CN115137704A - Captopril orally disintegrating tablet - Google Patents

Captopril orally disintegrating tablet Download PDF

Info

Publication number
CN115137704A
CN115137704A CN202210281651.7A CN202210281651A CN115137704A CN 115137704 A CN115137704 A CN 115137704A CN 202210281651 A CN202210281651 A CN 202210281651A CN 115137704 A CN115137704 A CN 115137704A
Authority
CN
China
Prior art keywords
captopril
orally disintegrating
disintegrating tablet
excipient
tablet
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN202210281651.7A
Other languages
Chinese (zh)
Inventor
孙钦勇
咸鑫
刘忠
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shandong New Time Pharmaceutical Co Ltd
Original Assignee
Shandong New Time Pharmaceutical Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Shandong New Time Pharmaceutical Co Ltd filed Critical Shandong New Time Pharmaceutical Co Ltd
Publication of CN115137704A publication Critical patent/CN115137704A/en
Pending legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Zoology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention provides a captopril orally disintegrating tablet, which comprises captopril as an active ingredient, a filling agent, a disintegrating agent, an excipient and other pharmaceutically acceptable auxiliary materials, wherein the excipient is selected from one or more of borneol, camphor, menthol, limonene, isoborneol and paeonol; the captopril orally disintegrating tablet prepared by the invention does not need to be swallowed, and has high disintegrating speed, high dissolution speed and quick effect; high medicine content, obviously reduced content of impurity captopril disulfide, high stability and simple preparation process.

