Bowel-relaxing composition with good adhesive power and fluidity and preparation method of bowel-relaxing composition

By using polyols and appropriate gel matrix in the laxative composition, a gel preparation with good adhesion and fluidity was prepared, which solved the problems of spillover and low absorption efficiency of existing constipation treatment preparations, and achieved more effective drug effects and convenient drug administration process.

CN119868260AInactive Publication Date: 2025-04-25REGENEX PHARMA LTD
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Patent Information

Application Number
CN202510120180.5
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-01-25
Publication Date
2025-04-25
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

The existing rectal administration preparations for treating constipation are mostly liquid preparations, which are prone to spillover and seepage, have low drug absorption efficiency, and are inconvenient in the administration process. Especially for people with weak bodies or loose anal sphincter, the efficacy of the medicine is greatly reduced.

Method used

Provide a laxative composition that has good adhesion and fluidity, including polyol as a therapeutic ingredient and gel matrix such as carbomer and hyaluronic acid, to prepare suitable gel preparations by adjusting the component ratio and preparation method.

Benefits of technology

This laxative composition makes the medicine liquid less likely to overflow, is retained in the intestinal cavity more completely, exerts the efficacy of the medicine, increases the time the medicine liquid acts in the intestinal tract, promotes defecation, and balances adhesion and flow performance, solving the problems of low absorption efficiency and inconvenience of mobility.

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Abstract

The invention discloses a bowel-relaxing composition with good adhesive force and flowability, the bowel-relaxing composition comprises a treatment component and a gel matrix, the treatment component is polyhydric alcohol, the content of the polyhydric alcohol is 40-65%, and the treatment component can increase the moisture content in intestinal tracts, soften excrement and promote defecation; the gel matrix is selected from one or more of carbomer, hyaluronic acid, xanthan gum, chitosan and mannan, when the gel matrix is selected from carbomer, the content of the gel matrix is 0.10-0.18%, when the gel matrix is selected from hyaluronic acid, the content of the gel matrix is 0.3-1%, and when the gel matrix is selected from others, the content of the gel matrix is 0.1-4%. The proper application concentration is adjusted according to the influence of the matrix on the components, the adhesive force and the flowing property of the prepared bowel-relaxing composition are balanced, the problems that an existing bowel-relaxing preparation is low in absorption efficiency and inconvenient to move in the using process are solved, and the bowel-relaxing composition is particularly friendly to people suffering from anal sphincter relaxation and neurological disorder.
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Description

Technical Field

[0001] The present invention relates to the technical field of pharmaceutical preparations, and in particular to a laxative composition having good adhesion and fluidity and a preparation method thereof. Background Art

[0002] Constipation refers to a change in an individual's bowel habits, which is manifested as a decrease in the number of bowel movements and / or the discharge of dry and hard feces. Its incidence rate has been increasing year by year around the world, and the influencing factors are complex and diverse. Among the drugs for treating constipation, mainstream rectal preparations mostly use liquid preparations containing polyols, which have good safety and stable clinical application effects. Common polyol preparations such as enema, whose main ingredients are glycerin, sorbitol or mannitol, all use the hypertonic effect of polyol sugars to soften stools, stimulate the intestinal wall, and reflexively induce defecation reactions. In addition, they have a lubricating effect, which can make stools easy to discharge.

[0003] However, since the current rectal preparations for treating constipation are all liquid preparations, they are prone to overflow and exudation during the rectal administration stage. The drug stays in the intestinal cavity for a short time and has low absorption efficiency, resulting in incomplete defecation. At the same time, patients must remain in a supine or prone position for several minutes or even 30 minutes after administration. In order to prevent the drug from overflowing, some patients are required to maintain a prone kneeling position, which brings inconvenience to the patient's movements. Especially for some people with weak bodies, relaxed anal sphincters and neurological disorders, such as the elderly, people in the postoperative recovery period, women with multiple births, anorectal surgery patients, patients with long-term constipation and patients with neurological diseases, even if these people maintain a stable position, it is difficult to avoid a large amount of drug loss, resulting in a significant reduction in drug efficacy. In addition, maintaining this position will bring a higher risk of injury to certain groups of people.

