CN114948896A - A new type of soft capsule material formulation - Google Patents

Abstract

The invention discloses a novel soft capsule material formula, which belongs to the technical field of medicinal materials, and comprises the following components in percentage by weight: 30-50% of a substrate, 10-22% of polyglycerol, 0.6-1.6% of sodium pyrophosphate, 35-55% of purified water and 1-5% of an additive; the matrix is one of sesbania gum, xanthan gum, K-carrageenan, gelatin, guar gum and peach gum and the combination of any two or more than two of the substances. The preparation process is simple, the raw material source is rich, and the green environmental protection is realized; the capsule material provided by the invention has low oxygen transmission rate, good thermal insulation performance and excellent disintegration rate; the capsule material provided by the invention has high safety, wide applicability and high stability, and is beneficial to protecting the content of the soft capsule which is easy to oxidize.

Description

A new type of soft capsule material formulation

technical field

The invention belongs to the technical field of medicinal materials, and in particular relates to a formula of a novel soft capsule material.

Background technique

Soft capsule refers to a dosage form in which medicinal material extract, liquid medicine or mixed with suitable excipients are sealed in a hydrophilic soft capsule material by drop method or compression method to make spherical, oval or other shapes. Soft capsules are suitable for unstable medicinal substances, such as chemical components that are sensitive to light, volatile, unstable and easily oxidized when exposed to heat and humidity, and medicinal substances with unpleasant taste and bad smell. After the soft capsule is taken orally, because the drug is wrapped by the hydrophilic gelatin skin and quickly disintegrates in the digestive tract, the drug is released quickly. The formulation of soft capsule materials includes four types of substances: glue, plasticizer, water, and additives. The glue is the main component of the capsule shell, such as gelatin and gelatin substitute materials; It can be mixed and used; additives include preservatives, colorants, disintegrants, sunscreens, antioxidants, etc., to maintain the quality stability of the drug and the soft capsule dosage form. The traditional soft capsule material formula mainly includes gelatin, water, glycerin and selected pigments.

Polyglycerol is a colorless and viscous liquid or semi-solid, soluble in water and ethanol, and has a slightly lower hygroscopicity than glycerin. It is a polyol. Compared with glycerin, polymerized glycerin has higher viscosity and boiling point, less volatility and hygroscopicity, good moisture retention, and has the characteristics of improving emulsion stability. Taking advantage of its hygroscopicity and moisturizing properties, it can be used as a raw material for cosmetics; immersing fibers in an aqueous solution of polymerized glycerol and other compounds can improve the surface flexibility and hydrophilicity of hydrophobic fibers, and can also be used as a primer for water-insoluble dyes. Dyeing auxiliaries. In the present invention, colloid, polyglycerol and sodium pyrophosphate are cross-linked to form a brand-new cross-linked substance, which has better toughness. The combined substance can significantly reduce the penetration of oxygen, thereby preventing the shell from aging too quickly.

The plant soft capsule materials include saffron gum, xanthan gum, carrageenan, gelatin, and guar gum. It is a soft capsule material made of plant polysaccharides instead of animal gelatin. It retains all the advantages of standard animal capsule materials. , such as convenient consumption, effective masking of taste and odor, transparent and visible contents, etc. In addition, the plant capsule material has better coating properties, and the plant itself has a good affinity with most polymer materials, which is especially suitable for the preparation of slow-release and controlled-release coated capsules. Compared with the traditional gelatin soft capsule material, the vegetable soft capsule material has the advantages of high safety, wide applicability, high stability and no cross-linking reaction.

SUMMARY OF THE INVENTION

The invention provides a new soft capsule material formula, which has high safety, wide applicability, high stability, low oxygen permeability, good moisturizing performance and excellent disintegration rate. It has the advantages of abundant raw material sources, green environmental protection and the like, and the preparation method is simple in process, which can be used for the capsule filling and production of oxygen-sensitive pharmaceutical active substances, and has a good application prospect in the field of capsule preparations.

The invention provides a formula of a novel soft capsule material. The components of the capsule material are based on the total weight of the capsule material, and the weight percentages of each component are: matrix 30-50%, polymerized glycerin 10-22%, coke Sodium phosphate 0.6-1.6%, purified water 35-55%, additives 1-5%;

The matrix is one of sapura gum, xanthan gum, K-carrageenan, gelatin, guar gum, and peach gum, or a combination of any two or more.

Further, the polymerization degree of the polymerized glycerin is 10-12.

Further, the additives are opacifying agent titanium dioxide, disintegrating agent polyethylene glycol-400.

Further, the disintegrant accounts for 2-5% of the total weight of the capsule material, and the weight ratio of the sunscreen agent to the matrix is 0.002-0.01:1.

Further, the preparation method of the capsule material is as follows: after mixing the matrix, polymerized glycerol and sodium pyrophosphate, add them into purified water at 50-90°C, then add additives, stir for 1-3h, and keep the temperature at 50-60°C for 0.5-2h, Let stand for defoaming and seal for later use.

