Coamorphous repaglinide–saccharin with enhanced dissolution

Gao, Yuan; Liao, Jiao; Xuan, Qi; Zhang, Jianjun

doi:10.1016/j.ijpharm.2013.04.032

Cited by 102 publications

(69 citation statements)

References 29 publications

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“…Co-amorphous dispersions can be prepared from solutions of crystalline drugs, especially when rapid co-precipitation is pursued using carboxylic acids as plasticizing agents (12,13). Stable coamorphous systems have been prepared from low solubility drugs and small molecular mass amino acids (14) or neutral molecules capable of forming strong H-bonding such as saccharin (15) or nicotinamide (16). Although numerous successful plasticized formulations have been prepared using carboxylic acids (17)(18)(19)(20), plasticized co-amorphous dispersions prepared from crystalline drugs with polycarboxylic acids are rare.…”

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confidence: 99%

Clozapine-carboxylic acid plasticized co-amorphous dispersions: Preparation, characterization and solution stability evaluation

Ali

Maghrabi

2015

Acta Pharmaceutica

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Clozapine-carboxylic acid plasticized co-amorphous dispersions:Preparation, characterization and solution stability evaluationThis study addressed the possibility of forming of co-amorphous systems between clozapine (CZ) and various carboxylic acid plasticizers (CAPs). The aim was to improve the solubility and oral bioavailability of clozapine. Co-amorphous dispersions were prepared using modifi ed solvent evaporation methodology at drug/plasticizer stoichiometric ratios of 1:1, 1:1.5 and 1:2. Solid state characterization was performed using diff erential scanning calorimetry, X-ray diff raction and infra red spectroscopy. Highly soluble homogeneous co-amorphous dispersions were formed between clozapine and CAPs via hydrogen bonding. The co-amorphous dispersions formed with tartaric acid (1:2) showed the highest dissolution percentage (> 95 % in 20 minutes) compared to pure crystalline CZ (56 %). Highly stable solutions were obtained from co-amorphous CZ-citric and CZ-tartaric acid at 1:1.5 molar ratio. The prepared dispersions suggest the possibility of peroral or sublingual administration of highly soluble clozapine at a reduced dose with the great chance to bypass the fi rst pass metabolism.

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confidence: 99%

Clozapine-carboxylic acid plasticized co-amorphous dispersions: Preparation, characterization and solution stability evaluation

Ali

Maghrabi

2015

Acta Pharmaceutica

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“…The type of water was not specified in 19 of 51 studies (37%) (38)(39)(40)(41)(42)(43)(44)(45)(46)(47)(48)(49)(50)(51)(52)(53)(54)(55)(56).…”

Section: Watermentioning

confidence: 99%

“…This literature review found that phosphate buffer solutions, in the range of pH 5.8-8.0, were employed in 32.6% of cases as medium for the shake-flask method (15 of 46 studies) (8,11,19,31,32,37,(41)(42)(43)45,46,48,51,57,58) and in 40.0% as dissolution medium (8 of 20 studies) (10,11,22,24,(51)(52)(53)56). Acetate buffer was used less frequently, in 4 of 46 studies (8.7%) (41,42,45,49) as medium for the shake-flask method and in 2 of 20 studies (10.0%) as dissolution medium (52,56).…”

Section: Buffer Solutionsmentioning

confidence: 99%

“…Acetate buffer was used less frequently, in 4 of 46 studies (8.7%) (41,42,45,49) as medium for the shake-flask method and in 2 of 20 studies (10.0%) as dissolution medium (52,56). Phosphate and acetate buffer solutions, which were claimed to have similar osmolality and ionic strength as the physiological fluids, were the most employed buffer solutions to determine solubility (27.3% for the phosphate buffer and 9.1% for the acetate buffer).…”

Section: Buffer Solutionsmentioning

confidence: 99%

“…In the last decade, biorelevant media have been extensively used to determine drug solubility and as dissolution media, especially for BCS class II compounds (14 studies or 25.0%) (8,9,13,22,27,33,35,42,44,45,47,51,54,55) as well as for BCS class I (4 studies or 7.1%) (33,34,49,51), class III (2 or 3.6%) (33,51), and class IV (2 or 3.6%) (33,51). As mentioned, biorelevant media contain generally components which are likely present in the human GI tract such as bile salts and lecithin aiming to mimic the physiological conditions in specific segments of the GI tract; thus, in these media, pH, osmolality, and surface tension are adapted to physiological values (75).…”

Section: Biorelevant Mediamentioning

confidence: 99%

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Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Bou‐Chacra

Melo

Morales

et al. 2017

AAPS J

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Abstract.The introduction of the biopharmaceutics drug classification system (Biopharmaceutics Classification System (BCS)), in 1995, provided a simple way to describe the biopharmaceutics behavior of a drug. Solubility and permeability are among the major parameters, which determine the fraction dose absorbed of a drug substance and consequently its chances to be bioavailable. The purpose of this review is to summarize the evolution of the media used for determining solubility and dissolution and how this can be used in modern drug development. Over the years, physiologically adapted media and buffers were introduced with the intention to better predict the in vivo solubility and dissolution of drug substances. Water, buffer solutions, compendial media, micellar solubilization media, and biorelevant media are reviewed. At this time point, there is no universal medium available which can be used to predict every drug substance's solubility or a drug product's in vivo dissolution behavior. However, there have been many improvements and additions made to media to optimize their in vivo predictability; for example, the current phosphate concentrations in buffers seem to be too high to correlate with the carbonate buffer concentrations in vivo. Biorelevant media were updated to correlate them better with the composition of human intestinal fluids. The BCS was introduced into regulatory sciences as a scientific risk management tool to waive bioequivalence studies under certain conditions. Today's different guidance documents define the dose-solubility ratio differently. As shown for amoxicillin, this can cause more confusion than certainty for globally operating companies. Harmonization of BCS guidelines is highly desirable.

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