[0004] In this regard, patent CN102670487A discloses a laxative gel and its preparation method, the raw materials of which include carbomer, nanosilver solution, ethanol, propylene glycol, ammonia water, ethyl paraben, natural plant extract essential oil, purified water and glycerol, which can effectively adhere to the intestinal wall and have a lasting effect. Patent JP1995291855A discloses a gel enema composition containing glycerol, carboxyvinyl polymer, water and alkaline substances, with a viscosity of 2,500 to 130,000 cps at 20 ° C and a pH of 6 to 10. However, although these preparations have a certain viscosity, it is difficult to take into account the fluidity of the liquid medicine, and the hypertonic characteristics of polyol sugars are weakened. There are still problems such as difficult extrusion, inconvenient administration, poor ductility, and limited absorption effect. In addition, a benzened polymer is added to the gel matrix of the formula, and there are safety hazards for long-term use. Summary of the invention

[0005] In order to overcome the problems existing in the prior art, one of the purposes of the present invention is to provide a laxative composition having both good adhesion and fluidity. Another purpose of the present invention is to provide a method for preparing the laxative composition having both good adhesion and fluidity.

[0006] In order to achieve the above object, the technical solution adopted by the present invention is: The first aspect of the present invention provides a laxative composition having good adhesion and fluidity, the laxative composition comprising a therapeutic component and a gel matrix, the therapeutic component being a polyol, the chemical formula of the polyol being: CH2OH-(CHOH)n-CH2OH, wherein n is an integer of 1-4; The gel matrix is ​​selected from one or more of carbomer, hyaluronic acid, xanthan gum, chitosan, and mannan; The content of the therapeutic ingredient is 40-65% by mass; When the gel matrix is ​​selected from carbomer, the content of the gel matrix is ​​0.10-0.18%; when the gel matrix is ​​selected from hyaluronic acid, the content of the gel matrix is ​​0.3-1%; when the gel matrix is ​​selected from others, the content of the gel matrix is ​​0.1-4%.

[0007] The gel matrix can also be a polymer with certain water solubility and safety, such as gelatin, sodium alginate, polyacrylamide, polyethylene glycol, sodium carboxymethylcellulose, povidone, and chitosan. The solvent of the laxative composition can be purified water.

[0008] Furthermore, the laxative composition having good adhesion and fluidity has a viscosity of 2600-20000 CP at room temperature, preferably 2600-13000 CP.

[0009] Further, when n is 1, the therapeutic ingredient is selected from glycerol; when n is 2, the therapeutic ingredient is selected from erythritol and / or threitol; when n is 3, the therapeutic ingredient is selected from one or more of xylitol, arabitol, lyxetol and ribitol; when n is 4, the therapeutic ingredient is selected from one or more of sorbitol, mannitol, iditol, altritol and talitol.

[0010] Furthermore, the carbomer is selected from carbomer 980, carbomer 971 and / or carbomer 974.

[0011] Furthermore, the molecular weight of the hyaluronic acid is 1.0-1.8M Da, preferably 1.4M Da.

[0012] Furthermore, it also includes an antibacterial agent and / or a pH adjusting agent; The antibacterial agent is selected from one or more of benzalkonium chloride, alkyl hydroxybenzoate, benzoate, sodium methylparaben, sodium ethylparaben, benzophenone-4, methylchloroisothiazolinone and sodium methylisothiazolinone benzoate; The pH regulator is selected from one or more of sodium chloride, sodium hydroxide, potassium hydrogen phosphate, sodium hydrogen phosphate, potassium hydroxide, potassium chloride, citric acid, hydrochloric acid, sodium acetate and sodium EDTA.

[0013] Wherein, the content of the antibacterial agent is 0.02-0.2% by mass, for example, it can be 0.18% sodium methylparaben and 0.02% sodium ethylparaben.

[0014] Further, it also includes a stabilizer; The stabilizer is selected from one or more of carboxyvinyl polymer, alginic acid, gum arabic, agar, carrageenan, gelatin, hydroxypropyl cellulose, carboxymethyl cellulose, and polyvinyl pyrrolidone.

[0015] Furthermore, when the gel matrix is ​​selected from carbomer, hyaluronic acid and xanthan gum, the content of the gel matrix is ​​0.1-2%, and the mass ratio of the carbomer, the hyaluronic acid and the xanthan gum is (0.02-0.3): (0.02-0.5): (0.06-1.2).

