CN-121985939-A - Excipient granulates

Abstract

Excipient granulates comprising a viscosity increasing agent, a disintegrant, and one or more additional excipients are disclosed. The excipient granulate may be combined with a pharmaceutical granulate to provide a pharmaceutical composition. The excipient granulates can be used to increase the viscosity of aqueous compositions such as oral pharmaceutical compositions. When added to an aqueous solution, the excipient granulates can be dissolved to provide a suspension of drug particles in a viscous solution. The excipient granulates can be used to improve the palatability of oral pharmaceutical compositions containing the drug granulates.

Inventors

• Sami Karaponi
• Daniel M. Canafex
• XIANG JIANING
• XIANG WEILIN

Assignees

• 凯瑞康宁公司

Dates

Publication Date

20260505

Application Date

20240731

Priority Date

20230731

Claims (20)

1. 1. An excipient granulate comprising a plurality of excipient particles, wherein the excipient particles comprise: A tackifier; disintegrating agent, and One or more additional excipients.
2. 2. The excipient granulate of claim 1, wherein the excipient granulate comprises: 1 wt% to 35% wt% of said tackifier; 1 wt to 25 wt% of said disintegrant, and 40 From wt% to 98 wt% of the one or more additional excipients; Wherein wt% is based on the total weight of the excipient particles.
3. 3. Excipient granulate according to claim 1, wherein the excipient particles have an average particle size of 100 to 600 μm, wherein the particle size is determined by sieve analysis or laser diffraction.
4. 4. The excipient granulate of claim 1, wherein the viscosity increasing agent comprises xanthan gum.
5. 5. The excipient granulate of claim 1, wherein the disintegrant comprises crospovidone.
6. 6. The excipient granulate of claim 1, wherein the one or more additional excipients comprise a diluent, a binder, a flavoring, a buffering agent, an acid, a sweetener, a filler, or a combination of any of the foregoing.
7. 7. The excipient granulate of claim 1, wherein after mixing a solution of 1.2 g of the excipient granulate and 40 mL water at a temperature of 23 ℃ for 90 seconds, the viscosity of the solution is in the range of 40 cP to 100 cP, wherein the viscosity is determined using a Brookfield digital viscometer LVDV-1+ model equipped with a Brookfield SC4-18 spindle at a spindle speed of 30 RPM.
8. 8. A pharmaceutical composition, in the form of a capsule, the pharmaceutical composition comprises: The excipient granulate of claim 1, and Active pharmaceutical ingredient.
9. 9. The pharmaceutical composition of claim 8, wherein the pharmaceutical composition comprises: 1 wt to 15 wt% of said excipient granulate, and Wherein wt% is based on the total weight of the pharmaceutical composition.
10. 10. The pharmaceutical composition of claim 8, wherein the pharmaceutical composition comprises a pharmaceutical granulate, wherein the pharmaceutical granulate comprises the active pharmaceutical ingredient.
11. 11. The pharmaceutical composition of claim 10, wherein the pharmaceutical composition comprises: 1 wt to 15 wt% of said excipient granulate, and 85 From about 99% to about wt% by weight of said pharmaceutical granulate, Wherein wt% is based on the total weight of the pharmaceutical composition.
12. 12. The pharmaceutical composition according to claim 10, wherein, The excipient granulate has a first bulk density; the drug granulate having a second bulk density, and The first volumetric density is within + -20% of the second volumetric density.
13. 13. A pharmaceutical product comprising the pharmaceutical composition of claim 8.
14. 14. The pharmaceutical product of claim 13, wherein the pharmaceutical product comprises the excipient granulate, the pharmaceutical granulate, or a combination thereof contained within a package.
15. 15. The pharmaceutical product of claim 14, wherein the package comprises a pouch.
16. 16. The pharmaceutical product of claim 14, wherein the pharmaceutical product comprises the excipient granulate and the pharmaceutical granulate in combination in the same package.
17. 17. The pharmaceutical product of claim 15, wherein the pharmaceutical product comprises a first package containing the excipient granulate and a second package containing the pharmaceutical granulate.
18. 18. An oral pharmaceutical composition for oral administration prepared using the pharmaceutical composition of claim 10, wherein the oral pharmaceutical composition comprises a viscous aqueous solution having a viscosity of 50 cP to 1,000 cP, wherein the viscosity is determined using a Brookfield digital viscometer LVDV-i+ type equipped with a Brookfield SC4-18 spindle at a spindle speed of 30 rpm at a temperature of 23 ℃.
19. 19. The oral pharmaceutical composition of claim 18, wherein the oral pharmaceutical composition comprises a drug granulation suspended in the viscous aqueous solution.
20. 20. The oral pharmaceutical composition of claim 18, wherein the oral pharmaceutical composition comprises an active pharmaceutical ingredient suspended in the viscous aqueous solution.

