CN110898003A - Novel bambuterol hydrochloride oral solution and preparation method thereof - Google Patents

Novel bambuterol hydrochloride oral solution and preparation method thereof Download PDF

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Publication number
CN110898003A
CN110898003A CN201911250365.9A CN201911250365A CN110898003A CN 110898003 A CN110898003 A CN 110898003A CN 201911250365 A CN201911250365 A CN 201911250365A CN 110898003 A CN110898003 A CN 110898003A
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Prior art keywords
bambuterol hydrochloride
preparation
parts
bambuterol
novel
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舒森
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YUEYANG XINHUADA PHARMACEUTICAL CO Ltd
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YUEYANG XINHUADA PHARMACEUTICAL CO Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Emergency Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The invention belongs to the technical field of pharmaceutical preparations, and discloses a novel bambuterol hydrochloride oral solution and a preparation method thereof. The oral liquid mainly comprises the following substances in parts by weight and volume: 1 part of bambuterol hydrochloride, 0-5 parts of sweetening agent, 0-2 parts of preservative, 0-10 parts of complexing agent and 0-1 part of flavoring agent. The preparation method comprises dissolving the above materials respectively, stirring thoroughly, diluting with purified water to constant volume, filtering with 0.45 μm and 0.22 μm filtration membrane for two-stage filtration, checking, canning, and sterilizing to obtain the final product. The preparation method is simple, fewer auxiliary materials are adopted, so that the side effect is small, and the obtained product is small in dosage, easy to absorb, stable in quality, easy to store and suitable for industrial production.