[0016] Furthermore, the laxative composition having good adhesion and fluidity comprises, by mass percentage, any one of the components (1) to (4): (1) Glycerin 40-65% and Carbomer 0.10-0.18%; (2) Glycerin 40-65% and hyaluronic acid 0.3-1%; (3), 40-65% glycerol and 0.1-4% other gel matrix, wherein the other gel matrix is ​​xanthan gum, chitosan or mannan; (4) A mixture of any two or three of (1) to (3).

[0017] Furthermore, the laxative composition having good adhesion and fluidity comprises, by mass percentage, any one of the components (1) to (4): (1) Glycerol 50-60% and carbomer 0.115-0.175%; (2) Glycerin 50-60% and hyaluronic acid 0.3-0.8%; (3), 50-60% glycerol and 1.5-3% other gel matrix, wherein the other gel matrix is ​​xanthan gum, chitosan or mannan; (4) A mixture of any two or three of (1) to (3).

[0018] Furthermore, the laxative composition having good adhesion and fluidity comprises, by mass percentage, any one of the components (1) to (4): (1) Glycerol 52.8-58.3% and Carbomer 0.13-0.17%; (2) Glycerin 52.8-58.3% and hyaluronic acid 0.5-0.8%; (3), 52.8-58.3% glycerol and 1.5-2.0% other gel matrix, wherein the other gel matrix is ​​xanthan gum, chitosan or mannan; (4) A mixture of any two or three of (1) to (3).

[0019] The second aspect of the present invention provides a method for preparing the laxative composition having good adhesion and fluidity, comprising the following steps: Weigh a prescribed amount of the therapeutic ingredient and stir and mix with purified water, then slowly add the prescribed amount of the gel matrix and stir and mix to obtain a mixed solution; The mixed solution is allowed to stand and swell, and the pH value is adjusted to obtain the laxative composition with good adhesion and fluidity.

[0020] The speed of stirring and mixing with purified water is 50-100 rpm, preferably 50 rpm; the time of stirring and mixing with purified water is 3-5 min, preferably 5 min. The speed of stirring and mixing with the gel matrix is ​​100-1000 rpm, preferably 500 rpm; the time of stirring and mixing with the gel matrix is ​​1-2 h, preferably 1 h. The time of standing and swelling is 10-30 h, preferably 12 h. The pH is adjusted to 6.8-7.0.

[0021] The beneficial effects of the present invention are: The present invention provides a laxative composition with good adhesion and fluidity, comprising a therapeutic component and a gel matrix, wherein C 3~6Polyol is used as the main drug, with a content of 40-65%, which can increase the moisture content in the intestine, soften feces, and promote defecation; Carbomer, hyaluronic acid, xanthan gum and other gel matrices are selected and adjusted according to the influence of the matrix on the components, and the appropriate application concentration is made into a gel preparation with certain adhesion and fluidity at the same time. The gel preparation of the present invention makes the liquid medicine not easy to overflow and more completely retained in the intestinal cavity, can give full play to the efficacy, effectively stimulate intestinal peristalsis, can increase the time of the liquid medicine acting on the intestinal tube, so that the defecation volume is increased more thoroughly; at the same time, the liquid medicine is easier to extend and absorb under the intestinal tube environment, making defecation more thorough and not easy to cause liquid medicine residue. The laxative composition of the present invention has reached a balance between adhesion and fluidity, solves the problems of low absorption efficiency and inconvenient action during the use of existing laxative preparations, and is especially friendly to anal sphincter relaxation and neurological disorders. At the same time, the improved laxative gel preparation has simple ingredients, good efficacy, no irritation, and has a good medicinal prospect.

[0022] The present invention also provides a method for preparing the laxative composition with good adhesion and fluidity. The prescribed amount of therapeutic ingredients is first stirred and mixed with purified water, and then the prescribed amount of gel matrix is ​​slowly added and fully swelled to obtain the laxative composition with good adhesion and fluidity. The preparation method is simple and easy, the physical properties of the obtained product are suitable, and the user experience is good. BRIEF DESCRIPTION OF THE DRAWINGS

[0023] Figure 1 Flow curves of gel preparations prepared for Example 1, Comparative Example 4 and Comparative Example 6; Figure 2 Viscoelastic modulus curves of the gel preparations prepared for Example 1, Comparative Example 4 and Comparative Example 6. DETAILED DESCRIPTION

[0024] The present invention is further described in detail below through specific examples. The materials used in the following examples, unless otherwise specified, can be obtained from conventional commercial sources or prepared and separated by simple synthesis; the processes used, unless otherwise specified, are conventional processes in the art.

