BOC Sciences is committed to providing high quality, customized oral solid dosage form development services to its customers.

Advantages of oral solid dosage forms

Patient friendliness and compliance

With its convenient dosing mode, portability, and low requirements for specific storage conditions, OSDF significantly improves patient compliance. Especially in tablet and capsule form, patients can easily carry and self-administer without relying on medical assistance, greatly enhancing the feasibility of treatment options.

Excellent stability performance

Compared to liquid preparations, OSDF shows better stability and longer shelf life. Solid formulations are designed to avoid the potential damage of the Active Pharmaceutical Ingredients (API) by environmental factors such as temperature, humidity and light, ensuring the long-term effectiveness of the drug.

Controlled release characteristic

With the help of cutting-edge formulation technology, OSDF with controlled release or sustained release function came into being. These advanced formulations release APIs at a preset rate and maintain a constant blood concentration, extending treatment effectiveness while reducing the inconvenience of frequent dosing and optimizing the patient experience.

Cost efficiency advantage

OSDF is often more economical in production and packaging, and is less expensive to manufacture than liquid or injectable forms. Coupled with the stability advantage of OSDF, the dependence on high storage and transportation conditions is greatly reduced, and cost savings are realized along the supply chain.

Oral solid dosage form development process

Selection of excipients

The selection of excipients is the first step in preparation development, and its importance should not be underestimated. It is not only related to the stability and bioavailability of apis, but also directly affects the manufacturability of the preparation and the safety of the final product. In this process, we carefully examine the physicochemical properties of the API, combined with the target release curve and the regulatory framework, and select the most preferred items from the massive excipients database. Our consideration of excipients is not limited to their chemical compatibility, but also focuses on their functionality in actual production, ensuring that the final formulation can meet the needs of drug release, but also adapt to large-scale production, providing a consistent and reliable treatment experience for patients.

Customized oral solid dosage form formulation

Our services go beyond simple formulations to deeply customised designs based on the unique characteristics and market needs of the drug. From the selection of active ingredients to the precise calculation of the proportion of excipients, every step involves the utmost attention to detail. We focus not only on the immediate efficacy of drugs, but also on their long-term safety and stability, ensuring that patients can get both efficient and peace of mind treatment.

Tablets: Our tablet development covers the full range from basic to advanced, including regular, sustained-release and controlled-release tablets. Using cutting-edge granulation technologies such as wet granulation, dry granulation and fluidized bed granulation, we ensure uniform drug distribution and rapid disintegration, paving the way for increased bioavailability. Especially for drugs that need to maintain a stable blood concentration for a specific period of time, our controlled-release tablet technology can release APIs at a preset rate to maintain therapeutic effectiveness and reduce patient burden.

Capsules: Whether hard or soft capsules, we can provide customized filling solutions that use microencapsulation technology to protect sensitive ingredients from the external environment, extend drug action time, and improve patient compliance. Hard capsules are suitable for encapsulating all kinds of apis, ensuring the precise ratio and uniform encapsulation of apis and excipients, maintaining consistency between batches, especially suitable for light and air sensitive drugs. Soft capsules are preferred for liquid or semi-solid filling and provide a solution for API with poor water solubility. By optimizing the capsule formulation, we can significantly increase the bioavailability of API and improve the therapeutic outcome.

Pills and granules: Through the use of advanced technologies such as spray drying and roll molding, we are able to produce a variety of pills and granules that are easy to swallow, especially for children and elderly patients, ensuring drug acceptability and compliance.

Powder formulations: For medicines that require precise dosing, we offer powder formulations solutions that significantly improve drug solubility through micropulverization technology, ensuring accurate dosing to meet specific therapeutic needs.

Optimize the composition of the formulation

To ensure the optimum level of a functional excipient in the formulation. In an immediate-release tablet formulation, excipient levels of binder, disintegrant, and lubricant can be varied and the functionality challenged. A partial or full factorial DOE can evaluate multiple excipients at different levels of the excipient. For an extended-release tablet formulation based on a hydrophilicgel matrix, polymer levels will affect the release rate of the drug from the tablet. Hence, the level of polymer is selected based on the specifications or the target release profile.

To optimize the drug load in a formulation to reduce the pill burden, especially for a large dose drug product. Many oral solid-dose products need tobe formulationted in doses above 100 mg per unit tablet or capsule. There are quite a few new chemical entities that need a much higher dose up to a 500 or 750 mg per unit dose. Fixed-dose combination therapies are becoming more popular, due to synergistic therapeutic effects and as a lifecycle management strategy. The number of actives and the dose per unit tablet are increasing. Thus, there is a need to formulationte such products in a way that the tablet size is reasonable to swallow, especially for geriatric patients. It is important, therefore, to optimize the formulation so that the drug load in a tablet is as high aspossible, which also means that there is little room for inert excipients. Selecting the right functional excipient in the right quantity thus becomes more crucial.

Preparation technology of oral solid dosage form

Fig. 1 Schematics of (a)direct compression (b) dry granulation (c) wet granulation processes.

Direct powder pressing/filling

Direct powder pressing tablet or direct powder capsule, consists of only two main steps, which refers to the bulk drug and suitable excipients (fillers, disintegrators, lubricants, etc.) mixed evenly before the preparation is pressed or capsule filling. Compared with dry granulation and wet granulation, the process is simple

Dry granulation

the drug powder is first mixed with auxiliary materials, and then the mixture is added to the screw feeding mechanism, the powder is transported by the screw feeding mechanism to the roller press area, in the roller press area is pressed into sheets, the discharge sheet is broken into the standard drug particles in the whole grain mechanism, and the whole dry granule production process is completed.

Wet granulation

During the wet granulation process, pellets are produced by adding a liquid/dry adhesive to the powder mixture. The drug is mixed with excipients and processed using solvents (water-based or organic), followed by drying and grinding to produce pellets. The solvent mixed into the powder can form a strong enough bond between the powder particles to lock them together. However, after the liquid dries, some of the powder may disperse. In this case, a liquid solution containing the adhesive is required. When water-sensitive drugs are involved or when rapid drying of particles is required, organic solvents such as ethanol are used. In addition, stabilizers, such as pH regulators in close contact with the drug, can be used, which can maximize product stability. After the solvent is removed or dried, the powder mixture forms more dense clumps. In the traditional wet granulation method, the soft material is forced through a sieve to produce a pre-determined size of wet particles, which are then dried. Subsequent post-drying, screening/grinding steps break the agglomerates into particles with the desired size and distribution.

Hot melt extrusion

By melting and mixing the active pharmaceutical ingredient (API) with the thermoplastic polymer at high temperatures, a uniform matrix is formed, and then the drug is evenly dispersed and cooled through the fine control of the extruder. This technology is particularly suitable for the treatment of insoluble apis, which can significantly improve the dissolution rate and bioavailability of drugs, overcoming the solubility bottleneck in traditional preparation methods.

BOC Sciences is committed to supporting its partners from concept design to clinical validation to create a new era of drug discovery. Our services cover all aspects from raw material evaluation, formulation optimization to production scale-up, aiming to provide customers with one-stop solutions to accelerate the process of drugs from the laboratory to the market, and ultimately benefit the majority of patients.

FAQ

1. What are oral solid dosage forms?

Oral solid dosage forms are pharmaceutical formulations that are administered orally and are solid at room temperature. They include tablets, capsules, powders, and granules, and are designed to deliver active pharmaceutical ingredients (APIs) efficiently and effectively.

2. What are controlled-release tablets?

Controlled-release tablets are designed to release the API at a predetermined rate over an extended period. This helps maintain consistent drug levels in the bloodstream and reduces the frequency of dosing, which can improve patient adherence to the medication regimen.

3. What is the difference between hard and soft gelatin capsules?

• Hard gelatin capsules: Typically used for powders, granules, or pellets. They consist of two rigid shells that fit together.
• Soft gelatin capsules: Used for liquid or semi-solid fills. They are made from a more flexible gelatin shell that can encapsulate oils or active ingredients with poor water solubility.

4. What are powders and granules for reconstitution?

• Powders for reconstitution: Dry powders that are mixed with a liquid before administration. They offer flexibility in dosing and are easy to prepare.
• Granules for reconstitution: Dry granules that are also mixed with a liquid before use. They have better flow properties and less dust generation compared to powders, making them easier to handle and use.

5. How do you ensure the stability of oral solid dosage forms?

We conduct rigorous stability testing under various environmental conditions to ensure that our formulations maintain their integrity, potency, and safety over their shelf life. This includes tests for moisture content, temperature stability, and light exposure.

6. What analytical testing do you perform for oral solid dosage forms?

• High-performance liquid chromatography (HPLC): For precise quantification of APIs and excipients.
• Gas chromatography (GC): For analyzing volatile compounds and residual solvents.
• Differential scanning calorimetry (DSC): For thermal analysis and stability testing.
• Fourier-transform infrared spectroscopy (FTIR): For identifying chemical structures and interactions.
• Particle size analysis: For ensuring uniformity in suspensions, emulsions, and lyophilized products.
• Automated dissolution testing: For evaluating drug release rates and bioavailability.

7. Can you develop customized oral solid dosage forms?

Yes, we specialize in tailoring formulations to meet the specific needs of our clients. Whether it's adjusting the release profile, improving bioavailability, or enhancing patient compliance, we work closely with our clients to develop customized solutions.