Pregabalin capsule and preparation method thereof

Abstract

The invention discloses a pregabalin capsule. The pregabalin capsule is composed of pregabalin and silicified microcrystalline cellulose, and in the pregabalin capsule, the weight percentage of the pregabalin is 25-75%. According to the pregabalin capsule and the preparation method thereof, a proper amount of the silicified microcrystalline cellulose is added as an auxiliary material to be mixed with the pregabalin, and the pregabalin and the silicified microcrystalline cellulose with proper particle size distribution are selected, so that the prepared pregabalin capsule is good in flowability, qualified in loading capacity, capable of avoiding the risk of gelatin crosslinking and good in stability; the dissolution behavior is stable and unchanged in a storage process, so that the long-term stability of the pregabalin capsule is ensured; and the method is suitable for industrial production (especially industrialization of 300 mg specification).

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pregabalin capsule and a preparation method thereof. Background technique [0002] Pregabalin is a new type of antiepileptic drug. Its molecular structure has γ-aminobutyric acid structure, so it has anticonvulsant effect. Pregabalin is a class I drug in the BCS classification system. Pregabalin reaches its peak concentration after 1.5 hours of oral administration, and its relative bioavailability is ≥90%, and its Cmax and AUC have a linear relationship with the dose. It is not combined with plasma proteins in vivo and has almost no metabolism. [0003] Pregabalin Capsules was successfully developed by Pfizer Europe MA EEIG. It was first approved for marketing by the European Medicines Agency (EMA) on July 6, 2004. The trade name is Lyrica, and the marketed dosage forms include hard capsules (specifications: 25mg, 50mg, 75mg , 100mg, 150mg, 200mg, 225mg, 300mg), ...

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Problems solved by technology

[0007] The Chinese patent with the publication number CN 105434395 A discloses a pregabalin capsule and a preparation method thereof. Adhesive and 1-10% lubricant) are obtained through repeated screening, mixing, and filling, and limit the particle size distribution of pregabalin and lactose; although this technical scheme can improve the flow of pregabalin capsule contents properties, mixing uniformity and impurity control, but there are the following deficiencies: ① This patent contains a high proportion of lactose, which will form ketose after rearrangement reaction, and ketose will react with lysine in gelatin to form cross-linked gelatin , there is a risk of affecting dissolution; 2. the process of this patent is loaded down with trivial details, and the material yield is low; 3. the weight percent of pregabalin of this patent is 5~50%, and the weight percent of lactose is 10~60%, which is not suitable for large-scale varieties ( Such as the production of 300mg specification), the patient's taking compliance is poor

[0008] The Chinese patent with the publication number CN 105520918 A discloses a pregabalin capsule, which is composed of pregabalin, a lactose compound, and a pharmaceutically acceptable carrier. The lactose compound is a lactose-microcrystalline cellulose compound. The weight percentage of rebalin is 5-50%, but there are the following disadvantages: ①This patent adopts the direct mixing process, and because the prescription contains a high proportion of starch, the prepared total mixed powder will have poor fluidity due to the starch itself. Risk of poor fluidity; ②This patent is not suitable for the production of large-scale varieties (such as 300mg specification), and the patient’s compliance with taking it is poor

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