[0025] Example

[0026] This embodiment provides a laxative composition with good adhesion and fluidity, and the preparation method thereof is as follows: (1) Weigh the prescribed amount of therapeutic ingredients and purified water in a beaker, turn on the stirrer, adjust the speed to 50 rpm, and stir for 5 minutes to mix the therapeutic ingredients and purified water evenly, wherein the therapeutic ingredient is glycerol; (2) slowly adding the prescribed amount of gel matrix to the above solution several times, and gradually adjusting the speed of the overhead electronic stirrer to 500 rpm; after the addition is completed, continue stirring for 1 hour, wherein the gel matrix is ​​carbomer 980, hyaluronic acid and / or xanthan gum; (3) Stop stirring and let the gel stand overnight to allow the gel matrix to fully swell. Then use hydrochloric acid solution and sodium hydroxide solution to adjust the gel pH to 6.8-7.0.

[0027] Referring to the above preparation method, a laxative composition with good adhesion and fluidity was prepared according to the components in Table 1.

[0028] Table 1 Components Example 1 Example 2 Example 3 Example 4 Example 5 Example 6 Example 7 Example 8 glycerin 53 58 56 53 58 54 55 55 Carbomer 0.17 (Carbomer 980) 0.13 (Carbomer 974) 0.15 (Carbomer 980) / / / / 0.1 (Carbomer 980) Hyaluronic acid / / / 0.5 0.7 / / 0.2 Xanthan gum / / / / / 1.5 2.0 0.8 water 46.82 41.85 43.84 46.5 41.3 44.5 43.0 43.9

[0029] Comparative Example Referring to the preparation method of the embodiment, a laxative composition was prepared according to the components in Table 2.

[0030] Table 2 Components Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Comparative Example 6 glycerin 55 57 55 54 55 75 Carbomer / 0.3 (Carbomer 934) 0.1 (Carbomer 980) 0.4 (Carbomer 940) / 0.2 (Carbomer 940) Hyaluronic acid / / / / 0.3 / water 45 42.7 44.9 45.6 44.7 24.8

[0031] Test Example 1 The viscosity of the gel preparations prepared in Examples 1 to 8 and Comparative Examples 1 to 6 was tested by using a commercially available common viscometer to set parameters and test under corresponding conditions. The test temperature was room temperature. The test setting parameters and test results are shown in Table 3.

[0032] Table 3 Group pH Viscometer Spindle Speed ​​(rpm) Torque (%) Viscosity (CP) Example 1 6.82 S64 30 60.8 12160 Example 2 6.86 S63 20 49.4 2963 Example 3 6.92 S64 50 45.0 5400 Example 4 6.83 S63 12 50.9 5089 Example 5 6.89 S64 20 42.7 12810 Example 6 6.90 S63 20 42.7 4500 Example 7 7.66 S63 6 63.0 12600 Example 8 6.90 S64 50 59.5 10980 Comparative Example 1 7.02 S61 100 20.8 12.48 Comparative Example 2 6.87 S64 4 70.8 106200 Comparative Example 3 6.90 S62 100 39.7 119 Comparative Example 4 6.85 S64 4 68.4 124600 Comparative Example 5 6.92 S63 100 51.3 615 Comparative Example 6 6.87 S64 10 62.3 69410 The data in Table 3 show that the viscosity of the gel composition obtained in Examples 1 to 8 is more suitable, ranging from 2963 to 12810 CP. The viscosity of the traditional enema preparation (Comparative Example 1) is only 12.48 CP. When the gel matrix content is low (Comparative Example 3 and Comparative Example 5), the product viscosity is low, 119 CP and 615 CP, respectively. When the gel matrix content is high (Comparative Example 2 and Comparative Example 4), the product viscosity is high, 106200 CP and 124600 CP, respectively. The viscosity of the gel composition (Comparative Example 6) obtained by reference to patent CN102670487A is high, 69410 CP.