Description

Captopril orally disintegrating tablet
Technical Field
The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a captopril orally disintegrating tablet.
Background
It is well known that hypertension is the leading factor in cardiovascular and cerebrovascular diseases, and causes various complications. The patients with hypertension have various serious consequences, namely complications of hypertension, because the arterial pressure is continuously increased to cause systemic arteriosclerotic diseases, thereby influencing the blood supply of tissues and organs. The common complications of hypertension include coronary heart disease, diabetes, heart failure, hyperlipidemia, nephropathy, peripheral artery disease, apoplexy, and left ventricular hypertrophy. Among various complications of hypertension, the damage to the heart, brain and kidneys is most significant. Captopril is an angiotensin converting enzyme inhibitor and is commonly used in the treatment of acute hypertension. Captopril exerts its greatest pharmacological effect within 1-2 hours after oral administration, whereas in the emergency room patients suffering from acute hypertension are often sublingually buccally taken instead of orally taken captopril tablets. This is because the drug is absorbed before passing through the gastric mucosa, and can exert an antihypertensive effect more quickly. The captopril is prepared into the rapid orally disintegrating tablet, so that the rapid orally disintegrating tablet not only can rapidly play a role in reducing blood pressure, but also can meet the requirements of patients who have difficulty in swallowing captopril conventional tablets, and the medicine taking compliance of the patients is improved.
At present, most of current captopril preparations are captopril conventional tablets, and most of the captopril preparations are wet granulation tabletting, so that the operation is complicated, the production cost is high, the impurity content is high, and the product quality is influenced. Chinese patent CN107595791A discloses a captopril tablet prepared by a direct tabletting method, which improves the stability of the product, but has large tablet weight and slow effect. No research on captopril orally disintegrating tablets is provided in China.
Disclosure of Invention
In view of the defects of the prior art and the clinical application requirements, the invention aims to provide a captopril orally disintegrating tablet which has the advantages of quick response, good stability and simple preparation process. Specifically, the purpose of the invention is realized by the following technical scheme:
an orally disintegrating tablet of captopril comprises captopril, a filler, a disintegrant, an excipient and other pharmaceutically acceptable auxiliary materials; the excipient is one or more selected from Borneolum Syntheticum, camphora, menthol, limonene, isoborneol, and paeonol.
Preferably, the excipient is selected from one or more of borneol, camphor and menthol.
Further preferably, the excipient is one selected from borneol and menthol.
Preferably, the captopril orally disintegrating tablet comprises, by weight, 20% -35% of captopril, 45% -70% of a filler, 1% -10% of a disintegrant and 2.5% -15% of an excipient; further preferably, the excipient accounts for 2.5-5% by weight.
Preferably, the filler is selected from one or more of mannitol, microcrystalline cellulose, compressible starch, lactose, sorbitol and inorganic calcium salt; further preferably, the filler is selected from one or more of compressible starch and lactose.
Preferably, the disintegrating agent is selected from one or more of sodium carboxymethyl starch, sodium bicarbonate, citric acid, cross-linked sodium carboxymethyl cellulose, cross-linked polyvinylpyrrolidone, dry starch and low-substituted hydroxypropyl cellulose; further preferably, the disintegrating agent is selected from one or more of sodium carboxymethyl starch, croscarmellose sodium and low-substituted hydroxypropyl cellulose.
Preferably, the other pharmaceutically acceptable auxiliary materials in the captopril orally disintegrating tablet comprise a binder, a lubricant and a flavoring agent.
Further preferably, the captopril orally disintegrating tablet comprises captopril, a filling agent, a disintegrating agent, an excipient, a binding agent, a lubricating agent and a flavoring agent; the excipient is menthol.
Preferably, the lubricant is selected from one or more of magnesium lauryl sulfate, polyethylene glycol 4000, polyethylene glycol 6000, magnesium stearate, aerosil, talcum powder and hydrogenated vegetable oil.
Preferably, the binder is selected from one or more of hydroxypropyl cellulose, povidone, polyethylene glycol 4000, crospovidone, croscarmellose sodium, polacrilin potassium and microcrystalline cellulose.
Preferably, the flavoring agent is one or more selected from sucrose, simple syrup, flavoring syrup, stevioside, sodium cyclamate, aspartame and saccharin sodium.
Preferably, the orally disintegrating tablet of captopril comprises the following components in percentage by weight:
Figure BDA0003557158960000021
further preferably, the orally disintegrating tablet of captopril comprises the following components in percentage by weight:
Figure BDA0003557158960000022
Figure BDA0003557158960000031
on the other hand, the invention provides a preparation method of the captopril orally disintegrating tablet, which is prepared by directly tabletting powder and drying after tabletting.
Preferably, the raw and auxiliary materials in the powder direct compression method are respectively sieved by a sieve of 40-80 meshes, and further preferably, the raw and auxiliary materials are respectively sieved by a sieve of 50-70 meshes.
Preferably, the preparation method of the orally disintegrating tablet of captopril comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a sieve of 40-80 meshes for later use;
2) Adding the sieved captopril, excipient, filler, disintegrant, correctant and adhesive into a mixer, and mixing thoroughly, wherein the excipient is selected from one or more of Borneolum Syntheticum, camphora, menthol, limonene, isoborneol and paeonol;
3) Adding the sieved lubricant, and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder;
5) And (3) placing the orally disintegrating tablets in a drying oven for drying.
Further preferably, the preparation method of the captopril orally disintegrating tablet comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a 50-mesh sieve for later use;
2) Adding the sieved captopril, excipient, filler, disintegrant, correctant and adhesive into a mixer, and mixing thoroughly, wherein the excipient is selected from one or more of Borneolum Syntheticum, camphora, menthol, limonene, isoborneol and paeonol;
