A kind of composite disintegrant system for oral solid preparation and oral solid preparation containing the composite disintegrant system
A technology for compounding disintegrants and solid preparations, which can be used in medical preparations containing active ingredients, medical preparations without active ingredients, and drug combinations, and can solve problems such as viscous active substances
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0081] Embodiment 1: Preparation of QR01019K
[0082] Dissolve QR01019 (1.0g) in dichloromethane (5ml), stir at room temperature to form a solution, add potassium phthalimide (0.27g) to the solution, keep it warm for 4 hours, cool to -50°C, filter, The solid obtained by spin-drying the solvent is amorphous QR01019K.
[0083] Melting point: 135-145°C.
[0084] MS / HRMS m / z: 717[M+H] + ;677[M-K] - .
[0085] 1 H-NMR (400MHz, DMSO-d 6)δ: 1.44(t, 3H), 1.46(t, 3H), 2.38(s, 3H), 2.41(s, 3H), 2.44(s, 3H), 4.64(q, 2H), 5.29(d, 1H ), 5.32(d, 1H), 5.52(d, 1H), 5.56(d, 1H), 6.86(q, 1H), 6.90(d, 2H), 7.18(m, 2H), 7.22(d, 2H) , 7.33 (m, 1H), 7.36 (m, 1H), 7.46 (d, 1H), 7.52 (dd, 1H), 7.75 (d, 1H).
[0086] H-NMR spectrum and X-ray powder diffraction spectrum are shown in figure 1 and figure 2 .
Embodiment 2
[0087] Example 2: Antihypertensive efficacy test of QR01019K on spontaneously hypertensive rats
[0088] Spontaneously hypertensive rats aged 12 weeks (hereinafter referred to as SHR, purchased from Beijing Weitong Lihua Experimental Animal Technology Co., Ltd.) were anesthetized by intraperitoneal injection of 2.5% sodium pentobarbital. The blood pressure sensing catheter was inserted into the abdominal aorta, the implant was fixed on the abdominal wall, and the postoperative daily care was performed after suturing. Animals whose systolic blood pressure exceeded 160mm Hg were selected into groups, with 8 animals in each group, 3 groups in total. The control group was given 0.5% sodium carboxymethylcellulose (hereinafter referred to as CMC-Na); the OR01019 group and the QR01019K group were dissolved in 0.5% CMC-Na, and the dosage was based on the effective dose of 1 mg / kg azilsartan. The drug volume is 4mL / kg, all administered by intragastric administration, with the systolic...
Embodiment 3
[0100] Embodiment 3: preparation and disintegration experiment of oral solid preparation
[0101] Tablets of Preparation Examples 1-11 and Comparative Examples 1-11 were respectively prepared according to the following three preparation methods, and the differences in prescription composition, tablet hardness and tablet weight of each preparation example and Comparative Examples are shown in Table 3 below.
[0102] Preparation examples 1, 7, 8 and 9, comparative examples 1, 7, 8 and 9 adopt the powder compression method: select 60 mesh sieves according to the material properties, and the material is sieved for subsequent use (in preparation example 7 and comparative example 7, active The ingredients and excipients are sieved together, and the disintegrating agent and the disintegrating agent are mixed and sieved for subsequent use; the remaining preparation examples and comparative examples are sieved separately); the active ingredients, excipients, disintegrants, There is no ...
PUM
Property | Measurement | Unit |
---|---|---|
hardness | aaaaa | aaaaa |
Abstract
Description
Claims
Application Information
- R&D Engineer
- R&D Manager
- IP Professional
- Industry Leading Data Capabilities
- Powerful AI technology
- Patent DNA Extraction
Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.
© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com