Further, the temperature of the purified water is 50-90°C, preferably 70-85°C; the holding time is 0.5-2h, preferably 1.5-2h.

Compared with the prior art, the beneficial effects of the present invention are mainly reflected in:

(1) The preparation process is simple, the source of raw materials is abundant, and it is green and environmentally friendly.

(2) The capsule material provided by the present invention has low oxygen permeability, good moisturizing performance and excellent disintegration rate.

(3) The capsule material provided by the present invention has high safety, wide applicability and high stability, and is beneficial to protect the contents of the easily oxidized soft capsule.

Detailed ways

1. Preparation of new soft capsule material

Example 1

A new type of soft capsule material formula:

Type K-Carrageenan 52.5g;

Polyglycerol 19.8g;

Sodium pyrophosphate 1.2g;

Purified water 72g;

Polyethylene glycol-400 4.05g;

Titanium dioxide 0.45g.

Preparation steps: when 72g of purified water is heated to 75°C, 52.5g of K-carrageenan, 19.8g of polymerized glycerol (degree of polymerization is 10), and 1.2g of sodium pyrophosphate are mixed and added to the purified water, and then 0.45g of titanium dioxide, 4.05g polyethylene glycol-400, after stirring for 2h, keep at 55°C for 2h, let it stand for defoaming, and seal it for later use.

Example 2

A new type of soft capsule material formula:

Sapura gum 60g;

Polyglycerol 22.22g;

Sodium pyrophosphate 1.78g;

Purified water 60g;

Polyethylene glycol-400 5.7g;

Titanium dioxide 0.3g.

Preparation steps: When 60g of purified water is heated to 80°C, 60g of saffron gum, 22.22g of polymerized glycerol (with a degree of polymerization of 10), and 1.78g of sodium pyrophosphate are mixed and added to the purified water, and then 0.3g of titanium dioxide, 5.7g of Polyethylene glycol-400, after stirring for 2 hours, keep the temperature at 55 °C for 1.5 hours, let it stand for defoaming, and seal it for later use.

Example 3

A new type of soft capsule material formula:

Gelatin 67.5g;

Polyglycerol 17.04g;

Sodium pyrophosphate 1.71g;

Purified water 60g;

Polyethylene glycol-400 3.6g;

Titanium dioxide 0.15g.

Preparation steps: when 60g of purified water is heated to 60°C, 67.5g of gelatin, 17.04g of polymerized glycerol (degree of polymerization is 10), and 1.71g of sodium pyrophosphate are mixed and added to purified water, and then 0.15g of titanium dioxide, 3.6g of poly Ethylene glycol-400, after stirring for 2h, keep the temperature at 55°C for 0.5h, let it stand for defoaming, and seal it for later use.

Example 4

A new type of soft capsule material formula:

peach gum 60g;

Polyglycerol 18.09g;

Sodium pyrophosphate 1.26g;

Purified water 67.5g;

Polyethylene glycol-400 3g;

Titanium dioxide 0.15g.

Preparation steps: when 67.5g of purified water is heated to 85°C, 60g of peach gum, 18.09g of polymerized glycerol (degree of polymerization is 11), and 1.26g of sodium pyrophosphate are mixed and added to the purified water, and then 0.15g of titanium dioxide and 3g of polyglycerol are added. Ethylene glycol-400, after stirring for 2h, keep the temperature at 55℃ for 1.5h, let it stand for defoaming, and seal it for later use.

Example 5

A new type of soft capsule material formula:

Xanthan gum 45g;

Polyglycerol 18.42g;

Sodium pyrophosphate 0.93g;

Purified water 82.5g;

Polyethylene glycol-400 3g;

Titanium dioxide 0.15g.

Preparation steps: when 82.5g of purified water is heated to 50°C, 45g of xanthan gum, 18.42g of polymerized glycerol (degree of polymerization is 12), and 0.93g of sodium pyrophosphate are mixed and added to the purified water, and then 0.15g of titanium dioxide, 3g of Polyethylene glycol-400, after stirring for 1 hour, keep the temperature at 55 °C for 1 hour, let it stand for defoaming, and seal it for later use.

Example 6

A new type of soft capsule material formula:

Guar gum 60g;

Polyglycerol 27.78g;

Sodium pyrophosphate 2.22g;

Purified water 52.5g;

Polyethylene glycol-400 7.35g;

Titanium dioxide 0.15g.

Preparation steps: When 52.5g of purified water is heated to 70°C, 60g of guar gum, 27.78g of polymerized glycerol (degree of polymerization is 11), and 2.22g of sodium pyrophosphate are mixed and added to purified water, and then 0.15g of titanium dioxide, 7.35g of g polyethylene glycol-400, after stirring for 3 hours, keep the temperature at 55°C for 1 hour, let it stand for defoaming, and seal it for later use.

Comparative Example 1

A new type of soft capsule material formula:

Gelatin 67.5g;

Glycerin 18.75g;

Purified water 60g;

Polyethylene glycol-400 3.6g;

Titanium dioxide 0.15g.

Preparation steps: when 60g of purified water is heated to 60℃, 67.5g of gelatin and 18.75g of glycerol are mixed and added to purified water, then 0.15g of titanium dioxide and 3.6g of polyethylene glycol-400 are added, and after stirring for 2h, at 55℃ Incubate for 0.5h, let it stand for defoaming, and seal it for later use.

2. Evaluation of Oxygen Transmission Rate of Soft Capsules

Wet rubber skins of Examples 1-6 and Comparative Example 1 were respectively made by a capsule machine: the thicknesses were respectively 0.25mm (about 0.15mm after drying) and 0.75mm (about 0.50mm after drying); dried to a moisture content of 9.0%-12.0% After the bag material is removed, use an oxygen permeability tester to measure its oxygen permeability (Note: RH is relative humidity, h is hour, cc is volume/volume measurement unit cubic centimeter, cc/m ² . 24h is oxygen permeability unit of overrun).

Table 1 Oxygen permeability of soft capsule materials of Examples 1-6 and Comparative Example 1

The data results in Table 1 above show that the oxygen permeability of the soft capsule material of the embodiment of the present invention is significantly reduced.

3. Evaluation of the disintegration time limit of soft capsules

The soft capsule preparation of the same content: the glue liquid of above-mentioned embodiment 1-6 and comparative example 1 are respectively introduced into the pressing soft capsule machine for compression, and the formed rubber skin enters the rolling mold, and the content (for example: nimodipine liquid medicine) Injected from two pieces of rubber, washed and dried to obtain 100 soft capsules of Examples 1-6 and Comparative Example 1 respectively.

Evaluation method of disintegration time limit: Take 6 capsules of this product, follow the disintegration time limit inspection method (capsule method: hang the hanging basket of the disintegration apparatus on the metal bracket through the stainless steel shaft at the upper end, immerse it in a 1000ml beaker, and adjust the suspension. When the basket is positioned so that the screen is 25mm away from the bottom of the beaker, the beaker is filled with water with a temperature of 37°C ± 1°C, and the water level is adjusted so that the screen is 15mm below the water surface when the hanging basket is raised.), add a baffle, start Check the disintegration apparatus, the soft capsule should be completely disintegrated within 1 hour, if 1 capsule cannot be completely disintegrated, another 6 capsules should be taken for retest, all of which should meet the regulations.

The disintegration time limit of table 2 embodiment 1-6 and comparative example 1 soft capsule

Example Disintegration time (min) Example 1 8.3 Example 2 8 Example 3 9.3 Example 4 8.5 Example 5 9.7 Example 6 9 Comparative Example 1 15.2

The data results in Table 2 above show that the soft capsules of the embodiments of the present invention have excellent disintegration rates.

4. Soft capsule stability test

The soft capsules of Examples 1-6 and Comparative Example 1 with the contents introduced above were used as test samples to test the stability of the samples under different conditions. The dry storage conditions at room temperature were 25°C and relative humidity of 20%, the storage conditions at high temperature and high humidity were 60°C and relative humidity of 90%, and the shaking conditions were 100 times/min shaking and shaking, and 20 samples were taken for each test.

The stability of table 3 implementation 1-6 and comparative example 1 soft capsule under different conditions

Note: There is no obvious change in the high temperature and high humidity test. After 3 months, the surface of the soft capsule has a phenomenon of moisture absorption and softening, but it is not deformed, and there is no change from the initial state after drying.

The data results of above-mentioned Table 3 show: the stability of the soft capsule of the embodiment of the present invention is high.

Claims (6)

1. a novel soft capsule capsule material formula, is characterized in that, described capsule material component is by the gross weight of capsule material, and the weight percent of each component is: matrix 30～50%, polyglycerol 10～22% , sodium pyrophosphate 0.6-1.6%, purified water 35-55%, additives 1-5%; The matrix is one of sapura gum, xanthan gum, K-carrageenan, gelatin, guar gum, and peach gum, or a combination of any two or more. 2 . The formulation of a novel soft capsule material according to claim 1 , wherein the polymerization degree of the polymerized glycerin is 10-12. 3 . 3. a kind of novel soft capsule material formula according to claim 1, is characterized in that, described additive is opacifying agent titanium dioxide, disintegrating agent polyethylene glycol-400. 4. a kind of novel soft capsule material formula according to claim 1-3, is characterized in that, described disintegrant accounts for 2～5% of the total weight of capsule material, and the weight ratio of opacifying agent and matrix is 0.002 ~0.01:1. 5. a kind of novel soft capsule capsule material formulation as claimed in claim 1-4, is characterized in that, the preparation method of capsule material is: after matrix, polyglycerol, sodium pyrophosphate are mixed and added to 50～90 ℃ Add additives to purified water, stir for 1 to 3 hours, keep the temperature at 50 to 60°C for 0.5 to 2 hours, let it stand for defoaming, and seal it for later use. 6 . The preparation method according to claim 5 , wherein the temperature of the purified water is 50-90° C., preferably 70-85° C.; the holding time is 0.5-2 h, preferably 1.5-2 h. 7 .