[0033] Test Example 2 The gel preparations prepared in Examples 1 to 8 and Comparative Examples 1 to 6 were subjected to simulated vaginal or anorectal retention tests, and the test method was as follows: (1) Take 600 ml of aqueous medium in a 1L beaker and place it in a disintegrator at a constant temperature of 37±1℃ in a water bath; (2) Take a sample loop (inner diameter 15 mm) and place it in the center area of ​​the flat plate. Weigh about 100 mg of the gel preparation samples prepared in Examples 1 to 8 and Comparative Examples 1 to 6 and spread them on the inner area of ​​the sample loop. Let the samples stand for 5 minutes. (3) Connect the plate to the disintegrator and move it up and down in the aqueous medium so that the preparation is completely above the medium liquid surface at the highest point and completely immersed in the medium at the lowest point, until the preparation completely disappears on the agar plate. The time recorded is the sample retention time.

[0034] The test results are shown in Table 4.

[0035] Table 4 Group Residence time Group Detention time Example 1 4min12s Example 8 3min23s Example 2 1min09s Comparative Example 1 2s Example 3 2min48s Comparative Example 2 9min04s Example 4 2min02s Comparative Example 3 14s Example 5 3min52s Comparative Example 4 10min12s Example 6 1min06s Comparative Example 5 29s Example 7 4min15s Comparative Example 6 7min58s The data in Table 4 show that the simulated retention time of the gel composition obtained in Examples 1 to 8 is more suitable, ranging from 1min06s to 4min15s. The traditional enema preparation (Comparative Example 1) is only 2s. When the gel matrix content is low (Comparative Example 3 and Comparative Example 5), the simulated retention time of the product is short, 14s and 29s respectively. When the gel matrix content is high (Comparative Example 2 and Comparative Example 4), the simulated retention time of the product is long, 9min04s and 10min12s respectively. The simulated retention time of the gel composition (Comparative Example 6) obtained by reference to patent CN102670487A is long, 7min58s.

[0036] Test Example 3 The gel preparations prepared in Example 1, Comparative Example 4 and Comparative Example 6 were subjected to flow curve testing, and the test application information is as follows: Rheometer: MARS iQ Air; rotor model: P20 / Ti / SB; temperature controller: MTMC-iQ (MARS iQAir); measuring gap: 0.4000 mm; measuring volume: 0.16 mL.

[0037] The parameters are set as follows: 1) Measurement position: sample scraping edge position = gap + 0.010mm; 2) Set temperature (preheating): CS; shear stress τ = 0.000 Pa; time t = 60.00 s; temperature T: 25.00 °C; 3) Rotation time scan: Mode: CR; Shear rate-continuous parameters: ɣ̇=0.1000 1 / s; Time t=60.00s; Temperature T: 25.00℃; No saving; 4) Rot step scan: Mode: CR; Shear rate-continuous parameter: ɣ̇=0.1000 1 / s~1000. 1 / s; Distribution: log; # of steps: 30; Temperature T: 25.00℃.

[0038] The viscoelastic modulus curve (frequency sweep) test was performed on the gel preparations prepared in Example 1, Comparative Example 4 and Comparative Example 6. The test application information is as follows: Rheometer: MARS iQ Air; rotor model: P20 / Ti / SB; temperature controller: MTMC-iQ (MARS iQAir); measuring gap: 0.4000 mm; measuring volume: 0.16 mL.

[0039] The parameters are set as follows: 1) Measurement position: sample scraping edge position = gap + 0.010mm; 2) Set temperature (preheating): CS; stress τ = 0.000 Pa; time t = 60.00 s; temperature: 25.00℃; 3) Osc oscillation frequency sweep: mode: CS; shear stress τ = 5.000 Pa; frequency-sweep parameters: f = 0.01592 ~ 1 Hz; distribution: log; steps / decade: 9; temperature: 25.00 °C.

[0040] Flow curve Figure 1 , the viscoelastic modulus curve is shown in Figure 2 .

[0041] Figure 1 The curve characterizes the difficulty of sample flow. The higher the curve appears, the more difficult the sample is to flow. The figure shows that the sample in Example 1 is easier to flow. The fluidity is from best to worst in the order of Example 1, Comparative Example 6 and Comparative Example 4.

[0042] Figure 2 In the figure, the elastic modulus and viscous modulus of the samples are characterized. The figure shows that as the frequency increases, the sample of Example 1 will show a viscous modulus higher than the elastic modulus within a certain frequency range, proving that it is easier to deform and flow. However, the samples of Comparative Examples 4 and 6 do not show the above characteristics, indicating that the samples of Comparative Examples 4 and 6 have poor fluidity.