Description

Novel bambuterol hydrochloride oral solution and preparation method thereof
Technical Field
The invention belongs to the field of pharmaceutical preparation production, and particularly relates to a novel bambuterol hydrochloride oral solution and a preparation method thereof.
Background
Bambuterol hydrochloride is an important antiasthmatic medicinal component, which is also called as β 2-adrenergic receptor agonist (β 2-2 receptor agonist), and the pharmacological action of the bambuterol hydrochloride is mainly that when β 2-adrenergic receptor agonist stimulates β 2-adrenergic receptor (β 2-2 receptor for short) in the airway, the bambuterol hydrochloride acts on different effector cells of the airway, so that smooth muscle of the airway is relaxed, the cilia clearance function is enhanced, the release of inflammatory mediators is inhibited, the vascular permeability is reduced, and the asthmatic symptoms are relieved and eliminated, the action strength and the onset speed of the bambuterol hydrochloride are superior to those of other antiasthmatic medicaments.
Disclosure of Invention
The object of the present invention is to provide a new oral solution of bambuterol hydrochloride that responds to the problems mentioned in the background above.
The purpose of the invention can be realized by the following technical scheme: selecting 1 part of bambuterol hydrochloride, 0-5 parts of sweetening agent, 0-2 parts of preservative, 0-10 parts of complexing agent and 0-1 part of flavoring agent
The method specifically comprises the following steps:
1. weighing the bambuterol hydrochloride with the feeding amount, adding the bambuterol hydrochloride into a preparation tank, completely dissolving the bambuterol hydrochloride, and fully and uniformly stirring the bambuterol hydrochloride for 0.2 to 2 hours.
2. Weighing the complexing agent in the feeding amount, adding the complexing agent into a preparation tank, completely dissolving, and fully and uniformly stirring for 0.2-2 h.
3. Weighing the preservative with the feeding amount, putting the preservative into a proportioning tank, completely dissolving the preservative, and fully stirring the preservative for 0.2 to 5 hours.
4. Weighing a sweetener with a feeding amount, adding the sweetener into a preparation tank, metering the volume with purified water, and fully stirring until the solution is uniformly mixed; secondary filtration was carried out with 0.45 μm and 0.22 μm filter membranes.
5. Sampling the filtered clear liquid to detect the pH value and the content, wherein the pH value is 3.0-4.5.
6. Checking clarity and canning.
7. After canning, leak detection and sterilization are carried out, lamp inspection is carried out, liquid leakage is eliminated, the product is obtained when the product is damaged, the content is unqualified, the product is mildewed, turbid, contains foreign matters or other abnormal conditions, and the product is obtained when the product passes through the leak detection.
As a further preferable scheme, a stabilizer may be further added in the production process of the invention, including but not limited to one or more of polyethylene glycol 600, polyethylene glycol 6000, polyethylene glycol 800, polyethylene glycol 400, polyethylene glycol 80, and polyethylene glycol 200.
As a further preferable scheme, the preservative in the production process of the invention comprises one or more of p-hydroxybenzoic acid, p-hydroxyphenylmethylacetic acid, p-hydroxyphenylmethylpropionic acid, p-hydroxyphenylmethylbutanoic acid, sodium benzoate, sorbic acid and potassium sorbate.
The invention has the beneficial effects that: by fully dissolving the bambuterol hydrochloride, the effective components with the medicinal effect in the bambuterol hydrochloride are reserved, and the solid auxiliary materials which are difficult to dissolve in water are filtered out by a secondary filtration method, so that the auxiliary materials in the finished product are fewer, and the side effect of the auxiliary materials is reduced.
Detailed Description
The technical solution of the present invention will be further described with reference to the following examples.
Example 1
The components in the invention are composed of the following substances according to the weight and volume ratio: 1 part of bambuterol hydrochloride, 5 parts of cane sugar, 1.5 parts of sodium benzoate and 10 parts of edetate disodium, and the volume is determined to be 1000 parts by using purified water.
1. Adding the bambuterol hydrochloride with the batch charge into a preparation tank, completely dissolving, and fully and uniformly stirring for 2 hours.
2. Weighing disodium edetate according to the feeding amount, adding the disodium edetate into a preparation tank, completely dissolving, and fully and uniformly stirring for 1.5 h.
3. Weighing sodium benzoate and sucrose in the amount, adding into the mixing tank, dissolving completely, and stirring thoroughly for 3 hr.
4. Adding purified water to constant volume, and fully stirring until the solution is uniformly mixed; secondary filtration was carried out with 0.45 μm and 0.22 μm filter membranes.
5. Sampling and detecting the pH value and the content, wherein the pH value is 3.0-4.5.
6. Checking clarity and canning.
7. After canning, leakage detection and sterilization are carried out, lamp inspection is carried out, leakage liquid is eliminated, and the cases with damage and unqualified filling amount, mildewing, turbidity, foreign matters or other abnormal conditions are avoided. And if the leakage is detected, the finished product is obtained.
Example 2
The components in the invention are composed of the following substances according to the weight and volume ratio: 1 part of bambuterol hydrochloride, 2.5 parts of steviosin, 3 parts of citric acid, 5 parts of sodium citrate and 1 part of orange essence, and the volume is determined to be 1000 parts by using purified water.
1. Weighing the batroxobin hydrochloride with the feeding amount, adding the batroxobin hydrochloride into a preparation tank, completely dissolving, and fully and uniformly stirring for 2 hours.
2. Weighing steviosin with a feeding amount, putting into a mixing tank, dissolving completely, and stirring thoroughly for 3 h.
3. Weighing the orange essence with the feeding amount, putting into a mixing tank, completely dissolving, and fully stirring for 2 h.
4. Weighing citric acid and sodium citrate with feeding amount, putting into a mixing tank, dissolving completely, stirring thoroughly for 5h, adding purified water to constant volume, and stirring thoroughly until the solution is mixed uniformly; secondary filtration was carried out with 0.45 μm and 0.22 μm filter membranes.
5. Sampling and detecting the pH value and the content, wherein the pH value is 3.0-4.5.
6. Checking clarity and canning.
7. After canning, leakage detection and sterilization are carried out, lamp inspection is carried out, leakage liquid is eliminated, and the cases with damage and unqualified filling amount, mildewing, turbidity, foreign matters or other abnormal conditions are avoided. And if the leakage is detected, the finished product is obtained.
Example 3
The components in the invention are composed of the following substances according to the weight and volume ratio: 1 part of bambuterol hydrochloride, 2.5 parts of steviosin, 1.6 parts of p-hydroxybenzoic acid, 0.6 part of p-hydroxyphenylmethyl propionic acid, 3 parts of citric acid and 5 parts of sodium citrate, and the volume is fixed to 1000 parts by using purified water.
1. Weighing the batroxobin hydrochloride with the feeding amount, adding the batroxobin hydrochloride into a preparation tank, completely dissolving, and fully and uniformly stirring for 2 hours.
2. Weighing p-hydroxybenzoic acid and p-hydroxybenzoic propionic acid in the amount of raw materials, adding into the preparation tank, dissolving completely, stirring well for 1.5 h.
3. Weighing steviosin with a feeding amount, putting into a mixing tank, dissolving completely, and stirring thoroughly for 3 h.
4. Weighing citric acid and sodium citrate with feeding amount, putting into a mixing tank, dissolving completely, stirring thoroughly for 5h, adding purified water to constant volume, and stirring thoroughly until the solution is mixed uniformly; secondary filtration was carried out with 0.45 μm and 0.22 μm filter membranes.
5. Sampling and detecting the pH value and the content, wherein the pH value is 3.0-4.5.
6. Checking clarity and canning.
7. After canning, leakage detection and sterilization are carried out, lamp inspection is carried out, leakage liquid is eliminated, and the cases with damage and unqualified filling amount, mildewing, turbidity, foreign matters or other abnormal conditions are avoided. And if the leakage is detected, the finished product is obtained.
In clinical practice, after the oral administration of the product, about 20% of the oral dose is absorbed by blood test. After absorption, it is slowly metabolized to active terbutaline. The bambuterol hydrochloride and the intermediate metabolites show affinity for lung tissue, and the metabolism of the bambuterol hydrochloride into terbutaline also takes place in the lung tissue. Higher concentrations of active drug can be achieved in the lung. After the medicine is orally taken, the maximum plasma concentration of active metabolite terbutaline can be reached in about 7 hours, and the half-life period is about 17 hours. Can reduce degranulation and mediator release of mast cells and basophils, reduce permeability of microvessels, and increase cilia swing of airway epithelium, thereby playing a better role in relieving asthma symptoms.
The preferred embodiments of the invention disclosed above are intended to be illustrative only. The preferred embodiments are not intended to be exhaustive or to limit the invention to the precise embodiments disclosed. Obviously, many modifications and variations are possible in light of the above teaching. The embodiments were chosen and described in order to best explain the principles of the invention and the practical application, to thereby enable others skilled in the art to best utilize the invention. The invention is limited only by the claims and their full scope and equivalents.