3) Then adding the sieved lubricant and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder;
5) And (3) placing the orally disintegrating tablets in a drying oven for drying at the temperature of 40-60 ℃ for 6-12 hours.
Compared with the prior art, the invention has the following technical effects:
(1) The prepared captopril orally disintegrating tablet does not need to be swallowed, and has high disintegrating speed, high dissolution speed, quick response and high bioavailability;
(2) The prepared captopril orally disintegrating tablet has high medicine content, obviously reduced content of impurity captopril disulfide and high stability;
(3) The prepared captopril orally disintegrating tablet adopts a powder direct tabletting method, simplifies the process route and saves the cost.
Detailed Description
The invention is further illustrated by the following examples, which should be properly understood: the examples of the present invention are intended to illustrate the present invention, not to limit the present invention, therefore, the simple modifications of the present invention in the method of the present invention are all within the scope of the present invention as claimed.
Example 1
Prescription:
Figure BDA0003557158960000041
the preparation method comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a 50-mesh sieve for later use;
2) Adding the sieved captopril, compressible starch, croscarmellose sodium, menthol, povidone and aspartame into a mixer, and fully mixing;
3) Then adding the sieved magnesium lauryl sulfate and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder according to the mass of each tablet being 100 mg;
5) And (3) placing the orally disintegrating tablets in a drying oven at 40 ℃, and drying for 10h.
Example 2
Prescription:
Figure BDA0003557158960000042
the preparation method comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a 50-mesh sieve for later use;
2) Adding the sieved captopril, lactose, sodium carboxymethyl starch, menthol, hydroxypropyl methylcellulose and saccharin sodium into a mixer for fully mixing;
3) Adding the sieved PEG4000, and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder according to the mass of each tablet being 100 mg;
5) The orally disintegrating tablets are placed in a drying oven at 40 ℃ and dried for 10h.
Example 3
Prescription:
Figure BDA0003557158960000051
the preparation method comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a 50-mesh sieve for later use;
2) Adding the sieved captopril, lactose, low-substituted hydroxypropyl cellulose, menthol, potassium polycryline and sodium cyclamate into a mixer for fully mixing;
3) Adding the sieved PEG6000, and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder according to the mass of each tablet being 100 mg;
5) The orally disintegrating tablets are placed in a drying oven at 40 ℃ and dried for 10h.
Example 4
Prescription:
Figure BDA0003557158960000052
Figure BDA0003557158960000061
the preparation method comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a 50-mesh sieve for later use;
2) Adding the sieved captopril, compressible starch, croscarmellose sodium, sodium carboxymethyl starch, menthol, povidone and simple syrup into a mixer for fully mixing;
3) Adding the sieved magnesium lauryl sulfate, and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder according to the mass of each tablet being 100 mg;
5) The orally disintegrating tablets are placed in a drying oven at 40 ℃ and dried for 10h.
Example 5
Prescription:
Figure BDA0003557158960000062
the preparation method comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a 80-mesh sieve for later use;
2) Adding the sieved captopril, mannitol, citric acid, sodium bicarbonate, borneol, hydroxypropyl methylcellulose and aspartame into a mixer for fully mixing;
3) Adding the sieved magnesium stearate, and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder according to the mass of each tablet being 100 mg;
5) The orally disintegrating tablets are placed in a drying oven at 40 ℃ and dried for 10h.
Example 6
Prescription:
Figure BDA0003557158960000071
the preparation method comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a 50-mesh sieve for later use;
2) Adding the sieved captopril, mannitol, crospovidone, menthol, povidone and aspartame into a mixer for fully mixing;
3) Adding the sieved magnesium lauryl sulfate, and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder according to the mass of each tablet being 100 mg;
5) The orally disintegrating tablets are placed in a drying oven at 40 ℃ and dried for 10h.
Example 7
Prescription:
Figure BDA0003557158960000072
the preparation method comprises the following steps:
1) Weighing the raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a 40-mesh sieve for later use;
2) Adding the sieved captopril, compressible starch, croscarmellose sodium, borneol, microcrystalline cellulose and aspartame into a mixer for fully mixing;
3) Adding the sieved magnesium stearate, and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder according to the mass of each tablet being 100 mg;
5) And (3) placing the orally disintegrating tablets in a drying oven at 40 ℃, and drying for 12h.
Example 8
Prescription:
Figure BDA0003557158960000081
the preparation method comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a 50-mesh sieve for later use;
2) Adding the sieved captopril, microcrystalline cellulose, crospovidone, borneol, hydroxypropyl methylcellulose and aspartame into a mixer for fully mixing;
3) Adding the sieved micropowder silica gel, and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder according to the mass of each tablet being 100 mg;
5) And (3) placing the orally disintegrating tablets in a drying oven at 60 ℃ and drying for 6h.
Example 9
Prescription:
Figure BDA0003557158960000082
the preparation method comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a 50-mesh sieve for later use;
2) Adding the sieved captopril, compressible starch, croscarmellose sodium, menthol, povidone and aspartame into a mixer, and fully mixing;
3) Adding the sieved magnesium lauryl sulfate, and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder according to the mass of each tablet being 100 mg;
5) The orally disintegrating tablets are placed in a drying oven at 40 ℃ and dried for 10h.
Example 10
Prescription:
Figure BDA0003557158960000091
the preparation method comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a 35-mesh sieve for later use;
2) Adding the sieved captopril, compressible starch, croscarmellose sodium, menthol, povidone and aspartame into a mixer, and fully mixing;
3) Adding the sieved magnesium lauryl sulfate, and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder according to the mass of each tablet being 100 mg;