[0043] Test Example 4 The samples (specification: 20 ml) prepared from Examples 1 to 8 (sample numbers A1 to A8) and Comparative Examples 1 to 6 (sample numbers B1 to B6) were distributed to 50 testers, with 2 bottles of each sample prepared (divided into a test group and a control group). Each tester was instructed to self-use the medication once every other day in a fixed time period every day according to the following operating method.

[0044] Experimental group: The participants sat flat, inserted the sample into the anus, squeezed out the sample for a while and then took out the applicator. They maintained the posture for 1-2 minutes and then stood for 1-5 minutes. They defecated when they felt the urge to do so. The defecation time and drug leakage time since the drug administration, as well as the comfort level from drug administration to defecation were recorded.

[0045] Control group: The participants lie in the knee-chest position, insert the sample deep into the anus, squeeze out the sample for a while and then take out the applicator, maintain the position for 1-5 minutes, and defecate when they feel the urge to do so. The defecation time and drug leakage time since the drug administration, as well as the comfort level from drug administration to defecation are recorded.

[0046] After the experience, the participants evaluated the experience according to the evaluation criteria in Table 5. The statistical examples of the evaluation results of leakage time, defecation time and comfort of all participants are shown in Tables 6 to 8.

[0047] Table 5

[0048] Table 6

[0049] The data in Table 6 show that the gel compositions obtained in Examples 1 to 8 have the same performance in the test group and the control group. Even if the body positions such as sitting and standing are adopted, the liquid medicine can be well retained in the body until defecation without leakage. However, the traditional enema preparation (Comparative Example 1) will also have a small number of early leakages when the knee-chest position is adopted, and this leakage phenomenon is more significant when the body positions such as sitting and standing are adopted. When the gel matrix content is low (Comparative Examples 3 and 5), there is basically no leakage when the knee-chest position is adopted, but leakage phenomena of varying degrees are presented in the test group. When the gel matrix content is high (Comparative Examples 2 and 4) and the gel composition obtained by reference to patent CN102670487A, its leakage time performance is the same as that of each embodiment.

[0050] Table 7

[0051] The data in Table 7 show that the gel compositions obtained in Examples 1 to 8 have the same performance in the test group and the control group, the drug solution can be well retained in the body, and the drug efficacy and absorption are good, and defecation can be performed within 10 minutes after administration. However, the traditional enema preparation (Comparative Example 1) will defecate within 10 to 20 minutes after administration when the knee-chest position is adopted, and defecation will occur 20 minutes after administration when the sitting position, standing position and other positions are adopted, which may be related to the problem of drug leakage. When the gel matrix content is low (Comparative Example 3 and Comparative Example 5), the performance in the test group and the control group is similar, and there is a slight phenomenon of delayed defecation time. The possible reason is that a small amount of drug leakage affects the absorption efficiency. When the gel matrix content is high (Comparative Example 2 and Comparative Example 4) and the gel composition obtained by reference to patent CN102670487A, the performance in the test group and the control group is similar, and the defecation time is delayed to varying degrees, which may be related to the poor fluidity of the drug solution, difficult absorption, and easy to cause residue.

[0052] Table 8

[0053] The data in Table 8 show that the gel compositions prepared in Examples 1 to 8 have the same performance in the test group and the control group, the drug effect is sufficient and the safety is good, and the experiencers do not feel pain or irritation during use, and there is no incomplete defecation phenomenon. The traditional enema preparation (Comparative Example 1) has similar performance in the test group and the control group, with irritation and incomplete defecation. The irritation may be related to the direct hypertonic effect of glycerol. Due to the absence of gel matrix, the drug effect is strong and has a certain irritation, which will cause the experiencer to defecate prematurely, shorten the drug action time, and thus cause the phenomenon of incomplete defecation. When the gel matrix content is low (Comparative Example 3 and Comparative Example 5), the performance in the test group and the control group is similar, with slight pain, irritation and incomplete defecation. The possible reason is that the gel matrix has a weak effect, the ability to alleviate hypertonicity is limited, and there is a slight adverse feeling to the body. When the gel matrix content is high (Comparative Example 2 and Comparative Example 4) and the gel composition prepared by reference patent CN102670487A, the performance in the test group and the control group is similar, with partial pain, irritation and incomplete defecation, which may be related to the poor fluidity of the drug solution, which is not easy to extend and absorb, and is easy to accumulate and remain in the body.

