Analysis on the Advantages of Developing Sustained and Controlled Release Preparations

When developing and designing pharmaceutical preparations, the drugs should be in the best form for diagnosing, treating or preventing human diseases, and the efficacy of the drugs must be maximized and safe. Sustained-release and controlled-release preparations have the advantages of less administration times, less fluctuation in blood concentration, diversified routes of administration, less irritation, long-lasting curative effect, and safety, etc., and are receiving more and more clinical attention. Therefore, sustained-release The development of formulations has a broad market and prospects.

Sustained-release preparations refer to preparations that can continue to release the drug for a long time to achieve a long-acting effect after administration. The drug release is not a constant rate, but is mainly a first-order rate process. A controlled-release preparation is a dosage form that releases drugs at a timed, quantitative, and uniform rate through a controlled-release coating film, so that the blood drug concentration is constant, and there is no “peak and valley” phenomenon, so as to better exert the effect. Sustained and controlled release preparations have the following advantages:

(1) Convenient medication is one of the important purposes of the development of sustained and controlled release formulations

Ordinary preparations generally need to be administered multiple times a day, so it often causes missed doses, and the way of multiple doses per day is prone to large “peak and valley” fluctuations. When the blood concentration is in the “trough”, it is likely to be lower than The therapeutic concentration can not exert the effect. The development of sustained and controlled release formulations has the advantages of extending the interval of dosing, reducing the number of doses, and improving the compliance of patients with medication.

Sustained and controlled-release preparations stay at the absorption site for a longer time and absorb more completely, so they have higher bioavailability, thereby increasing the efficacy of the drug. For example, liquid oral sustained and controlled-release preparations are convenient for children, the elderly and patients with dysphagia. Compound sustained-release preparations can reduce the leakage rate, improve the effect and reduce costs.

Different dosage forms may have different effects of drugs. Sometimes through formulation design, the release rate of drugs in the formulation can be controlled. Medicilon is committed to providing contract R&D services in solid formulations, semi-solid formulations, liquid formulations and innovative formulations. At the same time, Medicilon has extensive R&D experience in sustained and controlled release formulations, microparticle formulations, and protein and peptide pharmaceutical formulations. Many mature products have been handed over to customers. We have rich R&D experience in preparations and protein and peptide pharmaceutical preparations, and many mature products have been handed over to customers.

(2) Reduce side effects

Slow-release and controlled-release preparations can reduce the fluctuation of blood concentration by controlling the release rate of the drug, thereby reducing the toxic and side effects of the drug and improving the safety of the drug under the premise of ensuring the efficacy. In addition, some controlled and sustained-release preparations have a local positioning effect, which can improve the local therapeutic effect while reducing the toxic and side effects caused by systemic absorption of drugs.

(3) Extend the patent protection time of drugs, etc.

The development of sustained and controlled release preparations has the effect of extending the protection time of drug patents and opening up new effective patents. The investment of innovative compounds by domestic companies cannot be compared with that of multinational companies, and slow- and controlled-release new drugs are a viable route for pharmaceutical companies to participate in international competition. For some domestic pharmaceutical companies, investing in new formulations and new drugs has achieved obvious results. New formulations and new drugs have less average investment than NCE new drugs, shorter development cycles, and less risk. Novel drug delivery technologies can protect product developers when patents are about to expire Extend product exclusivity and seize market opportunities.

For example, in the 20-30 years of patent protection, researchers of innovative drugs can also make various optimizations of drugs, improve bioavailability, and make slow and controlled release preparations.

Sustained-release and controlled-release preparations are a kind of dosage form that has been developing rapidly recently. It has the advantages of low investment, short time, high success rate, high added value, more environmental protection, and can extend the life cycle of new drugs, making it a hot spot for research and development.