Glucosamine hydrochloride capsule and preparation method thereof

Abstract

The invention provides a glucosamine hydrochloride capsule and a preparation method thereof, the capsule content comprises the following components in parts by weight: 240 parts of glucosamine hydrochloride, 50-60 parts of starch and 2-7 parts of hydroxypropyl cellulose; the glucosamine hydrochloride capsule prepared by controlling the particle sizes of the glucosamine hydrochloride and the starch within a specific range and using a specific adhesive is high in dissolution rate (the dissolution rate in four dissolution media for 45 minutes is not lower than 85%), and the dissolution rate is stable after the glucosamine hydrochloride capsule is placed for 24 months for a long time.

Description

Technical Field

[0001] This invention belongs to the field of pharmaceutical preparations and relates to a glucosamine hydrochloride capsule and its preparation method. Background Technology

[0002] Glucosamine hydrochloride is a drug used to treat and prevent osteoarthritis. Its chemical name is 2-amino-2-deoxy-glucose hydrochloride, and its structural formula is shown below. It improves the metabolic function and nutrition of bone and cartilage tissue by stimulating the biochemical synthesis of mucopolysaccharides and increasing the uptake of calcium in bones. It can also improve and enhance the viscosity of synovial fluid, increase the synthesis of synovial fluid, and provide joint lubrication. Therefore, it can block the pathological process of osteoarthritis, prevent the progression of the disease, improve joint mobility, relieve joint pain, and inhibit and reverse the formation of joint degeneration.

[0003] There are no reports of glucosamine hydrochloride capsules in the existing technology, let alone reports of preparation methods for dissolving stable glucosamine hydrochloride capsules.

[0004] Therefore, it is necessary to conduct further research on the formulation and preparation process of glucosamine hydrochloride capsules to provide a drug with high dissolution and stability. Summary of the Invention

[0005] This invention provides a glucosamine hydrochloride capsule, wherein the capsule contents, by weight, are 240 parts glucosamine hydrochloride, 50-60 parts starch, and 2-7 parts hydroxypropyl cellulose.

[0006] In some embodiments of the present invention, the starch is tapioca starch.

[0007] In some embodiments of the present invention, the hydroxypropyl cellulose is a 5% aqueous solution of hydroxypropyl cellulose with a viscosity of 50-80 mPa·s at 25°C.

[0008] In some embodiments of the present invention, 240 parts of glucosamine hydrochloride, 52-58 parts of starch, and 3-6 parts of hydroxypropyl cellulose are used.

[0009] In some embodiments of the present invention, 240 parts of glucosamine hydrochloride, 55 parts of starch, and 5 parts of hydroxypropyl cellulose are used.

[0010] In some embodiments of the present invention, the glucosamine hydrochloride and starch particle sizes are as follows:

[0011]

[0012] In some embodiments of the present invention, the glucosamine hydrochloride and starch particle sizes are as follows:

[0013]

[0014] Furthermore, each capsule contains 240 mg of glucosamine hydrochloride.

[0015] Furthermore, the present invention provides a method for preparing the above-mentioned glucosamine hydrochloride capsules, comprising the following steps:

[0016] (1) Preparation of raw and auxiliary materials;

[0017] Preparation of adhesive: Hydroxypropyl cellulose is mixed with water to prepare a 5% aqueous solution, and the temperature is controlled at 35-40℃;

[0018] (2) Mixing and wet granulation

[0019] Mixing: Add glucosamine hydrochloride and starch to a wet granulator and premix for 6-8 minutes;

[0020] Wet granulation: Add the binder to the wet granulator at a time of 160-210 seconds, and then granulate for 2-5 minutes.

[0021] (3) Drying and granulation:

[0022] Dry at 55-65℃; add the dried granules into a granulator with a 2.0mm mesh size.

[0023] (4) Filling: Fill into capsules.