5) The orally disintegrating tablets are placed in a drying oven at 40 ℃ and dried for 10h.
Example 11
Prescription:
Figure BDA0003557158960000092
Figure BDA0003557158960000101
the preparation method comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a 50-mesh sieve for later use;
2) Adding the sieved captopril, compressible starch, croscarmellose sodium, menthol, povidone and aspartame into a mixer, and fully mixing;
3) Adding the sieved magnesium lauryl sulfate, and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder according to the mass of each tablet being 100 mg;
5) The orally disintegrating tablets are placed in a drying oven at 40 ℃ and dried for 10h.
Example 12
Prescription:
Figure BDA0003557158960000102
the preparation method comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a 50-mesh sieve for later use;
2) Adding sieved captopril, compressible starch, croscarmellose sodium, menthol, povidone and aspartame into a mixer, and mixing completely;
3) Adding the sieved magnesium lauryl sulfate, and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder according to the mass of each tablet being 100 mg;
5) The orally disintegrating tablets are placed in a drying oven at 40 ℃ and dried for 10h.
Comparative example 1
Prescription:
Figure BDA0003557158960000111
the preparation method comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a 50-mesh sieve for later use;
2) Adding the sieved captopril, compressible starch, croscarmellose sodium, povidone and aspartame into a mixer for fully mixing;
3) Then adding the sieved magnesium lauryl sulfate and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder according to the mass of each tablet being 100 mg;
comparative example 2
Prescription:
Figure BDA0003557158960000112
the preparation method comprises the following steps:
weighing the raw and auxiliary materials according to the prescription amount, uniformly mixing in a proper container, sieving by a 100-mesh sieve, directly tabletting on a tabletting machine according to the mass of each tablet being 100mg, placing in a drying oven at 40 ℃ after tabletting, and drying for 10 hours.
Comparative example 3
Prescription:
Figure BDA0003557158960000113
Figure BDA0003557158960000121
the preparation method comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount;
2) Sieving: screening all the weighed raw and auxiliary materials with a 80-mesh sieve respectively for later use;
3) Mixing: adding the sieved captopril, the PH102 microcrystalline cellulose, the crospovidone, the povidone and the menthol into a mixer, and fully mixing;
4) Total mixing: in the step 3), adding the sieved magnesium stearate and talcum powder, and fully mixing to obtain mixed powder;
5) Tabletting: the mixed powder obtained in step 4) was used in an amount of 100mg per tablet.
6) Placing in a drying oven at 40 deg.C, and drying for 10 hr.
Comparative example 4
Prescription:
Figure BDA0003557158960000122
the preparation method comprises the following steps:
1) Weighing raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a 50-mesh sieve for later use;
2) Adding the sieved captopril, compressible starch, croscarmellose sodium, ammonium bicarbonate, povidone and aspartame into a mixer for fully mixing;
3) Adding the sieved magnesium lauryl sulfate, and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder according to the mass of each tablet being 100 mg;
5) The orally disintegrating tablets are placed in a drying oven at 40 ℃ and dried for 10h.
Verification examples
1. Hardness, friability, dissolution rate and disintegration time of the orally disintegrating tablets of captopril prepared in examples 1 to 12 and comparative examples 1 to 4 were examined.
1.1 hardness
20 pieces were randomly extracted and subjected to hardness test using a hardness tester. The mean hardness of each prescription was calculated and the results were expressed as mean hardness (N). + -. SD.
1.2 friability
20 pieces were randomly drawn and accurately weighed (W) using an analytical balance 1 ) Then put into a friability apparatus, set at 25r/min for 4min, and then the tablets are dedusted and weighed precisely (W) 2 ). Friability% = ((W) was used 1 -W 2 )/W 1 ) X 100% equation.
1.3 in vitro disintegration time
6 tablets were randomly taken from each prescription, one tablet being placed in each of six units of a tablet disintegration time tester. The temperature of the disintegration medium (purified water) was maintained at 37 ℃, and the time required for complete disintegration of each tablet was recorded. The results are expressed as mean disintegration time(s). + -. SD.
1.4 dissolution determination
The dissolution medium was 900mL of pH 6.8 phosphate buffer, run at 37 ℃ at 75 r/min. 3mL were sampled at 2, 4, 6, 8, 10 and 20min points and an equal volume of fresh dissolution medium was added. The content was measured using an ultraviolet spectrophotometer. The measurements were repeated three times and the results are expressed as mean (%) ± SD.
The results of the experiment are shown in table 1.
TABLE 1 evaluation of quality of orally disintegrating tablets of captopril
Figure BDA0003557158960000131
Figure BDA0003557158960000141
Therefore, the captopril orally disintegrating tablet prepared by the prescription of the invention has the advantages of fast disintegration, high dissolution, low friability and convenient transportation. Compared with the orally disintegrating tablets prepared by the prescription of the invention, the orally disintegrating tablets prepared by the comparative examples 1, 2 and 3 have long disintegration time and low dissolution rate. The orally disintegrating tablet prepared in comparative example 4 has low hardness, friability of 1.06%, is not favorable for transportation, and ammonium bicarbonate has an irritating odor, is liable to cause a residue problem, and is not suitable for pharmaceutical use.
2. The content of captopril disulfide in the captopril orally disintegrating tablets prepared in examples 1 to 12 and comparative examples 1 to 4 was examined, and the content of captopril disulfide impurities on day 0, month 1 and month 3 under accelerated conditions (40 ℃ and RH 75%) was examined. The detection method refers to the detection method of captopril disulfide in the second part of Chinese pharmacopoeia 2015 edition.
The test results are shown in table 2.
TABLE 2 content of disulfide impurities in orally disintegrating tablets of captopril
Figure BDA0003557158960000142
Figure BDA0003557158960000151
From the stability investigation result, the captopril orally disintegrating tablet prepared by the invention has good stability, and the content of captopril disulfide as an impurity is lower than 0.3% when the captopril orally disintegrating tablet is stored for 3 months at 40 ℃ and under the condition of relative humidity of 75%.