[0054] The above embodiments are preferred implementation modes of the present invention, but the implementation modes of the present invention are not limited to the above embodiments. Any other changes, modifications, substitutions, combinations, and simplifications that do not deviate from the spirit and principles of the present invention should be equivalent replacement methods and are included in the protection scope of the present invention.

Claims

1. A laxative composition having good adhesion and fluidity, characterized in that: The laxative composition comprises a therapeutic component and a gel matrix, wherein the therapeutic component is a polyol, and the chemical formula of the polyol is: CH2OH-(CHOH)n-CH2OH, wherein n is an integer of 1-4; The gel matrix is ​​selected from one or more of carbomer, hyaluronic acid, xanthan gum, chitosan, and mannan; The content of the therapeutic ingredient is 40-65% by mass; When the gel matrix is ​​selected from carbomer, the content of the gel matrix is ​​0.10-0.18%; when the gel matrix is ​​selected from hyaluronic acid, the content of the gel matrix is ​​0.3-1%; when the gel matrix is ​​selected from others, the content of the gel matrix is ​​0.1-4%.

2. The laxative composition having good adhesion and fluidity according to claim 1, characterized in that: The laxative composition having good adhesion and fluidity has a viscosity of 2600-20000 CP at room temperature.

3. The laxative composition having good adhesion and fluidity according to claim 1, characterized in that: When n is 1, the therapeutic ingredient is selected from glycerol; when n is 2, the therapeutic ingredient is selected from erythritol and / or threitol; when n is 3, the therapeutic ingredient is selected from one or more of xylitol, arabitol, lyxetol and ribitol; when n is 4, the therapeutic ingredient is selected from one or more of sorbitol, mannitol, iditol, altritol and talitol.

4. The laxative composition having good adhesion and fluidity according to claim 1, characterized in that: The carbomer is selected from carbomer 980, carbomer 971 and / or carbomer 974.

5. The laxative composition having good adhesion and fluidity according to claim 1, characterized in that: The molecular weight of the hyaluronic acid is 1.0~1.8M Da.

6. The laxative composition having good adhesion and fluidity according to claim 1, characterized in that: When the gel matrix is ​​selected from carbomer, hyaluronic acid and xanthan gum, the content of the gel matrix is ​​0.1-2%, and the mass ratio of the carbomer, the hyaluronic acid and the xanthan gum is (0.02-0.3): (0.02-0.5): (0.06-1.2).

7. The laxative composition having good adhesion and fluidity according to claim 1, characterized in that: The laxative composition having good adhesion and fluidity comprises, by mass percentage, any one of the components (1) to (4): (1) Glycerin 40-65% and Carbomer 0.10-0.18%; (2) Glycerin 40-65% and hyaluronic acid 0.3-1%; (3), 40-65% glycerol and 0.1-4% other gel matrix, wherein the other gel matrix is ​​xanthan gum, chitosan or mannan; (4) A mixture of any two or three of (1) to (3).

8. The laxative composition having good adhesion and fluidity according to claim 1, characterized in that: The laxative composition having good adhesion and fluidity comprises, by mass percentage, any one of the components (1) to (4): (1) Glycerol 50-60% and carbomer 0.115-0.175%; (2) Glycerin 50-60% and hyaluronic acid 0.3-0.8%; (3), 50-60% glycerol and 1.5-3% other gel matrix, wherein the other gel matrix is ​​xanthan gum, chitosan or mannan; (4) A mixture of any two or three of (1) to (3).

9. The laxative composition having good adhesion and fluidity according to claim 1, characterized in that: The laxative composition having good adhesion and fluidity comprises, by mass percentage, any one of the components (1) to (4): (1) Glycerol 52.8-58.3% and Carbomer 0.13-0.17%; (2) Glycerin 52.8-58.3% and hyaluronic acid 0.5-0.8%; (3), 52.8-58.3% glycerol and 1.5-2.0% other gel matrix, wherein the other gel matrix is ​​xanthan gum, chitosan or mannan; (4) A mixture of any two or three of (1) to (3).

10. The method for preparing the laxative composition having good adhesion and fluidity according to any one of claims 1 to 9, characterized in that: The steps include: Weigh a prescribed amount of the therapeutic ingredient and stir and mix with purified water, then slowly add the prescribed amount of the gel matrix and stir and mix to obtain a mixed solution; The mixed solution is allowed to stand and swell, and the pH value is adjusted to obtain the laxative composition with good adhesion and fluidity.

Citation Information

Patent Citations

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