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WO2023279381A1 - Composition pharmaceutique de prégabaline, procédé de préparation s'y rapportant et utilisation associée - Google Patents

Composition pharmaceutique de prégabaline, procédé de préparation s'y rapportant et utilisation associée Download PDF

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Publication number
WO2023279381A1
WO2023279381A1 PCT/CN2021/105518 CN2021105518W WO2023279381A1 WO 2023279381 A1 WO2023279381 A1 WO 2023279381A1 CN 2021105518 W CN2021105518 W CN 2021105518W WO 2023279381 A1 WO2023279381 A1 WO 2023279381A1
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WO
WIPO (PCT)
Prior art keywords
pregabalin
pharmaceutical composition
preparation
pharmaceutically acceptable
release
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.)
Ceased
Application number
PCT/CN2021/105518
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English (en)
Chinese (zh)
Inventor
郭桢
王璇
董睿
王婷婷
应述欢
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.)
Shanghai Bocimed Pharmaceutical Co Ltd
Shanghai Bocimed Pharmaceutical Research Co Ltd
Original Assignee
Shanghai Bocimed Pharmaceutical Co Ltd
Shanghai Bocimed Pharmaceutical Research 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 Shanghai Bocimed Pharmaceutical Co Ltd, Shanghai Bocimed Pharmaceutical Research Co Ltd filed Critical Shanghai Bocimed Pharmaceutical Co Ltd
Priority to PCT/CN2021/105518 priority Critical patent/WO2023279381A1/fr
Publication of WO2023279381A1 publication Critical patent/WO2023279381A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • 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
    • A61K47/02—Inorganic compounds
    • 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
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system