Claims (10)

1. An orally disintegrating tablet of captopril comprises captopril, a filler, a disintegrant, an excipient and other pharmaceutically acceptable auxiliary materials; the excipient is one or more selected from Borneolum Syntheticum, camphora, menthol, limonene, isoborneol, and paeonol.
2. The orally disintegrating tablet of captopril according to claim 1, wherein the excipient is selected from one or more of borneol, camphor and menthol.
3. The captopril orally disintegrating tablet according to claim 1, wherein the weight percentage of captopril is 20-35%, the weight percentage of filler is 45-70%, the weight percentage of disintegrant is 1-10%, and the weight percentage of excipient is 2.5-15%.
4. The orally disintegrating tablet of captopril according to claim 1, wherein the excipient is 2.5-5% by weight.
5. The orally disintegrating tablet of captopril according to claim 1, wherein the filler is one or more selected from the group consisting of mannitol, microcrystalline cellulose, compressible starch, lactose, sorbitol and inorganic calcium salts.
6. The orally disintegrating tablet of claim 1, wherein the disintegrant is one or more selected from the group consisting of sodium carboxymethyl starch, sodium bicarbonate, citric acid, croscarmellose sodium, crospovidone, dry starch, and low substituted hydroxypropyl cellulose.
7. The orally disintegrating tablet of captopril according to claim 1, wherein the pharmaceutically acceptable excipients comprise binders, lubricants, flavoring agents.
8. The captopril orally disintegrating tablet of claim 7, which comprises the following components in percentage by weight:
Figure FDA0003557158950000011
9. a process for preparing the orally disintegrating tablet of captopril as claimed in any one of claims 1 to 8, wherein the tablet is prepared by direct powder compression and drying.
10. The process for preparing orally disintegrating tablets of captopril according to claim 9, comprising the steps of:
1) Weighing the raw and auxiliary materials according to the prescription amount, and respectively sieving the raw and auxiliary materials by a sieve of 40-80 meshes for later use;
2) Adding the sieved captopril, excipient, filler, disintegrant, flavoring agent and adhesive into a mixer for fully mixing;
3) Then adding the sieved lubricant and fully mixing to obtain mixed powder;
4) Directly tabletting the mixed powder;
5) And (3) placing the orally disintegrating tablets in a drying oven for drying.
CN202210281651.7A 2021-03-29 2022-03-21 Captopril orally disintegrating tablet Pending CN115137704A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2021103448024 2021-03-29
CN202110344802 2021-03-29