Claims (8)

1. The novel bambuterol hydrochloride oral solution and the preparation method thereof are characterized by comprising the following components in parts by weight: 1 part of bambuterol hydrochloride, 0-5 parts of sweetening agent, 0-2 parts of preservative, 0-10 parts of complexing agent and 0-1 part of flavoring agent.
2. The novel bambuterol hydrochloride oral solution and the preparation method thereof according to claim 1 are characterized by comprising the following steps:
(1) weighing the bambuterol hydrochloride with the feeding amount, adding the bambuterol hydrochloride into a preparation tank, completely dissolving the bambuterol hydrochloride, and fully and uniformly stirring the bambuterol hydrochloride for 0.2 to 2 hours.
(2) Weighing the complexing agent in the feeding amount, adding the complexing agent into a preparation tank, completely dissolving, and fully and uniformly stirring for 0.2-2 h.
(3) Weighing the preservative with the feeding amount, putting the preservative into a proportioning tank, completely dissolving the preservative, and fully stirring the preservative for 0.2 to 5 hours.
(4) Weighing a sweetener with a feeding amount, adding the sweetener into a preparation tank, metering the volume with purified water, and fully stirring until the solution is uniformly mixed; secondary filtration was carried out with 0.45 μm and 0.22 μm filter membranes.
(5) Sampling the filtered clear liquid to detect the pH value and the content, wherein the pH value is 3.0-4.5.
(6) Checking clarity and canning.
(7) After canning, leak detection and sterilization are carried out, lamp inspection is carried out, liquid leakage is eliminated, the product is obtained when the product is damaged, the content is unqualified, the product is mildewed, turbid, contains foreign matters or other abnormal conditions, and the product is obtained when the product passes through the leak detection.
3. The novel bambuterol hydrochloride oral solution and the preparation method thereof according to claim 1 are characterized in that the sweetening agent in the ingredients can be sucrose or stevioside, and the weight ratio of bambuterol hydrochloride to sucrose is 1: 5-5.2; the weight ratio of the bambuterol hydrochloride to the stevioside is 1: 2.5-2.6.
4. The novel bambuterol hydrochloride oral solution and the preparation method thereof according to claim 1, characterized in that the preservative in the composition can be sodium benzoate or p-hydroxybenzoic acid, p-hydroxybenzoic propionic acid. The weight ratio of the bambuterol hydrochloride to the sodium benzoate is 1: 1.5; bambuterol hydrochloride, p-hydroxybenzoic acid methyl ester: the weight ratio of the p-hydroxyphenylmethyl propionic acid is 1: 1.6-1.8: 0.16-0.2.
5. The novel bambuterol hydrochloride oral solution and the preparation method thereof according to claim 1, wherein the complexing agent in the composition can be edetate disodium or citric acid, sodium citrate. The weight parts of the bambuterol hydrochloride, the edetate disodium, the citric acid and the sodium citrate are 1:10:3: 5.
6. The invention as claimed in claim 1, wherein the volume of the selected raw materials is 1000 parts by volume based on purified water.
7. The novel bambuterol hydrochloride oral solution and the preparation method thereof according to claim 1, characterized in that the flavoring agent includes but is not limited to one or more of sucrose, menthol, aspartame, saccharin sodium, sucralose, cherry essence, strawberry essence, vanilla essence, orange essence and other essences.
8. The new bambuterol hydrochloride oral solution and the process for its preparation according to claim 1, characterized in that the correspondence between the weights and volumes described is defined as: g for ml and kg for L.
CN201911250365.9A 2019-12-09 2019-12-09 Novel bambuterol hydrochloride oral solution and preparation method thereof Pending CN110898003A (en)

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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1210464A (en) * 1996-12-20 1999-03-10 阿斯特拉公司 Aqueous formulation comprising bambuterol and use thereof
CN104784106A (en) * 2014-01-17 2015-07-22 南京瑞尔医药有限公司 Bambuterol Hydrochloride oral liquid preparation method
CN104784108A (en) * 2014-01-17 2015-07-22 南京瑞尔医药有限公司 Bambuterol hydrochloride oral liquid composition

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1210464A (en) * 1996-12-20 1999-03-10 阿斯特拉公司 Aqueous formulation comprising bambuterol and use thereof
CN104784106A (en) * 2014-01-17 2015-07-22 南京瑞尔医药有限公司 Bambuterol Hydrochloride oral liquid preparation method
CN104784108A (en) * 2014-01-17 2015-07-22 南京瑞尔医药有限公司 Bambuterol hydrochloride oral liquid composition

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