Definitions

  • the invention belongs to the field of pharmaceutical preparations, and in particular relates to a pharmaceutical composition of pregabalin, especially a pharmaceutical composition of pregabalin, a preparation method and application thereof.
  • Pregabalin is a gamma-aminobutyric acid (GABA) analog developed by Pfizer (trade name Lyrica), which has been approved by the FDA for adults with partial-onset diabetic peripheral neuralgia, postherpetic neuralgia, muscle fiber Adjunctive treatment of neuropathic pain caused by pain and spinal cord injury. In addition, it is also approved for the adjunctive treatment of partial-onset epilepsy in patients with epilepsy 4 years of age and older.
  • GABA gamma-aminobutyric acid
  • domestically sold pregabalin preparations include Pfizer's Lyrica immediate-release capsules (25, 50, 75, 100, 150, 200, 300mg specifications) and Chongqing Saiwei Pharmaceutical Co., Ltd.'s immediate-release capsules (25, 75, 100mg), both need to be administered 2 to 3 times a day.
  • pregabalin is a class I drug of the BCS classification system. It reaches its peak concentration 1.5 hours after oral administration, and its relative bioavailability is ⁇ 90%. Poor compliance. However, if the drug is taken QD (once a day), it can not only improve the patient's compliance, but also reduce the C max of the drug in the blood, reduce or avoid the potential, undesired side effects related to the dosage, and can increase the C max of the drug in the plasma. The lowest concentration of C min increases drug efficacy.
  • pregabalin in the gastrointestinal tract is heterogeneous, it is absorbed in the small intestine and ascending colon, but it is rarely absorbed in intestinal segments other than the hepatic flexure of the colon, which means that the average pregabalin
  • the absorption window is on average about 6 hours or less. Therefore, the drug released in the existing immediate-release dosage form or sustained-release dosage form after about 6 hours cannot be absorbed by the human body, resulting in a large waste of medicine.
  • Patent document CN103040785A relates to a pregabalin osmotic gastric-retentive tablet, which makes the osmotic gastric-retentive tablet stay in the stomach for a long time and achieve zero-order release through expansion and osmotic pump principles.
  • this invention is a perforated osmotic pump preparation, which has high requirements for laser or other mechanical perforation equipment.
  • the release of drugs from single-sided or double-sided drug release holes may cause side effects caused by excessive local drug concentration, while drug release holes Blockage can easily cause drug release.
  • Patent document CN103702664A relates to a pregabalin sustained-release tablet of a two-phase controlled-release system, which is prepared by a wet granulation process.
  • pregabalin is easily soluble in water, and 50% HPC alcohol solution is selected as the binder in the wet granulation process of the invention, it is easy to cause mold sticking during the tableting process, resulting in rough or flawed edges of the tablet ,
  • it is easy to cause mold sticking during the tableting process, resulting in rough or flawed edges of the tablet significantly affect the quality of sustained-release tablets, not only difficult to industrialized production, and the consistency of the product is also difficult to meet regulatory requirements.
  • Patent document CN104906064A relates to gastric floating sustained-release tablets containing pregabalin, which believes that there are many disadvantages in water-swellable drugs, such as damage to the gastrointestinal mucosa at the edge of the tablet, and easy accumulation in the stomach. For this reason, this document makes the surface of the tablet hydrated to form a gel by using a hydrophilic polymer material and a swelling agent, so that the volume expands, and then floats on the gastric juice to prolong the residence time in the stomach.
  • the floating of the gastric floating sustained-release tablet in the stomach requires a large amount of gastric juice, and has high requirements on the density of gastric content and the pH of gastric juice, and the individual differences of patients will significantly affect the floating effect.
  • the present invention provides a pharmaceutical composition
  • a pharmaceutical composition comprising the following components:
  • the active ingredient can be in any pharmaceutically acceptable form of pregabalin, for example, one or two selected from pregabalin, its pharmaceutically acceptable salt, complex, solvate or polymorph. species or more.
  • the content of the active ingredient is calculated as pregabalin.
  • the pharmaceutically acceptable salt of pregabalin may include a pharmaceutically acceptable salt, including a half-salt, of pregabalin with an organic acid, an inorganic acid, an organic base or an inorganic base.
  • the pharmaceutically acceptable salt may be one, two or more selected from pregabalin hydrochloride, hydrobromide, bisulfate, sodium salt, potassium salt, magnesium salt and the like.
  • a solvate of pregabalin means pregabalin and stoichiometric or non-stoichiometric amounts of one, two or more pharmaceutically acceptable solvent molecules (e.g. alcohols such as ethanol, water, or mixture) molecular complexes.
  • solvent molecules e.g. alcohols such as ethanol, water, or mixture
  • the weight percentage content of the at least one active ingredient selected from pregabalin, its pharmaceutically acceptable salt or solvate can be 5-40%, such as 5%, 10% , 15%, 20%, 25%, 30%, 35% or 40%.
  • the skeleton material may be selected from hydroxypropylmethyl cellulose, hydroxypropyl cellulose, polyacrylic acid resin, carbomer, polyvinyl acetate povidone mixture, hydroxyethyl cellulose, ethyl One, two or more of cellulose, polyvinyl alcohol, and polyoxyethylene.
  • the weight percentage content of the skeleton material can be 10-60%, such as 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50% %, 55% or 60%.
  • the expansion agent may be selected from cross-linked polyvinylpyrrolidone (crospovidone), cross-linked sodium carboxymethylcellulose, sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, One, two or more of carmellose calcium, carmellose, and polacrilin potassium.
  • crospovidone cross-linked polyvinylpyrrolidone
  • sodium carboxymethylcellulose sodium carboxymethyl starch
  • low-substituted hydroxypropyl cellulose One, two or more of carmellose calcium, carmellose, and polacrilin potassium.
  • the weight percentage content of the bulking agent can be 1-25%, such as 1%, 2%, 3%, 4%, 5%, 10%, 15%, 20% or 25% %.
  • the filler may be selected from one, two or more of lactose, starch, mannitol, microcrystalline cellulose, and calcium hydrogen phosphate.
  • the weight percentage content of the filler can be 0-20%, such as 0% or higher than 0% and not more than 20%, such as 1%, 2%, 3%, 4%. , 5%, 10%, 15% or 20%.
  • the lubricant may be selected from one, two or more of talcum powder, magnesium stearate, and micronized silica gel.
  • the weight percent content of the lubricant can be 0.5-5%, such as 0.5%, 1.0%, 1.5%, 2.0%, 2.5%, 3.0%, 3.5%, 4.0%, 4.5% % or 5.0%.
  • the pharmaceutical composition may be a preparation (such as a tablet), for example, a gastric-floating sustained-release preparation of pregabalin, preferably a pregabalin gastric-floating sustained-release tablet.
  • the pharmaceutical composition may further include a coating covering the outer surface of the above-mentioned components.
  • the present invention also provides a preparation method of the pharmaceutical composition, comprising mixing the above components.
  • the preparation method includes uniformly mixing the active ingredient, skeleton material, expansion agent and filler, and then adding a lubricant.
  • the preparation method further includes mixing the above-mentioned components, and then preparing the obtained mixture into a preparation, for example, preparing a tablet through a compression step and an optional coating step.
  • composition of the present invention it is used for treating or preventing postherpetic neuralgia.
  • the present invention also provides a method for treating or preventing postherpetic neuralgia, comprising administering the above pharmaceutical composition to a patient in need.
  • the present invention also provides a method for reducing the frequency of medication for patients, comprising administering the above pharmaceutical composition to patients in need, such as patients with postherpetic neuralgia.
  • the frequency of dosing by the patient is at most one dose per day.
  • the present invention also provides a method for improving patients' medication compliance, comprising administering the above pharmaceutical composition to patients in need, such as patients with postherpetic neuralgia.
  • the present invention also provides the use of the above-mentioned pharmaceutical composition for preparing a medicament, wherein the medicament is used for treating or preventing postherpetic neuralgia.
  • the drug release performance of the pharmaceutical composition of the present invention is excellent. In the in vitro dissolution test, it releases 25%-40% in the 2nd hour, 40%-50% in the 4th hour, 55%-65% in the 6th hour, and more than 80% in the 12th hour. It can release the drug stably. Conform to Chinese Pharmacopoeia standard.
  • the coating layer of the pharmaceutical composition of the present invention further improves the stability of the drug, masks the bitter taste of the active ingredient, and the coating layer has no obvious influence on the release rate of the tablet.
  • the pharmaceutical composition of the present invention can be prepared as a gastric-floating sustained-release tablet of pregabalin once a day, and the gastric-retentive tablet has excellent swelling and floating properties in the stomach, thereby realizing the delayed release of pregabalin It can effectively prolong the residence time of pregabalin in the stomach and upper small intestine, improve bioavailability, obtain stable blood drug concentration, and reduce the frequency of administration.
  • the pharmaceutical composition of the present invention can hydrate and expand in the stomach to a size with a width greater than 13 mm after being taken by a patient.
  • the sustained-release tablet after the sustained-release tablet contacts the gastric juice, its density is lower than that of the gastric juice, so it quickly floats on the upper part of the gastric juice, and the floating time can last up to more than 24 hours, achieving the effect of gastric retention and improving bioavailability.
  • the sustained-release tablet has larger swelling size and stronger gel strength, thereby reducing individual differences under different physiological conditions.
  • the excipients of the pharmaceutical composition of the present invention have good fluidity and strong anti-adhesive properties, and can be directly compressed to obtain pregabalin gastric retention sustained-release tablets after mixing.
  • the process is simple and easy, the cost is low, and it is suitable for industrial production.
  • Pregabalin was provided by Orient Pharmaceutical Co., Ltd. with a purity of 99.2%;
  • Crospovidone (PVPP) and polyvinyl acetate povidone blend (KSR) are available from BASF under the tradenames and in Nominal 80/19 (w/w) mixture of PVAc and PVP;
  • HEC Hydroxyethyl cellulose
  • Natrosol TM Hydroxyethyl cellulose
  • Mv molecular weight in the range of about 9 ⁇ 10 4 to 13 ⁇ 10 5 (Mv), such as HEC (HX Pharm), HEC (M Pharm );
  • Ethylcellulose is available from Ashland under the trade name Aqualon TM , with a molecular weight in the range of 75000 to 215000 (Mv) and a Brookfield viscosity in the range of 8 to 105 mPa.s, such as EC (T10 Pharm);
  • Polyacrylic acid resin is a cationic or anionic copolymer obtained by polymerization of dimethylaminoethyl methacrylate, methacrylic acid, and methacrylate in different proportions. It can be obtained from Rohm, Germany, and its trade name is
  • Hypromellose can be obtained from IFF Company, its trade name is METHOCEL TM , and the model can be selected from K100LV, K4M and K100M;
  • SRP 80 is a functional excipient based on the hydrophilic polymer polyvinyl alcohol (PVA), containing only a single component - PVA 40-88*, without any other additives, available from Merck;
  • PVA polymer polyvinyl alcohol
  • Polyethylene oxide is available from DOW Corporation under the trade name POLYOX TM , and its molecular weight is in the range of about 9 ⁇ 10 5 to 7 ⁇ 10 6 (Mv);
  • Carbomer is available from RITA under the trade name Available from Lubrizol under the tradename
  • the viscosity range can be selected from 4000 to 39400cPs, such as Carbomer 971P;
  • Carmellose calcium (CMC-Ca) can be obtained from Bolak Company, and the particle size range can be selected from 90 to 250 mesh;
  • the lubricant can be selected from one, two or more of talcum powder, magnesium stearate, and micronized silica gel, wherein magnesium stearate can be obtained from Anhui Shanhe;
  • the filler can be selected from one, two or more of lactose, starch, mannitol, microcrystalline cellulose, and calcium hydrogen phosphate.
  • lactose can be obtained from MEGGLE
  • microcrystalline cellulose can be obtained from Riddenmayer (Shanghai) Fiber Trading Co., Ltd.
  • This product is a film-coated tablet available from Colorcon as series.
  • Examples 1 to 24 Pharmaceutical compositions containing pregabalin
  • the active ingredients and auxiliary materials except magnesium stearate were mixed in a three-dimensional motion mixer for 20 minutes, and then magnesium stearate was added and mixed for 5 minutes to obtain the final mixture.
  • magnesium stearate was added and mixed for 5 minutes to obtain the final mixture.
  • a rotary tablet press 22.0 ⁇ 10.9mm almond-shaped punched into tablets, and coated.
  • the film coating premix manufacturer is Colorcon
  • the model is 85F140030-CN.
  • Example 8 Pregabalin 30 30 Polyvinyl acetate povidone blend 40 40 MCC 102 55 55 CMC-Ca 15 15 PEO WSR N60K 6 the PEO WSR Coagulat the 6 Carbomer 971P 3 3 Magnesium stearate 1 1
  • Example 15 Example 16
  • Example 17 Pregabalin 30
  • 30 Polyvinyl acetate povidone blend 40
  • 40 CMC-Ca 10 17
  • 20 PEO WSR N60K 14
  • the Carbomer 971P 5 4 3
  • the fluidity of the material is judged by the result of the Carr index, and the evaluation method is as follows:
  • the present invention adopts the pregabalin sustained-release tablet (330mg) produced by Pfizer Pharmaceutical Co., Ltd. of the United States as a control example.
  • the composition of the sustained-release tablet is: containing 330 mg of active ingredient pregabalin, and other components include polyvinyl acetate povidone mixture, cross-linked povidone, polyoxyethylene, carbomer and magnesium stearate.
  • two other batches were used, which are respectively counted as comparative example 1 and comparative example 2.
  • the pregabalin formulations prepared according to the present invention exhibit excellent sustained-release dissolution patterns.
  • the prepared pregabalin sustained-release preparation has basically no burst release effect in 1 hour, the dissolution rate is 50% to 70% in 8 hours, and the release rate exceeds 80% in 16 hours.
  • the cumulative dissolution rate of the tablets in the comparative example was about 20% in 1 hour, showing a certain burst release effect, while the tablet prepared according to the present invention significantly weakened this burst release effect, making pregabalin release in a more gradual manner, Increased the safety of medication.
  • the tablets prepared by the present invention As shown in Table 13, compared with the tablets in Comparative Examples, the tablets prepared by the present invention (Example 13 and Example 15) have better rigidity after swelling for 24 hours, showing good gastric retention characteristics, and effectively controlling drug release. , improve bioavailability.