[0024] This invention, by controlling the particle size of glucosamine hydrochloride and starch excipients within a specific range and using a specific binder, produces glucosamine hydrochloride capsules with high dissolution (dissolution rate not less than 85% in 45 minutes in 4 dissolution media) and stable dissolution after long-term storage for 24 months. Detailed Implementation

[0025] This invention discloses a method for preparing glucosamine hydrochloride capsules. Those skilled in the art can refer to the content of this invention and, in conjunction with the relevant principles of pharmaceutical preparations, appropriately modify the process parameters to achieve the desired result. It should be particularly noted that all similar substitutions and modifications are obvious to those skilled in the art and are considered to be included within the scope of this invention. The application of this invention has been described through preferred embodiments, and those skilled in the art can clearly modify or appropriately change and combine the methods and applications described herein without departing from the content, spirit, and scope of this invention to realize and apply the technology of this invention.

[0026] To better understand the invention and not to limit its scope, all figures indicating amounts, percentages, and other numerical values ​​used in this application should, in all cases, be understood to be modified by the word "approximately." Each numerical parameter should at least be considered as obtained based on reported significant figures and through conventional rounding methods.

[0027] The present invention will be further illustrated by the following examples, but the examples do not limit the present invention in any way.

[0028] The particle sizes of glucosamine hydrochloride and cassava starch micronized in the embodiments of this invention are shown in the table below:

[0029]

[0030] The viscosity of the hydroxypropyl cellulose used in the embodiments of this invention is shown in the table below:

[0031]

[0032] Examples 1-27: Glucosamine Hydrochloride Capsules

[0033] I. Prescription Composition:

[0034]

[0035] The glucosamine hydrochloride and starch used are shown in Tables 1-4.

[0036] Table 1: List of glucosamine hydrochloride, starch, and hydroxypropyl cellulose used in Examples 1-5

[0037]

[0038] Table 2: List of glucosamine hydrochloride, starch, and hydroxypropyl cellulose used in Examples 6-10

[0039]

[0040] Table 3: Glucosamine hydrochloride, starch, and hydroxypropyl cellulose used in Examples 11-15

[0041]

[0042] Table 4: Glucosamine hydrochloride, starch, and hydroxypropyl cellulose used in Examples 16-27

[0043]

[0044] II. Preparation method:

[0045] (1) Preparation of raw and auxiliary materials;

[0046] Preparation of adhesive: Hydroxypropyl cellulose is mixed with water to prepare a 5% aqueous solution, and the temperature is controlled at 35-40℃;

[0047] (2) Mixing and wet granulation

[0048] Mixing: Add glucosamine hydrochloride and starch to a wet granulator and mix for 7 minutes;

[0049] Wet granulation: Add the binder to the wet granulator at a time of 180 seconds, and then granulate for 4 minutes.

[0050] (3) Drying and granulation:

[0051] Dry at 55-65℃; add the dried granules into a granulator with a 2.0mm mesh size.

[0052] (4) Filling: Fill into capsules, each capsule containing 240mg of glucosamine hydrochloride.

[0053] III. Dissolution results:

[0054] 1. The dissolution rate of the prepared glucosamine hydrochloride capsules was tested in four dissolution media, and the results are shown in Table 5.

[0055] Table 5: Dissolution rate of the dissolution medium in glucosamine hydrochloride capsules 4 of Examples 1-27

[0056]

[0057] 2. After being stored for 24 months, the dissolution rate of Examples 1-15 and Examples 24-27 was tested in four dissolution media. The results are shown in Table 6.

[0058] Table 6: Dissolution rates of Examples 1-15 and Examples 24-27 after 24 months of long-term storage

[0059]

[0060] By combining Tables 5 and 6 and comparing and analyzing Examples 1-27, we found that:

[0061] (1) Glucosamine hydrochloride capsules prepared from glucosamine hydrochloride with a specific particle size range, cassava starch, and hydroxypropyl cellulose with a specific viscosity, such as Examples 1-3, 6-8, and 11-13, have high solubility in four media and stable solubility in four media after being stored for 24 months.

[0062] (2) When only glucosamine hydrochloride of other particle sizes is used, as shown in Examples 4-5, the prepared glucosamine hydrochloride capsules have high solubility in four media, but after being stored for 24 months, the solubility in water and pH 6.8 phosphate buffer media is unstable and the quality is poor.

[0063] (3) When only cassava starch of other particle sizes is used, as shown in Examples 9-10, the glucosamine hydrochloride capsules prepared have high solubility in four media, but after being stored for 24 months, the solubility in water is unstable and the quality is poor.

[0064] (4) When other starches with the same particle size range are used instead of cassava starch, such as those shown in Examples 24-27, the prepared glucosamine hydrochloride capsules have high solubility in four media, but after being stored for 24 months, the solubility is unstable in all four media, resulting in poor quality.

[0065] (5) When only hydroxypropyl cellulose of other viscosities is used, as shown in Examples 14-15, the glucosamine hydrochloride capsules prepared have high solubility in four media, but after being stored for 24 months, the solubility in water is unstable and the quality is poor.

[0066] (6) When tapioca starch of other particle size ranges and hydroxypropyl cellulose of other viscosities are used at the same time, as shown in Examples 16-17, the prepared glucosamine hydrochloride has unstable water solubility and poor quality. Therefore, long-term 24-month solubility test was not carried out.

[0067] (7) When glucosamine hydrochloride of other particle size ranges and hydroxypropyl cellulose of other viscosities are used at the same time, as shown in Examples 18-19, the glucosamine hydrochloride prepared is unstable in water solubility and of poor quality. Therefore, long-term 24-month solubility test was not carried out.

[0068] (8) When glucosamine hydrochloride and cassava starch of other particle size ranges are used at the same time, as shown in Examples 20-21, the glucosamine hydrochloride prepared is unstable in water solubility and of poor quality. Therefore, long-term 24-month solubility test was not carried out.

[0069] (9) When glucosamine hydrochloride of other particle size ranges, tapioca starch and other hydroxypropyl cellulose of other viscosities are used at the same time, as shown in Examples 22-23, the glucosamine hydrochloride prepared is unstable in water and pH 6.8 phosphate buffer solution and has poor quality. Therefore, long-term 24-month dissolution test was not carried out.

[0070] Glucosamine hydrochloride capsules prepared from glucosamine hydrochloride with a specific particle size range, tapioca starch, and hydroxypropyl cellulose with a specific viscosity exhibit significantly better dissolution rate and dissolution stability than glucosamine hydrochloride capsules prepared from glucosamine hydrochloride with other particle size ranges, tapioca starch with other particle size ranges, or hydroxypropyl cellulose with other viscosities.

Claims

1. A glucosamine hydrochloride capsule, wherein, by weight, the capsule contents are 240 parts glucosamine hydrochloride, 50-60 parts starch, and 2-7 parts hydroxypropyl cellulose; The starch mentioned is tapioca starch; The hydroxypropyl cellulose mentioned is a 5% aqueous solution of hydroxypropyl cellulose with a viscosity of 50-80 mPa·s at 25°C.

2. The glucosamine hydrochloride capsule according to claim 1, wherein By weight, it contains 240 parts glucosamine hydrochloride, 52-58 parts starch, and 3-6 parts hydroxypropyl cellulose.

3. The glucosamine hydrochloride capsule according to claim 1, wherein By weight, there are 240 parts glucosamine hydrochloride, 55 parts starch, and 5 parts hydroxypropyl cellulose.

4. The glucosamine hydrochloride capsule according to claim 1, wherein The particle sizes of the glucosamine hydrochloride and starch are as follows: 。 5. The glucosamine hydrochloride capsule according to claim 1, wherein The particle sizes of the glucosamine hydrochloride and starch are as follows: 。 6. The glucosamine hydrochloride capsule as described in claim 1, wherein each capsule contains 240 mg of glucosamine hydrochloride.

7. A method for preparing any one of the glucosamine hydrochloride capsules as described in claims 1 to 6, comprising the following steps: (1) Preparation of raw and auxiliary materials; Preparation of adhesive: Hydroxypropyl cellulose is mixed with water to prepare a 5% aqueous solution, and the temperature is controlled at 35-40℃; (2) Mixing and wet granulation Mixing: Add glucosamine hydrochloride and starch to a wet granulator and premix for 6-8 minutes; Wet granulation: Add the binder to the wet granulator at a time of 160-210 seconds, and then granulate for 2-5 minutes. (3) Drying and granulation: Dry at 55-65℃; add the dried granules into a granulator with a 2.0mm mesh size. (4) Filling: Fill into capsules.

Images