Description

Excipient granulates The present application claims the benefit of U.S. provisional application No. 63/529,880 filed on day 31, 7, 2023, in accordance with 35 u.s.c. ≡119 (e), which is incorporated herein by reference in its entirety. Technical Field The present disclosure relates to excipient granulates, compositions comprising excipient granulates, and uses of excipient granulates. Excipient granulates can be used to improve the palatability of oral pharmaceutical compositions. Background The active pharmaceutical ingredient may be administered as a pharmaceutical granulate. In order to improve the palatability of the drug granulation administered to a patient, the drug granulation may be dispersed and/or suspended in a viscous solution. It may be convenient to provide a viscosity enhancing agent and additional excipients with the pharmaceutical granulation such that the viscosity enhancing agent, additional excipients, and pharmaceutical granulation may be combined with water to provide a palatable oral pharmaceutical composition. Disclosure of Invention According to the present invention, an excipient granulate comprises a plurality of excipient particles, wherein the excipient particles comprise a viscosity enhancing agent, a disintegrant, and one or more additional excipients. According to the present invention, a method of preparing excipient particles includes dry mixing a viscosity increasing agent, a disintegrant, and the one or more excipients to provide a dry mixture, granulating the dry mixture with a buffer solution to provide a first granulation, wet agglomerating the first granulation to form a first wet mass, granulating the first wet mass with water to provide a second granulation, wet agglomerating the second granulation to form a second wet mass, and drying the second wet mass to provide excipient particles. According to the present invention, the excipient granulate comprises excipient particles prepared according to the present invention. According to the invention, the composition comprises excipient granulates according to the invention. According to the invention, the pharmaceutical composition comprises an excipient granulate according to the invention and an active pharmaceutical ingredient. According to the invention, the product comprises an excipient granulate according to the invention or a composition according to the invention. According to the invention, the pharmaceutical product comprises a pharmaceutical composition according to the invention. According to the invention, a composition for oral administration is prepared using the excipient granulate according to the invention. According to the present invention, an oral pharmaceutical composition for oral administration is prepared using the excipient granulate according to the present invention. Drawings Those skilled in the art will appreciate that the drawings described herein are for illustrative purposes only. The drawings are not intended to limit the scope of the present disclosure. Fig. 1 shows an example of the particle size distribution of excipient granulates provided by the present disclosure. Fig. 2 shows an example of the reconstituted viscosity of a solution prepared using excipient granulates. Fig. 3 shows an example of the reconstitution luminosity of a solution prepared using an excipient. Detailed Description For the purposes of the following detailed description, it is to be understood that the embodiments provided by the disclosure may assume various alternative variations and step sequences, except where expressly specified to the contrary. Furthermore, all numbers expressing, for example, quantities of ingredients used in the specification and claims, other than in any operating example or where otherwise indicated, are to be understood as being modified in all instances by the term "about". Accordingly, unless indicated to the contrary, the numerical parameters set forth in the following specification and attached claims are approximations that may vary depending upon the desired properties to be obtained by the present invention. At the very least, and not as an attempt to limit the application of the doctrine of equivalents to the scope of the claims, each numerical parameter should at least be construed in light of the number of reported significant digits and by applying ordinary rounding techniques. Notwithstanding that the numerical ranges and parameters setting forth the broad scope of the invention are approximations, the numerical values set forth in the specific examples are reported as precisely as possible. Any numerical value, however, inherently contains certain errors necessarily resulting from the standard deviation found in their respective testing measurements. Moreover, it should be understood that any numerical range recited herein is intended to include all sub-ranges subsumed therein. For example, a range of "1 to 10" is intended to include all subranges between (and inclusiv