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  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Inorganic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Oil, Petroleum & Natural Gas (AREA)
  • Biomedical Technology (AREA)
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  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne une composition pharmaceutique de prégabaline ou un sel pharmaceutiquement acceptable de celle-ci, un procédé de préparation s'y rapportant et une utilisation associée. La composition pharmaceutique selon l'invention comprend un ingrédient actif, un matériau squelettique, un agent d'expansion, une charge et un lubrifiant, le principe actif pouvant être n'importe quelle forme pharmaceutiquement acceptable de prégabaline. La composition pharmaceutique présente d'excellentes performances de libération de médicament, ainsi que d'excellentes propriétés de gonflement et de flottement dans l'estomac, ce qui permet d'obtenir la caractéristique de libération retardée de la prégabaline, et le temps de rétention de la prégabaline à l'extrémité supérieure de l'estomac et de l'intestin grêle peut être efficacement prolongé, améliorant la biodisponibilité, obtenant une concentration de médicament stable dans le sang et réduisant le nombre d'administrations.
PCT/CN2021/105518 2021-07-09 2021-07-09 Composition pharmaceutique de prégabaline, procédé de préparation s'y rapportant et utilisation associée Ceased WO2023279381A1 (fr)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN118557537A (zh) * 2024-05-30 2024-08-30 中国农业大学 普瑞巴林缓释片及其制备方法和应用