Publications (1)

Publication Number Publication Date
CN115137704A true CN115137704A (en) 2022-10-04

Family

ID=83405590

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202210281651.7A Pending CN115137704A (en) 2021-03-29 2022-03-21 Captopril orally disintegrating tablet

Country Status (1)

Country Link
CN (1) CN115137704A (en)

Similar Documents

Publication Publication Date Title
US10857097B2 (en) Solid dosage form
RU2492853C2 (en) Tablets of ulipristal acetate
JP4171091B2 (en) Tablet composition
US20090131383A1 (en) Pharmaceutical compositions of a neuroactive steriod and methods of use thereof
US20160193196A1 (en) Immediate-release tablet formulations of a thrombin receptor antagonist
US20060240101A1 (en) Orally disintegrating pharmaceutical tablet formulations of olanzapine
CZ286417B6 (en) Pharmaceutical preparation that is useful for preparing dosage forms for oral administration with prolonged release of gepirone
US20230248716A1 (en) Pharmaceutical compositions comprising nitroxoline lysinate, preparation method therefor and use thereof
JP2003535895A (en) Solid valsartan pharmaceutical composition
CN107913256A (en) A kind of macitentan oral disnitegration tablet for treating pulmonary hypertension and preparation method thereof
WO2021254409A1 (en) Pharmaceutical composition of complex and preparation method therefor
CN103054820B (en) A kind of Dronedarone hydrochloride pharmaceutical composition and preparation method thereof
RU2613192C1 (en) Tablets of clozapine with sustained release
JP2001522882A (en) Pharmaceutical composition containing zafarukast
CN115137704A (en) Captopril orally disintegrating tablet
AU2013200682C1 (en) Fast Dissolving Solid Dosage Form
US20220347095A1 (en) Solid Dosage Form
CN106943368A (en) Mirtazapine tablet and preparation method thereof
KR20220066126A (en) Tandospiron pharmaceutical composition and its manufacturing method and use
CN112220765A (en) Oral preparation containing simvastatin and preparation method thereof
CN112516097B (en) Levamlodipine besylate composition
KR20090013736A (en) Sustained-release formulation comprising metformin acid salt
BRPI0713647A2 (en) pharmaceutical formulations and compositions of a selective cxcr2 or cxcr1 antagonist and methods for its use for the treatment of inflammatory disorders
EP3431078B1 (en) Non-pulsatile prolonged-release betahistine oral solid compositions
US20040009971A1 (en) Use of alprazolam in treatment of disorders of the central nervous system

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination