The natural bile acid surfactant sodium taurocholate (NaTC) as a coformer in coamorphous systems: Enhanced physical stability and dissolution behavior of coamorphous drug-NaTc systems

Gniado, Katarzyna; MacFhionnghaile, Pól; McArdle, Patrick; Erxleben, Andrea

doi:10.1016/j.ijpharm.2017.10.049

Cited by 45 publications

(25 citation statements)

References 41 publications

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“…With this result, it can be established that SIM is a good stabilizer for NIF. It is important to mention that NIF has been reported as very unstable API in the amorphous state even in the presence of surfactants and excipients [ 28 , 29 ]. A zoom in to the glass transition temperatures (Tg) of the amorphous samples prepared in situ is presented in Figure 2 c, in which the thermograms for the amorphous materials measured after one year storage are also added.…”

Section: Resultsmentioning

confidence: 99%

Co-Amorphous Simvastatin-Nifedipine with Enhanced Solubility for Possible Use in Combination Therapy of Hypertension and Hypercholesterolemia

2018

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The high index of simultaneous incidence of hypertension and hypercholesterolemia in the population of many countries demands the preparation of more efficient drugs. Therefore, there is a significant area of opportunity to provide as many alternatives as possible to treat these illnesses. Taking advantage of the solubility enhancement that can be achieved when an active pharmaceutical ingredient (API) is obtained and stabilized in its amorphous state, in the present work, new drug-drug co-amorphous formulations (Simvastatin SIM- Nifedipine NIF) with enhanced solubility and stability were prepared and characterized. Results show that the co-amorphous system (molar ratio 1:1) is more soluble than the pure commercial APIs studied separately. Aqueous dissolution profiles showed increments of solubility of 3.7 and 1.7 times for SIM and NIF, correspondingly, in the co-amorphous system. The new co-amorphous formulations, monitored in time, (molar fractions 0.3, 0.5 and 0.7 of SIM) remained stable in the amorphous state for more than one year when stored at room temperature and did not show any signs of crystallization when re-heating. Inspection on the remainder of a sample after six hours of dissolution showed no recrystallization, confirming the stability of co-amorphous system. The enhanced solubility of the co-amorphous formulations makes them promising for simultaneously targeting of hypertension and hypercholesterolemia through combination therapy.

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Section: Resultsmentioning

confidence: 99%

Co-Amorphous Simvastatin-Nifedipine with Enhanced Solubility for Possible Use in Combination Therapy of Hypertension and Hypercholesterolemia

2018

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“…Thus, the IR data of these coamorphous systems give no evidence for specific H bonding interactions between the two drug molecules. The formation of stable single-phase coamorphous systems in which molecular level mixing is sufficient to stabilize the amorphous state towards recrystallization has been described in the literature (Löbmann et al, 2012;Gniado et al, 2017). By contrast, there are clear differences between the IR spectrum of coamorphized GLZ-TRI and that calculated for physically mixed amorphous GLZ and TRI (Fig.…”

Section: Ball-milling Of Binary Mixturesmentioning

confidence: 73%

Investigation of the formation of drug-drug cocrystals and coamorphous systems of the antidiabetic drug gliclazide

Aljohani

MacFhionnghaile

McArdle

et al. 2019

International Journal of Pharmaceutics

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The antidiabetic drug gliclazide (GLZ) has a slow absorption rate and a low bioavailability due to its poor solubility. GLZ is often prescribed along with an antihypertensive, as many diabetic patients have coexistent hypertension. Cocrystallization and coamorphization are attractive strategies to enhance dissolution rates and to reduce the number of medications a patient has to take. In this work the formation of cocrystals and coamorphous systems of GLZ with various antihypertensive drugs was studied, namely chlorothiazide (CTZ), hydrochlorothiazide (HTZ), indapamide (IND), triamterene (TRI) and nifedipine (NIF) as well as benzamidine (BZA) as a model for the amidine pharmacophore. TRI, IND and HTZ were found to form coamorphous systems with GLZ that are stable for at least six months at 22  2 C and 56 % relative humidity. Coamorphous GLZ-TRI is also stable in dissolution medium. Coamorphization of GLZ-TRI with 15 % sodium taurocholate gave a viable coamorphous formulation with an enhanced dissolution rate. Comilling of GLZ with BZA and cocrystallization from solution gave the amorphous and crystalline salt, respectively and the X-ray structure is reported. During attempts to obtain X-ray suitable cocrystals crystals of 2 Na + GLZand IND . 0.5H2O were obtained. Redetermination of the published structure of IND . 0.5H2O revealed a unit cell with the length of the a axis doubled, a different space group and no disorder. Liquid-assisted grinding of a 1:1 mixture of GLZ and IND indicated the transformation of IND to a new solid-state form, while GLZ remained unaltered. Milling-and heating-induced solid-state transformations of IND are discussed.

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“…In drug-excipient combinations, the excipients with a small molecular weight, generally called co-formers in this field, act as stabilizers in co-amorphization to enhance the physical stability and dissolution rate of drugs [ 33 , 34 , 35 , 36 , 37 , 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 ]. The selection of an adequate conformer which can form sufficient intermolecular interactions with the drug, such as charge-assisted interactions and hydrogen bonding, is therefore an important step.…”

Section: Emerging Pharmaceutical Techniques For Amorphization Of Poorly Water-soluble Drugsmentioning

confidence: 99%

Recent Technologies for Amorphization of Poorly Water-Soluble Drugs

Kim

Tin

et al. 2021

Pharmaceutics

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Amorphization technology has been the subject of continuous attention in the pharmaceutical industry, as a means to enhance the solubility of poorly water-soluble drugs. Being in a high energy state, amorphous formulations generally display significantly increased apparent solubility as compared to their crystalline counterparts, which may allow them to generate a supersaturated state in the gastrointestinal tract and in turn, improve the bioavailability. Conventionally, hydrophilic polymers have been used as carriers, in which the amorphous drugs were dispersed and stabilized to form polymeric amorphous solid dispersions. However, the technique had its limitations, some of which include the need for a large number of carriers, the tendency to recrystallize during storage, and the possibility of thermal decomposition of the drug during preparation. Therefore, emerging amorphization technologies have focused on the investigation of novel amorphous-stabilizing carriers and preparation methods that can improve the drug loading and the degree of amorphization. This review highlights the recent pharmaceutical approaches utilizing drug amorphization, such as co-amorphous systems, mesoporous particle-based techniques, and in situ amorphization. Recent updates on these technologies in the last five years are discussed with a focus on their characteristics and commercial potential.

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The natural bile acid surfactant sodium taurocholate (NaTC) as a coformer in coamorphous systems: Enhanced physical stability and dissolution behavior of coamorphous drug-NaTc systems

Cited by 45 publications

References 41 publications

Co-Amorphous Simvastatin-Nifedipine with Enhanced Solubility for Possible Use in Combination Therapy of Hypertension and Hypercholesterolemia

Co-Amorphous Simvastatin-Nifedipine with Enhanced Solubility for Possible Use in Combination Therapy of Hypertension and Hypercholesterolemia

Investigation of the formation of drug-drug cocrystals and coamorphous systems of the antidiabetic drug gliclazide

Recent Technologies for Amorphization of Poorly Water-Soluble Drugs

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