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CN104906064A (zh) * 2015-05-15 2015-09-16 中国药科大学 一种普瑞巴林胃漂浮缓释片剂及其制备方法
US20170239203A1 (en) * 2014-10-24 2017-08-24 Jiangsu Hengrui Medicine Co., Ltd. Pregabalin sustained-release preparation
CN107961225A (zh) * 2017-12-07 2018-04-27 中国药科大学 一种普瑞巴林微孔渗透泵片及其制备方法
CN108159011A (zh) * 2018-03-16 2018-06-15 中国药科大学 一种双相控释的普瑞巴林胃滞留缓释片及其制备方法
CN108478537A (zh) * 2018-05-03 2018-09-04 南京易亨制药有限公司 一种含普瑞巴林的单室渗透泵控释片剂
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CN104906064A (zh) * 2015-05-15 2015-09-16 中国药科大学 一种普瑞巴林胃漂浮缓释片剂及其制备方法
CN107961225A (zh) * 2017-12-07 2018-04-27 中国药科大学 一种普瑞巴林微孔渗透泵片及其制备方法
CN108159011A (zh) * 2018-03-16 2018-06-15 中国药科大学 一种双相控释的普瑞巴林胃滞留缓释片及其制备方法
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CN110974798A (zh) * 2019-12-19 2020-04-10 江苏优仿医药科技有限公司 药物组合物、缓释片剂及其制备方法

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN118557537A (zh) * 2024-05-30 2024-08-30 中国农业大学 普瑞巴林缓释片及其制备方法和应用

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